In vivo toxicity, anti-hyperlipidaemic, antioxidant and anti-atherogenic activities of 'LIPO A' A traditional herbal product in rodents.

Hyperlipidemia accounts for about 17 million deaths worldwide each year. High cost and side effects have limited the use of conventional anti-lipidaemic agents in some cases, majority of whom resort to traditional medicine. The current research focused on validating the safety and efficacy of a herbal product, 'LIPO A' used in the management of hyperlipidaemia. Induction of hyperlipidaemia was achieved by oral administration of 3 mL of cholesterol in coconut oil for 4 weeks in male Sprague Dawley rats with water available as 40 % sucrose. Subsequently, the animals were treated with 100, 200 and 400 mg/kg of the product 'LIPO A' for 4 additional weeks with atorvastatin as reference drug (at 2 mg/kg body weight). Blood samples were taken for serum biochemistry and atherogenic ratios were then calculated. 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) scavenging assay, total antioxidant capacity, physicochemical and phytochemical analysis were also carried out using standard methods. Treatment resulted in a dose-dependent reduction in total cholesterol with maximum reduction of 46.01 % at 400 mg/kg compared to atorvastatin with 49.30 %. There were significant changes in the low-density lipoprotein cholesterol and high-density lipoprotein cholesterol (LDL-c/HDL-c) and Total Cholesterol (TC/HDL-c) ratios which measures the atherogenic and coronary risk indices respectively. Acute and subacute toxicity studies did not reveal any signs of toxicity. High Performance Liquid Chromatography (HPLC) fingerprint revealed six well resolved peaks with two prominent compounds with retention times 24.88 and 23.95 min, which could serve as quality control markers for the product. The herbal product showed considerable antihyperlipidemic and antioxidant actions in rodent models and lend credence to its use in traditional medicine for hyperlipidaemia.

Knowledge, perception, and pesticide application practices among smallholder cocoa farmers in four Ghanaian cocoa-growing regions.

Pesticides are widely used in Ghana, especially in cocoa farming. However, the practice is suboptimal and unsupervised. Incorrect use of these chemicals can seriously harm human health, the environment, and economies that rely on these farmers' output. The study assessed cocoa farmers' pesticide knowledge, practices, and risk perception. Four hundred and four cocoa farmers were chosen randomly from 26 communities in four cocoa-growing regions of Ghana to answer questions about their risk knowledge, awareness, and practices, including personal protective equipment, storage and disposal of leftover pesticides, and used containers. The study revealed that 87% of the respondents belonged to cooperatives and certification groups. There was a significant positive relationship between group membership and benefits derived from inputs and training in pesticide use. About 70% of insecticides used were approved by the Ghana Cocoa Board, with neonicotinoids and pyrethroids being the most highly used insecticide classes in cocoa farms. Although farmers claimed adequate pesticide knowledge, this did not translate into practice, with the majority exhibiting improper pesticide storage, application, and disposal practices. Farmers appeared to know a lot but lacked the skills and attitude to put their knowledge to use. The improper practices appear to manifest in a variety of health symptoms experienced by farmers as a result of chemical exposure. The findings from this study suggest that cocoa farmers in Ghana require adequate practical training and support on pesticide use to reduce their associated health risks, protect the environment and ensure sustainable cocoa production in the world's second-largest cocoa bean exporter.

Antibacterial, Resistance Modulation, Anti-Biofilm Formation, and Efflux Pump Inhibition Properties of Loeseneriella africana (Willd.) N. Halle (Celastraceae) Stem Extract and Its Constituents.

