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Background Combretum paniculatum (Combretaceae) Vent. is commonly used in traditional medicine to treat ulcers and gastrointestinal disorders, including distended spleens and the liver. This study investigated the gastroprotective effects... more
Background Combretum paniculatum (Combretaceae) Vent. is commonly used in traditional medicine to treat ulcers and gastrointestinal disorders, including distended spleens and the liver. This study investigated the gastroprotective effects of C. paniculatum leaf extract and its fractions on absolute ethanol-induced gastric ulcers in rats and explored their effects on endogenous antioxidant (SOD, MDA, GSH, and Catalase) levels. Butanol, n-hexane, and ethyl acetate extracts (100 and 200 mg/kg), omeprazole (20 mg/kg), and control (3% Tween 80) were administered orally. Results The methanolic extract and fractions of C. paniculatum exhibited varying degrees of ulcer protection. MECP exhibited significant (P < 0.05) ulcer protection (55.56%) at 200 mg/kg; at 100 and 200 mg/kg, HFCP induced considerable (P < 0.01 & 0.001) ulcer reduction (64.44% and 80.00%), respectively; EAFCP offered substantial (P < 0.05) ulcer reduction (57.78%) at 200 mg/kg, whereas BFCP produced significant ...
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In the present study, the antimalarial activity of the extracts and fractions of the leaves of Persea americana and Dacryodes edulis as well as their phytochemical compositions were examined. Each of the extracts of the plants was... more
In the present study, the antimalarial activity of the extracts and fractions of the leaves of Persea americana and Dacryodes edulis as well as their phytochemical compositions were examined. Each of the extracts of the plants was successively fractionated to obtain hexane, ethyl acetate, methanol, and water fractions. The extracts and fractions were tested against Plasmodium berghei in both curative and suppressive antimalarial mouse models. Their major phytochemical composition was studied by the standard chemical tests and HPLC analysis. The extracts and fractions of P. americana and D. edulis demonstrated significant ( p < 0.05 ) maximal plasmodial inhibition as 52.16 ± 2.77% and 57.10 ± 1.98%, respectively, and chemosuppression of parasitemia as 64.01 ± 0.08% and 71.99 ± 0.06%, respectively. The major secondary metabolites identified in the plants include alkaloids, flavonoids, and saponins. It was concluded that P. americana and D. edulis possess promising antimalarial acti...
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Background: In most parts of the world, especially in underdeveloped countries, Acquired Immunodeficiency Syndrome (AIDS) still remains a major cause of death, disability and unfavorable economic outcomes. This has necessitated intensive... more
Background: In most parts of the world, especially in underdeveloped countries, Acquired Immunodeficiency Syndrome (AIDS) still remains a major cause of death, disability and unfavorable economic outcomes. This has necessitated intensive research to develop effective therapeutic agents for the treatment of Human Immunodeficiency Virus (HIV) infection, which is responsible for AIDS. Peptide cleavage by HIV-1 protease is an essential step in the replication of HIV-1. Thus, correct and timely prediction of the cleavage site of HIV-1 protease can significantly speed up and optimize the drug discovery process of novel HIV-1 protease inhibitors. In this work, we built and compared the performance of selected machine learning models for the prediction of HIV-1 protease cleavage site utilizing a hybrid of octapeptide sequence information comprising bond composition, amino acid binary profile (AABP), and physicochemical properties as numerical descriptors serving as input variables for some ...
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Background: The 2’-O-methyltransferase is responsible for the capping of SARS-CoV-2 mRNA and consequently the evasion of the host’s immune system. This study aims at identifying prospective natural inhibitors of the active site of... more
Background: The 2’-O-methyltransferase is responsible for the capping of SARS-CoV-2 mRNA and consequently the evasion of the host’s immune system. This study aims at identifying prospective natural inhibitors of the active site of SARS-CoV-2 2’O-methyltransferase (2’-OMT) through an in silico approach. Materials and methods: The target was docked against a library of natural compounds obtained from edible African plants using PyRx - virtual screening software. The antiviral agent, Dolutegravir which has a binding affinity score of -8.5 kcal mol−1 with the SARS-CoV-2 2’-OMT was used as a standard. Compounds were screened for bioavailability through the SWISSADME web server using their molecular descriptors. Screenings for pharmacokinetic properties and bioactivity were performed with PKCSM and Molinspiration web servers respectively. The PLIP and Fpocket webservers were used for the binding site analyses. The Galaxy webserver was used for simulating the time-resolved motions of the a...
