Abstract
Avermectins are a group of drugs that occurs naturally as a product of fermenting Streptomyces avermitilis, 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.
Highlights
Avermectins are a group of drugs with a multiple treatment target
Avermectins are generally soluble in organic solvents, such as ethanol, chloroform, diethyl ether, ethyl acetate
The lack of ivermectin effect on P. falciparum in vitro might be due to the absence of the glutamate-gated chloride channel and GABA-gated chloride channels in P. falciparum where ivermectin binds to insects [104,105] it was reported that ivermectin has no significant effect on P. falciparum at the blood stage of development in vitro, while the possible mechanism of ivermectin in inhibiting the parasite at the blood stage might be by blocking nucleo-cytoplasmic shuttling of P. falciparum signal transduction particle (SRP) components [104]
Summary
Avermectins are a group of drugs with a multiple treatment target. They are generally used as a pesticide for the treatment of pests and parasitic worms as a result of their anthelmintic and insecticidal properties [1]. Eight different structures were isolated and divided into four major components (A1a, A2a, B1a and B2a) and four minor components (A1b, A2b, B1b, and B2b). Examples of avermectins include ivermectin, abamectin, doramectin, eprinomectin, moxidectin, and selamectin [2]. Their structures share similarity with antibacterial macrolides and antifungal macrocyclic polygenes but differ in the mechanism of action [3]
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