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Garcinia kola is a medicinal food commonly consumed in Sub-Sahara Africa, for which Kolaviron (KV) is the active portion. As a follow-up to our earlier chemopreventive studies, we investigated the chemotherapeutic effects of KV on experimentally induced mammary carcinogenesis in female Wistar rats. Mammary carcinogenesis was induced using 80 mg/kg of 7,12-dimethylbenzanthracene (DMBA) administered by oral gavage. One hundred-fifty days post-DMBA induction, estrogen receptor-α (ER-α) levels were determined in the experimental rats before treatment with KV commenced. Treatment was done using 50, 100, and 200 mg/kg KV thrice a week for 4 weeks, after which the experiment was terminated. Significantly higher levels of estrogen receptor-α, CYP 1A1, malondialdehyde, formation of lobular neoplastic cells, epithelial hyperplasia, lymphocyte infiltration, and increased cytokine (interleukin-6 and tumor necrosis factor-α) activity were observed in DMBA-induced rats, which were attenuated in KV-treated rats. Tyrosine metabolism was exclusively enriched in DMBA-induced rats in contrast to KV-treated rats. Collectively, the results point to the chemotherapeutic potential of KV.

Ethnopharmacological Relevance: Pastoralists in Nigeria mix Garcinia kola seed (GK), Khaya senegalensis stem bark (KS), and Vernonia amygdalina leaves (VA) to treat leptospirosis., Aim: To determine the in vitro and in vivo effect on single and combination therapy on Leptospira interrogans-infected mice., Materials and Methods: Evaluation of in vitro assay for anti-leptospiral motility of the extracts was carried out in triplicates. For the in vivo assessment, 40 adult male mice inoculated with Leptospira were randomly allocated into 8 groups of 5 mice each. Groups IV-IX were treated with 800 mg/kg b.w. of KS, GK, VA, KS + GK, KS + VA, GK + VA for 5 days. Group I was negative control, II was model control, and III was treated with penicillin (3.7 mg/kg b.w.) intramuscularly., Results: In vitro, at 90 min, all the extracts at 800, 400, and 200 mg/ml showed complete cessation of motility which was significantly (p < 0.05) different when compared to the negative control. A significant (p < 0.05) IC 50 of 0.18 mg/ml was recorded with GK when compared to KS (0.40 mg/ml), VA (0.25 mg/ml), and procaine penicillin (0.31 mg/ml). Mean packed cell volume, haemoglobin concentration, and mean corpuscular haemoglobin concentration decreased significantly (p < 0.05) in all infected groups and returned to almost pre-infection values. However, significant leucocytosis (p < 0.05) was observed in group II. AST and ALP showed a significant increase (p < 0.001). Histopathological evaluation showed the extracts to prevent the distortion of normal architecture of the selected organs., Conclusion: This study demonstrates the significant potential of Garcinia kola, Khaya senegalensis, and Vernonia amygdalina extracts singly and in combination to combat leptospirosis., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

Purpose: Garcinia kola is a medicinal plant commonly known as bitter kola. It is utilised in ethnomedicine for the treatment of diarrhoea, bronchitis, bacterial infection, cough, hepatitis, gonorrhoea, laryngitis, food poison, liver and gastric diseases., Objective: This study reviewed the phytochemistry, pharmacological activities, and ethnomedicinal potentials of G. kola ., Materials and Methods: An extensive review was performed using electronic literature collated from ScienceDirect, Springer, Wiley, and PubMed databases., Results: Phytochemical analysis revealed the isolation of several chemical compounds including 9-octadecenoic acid, linoleic acid, 14-methylpentadecanoic acid, 1-butanol, hexadecanamide, I-4',II-4',I-5,II-5,I-7,II-7-hexahydroxy-I-3,II-8-biflavanone, lanost-7-en-3-one, kolaflavanone (8E)-4-geranyl-3,5-dihydroxybenzophenone, glutinol, Garcinia biflavonoid (GB-2a-II-4'-OMe), 9,19-cyclolanost-24-en-3-ol, 24-methylene, tirucallol, lupeol, β-amyrin, obtusifoliol and Kolaviron. Diverse pharmacological in-vivo and in vitro investigations revealed that G. kola has anti-inflammatory, antimalarial, hepatoprotective, cardioprotective, anti-asthmatic, neuroprotective, antioxidant, and antidiabetic activities., Conclusion: The present study revealed that G. kola has preventive and therapeutic potentials against various diseases in both in vivo and in vitro studies and therefore can be utilised as a raw material in the pharmaceutical industries for the development of therapeutic products. However, there is a need for clinical trial experiments to validate and provide accurate and substantial information on the required safe dosage and efficacy for the treatment of several diseases.

Background: Individual extracts of Garcinia kola and Kigelia africana have been shown to have therapeutic effects against a variety of variables linked to the development of diabetes mellitus. However, there is still a lack of information about the combined effects of these extracts on Insulin and Paraoxonase 1 (PON-1) in Streptozotocin-Nicotinamide-induced type-2 diabetic Wistar rats., Methods: Forty-two young male rats (180-200g) were randomly divided into six groups (n = 7/group). Diabetes was intraperitoneally induced with 110 mg/kg of nicotinamide constituted in distilled water and fifteen minutes later with 65 mg/kg of streptozocin freshly prepared in 0.1M citrate buffer (pH of 4.5) and treated for six weeks as follows: the control rats received either 0.9% normal saline (NS) or 250 mg/kg extract by gavage. The remaining animals were diabetes induced and subsequently treated with either NS, graded doses of the extract (250 mg/kg and 500 mg/kg), or 5 mg/kg Glibenclamide + 100mg/kg Metformin. Gas chromatography-mass spectrometry (GCMS) of the combined extracts was also analyzed to identify the bioactive compounds present in it. Insulin, PON-1 levels, lipid profiles, and atherogenic index were assessed., Results: Our findings show that Insulin and PON-1 levels in the plasma of diabetic rats treated with the combined extracts were significantly increased when compared to the control rats. Moreover, the GCMS of the extract shows the presence of both monounsaturated (oleic acid) and polyunsaturated (linoleic acid) fatty acids., Conclusion: The current findings suggest that the extract may help improve glucose homeostasis and prevent atherosclerosis through the established mechanism of the identified bioactive compounds., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Symptoms and complications associated with severe SARS-CoV-2 infection such as acute respiratory distress syndrome (ARDS) and organ damage have been linked to SARS-CoV-2 spike protein S1-induced increased production of pro-inflammatory cytokines by immune cells. In this study, the effects of an extract of Garcinia kola seeds and garcinoic acid were investigated in SARS-CoV-2 spike protein S1-stimulated human PBMCs. Results of ELISA experiments revealed that Garcinia kola extract (6.25, 12.5, and 25 μg/ml) and garcinoic acid (1.25, 2.5, and 5 μM) significantly reduced SARS-CoV-2 spike protein S1-induced secretion of TNFα, IL-6, IL-1β, and IL-8 in PBMCs. In-cell western assays showed that pre-treatment with Garcinia kola extract and garcinoic acid reduced expressions of both phospho-p65 and phospho-IκBα proteins, as well as NF-κB DNA binding capacity and NF-κB-driven luciferase expression following stimulation of PBMCs with spike protein S1. Furthermore, pre-treatment of PBMCs with Garcinia kola extract prior to stimulation with SARS-CoV-2 spike protein S1 resulted in reduced damage to adjacent A549 lung epithelial cells. These results suggest that the seed of Garcinia kola and garcinoic acid are natural products which may possess pharmacological/therapeutic benefits in reducing cytokine storm in severe SARS-CoV-2 and other coronavirus infections., (© 2021 John Wiley & Sons Ltd.)

Busulfan is a popular antileukemia chemotherapeutic alkylating agent widely known to induce variety of serious adverse effects including chemobrain-related cognitive impairments and dysfunction in male reproductive system. Whether kolaviron, a neuro- and repro-active compound obtained from Garcinia kola, with neuroprotective and reproductive-promoting activities, mitigates busulfan-induced cognitive and male reproductive impairments remain unknown. Hence, we investigated the reversal effects of kolaviron on busulfan-induced episodic memory deficit and testicular dysfunction, and its underlying mechanisms in male rats. In the treatment-protocol, rats in groups 1 and 2 received saline (10 mL/kg/p.o./day) and DMSO (10 mL/kg/p.o./day) respectively, group 3 was given kolaviron (200 mg/kg/p.o./day), group 4 received busulfan (50 mg/kg/p.o./day) and group 5 was pretreated with busulfan (50 mg/kg/p.o./day) consecutively for 56 days prior to kolaviron treatment (200 mg/kg/p.o./day) from days 29-56. Episodic memory deficit was assessed using passive avoidance task (PAT). Following euthanization, blood samples, epididymal sperm, testes and brain were harvested and hormonal and neurochemical contents and their metabolizing enzymes were assayed. Kolaviron reversed busulfan-induced episodic cognitive deficit in the PAT. The reduced serotonin, dopamine, noradrenaline concentrations, elevated glutamate levels, acetylcholinesterase, monoamine oxidase-A and B activities were normalized by kolaviron. Kolaviron also reversed the busulfan-induced decreased testicular/body weights and spermatogenesis. Kolaviron abated busulfan-induced changes in androgenic hormones (testosterone, FSH, LH), dehydrogenase enzymes (3ß-HSD and 17ß-HSD), altered sperm-chromatin, sperm-membrane integrity and sperm-acrosomal reaction and capacitation impairments. Our findings suggest that kolaviron could mitigate busulfan-induced episodic memory deficit and dysfunction in male reproductive system via neurochemical modulations and increase testicular androgenic hormones/enzymes in rats., (Copyright © 2021. Published by Elsevier Masson SAS.)

