文献类型：期刊文献

中文题名：Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins

英文题名：Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins.

作者：Zhang, Shou-De[1];Shan, Lei[2];Li, Wei[3];Li, Hong-Lin[4];Zhang, Wei-Dong[5]

机构：[1]Shanghai Key Laboratory of New Drug Design, State Key Laboratory of Bioreactor Engineering, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.;[2]School of Pharmacy, Second Military Medical University, Shanghai 200433, China.;[3]Qinghai Academy of Agriculture and Forestry Science, Xining 810016, China.;[4]Shanghai Key Laboratory of New Drug Design, State Key Laboratory of Bioreactor Engineering, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China. Electronic address: hlli@ecust.edu.cn.;[5]Shanghai Key Laboratory of New Drug Design, State Key Laboratory of Bioreactor Engineering, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China; School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: wdzhangy@hotmail.com.

年份：2015

卷号：13

期号：9

起止页码：660

中文期刊名：Chinese Journal of Natural Medicines

外文期刊名：Chinese journal of natural medicines

收录：MEDLINE(收录号：26412425);CSTPCD;;Scopus;CSCD:【CSCD2015_2016】；PubMed;

基金：supported by the National Natural Science Foundation of China(Nos.81302651,81230090,and 81222046);the Fundamental Research Funds for the Central Universities(No.222201314041);the Global Research Network for Medicinal Plants(GRNMP);King Saud University,the Shanghai Leading Academic Discipline Project(No.B906);the Key Laboratory of Drug Research for Special Environments,PLA,the Shanghai Engineering Research Center for the Preparation of Bioactive Natural Products(No.10DZ2251300);the Scientific Foundation of Shanghai China(Nos.12401900801,09DZ1975700,09DZ1971500,and 10DZ1971700)

语种：英文

中文关键词：Stellera chamaejasme L. Isochamaejasmin Bcl-2 3D Similarity search （–）-Gossypol Apoptosis

外文关键词：(?)-Gossypol;3D Similarity search;Apoptosis;Bcl-2;Isochamaejasmin;Stellera chamaejasme L.

摘要：The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand(–)-gossypol through 3D similarity search. It selectively bound to Bcl-xL and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L-1 and 9.98 ± 0.21 μmol·L-1, respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L-1 and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L-1. Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L..
The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L. (Thymelaeaceae) that is used in traditional Chinese medicine (TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand (-)-gossypol through 3D similarity search. It selectively bound to Bcl-xl and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L(-1) and 9.98 ± 0.21 μmol·L(-1), respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L(-1) and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L(-1). Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L.