瓜馥木三萜 A-C，具有 5/6/3/6/5-稠合五环碳骨架的重排三萜，来自 ，作为多药耐药逆转剂。
Cucurbalsaminones A-C, Rearranged Triterpenoids with a 5/6/3/6/5-Fused Pentacyclic Carbon Skeleton from , as Multidrug Resistance Reversers.
机构信息
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy , Universidade de Lisboa , Avenida Prof. Gama Pinto , 1649-003 Lisbon , Portugal.
ATLÂNTICA - Escola Universitária de Ciências Empresariais, Saúde, Tecnologias e Engenharia , Fábrica da Pólvora de Barcarena, 2730-036 Barcarena, Oeiras , Portugal.
出版信息
J Nat Prod. 2019 Aug 23;82(8):2138-2143. doi: 10.1021/acs.jnatprod.9b00019. Epub 2019 Jul 24.
Three new triterpenoids, cucurbalsaminones A-C (-), featuring a unique 5/6/3/6/5-fused pentacyclic carbon skeleton, named cucurbalsaminane, were isolated from a methanol extract of . Their structures were elucidated by spectroscopic methods and corroborated, for , by structure solution using single-crystal X-ray diffraction analysis. A hypothetical biogenetic pathway for these compounds is proposed. Compounds - were evaluated for their P-glycoprotein (P-gp/ABCB1) modulation ability, using a mouse T-lymphoma -transfected cell model by the rhodamine-123 accumulation assay, and displayed potent multidrug resistance (MDR)-reversing activity.
从. 的甲醇提取物中分离得到三个新的三萜类化合物 cucurbalsaminones A-C(-)，具有独特的 5/6/3/6/5-稠合的五环碳骨架，命名为 cucurbalsaminane。通过光谱方法阐明了它们的结构，并通过单晶 X 射线衍射分析确定了 的结构。提出了这些化合物的假设生物合成途径。-通过 rhodamine-123 积累测定法，使用小鼠 T 淋巴细胞瘤转染细胞模型，评估了它们对 P 糖蛋白（P-gp/ABCB1）的调节能力，并显示出强大的多药耐药（MDR）逆转活性。
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