Drug resistant Salmonella species and shortcomings related to current drugs stress the urgent need to search for new antimicrobial agents to control salmonellosis. This study investigated the antisalmonellal and antioxidant potentials of methanolic and hydro-ethanolic extracts of Garcinia kola and Alchornea cordifolia as potential sources of drugs to control Salmonella species and to reduce related oxidative stress. The antisalmonellal activity was assessed using the broth microdilution, membrane destabilization and time-kill kinetic assays. While, the DPPH, ABTS and FRAP assays were used for the determination of the antioxidant activities. The minimum inhibitory concentrations ranged from 125 to 1000 μg/mL, with the methanolic root extract of G. kola being the most active. The time kill kinetic assay revealed a concentration-dependent bacteriostatic activity for promising extracts. Potent extracts from G. kola showed the ability to destabilize S. typhi outer membrane, with the methanolic root extract presenting the highest activity; two-fold higher than those of polymyxin B tested as reference. In addition, this methanolic root extract of G. kola also provoked nucleotide leakage in a concentration-dependent manner. From the antioxidant assays, the hydro-ethanolic extract from the stem bark of A. cordifolia presented significant activities comparable to that of Vitamin C. The methanolic root extract of G. kola also presented appreciable antioxidant activities, though less than that of A. cordifolia. Overall, the phytochemical screening of active extracts revealed the presence of anthocyanins, flavonoids, glycosides, phenols, tannins, triterpenoids and steroids. These results provide evidence of the antibacterial potential of G. kola and offer great perspectives in a possible standardisation of an antisalmonellal phytomedicine., Competing Interests: The authors have declared that no competing interests exist.

Gakolanone (3',5'-digeranyl-2',4',6',3-tetrahydroxybenzophenone; 1 ), a novel benzophenone derivative was isolated from the hexane extract of Garcinia kola Heckel stem-bark along with three known 3-8'' linked biflavonoids: 3'',4',4''',5,5'',7,7''-heptahydroxy-3,8''-biflavanone ( 2 ); 3'',4',5,5'',5''',7,7''-heptahydroxy-4-methoxy-3,8''-biflavanone ( 3 ) and 4',4''',5,5'',7,7''-hexahydroxy-3,8''-biflavanone ( 4 ) from the ethanol extract. The compounds were characterized primarily using 1 D and 2 D nuclear magnetic resonance spectroscopy and mass spectrometry and by comparing with literature. The compounds were subjected to in-vitro alpha-amylase enzyme inhibitory assay using DNSA (3,5-dinitrosalicylic acid) reagent with acarbose used as the standard drug. All the compounds were found to show alpha-amylase inhibitory activities with IC 50 of 21.4 ± 1.5, 9.9 ± 0.2, 15.3 ± 2.3, 12.9 ± 2.3 µg/mL respectively. All the compounds exhibited better alpha-amylase inhibitory activities than the standard drug, acarbose (IC 50 = 38.1 ± 8.3 µg/mL).

Garcinia kola (GK) stem bark, Uvaria chamae (UC) root, and Olax subscorpioidea (OS) root are components of various indigenous/traditional anticancer regimens. It is, therefore, possible that they might combat oxidative stress and impair cellular proliferation linked to carcinogenesis. In this study, we investigated the antioxidative, mito-depressive, and DNA-damaging activities of the three plant extracts in order to provide further mechanistic insights into their potential anticancer roles in documented cancer remedies that include them. Antioxidative properties were investigated in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging assays and an animal model of drug (cisplatin)-induced oxidative stress. The Allium cepa assay and the single cell gel electrophoresis (SCGE) assay were used to assess mito-depressive and DNA-damaging activities. GK and OS showed significantly higher antioxidant activities in the DPPH assay than ascorbic acid; OS had the lowest IC50 of the three plants in the NO assay, comparable to that of ascorbic acid. Pretreatment with the extracts produced an ameliorative and protective effect against the cisplatin-induced oxidative stress as shown by inhibition of lipid peroxidation and improved or restored reduced glutathione and superoxide dismutase levels. In the Allium test, the three extracts produced significant decreases in root growth and also significant cytotoxicity as evidenced by decreased mitotic index. Each of the extracts also showed significantly increased tail DNA (%) in the SCGE assay, indicating the significant DNA-damaging effect. Taken together, this study demonstrates the possible chemopreventive and chemotherapeutic potentials of the three study extracts, which may explain the roles of their source plants in traditional remedies in the therapy of cancers.

Four fungal isolates were identified in this study of which three were Aspergillus species with Aspergillus flavus having the highest frequency followed by A. parasiticus. The result of high frequency of Aspergillus flavus and Aspergillus parasiticus in the Zea mays sample revealed production of aflatoxins. Maize sample in Awka was found to contain aflatoxin B1 (9.60ppb) and B2 (13.3ppb). Inhibition of A. flavus and A. parasiticus with Azadirachta indica and Garcinia kola seed extracts showed that the test plant extracts were effective for reducing mycelial growth on the test organism. Methanolic extract of G. kola showed antifungal inhibitory activity on the test organisms and the highest at 10% concentration. With ethanol extracts of G. kola, the antifungal activity was effective i.e. for inhibition of A. flavus and A. parasiticus, with A. parasiticus having the higher percentage inhibition at 10%. Inhibiting growth of Aspergillus flavus and Aspergillus parasiticus using methanolic and ethanolic extracts of neem seeds was effective in the inhibition of the test organism at 10%. The methanolic and ethanolic extracts of combined Garcinia kola and neem seeds revealed effective inhibition of A. flavus and A. parasiticus with ethanolic extracts of the combined test plants exerting the highest inhibition against A. flavus (80.43±3.62). The extracts from this plant show the ability to suppress growth of toxigenic A. flavus and A. parasiticus. Phytochemical analysis showed that the methanolic and ethanolic extracts of G. kola and neem seeds showed the presence of secondary metabolites and this may be a reason for the inhibitory activity on A. flavus and A. parasiticus. Results from this study will be important in planning a management strategy against aflatoxin-producing fungi and other fungi associated with spoilage of stored food products.

The plant Garcinia kola is used in African ethno-medicine to treat various oxidation- and inflammation-related diseases but its bioactive compounds are not well characterized. Garcinoic acid (GA) is one of the few phytochemicals that have been isolated from Garcinia kola. We investigated the anti-inflammatory potential of the methanol extract of Garcinia kola seeds (NE) and purified GA, as a major phytochemical in these seeds, in lipopolysaccharide (LPS)-activated mouse RAW264.7 macrophages and its anti-atherosclerotic potential in high fat diet fed ApoE -/- mice. This study outlines an optimized procedure for the extraction and purification of GA from Garcinia kola seeds with an increased yield and a purity of >99%. We found that LPS-induced upregulation of iNos and Cox2 expression, and the formation of the respective signaling molecules nitric oxide and prostanoids, were significantly diminished by both the NE and GA. In addition, GA treatment in mice decreased intra-plaque inflammation by attenuating nitrotyrosinylation. Further, modulation of lymphocyte sub-populations in blood and spleen have been detected, showing immune regulative properties of GA. Our study provides molecular insights into the anti-inflammatory activities of Garcinia kola and reveals GA as promising natural lead for the development of multi-target drugs to treat inflammation-driven diseases., (Copyright © 2019 The Authors. Published by Elsevier B.V. All rights reserved.)

Foods and beverage aroma results from multicomponent mixtures of volatile compounds present in the food that interact with olfactory receptors and produce a perceptual response in the brain. However, the perceptual interactions that occur when complex odor mixtures are combined are not well understood. Here we used Gas chromatography-Recomposition-Olfactometry (GC-R) to better understand the role that individual compounds have on the perceived sensory aroma of bitters. Bitters are the concentrated alcoholic extract of flavorful plant materials with a wide range of complex sensory and chemical aroma profiles that have not been extensively studied. Previously, we demonstrated that Angostura bitters are characterized by complex aroma attributes described as cola, ginger, orange peel, and black pepper and that the volatile composition of Angostura bitters is predominantly composed of terpenoids. Using GC-R to create in-instrument mixtures of the Angostura headspace extracts, the sensory attributes of Angostura extracts with linalool, α-terpinyl-acetate and caryophyllene omitted were evaluated. The omission experiments demonstrated direct and indirect effects of the individual compounds on the aroma attributes of Angostura bitters, through masking, additive, and synergistic interactions. Caryophyllene in particular, which was present in the headspace extracts at concentration only slightly above sensory threshold levels, had a large and unexpected impact on the sensory properties of the mixtures and may be most responsible for the aromas associated with the whole sample. The GC-R and statistical approaches used here provided valuable tools to reveal relationships among individual compounds and aroma attributes of foods that have not been currently theorized using existing analytical approaches.