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Dolichyl-phosphate N-acetylglucosaminephosphotransferase (dpagt1) inhibition is reported to kill tumor cells whose growth progression requires increased branching of N-linked glycans. Available dpagt1 inhibitors are grossly limited and... more
Dolichyl-phosphate N-acetylglucosaminephosphotransferase (dpagt1) inhibition is reported to kill tumor cells whose growth progression requires increased branching of N-linked glycans. Available dpagt1 inhibitors are grossly limited and are faced with problems of heamolytic effect and aqueous solubility thereby necessitating the search for new, safe and effective dpagt1 inhibitors. We employed computational methods to screen a dataset of ∼1300 FDA approved drugs in order to obtain theoretical dpagt1 inhibitors which could be repurposed as chemotherapeutic drugs. Top six better performing drugs, binding affinity for dpagt1 at the range of -17.63 to -20.40 kcal/mol, than the reference ligand (tunicamycin; -14.86 kcal/mol) were obtained at the end of structure-based-pharmacophore- and virtual-screening and 'induced fit' docking calculations. Analysis of their binding poses identified essential pharmacophores involved in target-ligand complexation that could be targeted in chemical modification to develop more effective and safe dpagt1 inhibitors.Communicated by Ramaswamy H. Sarma.
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The present study evaluated the wound healing activity of gel formulation of Albemoshus esculenta gumand Vernonia amygdalina Del. (Astereaceae) leaf extract. Cicatrin® antibiotic powder was used as standard wound healing formulation. Gels... more
The present study evaluated the wound healing activity of gel formulation of Albemoshus esculenta gumand Vernonia amygdalina Del. (Astereaceae) leaf extract. Cicatrin® antibiotic powder was used as standard wound healing formulation. Gels containing different proportions of A. esculenta gum: V. amygdalina leaf extract were prepared and all the formulations were evaluated using the excision wound model. Gel preparations were smeared on the wound of known diameter inflicted on the dorsumof albino rats. To determine the rate of wound healing, the diameter of each wound was measured daily for 15 days. The wound healing effects of the preparation were compared within the batches to find the proportion that healed faster and to that of Cicatrin®. In all the formulations, there was a progressive reduction in the wound diameter with time and there was a complete wound closure in all the gels formulated with the extracts by the 15th day. It was concluded that the gel formulations of V. amygd...
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The rate of psychoactive substance (PAS) use in the adolescent group is increasing around the world. Drug abuse has a negative impact on students’ education especially that of secondary school students. This study aimed to assess the... more
The rate of psychoactive substance (PAS) use in the adolescent group is increasing around the world. Drug abuse has a negative impact on students’ education especially that of secondary school students. This study aimed to assess the prevalence of psychoactive substance use and knowledge of the health consequences among secondary school students in Ogun State, Nigeria. A cross-sectional study was carried out among 528 consenting students selected using random sampling method. Data obtained using a validated modified World Health Organization’s guidelines questionnaire were analyzed with SPSS 20, p-Value ≤ 0.05 was considered significant. Majority (78.8%) were within the age group 15-18 years, males were 61.4%. Alcohol (95.0%) ranked first of all the substances been consumed among the current PAS users. Age was highly significantly associated with PAS use. Average knowledge of health consequences of PAS use was 11.5%. There is need for continuous health educational intervention to bo...
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Purpose: To evaluate the antimalarial effect of Ananas comosus extract and fractions and also to identify the likely bioactive compounds.Method: The fruit peel of the plant was extracted with methanol, and the extract successively... more
Purpose: To evaluate the antimalarial effect of Ananas comosus extract and fractions and also to identify the likely bioactive compounds.Method: The fruit peel of the plant was extracted with methanol, and the extract successively fractionated with n-hexane, dichloromethane, ethyl acetate, methanol and water. The n-hexane fraction was further subjected to vacuum liquid chromatography to afford four sub-fractions, one of which was also analyzed using gas chromatography-mass spectroscopy (GC-MS). Plasmodium berghei-infected mice were treated orally with three doses (100, 200 and 400 mg/kg) of the plant extract and a single dose (200 mg/kg) of each of the fractions and sub-fractions in a curative antimalarial model using artemisinin combination therapy (ACT) as the reference drug.Results: The extract exhibited significant (p < 0.001) non-dose dependent parasitemia inhibitory activity in the range of 44.84 to 76.09 %. All fractions displayed inhibitory effect (p < 0.001) in the ra...
