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抑咽侧体素(Allatostatin,AST)是一类具有抑制咽侧体合成保幼激素(JH)功能的昆虫神经肽.然而,由于天然AST易代谢失活,限制了其在害虫控制方面的应用.本研究在前期工作基础上,以高活性拟肽类化合物B1作为二级先导,采用模拟肽学方法进行结构改造,通过N端引入脲桥结构消除酶解位点,以提高抗酶解能力,共设计合成了10个目标化合物II01~II10,并对其抑制保幼激素合成离体生物活性进行了测定.结果表明,10个化合物均具有抑制保幼激素合成活性,其中,II04(IC_(50)=0.21μmol/L)抑制活性略高于一级先导天然核心五肽(IC_(50)=0.24μmol/L).虽然抑制活性比二级先导B1(IC_(50)=0.09μmol/L)略低,但简便的合成路线,使其成为具有研究潜力的先导化合物.
Allestiostatin (AST) is a kind of insect neuropeptide which inhibits the function of juvenile hormone (JH) in the lateral part of the rat’s throat.However, due to its metabolic inactivation, the natural AST limits its application in pest control In this work, based on the previous work, high-activity peptidomimetic compounds B1 as the second-level leader, the use of mimotope peptide structure modification method, through the introduction of urea bridge N-terminal structure to eliminate enzyme sites to improve anti-enzymatic ability , A total of 10 target compounds II01 ~ II10 were designed and synthesized, and their in vitro biological activities for inhibiting the synthesis of juvenile hormones were studied.The results showed that 10 compounds all inhibited the synthesis of juvenile hormone, among which, II04 (IC_ ( (IC 50 = 0.24μmol / L), although the inhibitory activity was lower than that of the first-class leader natural core pentapeptide (IC 50 = 0.09μmol / L) ) Is slightly lower but a simple synthesis route makes it a lead compound with potential for research.