The beneficial effects of kolaviron, a natural biflavonoid from the seeds of Garcinia kola, have been attributed to its antioxidant and anti-inflammatory activities. This study was designed to investigate the renoprotective effect of kolaviron in rat model of diclofenac (DFC)-induced acute renal failure. Thirty-five male Wistar rats were divided into 7 groups of 5 rats each as follows: a control group that received propylene glycol orally and treatment groups that received DFC, DFC recovery, DFC followed by kolaviron at 3 different doses, and kolaviron only. DFC-treated rats showed sluggishness, illness, and anorexia. Their urine contained appreciable protein, glucose, and ketone bodies. Histopathological examination of their kidneys revealed profound acute tubular necrosis. DFC treatment significantly increased levels of plasma creatinine, urea, sodium, chloride, potassium ions, and increased renal tissue activities of superoxide dismutase, catalase, levels of malondialdehyde, and hydrogen peroxide. Fractional excretion of sodium and potassium and renal tissue levels of reduced glutathione and prostaglandin E 2 (PGE 2 ) decreased significantly in DFC-treated groups. However, kolaviron administration significantly reduced the toxic effect of DFC on PGE 2 release; plasma levels of creatinine, urea, glucose, and electrolytes; and significantly attenuated renal tubular and oxidative damages. Furthermore, the effects of DFC administration on food consumption, water intake, urine output and urine protein, glucose, ketone bodies, and electrolytes were significantly attenuated in animals treated with kolaviron. The results suggested that kolaviron ameliorated DFC-induced kidney injury in Wistar rats by decreasing renal oxidative damage and restoration of renal PGE 2 release back to the basal levels.

Background: The incidence of cardiovascular diseases and its associated complications have increased greatly in the past three decades. The purpose of this study was to evaluate the acute cardioprotective effects of Garcinia kola (GK) seed extract and Kolaviron (KV) and determine mechanisms of action involving RISK signalling pathways., Methods: Male Wistar rats were used in this study. Hearts were excised and mounted on the Langendorff perfusion system. The control, group 1 was perfused with dimethyl sulfoxide (DMSO), group II with KV and group III with GK respectively. Western blot analyses were performed on frozen heart tissues., Results: Isolated rat hearts perfused with KV and GK attenuated apoptotic pathways with significant reduction in p38 MAPK protein phosphorylation, as well as reduction in total caspase 3, cleaved caspase 3 (Asp 175) and PARP cleavage. KV and GK also down-regulated p-JNK1 (Tyr 185) and p-JNK 2 (Thr 183) protein expression at the 10 min reperfusion time ponit. Cardioprotection was achieved in part, by enhancement of the reperfusion injury signalling kinase (RISK) pathway; as evidenced by significant increases in protein expresion of Akt/PKB and p-Akt/PKB (Ser 473) in KV and GK respectively., Conclusions: KV and GK supplementation led to significant increases in the expressions of survival proteins. It is noteworthy that both KV and GK supplementation offered cardioprotection in ischaemic/reperfusion injury rat heart model. In all, GK showed better cardioprotective effect that KV., Competing Interests: There is no conflict of interest (political, religious, academic or financial) whatsoever attached with this manuscript., (© Georg Thieme Verlag KG Stuttgart · New York.)

Background: Cyclophosphamide (CP) is a nitrogen mustard alkylating drug used for the treatment of chronic and acute malignant lymphomas, myeloma, leukemia, neuroblastoma, adenocarcinoma, retinoblastoma, breast carcinoma, and immunosuppressive therapy. Despite its vast therapeutic uses, it is known to cause severe cardiac toxicity. Kolaviron (KV), a Garcinia kola seed extract containing a mixture of flavonoids, is reputed for its antioxidant and membrane stabilizing properties., Objective: This study investigated the protective effect of KV on CP-induced cardiotoxicity in rats., Methods: Thirty rats were used, and they were divided into 6 groups of 5 rats each. Group I received 2 mL/kg propylene glycol orally for 14 days; group II received CP (50 mg/kg/d, intraperitoneally [i.p.]) for 3 days; groups III and IV received 200 and 400 mg/kg/d KV, respectively, orally for 14 days and groups V and VI were pretreated with 200 and 400 mg/kg/d KV, respectively, orally for 14 days followed by CP (50 mg/kg/d, i.p.) for 3 days., Results: CP treatment resulted in a significantly lower food consumption and body weight in rats. The lactate dehydrogenase and creatine kinase enzymes in cardiac tissues of rats treated with CP were significantly higher. In cardiac tissues, 3-day doses of CP resulted in significantly higher heart weight, cardiac troponin I, myeloperoxidase, malondialdehyde, hydrogen peroxide and lower superoxide dismutase, catalase, glutathione peroxidase activities, and reduced glutathione levels. Histological examination of cardiac tissues showed sign of necrosis of myocardium after CP treatment. However, administration of KV at 200 and 400 mg/kg for 14 days prior to CP treatment, increase food consumption, body weight, and attenuates the biochemical and histological changes induced by CP., Conclusions: These results revealed that KV attenuates CP-induced cardiotoxicity by inhibiting oxidative stress and preserving the activity of antioxidant enzymes.

Background The Garcinia kola seeds have been reported for its antibacterial, antioxidant, antidiabetic and also for its chemoprevention property. The use of doxorubicin as an anticancer drug has been accompanied with avalanche of side effects including cardiotoxicity. The aim of this study was to investigate the cardioprotective effect of Kolaviron and Garcinia kola and their mechanisms of action. Methods Sixty male rats (Wistar strain) were used in this study. They were divided into 6 groups (A-F) each containing 10 animals. Group A was the control. Rats in Groups B, C, D, E and F were treated with doxorubicin at the dosage of 15 mg/kg body weight i.p. Prior to this treatment, rats in groups C, D, E and F were pre-treated orally with Kolaviron at the dosage of 100 mg/kg and 200 mg/kg, and Garcinia kola 100 mg/kg and 200 mg/kg for 7 days, respectively. Results The results show that doxorubicin caused a significant increase in heart rate and prolonged QT, reduced antioxidant status, increased oxidative stress, inflammation and markers of cardiac damage which were reversed by pre-treatment with Kolaviron and Garcinia kola. Conclusions Overall, pre-treatment with Kolaviron or Garcinia kola caused reversal of cardiac damage, ECG alteration and oxidative stress by increasing the activity of antioxidant enzymes and reducing the markers of inflammation on doxorubicin-induced cardiotoxicity.

The anti-proliferative effect and down regulation of vascular endothelial growth factor C and toll like receptor-2 by kolaviron on Wuchereria bancrofti infected peripheral blood lymphocytes were investigated. Blood were collected from consenting volunteers in Talata Mafara, Nigeria, between the hours of 10pm to 12am, and microscopically identified for microfilariae. W. bancrofti positive samples were cultured for 72h treated with Doxycycline (2μg/ml) and kolaviron (5μg/ml) in vitro. Mitotic index, expression of vascular endothelial growth factor-C (VEGF-c), toll like receptor-2 (TLR-2) were determined using standard procedures. Mitotic index was significantly (P<0.05) reduced in the kolaviron treated group compared to negative control. Kolaviron also significantly (P<0.05) down regulated the expression of VEGF-c and TLR-2 when compared with the untreated group. In both cases, the effects of kolaviron was not significantly different (P<0.05) to that of doxycycline. Furthermore, strong positive correlations between mitotic index, VEGF-c and TLR-2 expressions were observed. The study suggests that kolaviron rich portion of Garcinia kola exhibited anti-proliferative effect and down regulation of VEGF-c and TLR-2 in W. bancrofti infected blood. Thus, the results from this study might have unravelled the potency of kolaviron in the management of complications associated with lymphatic filariasis., (Copyright © 2017 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Ethnopharmacological Relevance: The development of compounds able to improve metabolic syndrome and mitigate complications caused by inappropriate glycemic control in type 1 diabetes mellitus is challenging. The medicinal plant with established hypoglycemic properties Garcinia kola Heckel might have the potential to mitigate diabetes mellitus metabolic syndrome and complications., Aim of the Study: We have investigated the neuroprotective properties of a suspension of G. kola seeds in long-term type 1 diabetes mellitus rat model., Materials and Methods: Wistar rats, made diabetic by single injection of streptozotocin were monitored for 8 months. Then, they were administered with distilled water or G. kola oral aqueous suspension daily for 30 days. Body weight and glycemia were determined before and after treatment. After sacrifice, cerebella were dissected out and processed for stereological quantification of Purkinje cells. Histopathological and immunohistochemical analyses of markers of neuroinflammation and neurodegeneration were performed., Results: Purkinje cell counts were significantly increased, and histopathological signs of apoptosis and neuroinflammation decreased, in diabetic animals treated with G. kola compared to diabetic rats given distilled water. Glycemia was also markedly improved and body weight restored to non-diabetic control values, following G. kola treatment., Conclusions: These results suggest that G. kola treatment improved the general condition of long-term diabetic rats and protected Purkinje cells partly by improving the systemic glycemia and mitigating neuroinflammation., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

Ethnopharmacological Relevance: Phytochemicals with anti-oxidative and anti-inflammatory properties are known to inhibit tumour initiation, promotion and progression. Hence, there is an increasingly-convincing rationale for employing remedies containing those phytochemicals in the treatment of cancers and also as analgesic and anti-inflammatory adjuvants in therapy. The plants Garcinia kola Heckel (Clusiaceae), stem bark; Uvaria chamae P. Beauv. (Annonaceae), root; and Olax subscorpioidea Oliv. (Olacaceae), root, have been documented to be part of various indigenous anti-cancer regimens., Aim of the Study: To determine if the three plants exhibit significant anti-oxidative and anti-inflammatory properties., Materials and Methods: Using established models, the analgesic and anti-inflammatory activities of the three plants were investigated., Results: Pre-treatment with the plant extracts at 100, 200 and 400mg/kg produced inhibition of writhes; G. kola and U. chamae showed no significant effect on formalin-induced pain, but O. subscorpioidea produced inhibition in both phases of the formalin test. Similarly, while G. kola and U. chamae did not produce any significant inhibitory effect in the xylene-induced ear oedema model, the oedema was significantly reduced by O. subscorpioidea pre-treatment. However, all the three plants significantly inhibited the time-dependent increase in paw circumference in the carrageenan- and formaldehyde-induced rat paw oedema tests, with peak effects observed at 400mg/kg, 6h after the induction of oedema, comparable in some cases to the effects of two standard drugs, the non-steroidal anti-inflammatory drug diclofenac and the anti-inflammatory antibiotic doxycycline., Conclusion: We conclude that the three plant extracts possess analgesic and anti-inflammatory properties, thus providing a scientific rationale for their inclusion in some traditional anti-cancer regimens., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

