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This study investigated the effect of African peach (AP) and Uvaria afzelii (UA) extracts on arginase, nitric oxide (NO), angiotensin-1 converting enzyme (ACE), and cholinergic and purinergic enzymes in platelets of complete Freund adjuvant (CFA)-induced arthritic rat model to explain a possible anti-arthritic mechanism of extracts. Sixty adult Wistar female rats (140–280 g) were divided into twelve groups (n = 5). Group I received oral administration of 0.9% NaCl; group II received 10 mg/kg of indomethacin; group III and IV rats received oral administration of 150 and 300 mg/kg of AP extract, respectively; and group V and VI rats received oral administration of 150 and 300 mg/kg of UA extract, respectively. While group VII rats were injected with 0.2 ml CFA (arthritic control rat group), in group VIII, IX, and X, arthritic rats received 10 mg/kg indomethacin, 150 and 300 mg/kg of AP extract orally, respectively, while group XI and XII arthritic rats received 150 and 300 mg/kg of UA extract, respectively. The animals were treated for 21 days. The results revealed decreased NO level, activities of arginase and ACE, and adenosine triphosphate and adenosine monophosphate hydrolyses were significantly decreased while adenosine deaminase activity was significantly decreased in arthritic rat groups administered with different doses of AP and UA extracts. Therefore, AP and UA could be a natural complement and alternative promising anti-arthritic agent.

This study was carried out to assess the in vitro antioxidant, anti-inflammatory and antidiabetic effects of Nauclea latifolia (Sm.) leaf extracts. Ethanolic (NLE) and aqueous (NLA) extract of N. latifolia leaves were prepared and assessed for their anti-inflammatory activity, antioxidant potential, α-amylase and α-glucosidase inhibitory activities, and the mechanism of enzyme inhibition in vitro using standard established methods. From the results, phytochemicals such as flavonoids, phenolics, glycosides, and tannins were detected in both extracts of N. latifolia with NLE having a significantly (p<0.05) higher phytochemical content. NLE displayed significantly (p<0.05) better total antioxidant capacity, reducing power, 2,2-diphenyl-2-picrylhydrazyl, and hydrogen peroxide radical scavenging activities. For anti-inflammatory activities, 70.54±2.45% albumin denaturation inhibition was observed for NLE while 68.05±1.03% was recorded for NLA. Likewise, 16.07±1.60 and 14.08±1.76% were obtained against hypotonic solution and heat-induced erythrocyte haemolysis, respectively, for NLE while 20.59±4.60 and 24.07±1.60% were respective NLA values. NLE (IC50: 4.20±0.18 and 1.19±0.11 mg/mL) and NLA (IC50: 11.21±0.35 and 2.64±0.48 mg/mL) α-glucosidase and α-amylase inhibitory activities were dose-dependent with uncompetitive and competitive inhibition elicited, respectively, by the extracts. A significant positive association (p<0.01 and 0.05) was identified between antioxidant activity and carbohydrate-metabolising enzyme inhibitory activity. The obtained result suggests N. latifolia leaf could serve as an alternative candidate for managing diabetes mellitus due to its antioxidant and anti-inflammatory association with diabetes-linked enzymes.

Objective: To explore the immunomodulatory, anti-inflammatory, anti-oxidant and anti-arthritic activity of aqueous and methanolic extracts of Nauclea pobeguinii stem bark. Methods: For in vitro assays, the production of reactive oxygen species (chemiluminescence technique), the proliferation of T cells (liquid scintillation counter method), as well as the inhibition of cyclooxygenase, lipoxygenase, protein denaturation, and free radicals [DPPH, ABTS and nitric oxide (NO) inhibition methods] were evaluated. For in vivo assays, a polyarthritis model was induced by complete Freund’s adjuvant in rats. The aqueous and methanolic extracts of Nauclea pobeguinii stem bark were administered orally at 150 and 300 mg/kg. After 28 days of treatment, the total blood was taken to quantify the hematological parameters and the serum was used to evaluate the biochemical parameters (alanine aminotransferase, aspartate transaminase, phenylalnine ammonialyase, and proteins) and oxidative stress parameters (malondialdehyde, catalase, superoxide dismutase, glutathione and NO), and then the knee joint was removed for histological analysis. Results: The extracts of Nauclea pobeguinii significantly reduced the production of intra- and extracellular reactive oxygen species and decreased T cell proliferation. They had an inhibitory effect on cyclooxygenase, lipoxygenase, and protein denaturation, and both extracts had antioxidant capacity on DPPH, ABTS and NO. Both extracts alleviated joint inflammation and pain sensitivity after complete Freund’s adjuvant injection, reduced alanine aminotransferase, aspartate transaminase, alkaline phosphatase, NO and malondialdehyde levels, increased protein concentration, superoxide dismutase, catalase and glutathione activity, and restored the cytoarchitecture of the joint after complete Freund’s adjuvant injection. Conclusions: The aqueous and methanolic extracts of Nauclea pobeguinii have immunomodulatory, anti-inflammatory, anti-oxidant and anti-arthritic properties.

Liver and kidney diseases are becoming order of the day in both developed and developing countries as a result of environmental pollutants such as lead. Restorative activities of methanol and methanol/acetone phenolic-rich extracts (MPR and MAPR, respectively) of theN. latifoliafruit (NLF) on lead acetate-induced liver and kidney damaged were assessed in Wistar rats. The antioxidant activities of both phenolic-rich extracts of NLF were also carried out using standard methods. Seven groups of Wistar rats comprising of 5 rats each were used for the study and 1000 mg/kg body weight (bw.) of lead acetate solution was administered orally to the 6 groups of animals to induce liver and kidney damage. The high and low dosages of 300 and of 150 mg/kg body weight (bw.) of both MPR and MAPR were administered orally to four groups for 14 days along positive (100 mg/kg bw. of silymarin), negative (treated with the placebo) and naïve control (non-induced). The percentage DPPH radical scavenging activities, ferric reducing antioxidant power and percentage inhibition of lipid peroxidation show high antioxidants activities dose-dependently. Furthermore, administration of lead acetate significantly (p > 0.05) reduces the weight gain and elevates the liver and kidney relative weight as well as their respective damage biomarkers with distortions in their histologies. However, treatment with MPR and MAPR resulted in significant (p p N. latifoliafruit can be exploited further for drug development for the management kidney and liver damage arise from lead-induced toxicity.

Background Proprotein convertase subtilisin/kexin type 9 (PCSK9) has been found to play a major role in atherosclerotic cardiovascular disease (ASCVD) by promoting hyperlipidemia. Its inhibition has therefore emerged as a viable drug target for improving the outcome of ASCVD. However, current monoclonal antibody PCSK9 inhibitors are considered cost ineffective and there is the need to discover new effective and cheaper small molecule alternatives. Purpose The methanolic and ethanolic crude extracts of Nauclea latifolia have been shown to possess anti-hyperlipidemic activity, but the chemical component(s) responsible for this activity and the mechanism of action have remained unknown. The objective of this study was therefore to identify N. latifolia constituents with anti-hyperlipidemic activity and to investigate the inhibition of PCSK9 as a probable mechanism of action. Method In the present study, compounds were isolated from the ethanolic extract of the stem of N. latifolia. The alkaloids were evaluated for their DiI-LDL uptake promoting activity in HepG2 cell. The most active compound was further assessed for its effect on low density lipoprotein receptor (LDLR) and PCSK9 protein expressions by western blot. Results 3R-3,14-dihydroangustoline (5), showed a relatively good activity in promoting LDL uptake (1.26-fold). It further increased LDLR protein expression and decreased the protein expression of PCSK9 in a dose dependent manner (1–50 µM). Conclusion Alkaloids from N. latifolia may serve as a source of new PCSK9 inhibitors.

