Siva Bandi, Venkanna Arramshetti, Poornima Borra, Divya Reddy Solipeta, Boustie Joel, Bastien Schnell, Jain Nishant, Usha Rani Pathipati, Suresh Babu Katragadda
Natural Products Laboratory, Division of Natural Product Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
UMR CNRS 6226 ISCR PNSCM, Université de Rennes 1, 2 Avenue du Professeur Léon Bernard, 35043 Rennes, France.
Fitoterapia. 2017 Mar;117:34-40. doi: 10.1016/j.fitote.2017.01.003. Epub 2017 Jan 5.
A comprehensive reinvestigation of chemical constituents from CHCl-soluble extract of Cipadessa baccifera led to the isolation of two new limonoids 1, 2 together with six known compounds 3-8. Their structures were established on the basis of extensive analysis of spectroscopic (IR, MS, 2D NMR) data. Further, a series of cipaferen G (3) derivatives were efficiently synthesized utilizing Yamaguchi esterification (2, 4, 6-trichlorobenzoyl chloride, EtN, THF, DMAP, toluene) at the C-3 position of the limonoids core, which is being reported for the first time. The anti-proliferative activity of the isolates and the synthetic analogues were studied against HeLa, PANC 1, HepG2, SKNSH, MDA-MB-231 and IMR32 cancer cells using the sulphorodamine B assay. Among the tested compounds, 13d and 13h manifested potent activity against IMR32, HepG2 cell lines with GI 0.013 and 0.01μM, respectively.
对浆果楝氯仿可溶提取物的化学成分进行全面重新研究，从中分离出两个新的柠檬苦素1、2以及六个已知化合物3 - 8。它们的结构是在对光谱（红外、质谱、二维核磁共振）数据进行广泛分析的基础上确定的。此外，利用山口酯化反应（2,4,6 - 三氯苯甲酰氯、乙腈、四氢呋喃、4 - 二甲氨基吡啶、甲苯）在柠檬苦素核心的C - 3位高效合成了一系列西帕费伦G（3）衍生物，这是首次报道。使用磺酰罗丹明B测定法研究了分离物和合成类似物对HeLa、PANC 1、HepG2、SKNSH、MDA - MB - 231和IMR32癌细胞的抗增殖活性。在测试的化合物中，13d和13h对IMR32、HepG2细胞系表现出强效活性，其GI分别为0.013和0.01μM。