African populations use traditional medicines in their initial attempt to treat a range of diseases. Nevertheless, accurate knowledge of the composition of these drugs remains a challenge in terms of ensuring the health of population and in order to advance towards improved traditional medicines (ITMs). In this paper chromatographic methods were developed for qualitative and quantitative analyses of a per os antimalarial ITM containing Garcinia kola. The identified analytical markers were used to establish TLC and HPLC fingerprints. G. kola seeds were analysed by HPLC to confirm the identity of the extract used by the Congolese manufacturer in the ITM. The main compounds (GB1, GB2, GB-1a and Kolaflavanone) were isolated by preparative TLC and identified by UPLC-MS and NMR. For the quantification of the major compound GB1, a simple and rapid experimental design was applied to develop an LC method, and then its validation was demonstrated using the total error strategy with the accuracy profile as a decision tool. The accurate results were observed within 0.14-0.45mg/mL range of GB1 expressed as naringenin. The extracts used in several batches of the analysed oral solutions contained GB1 (expressed as naringenin) within 2.04-2.43%. Both the fingerprints and the validated LC-DAD were found suitable for the quality control of G. kola-based raw material and finished products, respectively., (Copyright © 2016 Elsevier B.V. All rights reserved.)

Background: Tuberculosis (TB) is a global health problem. The effects of anti-TB drugs on male reproductive system have not been properly evaluated. We investigated the effects of anti-TB drugs on testicular antioxidant indices, sperm characteristics and hormonal levels in rats, and the protective role of kolaviron (KV), a biflavonoid from Garcinia kola seed., Methods: Twenty-eight male Wistar rats were assigned into four groups and orally treated with corn oil (control), anti-TB drugs [4-Tabs=isoniazid (5 mg/kg), rifampicin (10 mg/kg), pyrazinamide (15 mg/kg) and ethambutol (15 mg/kg) in combination], anti-TB drugs +KV and KV alone (200 mg/kg). Anti-TB drugs and KV were given three times per week for 8 weeks. In vitro, reducing power, inhibition of lipid peroxidation (LPO), diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl radical scavenging effects of KV were examined., Results: KV at 10, 20, 50 and 100 μg/mL showed strong reducing potential and effectively scavenged DPPH and OH radicals in a concentration-dependent manner. Furthermore, KV significantly inhibited LPO in rats' liver homogenate. In vivo, administration of 4-Tabs caused a significant (p<0.05) decrease in body weight gain and weight of testis of rats. Body weight gain and weight of testis decreased by 45% and 36%, respectively, in the 4-Tabs-treated rats. Also, 4-Tabs increased testicular lipid peroxidation by 82%, with a concomitant decrease in antioxidant indices. Testicular reduced glutathione, superoxide dismutase and glutathione peroxidase decreased by 2.2-, 1.9- and 1.6-folds, respectively. Likewise, 4-Tabs markedly decreased sperm count, motility, luteinizing hormone and testosterone. Co-administration of KV with 4-Tabs normalized body weight, enhanced antioxidant system and improved sperm characteristics., Conclusions: Kolaviron protects male reproductive system from oxidative damage by anti-tuberculosis drugs via the antioxidative mechanism.

Background: Tuberculosis (TB) is an infectious disease of international health priority. The combination of anti-TB drugs (4-Tabs)- isoniazid (INH), rifampicin (RIF), pyrazinamide (PZA) and ethambutol (ETB) are effective in the management of the disease, however, their toxic effect is a major concern., Purpose: The study was designed to evaluate the toxicity of anti-TB drugs in male Wistar rats and possible ameliorative effects of kolaviron (KV), a biflavonoid from Garcinia kola seeds., Methods: Twenty-eight rats were assigned into four groups; Group 1 (Control) received corn oil, Group 2 (4-Tabs) received therapeutic doses of INH (5 mg/kg), RIF (10 mg/kg), PZA (15 mg/kg) and ETB (15 mg/kg) in combination, Group 3 (4-Tabs + KV) received INH, RIF, PZA, ETB and KV (200 mg/kg) and Group 4 (KV) received KV (200 mg/kg) by oral gavage three times per week for 8 consecutive weeks., Results: Administration of 4-Tabs caused oxidative stress resulting in significant (p = 0.031, 0.027) increase in malondialdehyde levels in the liver and kidney of rats by 101% and 34%, respectively. Also, 4-Tabs caused significant (p = 0.023-0.035) elevation of serum alanine and aspartate aminotransferases by 41% and 48%, creatinine by 252% and total bilirubin by 89%, respectively. In contrast, hepatic and renal antioxidant indices- reduced glutathione, glutathione peroxidase, glutathione-s-transferase and superoxide dismutase were significantly (p = 0.028-0.039) decreased in 4-Tabs-treated rats. Co-administration of KV with 4-Tabs significantly restored the antioxidant parameters and biochemical indices to near normal., Conclusion: These findings suggest that anti-TB drugs elicit oxidative damage in liver and kidney of rats while KV protects against the adverse effects via antioxidative mechanism.

Kolaviron is a phytochemical isolated from Garcina kola (G. kola); a common oral masticatory agent in Nigeria (West Africa). It is a bioflavonoid used--as an antiviral, anti-inflammatory and antioxidant--in relieving the symptoms of several diseases and infections. In this study we have evaluated the neuroprotective and regenerative effect of kolaviron in neurons of the prefrontal cortex (Pfc) before or after exposure to sodium azide (NaN3) induced oxidative stress. Separate groups of animals were treated as follows; kolaviron (200 mg/Kg) for 21 days; kolaviron (200 mg/Kg for 21 days) followed by NaN3 treatment (20 mg/Kg for 5 days); NaN3 treatment (20 mg/Kg for 5 days) followed by kolaviron (200 mg/Kg for 21 days); 1 ml of corn-oil (21 days-vehicle); NaN3 treatment (20 mg/Kg for 5 days). Exploratory activity associated with Pfc function was assessed in the open field test (OFT) following which the microscopic anatomy of the prefrontal cortex was examined in histology (Haematoxylin and Eosin) and antigen retrieval Immunohistochemistry to show astroglia activation (GFAP), neuronal metabolism (NSE), cytoskeleton (NF) and cell cycle dysregulation (p53). Subsequently, we quantified the level of Glucose-6-phosphate dehydrogenase (G6PDH) and lactate dehydrogenase (LDH) in the brain tissue homogenate as a measure of stress-related glucose metabolism. Kolaviron (Kv) and Kolaviron/NaN3 treatment caused no prominent change in astroglia density and size while NaN3 and NaN3/Kv induced astroglia activation and scar formation (astrogliosis) in the Pfc when compared with the control. Similarly, Kolaviron and Kv/NaN3 did not alter NSE expression (glucose metabolism) while NaN3 and NaN3/Kv treatment increased cortical NSE expression; thus indicating stress related metabolism. Further studies on enzymes of glucose metabolism (G6PDH and LDH) showed that NaN3 increased LDH while kolaviron reduced LDH in the brain tissue homogenate (P < 0.001). In addition kolaviron treatment before (P < 0.001) or after (P < 0.05) NaN3 treatment also reduced LDH expression; thus supporting its role in suppression of oxidative stress. Interestingly, NF deposition increased in the Pfc after kolaviron treatment while Kv/NaN3 showed no significant change in NF when compared with the control. In furtherance, NaN3 and NaN3/Kv caused a decrease in NF deposition (degeneration). Ultimately, the protective effect of KV administered prior to NaN3 treatment was confirmed through p53 expression; which was similar to the control. However, NaN3 and NaN3/Kv caused an increase in p53 expression in the Pfc neurons (cell cycle dysregulation). We conclude that kolaviron is not neurotoxic when used at 200 mg/Kg BW. Furthermore, 200 mg/Kg of kolaviron administered prior to NaN3 treatment (Kv/NaN3) was neuroprotective when compared with Kolaviron administered after NaN3 treatment (NaN3/Kv). Some of the observed effects of kolaviron administered before NaN3 treatment includes reduction of astroglia activation, absence of astroglia scars, antioxidation (reduced NSE and LDH), prevention of neurofilament loss and cell cycle regulation.

