从利比亚蜂胶中分离得到一种新型黄烷醇和烷基间苯二酚，具有很强的抗锥虫活性。
Isolation of a Novel Flavanonol and an Alkylresorcinol with Highly Potent Anti-Trypanosomal Activity from Libyan propolis.
机构信息
Strathclyde Institute of Pharmacy and Biomedical Science, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0RE, UK.
Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8TA, UK.
出版信息
Molecules. 2019 Mar 15;24(6):1041. doi: 10.3390/molecules24061041.
Twelve propolis samples from different parts of Libya were investigated for their phytochemical constituents. Ethanol extracts of the samples and some purified compounds were tested against and against two helminth species, and , showing various degrees of activity. Fourteen compounds were isolated from the propolis samples, including a novel compound Taxifolin-3-acetyl-4'-methyl ether (), a flavanonol derivative. The crude extracts showed moderate activity against and , while the purified compounds had low activity against . Anti-trypanosomal activity (EC = 0.7 µg/mL) was exhibited by a fraction containing a cardol identified as bilobol () and this fraction had no effect on Human Foreskin Fibroblasts (HFF), even at 2.0 mg/mL, thus demonstrating excellent selectivity. A metabolomics study was used to explore the mechanism of action of the fraction and it revealed significant disturbances in trypanosomal phospholipid metabolism, especially the formation of choline phospholipids. We conclude that a potent and highly selective new trypanocide may be present in the fraction.
从利比亚不同地区采集了 12 个蜂胶样品，研究其植物化学成分。对这些样品的乙醇提取物和一些纯化化合物进行了抗 和抗两种寄生虫物种 和 的测试，显示出不同程度的活性。从蜂胶样品中分离出 14 种化合物，包括一种新化合物 Taxifolin-3-acetyl-4'-methyl ether ()，一种黄烷酮醇衍生物。粗提取物对 和 表现出中等活性，而纯化化合物对 活性较低。含有一种被鉴定为双醇（）的 cardol 的馏分表现出抗锥虫活性（EC = 0.7 µg/mL），即使在 2.0 mg/mL 时，该馏分对人包皮成纤维细胞（HFF）也没有影响，因此表现出极好的选择性。代谢组学研究用于探索馏分的作用机制，结果表明锥虫磷脂代谢，特别是胆碱磷脂的形成，存在显著紊乱。我们得出结论，馏分中可能存在一种有效且高度选择性的新型抗锥虫药物。
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