The medicinal plant Peliosanthes micrantha of Vietnam has been researched recently. This study explored water extracts of ethanol-extracted P. micrantha rhizome. P. micrantha rhizome was first extracted by ethanol (PM-R-ET). Then, sequential water extract of ethanol-extracted P. micrantha rhizome was carried out (PM-R-ET-W), analyzed by Ultra High-Performance Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry (QTOF-MS), and Gel Permeation Chromatography analysis (GPC). Its cytotoxicity was evaluated against five cancer cell lines using MTT assay. In the PM-R-ET-W extract, QTOF-MS tentatively assigned five known compounds, pumilaside A, pumilaside C, β–sitosterol, glycoside J-1, and peliosanthoside B. GPC showed one structurally-unresolved high molecular compound with MW 16.293 Da enriched to 19.3% w/w. PM-R-ET-W cytotoxicity values were moderate against all five MCF-7, Hela, HT-29, HepG2, and A549 cancer cells. The QTOF-MS-identified known compounds in the PM-R-ET-W extract should be later isolated for further biological assays. The GPC-analyzed high molecular compound of 16.293 Da quantified at 19.3 % w/w should be structurally determined. All the tested cell lines’ cytotoxicity values of the PM-R-ET-W were moderate. Six identified compounds should be isolated and tested for their cytotoxicity.
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