Ethnopharmacological Relevance: Garcinia kola is a medicinal plant traditionally used for malaria therapy in Central Africa., Aim of the Study: To evaluate the antimalarial potencies in vitro and in vivo of pure biflavanones from G. kola., Materials and Methods: The pure biflavanones were obtained by bioassay-guided fractionation of a 70% ethanol extract of G. kola seeds and their chemical structures were elucidated by comparison of their NMR ((1)H and (13)C) and mass spectral data with those provided in the literature. Plasmodium falciparum (FCR-3, cycloguanil-resistant strain from Gambia) was used for in vitro assessments of antimalarial activities. Growth inhibition, intraerythrocytic development and parasite morphology were evaluated in culture by the microscopic observation of Giemsa-stained thin blood films. The cytotoxicity of the antimalarial compounds was evaluated against KB 3-1 (human epidermoid carcinoma) cells by MTT assay. In vivo antimalarial activities were determined in mice infected with Plasmodium berghei (ANKA strain) following a four-day suppressive test., Results: The bioassay-guided fractionation of an extract of G. kola resulted in the isolation of three biflavanones (GB-1a, GB-1, and GB-2) as its active principles. These three biflavanones displayed not only potent inhibitory activity in vitro against P. falciparum proliferation but also antimalarial potency through oral administration in mice infected with P. berghei without signs of acute toxicity. GB-1 was found to exhibit the strongest in vitro antimalarial potency on P. falciparum with an IC50 of 0.16μM, whereas it exhibited a very low in vitro cytotoxicity on KB 3-1 cells with an IC50 of greater than 150μM. During an in vivo antimalarial assay in mice infected with P. berghei, GB-1 was found to exhibit biological potency with an approximate ED50 of 100mg/kg following oral administration. GB-1 was also shown to increase the average life span of the infected mice significantly compared to that of control mice (p<0.01 Student's t-test)., Conclusions: The antimalarial outcome of GB-1a, GB-1, and GB-2 may be related to the traditional utilization of this crude drug against malaria judging from their significant content in G. kola nuts. GB-1 showed the most potent antimalarial activity with a high selectivity index and, therefore could be exploited to identify the molecular target, which subsequently could be helpful to design novel therapeutics against malaria. GB-1 may be considered a promising antimalarial candidate for trial in vivo using higher animals infected with P. falciparum., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

Background: Alteration in antioxidant defence and increase in oxidative stress that results in tissue injury is characteristic of diabetes. We evaluated the protective effects of kolaviron (a flavonoid complex extracted from the seeds of Garcinia kola) on hepatic antioxidants, lipid peroxidation and apoptosis in diabetic rats., Methods: To induce diabetes, rats were injected with streptozotocin intraperitoneally at a single dose of 50 mg/kg. Kolaviron (100 mg/kg) was administered orally for 6 weeks (5 times weekly). Activities of liver antioxidant enzymes was analysed with Multiskan Spectrum plate reader. High performance liquid chromatography (HPLC) was used in the analysis of MDA (malondialdehyde), a product of lipid peroxidation. Apoptosis was assessed by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay., Result: Diabetic rats exhibited a significant increase in the peroxidation of hepatic lipids as observed from the elevated level of malondialdehyde (MDA). In addition, Oxygen Radical Absorbance Capacity (ORAC), level of reduced glutathione (GSH), ratio of reduced to oxidized glutathione (GSH: GSSG) and catalase (CAT) activity were decreased in the liver of diabetic rats. The activities of GPX (glutathione peroxidase) and SOD (superoxide dismutase) were unaltered in diabetic rats. TUNEL assay revealed increased apoptotic cell death in the liver. Kolaviron attenuated lipid peroxidation and apoptosis, increased CAT activity, GSH levels and GSH: GSSG ratio. The ORAC of kolaviron-treated diabetic liver was restored to near-normal values., Conclusion: Kolaviron protects the liver against oxidative and apoptotic damage induced by hyperglycemia.

Phenytoin, an anticonvulsant agent used for the treatment of epilepsy has been reported to exhibit toxic side effects on the liver and testes. The present study investigated the protective effects of kolaviron (KV, a bioflavonoid from Garcinia kola seeds) against hepatic and testicular damage in rats exposed to phenytoin. The study consisted of four groups of six rats per group. Group I rats received 2 mL/kg of corn alone while group II received 75 mg/kg of phenytoin (PHT) alone. Groups III and IV were co-treated with kolaviron (200 mg/kg KV) and vitamin E (500 mg/kg VTE), respectively, for 14 days. The antioxidant status, hepatic and reproductive functional parameters were subsequently determined. PHT treatment significantly (p < 0.05) increased superoxide dismutase (SOD) and catalase (CAT) activities, elevated lipid peroxidation (LPO) and hydrogen peroxide (H2O2) levels along with significant reduction in the hepatic and testicular levels of glutathione (GSH). Moreover, PHT exposure elicited significant increases in alkaline phosphatase (ALP) and aspartate aminotransferase (AST) levels. The significant reduction in seminal epithelium thickness and the diameter of seminiferous tubules was accompanied with marked decrease in sperm motility, sperm count, and viability in PHT-treated rats. However, antioxidant status and the functional indices of liver and testes were restored to near control levels in rats co-treated with KV and VTE. In conclusion, KV and VTE protect the liver and testes against functional impairment due to PHT treatment.

Background: The aim of this study was to evaluate the cardioprotective effects of kolaviron (KV), a biflavonoid from Garcinia kola seeds, in rats intoxicated with isoproterenol chloride (ISO) while quercetin (QUE) served as standard., Methods: Forty-two male Wistar rats (180-200 g) were randomly divided into seven groups of six rats each. Group 1 served as control; group 2 received ISO (85 mg/kg subcutaneously); groups 3, 4 and 5 received ISO and KV1 [100 mg/kg orally (p.o.)], KV2 (200 mg/kg, p.o.) and QUE (25 mg/kg, p.o.), respectively; and groups 6 and 7 received QUE and KV2, respectively., Results: Administration of ISO caused significant (p<0.05) elevation of serum creatine phosphokinase, lactate dehydrogenase, alkaline phosphatase, alanine aminotransferase and aspartate aminotransferase by 2.2-, 1.9-, 2.1-, 1.9- and 1.7-fold, respectively, relative to controls, with a concomitant decrease in cardiac activities of these enzymes. Administration of ISO led to significant decrease (p<0.05) in the levels of cardiac superoxide dismutase, catalase, glutathione S-transferase, reduced glutathione and increase in malondialdehyde (MDA). Also, ISO-treated rats had significantly higher values of serum total cholesterol, triglycerides and low-density lipoprotein cholesterol relative to controls. Supplementation with KV2 and QUE caused significant elevation of cardiac antioxidant enzymes, normalized the marker enzymes and reduced MDA levels., Conclusions: KV protects against ISO-induced cardiotoxicity in vivo, suggesting its usefulness as a possible chemoprophylactic agent against cardiotoxic drugs.

Diabetic nephropathy is a complex disease that involves increased production of free radicals which is a strong stimulus for the release of pro-inflammatory factors. We evaluated the renal protective effect of kolaviron (KV) - a Garcinia kola seed extract containing a mixture of 5 flavonoids, in diabetes-induced nephrotoxic rats. Male Wistar rats were divided into 4 groups: untreated controls (C); normal rats treated with kolaviron (C+KV); untreated diabetic rats (D); kolaviron treated diabetic rats (D+KV). A single intraperitoneal injection of streptozotocin (STZ, 50mg/kg) was used for the induction of diabetes. Renal function parameters were estimated in a clinical chemistry analyzer. Markers of oxidative stress in the kidney homogenate were analyzed in a Multiskan Spectrum plate reader and Bio-plex Promagnetic bead-based assays was used for the analysis of inflammatory markers. The effect of kolaviron on diabetes-induced apoptosis was assessed by TUNEL assay. In the diabetic rats, alterations in antioxidant defenses such as an increase in lipid peroxidation, glutathione peroxidase (GPX) activity and a decrease in catalase (CAT) activity, glutathione (GSH) levels and oxygen radical absorbance capacity (ORAC) were observed. There was no difference in superoxide dismutase (SOD) activity. Diabetes induction increased apoptotic cell death and the levels of interleukin (IL)-1β and tumor necrosis factor (TNF)-α with no effect on IL-10. Kolaviron treatment of diabetic rats restored the activities of antioxidant enzymes, reduced lipid peroxidation and increased ORAC and GSH concentration in renal tissues. Kolaviron treatment of diabetic rats also suppressed renal IL-1β. The beneficial effects of kolaviron on diabetes-induced kidney injury may be due to its inhibitory action on oxidative stress, IL-1β production and apoptosis., (Copyright © 2014 The Authors. Published by Elsevier GmbH.. All rights reserved.)

Background: Kolaviron (Kol-v), an important component of Garcinia kola seed has a variety of biologic activities, including anti-inflammatory properties., Methods: We tested the ability of Kol-v to block signalling pathways implicated in lipopolysaccharide (LPS)-induced inflammatory gene expression in RAW 264.7 macrophage cell line., Results: When macrophages pre-treated with Kol-v (15 and 25μM) were activated with LPS, phosphorylation of p38 and p-c-JUN but not IκBα degradation and phosphorylation of NF-κB (p65), ERK1/2, and IκBα were blocked. Furthermore, Kol-v suppressed LPS-induced increase in the expression of IL-18 gene and LPS-induced decrease in the mRNA expression of IP-10 but it had no effect on the LPS-induced decrease in the gene expression levels of IL-1α, IL-33, IL-1β, and IFNβ1-1. When macrophages pre-treated with Kol-v (50 and 100μM) were activated with LPS, phosphorylation of Akt, ERK1/2, IκBα, and NFκB (p65) but not that of CREB was blocked by Kol-v. The protective effect of Kol-v on the LPS-induced phosphorylation of the mitogen activated protein kinase (MAPK) family member JNK was only observed at 100μM. At all concentrations of Kol-v (0-100μM) tested in this study, there was no effect of Kol-v on LPS-induced secretion of the pro-inflammatory cytokine TNF-α but a concentration dependent inhibition of Kol-v on IL-6 secretion was observed., Conclusion: Kol-v interferes with LPS signalling by reducing the activation of several inflammatory transcription factors and that its inhibitory action on IL-6 secretion correlates with inhibition of ERK1/2, p38, Akt, p-c-JUN and JNK signalling pathways., General Significance: The anti-inflammatory potential of Kol-v via inhibition of IL-6 secretion in RAW macrophage was established in this study., (Copyright © 2014 Elsevier B.V. All rights reserved.)

