Currently, there is no known cure for diabetes. Different pharmaceutical therapies have been approved for the management of type 2 diabetes mellitus (T2DM), some are in clinical trials and they have been classified according to their route or mechanism of action. Insulin types, sulfonylureas, biguanides, alpha-glucosidase inhibitors, thiazolidinediones, meglitinides, sodium–glucose cotransporter type 2 inhibitors, and incretin-dependent therapies (glucagon-like peptide-1 receptor agonists: GLP-1R, and dipeptidyl peptidase 4 inhibitors: DPP-4). Although some of the currently available drugs are effective in the management of T2DM, the side effects resulting from prolonged use of these drugs remain a serious challenge. GLP-1R agonists are currently the preferred medications to include when oral metformin alone is insufficient to manage T2DM. Medicinal plants now play prominent roles in the management of various diseases globally because they are readily available and affordable as well as having limited and transient side effects. Recently, studies have reported the ability of phytochemicals to activate glucagon-like peptide-1 receptor (GLP-1R), acting as an agonist just like the GLP-1R agonist with beneficial effects in the management of T2DM. Consequently, we propose that careful exploration of phytochemicals for the development of novel therapeutic candidates as GLP-1R agonists will be a welcome breakthrough in the management of T2DM and the co-morbidities associated with T2DM.

Skin aging and wrinkle formation are processes that are largely influenced by the overexpression of enzymes like tyrosinase, elastase, and collagenase. This study aimed to validate the skin anti-aging properties of phytochemicals from Peperomia pellucida (PP) as well as its attendant mechanism of action. Compounds previously characterized from PP were retrieved from the PubChem database and docked to the active sites of tyrosinase, elastase, and collagenase using Schrödinger’s Maestro 11.5 and AutoDock tools to predict compounds with the best inhibitory potential to block these enzymes in preventing skin aging. It was observed that our hit compounds had favorable affinity and displayed key interactions at the active sites of these enzymes similar to those of the standards. With elastase, we observed key interactions with the amino acids in the S1 sub-pocket (especially ALA-181), Zn chelation, and histidine residues, which are key for inhibitory activity and ligand stability. The hit compounds showed H-bonds with the key amino acids of collagenase, including LEU-185 and ALA-186; phlobaphene and patuloside B were found to have better docking scores and inhibition constants (Ki) (−12.36 Kcal/mol, 0.87 nM and −12.06 Kcal/mol, 1.45 nM, respectively) when compared with those of the synthetic reference compound (−12.00 Kcal/mol, 1.67 nM). For tyrosinase, our hit compounds had both better docking scores and Ki values than kojic acid, with patuloside B and procyanidin having the best values of −9.43 Kcal/mol, 121.40 nM and −9.32 Kcal/mol, 193.48 nM, respectively (kojic acid = −8.19 Kcal/mol, 898.03 nM). Based on this study, we propose that acacetin, procyanidin, phlobaphene, patulosides A and B, palmitic acid, and hexahydroxydiphenic acid are responsible for the anti-aging effects of PP on the skin, and that they work synergistically through a multi-target inhibition of these enzymes.

The burden of human schistosomiasis, a known but neglected tropical disease in Sub-Saharan Africa, has been worrisome in recent years. It is becoming increasingly difficult to tackle schistosomiasis with praziquantel, a drug known to be effective against all Schistosoma species, due to reports of reduced efficacy and resistance. Therefore, this study seeks to investigate the antischistosomal potential of phytochemicals from Azadirachta indica against proteins that have been implicated as druggable targets for the treatment of schistosomiasis using computational techniques. In this study, sixty-three (63) previously isolated and characterized phytochemicals from A. indica were identified from the literature and retrieved from the PubChem database. In silico screening was conducted to assess the inhibitory potential of these phytochemicals against three receptors (Schistosoma mansoni Thioredoxin glutathione reductase, dihydroorotate dehydrogenase, and Arginase) that may serve as therapeutic targets for schistosomiasis treatment. Molecular docking, ADMET prediction, ligand interaction, MMGBSA, and molecular dynamics simulation of the hit compounds were conducted using the Schrodinger molecular drug discovery suite. The results show that Andrographolide possesses a satisfactory pharmacokinetic profile, does not violate the Lipinski rule of five, binds with favourable affinity with the receptors, and interacts with key amino acids at the active site. Importantly, its interaction with dihydroorotate dehydrogenase, an enzyme responsible for the catalysis of the de novo pyrimidine nucleotide biosynthetic pathway rate-limiting step, shows a glide score and MMGBSA of −10.19 and −45.75 Kcal/mol, respectively. In addition, the MD simulation shows its stability at the active site of the receptor. Overall, this study revealed that Andrographolide from Azadirachta indica could serve as a potential lead compound for the development of an anti-schistosomal drug.

