New chalcone and pterocarpoid derivatives from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property.
Investigation of the roots of Flemingia philippinensis resulted in the isolation of two new chalcones, flemiphilippinones B (1) and C (2), and one new pterocarpoid, demethylwedelolactone-11-methyl ether (3), together with 12 known compounds (4-15). The antiproliferative activity against PC-3 cells was evaluated and most compounds showed cytotoxicity, among which, compound 2 exhibited GI50 value of 14.12μM. The antiproliferative activity of 2 against Bel-7402 and CaEs-17 cells was also measured, with GI50 values of 1.91 and 2.58μM, respectively. Intensive mechanism study showed that 2 caused cell-cycle arrest at S/G2 phase and induced apoptosis in Bel-7402 cells through mitochondria-related pathway.
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Wen-Jia
WJ
Kang
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Da-Hong
DH
Li
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Tong
T
Han
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Lin
L
Sun
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Yan-Bin
YB
Fu
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Chun-Mei
CM
Sai
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: lzl1030@hotmail.com.
Zhan-Lin
ZL
Li
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: huimhua@163.com.
Hui-Ming
HM
Hua
D017209:Apoptosis; D059447:Cell Cycle Checkpoints; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry* / Q000302:isolation & purification; D007887:Fabaceae / Q000737:chemistry*; D006801:Humans; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry*; D036343:Pterocarpans / Q000737:chemistry* / Q000302:isolation & purification
D047188:Chalcones; D036343:Pterocarpans; C000614044:flemiphilippinone C
Apoptosis; Chalcone; Flemingia philippinensis; Leguminosae; Pterocarpoid