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Abstract Pseudospondias microcarpa is used in ethnomedicine to manage central nervous system diseases. The hydroethanolic extract (PME) from the leaves of the plant has shown anxiolytic-like properties in mice anxiety models. However, its effects in chronic anxiety models and possible mechanism(s) of action were not studied. Therefore, the current study evaluated the anxiolytic-like mechanisms of PME in zebrafish models of anxiety. The zebrafish light dark test (LDT) and novel tank test (NTT) were employed to assess the anxiolytic-like effects of PME (0.1, 0.3, 1.0 mg mL−1), fluoxetine (3 × 10−5 mg mL−1) and diazepam (1.5 × 10−7 mg mL−1). The chronic unpredictable stress (CUS) test was used to further evaluate the extract’s anxiolytic-like properties. The potential mechanisms of anxiolytic action of the extract was evaluated after pre-treated with flumazenil, granisetron, methysergide, or pizotifen, all at 1 × 10−3 mg mL−1. The extract significantly decreased anxiety behaviours in the NT and LD tests. These observed effects of the extract were however counteracted by flumazenil, granisetron, methysergide and pizotifen pre-treatment. In addition, PME treatment significantly reversed CUS-induced anxiety behaviours in zebrafish. Results show that PME possesses anxiolytic-like effects possibly through interaction with serotonergic and gamma-aminobutyric acid mediated pathways. Graphical abstract

Aidia genipiflora (DC.) Dandy (Rubiaceae) is used to treat various microbial and inflammatory conditions by traditional healers in West African countries. However, there is no information on anti-inflammatory potential of A. genipiflora. This work therefore provides information on the anti-inflammatory and the antioxidant activities of the stem bark extracts and some bioactive constituents of Aidia genipiflora. Method: The anti-inflammatory activities of the extracts and compounds from A. genipiflora were investigated using the carrageenan-induced footpad oedema assay and the egg albumin denaturation assay. The antioxidant activities of the extract and compounds were investigated using the DPPH radical scavenging assay and the phosphomolybdenum total antioxidant capacity assay. The whole extract of A. genipiflora was also investigated for its acute oral toxicity using the fixed-dose procedure described by the Organization for Economic Cooperation Development guidelines. Result: The whole extract showed no acute toxicity effect and the LD50 was estimated to be greater than 3000 mg/kg body weight. The whole extract, methanol, and ethyl acetate fractions (30, 100, and 300 mg/kg) showed in vivo anti-inflammatory activity with respective percentage inhibition of oedema of 45.11 ± 3.41, 31.12 ± 3.42 and 29.28 ± 3.58 (p < 0.001) at the highest dose of 300 mg/kg. Diclofenac, used as a reference drug, gave a % inhibition of 48.94 ± 3.58. The compounds isolated from A. genipiflora demonstrated in-vitro anti-inflammatory activity at the IC50 range (16–96 μg/mL) compared to diclofenac (IC50 of 74.48 μg/mL). Oleanonic acid (AG1) and D-mannitol (AG4) further demonstrated in vivo anti-inflammatory activity (ED50 = 20.61 ± 1.29; 23.51 ± 1.26 mg/kg respectively) which was less potent compared to diclofenac (ED50 = 12.50 ± 1.41 mg/kg) in the carrageenan-induced oedema assay. The whole extract, pet. ether, ethyl acetate, and methanol fractions of A. genipiflora exhibited DPPH scavenging activities with respective IC50 of 222.2, 169.7, 121.5, and 40.7 μg/mL. The whole extract of A. genipiflora exhibited considerable total antioxidant capacity with respective values of 248.5 mg/g of ascorbic acid equivalent. All the compounds exhibited low DPPH scavenging activity with IC50 (64–86 μg/mL), compared to ascorbic acid (IC50 of 3.13 ± 1.20 μg/mL). These results highlight the anti-inflammatory and antioxidant activities of Aidia genipiflora stem bark extract and its constituents as evidence to support its traditional uses.