Diabetes is a group of medical conditions characterized by the body's inability to effectively control blood glucose levels, due to either insufficient insulin synthesis in type 1 diabetes or inadequate insulin sensitivity in type 2 diabetes. According to this research, the PI3K/AKT pathway of Ocimum gratissimum leaf flavonoid-rich extracts in streptozotocin-induced diabetic rats was studied. We purchased and used a total of forty (40) male Wistar rats for the study. We divided the animals into five (5) different groups: normal control (Group A), diabetic control (Group B), low dose (150 mg/kg body weight) of Ocimum gratissimum flavonoid-rich leaf extract (LDOGFL) (Group C), high dose (300 mg/kg body weight) of Ocimum gratissimum flavonoid-rich leaf extract (HDOGFL) (Group D), and 200 mg/kg of metformin (MET) (Group E). Streptozotocin induced all groups except Group A, which serves as the normal control group. The experiment lasted for 21 days, following which we sacrificed the animals and harvested their brains for biochemical analysis on the 22nd day. We carried out an analysis that included reduced glutathione (GSH), glutathione transferases (GST), catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD), along with GLUT4, MDA, pro-inflammatory cytokines, NO, neurotransmitters, cholinergic enzyme activities, cardiolipin, and the gene expression of PI3K/AKT. The obtained result indicates that the flavonoid-rich extracts of O. gratissimum significantly enhanced the levels of GSH, GST, CAT, GPx, and SOD, as well as GLUT4 and cardiolipin. The levels of GSH, GST, CAT, GPx, and SOD, as well as GLUT4 and cardiolipin, were significantly increased by gratissimum. Moreover, the extracts decrease the levels of MDA, pro-inflammatory cytokines, NO, neurotransmitters, and cholinergic enzyme activities. Additionally, the flavonoid-rich extracts of O. gratissimum significantly improved the AKT and PI3K gene expressions in diabetic rats. gratissimum had their AKT and PI3K gene expressions significantly (p < 0.05) improved. The findings indicate that O. gratissimum leaf flavonoids have the potential to treat diabetes mellitus. gratissimum leaf flavonoids possess therapeutic potential in themselves and can be applied in the management of diabetes mellitus. Although further analysis can be carried out in terms of isolating, profiling, or purifying the active compounds present in the plant's extract.

Background: Datura contains a mixture of anticholinergic agents (alkaloids such as atropine, scopolamine and hyoscyamine) that are responsible for its pharmacological actions. The objective was to evaluate the effect of Datura stramonium in the testes of wistar rats. Methods: Twenty (20) adult male rats weight ranging from 106g-180g were distributed into five groups (A-E) of four (4) animals each. Animals were administered with Datura extract once daily for 21 days as Group A- 50mg/kg, Group B -100 mg/kg, Group C -200 mg/kg ,Group D -400 mg/kg. While, Group E were given distilled water daily. Testes and blood samples were collected from all the groups, for the histological and biochemical activities. Result: Results showed overall, increase in body weight with siginificant differences in sperm count in all the treatment groups. Administration of high dose of Datura extract was found to have adverse effect on the histological findings in the testes. Extract of Datura stramonium plant is toxic since single extraction shows presence of scopolamine. Abuse of the flower of the plant pose cholinergic poisoning due to scopolamine, significantly reduces male fertility evidenced by increase in the number of abnormal sperm motility and altered testicular morphology.

Oxidative injury or cellular damage arising from free radicals or reactive oxygen species (ROS) has been implicated in the pathogenesis of many human diseases. These ROS are generated through normal metabolism of drugs, environmental chemicals and other xenobiotics as well as endogenous chemicals. Accumulated evidence suggests that ROS can be scavenged through chemoprevention utilizing natural antioxidant compounds present in foods and medicinal plants. The aim of this study is to evaluate antioxidant activities of aqueous extract of Bryophyllum pinnatum using carbon tetrachloride-induced albino rats as model. An in-vivo antioxidant activity was carried out on the CCl4 induced rats by administration of aqueous extract of Bryophyllum pinnatum at doses of 50, 100 and 200mg/Kg bw for 14 consecutive days, and one group was treated with Silymarin at a dose of 50 mg/Kg as a standard drug. The antioxidant activities were estimated by evaluating its effects on antioxidant parameters in the tissues of albino rats (Serum, Liver and Heart). The activity of catalase (CAT), Superoxide dismutase (SOD), Glutathione peroxidase (GPx) and the levels of MDA and GSH were evaluated in tissue homogenates. Results showed that the rats fed with the higher concentrations of Bryophyllum pinnatum had significant increase (p<0.05) in glutathione content (GSH), GPx, SOD and catalase activities relative to normal and standard control. However, the level of MDA was decreased (p<0.05) for the treated groups (100 and 200mg/kg). These results suggest that aqueous extracts of Bryophyllum pinnatum has active substances contributing to varied degrees of potent antioxidant activity and could serve as important source of antioxidants in food, cosmetics and pharmaceutical industries. Keywords: Oxidative injury, Bryophyllum pinnatum, antioxidant, Diseases, Tissues