Kim Min-sik, Wessely Vilena, Lan Que
Department of Entomology, University of Wisconsin-Madison, Madison, Wisconsin, USA.
J Lipid Res. 2005 Apr;46(4):650-7. doi: 10.1194/jlr.M400389-JLR200. Epub 2005 Jan 1.
A mosquito sterol carrier protein-2, AeSCP-2, has been shown to aid in the uptake of cholesterol in mosquito cells. The discovery of chemical inhibitors of AeSCP-2 is reported here. AeSCP-2 inhibitors (SCPIs) belong to several chemotypes of hydrophobic compounds. Those inhibitors competed with cholesterol for AeSCP-2, binding with relatively high binding affinities. In cultured insect cells, SCPIs reduced cholesterol uptake by as much as 30% at 1-5 microM concentrations. SCPIs were potent larvicides to the yellow fever mosquito, Aedes aegypti, and to the tobacco hornworm, Manduca sexta, with 50% lethal doses (LD50s) of 5-21 microM and 0.013-15 ng/mg diet, respectively. The results indicate that sterol carrier protein-2 has functional similarity in two different insect species.
一种蚊子固醇载体蛋白2（AeSCP - 2）已被证明有助于蚊子细胞摄取胆固醇。本文报道了AeSCP - 2化学抑制剂的发现。AeSCP - 2抑制剂（SCPIs）属于几种疏水化合物的化学类型。这些抑制剂与胆固醇竞争AeSCP - 2，具有相对较高的结合亲和力。在培养的昆虫细胞中，SCPIs在1 - 5 microM浓度下可使胆固醇摄取减少多达30%。SCPIs对黄热病蚊子埃及伊蚊和烟草天蛾烟草天蛾是有效的杀幼虫剂，50%致死剂量（LD50s）分别为5 - 21 microM和0.013 - 15 ng/mg饲料。结果表明，固醇载体蛋白2在两种不同昆虫物种中具有功能相似性。