Trichilia monadelpha is reported to have acute anti-inflammatory effects. This study sought to establish the possible effects of the petroleum ether, ethyl acetate, and ethanolic extracts of Trichilia monadelpha stem bark (i.e., PEE, EAE, and EthE, respectively) on C-reactive proteins, using various acute inflammatory models. Changes in hind paw volume of Sprague-Dawley rats were measured before and after intraplantar injection of; 50 μL of 0.5% λ-carrageenan, 0.1 ml of 0.1% histamine, 0.1 ml of 0.02% serotonin, 1 nmol Prostaglandin E2, or 10 nmol bradykinin, to induce paw oedema, and during treatment with 10, 30, or 100 mgkg−1 PEE, EAE, or EthE, or various reference drugs. Changes in rectal temperature, and plasma C-reactive protein levels were also measured after injecting, intraperitoneally, 0.1 mgkg−1 Lipopolysaccharide (Escherichia coli) to induce pyrexia.PEE, EAE, and EthE reduced significantly (P ≤ 0.01–0.001; maximum inhibition at 100 mgkg−1 (imax) = 55.0–76.7%) paw oedema induced by carrageenan; comparable to diclofenac (P ≤ 0.0001; imax = 93.1%). PEE, EAE and chlorpheniramine prevented significantly (P ≤ 0.0001; imax = 115–144%) or reduced significantly (P ≤ 0.0001; imax = 80–85%) histamine-induced paw oedema. PEE, EAE and ondansetron significantly decreased (curative: P ≤ 0.01–0.001, imax = 51–82%; prophylactic: P ≤ 0.01–0.001, imax = 56–77%) serotonin-induced inflammation. In prostaglandin E2 –induced inflammation PEE and EAE significantly reduced (curative: P ≤ 0.05–0.01, imax = 60–70%; prophylactic: P ≤ 0.0001, imax = 86–332%) oedema; PEE and EAE also significantly decreased (curative: P ≤ 0.050–0001, imax = 46–98%; prophylactic: P ≤ 0.01–0.001 imax = 62–78%) in bradykinin-induced inflammation. PEE, EAE, Diclofenac and Dexamethasone significantly reduced (P ≤ 0.05–0.001) plasma C-reactive protein levels. PEE, EthE, EAE and Aspirin significantly reduced (P ≤ 0.05–0.001) febrile response.Trichilia monadelpha stem bark extracts had anti-inflammatory and anti-pyretic properties and significantly reduced C-reactive proteins associated with carrageenan-induced inflammation.

The present study evaluated the antidiabetic activities of the 70% ethanol stem bark extract of Aidia genipiflora (AGB) and one of its constituents, oleanonic acid in streptozotocin (40 mg/kg)-induced diabetic rats. In vitro assays of glucose uptake and inhibition of carbohydrate metabolizing enzymes were then used to investigate their mechanism(s) of hypoglycaemic action. In silico evaluation of the pharmacokinetic and toxicity properties of the compound was also carried out. Administration of AGB (100–400 mg/kg) and oleanonic acid (15 – 60 mg/kg) resulted in significant reductions (p

Background: Zingiber officinale Roscoe (ginger) rhizome is a global spice with marked pharmacological activities and industrial applications. The demand for the powdered spice soared in the wake of the COVID-19 global pandemic. The present study sought to assess powdered ginger products on the Ghanaian market for some quality parameters and compare their chemical composition via chemometric analysis of their FT-IR data. Methods: A survey was conducted in three major markets in Ghana to determine the commercially available powdered ginger products. These products were purchased and assessed for microbial load, heavy metals contents and ash values using official methods. Also, principal component and hierarchical cluster analysis, as multivariate algorithms, were applied to their FT-IR spectral fingerprints, using Z. officinale, Z. zerumbet and some dried ginger rhizomes from Nigeria as reference samples. Results: Seven products were found in the survey: three local and four foreign. The local products failed to meet regulatory label requirements. The microbial load, heavy metals and ash values of all commercial samples were generally within specifications except for the aerobic bacterial counts of some local samples. Pharmacopoeial identity test and the chemometric analysis revealed all the products to contain Z. officinale. The reference ginger sample from Nigeria also demonstrated some level of similarity with Z. officinale. The variations in physical attributes and slight difference in chemical composition of the different products was presumed to be due to chemical changes arising from different processing methods and possible adulteration with other flours. Conclusion: The sampled ginger products on the market originate from Z. officinale and have quality attributes that make them suitable for food and medicinal applications. The observed deviations, however, suggest an urgent need for standardized processing methods to ensure consistency in quality indices, as well as regular quality checks by regulatory bodies.