Adsorption chromatography was used to separate the bioactive constituents of the crude n-hexane extract of Garcinia kola seeds. The silica gel 60 column fractions were eluted using the solvent combination of benzene: ethanol : ammonium hydroxide (BEA) in the ratio combination of 36 : 4 : 0.4 v/v. The fractions were tested for anti-Listeria activities by determining their MIC50, MIC90 or MIC against 4 Listeria isolates. The fractions were labelled BEA1 to BEA5 and 3 out of the 5 fractions eluted were active against the test Listeria species with MIC's ranging from MIC 0.57 mg/mL to MIC50 0.625 mg/mL. The most active fractions, BEA2 and BEA3, were subjected to gas chromatography coupled to mass spectrometry (GC-MS) to identify their composition. Fraction BEA2 constituted of 18 compounds mostly sterols and the BEA3 fraction contained 27 compounds with the most abundant compounds being fatty acids derivatives. The BEA2 fraction's interactions with antibiotics proved to be 100% synergistic with ciprofloxacin and ampicillin whilst it exhibited 50% additivity and 50% synergism with penicillin G. However, all the interactions of the BEA2 fraction with each of the conventional antibiotics used were synergistic against the human listeriosis causative bacteria Listeria monocytogenes.

Objective: To investigate the antimalarial potential of kolaviron (KV), a biflavonoid fraction from Garcinia kola seeds, against Plasmodium berghei (P. berghei) infection in Swiss albino mice., Methods: The study consists of seven groups of ten mice each. Groups I, II and III were normal mice that received corn oil, KV1 and chloroquine (CQ), respectively. Groups IV, V, VI and VII were infected mice that received corn oil, CQ, KV1 and KV2, respectively. CQ, KV1 and KV2 were given at 10-, 100- and 200-mg/kg daily, respectively for three consecutive days., Results: Administration of KV1 and KV2 significantly (P<0.05) suppressed P. berghei-infection in the mice by 85% and 90%, respectively, while CQ produced 87% suppression relative to untreated infected group after the fifth day of treatment. Also, KV2 significantly (P<0.05) increased the mean survival time of the infected mice by 175%. The biflavonoid prevented a drastic reduction in PCV from day 4 of treatment, indicating its efficacy in ameliorating anaemia. Significant (P<0.05) oxidative stress assessed by the elevation of serum and hepatic malondialdehydewere observed in untreated P. berghei-infected mice. Specifically, serum and hepatic malondialdehyde levels increased by 93% and 78%, respectively in the untreated infected mice. Furthermore, antioxidant indices, viz; superoxide dismutase, catalase, glutathione-s-transferase, gluathione peroxidase and reduced gluathione decreased significantly (P<0.05) in the tissues of untreated P. berghei-infected mice. KV significantly (P<0.05) ameliorated the P. berghei-induced decrease in antioxidant status of the infected mice., Conclusions: This study shows that kolaviron, especially at 200 mg/kg, has high antimalarial activities in P. berghei-infected mice, in addition to its known antioxidant properties., (Copyright © 2014 Hainan Medical College. Published by Elsevier B.V. All rights reserved.)

Background: Chronic inflammation plays a crucial role in hyperglycemia-induced liver injury. Kolaviron (KV), a natural biflavonoid from Garcinia kola seeds have been shown to possess anti- inflammatory properties which has not been explored in diabetes. To our knowledge, this is the first study to investigate the effect of KV on pro-inflammatory proteins in the liver of diabetic rats., Methods: Diabetes was induced by a single intraperitoneal injection of streptozotocin (STZ) (50 mg/kg) in male Wistar rats. Kolaviron (100 mg/kg) was administered orally five times a week for six weeks. The concentrations of cytokines and chemokine were measured using Bio-plex Pro™ magnetic bead-based assays (Bio-Rad Laboratories, Hercules, USA). Plasma glucose and serum biomarkers of liver dysfunction were analyzed with diagnostic kits in an automated clinical chemistry analyzer. Insulin concentration was estimated by radioimmunoassay (RIA)., Result: Kolaviron (100mg/kg) treatment significantly ameliorated hyperglycemia and liver dysfunction. Serum levels of hepatic marker enzymes were significantly reduced in kolaviron treated diabetic rats. Kolaviron prevented diabetes induced increase in the hepatic levels of proinflammatory cytokines; interleukin (IL)-1beta, IL-6, tumour necrosis factor (TNF-α) and monocyte chemotactic protein (MCP-1)., Conclusion: The results of this study demonstrate that the hepatoprotective effects of kolaviron in diabetic rats may be partly associated with its modulating effect on inflammatory responses.

This study investigated the protective role of kolaviron, a natural antioxidant biflavonoid isolated from the seed of Garcinia kola, in ethylene glycol monoethyl ether (EGEE)-induced testicular dysfunction in male rats. Adult male Wistar rats were exposed to EGEE (200 mg/kg) separately or in combination with either kolaviron (100 or 200 mg/kg) or vitamin E (50 mg/kg) for 14 days. Immunoblot analysis revealed that EGEE exposure alone significantly increased stress-inducible proteins levels. The increased protein expression of active caspases, Fas and Fas-L, was accompanied by nuclear factor kappa B downregulation and elevation of cytosolic cytochrome c level in EGEE-treated rats. In addition, the observation from immunofluorescence staining was consistent with the increased TUNEL-positive nuclei in the testes of EGEE-treated rats. Kolaviron and vitamin E significantly inhibited induction of stress proteins and germ cell apoptosis in EGEE-treated rats. Overall, kolaviron by virtue of its antioxidant and anti-apoptotic properties prevented EGEE-induced reproductive toxicity in rats.

Background: Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used in the treatment of HIV infections and has been reported to be toxic to the male reproductive system. This study was designed to evaluate the ameliorative effects of kolaviron (KV), a biflavonoid from Garcinia kola, on NVP-induced testicular toxicity., Methods: The adult male Wistar rats were given two and four times therapeutic doses of NVP (NVP-2T and NVP-4T; 18 and 36 mg/kg NVP) alone or in combination with KV (200 mg/kg). NVP was given daily, whereas KV was administered five times in a week by oral gavage., Results: Treatment with NVP did not alter the body weight gain and relative weight of testis of the rats. NVP-4T significantly (p<0.05) decreased the sperm motility, protein content, and live-dead ratio and also increased the percentage sperm abnormalities of the rats. Although NVP-4T significantly increased sperm abnormalities, it has no effect on epididymal sperm count. Also, NVP-4T caused a significant (p<0.05) elevation of serum aminotransferases and γ-glutamyl transferase activities. In addition, NVP-4T significantly (p<0.05) decreased the levels of testicular superoxide dismutase, catalase, glutathione S-transferase, and glutathione with marked elevation of malondialdehyde (index of lipid peroxidation) in the rats. In contrast, NVP-2T did not produce an adverse effect on the biochemical indices studied in testes and sperm of rats. Supplementation with KV significantly ameliorated the biochemical changes caused by NVP-4T., Conclusions: Taken together, KV reversed the adverse effects of NVP-4T on testicular antioxidant enzymes and markers of oxidative stress in the rats.

Objective: To investigate the abilities of two flavonoids - Garcinia biflavanol-1 (GB-1) and Garcinia biflavanol-2 (GB-2) from Garcinia kola (G. kola) in reducing cadmium-induced effects on raw U937 cells and U937-derived macrophages., Methods: Macrophage U937 cells were incubated with cadmium followed by treatment with the flavonoids and cell viability assessed via trypan blue staining. In the other experiment, the U937 cells were transformed to the macrophage form and treated with cadmium in order to activate them. The cells were later incubated with the flavonoids and finally the supernatant of each cell culture was analysed for the secretion of nitric oxide, catalyse activity, and the release of tumour necrosis factor-alpha, interleukin-1 and interleukin-2 as indices of macrophage activation. Quercetin (a flavonol) was used as the reference flavonoid in all experiments., Results: It revealed that the flavonoids significantly increased the viability of the cells and also reduced the cadmium-induced activation of the macrophage cells in a concentration-dependent manner. The flavanols GB-1 and GB-2 possessed higher activities than quercetin in all cases (P<0.05). Garcinia biflavanol-2 possessed a higher bioactivity than GB-1 significantly (P<0.05)., Conclusions: In addition to corroborating the several reported importance of G. kola as a potential neutraceutical and pharmacological condiment, the study also clearly indicates the role hydroxylation especially at the 3'- position of polyphenols could play in enhancing bioactivities of flavonoids., (Copyright © 2013 Hainan Medical College. Published by Elsevier B.V. All rights reserved.)

Background: Hypoglycaemic effect of kolaviron (KV), (biflavonoid from Garcinia kola) in streptozotocin (STZ)-diabetic rats has been established., Objectives: To evaluate the possible protective effects of KV on cardiac, renal and hepatic tissues of STZ-diabetic rats., Methods: This study consists of four groups of 6 rats each. Groups one and two contained non-diabetic and untreated-diabetic rats, respectively. Groups three and four were made up of KV- and glibenclamide (GB) - treated diabetic rats, respectively., Results: STZ-intoxication caused a significant (p<0.05) increase in the relative weight of liver in diabetic rats. STZ-diabetic rats had significant increase (p<0.05) in the levels of fasting blood glucose (FBG), á-amylase and HbA1c. A marked and significant (p<0.05) increase in the levels of cardiac, renal and liver marker indices such as serum creatine kinase, lactate dehydrogenase, creatinine, urea and alanine aminotransferase were observed in untreated diabetic rats. Also, untreated diabetic rats had significantly (p<0.05) elevated urinary glucose and protein and, lowered creatinine clearance. In KV- and GB- treated groups, the levels of FBG, á-amylase and HbA1c were significantly (p<0.05) reduced, while treatment with KV significantly (p<0.05) attenuated the cardiac, renal and liver marker indices., Conclusion: KV offered significant antidiabetic and tissues protective effects in the rats.

