短瓣钩吻中的五环三萜类化合物农吉利醇乙酸酯是一种抗锥虫药物。
Bauerenol Acetate, the Pentacyclic Triterpenoid from Tabernaemontana longipes, is an Antitrypanosomal Agent.
机构信息
Department of Chemistry, Jackson State University, Jackson, MS 39217, USA.
X-ray Crystallography Laboratory, Scripps Research Institute-FL, Jupiter, FL 33458, USA.
出版信息
Molecules. 2018 Feb 8;23(2):355. doi: 10.3390/molecules23020355.
The Latin American plant was studied in this work as a potential source of antiparasitic agents. The chloroform extract of leaves was separated into several fractions, and tested for antitrypanosomal activity. One of the fractions displayed significant growth inhibitory activity against . The active principle in the fraction was isolated, purified, and characterized by NMR and mass spectrometry. The antitrypanosomal agent in the CHCl₃ extract of leaves is the pentacyclic triterpenoid bauerenol acetate. A metabolite profiling assay suggest that the triterpenoid influences cholesterol metabolism. The molecular target(s) of bauerenol and its acetate, like many other antiparasitic pentacyclic triterpenoids is/are unknown, but they present privileged structural scaffolds that can be explored for structure-based activity optimization studies using phenotypic assays.
本工作研究了这种拉丁美洲植物，将其作为抗寄生虫药物的潜在来源。 的氯仿提取物被分离成几个部分，并测试其抗变形虫活性。 其中一个部分对 表现出显著的生长抑制活性。 在该部分中分离出活性成分，并通过 NMR 和质谱进行了鉴定和表征。 在 叶的 CHCl₃提取物中的抗变形虫剂是五环三萜酸 bauerenol 乙酸酯。 代谢产物分析表明，三萜类化合物会影响胆固醇代谢。 与许多其他抗寄生虫五环三萜类化合物一样，bauerenol 及其乙酸酯的分子靶标尚不清楚，但是它们具有特权结构支架，可以使用表型测定法进行基于结构的活性优化研究。
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