白花鬼针草中多烯炔类成分的分离及其生物活性研究

Studies on Isolation of Polyacetylenes from Bidens pilosa var. radiata and Their Biological Activities

摘要:

为了解白花鬼针草（Bidens pilosa var. radiata）的化学成分，采用多种色谱技术从其提取物中分离多烯炔类成分，并对其生物活性进行研究。结果表明，从白花鬼针草乙酸乙酯提取部位中分离鉴定出4个多烯炔类化合物，分别为5-acetoxy-2-phenyl-ethinyl-thiophene （1）、1-phenylhepta-1，3，5-triyne （2）、5-phenyl-2-（1-propynyl）-thiophene （3）和icthyothereol acetate （4）。体外活性评价结果表明，化合物1~4均具有中等抗MRSA活性，且均对人肝LO₂细胞无毒性。首次为化合物1提供核磁数据并进行结构解析，化合物3、4为首次从该属植物中分离得到。

Abstract:

In order to understand the chemical constituents ofBidens pilosavar. radiate, the four polyacetylenes were isolated from ethyl acetate extract of B. pilosavar. radiate by using multiple column chromatography, and their biological activities were studied. Four polyacetylenes were identified as 5-acetoxy-2-phenylethinyl- thiophene (1), 1-phenylhepta-1,3,5-triyne (2), 5-phenyl-2-(1-propynyl)-thiophene (3), and icthyothereol acetate (4). In vitro activity screening, all these compounds showed moderate anti-MRSA activity, and were not toxic to human liver LO₂ cells. The NMR spectroscopic data along with the detailed elucidation of compound 1 was firstly presented, besides, compounds 3 and 4 were isolated from Bidens genus for the first time.