TY - JOUR
T1 - Inflammation Modulatory Phorbol Esters from the Seeds of Aquilaria malaccensis
AU - Wagh, Vitthal D.
AU - Korinek, Michal
AU - Lo, I. Wen
AU - Hsu, Yu Ming
AU - Chen, Shu Li
AU - Hsu, Hsue Yin
AU - Hwang, Tsong Long
AU - Wu, Yang Chang
AU - Chen, Bing Hung
AU - Cheng, Yuan Bin
AU - Chang, Fang Rong
N1 - Publisher Copyright:
© 2017 The American Chemical Society and American Society of Pharmacognosy.
PY - 2017/5/26
Y1 - 2017/5/26
N2 - 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).
AB - 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).
UR - http://www.scopus.com/inward/record.url?scp=85019698087&partnerID=8YFLogxK
U2 - 10.1021/acs.jnatprod.6b01096
DO - 10.1021/acs.jnatprod.6b01096
M3 - 文章
C2 - 28445049
AN - SCOPUS:85019698087
SN - 0163-3864
VL - 80
SP - 1421
EP - 1427
JO - Journal of Natural Products
JF - Journal of Natural Products
IS - 5
ER -
