Archives of Pharmacal Research

, Volume 31, Issue 2, pp 171–177

Selective toxicity of ginsenoside Rg3 on multidrug resistant cells by membrane fluidity modulation

  • Hyog-Young Kwon
  • Eun-Hye Kim
  • Seung-Whan Kim
  • Su-Nam Kim
  • Jong-Dae Park
  • Dong-Kwon Rhee
Articles Drug Efficacy and Safety

DOI: 10.1007/s12272-001-1137-y

Cite this article as:
Kwon, HY., Kim, EH., Kim, SW. et al. Arch. Pharm. Res. (2008) 31: 171. doi:10.1007/s12272-001-1137-y

Abstract

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 μM 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 μM 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.

Key words

Panax ginseng Ginsenosides 20(S)-ginsenoside Rg3 Multidrug resistance (MDR) 

Abbreviations

ADR

adriamycin

DPH

1, 6-diphenyl-1,3,5,-hexatriene

MDR

multi-drug resistance

P-gp

Phospho-glycoprotein

TMA-DPH

1-[4-(trimethyl-ammonio)-phenyl]-6-phenyl-1,3,5,-hexatriene

Copyright information

© The Pharmaceutical Society of Korea 2008

Authors and Affiliations

  • Hyog-Young Kwon
    • 1
  • Eun-Hye Kim
    • 1
  • Seung-Whan Kim
    • 2
  • Su-Nam Kim
    • 3
  • Jong-Dae Park
    • 4
  • Dong-Kwon Rhee
    • 1
  1. 1.College of PharmacySungKyunKwan UniversitySu-WonKorea
  2. 2.Department of PharmacologyUniversity of Ulsan College of MedicineSeoulKorea
  3. 3.KIST Gangneung InstituteGangneungKorea
  4. 4.Ginseng Science Research GroupKT & G Central Research InstituteDaejeonKorea

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