首页> 美国卫生研究院文献>Cellular Molecular Biology Letters >The influence of 8-prenylnaringenin on the activity of voltage-gated kv1.3 potassium channels in human jurkat t cells
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The influence of 8-prenylnaringenin on the activity of voltage-gated kv1.3 potassium channels in human jurkat t cells

机译:8-异戊烯基柚皮苷对人Jurkat T细胞电压门控的kv1.3钾通道活性的影响

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摘要

Using the whole-cell patch-clamp technique, we investigated the influence of 8-prenylnaringenin on the activity of the voltage-gated Kv1.3 potassium channels in the human leukemic T lymphocyte cell line Jurkat. 8-prenylnaringenin is a potent plant-derived phytoestrogen that has been found to inhibit cancer cell proliferation. The results show that it inhibited the Kv1.3 channels in a concentration-dependent manner. Complete inhibition occurred at concentrations higher than 10 μM. The inhibitory effect of 8-prenylnaringenin was reversible. It was accompanied by a significant acceleration of channel inactivation without any pronounced change in the activation rate. Of the naringenin derivatives tested to date, 8-prenylnaringenin is the most potent inhibitor of the Kv1.3 channels. The potency of the inhibition may be due to the presence of a prenyl group in the molecule of this flavonoid. The inhibition of the Kv1.3 channels might be involved in the antiproliferative and pro-apoptotic effects of 8-prenylnaringenin that have been observed in cancer cell lines expressing these channels.
机译:使用全细胞膜片钳技术,我们调查了8-异戊烯基柚皮苷对人白血病T淋巴细胞细胞Jurkat中电压门控的Kv1.3钾通道活性的影响。 8-异戊二烯柚皮苷是一种有效的植物来源的植物雌激素,已被发现能抑制癌细胞的增殖。结果表明,它以浓度依赖性方式抑制Kv1.3通道。浓度高于10μM时会发生完全抑制。 8-异戊烯基柚皮苷的抑制作用是可逆的。它伴随着通道失活的显着加速,而激活速率没有任何明显的变化。在迄今测试的柚皮苷衍生物中,8-异戊烯基柚皮苷是Kv1.3通道最有效的抑制剂。抑制的效力可能是由于该类黄酮分子中存在异戊二烯基。 Kv1.3通道的抑制作用可能参与了在表达这些通道的癌细胞系中观察到的8-异戊烯基柚皮素的抗增殖和促凋亡作用。

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