This study investigated the antibacterial, resistance modulation, biofilm inhibition, and efflux pump inhibition potentials of Loeseneriella africana stem extract and its constituents. The antimicrobial activity was investigated by the high-throughput spot culture growth inhibition (HT-SPOTi) and broth microdilution assays. The resistance modulation activity was investigated using the anti-biofilm formation and efflux pump inhibition assays. Purification of the extract was carried out by chromatographic methods, and the isolated compounds were characterized based on nuclear magnetic resonance, Fourier transform infrared and mass spectrometry spectral data and comparison with published literature. The whole extract, methanol, ethyl acetate, and pet-ether fractions of L. africana all showed antibacterial activity against the test bacteria with MICs ranging from 62.5 to 500.0 µg/mL The whole extract demonstrated resistance modulation effect through strong biofilm inhibition and efflux pump inhibition activities against S. aureus ATCC 25923, E. coli ATCC 25922 and P. aeruginosa ATCC 27853. Chromatographic fractionation of the ethyl acetate fraction resulted in the isolation of a triterpenoid (4S,4αS,6αR,6ßS,8αS,12αS,12ßR,14αS,14ßR)-4,4α,6ß,8α,11,11,12ß,14α-Octamethyloctadecahydropicene-1,3(2H,4H)-dione) and a phytosterol (ß-sitosterol). These compounds showed antibacterial activity against susceptible bacteria at a MIC range of 31-125 µg/mL and potentiated the antibacterial activity of amoxicillin (at » MIC of compounds) against E. coli and P. aeruginosa with modulation factors of 32 and 10, respectively. These compounds also demonstrated good anti-biofilm formation effect at a concentration range of 3-100 µg/mL, and bacterial efflux pump inhibition activity at ½ MIC and » MIC against E. coli and P. aeruginosa. Loeseneriella africana stem bark extracts and constituents elicit considerable antibacterial, resistance modulation, and biofilm and efflux pump inhibition activities. The results justify the indigenous uses of L. africana for managing microbial infections.

Multi-drug resistant bacteria isolates from lymphatic filariasis patients in the Ahanta West District, Ghana.

BACKGROUND: Antimicrobial resistance is associated with increased morbidity in secondary infections and is a global threat owning to the ubiquitous nature of resistance genes in the environment. Recent estimate put the deaths associated with bacterial antimicrobial resistance in 2019 at 4.95 million worldwide. Lymphatic filariasis (LF), a Neglected Tropical Disease (NTD), is associated with the poor living in the tropical regions of the world. LF patients are prone to developing acute dermatolymphangioadenitis (ADLA), a condition that puts them at risk of developing secondary bacterial infections due to skin peeling. ADLA particularly worsens the prognosis of patients leading to usage of antibiotics as a therapeutic intervention. This may result in inappropriate usage of antibiotics due to self-medication and non-compliance; exacerbating antimicrobial resistance in LF patients. In this perspective, we assessed the possibilities of antimicrobial resistance in LF patients. We focused on antibiotic usage, antibiotic resistance in Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa isolates and looked at genes (mecA and Extended-spectrum beta-lactamase [blaCTX-M, blaSHV and blaTEM]) coding for resistance in multi-drug resistant (MDR) bacterial isolates. RESULTS: Of the sixty (60) participants, fifty-four (n = 54, 90%) were within 31-60 years of age, twenty (n = 20, 33.33%) were unemployed and thirty-eight (n = 38, 50.67%) had wounds aged (in months) seven (7) months and above. Amoxicillin (54%) and chloramphenicol (22%) were the most frequently used antibiotics for self-medication. Staphylococcus aureus isolates (n = 26) were mostly resistant to penicillin (n = 23, 88.46%) and least resistant to erythromycin (n = 2, 7.69%). Escherichia coli isolates (n = 5) were resistant to tetracycline (n = 5, 100%) and ampicillin (n = 5, 100%) but were sensitive to meropenem (n = 5, 100%). Pseudomonas aeruginosa isolates (n = 8) were most resistant to meropenem (n = 3, 37.50%) and to a lesser ciprofloxacin (n = 2, 25%), gentamicin (n = 2, 25%) and ceftazidime (n = 2, 25%). Multi-drug resistant methicillin resistant Staphylococcus aureus (MRSA), cephalosporin resistant Escherichia coli. and carbapenem resistant Pseudomonas aeruginosa were four (n = 4, 15.38%), two (n = 2, 40%) and two (n = 2, 25%) respectively. ESBL (blaCTX-M) and mecA genes were implicated in the resistance mechanism of Escherichia coli and MRSA, respectively. CONCLUSION: The findings show presence of MDR isolates from LF patients presenting with chronic wounds; thus, the need to prioritize resistance of MDR bacteria into treatment strategies optimizing morbidity management protocols. This could guide antibiotic selection for treating LF patients presenting with ADLA.

Trace Metals in Cannabis Seized by Law Enforcement in Ghana and Multivariate Analysis to Distinguish among Different Cannabis Farms.