In this study, the morphological and biochemical susceptibility of the rat brain to vanadium, in the form of sodium metavanadate, and the comparative ameliorative effect of Garcinia kola and kolaviron (G. kola extract), was examined. Brain regions examined were the cerebrum, cerebellum, hippocampus and the olfactory bulb. We showed that vanadium administration caused cellular vacuolation, congestion, and Purkinje cell degeneration and a marked reduction in myelin tracts. Biochemical tests revealed increased lipid peroxidation induced by vanadium, which was ameliorated with the administration of G. kola and kolaviron. Vanadium administration caused an increase in thiobarbituric acid-reactive substances (TBARS) in the cerebrum and hippocampus, whereas the administration of kolaviron resulted in a reduction of the TBARS level by 65.7 and 80%, respectively, in the regions aforementioned. Also, the administration of kolaviron resulted in an increased activity of superoxide dismutase (61.24%) in all brain regions assessed, when compared with the group administered vanadium alone. Results obtained from this study led to the conclusion that kolaviron reduces vanadium-induced oxidative stress in the brain.

The age long acclaimed aphrodisiac potentials of Garcinia kola seeds in some parts of Western Nigeria has not been substantiated with scientific evidence. In this study, we have decided to evaluate the effect of aqueous seed extract of G. kola at the doses of 25, 50 and 100 mg/kg body weight on sexual behaviour of male rats. Male rats weighing 215.00 ± 18.58 g were randomized completely into four groups (A-D) of six animals each. Animals in group A received, orally, 0.5 ml of distilled water only while those in groups B, C and D received same volume containing 25, 50 and 100 mg/kg body weight of the seed extract respectively. Frequencies of mount (MF), intromission (IF), genital toilet (GTF) and ejaculation (EF) as well as latencies of mount (ML), intromission (IL) and ejaculation (EL) were evaluated following the pairing of male rats (1:1) with non-oestrous female rats. The parameters were monitored for the first (15-30 min), second (75-90 min) and third (180195 min) observatory periods. The levels of testosterone, luteinizing (LH) and follicle stimulating hormones (FSH) were also determined. Phytochemical screening of the extract revealed the presence of saponins (2.78%), cardiac glycosides (0.26%), cardenolides and dienolides (0.24%), flavonoids (1.28%) and steroids (1.14%). The 25 and 100 mg/kg body weight increased (P<0.05) the MF whereas the ML was decreased by all the doses of the extract. MF and ML were not altered during the second observatory period whereas the 50 mg/kg body weight increased these parameters during the third observatory period. Other sexual behaviour parameters as well as serum testosterone, FSH and LH were not significantly altered throughout the observatory periods. Overall, the results revealed that G. kola seeds did not have sex enhancing potential as claimed. Therefore, the acclaimed pro sexual effect of Garcinia kola seeds is scientifically untrue. This study has refuted the claim that one of the rationales for consuming the seeds by the aged population of Nigeria is to enhance sexual invigoration in males.

We sought to explore the mechanism by which kolaviron (Kol) protects against atrazine (ATZ)-induced toxicity of cultured interstitial Leydig cells (ILCs). In our experiments, treatment with Kol improved Leydig cell viability and significantly reduced malondialdehyde (MDA) and reactive oxygen species (ROS) levels. Further investigations revealed a reduction in glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione-S-transferase (GST) and elevation of superoxide dismutase 1 (SOD-1) and superoxide dismutase 2 (SOD-2) as measured by messenger RNA (mRNA) expression. Additionally, the ATZ-induced alterations in the mRNA transcript copy numbers of steroidogenesis genes: steroidogenic acute regulatory protein (StAR), cytochrome P450 side-chain cleavage enzyme (CYP11A1), and 3β-hydroxysteroid dehydrogenase (3β-HSD) were shifted toward the control values by Kol. Taken together, these findings indicate that Kol protects ILCs from ATZ-induced toxicity via the reduction in ROS and MDA levels and induce normalization of mRNA levels of all the tested genes.

We assessed the bioactivity of G. kola seeds on Streptococcus pyogenes, Staphylococcus aureus, Plesiomonas shigelloides and Salmonella typhimurium. The crude ethyl acetate, ethanol, methanol, acetone and aqueous extracts were screened by the agar-well diffusion method and their activities were further determined by Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) assays. The extracts were fractionated by Thin Layer Chromatography (TLC). Bioautography was used to assess the activity of the possible classes of compounds present in the more active extracts. Column chromatography was used to purify the active compounds from the mixture, while GC-MS was used to identify the phytocomponents of the fractions. The inhibition zone diameters of the extracts ranged from 0-24 ± 1.1 mm, while MIC and MBC values ranged between 0.04-1.25 mg/mL and 0.081-2.5 mg/mL, respectively. The chloroform/ethyl acetate/formic acid (CEF) solvent system separated more active compounds. The MIC of the fractions ranged between 0.0006-2.5 mg/mL. CEF 3 (F3), CEF 11 (F11) and CEF 12 (F12) revealed the presence of high levels of linoleic acid, 1,2-benzenedicarboxylic acid and 2,3-dihydro-3,5-dihydroxy-6-methyl ester, respectively. The results obtained from this study justify the use of this plant in traditional medicine and provide leads which could be further exploited for the development of new and potent antimicrobials.

Ionizing radiation is one of the environmental factors that may contribute to reproductive dysfunction by a mechanism involving oxidative stress. We investigated the possible ameliorative effects of kolaviron (KV) (a biflavonoid from the seeds of Garcinia kola) on sperm characteristics, testicular lipid peroxidation (LPO) and antioxidant status after a whole body γ-irradiation in Wistar rats. Vitamin C (VC) served as standard antioxidant in this study. The study consists of four groups of 6 rats each. Group I received corn oil, whereas group II received a single dose of γ-radiation (5 Gy). The animals in groups III and IV were pretreated with KV (250 mg/kg) and VC (250 mg/kg) by oral gavage five times in a week, respectively, for 6 weeks prior to and 8 weeks after exposure to γ-radiation. Gamma-irradiation resulted in a significant (p<0.05) decrease in body weight and relative testes weight. Also, γ-irradiation significantly (p<0.05) decreased the activities of superoxide dismutase, catalase and glutathione S-transferase as well as glutathione level, but markedly elevated malondialdehyde levels in the serum and testes. Irradiated rats showed testicular degeneration with concomitant decrease in sperm motility and viability. Although sperm abnormalities significantly increased, it has no effect on the epididymal sperm count. KV and VC significantly (p<0.05) decreased the body weight loss and increased relative testes weights of the rats. Furthermore, supplementation of KV and VC ameliorated radiation-induced toxicity by increasing the activities of antioxidant enzymes, decreased LPO and abrogated testicular degeneration. Taken together, γ-irradiation caused reproductive dysfunction by depleting the antioxidant defence system in the rats, while administration of KV or VC ameliorated the radiation-induced testicular toxicity., (Copyright © 2010 Elsevier GmbH. All rights reserved.)

Crude methanol extracts of Garcinia kola (Heckel) seeds were screened for their antilisterial activities against 42 Listeria bacteria isolated from wastewater effluents. The extract had activity against 45% of the test bacteria and achieved minimum inhibitory concentrations (MICs) ranging between 0.157 and 0.625 mg/mL. The rate of kill of the extract was determined against four representative Listeria species in the study, and the results showed that the highest percentage of bacteria cells were killed after the maximum exposure time of 2 h at the highest concentration of 4 × MIC value, with the maximum number of bacteria cells killed being for L. ivanovii (LEL 30) 100%, L. monocytogenes (LAL 8) 94.686%, L. ivanovii (LEL 18) 60.330%, and L. grayi (LAL 15) 56.071% We therefore conclude that the nature of inhibition of the crude methanol extracts of Garcinia kola seeds can be either bactericidal or bacteriostatic depending on the target Listeria species and can also differ among same species as evidenced by L. ivanovii strains LEL 30 and LEL 18.

Objective: To investigate three tropical plant materials - clove seeds [Syzygium aromaticum (S. aromaticum)], bitter kola fruits [Garcinia kola (G. kola)] and tobacco leaves (Nicotiana species) as potential targeted killers of Streptococcus mutans (S. mutans), a cavity-causing bacterium (gram-positive, facultative anaerobe) that resides in a multispecies microbial community (dental plaque) for the treatment of dental caries (tooth decay)., Methods: Thirty one (31) teeth samples were collected from patients with obvious signs of tooth decay (swollen gum, weak or fallen tooth, etc.) using sterile swab sticks. These samples were collected from two major dental clinics in Nsukka, Enugu State, Nigeria and investigated by spread inoculation onto sterile blood agar and Mueller Hinton agar (MHA) respectively and incubated at 37 °C for 24 h. The discrete colonies obtained were further re-inoculated onto sterile Mitis salivarius agar (MSA) plates and incubated as above. The isolates were characterized by gram staining and catalase test. Tobacco leaves, clove seeds and bitter kola fruits were ground into powder, extracted with three different solvents (n-hexane, hot water and ethanol), filtered, dried and stored in clean containers, corked and kept until used. The plant extracts were investigated for phytochemistry, minimum inhibitory concentration (MIC), minimum cidal concentration (MCC) and compared with some conventional antibiotics commonly used against tooth decay. Antibiotic sensitivity test was also carried out. The results were statistically analyzed., Results: The extracts showed varied phytochemical composition but most abundantly the flavonoids. Our result also shows that females (16) have more tooth decay than males (15) and that 16 samples were very bloody while 15 were slightly bloody. The microbial characterization showed that 18 samples were catalase-positive indicating the presence of S. mutans while 13 were catalase-negative suspected to be Staphylococcus spp. The Gram reaction confirmed 13 Gram-negative and 18 Gram-positive organisms. The n-hexane extract had the best antimicrobial activity followed by the ethanol and lastly hot water. MIC showed that n-hexane clove extract had the largest inhibition zone diameter, followed by bitter kola extract and lastly tobacco extract. The antibiotic sensitivity test credited ciprofloxacin the best because it exhibited broad spectrum of action., Conclusions: Since the n-hexane extract of clove seeds demonstrated preferential growth-inhibitory activity against the causal cariogenic pathogens (S. mutans) in dental caries, we therefore, report here that clove extract be henceforth considered as a potential ingredient in toothpaste preparation., (Copyright © 2011 Hainan Medical College. Published by Elsevier B.V. All rights reserved.)

