Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins

Shou De Zhang; Lei Shan; Wei Li; Hong Lin Li; Wei Dong Zhang

doi:10.1016/S1875-5364(15)30063-7

Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins

Shou De Zhang
, Lei Shan
, Wei Li
, Hong Lin Li^*
, Wei Dong Zhang

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

25 Scopus citations

Abstract

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-x_l and Mcl-1 with K_i 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.

Original language	English
Pages (from-to)	660-666
Number of pages	7
Journal	Chinese Journal of Natural Medicines
Volume	13
Issue number	9
DOIs	https://doi.org/10.1016/S1875-5364(15)30063-7
State	Published - 1 Sep 2015
Externally published	Yes

Keywords

(-)-Gossypol
3D Similarity search
Apoptosis
Bcl-2
Isochamaejasmin
Stellera chamaejasme L.

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/S1875-5364(15)30063-7

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title = "Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins",

abstract = "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.",

keywords = "(-)-Gossypol, 3D Similarity search, Apoptosis, Bcl-2, Isochamaejasmin, Stellera chamaejasme L.",

author = "Zhang, \{Shou De\} and Lei Shan and Wei Li and Li, \{Hong Lin\} and Zhang, \{Wei Dong\}",

note = "Publisher Copyright: {\textcopyright} 2015 China Pharmaceutical University.",

year = "2015",

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doi = "10.1016/S1875-5364(15)30063-7",

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journal = "Chinese Journal of Natural Medicines",

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TY - JOUR

T1 - Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins

AU - Zhang, Shou De

AU - Shan, Lei

AU - Li, Wei

AU - Li, Hong Lin

AU - Zhang, Wei Dong

PY - 2015/9/1

Y1 - 2015/9/1

N2 - 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.

AB - 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.

KW - (-)-Gossypol

KW - 3D Similarity search

KW - Apoptosis

KW - Bcl-2

KW - Isochamaejasmin

KW - Stellera chamaejasme L.

UR - https://www.scopus.com/pages/publications/84942120112

U2 - 10.1016/S1875-5364(15)30063-7

DO - 10.1016/S1875-5364(15)30063-7

M3 - 文章

C2 - 26412425

AN - SCOPUS:84942120112

SN - 2095-6975

VL - 13

SP - 660

EP - 666

JO - Chinese Journal of Natural Medicines

JF - Chinese Journal of Natural Medicines

IS - 9

ER -

Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins

Abstract

Keywords

UN SDGs

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