For hundreds of years, cannabis has been one of the most known cultivated plants due to its variety of uses, which include as a psychoactive drug, as well as for medicinal activity. Although prohibiting cannabis products, the countries of the African continent are the largest producers of cannabis in the world; a fact that makes the trafficking of cannabis-based illicit drugs a high priority for local law enforcement authorities. The latter are exceedingly interested in the use of chemical analyses for facilitating quantification, identification, and tracing of the origin of seized cannabis samples. Targeting these goals, and focusing on the country of Ghana, the present study used inductively coupled plasma mass spectrometry (ICP-MS) for the determination of 12 elements (Pb, Cu, Ca, Mg, Mn, Zn, Cd, As, Hg, Fe, Na, and K) in cannabis seized by Ghana's law enforcement authorities and soils of cannabis farms. Furthermore, multivariate analysis was applied to distinguish among different cannabis farms and match them with the samples. As a result, 22 seized cannabis samples and 12 other cannabis samples with their respective soils were analyzed to reveal considerable As and Pb concentrations. As and Pb levels in cannabis were found up to 242 ppb for As and 854 ppb for Pb. Multivariate analysis was applied for separating different cannabis farms and seized samples based on elemental analysis, evidently linking the seized samples with two Ghana regions.

Evaluation of the anti-inflammatory and antioxidant potential of the stem bark extract and some constituents of Aidia genipiflora (DC.) dandy (rubiaceae).

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.

Assessment of some quality parameters and chemometric-assisted FTIR spectral analysis of commercial powdered ginger products on the Ghanaian market.

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.

Hypoglycaemic activity of Oleanonic acid, a 3-oxotriterpenoid isolated from Aidia Genipiflora (DC.) Dandy, involves inhibition of carbohydrate metabolic enzymes and promotion of glucose uptake.

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 < 0.001) in the blood glucose and considerable decrease (p < 0.05) in the elevated lipid parameters of the diabetic animals. AGB activity at 200 and 400 mg/kg; and oleanonic acid at 60 mg/kg were comparable to glibenclamide (5 mg/kg). The extract and its isolate strongly inhibited α-glucosidase and α-amylase activity with IC50 values of (10.48 ± 1.39 µg/mL and 14.51 ± 1.26 µg/mL) and (36.52 ± 1.95 µM and 105.84 ± 1.08 µM) respectively. The glucose uptake assays showed that AGB and oleanonic acid exerted both insulin-dependent and independent promotional effect of glucose transport into the periphery by upregulating the expression of PI3K and PPARγ transcripts with a concomitant increase in GLUT-4 transcripts. Although oleanonic acid was predicted to be teratogenic, it was found to be generally non-lethal with favourable pharmacokinetics properties making it suitable for further studies. The study has shown that the stem bark of A. genipiflora is a source of new hypoglycaemic agents and that oleanonic acid possesses hypoglycaemic and anti-hyperlipidaemic activities.

Antinociceptive effects of a hydroethanolic stem bark extract of Burkea africana.

INTRODUCTION: Pain is a major symptom of many clinical disorders and its relief has long been a concern for individuals across the globe. There is therefore an unmet need to search for new efficacious agents for the effective management of pain. The stem bark of the savanna tree Burkea africana (Hook) (Family: Leguminosae) is used in the Ghanaian traditional medicine for the treatment and management of various pain-related diseases. METHOD: An acute oral toxicity study in mice was conducted by administering BAE (50-5000 mg kg-1 p.o.). Antinociceptive effect of BAE (50-1000 mg kg-1 p.o.) was evaluated using the acetic acid-induced abdominal constriction, acidic saline-induced muscle pain and formalin-induced pain models. The antinociceptive mechanism of BAE was also assessed using the formalin-induced pain model. RESULTS: The LD50 of BAE was thus estimated to be above 5000 mg kg-1 since none of the animals died in the acute toxicity study. Pretreatment with BAE (50-1000 mg kg-1 p.o.) significantly reduced the number of writhes after acetic-acid administration compared to the vehicle treated group. BAE also produced a significant and dose-dependent reversal of mechanical hyperalgesia induced by the injection of the acidic saline. Administration of BAE was able to significantly suppress both phases of the formalin test. This effect of the extract was however reversed by pretreatment with naloxone and granisetron. CONCLUSIONS: BAE exhibits antinociceptive effects in rodent pain models with a possible involvement of 5-HT3 receptors and opioidergic pathways.

Amphimas pterocarpoides harms.: An Evaluation of flavonoid and phenolic contents, wound healing, anthelmintic and antioxidant activities of the leaves and stem bark.

