El-Saber Batiha Gaber, Alqahtani Ali, Ilesanmi Omotayo B, Saati Abdullah A, El-Mleeh Amany, Hetta Helal F, Magdy Beshbishy Amany
Department of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour University, Damanhour 22511, Egypt.
Department of Pharmacology, College of Pharmacy, King Khalid University, Guraiger, Abha 62529, Saudi Arabia.
Pharmaceuticals (Basel). 2020 Aug 17;13(8):196. doi: 10.3390/ph13080196.
Avermectins are a group of drugs that occurs naturally as a product of fermenting , an actinomycetes, isolated from the soil. Eight different structures, including ivermectin, abamectin, doramectin, eprinomectin, moxidectin, and selamectin, were isolated and divided into four major components (A1a, A2a, B1a and B2a) and four minor components (A1b, A2b, B1b, and B2b). Avermectins are generally used as a pesticide for the treatment of pests and parasitic worms as a result of their anthelmintic and insecticidal properties. Additionally, they possess anticancer, anti-diabetic, antiviral, antifungal, and are used for treatment of several metabolic disorders. Avermectin generally works by preventing the transmission of electrical impulse in the muscle and nerves of invertebrates, by amplifying the glutamate effects on the invertebrates-specific gated chloride channel. Avermectin has unwanted effects or reactions, especially when administered indiscriminately, which include respiratory failure, hypotension, and coma. The current review examines the mechanism of actions, biosynthesis, safety, pharmacokinetics, biological toxicity and activities of avermectins.
阿维菌素是一类通过发酵从土壤中分离出的放线菌天然产生的药物。已分离出包括伊维菌素、阿维菌素、多拉菌素、埃普利诺菌素、莫西菌素和塞拉菌素在内的8种不同结构，并分为4种主要成分（A1a、A2a、B1a和B2a）和4种次要成分（A1b、A2b、B1b和B2b）。由于其驱虫和杀虫特性，阿维菌素通常用作治疗害虫和寄生虫的杀虫剂。此外，它们具有抗癌、抗糖尿病、抗病毒、抗真菌作用，并用于治疗多种代谢紊乱。阿维菌素通常通过放大谷氨酸对无脊椎动物特异性门控氯离子通道的作用，来阻止无脊椎动物肌肉和神经中的电冲动传递。阿维菌素有不良影响或反应，尤其是在滥用时，包括呼吸衰竭、低血压和昏迷。本综述研究了阿维菌素的作用机制、生物合成、安全性、药代动力学、生物毒性和活性。