Objective: To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum. Methods: The effects of oral treatment with hydro-ethanolic extract (125, 250 and 500 mg/kg) of the stem bark of Chrysophyllum albidum and glibenclamide for 21 d on glucose level, serum enzyme markers for liver function, lipid profile, total protein, serum urea, serum creatinine, and body weight were evaluated in experimental diabetic rats administered with 45 mg/kg of streptozotocin. In vitro assays including glucose uptake in C2C12 cells and 3T3-L1 adipose tissues, α-glucosidase and α-amylase inhibition were employed to evaluate the possible mechanism of hypoglycemic action of the extract. DPPH and nitric oxide radical antioxidant activity of the extract was also measured. Results: The increased levels of blood glucose, triglycerides, low- density lipoprotein, total cholesterol, serum aspartate, and alanine transaminases, creatinine, and urea in the diabetic animals were reduced significantly (P

The antifungal activity of the 70% ethanol stem bark extract of Erythrina senegalensis (ESB) against different strains and drug resistant clinical isolates of Candida albicans and Candida glabrata were evaluated in the study. The effect of ESB on biofilms as well as its activity in combination with fluconazole, nystatin or caspofungin against the Candida strains were also evaluated. We then evaluated the antifungal activity of a microemulsion formulation of ESB against planktonic and biofilms of the Candida species. UPLC-QTOF-MS2 analysis was then undertaken to identify the phytoconstituents of the extract and UPLC fingerprints developed for the routine authentication as part of quality control measures. ESB exerted strong antifungal activities against C. albicans ATCC 10231 and SC5314 strains, and C. glabrata ATCC 2001 strain with minimum inhibitory concentration (MIC) values from 3.91 to 31.25 μg/mL and minimum fungicidal concentrations (MFCs) that ranged from 62.5 to 250 μg/mL. It also exhibited potent antifungal activities (MIC = 4-64 μg/mL) against a collection of C. albicans and C. glabrata clinical isolates that were resistant to either nystatin or azole antifungals. The formulated ESB demonstrated higher antifungal potency against the C. albicans and C. glabrata strains with MIC values of 3.91-31.25 μg/mL which was the same as the MFC values. The extract and its microemulsion formulation were active against biofilms of the strains of the Candida species inhibiting their biofilm formations (SMIC50 = 16-64 μg/mL) and their preformed biofilms (SMIC50 = 128 ->512 μg/mL). ESB also exhibited synergistic antifungal action with fluconazole and nystatin against C. albicans ATCC 10231 and C. glabrata ATCC 2001 strains in the checkerboard assay. Chemical characterization of the extract revealed the presence of phenolic compounds such as flavonoids and their prenylated derivatives, anthracene glycosides and alkaloids. UPLC Fingerprints of the extract was also developed and validated for routine identification and authentication of the stem bark of E. senegalensis. The study findings have demonstrated that the stem bark of E. senegalensis is as a potential source of bioactive compounds that could be developed as novel antifungal agents.

A library of six compounds with new hybrids in a single molecule triazole ring attached to the phosphonium salts was synthesized. Click chemistry was, however, used to synthesize the 1-, 2-, and 3-triazole intermediates as a tether for the hybrid phosphonium salts. Their antibacterial activity against Gram-positive bacteria (Staphylococcus aureus and Enterococcus faecalis), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and Mycobacterium smegmatis mc2155 was determined using the HT-SPOTi assay. Compound 2 showed the most effective antimicrobial activity as it inhibited the growth of Pseudomonas aeruginosa and Staphylococcus aureus at 0.0125 µg/mL and 31.25 µg/mL, respectively. From the FICI data, compounds 2ET-TOL (2) and RABYL-TOL (4) successfully modulated the activities of amoxicillin against Pseudomonas aeruginosa and Staphylococcus aureus. All the test compounds exhibited a concentration-dependent biofilm formation inhibition against S. aureus, except P-Z (compound 6). Compounds P-MEOXY (1) and 2ET-TOL (2) exhibited mild activity against P. aeruginosa with compound 4 showing antimycobacterial activity at 500 µg/mL.