The present study evaluated the wound healing, anthelmintic and antioxidant potentials of crude methanol extracts and fractions (petroleum ether, ethyl acetate and methanol) of the leaves and stem bark of Amphimas pterocarpoides. Wound healing activity was determined by the dermal excision model in rats; anthelmintic activity was evaluated by the adult worm motility test using the adult Indian worm, Pheretima postuma. Total flavonoid, phenolic content and antioxidant activity were assessed by the aluminum chloride colorimetric, Folin Ciocalteu, 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and total antioxidant capacity (TAC) assays respectively. HPLC/UV fingerprints were developed for quality control. The maximum amount of phenolics and flavonoids were detected in the methanol fractions of the stem bark (225.0 ± 20.0 mg/g gallic acid equivalent (GAE) and 201.0 ± 1.41 mg/g quercetin equivalent (QCE) respectively) and leaves (84.54 ± 1.36 mg/g GAE and 130.7 ± 1.71 mg/g QCE, respectively). Both leaf and bark displayed remarkable free radical scavenging and TAC with the highest effect given by the methanol fractions. Significant (p < 0.05) wound contraction was achieved by topical application of the leaf (APL) and stem bark (APS) ointments (5-15%) with >90 % wound surface closure for 1% silver sulphadiazine, APS 15% and APL 10% treated groups by day 15. APL and APS demonstrated a concentration- and time-dependent paralysis and mortality of the P. posthuma with APL (6.25 mg/mL) causing worm paralysis at 82.60 min and death at 93 min, better than 10 mg/mL albendazole (paralysis at 76.30 min; death at 117 min). Tannins, triterpenoids, phytosterols, flavonoids, saponins and coumarins were detected in the leaves and bark. The results have proven the potential of A. pterocarpoides as a wound healing and anthelmintic agent, giving scientific credence to its use in traditional medicine.

Fruits of Vitex doniana sweet: toxicity profile, anti-inflammatory and antioxidant activities, and quantification of one of its bioactive constituents oleanolic acid.

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.

Antidepressant and Anxiolytic Effects and Subacute Toxicity of the Aerial Parts of Psychotria ankasensis J.B.Hall (Rubiaceae) in Murine Models.

BACKGROUND: The present study aimed at validating the traditional use and toxicity profile of a methanolic extract of the aerial parts of Psychotria ankasensis in alleviating depression and anxiety disorders. METHOD: The antidepressant effect of methanolic extract of Psychotria ankasensis (PAE 30, 100, and 300 mg/kg, p.o.) was assessed in mice using the forced swim test (FST) and the tail suspension test (TST). The plant's anxiolytic potential was also evaluated in mice using the elevated plus-maze (EPM) and the open field tests (OFT). The subacute toxicity was assessed via oral administration of PAE at doses of 100, 300, and 1000 mg/kg in rats for 28 days. RESULTS: PAE 100 and 300 mg/kg showed antidepressant-like properties by significantly (at least p < 0.05) decreasing the frequency and duration of immobility in FST and TST. PAE (100 and 300 mg/kg) also showed a significant (at least p < 0.05) anxiolytic effect in both EPM and OFT. In the EPM test, E max for PAE and diazepam were 92.52 ± 40.11% and 85.95 ± 45.92%, respectively, whereas E max was approximately 100% for both test drugs in the OFT. Subacute administration of PAE did not reveal any toxic effects with respect to organ weight index, haematological, serum biochemical, and histopathological parameters. CONCLUSIONS: Methanolic extract of P. ankasensis exhibited antidepressant-like and anxiolytic-like effects devoid of significant toxicity at the doses tested in murine models.

Investigating Ghanaian Allium Species for Anti-Infective and Resistance-Reversal Natural Product Leads to Mitigate Multidrug-Resistance in Tuberculosis.

