State Key Laboratory for Conservation and Utilization of Subtropical Agro-bioresources and Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, South China Agricultural University , Guangzhou, Guangdong 510642, People's Republic of China.
J Agric Food Chem. 2014 Nov 19;62(46):11037-46. doi: 10.1021/jf5034575. Epub 2014 Nov 6.
Mobile glucose-pesticide conjugates in the phloem are often restricted by decreases in biological activity. However, plants can bioactivate endogenous glucosides, which are assumed as able to bioactivate exogenous conjugates. In this study, four glycosidic bonds (O-, S-, N-, and C-glycosidic bonds) of glucose-pesticide conjugates were designed and synthesized, and then metabolism assays were carried out in vitro and in vivo. Results showed that β-glucosidases played a role in the hydrolysis of O-glycosidic bond conjugates in Ricinus communis L. The liberated aglycons possessed insecticidal activities against Plutella xylostella L. and Spodoptera litura F. These results could help establish methods of circumventing the mutual exclusivity of phloem mobility and biological activity by hydrolyzing endogenous β-glucosidases.
在韧皮部中，移动的葡萄糖-农药缀合物通常受到生物活性降低的限制。然而，植物可以生物激活内源性糖苷，这些糖苷被认为能够生物激活外源性缀合物。在这项研究中，设计和合成了葡萄糖-农药缀合物的四种糖苷键（O-、S-、N-和 C-糖苷键），然后进行了体外和体内代谢测定。结果表明，β-葡萄糖苷酶在蓖麻 O-糖苷键缀合物的水解中发挥作用。释放的非糖部分对小菜蛾和斜纹夜蛾具有杀虫活性。这些结果有助于建立通过水解内源性β-葡萄糖苷酶来规避韧皮部流动性和生物活性相互排斥的方法。
