New derivatives of tenvermectins through biotransformation as potential insecticides

Ge, Haixia; Zhang, Shaoyong; Guo, Huanyu; Qi, Huan; Wang, Ruijun; Xiang, Wensheng; Zhang, Liqin; Wang, Jidong

doi:10.1016/j.phytol.2022.02.004

Cited by 1 publication

(2 citation statements)

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“…Veterinary antiparasitic drugs, represented by ivermectin (IVM), have been widely used in clinical practice (Ge et al., 2022 ; Wan et al., 2017 ; Wang et al., 2016 ; Zhang et al., 2019 ; Zhang et al., 2022 ), but IVM has a long metabolic cycle leading to a large amount of drug residues in the faeces (Mckellar & Gokbulut, 2012 ); it slows down the rate of treating the animal manure by insects such as dung beetle (Ambrožová et al., 2021 ). Tenvermectin (TVM) is a novel 16‐membered macrolide compound isolated and purified from the fermentation broth of genetically engineered Streptomyces avermitilis strain MHJ1011 (Wan et al., 2017 ; Zhang et al., 2019 ).…”

Section: Introductionmentioning

confidence: 99%

“…Tenvermectin (TVM) is a novel 16‐membered macrolide compound isolated and purified from the fermentation broth of genetically engineered Streptomyces avermitilis strain MHJ1011 (Wan et al., 2017 ; Zhang et al., 2019 ). TVM is composed of two components: TVM A (25‐methyl‐22,23‐dihydro avermectin; R = CH 3 ) and TVM B (25‐ethyl‐22,23‐dihydro avermectin; R = C 2 H 5 ) (Ge et al., 2022 ) (Figure 1 ). There is a difference at the C25 site between these structures, with a methyl group for TVM A and an ethyl group for TVM B.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics of tenvermectin in swine, a novel antiparasitic drug candidate—comparison with ivermectin

Cao

Liu³

et al. 2023

Veterinary Medicine & Sci

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Tenvermectin (TVM) is a novel 16-membered macrolide compound isolated and purified from the fermentation broth of genetically engineered Streptomyces avermitilis strain MHJ1011. TVM and ivermectin were administered at the dose of 0.3 mg/kg body weight through a single subcutaneous injection route followed by plasma collectiom and analysis at different time intervals. Plasma concentrations of TVM and IVM were determined by high-performance liquid chromatography with fluorescence detector.Pharmacokinetic analysis was completed using the non-compartmental method with WinNonlin™ 6.4 software. TVM is rapidly absorbed after administration with peak plasma concentrations (C max , 9.78 ± 2.34 ng/ml) obtained within 6-22 h. AUC 0-last was 586.86 h⋅ng/ml ± 121.24 h⋅ng/ml. The mean elimination half-life of TVM (T 1/2λz ) was 97.99 h ± 46.41 h. The T 1/2λz of IVM was 146.59 h ± 22.26 h in the study. The present study showed that subcutaneous administration of TVM at 0.3 mg/kg body weight (BW) in swine is absorbed more rapidly than IVM in swine. Compared to the pharmacokinetic characteristics of IVM, there was little difference in the half-life of TVM among different individuals. The data will contribute to refining the formulation and dosage regime for TVM administration.

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