The challenges concerning the control of malaria remain due to the continuous emergence of drug resistant strains. Over the years, the use, misuse, and abuse of antimalarials have created a conducive environment for the development of resistant Plasmodium falciparum strains. We herein report on the synthesis, characterization and antimalarial activity of a library of seven novel 1,2,3-triazoles as part of the drug discovery campaign against drug-resistant Plasmodium falciparum. The interactions of the triazoles with plasmepsin II, plasmepsin IV, falcipain-2 and the heme detoxifying protein-all key proteins of Plasmodium falciparum degradosequesterome (Dsq) were also investigated by molecular docking. The compounds 3a-d, 4–6 were synthesized by CuAAC click reaction in good to excellent yields of 73–98% and characterized by melting point, UVvisible, infrared and nuclear magnetic resonance (1H and 13C) and MS techniques. Compounds 3a-d displayed high in vitro potency (IC50s: 0.62–22.11 ug/ml) against the chloroquine-resistant Dd2 lab strain of Plasmodium falciparum and low toxicity (SI > 1 except compound 4) to human erythrocytes. Computational studies indicated that the compounds 3a-3d had an absorption of 76–91%, and they were category III acute oral toxins (LD50 from 500 to 5000 mg/kg). The molecular docking study suggests that compounds 3a-d interacted with plasmepsin IV and the heme detoxifying protein with high affinity and a moderate affinity for falcipain-2.

Buruli ulcer disease, a necrotising skin and subcutaneous tissue disease, is endemic to tropical Africa. People in endemic communities’ resort to topical and oral consumption of plant extracts which have not been validated. The present study focused on validating the antimycobacterial properties and toxicity of different solvent extracts of the stem bark of P. angolensis and establish pharmacognostic standards for quality control purposes. In vitro antimycobacterial activity of the aqueous, 70% hydro-ethanol and ethyl acetate stem bark extracts of P. angolensis against M. ulcerans (NM 203 strain) was done using the Resazurin Microtiter Assay and their cytotoxicity assessed on normal Chang liver cells via the Alamar Blue assay. Pharmacognostic parameters were also evaluated according to standard methods. The ethyl acetate extract of the stem bark showed considerable activity against the M. ulcerans (MIC = 256 µg/mL) but was less active than the reference drugs streptomycin (MIC = 0.25 µg/mL) and rifampicin (MIC = 0.125 µg/mL). The aqueous and hydroethanolic extracts showed no activity. The active ethyl acetate extract was not cytotoxic (CC50=383.9 ± 69.7 µg/mL). Micromorphological analysis of the leaf surface revealed stellate trichomes and schizogenous cavities. Stem bark powder microscopy showed abundant starch grains, prismatic calcium oxalate crystals and large striated stone cells with a wide lumen. Morphological features, physicochemical, chromatographic, and spectroscopic standards have been established to guarantee consistency in the quality of herbal products containing P. angolensis. The activity of P. angolensis extract against M. ulcerans substantiates the traditional use of P. angolensis stem bark for Buruli ulcer management and as a potential source of antimycobacterial agents.

Background: Vitex doniana Sweet fruit, an under-utilised crop specie of Ghana, has not been validated for its ethnomedical use in managing inflammatory conditions. Therefore, the study sought to investigate its anti-inflammatory and antioxidant activities as well as isolate and quantify one of its active constituents. Materials and methods: In-vivo anti-inflammatory activity of the methanol fruit extract was evaluated using the carrageenan-induced oedema model in chicks. The in-vitro antioxidant property was also investigated using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. The acute and subacute toxicity studies of the fruit extract were evaluated in rodent models. Results: No signs of autonomic and central nervous system stimulation/depression were recorded. The LD50 by oral route, was estimated to be beyond 3000 mg/kg. Subacute studies revealed an increase in red blood cell and lymphocyte counts. Liver enzymes, serum proteins and bilirubin levels did not significantly increase. The crude extracts at doses of 10, 30 and 100 mg/kg inhibited paw oedema considerably. The ethyl acetate fraction showed the highest antioxidant activity (IC50 = 99.35 ± 0.77 μg/mL). Oleanolic acid, isolated from the ethyl acetate extract, showed significant anti-inflammatory and antioxidant activities. A sensitive high-performance liquid chromatography method for the detection and estimation of oleanolic acid, as a biomarker compound for V. doniana fruit, was developed and validated for quality assurance purposes. Conclusion: The extract of V. doniana fruits possesses considerable anti-inflammatory and antioxidant properties and was non-toxic under laboratory conditions.