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Malaria is one of the major health problems in developing countries. The disease kills a large number of people every year and also affects financial status of many countries. Resistance of the plasmodium parasite, the causative agent, to... more
Malaria is one of the major health problems in developing countries. The disease kills a large number of people every year and also affects financial status of many countries. Resistance of the plasmodium parasite, the causative agent, to the existing drugs, including chloroquine, mefloquine, and artemisinin based combination therapy (ACT), is a serious global issue in malaria treatment and control. This warrants an urgent quest for novel compounds, particularly from natural sources such as medicinal plants. Alkaloids have over the years been recognized as important phytoconstituents with interesting biological properties. In fact, the first successful antimalarial drug was quinine, an alkaloid, which was extracted from Cinchona tree. In the present review work, the alkaloids isolated and reported recently (2013 till 2019) to possess antimalarial activity are presented. Several classes of alkaloids, including terpenoidal, indole, bisindole, quinolone, and isoquinoline alkaloids, wer...
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Anti-inflammatory activity study involves developing a model that mimics, or provokes the production or release of, the biochemical mediators of inflammation, and monitoring the response of these biochemicals to the test drugs. This... more
Anti-inflammatory activity study involves developing a model that mimics, or provokes the production or release of, the biochemical mediators of inflammation, and monitoring the response of these biochemicals to the test drugs. This report constitutes an updated review of the in vitro and in vivo study models for assessing anti-inflammatory activity in plant extracts and synthetic drugs. The materials, instrumentation, and methods involved, as well as the mechanism of anti-inflammatory activity tested in each model, are extensively described. The merits and limitations of each method have also been discussed. A comparative assessment of the in vivo animal models vis-à-vis, the in vitro enzyme models have been made to assist scientists and researchers in the choice of assay method in terms of sensitivity, reliability, duration of test, ethical, and cost considerations.
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The present study was aimed at a comparative study of the phytoconstituents, antioxidant and antimicrobial properties of four medicinal plants, Ficus capensis, Aristolochia ringens, Albizia zygia and Lannea welwitschii. The leaf of F.... more
The present study was aimed at a comparative study of the phytoconstituents, antioxidant and antimicrobial properties of four medicinal plants, Ficus capensis, Aristolochia ringens, Albizia zygia and Lannea welwitschii. The leaf of F. capensis and stem bark of A. ringens, A. zygia and L. welwitschii were extracted using methanol. Phytochemical analysis was done spectrophotometrically. Three in vitro antioxidant tests-hydrogen peroxide (H2O2), nitric oxide (NO) and 2, 2-diphenyl-1-picrylhydroxyl (DPPH) scavenging models were employed. Antimicrobial test was done by agar diffusion method against E. coli, Staphylococcus aureus, Klebsiela pneumonia, Bacillus subtilis, Pseudomonas aeruginosa, Salmonella typhi, Candida albicans and Aspergittus spp. Phytochemical analysis revealed that the most abundant phytoconstituents were flavonoids (F. capensis and A. zygia), reducing sugar, terpenoids, alkaloids and tannins. In the antioxidant models, A. zygia was found to produce the least IC50 in t...
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People living with diabetes mellitus across the world are expected to rise to 592 million by 2035 and the pandemic disease is worst in the developing countries like Nigeria, where the cost of treating/managing diabetes mellitus is... more
People living with diabetes mellitus across the world are expected to rise to 592 million by 2035 and the pandemic disease is worst in the developing countries like Nigeria, where the cost of treating/managing diabetes mellitus is relatively out of the reach of many diabetic patients. The study investigated the effect of Anogeissus leiocarpus Guill and Perr ethanolic leaf extract on blood glucose and other biochemical indices in alloxan-induced diabetic adult male Wistar albino rats. Diabetes mellitus was induced in overnight-fasted rats by a single intraperitoneal injection of alloxan monohydrate (150 mg/kg body weight). Diabetic rats were then treated with the extract for 14 days. Blood glucose, lipid profile and liver glycogen levels were determined. After the treatment with the extract, the fasting blood glucose levels significantly reduced (p < 0.05) in treated diabetic rats (62.2 ± 18.4 mg/dl) compared to untreated diabetic rats (73.8± 8.2 mg/dl). There was also significant...
