Department of Entomology, University of Wisconsin, 840 Russell Labs, 1630 Linden Drive, Madison, WI 53706, USA.
J Med Entomol. 2012 Mar;49(2):350-5. doi: 10.1603/me11117.
Because of resistance to current insecticides and to environmental, health, and regulatory concerns, naturally occurring compounds and their derivatives are of increasing interest for the development of new insecticidal compounds against vectors of disease-causing pathogens. Fifty-eight compounds, either extracted and purified from plants native to China or synthetic analogs of curcumin, were evaluated for both their larvicidal activity against Aedes aegypti (L.) and their ability to inhibit binding of cholesterol to Ae. aegypti sterol carrier protein-2 in vitro. Of the compounds tested, curcumin analogs seem especially promising in that of 24 compounds tested five were inhibitors of Ae. aegypti sterol carrier protein-2 with EC50 values ranging from 0.65 to 62.87 microM, and three curcumin analogs exhibited larvicidal activity against fourth instar Ae. aegypti larvae with LC50 values ranging from 17.29 to 27.90 microM. Adding to the attractiveness of synthetic curcumin analogs is the relative ease of synthesizing a large diversity of compounds; only a small fraction of such diversity has been sampled in this study.
由于对现有杀虫剂的抗性以及对环境、健康和监管方面的考虑，天然存在的化合物及其衍生物越来越受到关注，可用于开发针对致病病原体传播媒介的新型杀虫剂。评估了 58 种化合物，包括从中国本土植物中提取和纯化的化合物以及姜黄素的合成类似物，评估其对埃及伊蚊（Aedes aegypti）（L.）的幼虫毒力以及体外抑制胆固醇与埃及伊蚊甾醇载体蛋白-2 结合的能力。在所测试的化合物中，姜黄素类似物似乎特别有希望，因为在测试的 24 种化合物中，有 5 种是埃及伊蚊甾醇载体蛋白-2 的抑制剂，EC50 值范围为 0.65 至 62.87 μM，有 3 种姜黄素类似物对第四龄埃及伊蚊幼虫具有杀虫活性，LC50 值范围为 17.29 至 27.90 μM。合成姜黄素类似物的吸引力在于可以相对容易地合成大量的化合物；在这项研究中，只对这种多样性的一小部分进行了采样。