The greatest common and devastating complication of diabetes is painful neuropathy that can cause hyperalgesia and allodynia. It can disturb psychosocial functioning by increasing levels of anxiety and depression. This work was designed to evaluate the antihyperalgesic, antidepressant, and anxiolytic-like effects of the aqueous and methanol extracts of Nauclea pobeguinii stem-bark in diabetic neuropathy induced by streptozotocin in mice. Diabetic neuropathy was induced in mice by the intraperitoneal administration of 200 mg/kg streptozotocin (STZ) to provoke hyperglycemia. Nauclea pobeguinii aqueous and methanol extracts at the doses of 150 and 300 mg/kg were administered by oral route, and their effects were evaluated on antihyperalgesic activity (Von Frey filaments, hot plate, acetone, and formalin tests), blood glucose levels, body weight, serum, sciatic nerve proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and sciatic nerve growth factor (IGF and NGF) rates, depression (open field test, forced swimming test, tail suspension test), and anxiety (elevated plus maze, light-dark box test, social interaction). Oral administration of Nauclea pobeguinii stem-bark aqueous and methanol extracts (150 and 300 mg/kg) produced antihyperalgesic, antidepressant, and anxiolytic-like effects in STZ-induced diabetic neuropathic mice. Extracts also triggered a decrease in glycaemia and increased body weight in treated animals. They also significantly ( p p

Ethnopharmacological relevance Cameroonian medicinal plants are traditionally used to treat many ailments, including cancer and related diseases. Cancer is characterized as a condition with complex signs and symptoms. It has been recommended that ethnopharmacological usages such as immune and skin disorders, inflammatory, infectious, parasitic and viral diseases should be taken into account when selecting plants for anticancer screenings, since these reflect disease states bearing relevance to cancer or cancer-like symptoms. Aim of the study The present study aims at investigating 20 methanol extracts from 15 Cameroonian medicinal plants on a panel of human cancer cell lines, including various drug-resistant phenotypes. Possible modes of action of the of the most active plant were analyzed. Materials and methods Methanol extracts from different plant parts (leaves, bark, roots, fruits or whole plant) were evaluated for their cytotoxicity using resazurin reduction assay on a panel of nine sensitive and multi-drug resistant (MDR) cancer cell lines. Cell cycle, apoptosis, mitochondrial membrane potential (MMP), and reactive oxygen species (ROS) were measured by flow cytometry. Results Prescreening of extracts at 80 µg/mL showed that 6 extracts out of 20 inhibited more than 50% proliferation of leukemia CCRF-CEM cells; these include extracts from Anthocleista schweinfurthii fruits (ASF; 48.28%), Morus mesozygia bark (MMB; 42.76%), Nauclea latifolia bark (NLB; 38.75%), Tridesmostemon omphalocarpoides bark (TOB; 38.53%), Nauclea latifolia leaves (NLL; 35.17%) and Erythrina sigmoidea bark (ESB; 33.77%). Subsequent investigations revealed IC50 values below or around 20 µg/mL for extracts from MMB, NLB, NLL and ESB towards sensitive CCRF-CEM cells and its resistant P-glycoprotein over-expressing subline CEM/ADR5000. The best extract, ESB also displayed IC50 values below 20 µg/mL colon carcinoma HCT116 (p53+/+) cells with an IC50 value of 19.63 µg/mL and it resistant p53 knockout subline HCT116 (p53−/−) with an IC50 value of 16.22 µg/mL. Conclusion Erythrina sigmoidea, Anthocleista schweinfurthii, Morus mesozygia, Nauclea latifolia, Tridesmostemon omphalocarpoides used in African traditional medicine are good cytotoxic plants that can be exploited to develop phytomedicine to fight cancers including MDR phenotypes.

The prophylactic effect of ethanolic leaf extract of Nauclea latifolia, widely used in herbal malarial treatment, was compared against standard drug Coartem® (Artemether/Lumefantrine) in Plasmodium-infected mice was investigated, and thereafter analysed for organosomatic index, parasitemia, histomorphological and immunohistochemical changes in the hippocampus. Twenty male mice about 6 to 8 weeks weighing 20 to 24 g were alloted into four groups of five mice each. Group 1 served as control received placebo; group 2 received extract 500 mg/kg; group 3 received extract 1000 mg/kg; and group 4 received 5 mg/kg of Artemether/Lumefantrine. Extract and drug administrations were performed for 3 days, and thereafter mice were infected with 106 of Plasmodium berghei parasites, and monitored for 4 days, after which the experiment was terminated. Thick blood smear were prepared from lateral tail vein, then under anesthesia via a cocktail of xylaxine and ketamine, intracardiac perfusion was performed first with phosphate buffered saline to clear systemic blood, and then 4% paraformaldehyde to fixed brain for routine histology and immunohistochemistry. Result indicates organosomatic index was not statistically significant, parasitemia in the treated groups were significantly (p

This study is aimed at determining the efficacy of some of the claims and to evaluate the hypocholesterolemic properties of N. latifolia in comparison with metformin in diabetic Albino rats. The objectives are to evaluate the phytochemistry and the effect of N. latifolia on lipid profile in alloxan induced diabetes in comparism with metformin as drug control. Thirty male albino Wister rats weighing 60g-90g were used. The rats were divided into six groups of five animals each. Group 1(normal control, group 2 (-ve control), group 3 (+ve control), group 4, 5 and 6 were given 10%, 30% and 60% of the fruit as feed supplement as treatment. The abnormal lipid profiles and lipoprotein oxidation especially, Low density lipoprotein cholesterol is more common in diabetics and is aggravated with poor glycaemia control. In this study, hypoglycemic and hypocholesterolemic properties of Nauclea latifolia fruits were investigated. Fruit sample was administered on percentage basis to alloxan - induced diabetic rats once daily for a period of twenty one days. Their blood glucose level was measured every three days while Lipid profile was assayed at the end of the experiment. The fruit sample significantly reduced (p

