Inflammation Modulatory Phorbol Esters from the Seeds of Aquilaria malaccensis.

The tree Aquilaria malaccensis is a valuable source of agarwood, which is used in herbal medicinal preparations. Phytochemical research on A. malaccensis seeds has led to the isolation of four new phorbol esters (1-4), two known phorbol esters (5, isolated from Nature for the first time, and 6), and two known glycerides (7 and 8). The structures of these isolates were elucidated by means of spectroscopic data interpretation. The inflammation-modulatory activities of the isolates on elastase release and superoxide anion generation in human neutrophils were evaluated. Interestingly, phorbol esters 1, 5, and 6 showed potent inhibitory activity on elastase release in human neutrophils, with IC50 values of 2.7, 0.8, and 2.1 μM, respectively. All isolated phorbol esters exerted enhancing activity on superoxide anion generation. The results indicated that phorbol esters may play a bilateral modulatory role in the processes of inflammation. In addition, the compounds were evaluated for their cytotoxic properties against HepG2 (hepatoma), MDA-MB-231 (breast), and A549 (lung) cancer cells, but all compounds were inactive for all cell lines used (IC50 > 10 μM).

Citation

Vitthal D Wagh, Michal Korinek, I-Wen Lo, Yu-Ming Hsu, Shu-Li Chen, Hsue-Yin Hsu, Tsong-Long Hwang, Yang-Chang Wu, Bing-Hung Chen, Yuan-Bin Cheng, Fang-Rong Chang. Inflammation Modulatory Phorbol Esters from the Seeds of Aquilaria malaccensis. Journal of natural products. 2017 May 26;80(5):1421-1427

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PMID: 28445049

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