To develop new potential pesticide candidates from low value-added natural bioactive products, a series of new cholesterol–matrine conjugates (I(a–e)–IV(a–e)) were prepared from two lead compounds cholesterol and matrine. Against Mythimna separata Walker, compound IVa exhibited 3.0 and 2.6 folds promising insecticidal activity of cholesterol and matrine, respectively; against Aphis citricola Van der Goot, compound IVd showed 4.3 and 2.2 folds potent aphicidal activity of their precursors; notably, it also showed good control effects in the greenhouse; against Plutella xylostella Linnaeus at a dose of 20 μg/nymph, compound IIIe exhibited 2.8 and 2.0 folds oral toxicity of cholesterol and matrine, respectively. Compounds IIIe, IVd and IVe can be used as the leads for further structural optimization as the insecticidal and aphicidal agents.

为了从低附加值的天然生物活性产品中开发新的潜在农药候选物，由两种先导化合物胆固醇和苦参碱制备了一系列新的胆固醇-苦参碱偶联物 ( I ( a - e ) -IV ( a - e ))。针对Mythimna separata Walker，化合物IVa对胆固醇和苦参碱的杀虫活性分别是 3.0 和 2.6 倍；针对Aphis citricola Van der Goot，化合物IVd 的杀蚜活性是其前体的 4.3 倍和 2.2 倍；值得注意的是，它在温室中也表现出良好的防治效果；反对Plutella xylostella Linnaeus 在 20 μg/若虫的剂量下，化合物IIIe表现出胆固醇和苦参碱的 2.8 倍和 2.0 倍的口服毒性。化合物IIIe、IVd和IVe可用作进一步结构优化的前驱物作为杀虫剂和杀蚜剂。