The antidiabetic effects of methanol, N-hexane and ethyl acetate leaf fractions of Nauclea latifolia were investigated in diabetic model rats. 150 and 300mg/kg fractions of N. latifolia were administered orally to the experimental animals at two weeks interval, while their blood glucose levels were taken daily. At the end of the experiment, their lipid profiles were assayed using standard methods. The research data indicated significant decreases (P=0.05) of the blood glucose in all the fractions at a dose-dependent manner (ethyl acetate (150 mg/kg = 47.83%; 300 mg/kg = 64.17%), N-hexane (150 mg/kg = 58.45%; 300 mg/kg = 64.18%), methanol (150 mg/kg = 44.5%), except for the 300 mg/kg dose methanol fraction (0.82%) as compared to the increased level in the negative control (33.33%). In the lipid profile assay, there were also a dose dependent significant decrease (P=0.05) of serum Total Cholesterol (TC) and Low Density Lipoprotein (LDL) cholesterol in all the fraction groups (ethylacetate (150 mg/kg- TC = 69.88 ± 8.52 mg/dl, LDL-cholesterol = 8.23±7.76 mg/dl; 300 mg/kg-TC = 51.08±9.93 mg/dl, LDL-cholesterol = 6.44±7.66 mg/dl), N-hexane (150 mg/kg-TC = 73.16 ± 18.62mg/dl, LDL-cholesterol = 33.24±16.19 mg/dl; 300 mg/kg-TC = 69.78±8.41 mg/dl, LDL-cholesterol = 9.29±5.62 mg/dl and methanol (150 mg/kg; TC = 116.86 ± 13.34 mg/dl, LDL-cholesterol = 50.68±14.13 mg; 300 mg/kg-TC = 108.66 ± 12.77 mg/dl, LDL-cholesterol = 42.09±9.93mg/dl) as compared to the high concentration of the negative control group (TC = 383.76 ± 79.68 mg/dl, LDL-cholesterol = 299.46 ± 79.23 mg/dl). Ethylacetate and N-hexane fractions showed significant reductions (P=0.05) of TC and LDL-cholesterol as compared to the positive control (TC=116.36±14.69 mg/dl, LDL-cholesterol = 32.06±13.23mg/dl) also at a dose-dependent manner; thus, portraying a more efficient hypolipidaemic activity than the standard drug. This antidiabetic research on N. latifolia suggest that ethylacetate fraction produces the best effect, followed by N-hexane and lastly by methanol fraction. Key words: Nauclea latifolia, ethyl acetate, n-hexane, methanol, leaf fractions, glibenclamide, antidiabetic, blood glucose, lipid profile.

Some herbal antiplasmodial plants have not been investigated for their hepatotoxic and glycogen lowering effects in experimental malaria models. We investigated the histochemical and immunohistochemical effects of ethanolic leaves extract of Nauclea latifolia (NL) an antiplasmodial plant on the liver of experimental prophylactic malaria mice. Twenty (20) mice (20-24 g) were grouped after acclimatization as follows: group A administered normal saline for 3 days, then inoculated with Plasmodium berghei (Pb); group B received 500 mg per kg body weight extract for 3 days then infected with Pb; group C received 1000 mg per weight extract for 3 days then infected with Pb; group D received 5 mg per kg body weight Artemether/lumefantrine (AL) for 3 days then infected with Pb. Extracts and drug were administered orally via oro-gavage needle. Inoculums of Pb at 1x106 were injected intraperitoneally and were subsequently monitored for 72 hrs, then fasted over night, and humanely sacrificed with liver tissues excised and processed for light microscopy. Result of routine hematoxylin and eosin stain in Figure 1 revealed that group A had the most heptocellular distortions and inflammation with prominent hyperplasia compared to extract and drug treated groups (groups B - D); in figure 2 periodic acid-Schiff (PAS) showed that group A had moderate PAS expression of glycogen stores; extract groups had depleted glycogen stores compared to group D – the AL group had more glycogen stores. In figure 3 the cytokeratin-7 showed that groups A - C had moderate positivity, while group D was mild/lower. In conclusion NL ethanolic leaf extract is moderately hepatoprotective in a dose dependent manner, but decreased periodic acid-Schiff (PAS) expression of glycogen granules and moderately up-regulated cytokeratin-7 in experimental prophylaxis malaria mice.

Three previously undescribed indole alkaloids, named latifolianine A (1) and latifoliaindoles A and B (2 and 3), along with 10 known compounds (4-13), were isolated from the heartwood of Nauclea latifolia. Their structures were elucidated based on the analysis of their NMR and MS data. Latifolianine A (1) represents an unusual and unprecedented monoterpene indole alkaloid unit condensed with an ursane-type pentacyclic triterpenoid moiety. Plausible biogenetic routes toward latifolianine A (1) and latifoliaindoles A and B (2 and 3) were proposed. All the isolates were assessed in vitro for their inhibitory effects on Haemophilus influenzae. Naucleidinal (7) exhibited potent antibacterial activity (MIC value of 3.1 mug/mL) as compared to a reference drug, ciprofloxacin (MIC value of 1.6 mug/mL).

Lead toxicity is a worldwide problem that needs to be ameliorated with harmless or less toxic medications contrary to available drugs. As such, ameliorated effects of methanol and methanol/acetone phenolic-rich extracts of N. latifolia fruit (NLF) was assessed on haematological parameters and lung histology of lead acetate induced toxicity rats after acute toxicological study and phenolics analysis of the extracts. Seven groups of Wistar rats comprising of 5 rats each were used for the study. Dosages of 150 mg/kg and 300 mg/kg body weight (bw.) of both extracts NLF were administered orally to four of the groups while two groups were administered 100 mg/kg bw. of silymarin and 2 mL/kg bw. of normal saline (Untreated) followed with control group for 14 days. Phenolics contents (mg/g) of both extracts showed the following order; tannins < flavonoids < total phenols (9.29 < 10.02 < 23.82) and (10.72 < 18.09 < 61.39) for both methanol and methanol/acetone phenolic-rich extracts of NLF respectively with LD50 > 2000 mg/kg bw. Significant depression of PCV, RBC, MCHC, HB, MCV, MCH, platelet counts, neutrophils and lymphocytes counts with elevation of WBC were observed in untreated group when compared with non-toxic control group. The administration of both extracts of NLF at 150 and 300 mg/kg bw. were capable of reverting the haematological changes in lead acetate induced toxicity rats with minimal injury to the lung tissues. Therefore, methanol and methanol/acetone phenolic-rich extracts of NLF can restore haematological abnormalities as well as sustain the integrity of the lung tissues of the experimental rats. Hence, phenolics content of N. latifolia fruit can be exploited further for drug development for the management of lead toxicity.

Acanthospermum hispidum, Alchornea laxiflora, Calyptrochilum christyanum, Heliotropicum indicum, Holarrhena floribunda, Ipomoea asarifolia, Nauclea diderrichii, Piper guineense, and Tetracera scandens were extracted into methanol and screened for the availability of alpha-amylase inhibitors. Plant extracts’ toxicity was determined by brine shrimp lethality assay (BSLA). The most active plant, Nauclea diderichii, was fractionated into four solvent systems (n-hexane fractions, ethyl acetate, dichloromethane, and n-butanol) and tested. All the extracts showed varying degrees of alpha-amylase inhibitory activity. N. diderrichii with IC50 = 248.30 ± 0.27 µg.mL–1 had the highest inhibitory activity, while its butanol fraction with IC50 = 137.8 µg.mL–1 had activity comparable to the standard α-amylase inhibitor acarbose (IC50 = 177.50 ± 0.42 µg.mL–1). LC50 values for BSLA ranged from 11.35 to 1,127.50 µg.mL–1, with T. scandens being the most toxic with 11.35 µg.mL–1 and N. diderrichii the least toxic wit...