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Diabetes mellitus remains a global health challenge and herbal medicines are known to be effective and safe for use in its management. Anthocleista nobilis is used in the traditional management of the disorder but this claimed use has not... more
Diabetes mellitus remains a global health challenge and herbal medicines are known to be effective and safe for use in its management. Anthocleista nobilis is used in the traditional management of the disorder but this claimed use has not been validated. The present study was designed to establish and hence validate the use of the plant for the management of diabetes and also identify the bioactive phytoconstituents of the plant. The root and stem bark extracts of the plant were investigated for antidiabetic activity in alloxan-induced diabetic rats. The animals were treated orally with 100, 200 and 400 mg/kg bw of both extracts for seven days. The fasting blood glucose concentration (FBGC) of the animals was monitored for seven days with a glucometer. Ultra-high performance liquid chromatography/electrospray ionization-quadrupole time-of-flight mass spectrometric (UHPLC/ESI-QTOF-MS) technique was adopted for partial dereplication of secondary metabolites of the plant. The extracts ...
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Background: Respiratory syncytial virus (RSV) is known to cause severe respiratory infections particularly in infants younger than 2 years of age. The only approved drug, ribavirin, is expensive and is not likely to improve therapeutic... more
Background: Respiratory syncytial virus (RSV) is known to cause severe respiratory infections particularly in infants younger than 2 years of age. The only approved drug, ribavirin, is expensive and is not likely to improve therapeutic outcome, thereby necessitating the search for safer and more potent alternatives from natural sources such as endophytic fungi. The present study aimed to investigate the anti-RSV activity of compounds from endophytic fungi. Methods: Two endophytic fungi Colletotrichum gloeosporioides and Pestalotiopsis thea were isolated from the fresh leaves of the host Nigerian plants Anthocleista djalonensis and Fagara zanthoxyloides, respectively. After fermentation in solid rice media, C. gloeosporioides afforded 4 known compounds 4-hydroxybenzoic acid (1), vanillic acid (2), ferulic acid (3) and Nb-acetyltryptamine (4) while P. thea afforded 3 known compounds chloroisosulochrin (5), ficipyrone A (6) and pestheic acid (7). The compounds were investigated for their anti-RSV activity using the HEP-2 cell lines and ribavirin as the standard drug. Results: Compound 5 was found to show the strongest inhibition of the RSV with IC50 of 4.22±1.03 µM (ribavirin 4.91±1.85 µM). Other compounds showed moderate inhibition of the virus (IC50 ranging from 45.00±0.98 to 259.23±2.36 µM). Conclusion: The results of the present study have shown that chloroisosulochrin (5), isolated from an endophytic fungus P. thea, possesses strong activity against RSV.
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This study investigated the antidiabetic activity of the various combinations (ratios) of metformin (50 mg/kg) and aqueous extracts of the leaves of Vernonia amygdalina (100 mg/kg). The ratios of Extract to Metformin were 1:1, 2 1, and... more
This study investigated the antidiabetic activity of the various combinations (ratios) of metformin (50 mg/kg) and aqueous extracts of the leaves of Vernonia amygdalina (100 mg/kg). The ratios of Extract to Metformin were 1:1, 2 1, and 2:1 and distilled water (control, p.o.) were given to both normoglycemic and alloxan-induced diabetic Wister albino rats. Blood was withdrawn and tested at 0, 1, 3 and 6 hours. Results showed that the combinations of the extract and metformin caused more reduction in glycemia compared to any of the agents acting alone in either of the two categories of animals. The ratio of 1:2 caused the most significant (p<0.05) reduction in blood sugar (-66.07%) compared to distilled water (-7.2%). However, the ratio of metformin: extract (2:1) caused a reduction of -62.66% but was found a better combination considering the safety of the drugs. The combination of Vernonia amygdalina with metformin for the management of diabetes should be highly encouraged with a...
This study investigated the antidiabetic activity of the various combinations (ratios) of metformin (50 mg/kg) and aqueous extracts of the leaves of Vernonia amygdalina (100 mg/kg). The ratios of Extract to Metformin were 1:1, 2 1, and... more
This study investigated the antidiabetic activity of the various combinations (ratios) of metformin (50 mg/kg) and aqueous extracts of the leaves of Vernonia amygdalina (100 mg/kg). The ratios of Extract to Metformin were 1:1, 2 1, and 2:1 and distilled water (control, p.o.) were given to both normoglycemic and alloxan-induced diabetic Wister albino rats. Blood was withdrawn and tested at 0, 1, 3 and 6 hours. Results showed that the combinations of the extract and metformin caused more reduction in glycemia compared to any of the agents acting alone in either of the two categories of animals. The ratio of 1:2 caused the most significant (p%0.05) reduction in blood sugar (-66.07%) compared to distilled water (-7.2%). However, the ratio of metformin: extract (2:1) caused a reduction of -62.66% but was found a better combination considering the safety of the drugs. The combination of Vernonia amygdalina with metformin for the management of diabetes should be highly encouraged with a re...