The bulbs of Allium species are a known source of antibacterial phytochemicals. Anti-infective, efflux pump and biofilm inhibitory activities of bulb extracts of selected Ghanaian shallots Allium cepa var aggregatum were evaluated using the HT-SPOTi assay and other whole-cell phenotypic screening techniques to determine their possible mechanisms of action. Ethanol and aqueous extracts of white A. cepa inhibited the growth of Mycobacterium smegmatis mc2 155 and Escherichia coli, respectively. The majority of the Allium extracts significantly (p < 0.05) exhibited efflux pump inhibitory activity against all the acid-fast, Gram-positive and Gram-negative strains used. Hexane and chloroform extract of the pink A. cepa and the aqueous extract of the white A. cepa significantly inhibited M. smegmatis biofilm formation. For Pseudomonas aeruginosa, the inhibition was observed at 250 µg/mL for the aqueous extract (~77.34%) and 125 µg/mL for the hexane extract (~76.51%). The results suggest that Ghanaian shallots could potentially be useful when further developed to tackle antimicrobial resistance, particularly in tuberculosis (TB).

Alkaloidal extract from Zanthoxylum zanthoxyloides stimulates insulin secretion in normoglycemic and nicotinamide/streptozotocin-induced diabetic rats.

INTRODUCTION: Increase in the prevalence of type-2 diabetes in Sub-Sahara Africa has created the need for robust treatment and management programs. However, an effective diabetes management program requires a high annual budget that most countries in this region cannot afford. That said, various plants and plant products in this region have either been confirmed and/or ethnopharmacologically used for the management of type-2 diabetes. AIM: To investigate the antidiabetic and insulin secretory effects of an alkaloidal extract derived from Zanthoxylum zanthoxyloides in normoglycemic and experimental diabetic rats. MATERIALS AND METHODS: Alkaloidal extract was prepared from leaves of Z anthoxylum zanthoxyloides (ZZAE). Nicotinamide/streptozotocin-induced type-2 diabetes was modeled in male Sprague Dawley rats weighing between 130 to 150 g. The experimental diabetic rats were grouped into six treatment groups [Model, 20% Tween20, chlorpropamide, and ZZAE (50, 100, and 150 mg/kg)], and one control group. Fasting blood glucose (FBG), and body weight were measured weekly. Rats were sacrificed 2 days after treatment under chloroform anesthesia to collect blood samples and to isolate major organs for biochemical, and histological analyses respectively. Islets of Langerhans were isolated from normoglycemic rats and co-cultured with ZZAE and chlorpropamide (10 µg/mL) to assess the insulin secretory effect of ZZAE. RESULTS: ZZAE improved glucose kinetics curve in normoglycemic (p < 0.001) and experimental diabetic rats (p < 0.05) compared to the model. ZZAE (100 and 150 mg/kg) restored islets population, and improved kidney, and liver, histoarchitecture. ZZAE (150 mg/kg) improved post-treatment serum insulin levels compared to the model group (p < 0.001) and the Chlorpropamide group (p < 0.05). ZZAE also restored glycogen synthesis in skeletal muscles of experimental diabetic rats and stimulated insulin secretion in pancreatic islets of Langerhans isolated from normoglycemic rats. CONCLUSION: These results showed that ZZAE has active alkaloids that can be explored for diabetes management.

Myrianthus libericus: Possible mechanisms of hypoglycaemic action and in silico prediction of pharmacokinetics and toxicity profile of its bioactive metabolite, friedelan-3-one.

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 < 0.001) reduced the elevated blood glucose levels and corrected considerably (p < 0.01) the altered serum lipid profiles of the diabetic rats which was comparable to glibenclamide (5 mg/kg). Together with friedelan-3-one, the extract markedly inhibited the activity of α-amylase and promoted glucose uptake in C2C12 cells. Whereas MLB significantly (p < 0.001) up-regulated PI3K and PPARγ transcripts with a corresponding increase in GLUT-4 transcripts within the muscle cells, friedelan-3-one only up-regulated PI3K and GLUT-4 transcripts to promote glucose transport. Friedelan-3-one was shown to be non-carcinogenic, non-hepatotoxic, has decent oral bioavailability and a good compound for optimisation into a drug candidate. The study has demonstrated that MLB possess hypoglycaemic and anti-hyperlipidaemic activities and could be used as a therapeutic agent in the management of diabetes mellitus.

In vitro Anti-Mycobacterium ulcerans and cytotoxic activities of some selected medicinal plants and an indoloquinoline alkaloid.