The hypoglycaemic and anti-hyperlipidaemic effects of the 70% ethanol stem bark extract of Myrianthus libericus (MLB), used traditionally in the management of diabetes in Ghana, was evaluated in this study using streptozotocin (45 mg/kg)-induced diabetic rats. In vitro hypoglycaemic activities of the extract and one of its principal compounds, friedelan-3-one were then investigated using α-amylase inhibitory and glucose uptake assay in C2C12 myotubes. In silico analysis of the pharmacokinetic and toxicity properties of the compound was also performed. MLB significantly (p

Vulvovaginal candidiasis (VVC) is the second most common vaginal infection that affects women of reproductive age. Its increased occurrence and associated treatment cost coupled to the rise in resistance of the causative pathogen to current antifungal therapies has necessitated the need for the discovery and development of novel effective antifungal agents for the treatment of the disease. We report in this study the anti-Candida albicans activity of Solanum torvum 70% ethanol fruit extract (STF), fractions and some isolated compounds against four (4) fluconazole-resistant strains of C. albicans. We further report on the effect of the isolated compounds on the antifungal activity of fluconazole and voriconazole in the resistant isolates as well as their inhibitory effect on C. albicans biofilm formation. STF was fractionated using n-hexane, chloroform (CHCl3) and ethyl acetate (EtOAc) to obtain four respective major fractions, which were then evaluated for anti-C. albicans activity using the microbroth dilution method. The whole extract and fractions recorded MICs that ranged from 0.25 to 16.00 mg/mL. From the most active fraction, STF- CHCl3 (MIC = 0.25-1.00 mg/mL), four (4) known compounds were isolated as Betulinic acid, 3-oxo-friedelan-20α-oic acid, Sitosterol-3-β-D-glucopyranoside and Oleanolic acid. The compounds demonstrated considerably higher antifungal activity (0.016 to 0.512 mg/mL) than the extract and fractions and caused a concentration-dependent anti-biofilm formation activity. They also increased the sensitivity of the C. albicans isolates to fluconazole. This is the first report of 3-oxo-friedelan-20α-oic acid in the plant as well as the first report of betulinic acid, sitosterol-3-β-D-glucopyranoside and oleanolic acid from the fruits of S. torvum. The present study has demonstrated the anti-C. albicans activity of the constituents of S. torvum ethanol fruit extract and also shown that the constituents possess anti-biofilm formation and resistance modulatory activities against fluconazole-resistant clinical C. albicans isolates.

Myrianthus arboreus is use traditionally as an antidiabetic agent in Ghana. We reported the in vivo antidiabetic activity of its 70 % ethanol stem bark extract (MAB) which we found to be strongly concentrated in its EtOAc fraction using glucose uptake and enzyme inhibitory assays. The present study sought to investigate the in vivo hypoglycaemic and anti-hyperlipidaemic activity of this ethyl acetate fraction of MAB (MAB-EtOAc, 50 and 100 mg/kg) in streptozotocin (STZ)-induced diabetic rats for 21 days, isolate and evaluate the bioactive constituents responsible for the antidiabetic activity. In silico pharmacokinetic and toxicity properties of the most active compound was also determined. MAB-EtOAc significantly (p < 0.001) reduced the blood glucose levels while normalizing considerably the altered serum lipid parameters of the diabetic rats which was comparable to glibenclamide (5 mg/kg). Chemical investigation of MAB-EtOAc led to the isolation of seven known compounds including three flavanols which are reported for the first time in the plant: epicatechin (1), epigallocatechin (2), dulcisflavan (3), euscaphic acid (4), tormentic acid (5), sitosterol-3-O-β-d-glucopyranoside (6) and arjunolic acid (7). The compounds markedly inhibited the action of α-amylase and, except for 4 and 6, which stimulated considerably glucose uptake in C2C12 cells. Compounds 2, 3, 5, 6 and 7 which were further evaluated in STZ-induced diabetic rats demonstrated hypoglycaemic and anti-hyperlipidaemic activities which, however, were not comparable with MAB-EtOAc. Compound 3, the most active compound was predicted to be non-toxic, non-mutagenic, has reasonable oral bioavailability and a decent substrate for further drug development. The findings of this study show that the isolated compounds may contribute to the antidiabetic activity of M. arboreus and could serve as marker compounds for the quality control of herbal medicines that would be made from the plant.