Cytotoxic polyhydroxylated pregnane glycosides from Cissampelos pareira var. hirsuta .
Yan-Jun SunHao-Jie ChenRui-Jie HanChen ZhaoYing-Ying SiMeng LiKun DuHui ChenWei-Sheng FengPublished in: RSC advances (2021)
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 IC 50 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.
Keyphrases
- structure activity relationship
- lps induced
- endothelial cells
- papillary thyroid
- inflammatory response
- induced pluripotent stem cells
- molecular docking
- induced apoptosis
- squamous cell
- pluripotent stem cells
- single cell
- lymph node metastasis
- high resolution
- electronic health record
- endoplasmic reticulum stress
- cell proliferation
- climate change
- mass spectrometry
- machine learning
- breast cancer cells
- data analysis