阿维菌素B2聚硅氧烷微球的制备及生物活性评价  

Preparation and biological activity evaluation of avermectin B2 polysiloxane microspheres

作　　者：黄佩然 江定心[1] HUANG Peiran;JIANG Dingxin(National Key Laboratory of Green Pesticide,Key Laboratory of Natural Pesticide and Chemical Biology,Ministry of Education,South China Agricultural University,Guangzhou 510642,China)

机构地区：[1]华南农业大学绿色农药全国重点实验室天然农药与化学生物学教育部重点实验室,广州510642

出　　处：《农药》2024年第3期174-180,共7页Agrochemicals

基　　金：国家自然科学基金(32372576);广东省基础与应用基础研究基金(2021A1515011277);广东省企业科技特派员专项(GDKTP2021024200)。

摘　　要：[目的]为了利用阿维菌素B1(AVMB1)发酵过程中产生的20%~30%低活性阿维菌素B2(AVMB2)化合物,针对AVMB2易光解和残效期短的缺点,制备防紫外光降解的控释AVMB2聚硅氧烷微球。[方法]以甲基三甲氧基硅烷为前体,通过“溶胶-凝胶”法制备聚硅氧烷微球(PSQ)包埋AVMB2(AVMB2@PSQ),对载药微球的组成和形貌进行了FTIR、TGA、SEM、DLS表征以及缓释和抗紫外光解性能分析,并采用浸渍法评价了载药微球对松材线虫的室内生物活性。[结果]AVMB2成功包埋在PSQ中,形成平均粒径为1.1μm、载药率为32.74%的中空结构光滑球形的AVMB2@PSQ微球;12 h溶出率为55.492%,明显优于AVMB2溶出率87.862%;紫外光照射6 h降解率为39.074%,优于AVMB2降解率69.986%;对松材线虫48 h的半致死剂量(LC50)为19.743 mg/L,比AVMB2的LC50值37.992 mg/L高1.9倍。[结论]AVMB2@PSQ微球具有优异的缓释和防紫外光降解性能以及提高AVMB2对松材线虫的毒杀活性,为阿维菌素B2应用于防治松材线虫病农业生产提供了参考。[Aims] In order to make full use of low-activity avermectin B2 produced in the fermentation process of avermectin B1 by account of 20%-30%, a controlled-release avermectin B2 polysiloxane microspheres(PSQ) with anti-ultraviolet degradation were prepared, in response to its drawbacks of easy photolysis and short residual efficacy.[Methods] AVMB2@PSQ was prepared by 'sol-gel' method using methyltrimethoxysilane as precursor, its composition and morphology were characterized by FTIR, TGA, SEM, DLS, its sustained release and anti-ultraviolet photolysis properties were studied, and its laboratory activity against Bursaphelenchus xylophilus was determined by immersion method. [Results] AVMB2 was successfully embedded in PSQ. The AVMB2@PSQ microspheres with smooth spherical hollow structure having an average particle size of 1.1 μm were formed, and the pesticide loading rate was 32.74%. The dissolution rate of 12 h was 55.492%, which was significantly better than that of AVMB2(87.862%). The degradation rate was 39.074% under UV irradiation for 6 h, which was better than that of AVMB2(69.986%). The median lethal dose(LC_(50)) for B. xylophilus at 48 h was 19.743 mg/L, which was 1.9 times better than that of AVMB2(37.992 mg/L). [Conclusions] AVMB2@PSQ microspheres with excellent sustained release and anti-ultraviolet degradation properties can improve the activity of AVMB2 against B. xylophilus. It provides a reference for the application of abamectin B2 in agricultural production to control pine wilt disease.

关 键 词：阿维菌素B2 聚硅氧烷微球 松材线虫“ 溶胶-凝胶”法 

分 类 号：TQ450.6[化学工程—农药化工]