Objective: To assess the effects of hot water leaf extract of Nauclea latifolia (N. latifolia) on antioxidant status, lipid peroxidation values and parasite levels in hepatic and brain tissue of experimental mice (BALB/c) infected with Plasmodium berghei (P. berghei) malaria. Methods: Forty nine mice were divided into seven groups (n = 7) and used for the study. Group A (control) were given 0.2 mL/kg phosphate buffer saline; Group B mice were infected with P. berghei and treated with phosphate buffer saline. Groups C and D mice were also infected but treated with 200 and 300 mg/kg body weight of leaf extract respectively. Groups E and F mice were not infected, but received 200 and 300 mg/kg of leaf extract respectively. Group G mice were infected and treated with chloroquine (5 mg/kg). Liver and brain tissues of mice were prepared for both biochemical assay and microscopic examination. Results: Results showed that P. berghei malaria infection induced oxidative stress in both liver and brain tissues as evidenced by the significant (P

Nauclea latifolia is used in traditional medicine for the treatment of male reproductive diseases. Despite its vast uses, its effects on the male reproductive system have not been scientifically proven. This study aimed to investigate the effects of Nauclea latifolia root decoction on sexual behavior and functions in male rabbits. Twenty-four male rabbits were divided into four groups: The first group received daily distilled water orally. The second, third, and fourth groups were orally treated with 100, 200, and 400 mg/kg body weight of Nuclea latifolia root, respectively. Sexual behavior parameters were carried out on weeks 1, 2, and 3 of the study. Testosterone, follicle-stimulating hormone (FSH), and luteinizing hormone (LH) were measured from the serum, while the testes tissue samples were used for antioxidant and histopathological examinations. Treatment with 200 and 400 mg/kg body weight resulted in significantly (p.05) increased frequencies of mounting and intromission. In addition, the ejaculation latency was significantly prolonged (p.05). The latencies of mounting and intromission were significantly decreased (p.05), whereas ejaculation frequency increased. Serum testosterone, FSH, and LH increased significantly (p.05) after treatment with Nuclea latifolia. There was an increase in epididymal sperm counts at 200 and 400 mg/kg body weight doses compared to the control. The extract also increased sperm motility and viability and improved testicular oxidative status. Histological examination revealed an increase in germinal layer thickness. The present study suggests that treatment with N. latifolia improves male sexual function and fertility and protects the testes from oxidative damage.

Ethnopharmacoalogical relevance The genus Nauclea in Africa comprises seven species. Among them, N. latifolia , N. diderrichii and N. pobeguinii are widely used by the local population in traditional remedies. Preparation from various parts of plants (e.g. roots, bark, leaves) are indicated by traditional healers for a wide range of diseases including malaria, pain, digestive ailments or metabolic diseases. Materials and methods A literature search was conducted on African species of the genus Nauclea using scientific databases such as Google Scholar, Pubmed or SciFinder. Every document of ethnopharmacological, phytochemical or pharmacological relevance and written in English or French were analyzed. Results and discussion The Nauclea genus is used as ethnomedicine all along sub-Saharan Africa. Several local populations consider Nauclea species as a major source of remedies for malaria. In this regard, two improved traditional medicines are currently under development using extracts from N. latifolia and N. pobeguinii . Concerning the chemical composition of the Nauclea genus, indoloquinolizidines alkaloids could be considered as the major class of compounds as they are reported in every analyzed Nauclea species, with numerous structures identified. Based on traditional indications a considerable amount of pharmacological studies were conducted to ensure activity and attempt to link them to the presence of particular compounds in plant extracts. Conclusion Many experimental studies using plant extracts of the African species of the genus Nauclea validate traditional indications (e.g. malaria and pain). However, bioactive compounds are rarely identified and therefore, there is a clear need for further evaluations as well as for toxicity experiments. The sustainability of these plants, especially of N. diderrichii , a threatened species, should be kept in mind to adapt local uses and preparation modes of traditional remedies.

Sacrocephalus latifolius (Sm.) Bruce (Rubiaceae) formerly known as Nauclea latifolia (Sm.), is a highly valued medicinal plant used in ethnomedicine in the treatment of various infectious diseases due to its insecticidal and antiparasitic properties. The proximate, mineral composition and antimicrobial properties of the leaves were analyzed with a view to evaluate its nutritional and medicinal potentials. The proximate analysis revealed that the moisture content, ash, lipid, crude fibre, crude protein and the carbohydrate content of the leaves were 56.36 ± 0.50, 5.93 ± 0.2, 0.28 ± 0.50, 4.48 ± 0.20, 6.55 ± 0.10 and 3.21 ± 0.30%, respectively. Mineral compositions of the leaves showed that the vitamins content, potassium, calcium, iron and zinc content of the leaves were 3.41 + 0.30, 1.52 + 0.20, 2.28 + 0.30, 3.51 + 0.20 and 2.71 + 0.20%, respectively. The phytochemical screening revealed the presence of glycosides, alkaloids, flavonoids, tannins, triterpenoids and saponins in the methanolic extracts of the sample. Aqueous, choloroform and methanol extracts exhibited broad spectrum activity against Staphyococcus aureus and Escherichia coli by using disc diffusion method. The results indicate that S. latifolius contains substantial amounts of organic constituents and minerals, suggesting its potential for nutrient composition. As such, the results of phytochemical screening could justify observed antimicrobial herbal medicine. Key words: Sacrocephalus latifolius, nutrients, ethnomedicine, Antimicrobial, phytochemicals.

Various combinations of Nauclea latifolia root, Artocarpus altilis stem bark, Murraya koenigii leaf and Enantia chlorantha stem bark used in African ethnomedicine as decoctions for malaria and fevers, and combinations with standard drugs, were investigated for antiplasmodial activities using Plasmodium berghei berghei-infected mice. The respective prophylactic and curative ED50 values of 189.4 and 174.5 mg/kg for N. latifolia and chemosuppressive ED50 value of 227.2 mg/kg for A. altilis showed that they were the best antimalarial herbal drugs. A 1.6-fold increase of the survival time given by the negative control was elicited by M. koenigii, thereby confirming its curative activity. Pyrimethamine with an ED50 of 0.5 ± 0.1 mg/kg for the prophylactic, and chloroquine with ED50 = 2.2 ± 0.1 and 2.2 ± 0.0 mg/kg for the chemosuppressive and curative tests, respectively, were significantly (p < 0.05) more active. Co-administrations of N. latifolia with the standard drugs significantly reduced their prophylactic, chemosuppressive and curative actions, possibly increasing the parasites’ resistance. Binary combinations of N. latifolia or M. koenigii with any of the other plants significantly increased the prophylactic and suppressive activities of their individual plants, respectively. Also, E. chlorantha with A. altilis or N. latifolia enhanced their respective prophylactic or curative activities, making these combinations most beneficial against malaria infections. Combinations of three and four extracts gave varied activities. Hence, the results justified the combinations of ethnomedicinal plants in antimalarial herbal remedies and showed the importance of the three in vivo models in establishing antimalarial activity.

This study was aimed at evaluating the acute and subchronc toxicities of aqueous extracts of Newbouldia laevis stem bark and Nauclea latifolia roots, used extensively, in Nigerian herbal medicine. Acute toxicity study was carried out on Swiss albino mice. The extracts mixed (1:1) in the doses ranging between 1.0 g to 20.0 g/kg body weight (bwt) were administered orally to the mice (22.52.5 g) and observed continuously for the first 4 h and hourly for the next 12 h, then 6 hourly for 56 h. In subchronic toxicity study, wistar rats (15020 g) were fed with 100, 250 and 500 mg/kg bwt daily of the extract mixture (1:1) combination and 500 mg/kg bwt dose of the respective extracts for 30 days. The effects on the biochemical and haematological parameters were evaluated and also the effects on some vital organs were histologically examined. The results showed that all the animals that received 20 g/kg bwt of the extracts (1:1) combination survived beyond 24 h. Significant (p

