Department of Entomology, University of Wisconsin, Madison, WI 53706, USA.
J Med Entomol. 2010 Mar;47(2):249-57. doi: 10.1603/me09160.
alpha-Mangostin derived from mangosteen was identified as a mosquito sterol carrier protein-2 inhibitor via high throughput insecticide screening, alpha-Mangostin was tested for its larvicidal activity against third instar larvae of six mosquito species, and the median lethal concentration values range from 0.84 to 2.90 ppm. The residual larvicidal activity of alpha-mangostin was examined under semifield conditions. The results indicated that alpha-mangostin was photolytic with a half-life of 53 min in water under full sunlight exposure. The effect of alpha-mangostin on activities of major detoxification enzymes such as P450, glutathione S-transferase, and esterase was investigated. The results showed that alpha-mangostin significantly elevated activities of P450 and glutathione S-transferase in larvae, whereas it suppressed esterase activity. Toxicity of alpha-mangostin against young rats was studied, and there was no detectable adverse effect at dosages as high as 80 mg/kg. This is the first multifaceted study of the biological activity of alpha-mangostin in mosquitoes. The results suggest that alpha-mangostin may be a lead compound for the development of a new organically based mosquito larvicide.
从山竹果中提取的α-倒捻子素被鉴定为一种通过高通量杀虫剂筛选的蚊子固醇载体蛋白-2抑制剂。α-倒捻子素对 6 种蚊子的三龄幼虫进行了杀幼虫活性测试，其半数致死浓度值范围为 0.84 至 2.90ppm。在半野外条件下检查了α-倒捻子素的残留杀幼虫活性。结果表明，α-倒捻子素在全阳光暴露下的水中具有光解性，半衰期为 53 分钟。研究了α-倒捻子素对主要解毒酶如 P450、谷胱甘肽 S-转移酶和酯酶活性的影响。结果表明，α-倒捻子素显著提高了幼虫中 P450 和谷胱甘肽 S-转移酶的活性，而抑制了酯酶的活性。研究了α-倒捻子素对幼鼠的毒性，在高达 80mg/kg 的剂量下没有检测到明显的不良影响。这是首次对α-倒捻子素在蚊子中的生物学活性进行多方面研究。结果表明，α-倒捻子素可能是开发新型有机蚊子幼虫杀虫剂的先导化合物。
