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    Please use this identifier to cite or link to this item: https://ir.fy.edu.tw:8080/ir/handle/987654321/8426

    Title: Inhibition of intermediate-conductance Ca2+-activated K+ channel and cytoprotective properties of 4-piperidinomethyl-2-isopropyl-5-methylphenol.
    Authors: SHEN Ai-Yu;TSAI Jen-Hsiang;TENG Hsiu-Chen;HUANG Mei-Han;WU Sheng-Nan
    Contributors: 輔英科技大學 醫學檢驗生物技術系
    Date: 2007-05-01
    Issue Date: 2010-10-27 15:20:33 (UTC+8)
    Abstract: The ionic mechanisms and cytoprotective activities of 4-piperidinomethyl-2-isopropyl-5-methylphenol (THPI), an analogue of thymol, were investigated in HL-60 granulocytes and in human erythrocytes, respectively. THPI inhibited K+ outward current (ΙK) in a concentration-dependent manner in HL-60 leukocytes, with an IC50 value of 4μM. Neither iberiotoxin (200 nM) nor paxilline (1 μM) suppressed the amplitude of IK, whereas clotrimazole (5μM) significantly inhibited it. In the inside-out configuration of single channel recordings, application of THPI (5μM) into the bath medium did not alter the single-channel conductance of intermediate-conductance Ca2+-activated K+ (IKca) channels (i.e Kca3.1 channels), but it suppressed the channel activity significantly. THPI-induced inhibition of IKca channels was reversed by a further application of 1-ethyl-2-benzimidazolinone (10μM). THPI-induced reduction in IKca-channel activity in these cells was primarily due to a decrease in mean open time. These results provide direct evidence that THPI is capable of suppressing the activity of IKca channels in HL-60 cells. The antioxidant action of THPI also revealed a beneficial cytoprotective effect against mitomycin C-mediated haemolytic effect in human erythrocytes. The results of this study suggest that blockade of IKca channels and the membrane-protecting activity of THPI would combine to have beneficial effects in lessening the severity of haemolytic crisis and reducing anaemia in sickle cell disease.
    Relation: J Pharm Pharmacol.59(5),679-685
    Appears in Collections:[醫學檢驗生物技術系] 期刊論文

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