Document Detail

Selective toxicity of ginsenoside Rg3 on multidrug resistant cells by membrane fluidity modulation.
MedLine Citation:
PMID:  18365686     Owner:  NLM     Status:  MEDLINE    
Multidrug resistance (MDR) is a major problem in cancer chemotherapy. It was previously reported that a red ginseng saponin, 20(S)-ginsenoside Rg3 could modulate MDR in vitro and extend the survival of mice implanted with ADR-resistant murine leukemia P388 cells. This study examined the cytotoxicity of Rg3 on normal and transformed cells, along with its effect on the membrane fluidity. The cytotoxicity study revealed that 120 microM of Rg3 was cytotoxic against a multidrug-resistant human fibroblast carcinoma cell line, KB V20C, but not against normal WI 38 cells in vitro. Flow cytometric analysis using rhodamine 123 as the artificial substrate showed that Rg3 promoted the accumulation of rhodamine 123 in ADR-resistant murine leukemia P388 cells in vivo. Fluorescence polarization studies using the hydrophilic fluorescent probe, DPH, and hydrophobic probe, TMA-DPH, showed that 20 microM Rg3 induced a significant increase in fluorescence anisotropy in KB V20C cells but not in the parental KB cells. These results clearly show that Rg3 decreases the membrane fluidity thereby blocking drug efflux.
Hyog-Young Kwon; Eun-Hye Kim; Seung-Whan Kim; Su-Nam Kim; Jong-Dae Park; Dong-Kwon Rhee
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Archives of pharmacal research     Volume:  31     ISSN:  0253-6269     ISO Abbreviation:  Arch. Pharm. Res.     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2008-03-27     Completed Date:  2008-05-01     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8000036     Medline TA:  Arch Pharm Res     Country:  Korea (South)    
Other Details:
Languages:  eng     Pagination:  171-7     Citation Subset:  IM    
College of Pharmacy, SungKyunKwan University, Su-Won 440-746, Korea.
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MeSH Terms
Antibiotics, Antineoplastic / pharmacology
Antineoplastic Agents, Phytogenic / toxicity*
Doxorubicin / pharmacology
Drug Resistance, Multiple / drug effects*
Drug Resistance, Neoplasm / drug effects*
Flow Cytometry
Fluorescence Polarization
Fluorescent Dyes
Ginsenosides / toxicity*
KB Cells
Leukemia P388 / drug therapy
Membrane Fluidity / drug effects*
Neoplasm Transplantation
Rhodamine 123
Reg. No./Substance:
0/Antibiotics, Antineoplastic; 0/Antineoplastic Agents, Phytogenic; 0/Fluorescent Dyes; 0/Ginsenosides; 14197-60-5/ginsenoside Rg3; 23214-92-8/Doxorubicin; 62669-70-9/Rhodamine 123

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