title: Structure-activity relationships of diverse xanthones against multidrug resistant human tumor cells.
abstract: Thirteen xanthones were isolated naturally from the stem of Securidaca inappendiculata Hassk, and structure-activity relationships (SARs) of these compounds were comparatively predicted for their cytotoxic activity against three human multidrug resistant (MDR) cell lines MCF-7/ADR, SMMC-7721/Taxol, and A549/Taxol cells. The results showed that the selected xanthones exhibited different potent cytotoxic activity against the growth of different human tumor cell lines, and most of the xanthones exhibited selective cytotoxicity against SMMC-7721/Taxol cells. Furthermore, some tested xanthones showed stronger cytotoxicity than Cisplatin, which has been used in clinical application extensively. The SARs analysis revealed that the cytotoxic activities of diverse xanthones were affected mostly by the number and position of methoxyl and hydroxyl groups. Xanthones with more free hydroxyl and methoxyl groups increased the cytotoxic activity significantly, especially for those with the presence of C-3 hydroxyl and C-4 methoxyl groups.
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Qiwen
authors.initials: Q
authors.lastname: Wang
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Chenyao
authors.initials: C
authors.lastname: Ma
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Ma
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China; Jiangsu Key Laboratory for Chinese Material Medica Processing, Nanjing 210029, China. Electronic address: lixiang_8182@163.com.
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China. Electronic address: achenyongmail@163.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Chen
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China; Jiangsu Key Laboratory for TCM Formulae Research, Nanjing 210046, China.
authors.forename: Jianwei
authors.initials: J
authors.lastname: Chen
mesh_terms: D000072283:A549 Cells; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D006801:Humans; D061986:MCF-7 Cells; D018547:Plant Stems / Q000737:chemistry / Q000378:metabolism; D031802:Securidaca / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D044004:Xanthones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D044004:Xanthones
keywords: Cytotoxic activity; Multidrug resistant; Structure-activity relationships; Xanthone