Asano N, Takeuchi M, Kameda Y, Matsui K, Kono Y
School of Pharmacy, Hokuriku University, Kanazawa, Japan.
J Antibiot (Tokyo). 1990 Jun;43(6):722-6. doi: 10.7164/antibiotics.43.722.
Validoxylamine A showed a potent inhibitory activity against insect trehalase in a competitive manner with a Ki value of 4.3 x 10(-10) M. The other validoxylamines and validamycins also exhibited the activity in vitro. Injection of these compounds to young last instar larvae of the tobacco cutworm, Spodoptera litura, elicited the morphological abnormality followed by death after the cessation of feeding. Validoxylamine A showed 100% mortality at a dose of 10 micrograms/ last instar larva.
井冈胺A对昆虫海藻糖酶表现出强烈的抑制活性,呈竞争性抑制,抑制常数(Ki)值为4.3×10⁻¹⁰ M。其他井冈胺和井冈霉素在体外也表现出这种活性。将这些化合物注射到烟草夜蛾末龄幼虫体内,会引发形态异常,随后停止取食并死亡。井冈胺A在剂量为10微克/末龄幼虫时死亡率达100%。