Sarcocephalus latifolius (Synonym, Nauclea latifolia) is a shrub commonly seen in the South East of Nigeria. It is widely applied as herbal remedy in the treatment of various illnesses. The effect of ethanol extract of the root of the plant on some serum electrolytes was studied. A total of thirty Wistar albino rats were used to determine serum concentrations of K+, Ca2+, Cl- and HCO3-. The animals were divided into six groups of five rats each. Five groups labeled A, B, C, D and E, were administered orally with graded doses of root extract of Sarcocephalus latifolius at concentration of 300, 350, 400, 450 and 500 mg kg(-1) body weight, respectively. The sixth group (Group F) was used as the control and its animals were simply sustained on normal diet and water. Administration of the extract lasted for twenty-one days after which the animals were sacrificed by cardiac puncture. K+, Ca2+, Cl- and HCO3- were determined from each sample and the mean concentration was calculated for each dose and the control. Potassium, calcium and chloride determination were done by colorimetric methods while determination of bicarbonate concentration was done by simple titration. Na+ was separately assayed, by flame photometer, from a set of 18 rats of six animals in each of three groups. For K+, non dose dependent increases were observed which was non-significant (p0.05), for A, D and E but significant (p0.05) for B and C. Ca2+ showed a dose dependent and significant (p0.05) decreases, except for A (p0.05). Decreases (p0.05) for C, D, E and (p0.05) for A and B were observed for Cl-. Serum bicarbonate appeared almost completely unaffected by the extract, showing no significant changes. Na+ levels were depressed for the two test groups, A and B compared with the control (group C), with test group B showing a significant decrease (p0.05). From the analysis, it could be concluded that Sarcocephalus latifolius has the capacity to influence various electrolytes to physiologically important degrees. Significant reductions in sodium and calcium levels indicate the usefulness of the plant in treatment of hypertension and pain/fever, respectively. However, significant reductions in chloride may negatively affect the normal balance of fluid in the body. Therefore, more scientific research is needed to establish the best approach to optimizing the numerous medicinal potentials of the plant.

International audience; Today, ethno-pharmacology is a very important resource in order to discover new therapies for the current diseases. Moreover, another good justification for the ethno-pharmacological approach is to obtain new, effective, less expensive and simple therapies, limiting at the same time the cost of pharmaceutical research. Two major anti-malarial drugs widely used today, i.e. quinine and artemisinin, came respectively from Peruvian and Chinese ancestral treatments reported in the traditional medicines. In this contest, there is an urgent need for the discovery of new drugs, due to the critical epidemiological situation of this disease and to the growth of resistances. In Mali, malaria and liver diseases remain one of the leading public health problems. Many medicinal plants are often used, in local traditional medicine, for the treatment at the same time of malaria and liver diseases, including hepatic syndromes, jaundice, hepatitis and other hepatic disorders. Moreover, in the local language Bamanan, the word "Sumaya" is used both for malaria and some liver diseases. In addition, we noted that some of the improved traditional phytomedicines produced by the Department of Traditional Medicine are prescribed by modem doctors both for malaria and liver diseases. In this review, pharmacological, toxicological and phytochemical data on Argemone mexicana L. (Papaveraceae), Cochlospermum tinctorium Pen. ex A. Rich (Cochlospermaceae), Combretum micranthum G.Don (Combretaceae), Entada africana Guillet Pen. (Mimosaceae), Erythrina senegalensis A. DC (Fabaceae), Mitragyna inermis (Willd) Kuntze (Rubiaceae), Nauclea latifolia Smith syn. Sarcocephalus latifolius (Smith) Bruce (Rubiaceae), Securidaca longepedunculata Fresen (Polygalaceae), Trichilia emetica Vahl. (Meliaceae), and Vernonia colorata (Willd) Drake (Asteraceae) are reported. Some of the collected data could be used to improve the actual herbal drugs and to propose new phytomedicines for the management of malaria and liver diseases.

Aim of study The ethnobotanical study surveyed the different types of medicinal plants used for the treatment of malaria in the south-western region of Nigeria. Materials and methods Information was collected by interviewing indigenous people, using a semi-structured questionnaire. Collected plant samples were identified and authenticated in Forestry Research Institute of Nigeria, Ibadan, Nigeria. Results A total of 151 respondents were interviewed of which 64% were females and 36% males. This population comprised of herbal medicine sellers (39%), traditional doctors (15%), housewives (24%) and farmers (22%). Twenty two plants species used in the treatment of malaria belonging to 18 families were identified and compiled detailing information such as common and vernacular names, parts used, methods of preparation and previous scientific reports. Of the plants identified during the survey, Azadirachta indica (12.9%), Alstonia congensis (11.9%) and Cymbopogon citratus (11.3%) showed the highest incidence of encounter whereas Nauclea latifolia recorded the lowest incidence of encounter (0.2%). The traditional usage of Persea americana and Ludwigia peruviana in the treatment of malaria is reported here for the first time. Conclusion Though a large number of traditionally used plants for the treatment of malaria were identified, scientific validation of the traditional claims of anti-malarial properties is imperative. This would establish their candidature for any possible future research for active principles and the possible development of new cheaper and more effective anti-malarial drugs, as well as in the conservation of this rich diversity of anti-malarial plants.

Ethnopharmacological relevance Resistance against antibiotics of many bacteria is accumulating. Therefore, searches for new substances with antimicrobial activity have become an urgent necessity. Medicinal plants are frequently used in popular medicine as remedies for many infectious diseases (intestinal infection, malaria, tuberculosis, etc. ). Aim of the study This study aimed to determine the in vitro antimicrobial activity of hexane, ethyl acetate and methanol extracts from different parts (leaves, stem bark, entire plant) of five different plant species against bacteria and yeast of gastrointestinal relevance. Material and methods Twenty-one extracts from all the following plants ( Albizia gummifera (leaf), Ficus exasperata (leaf and stem bark), Nauclea latifolia (leaf and stem bark), Ricinodendron heudelotii (stem bark), Senna hirsuta (entire plant) have been screened for their antimicrobial activity against eight bacteria species including Gram-positive bacteria ( Staphylococcus aureus and Bacillus cereus ), Gram-negative bacteria ( Escherichia coli , Shigella dysenteriae , Shigella flexneri , Salmonella typhi , Pseudomonas aeruginosa , and Klebsiella pneumoniae ) and one yeast species ( Candida albicans ) using agar disc-diffusion, and microbroth dilution assays. Results Results demonstrated that F. exasperata and N. latifolia were active against the whole set of tested microorganisms. The methanol extract of N. latifolia (leaf and stem bark) was the most active against against C. albicans, E. coli, S. aureus, P. aeruginosa with a minimum inhibitory concentration (MIC) of 2, 32, 64 and 64 μg/ml, respectively. The methanol extract of leaf of F. exasperata was also most active with significant inhibitory activity against E. coli, S. dysenteriae, S. Typhi and P. aeruginosa with MIC values of 128 μg/ml. Only the extract of N. latifolia (stem bark and leaf) showed anticandidal property. Conclusion The results show that these plant extracts exhibit antimicrobial activity and N. latifolia proved to be most effective as an antibacterial and antifungal.

