Document Detail


Cepharanthin enhances adriamycin sensitivity by synergistically accelerating apoptosis for adriamycin-resistant osteosarcoma cell lines, SaOS2-AR and SaOS2 F-AR.
MedLine Citation:
PMID:  15201988     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Cepharanthin (CEP) is a biscoclaurine alkaloid extracted from Stephania cepharantha Hayata. CEP is reported to inhibit drug resistance by inhibiting P-glycoprotein, a drug efflux pump, and recently to induce apoptosis. In the present study, we examined the effects of CEP as an inhibitor of adriamycin (ADR) resistance on ADR-induced apoptosis and necrosis. First, we established p53-deficient ADR-resistant osteosarcoma cell lines, SaOS2-AR and SaOS2 F-AR. Resistant cells showed a higher level of intracellular glutathione peroxidase activity than parent cells. P-glycoprotein was overexpressed in resistant cells. The intracellular ADR level of resistant cells was lower than that of parent cells. One micro g/ml CEP eliminated the degradation of intracellular ADR of resistant cells; that is, to a level equivalent to that of the parent cells. CEP of 0.5 micro g/ml, which was not cytotoxic when used alone, significantly increased the ADR sensitivity of resistant cells, to a level similar to the parent cell level. Isosorbide 5-mononitrate, a potential nitric oxide-generation agent, combined with CEP further increased the ADR sensitivity of resistant cells, indicating a synergistic effect of CEP and isosorbide 5-mononitrate on ADR cytotoxicity. Time-lapse microscopic observation revealed that ADR dominantly induced apoptosis much more than necrosis for both parent and resistant cells, and that the use of 0.5 micro g/ml CEP with ADR synergistically accelerated apoptosis in resistant cells. Finally, we clarified the property by which CEP synergistically accelerates ADR-induced apoptosis. This property might be a new mechanism that explains how CEP overcomes ADR resistance.
Authors:
Kuniaki Katsui; Masahiro Kuroda; Yadi Wang; Megumi Komatsu; Kengo Himei; Mitsuhiro Takemoto; Shiro Akaki; Jun-Ichi Asaumi; Susumu Kanazawa; Yoshio Hiraki
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  International journal of oncology     Volume:  25     ISSN:  1019-6439     ISO Abbreviation:  Int. J. Oncol.     Publication Date:  2004 Jul 
Date Detail:
Created Date:  2004-06-17     Completed Date:  2005-04-25     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9306042     Medline TA:  Int J Oncol     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  47-56     Citation Subset:  IM    
Affiliation:
Department of Radiology, Okayama University Medical School, Okayama 700-8558, Japan.
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MeSH Terms
Descriptor/Qualifier:
Alkaloids / pharmacology*
Antineoplastic Agents, Phytogenic / pharmacology*
Apoptosis / drug effects*
Benzylisoquinolines
Biological Transport
Bone Neoplasms
Cell Line, Tumor
Doxorubicin / pharmacokinetics,  toxicity*
Drug Resistance, Neoplasm*
Drug Synergism
Humans
Osteosarcoma
Chemical
Reg. No./Substance:
0/Alkaloids; 0/Antineoplastic Agents, Phytogenic; 0/Benzylisoquinolines; 23214-92-8/Doxorubicin; 481-49-2/cepharanthine

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