Aladodo A Raliat, Ibrahim Ibrahim O, Sabiu Saheed
Department of Medical Biochemistry and Pharmacology, Faculty of Pure and Applied Sciences, Kwara State University, Malete, Nigeria.
Department of Biotechnology and Food Science, Durban University of Technology, Durban, South Africa.
Evid Based Complement Alternat Med. 2022 Jul 15;2022:4388941. doi: 10.1155/2022/4388941. eCollection 2022.
This study investigated the toxicological implications of a commercial polyherbal formulation, KWAPF01. Twenty-four Wistar rats were randomized into six groups of four animals per group. The animals in Group 1 were administered placebo and designated as control, while the rats in Groups 2 to 6 were administered 1000, 1500, 2000, 2500, and 3000 mg/kg bodyweight single oral dose of KWAPF01, respectively, and subsequently monitored for gross morphological and behavioural changes for 72 h. Piloerection, reduced motility, and tremor were observed in experimental groups, and the median lethal dose (LD) of the extract was 2225.94 mg/kg bodyweight. The 11 compounds identified through HPLC analysis of the extract were docked against acetylcholinesterase (AChE), and the docking scores ranged from -5.3 to -10.8 kcal/mol, with catechol (-5.3 kcal/mol) and berberine (-10.8 kcal/mol) having the highest and lowest binding energies, respectively. Judging by the results, it could be inferred that some of the constituents of KWAPF01 have a direct impact on the nervous system and this is possibly elicited via the cholinergic system as it contains a nicotinic acetylcholine receptors agonist and potential inhibitors of AChE. Therefore, the use of KWAPF01 needs to be cautiously guided.
本研究调查了一种商业多草药配方KWAPF01的毒理学影响。将24只Wistar大鼠随机分为6组，每组4只动物。第1组动物给予安慰剂并指定为对照组，而第2至6组大鼠分别给予1000、1500、2000、2500和3000 mg/kg体重的KWAPF01单次口服剂量，随后监测72小时的大体形态和行为变化。实验组观察到竖毛、运动减少和震颤，提取物的半数致死剂量（LD）为2225.94 mg/kg体重。通过对提取物的HPLC分析鉴定出的11种化合物与乙酰胆碱酯酶（AChE）进行对接，对接分数范围为-5.3至-10.8 kcal/mol，儿茶酚（-5.3 kcal/mol）和小檗碱（-10.8 kcal/mol）分别具有最高和最低结合能。从结果判断，可以推断KWAPF01的一些成分对神经系统有直接影响，这可能是通过胆碱能系统引发的，因为它含有烟碱型乙酰胆碱受体激动剂和AChE的潜在抑制剂。因此，KWAPF01的使用需要谨慎指导。
