Chemical constituents from Oldenlandia diffusa and their cytotoxic effects on human cancer cell lines

Abstract

Oldenlandia diffusa is an important Chinese traditional medicine with various biological activities such as anti-tumor, anti-inflammatory, anti-oxidant, antibacterial, neuroprotective and hepatoprotective effects. During our course of finding novel compounds from O. diffusa, two new alternariol derivatives named 9-O-(trans-p-coumaroyl)-alternariol (1), 9-O-(trans-caffeoyl)-alternariol (2), together with six known compounds (3-8) were isolated. Their structures were established on the basis of spectroscopic and physicochemical analysis. All isolates were evaluated for in vitro cytotoxic activities on MCF-7, HepG2, A549 and A2780 cancer cells. As a result, new compounds 1 and 2 exhibited potent cytotoxic activities on A2780 cancer cells with IC₅₀ values of 3.1 and 9.4 μM, respectively. And a conclusion was deduced that the p-coumaroyl or caffeoyl moiety could greatly increased the cytotoxic activity of alternariol on cancer cells.

Graphical Abstract

Keywords:

• Oldenlandia diffusa
• Rubiaceae
• alternariol derivatives
• cytotoxic activity

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

The authors wish to express thanks to the Central Hospital of Wuhan for providing a research grant and the Department of Instrumental Analysis of Wuhan University for the measurement of the UV, IR, HRESIMS and NMR.