The aim of this phase IIA clinical trial was to assess the efficacy of an 80 % ethanolic quantified extract (containing 5.6 % strictosamide as the putative active constituent) from Nauclea pobeguinii stem bark denoted as PR 259 CT1 in a small group of adult patients diagnosed with uncomplicated falciparum malaria. Results obtained from a phase I clinical trial on healthy male volunteers indicated that the oral administration during meals of two 500 mg capsules three times daily (each eight hours) during seven days was well tolerated and showed only mild and self-resolving adverse effects. This PR 259 CT1 drug regimen was obtained by mathematical conversion of animal doses obtained in several in vivo studies in mice to human equivalent doses as in falciparum malaria patients. The phase IIA study was an open cohort study in eleven appraisable adult patients suffering from proven Plasmodium falciparum malaria. The study was specifically designed to assess the efficacy of PR 259 CT1 administered with a dose regimen of two 500 mg capsules three times daily for three days, followed by outpatient treatment of one 500 mg capsule three times daily for the next four days, in order to prove that this therapeutic dose, which was calculated from animal doses, was effective to treat adult malaria patients and consequently useful for a future Phase IIB clinical trial. This study would then substitute a dose-escalating trial, which in general is used to find the appropriate dose for clinical studies. The phase IIA clinical trial was carried out according to the WHO 2003 14-day test, and the results revealed that all eleven patients were completely cleared of parasitemia and fever on days 3, 7, and 14 except for one patient, who experienced a recurrence of parasitemia at days 7 until 14. Besides this adequate clinical and parasitological response (ACPR), this trial also demonstrated that PR 259 CT1 was well tolerated with only mild and self-resolving adverse effects including fatigue and headache, which were in accordance with those found in the phase I clinical trial. Moreover, all symptoms progressively disappeared, and no symptoms were observed on day 14. Although the number of patients included in this study was rather limited, the statistical analysis nevertheless suggested the efficacy and tolerability of PR 259 CT1, which indicated that this herbal medicinal product might be considered as a putative candidate for a large scale clinical trial.

Ethnopharmacological relevance Bark extracts of Nauclea latifolia, Nauclea diderrichii, Nauclea pobeguinii and Nauclea vandergutchii are used in traditional medicine in West and South Africa for the treatment of fevers, diarrhea and malaria. Aim of the study To estimate the possible long-term toxicity and genotoxicity of plant extracts (dichloromethane, methanol, water/methanol, water) and saponins. Materials and methods The clastogenicity of plant extracts and saponins was assessed by the micronucleus assay performed on Chinese Hamster Ovary cells. The DNA-damaging activity of saponin mixture was assessed by the comet assay on Chinese Hamster ovary cells. Results Hydromethanolic extracts from Nauclea latifolia, Nauclea diderrichii and Nauclea pobeguinii exhibited a significant clastogenic/aneugenic activity without S9 mix. The hydromethanolic extract from Nauclea diderrichii was the most clastogenic/aneugenic fraction with a Minimal Active Concentration (MAC) of 23.1 μg mL−1. It was submitted to a separation step leading to six main saponins identified as quinovic acid glycosides (saponins A, D, E, G, J, K). None of the isolated saponins exerted a significant clastogenic/aneugenic activity by the micronucleus assay, however a mixture made with equal quantities of each of the six saponins exhibited a direct genotoxic/clastogenic activity as assessed by both the micronucleus assay and the comet assay on Chinese Hamster Ovary cells. Conclusion Saponins present in the hydromethanolic extracts of Nauclea induced synergistic in vitro DNA-damage and chromosome mutations in mammalian cells. This genotoxic activity was probably due to the capacity of Nauclea saponins to reduce cell defense against oxidative stress through the inhibition of glutathione-S-transferase activity.

Nauclea latifolia Smith is used traditionally in the treatment of uncomplicated malaria and painful conditions among its several other applications. The objective of this study is to investigate the pharmacological activities of the plant relevant to the symptomatic treatment of malaria fever and other painful conditions as an initial step towards developing an effective therapy for the symptomatic management of malaria fever and relief of other painful conditions.Various concentrations of the aqueous extract of the root bark of this plant were evaluated for its anti-nociceptive, anti-inflammatory and anti-pyretic activities in mice and rats. Investigation of the anti-nociceptive activities was performed using the acetic acid-induced abdominal constriction and hot-plate tests in mice and formalin-induced pain test in rats, as models of nociception. The extract was also investigated for its effect against inflammation induced by egg-albumin and pyrexia induced by yeast in rats.Our data showed that the aqueous extract of Nauclea latifolia root bark (50-200mg/kg p.o.) significantly (P0.05) attenuated writhing episodes induced by acetic acid and increased the threshold for pain perception in the hot-plate test in mice, dose-dependently. The product also remarkably decreased both the acute and delayed phases of formalin-induced pain in rats and also caused a significant reduction in both yeast-induced pyrexia and egg-albumin-induced oedema in rats. These effects were produced in a dose-dependent manner.The results suggest the presence of biologically active principles in the extract with anti-nociceptive, anti-inflammatory and anti-pyretic activities that justifies its use in malaria ethnopharmacy and subsequent development for clinical application.

Ethnopharmacological relevance: Although traditional antimalarial plant remedies in herbal markets are a very important component of the health care system in Ghana this has not been previously studied to allow for the formulation of effective strategy for malaria control in Ghana. Aim of study: The main objective of the present study was to collect and analyse data on the antimalarial plant remedies in herbal markets in southern Ghana. Materials and methods: Herborists were interviewed using a validated questionnaire and species of plants were identified using a combination of field photo guides, local names and voucher specimens. Results: A total of 71 herborists (95.8% female) were interviewed. There were potential correlations between different parameters and variables such as ethnic groups, type of vendor and age-groups. The study revealed 29 species of plants belonging to 22 families being sold for the treatment of malaria. The detailed use of these plants is documented. The most frequently mentioned species of plants were Morinda lucida Benth., Indigofera sp. and Nauclea latifolia Sm. The majority (82.8%) of the plant materials were sold in the dried state and 6.9% were sold in fresh state. About 76.2% of the herbal remedies were sold throughout the year while 23.8% were scarce in the dry season. The cost of treatment of malaria using the herbal remedies ranged from 1 to 2 United States Dollars (USD). Conclusion: Standardization of names and authentication of plant materials using organoleptic, phytochemical and DNA barcoding techniques as well as further research on efficacy, safety and dosage prescriptions for both fresh and dried plant materials being sold for the treatment of malaria in southern Ghana are needed.

We investigated the histomorphological effects of Nauclea latifolia and Coartem® on the antioxidant levels and hippocampus in Plasmodium berghei ANKA infected mice. Forty-two mice, 6 per group, bet...

International audience; Thirty-three plants commonly used in West tropical Africa by traditional healers for the treatment of malaria were collected and ethanolic extracts were obtained by decoction. The antiplasmodial activity of extracts was evaluated in vitro against the chloroquine-resistant FcB1 strain of Plasmodium falciparum. Cytotoxicity was determined on the human MRC-5 and the rat L-6 cell lines. Of the 33 plant extracts, eight (24.5%) showed significant antimalarial activity (IC(50) values ranging from 2.3 to 13.7 microg/ml), 14 (42.5%) weak activity (IC(50) values ranging from 15 to 50 microg/ml) and 11 (33%) appeared inactive (IC(50) values >50 microg/ml). Five plants were of particular interest, associating good antiplasmodial activity and weak cytotoxicity. These five included Nauclea latifolia with known antiplasmodial activity and four, Fagara macrophylla, Funtumia elastica, Phyllanthus muellerianus and Rauvolfia vomitoria, for which the description of antiplasmodial activity is entirely novel.

