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Bioorg Med Chem Lett. 2017 Feb 1;27(3):447-449. doi: 10.1016/j.bmcl.2016.12.045. Epub 2016 Dec 20.

Structure-activity relationships of diverse xanthones against multidrug resistant human tumor cells.

Author information

1
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
2
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.
3
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China. Electronic address: achenyongmail@163.com.
4
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China; Jiangsu Key Laboratory for TCM Formulae Research, Nanjing 210046, China.

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.

KEYWORDS:

Cytotoxic activity; Multidrug resistant; Structure-activity relationships; Xanthone

PMID:
28065566
DOI:
10.1016/j.bmcl.2016.12.045
[Indexed for MEDLINE]

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