Anti-Inflammatory Chemical Profiling of the Australian Rainforest Tree Alphitonia petriei (Rhamnaceae)

作者：Raju Ritesh; Gunawardena Dhanushka; Ahktar Most Afia; Low Mitchell; Reddell Paul; Munch Gerald^*

来源：Molecules, 2016, 21(11): 1521.

DOI：10.3390/molecules21111521

• anti-inflammatory
• alphitolic acid
• nitric oxide
• TNF-alpha
• natural products

Chronic inflammation is an important pathological condition in many human diseases, and due to the side effects of the currently used non-steroidal anti-inflammatory drugs, discovery of novel anti-inflammatory drugs is of general interest. Anti-inflammatory activity guided compound isolation from the plant Alphitonia petriei led to the isolation of the known plant sterols emmolic acid (1), alphitolic acid (2), trans-and cis-coumaroyl esters of alphitolic acid (3 and 4) and betulinic acid (5). A detailed spectroscopic analysis led to the structure elucidation of the alphitolic acid derivatives (1-5), and the semi-synthetic emmolic acid acetate (6). When tested in LPS (Lipopolysaccharides) + IFN-gamma (Interferon gamma) activated RAW 264.7 macrophages, all compounds except (1) exhibited potent anti-inflammatory activity (IC50 values as low as 1.7 mu M) in terms of downregulation of NO and TNF-alpha production, but also demonstrated some considerable cytotoxicity.

• 出版日期2016-11