The present study evaluated the neuropharmacological effects of the aqueous extract of Nauclea latifolia root bark in rodents. Effects on the spontaneous motor activity (SMA), exploratory behaviour, pentobarbital sleeping time, apomorphine-induced stereotypic behaviour and motor coordination (rota-rod performance) were investigated. The extract (50-200 mg/kg p.o.) significantly (P

Seven methanol extracts of seven plants from seven plant families were screened for antimalarial properties. The plants were identified and selected from Gboko and Kastina-Ala local government areas in the Tivland ethnobotany in the Middle Belt Zone of Nigeria. Methanol plant extracts were evaluated for in vitro. antimalarial properties using the lactate dehydrogenase technique, with a multiresistant strain of Plasmodium falciparum. K1. Quantification of activity was by estimation of the concentration of extracts that inhibited 50% growth of parasite (IC50) in µg/ml. Of the seven plants screened, Erythrina senegalensis. DC (Leguminosae), Pericopsis elata. Harms (Papilionaceae), and Bridelia micrantha. Benth (Fabaceae) had IC50 values of 99.7, 124.8, and 158.7 µg/ml, respectively. Nauclea latifolia. SM (Rubiaceae) extract exhibited the least activity in the assay with an IC50 value of 478.9 µg/ml.

This work focuses primarily on the comparative response of rat liver enzymes to oral administration of the watersoluble fraction of 95% ethanol extract of Nauclea latifolia Sm. (Rubiaceae) leaves with 10% coconut oil meal and normal rat chow fed for 8 weeks. Forty-eight mature male albino rats of the Wistar strain weighing between 200 and 230 g were divided into two experimental groups. In experiment 1, group 1 (n ¼ 6) was fed normal rat chow for 8 weeks, and groups 2, 3, and 4 (n ¼ 6) were on normal rat chow for 8 weeks before treatment with 170, 340, and 510 mg=kg body weight, respectively, of oral dose of the water-soluble fraction of the ethanol extract of N. latifolia leaves. In experiment 2, group 1 (n ¼ 6) was fed the 10% coconut oil meal as the experimental control, and groups 2, 3, and 4 (n ¼ 6) were fed the 10% coconut oil meal for 8 weeks before commencing treatment for 2 weeks with the extract of N. latifolia leaves. The effects of the N. latifolia leaf extract on some marker enzymes were analyzed. There was a significant increase ( p 0:05) in experiment 1 animals when compared with control. Increase in ALT activity was however observed in experiment 2 (p 0:05) change in c-GT activity in experiment 1, but in experiment 2 glutamyl transferase (GGT) decreased in the water-soluble fraction of the ethanol extract. N. latifolia leaf extract is capable of reducing the activity of c-GT if raised by other factors. We also concluded that feeding animals with 10% coconut oil meal predisposes them to more adverse effects by the extract of N. latifolia leaves.

International audience; ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Nauclea latifolia Smith (Rubiaceae) popularly known as "koumkouma" is used in traditional Cameroonian medicine as neuropathic pain remedy and for the treatment of headache, inflammatory pain and convulsion. This study was conducted to evaluate the antinociceptive effects of the alkaloid fraction isolated from Nauclea latifolia in neuropathic pain induced by chronic constriction injury (CCI) of the sciatic nerve in rat. MATERIALS AND METHODS: Bioactive-guided fractionation of the root extracts of Nauclea latifolia using the Von Frey in a rat model of neuropathic pain (Benett model), afforded a potent anti-hyperalgesic fraction IV. Further fractionation of this fraction was performed by high-performance liquid chromatography (HPLC), yielded eight sub-fractions (F1-F8) which were tested for antinociceptive effects. The alkaloid fraction (F3) collected by HPLC, exhibited potent antinociceptive effects, and the anti-allodynic and anti-hyperalgesic effects of this fraction (8, 16, 40 and 80 mg/kg) were determined using the von Frey and acetone tests respectively in a rat model of neuropathic pain. Rota-rod performance and catalepsy tests were used for the assessment of motor coordination. RESULTS: The alkaloid fraction (80 mg/kg) administered intraperitoneally induced a completely decreased hyperalgesia 90 min post-dosing. In the acetone test, the Nauclea latifolia fraction at 80mg/kg showed its maximal anti-allodynic effects 120 min post-injection. The areas under the curve (AUC) of the anti-allodynic or anti-hyperalgesic effects produced by the alkaloid fraction at 80 mg/kg were significantly (p

The methanol extracts of Clematis papuasica leaves and stem bark and of Nauclea obversifolia leaves, stem and root barks showed awide spectrum of antibacterial activity which was increased on fractionation (petrol, dichloromethane, ethyl acetate), the ethyl acetate fractions being in all cases the most effective. None of the extractives was active against tested moulds.

Piliostigma thonningii, Ocimum gratissimum, Nauclea latifolia and Alstonia boonei are used in Nigerian traditional medicines against gastrointestinal helminths of animals and man. Proanthocyanidins were detected in Piliostigma and Nauclea, but not Alstonia or Ocimum. Extracts of these plants killed 50% of brine shrimp nauplii at

The toxicity and the genotoxicity of antimalarial alkaloid rich extracts derived from two plants used in traditional medicine in Mali (Mitragyna inermis (Willd.) O. Kuntze Rubiaceae and Nauclea latifolia (Sm.) Rubiaceae) were evaluated on in vitro and in vivo systems. The results demonstrated that an alkaloid rich extract derived from M. inermis induced a strong inhibition of protein synthesis in mammalian cells but did not exhibit mutagenic or genotoxic activity. An alkaloid rich extract derived from N. latifolia could interact in vitro with DNA of bacteria and mammalian cells, leading to G2-M cell cycle arrest and herita­ ble DNA-damage, as well as inducing in vivo single-strand breaks in liver, kidney and blood cells. Copy­ right © 2000 John Wiley & Sons, Ltd.

N. latifolia stem bark methanolic extract and the chloroform and ethyl acetate fractions significantly inhibited HLGP at a concentration of 5 mg/ml with 85%, 69% and 98%, respectively. On the other hand, i n vitro screening with 2,2-diphenyl-1-picrylhydrazyl (DPPH) at concentration of 12.5 ?g/ml revealed a prominent radical scavenging activity (RSA) of the chloroform fraction (85%) and relatively lower RSA of the methanolic (68%) and ethyl acetate fraction (77%) which seems not to be closely correlated with anti-diabetic activity. RP-HPLC-DAD coupled with tandem mass spectrometry performed on the ethyl acetate fraction which was associated with the most significant HLGP inhibitory activity resulted in the identification of chlorogenic acid, its glucoside, caffiec acid dimer, noengenin and noengenin dimmer, apigenin7- O-pentouronic acid, quercetin, luteolin 7-methoxy, isorhamnetin and isorhamnetin 3-methoxy

Root bark of Nauclea latifolia defatted with diethylether and then extracted with ethanol had an LD50 of 300 mg/kg in mice (i.p.) at 24 h. No significant effect of the extract on pentobarbitone-induced hypnosis in mice after i.p. injection was observed and challenged mice showed nervous signs prior to death. An oral administration of the ethanolic extract (100 mg/kg) significantly reduced pentobarbitone-induced sleep in rats poisoned with CCl4. The elevation of serum glutamic-oxalocetic trasaminase (SGOT), glutamic- pyruvic transaminne (SGPT), and alkaline phosphatase (SALP) induced by CCl4 intoxication in rats was also significantly attenuated by the extract. The ethanolic extract, at a dose of 1 mg/ml, remarkably reduced the leakage of lactate dehydrogenase (LDH) in isolated rat hepatocytes and exhibited a significant action on lipid peroxidation. Other fractions attenuated the leakage of LDH, but had no significant effect on lipid peroxidation. The ethanolic extract appeared to decrease the level of pa...

