Identification and evaluation of apoptotic compounds from Garcinia paucinervis.
Four new compounds, paucinervins A-D (1-4), and 15 known ones were isolated from the leaves of Garcinia paucinervis. The structures of the new compounds were elucidated by spectroscopic evidences. All of the 19 compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which have been genetically engineered to possess a fluorescent biosensor capable of detecting caspase-3 activation. Eight of them were found to activate caspase-3 in HeLa-C3 cells within 72 h at the concentration of 25 microM. Moreover, the values of IC50 were measured for all four new compounds on HeLa cells using the MTT assay. Among them, compound 2 (paucinervin B) had the lowest IC50 value of 9.5 microM, while the other three new compounds had much higher IC50 values of 29.5, 52.5, and 95.6 microM, respectively. This result shows that paucinervin B has the strongest inhibitory effect against HeLa cell growth among these four newly identified paucinervins and it may have the potential to be developed into a new anticancer candidate.
Gao
Xue-Mei
XM
Chinese Medicine Laboratory, Hong Kong Jockey Club Institute of Chinese Medicine, Shatin, N.T., Hong Kong, People's Republic of China.
Yu
Ting
T
Lai
Fanny Shuk Fan
FS
Zhou
Yan
Y
Liu
Xin
X
Qiao
Chun-Feng
CF
Song
Jing-Zheng
JZ
Chen
Shi-Lin
SL
Luo
Kathy Qian
KQ
Xu
Hong-Xi
HX
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001572:Benzofurans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D001578:Benzopyrans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D001584:Benzoxepins / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D053148:Caspase 3 / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D029760:Garcinia / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D018515:Plant Leaves / Q000737:chemistry; D012459:Salicylates / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D001572:Benzofurans; D001578:Benzopyrans; D001584:Benzoxepins; D012459:Salicylates; C553477:paucinervin A; C553478:paucinervin B; C553479:paucinervin C; C553480:paucinervin D; D053148:Caspase 3