Cytotoxic polyhydroxylated pregnane glycosides from Cissampelos pareira var. hirsuta |
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| Authors: | Yan-Jun Sun Hao-Jie Chen Rui-Jie Han Chen Zhao Ying-Ying Si Meng Li Kun Du Hui Chen Wei-Sheng Feng |
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| Institution: | Co-construction Collaborative Innovation Center for Chinese Medicine, Respiratory Diseases by Henan & Education Ministry of P. R. China, Henan University of Chinese Medicine, Zhengzhou 450046 P. R. China.; School of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046 P. R. China ; Henan Research Center for Special Processing Technology of Chinese Medicine, Zhengzhou 450046 P. R. China |
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| Abstract: | Fourteen new polyhydroxylated pregnane glycosides, cissasteroid A–N (1–14), and five known analogues (15–19), were isolated from the dried whole plant of Cissampelos pareira var. hirsuta. Their structures and stereochemistry were elucidated by extensive spectroscopic data, chemical hydrolysis, and ECD measurements. All the compounds were tested for their cytotoxicity against five human cancer cell lines, and inhibitory activity against NO release in LPS-induced RAW 264.7 cells. Compared with cisplatin, compound 7 showed more potent cytotoxicities against the HL-60, A549, SMMC-7721, MCF-7, and SW480 cell lines, with IC50 values of 2.19, 14.38, 2.00, 7.58, and 7.44 μM, respectively. The preliminary study of structure–activity relationship indicated that benzoic acid esterification at C-20 may have a negative effect on the cytotoxic activity of polyhydroxylated pregnane derivatives in these five human cancer cell lines. These results revealed the potential of compound 7 as an ideal antitumor lead compound.Fourteen new polyhydroxylated pregnane glycosides, cissasteroid A–N (1–14), and five known analogues (15–19), were isolated from the dried whole plant of Cissampelos pareira var. hirsuta. |
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