The leaf and root parts or their combination of Nauclea latifolia were separately extracted and their pharmacological effects on purinergic transmission in the bladder investigated. The leaf extract was very potent in potentiating purinergic neurotransmission by potentiating ATP induced contractions. These actions were more pronounced than the depression of potassium chloride evoked contraction of the bladder. The root extract depressed purinergic contraction of the bladder by a direct depressant action on the bladder smooth muscle since it did not modify ATP induced contractions. The leaf and root extracts antagonized each other when combined together. It is concluded that the leaf and root extracts of N. latifolia possess interesting pharmacological actions on the bladder.

treated groups. A significant (p < 0.05) decreased in Aspartate aminotransferases (AST) and Aminotransferases (Al T) levels was observed in all treated groups especially in the group treated with the mixture at a high dose. The photomicrographs of the organs — liver, kidney and heart- treated with 500 mg/kg body weight of the combination indicated no abnormalities while the liver of the animals treated with N. laevis extract (500 mg/kg body) showed slight hypertrophy of hepatocytes with apparent congestion at the sinusoidal spaces otherwise no other changes occurred. Also the renal corpuscles of the kidney treated with the same dose of N. laevis appeared partially shrunken with increase in bowman’s space. Cellular changes were not apparent while no abnormalities were observed in the heart and testes. There were no abnormalities observed in the photomocrographs of the testes, heart, liver and kidney of the animals treated with Nauclea latifolia (500mg/kg bodyweight) root extract. No significantly (p≥0.05) increase in the hb, RbC and PCV values were observed in animals treated with the extract combination compared to the control.

The aim of this study was to evaluate the short-term safety and tolerability of an antimalarial herbal medicinal product (PR 259 CT1) consisting of a quantified 80 % ethanol extract from the stem bark of Nauclea pobeguinii when given orally to healthy adult male volunteers. The amount of the major alkaloid strictosamide in the extract was determined by a validated HPLC method and was shown to be 5.6 %. The herbal preparation was formulated in a gelatine capsule form containing 500 mg of PCR 259 CT1. A sample of 15 healthy male volunteers, selected using the Lot Quality Assurance of Sampling (LQAS) method, was eligible for inclusion after fulfilment of the inclusion criteria and clinical examination by a physician. The volunteers were treated in an outpatient clinic with a drug regimen of two 500 mg capsules three times daily (each eight hours) for seven days, during meals. Safety and tolerability were monitored clinically, haematologically, biochemically and by electrocardiographic (ECG) examination at days 0, 1, 3, 7 and 14. Adverse effects were recorded by self-reporting of the participants or by detection of abnormalities in clinical examinations by a physician. The oral administration of PR 259 CT1 at high doses of 2 × 500 mg/capsule/day for 7 days was found to induce no significant changes in the concentration levels of all investigated haematological, biochemical, electrocardiogram and vital sign parameters and physical characteristics after 14 days of treatment compared to those seen in the baseline data. The concentration levels of all evaluated parameters were within the normal limits as reported in the literature. All adverse events noted were mild and self-resolving including increase of appetite (33 %), headache (20 %) and nausea (20 %). Other minor side effects were insomnia, somnolence and asthenia (7 %). Thus, PR 259 CT1 presented a significant safety and tolerability in healthy volunteers to allow its further development by starting a phase II clinical trial.

Nauclea latifolia (Rubiaceae) is a medicinal plant used in Nigeria folk medicine for the treatment of gastrointestinal disorders. The root bark of the plant was extracted with 70% ethanol and the extract screened for antidiarrheal activity by investigating castor oil-induced diarrhea and small intestinal motility in mice. The effects of the extract on isolated rat ileum were also investigated. The extract (125, 250 and 500 mg/kg) caused a significant decrease in the frequency of diarrhea and conferred protection following castor oil administration (P < 0.05). It also significantly (P < 0.0001) inhibited small intestinal motility in mice at the same doses. Its activity was dose-dependent and when compared to atropine, its antidiarrheal effects at 500 mg/kg were 179% and 165% respectively, in castor oil-induced diarrhea and small intestinal motility experiments. Extract effects on rat ileum revealed a significant (P < 0.0001) inhibition of acetylcholine-induced contractions at 0.2 and 2 mg/mL final bath concentrations used. These findings confirm the antidiarrheal activity of the root bark extract of N. latifolia.

International audience; CONTEXT: Nauclea latifolia Smith (Rubiaceae) is a small tree found in tropical areas in Africa. It is used in traditional medicine to treat malaria, epilepsy, anxiety, pain, fever, etc. Objective: The aim of this study was to investigate the effects of Nauclea latifolia roots decoction on the peripheral and central nervous systems and its possible mechanisms of action. MATERIALS AND METHODS: The analgesic investigation was carried out against acetic acid-induced writhing, formalin-induced pain, hot-plate and tail immersion tests. The antipyretic activity was studied in Brewer's yeast-induced pyrexia in mice. Rota-rod test and bicuculline-induced hyperactivity were used for the assessment of locomotor activity. RESULTS: Nauclea latifolia induced hypothermia and had antipyretic effects in mice. The plant decoction produced significant antinociceptive activity in all analgesia animal models used. The antinociceptive effect exhibited by the decoction in the formalin test was reversed by the systemic administration of naloxone, N(ω)-L-nitro-arginine methyl ester or glibenclamide. In contrast, theophylline did not reverse this effect. Nauclea latifolia (antinociceptive doses) did not exhibit a significant effect on motor coordination of the mice in Rota-rod performance. Nauclea latifolia protected mice against bicuculline-induced behavioral excitation. DISCUSSION AND CONCLUSION: Overall, these results demonstrate that the central and peripheral effects of Nauclea latifolia root decoction might partially or wholly be due to the stimulation of peripheric opioid receptors through the action of the nitric oxide/cyclic monophosphate guanosin/triphosphate adenosine (NO/cGMP/ATP)-sensitive- K(+) channel pathway and/or facilitation of the GABAergic transmission.

International audience; The neuropharmacological effects of the decoction of Nauclea latifolia Smith (Rubiaceae) roots were studied in mice Different experimental models (forced swimming test, horizontal wire test and hole-board test) were used for detecting antidepressant, myorelaxant and anxiolytic properties The results revealed that Nauclea latifolia induced a reduction of immobility, in a similar way to that of fluoxetine, along with a significant increase in the percentage of spent time in swimming behavior Nauclea latifolia displayed a myorelaxant activity in the horizontal wire test In the hole-board test, Nauclea laufolta significantly increased the number and duration of head-dips In addition, anxiolytic-like properties of Nauclea laufolta were blocked by anxiogenic agents as examined in the hole-board test This was the case for N-methyl-beta-carboline-3-carboxamide (FG7142), a partial Inverse agonist at the benzodiazepine site of the GABA(A) receptor complex, flumazenil (RO151788), a central benzodiazepine receptor antagonist and bicuculline, a light-sensitive competitive antagonist of GABA(A) receptors These results suggest that Nauclea latifolia roots decoction possess antidepressant, myorelaxant and anti-anxiety-like properties in the models employed The extracts might potentially act by GABAergic activation and/or by modulating the serotoninergic levels in the central nervous system However, further studies were still required