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KMID : 0617320030120010218
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Journal of Pharmacetical Sceiences Ewha Womans University
2003 Volume.12 No. 1 p.218 ~ p.223
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Modulation of P-glycoprotein Activity by Flavonoids in Human Uterine Sarcoma Cells
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Lee Hwa-Jeong
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Abstract
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One of the possible mechanisms of multi-drug resistance found in cancer cells is the over-expression of P-glycoprotein (P-gp). Studies have shown that compounds in plants including vegetables and fruits not only have anticancer activities bat may also modulate P-gp activity. The effect of flavonoids and organic isothiocyanate on P-gp activity was studied in human uterine sarcoma cell lines, MES-SA (sensitive) and MES-SA/DX5 (resistant) cells. The accumulation of daunomycin (DNM), a P-gp substrate, was approximately 10 times greater in the sensitive cell as compared to the resistant cells over the entire time course (up to 2 hours). The positive control, verapamil increased the two hour accumulation of DNM while quercetin decreased that of DNM in the resistant cells. l-Naphtyl-isothiocyanate (NITC) showed no effect on the two hour accumulation of DNM. The IC_(50) values for DNM in the resistant cells was about 20 times higher than that observed in the sensitive cells (10.1±1.7 μM vs. 0.58±0.28 μM). Verapamil reduced the IC_(50) value for DNM whereas flavonoids (quercetin and fisetin) increased those for DNM in the resistant cells.
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