Background: Buruli ulcer (BU) is a neglected tropical disease caused by the Mycobacterium ulcerans. BU is an endemic disease in many communities in sub-Saharan Africa where population have long history of using medicinal plants for treatment. Indeed, several medicinal plants have been documented against BU and related conditions. The present study was undertaken to prove the efficacy of seven medicinal plants documented for the treatment of mycobacterial infections and related symptoms in Ghana. Method: Antimycobacterial activity of the stem bark extracts and reference control drugs were conducted using the resazurin microtiter assay (REMA) assay method in clear round bottom 96-well microtiter plates. The extracts that showed anti-mycobacterium ulcerans activity were assessed for cytotoxicity using the Alamar blue assay. Results: Overall, The Cryptolepis sanguinolenta root aqueous extract exhibited the highest antimycobacterial activity (MIC=64 µg/mL) followed by Cleistopholis patens (MIC=256 µg/mL). Based on the marked activity of the Cryptolepis sanguinolenta extracts, pure cryptolepine, its major metabolite recorded a MIC value of 32 µg/mL. These extracts with considerable antimycobacterial activity showed 50% cytotoxic concentration (CC50) ranging from 94 to 384 µg/mL. Conclusions: Thus, Cleistopholis patens and Cryptolepis sanguinolenta are primed for further studies and could afford novel drugs for the mitigation of buruli ulcer disease.

Indigenous Medicinal Plants as Biofilm Inhibitors for the Mitigation of Antimicrobial Resistance.

The majority of indigenes in the rural areas of Ghana use herbal medicines for their primary health care. In this study, an ethnobotanical survey was undertaken to document medicinal plants used by traditional healers in the Ejisu-Juaben district in the Ashanti region of Ghana to treat infections and to further investigate the antibiofilm formation properties of selected plants in resisting pathogenic bacteria. Seventy medicinal plants used by traditional practitioners for the treatment of skin infections and wounds were documented from the ethnobotanical survey. Forty out of the seventy plants were collected and their methanol extracts evaluated for antimicrobial activity by the agar diffusion assay. Extracts that showed antibacterial activity were tested for biofilm inhibitory activity, and the most active plant was subsequently purified to obtain the active constituents. Biofilm formation was significantly mitigated by petroleum ether, ethyl acetate, and methanol extracts of Holarrhena floribunda stem bark. Bioassay-guided fractionation of an alkaloidal extract prepared from the methanol fraction led to the isolation of three steroidal alkaloids, namely, holonamine, holadienine, and conessine. The isolated compounds demonstrated varying degrees of biofilm formation inhibitory properties. The current study reveals that screening of indigenous medicinal plants could unravel potential leads to salvage the declining efficacy of conventional antibiotics. Holarrhena floribunda stem bark extract has strong biofilm formation inhibition properties, which could be attributed to the presence of steroidal alkaloids.

Flavanols and triterpenoids from Myrianthus arboreus ameliorate hyperglycaemia in streptozotocin-induced diabetic rats possibly via glucose uptake enhancement and α-amylase inhibition.

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-ß-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.

In Vivo Antiplasmodial Activity of Different Solvent Extracts of Myrianthus libericus Stem Bark and Its Constituents in Plasmodium berghei-Infected Mice.

The emergence and resurgence of P. falciparum resistance to generations of antimalarial drugs have prompted the search for new, effective, and safe antimalarial agents. This study aimed at investigating the in vivo antiplasmodial activity of the 70% hydroethanolic extract and constituents of the stem bark of Myrianthus libericus based on its ethnomedicinal use as an antimalarial agent. The antiplasmodial activity was assessed in Swiss albino mice employing the 4-day suppressive and Rane's tests. MLB significantly (p < 0.0001) suppressed parasitaemia by 52.26%, 65.40%, and 77.11% at 50, 100, and 200 mg·kg-1 doses, respectively, in the 4-day suppressive test. In Rane's test, the highest parasitaemia suppression of 72.50% was recorded at a dose of 200 mg·kg-1 of the extract. Fractionation of the bioactive ethyl acetate fraction by solvent-solvent partitioning and column chromatography led to the isolation of friedelan-3-one and stigmasterol being reported for the first time from this species. The compounds demonstrated remarkable antiplasmodial activity by suppressing parasitaemia by 65-72% in the suppressive test and 61-70% in the curative test at doses of 10-30 mg·kg-1. Both the extract and the isolated compounds significantly prolonged the survival time of infected mice and averted the cardinal signs associated with P. berghei-induced malaria including weight loss, hypothermia, and haemolysis. The results obtained confirm the prospect of M. libericus as an important source of new antimalarial compounds and justifies its folkloric use as an antimalarial agent.