頁籤選單縮合
題 名 | Inhibitory Effect of 2-Hydroxymethyl-1-naphthol Diacetate on K狇Currents in Neoplastic Plasma Ceels: Implication in Its Antiproliferative Effect |
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作 者 | 沈愛玉; | 書刊名 | 鄭氏藥學文教基金會研究彙刊 |
卷 期 | 3:1 1999.03[民88.03] |
頁 次 | 頁114-141 |
分類號 | 418.4 |
關鍵詞 | Voltage-activated K狇current; Ca[feb4]狇-activated K狇current; Myeloma cells; 2-hydroxymethyl-1-naphtol diacetate; |
語 文 | 英文(English) |
英文摘要 | The effects of 2-hydroxymethyl-1-naphthol diacetate (TAC) on cell proliferation and K�� currents were studied in RPMI-8226 human myeloma cells. In cells with intracellular Ca�� concentration ([Ca�ヅ)��)=10 nM, depolarizing square pulses from a holding potential of -80mV elicited instantaneous outward current with slow inactivation, corresponding to voltage-activated K current. TAC (1-100uM) inhibited of I in a concentration-dependent manner. A23187(1uM), a Ca�� ionophore, can potentiate Ca��-activated K�� current (I). Tetraethylammonium chloride (10mM) caused a small decrease in the amplitude of I elicited by A23187, whereas TAC (30uM) and quinidine (10uM) decreased I more effectively. The present results show that TAC directly blocks voltage-and Ca��-activated K�� currents in human myeloma cells. TAC inhibited both cell proliferation and voltage-activated K�� current with an effective dose inducing half-maximum effects at 3.8±0.8 uM and 10±1.5 uM, respectively. The present studies suggest that the cytotoxic effect of TAC in cancer cells may be partially explained by blockade of K�� channels. the delocalization energy of TAC and other analogues (e.g., 2-dimethylaminomethyl-1-naphthol) was employed to compare their ability to block the K�� channel in myeloma cells. It was found that the esterificantion of naphthol to produce TAC increased K�� channel blocking activity. |
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