Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
; (6): 660-666, 2015.
Article
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| WPRIM
| ID: wpr-812498
Biblioteca responsable:
WPRO
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.
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Texto completo:
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Bases de datos:
WPRIM
Medicinas Tradicionales:
Medicinas_tradicionales_de_asia
/
Medicina_china
Métodos Terapéuticos y Terapias MTCI:
Terapias_biologicas
Asunto principal:
Farmacología
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Gosipol
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Extractos Vegetales
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Transducción de Señal
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Leucemia
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Química
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Poli(ADP-Ribosa) Polimerasas
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Apoptosis
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Células HL-60
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Proteínas Proto-Oncogénicas c-bcl-2
Idioma:
En
Revista:
Chinese Journal of Natural Medicines (English Ed.)
Año:
2015
Tipo del documento:
Article