Objective: To assess the neuroprotective effects of aqueous extract of Garcinia kola on neurotoxin administered malnourished mice adopting histological procedure., Methods: The study was carried out using thirty-two adult malnourished mice which were randomly assigned into four groups (n=8): A, B, C and D. Group A served as control, while the other groups served as the experimental groups. Animals in group A were fed malnourished diet ad libitum and given water liberally. Animals in group B were administered with 3-Nitropropionic acid (3-NP) (neurotoxin) only at 20 mg/kg body weight, group C were given only Garcinia kola extracts, and group D were pre-treated with Garcinia kola extracts at 200 mg/kg for seven days prior to administration of neurotoxin at 20 mg/kg body weight. After three days of neurotoxins administration in the relevant groups, the brains were excised and fixed in formal calcium for histological processing., Results: The study showed that hippocampal and cerebellar neurons of animals in group B exhibited some cellular degeneration and blood vessel blockage, which were not seen in groups A, C and D. Cresyl violet staining was least intense in group B than in groups A, C and D. Despite the fact that animals in group D has equal administration of 3-Nitropropionic acid concentration, there were no traces of neural degeneration as it was evidenced in group B., Conclusions: It is concluded that Garcinia kola has protective effects on the neurons of the hippocampus and cerebellum of malnourished mice.

Problems associated with current treatment regimens have generated a considerable interest in alternative approaches for the eradication of Helicobacter pylori infections using phytochemical compounds. In an attempt to identify potential sources of such compounds, the antimicrobial activity of five solvent extracts of Garcinia kola seeds were investigated against 30 clinical strains of H. pylori and a standard control strain, NCTC 11638, using standard microbiological techniques. Metronidazole and amoxicillin were included in these experiments as positive control antibiotics. All the extracts tested exhibited anti-H. pylori activity with zone diameters of inhibition between 0 and 25 mm. The ethanol extract demonstrated considerable anti-H. pylori activity with a percentage susceptibility of 53.3% and minimum inhibitory concentration for 50% susceptibility (MIC₅₀) values ranging from 0.63 to 5.0 mg/mL. Ranges of MIC₅₀ values for amoxicillin and metronidazole were 0.01-0.63 mg/mL and 0.04-5.0 mg/mL, respectively. The inhibitory activity of the ethanol extract was similar to that of metronidazole (P > .05) as opposed to amoxicillin (P < .05). The extract caused a 12-hour extension of the lag phase of H. pylori at 1.25 mg/mL. The same observations were recorded when this concentration was doubled and quadrupled alongside a killing rate of 80.1% and 93.7%, respectively, after 24 hours and of 100% after 30 hours. These results demonstrate that the ethanol extract of G. kola may contain therapeutically useful compounds against H. pylori.

Anti-ulcer potential and proton pump inhibitory activity of kolaviron (KV) isolated from Garcinia kola Heckel has been evaluated using different ulcer models. Cold-restraint (CRU), aspirin (ASP), alcohol (AL), pyloric ligation (PL) induced gastric ulcer models were used to assess anti-ulcerogenic activity of KV in rats. Effects of KV on gastric juice for free and total acidity, peptic activity and mucin secretion were also evaluated. The H+, K+-ATPase activity was assayed in gastric microsomes, spectrophotometrically. Results of this study showed that KV (200 mg/kg) reduced the incidence of ulcers in CRU (69.0%), PL (67.6%), ASP (68.6%) and AL (51.5%). Reductions were also observed in free acidity (32.6%), total acidity (56.2%) and peptic activity (35.4%) with increase in mucin secretion by 40.1%. KV inhibited the H+,K+-ATPase activity with IC50 of 43.8 microg/ml compared with omeprazole with IC50 of 32.3 microg/ml. KV showed both cytoprotective and anti-secretory potentials against peptic ulcer models, and a proton pump inhibitory activity. KV may emerge as a potent anti-ulcer compound.

We assessed the anti-Listerial activities of crude n-hexane and aqueous extracts of Garcinia kola seeds against a panel of 42 Listeria isolates previously isolated from wastewater effluents in the Eastern Cape Province of South Africa and belonging to Listeria monocytogenes, Listeria grayi and Listeria ivanovii species. The n-hexane fraction was active against 45% of the test bacteria with zones of inhibition ranging between 8-17 mm, while the aqueous fraction was active against 29% with zones of inhibition ranging between 8-11 mm. The minimum inhibitory concentrations (MIC) were within the ranges of 0.079-0.625 mg/mL for the n-hexane extract and 10 to >10 mg/mL for the aqueous extract. The rate of kill experiment carried out for the n-hexane extract only, revealed complete elimination of the initial bacterial population for L. grayi (LAL 15) at 3× and 4× MIC after 90 and 60 min; L. monocytogenes (LAL 8) at 3× and 4× MIC after 60 and 15 min; L. ivanovii (LEL 18) at 3× and 4× MIC after 120 and 15 min; L. ivanovii (LEL 30) at 2, 3 and 4× MIC values after 105, 90 and 15 min exposure time respectively. The rate of kill activities were time- and concentration-dependant and the extract proved to be bactericidal as it achieved a more than 3log(10) decrease in viable cell counts after 2 h exposure time for all of the four test organisms at 3× and 4× MIC values. The results therefore show the potential presence of anti-Listerial compounds in Garcinia kola seeds that can be exploited in effective anti-Listerial chemotherapy.

The protective effect of Garcinia kola (GK) crude extract on acetic acid induced colitis in rats was investigated. Colitis, a form of inflammatory bowel disease (IBD) is characterized by inflammation of colon. The pathology in colitis includes disruption of crypt architecture, inflammation of crypts, frank crypt abscesses, and hemorrhage or inflammatory cells in the lamina propria. Since oxidative stress plays an important role in the etiology of Inflammatory Bowel diseases,and Garcinia kola (GK), have been shown to reduce oxidative stress in the rat stomach.The present study was designed to investigate the effects of Garcinia kola on ulcerative colitis (UC) induced by acetic acid. Albino rats were divided into five groups; Group one served as control, group two received Normal saline, group three received 2.5% ethanol while groups four and five were given 20mg/kg and 100mg/kg of crude extract of Garcinia kolarespectively. In another experiment, rats were fed for 2 weeks on normal rat diets but specially composed to contain 12.5%, 25% and 50% by weight of G kola. Colitis was induced by intra-rectal administration of 6% acetic acid. The colonic damage was elucidated by macroscopic damage scores; colon wet weight, stool consistency and colonic edema (thickness of the colon). Intra-luminal administration of 6% acetic acid resulted in observable clinical and macroscopic signs of colitis.Pre-orally administered of crude extract of GK significantly reduced the colonic damage score (p<0.001), colon weight (p<0.001), thickness of the colon (p<0.001) and diarrhea (p<0.001).Histological examinations also indicated a marked reduction in tissue injury and inhibition in neutrophil infiltration in rats pretreated with crude extract of Garcinia kola. Results of this investigation provide experimental evidence of Garcinia kola as an anti-colitis agent.

Kolaviron (KV), a biflavonoid fraction from the seeds of Garcinia kola has been shown to posess antiinflammatory properties in animal models of inflammation. In this study, the effect of KV on carrageenan-induced paw edema was investigated in mice. Furthermore, the effects of KV on the production of the pro-inflammatory mediators- nitric oxide (NO) and tumor necrosis factor alpha (TNF-alpha) were examined in an activated macrophage-like cell lines, RAW 264.7 cells. Administration of KV prior to injection of carrageenan significantly reduced the paw inflammation in a dose-dependent manner. KV consistently inhibited in-vitro production of NO and secretion of TNF-alpha in a dose-dependent manner. In addition, KV reduced the production of PGE2 in LPS-stimulated macrophages. Viability of cells at all concentrations studied was unaffected as determined MTT [3-(4,5- dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide] cytotoxicity assay. These results suggest that KV has inhibitory effects on LPS-induced TNF-alpha, NO and PGE2 production.

The biflavonoid, 3'',4',4''',5,5'',7,7''-heptahydroxy-3,8-biflavanone, known as GB1 (1), was isolated as a major constituent from Garcinia kola stem bark. GB1 (1) exhibited alpha-glucosidase and aromatase inhibitory activities, as well as antiplasmodial activity, but was not toxic against cell lines tested. GB1 (1) may be a potential dietary supplement or phytomedicine for the prevention of breast cancer and type 2 diabetes mellitus., (Georg Thieme Verlag KG Stuttgart-New York.)