Résumé
Background: Computer-aided repositioning of approved drugs is an increasingly popular strategy for the discovery of effective therapies. The potency of the newly repositioned drugs can be optimized using them as a component of an effective drug combination, thereby achieving the desired therapeutic effect at a lower and more tolerable drug concentration. Aim and Objectives: The aim of the study was to perform structure-based virtual screening and repurposing of FDA-approved drugs for the treatment of methicillin resistance by Staphylococcus aureus (SA) and perform an in vitro validation of the prediction. Materials and Methods: Following ethical clearance at the Department of Pharmacology and Therapeutics, College of Health Sciences, Usmanu Danfodiyo University Sokoto, molecular docking was performed against 5 validated protein targets involved in the development of methicillin resistance by SA and an in vitro validation of the prediction was done using 3 of the top-ranking drug candidates against methicillin-resistant vancomycin-susceptible strain of the pathogen (ATCC 43300). Results: Desmopressin and docetaxel, two of the 20 top-ranking repurposed drugs discovered through virtual screening, enhanced the inhibitory effect of oxacillin against the ATCC 43300 SA strain in a ratio-dependent manner, although each of the two drugs singly was only weakly effective against the bacterial strain. The standard drug, vancomycin (also among the top-scoring candidates), alone, was effective against ATCC 43300 strain and in combination with oxacillin, the two drugs produced a ratio-dependent synergistic effect against the bacterial strain. Conclusion: These findings suggest that oxacillin-based combinations with desmopressin, docetaxel, and the standard drug vancomycin, three of the 20 top-ranking drugs, at optimum ratios, may be beneficial in reversing the resistance of the ATCC 43300 SA strain to oxacillin, thus supporting the prediction of the molecular docking results.
Résumé
Objectives: Leptadenia hastata (Pers) Decne (Apocynaceae) is a common medicinal plant used in northern Nigeria either singly or together with conventional drugs to treat diabetes. This study investigated the influence of concurrent administration of the methanol leaf extract of L. hastata with metformin in streptozotocin/ nicotinamide-induced diabetic rats. Materials and Methods: Possible synergistic activity between the extract and metformin was assessed using 3 models of synergy analysis (Loewe additivity, Bliss independent and highest single agent [HSA] models). Eleven groups of Wistar rats (eight animals per group) consisting of ten groups of diabetic rats and one normal control group were used in this study. Six groups were administered with either the extract or metformin at three different doses each (50, 150 and 500 mg/kg for the extract and 30, 100 and 300 mg/kg for metformin), while another three groups were co-administered with the extract and metformin at three different ratios each (50 mg/kg: 30 mg/ kg, 150 mg/kg: 100 mg/kg and 500 mg/kg: 300 mg/kg). An oral glucose tolerance test (OGTT) was conducted at baseline and on day 14. Result: The results revealed that the extract-metformin combination brought about a synergistic reduction in the total area under the OGTT curve (based on Loewe and HSA models) as well as a synergistic reduction in blood glucose (based on Loewe, Bliss and HSA models). Conclusion: The methanol leaf extract of L. hastata produced a synergistic antidiabetic activity in streptozotocin/ nicotinamide-induced diabetic rats when combined with metformin.
Résumé
Background: Benign prostatic hyperplasia (BPH) represents one of the most prevalent urological disorders among older men. Medicinal plants have been used since antiquity in treating various types of human illnesses, including prostatic diseases. Despite the plethora of published ethnobotanical surveys on Nigerian medicinal plants for treating various diseases, there is a paucity of such research in the country with respect to botanical agents used in treating BPH. Aims and Objectives: The present study is aimed at obtaining ethnobotanical information regarding the use of herbs by the residents of Sokoto metropolis in the treatment of BPH. Materials and Methods: After permission from departmental ethics committee, an ethnobotanical survey was conducted on medicinal plants utilised for the treatment of prostatic hyperplasia in Sokoto state, North Western Nigeria using semistructured oral interviews. Results: Findings from this survey showed a total of 44 plant species belonging to 22 families. Among the species, Cassia sieberiana DC., Detarium microcarpum Guill. and Perr. and Lawsonia inermis L. were the most commonly utilised. The part most commonly used for BPH are the stembark, followed by the roots. Seeds, leaves, and bulbs were found to be infrequently used. Irrespective of the plant parts used water was the most frequently employed medium of extraction. Though less popular, fermented milk, fermented milk-millet mixture, and a traditional cereal-based beverage were also employed. The most common modes of preparation were decoctions and infusions, while oral was the main route of administration. Conclusion: This survey documented 44 plant species used traditionally in Sokoto metropolis as a remedy for BPH. Further studies are recommended to confirm the efficacy and evaluate the mechanisms of action of standardized formulations of the herbal recipes individually and in combination.
Résumé
Background: Benign prostatic hyperplasia (BPH) is defined as a progressive nonmalignant enlargement of smooth muscle and epithelial cells in the prostate. A lot of studies have been published on the efficacy and safety of phytotherapeutic agents against BPH, making it a daunting task to review comprehensively. Aim and Objectives: The present article aimed to review the existing systematic reviews of primary studies on the subject. Google Scholar and PubMed databases were used in searching the articles. Materials and Methods: After permission from the departmental ethics committee, the quality of the retrieved articles was assessed using a revised assessment of multiple systematic reviews scale. Results: Sixteen reviews were included, with the majority (11 out of 16) focusing on Serenoa repens extracts. Such evidence for other phytotherapeutic agents studied is either limited, conflicting, or lacking. Issues about the primary studies included in the reviews were discussed and some recommendations presented. Conclusion: The reviews that focused on the most widely studied hexanic extract of S. repens, Permixon, were consistent in their conclusions that the extract is beneficial in improving the symptoms of BPH.