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Medicinal plants have been the basis of treatment of various diseases in African traditional medicine as well as other forms of treatment from diverse cultures of the world. About 80% of the world’s population still depends solely on... more
Medicinal plants have been the basis of treatment of various diseases in African traditional medicine as well as other forms of treatment from diverse cultures of the world. About 80% of the world’s population still depends solely on traditional or herbal medicine for treatment of diseases, mostly in Africa and other developing nations. Most of the potent medicinal plants have relatively no toxic or adverse effects when used by humans, while some are very toxic to both humans and animals with the potential of damaging certain organs in the body. This calls for caution in the use of medicinal plants of which the use is presently on the increase due to easy availability, affordability, accessibility, and promising efficacy comparable to the often high cost and adverse effects of standard synthetic drug agents. This chapter highlights some safe medicinal plants with good toxicological profile in laboratory animals and/or cell culture experiment that are qualified for clinical trials in humans. Several medicinal plants were evaluated for their good toxicological profile using online research. After much screening, only those medicinal plants without serious toxic effects in animals and cell culture experiments were chosen and precisely discussed.
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Malaria is a serious public health problem especially in sub-Saharan African countries such as Nigeria. The causative parasite is increasingly developing resistance to the existing drugs. There is urgent need for alternative and... more
Malaria is a serious public health problem especially in sub-Saharan African countries such as Nigeria. The causative parasite is increasingly developing resistance to the existing drugs. There is urgent need for alternative and affordable therapy from medicinal plants which have been used by the indigenous people for many years. This study was conducted to document the medicinal plant species traditionally used by the people of Nsukka Local Government Area in south-eastern Nigeria for the treatment of malaria. A total of 213 respondents, represented by women (59.2%) and men (40.8%), were interviewed using a semi-structured questionnaire. The results were analysed and discussed in the context of previously published information on anti-malarial and phytochemical studies of the identified plants. The survey revealed that 50 plant species belonging to 30 botanical families were used in this region for the treatment of malaria. The most cited families were Apocynaceae (13.3%), Annonace...
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The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management of diabetes mellitus. Though some compounds have been isolated from it, the antidiabetic principles have not been identified. The present... more
The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management of diabetes mellitus. Though some compounds have been isolated from it, the antidiabetic principles have not been identified. The present study was designed to evaluate the chemical constituents from the root of C. dolichopetalum with a view to identifying the antidiabetic principles. The constituents include the alkaloids, echinulin (1) and arestrictin B (2), the terpenoids, arjunolic acid (3) and 4'-dihydrophaseic acid (4) as well as the phenolic acids, ellagic acid (5) and 3, 4, 3'-tri-O-methylellagic acid (6). Twenty eight mice (in seven groups, n = 4) were made diabetic using alloxan monohydrate (i.p., 120 mg/kg) and treated orally with either the vehicle (control group), any of the constituents or glibenclamide (standard drug). The fasting blood glucose of the diabetic animals was monitored for nine hours. Results showed that all the chemical constituents (1-6) exhibited sig...
The fungal extract as well as the 3 biosynthetic compounds, (S)-(+)-2-cis-4-trans-abscisic acid (1), , 7&#39;-hydroxy-abscisic acid (2) and 4-des-hydroxyl altersolanol A (3) from the endophytic fungus, Nigrospora oryzae, isolated from... more
The fungal extract as well as the 3 biosynthetic compounds, (S)-(+)-2-cis-4-trans-abscisic acid (1), , 7&#39;-hydroxy-abscisic acid (2) and 4-des-hydroxyl altersolanol A (3) from the endophytic fungus, Nigrospora oryzae, isolated from Combretum dolichopetalum leaf were investigated for their antidiabetic potential.The antidiabetic activity was determined in alloxan-induced diabetic mice by monitoring their fasting blood sugar for 9 h.The extract and the compounds (1-3) significantly (p&lt;0.001) reduced the fasting blood sugar of the diabetic mice.The present study has shown that the biosynthetic products of the endophytic fungus, N. oryzae, exhibited strong antidiabetic activity. It has further shown that endophytic fungi could be an alternative source of novel compounds for management of diabetes.