Phytochemicals are ubiquitous in naturally occurring dietary elements that exhibits diverse pharmacological properties over various pathological disorders, including cancer. Voltage gated K+ (KV) channel in the plasma membrane contributes to wide range of cellular processes including cancer progression. Therefore, modulation of KV channel is being considered as a novel potential target for cancer therapy. The whole cell patch clamp technique was used to record the modulatory effect of chrysin, naringenin, caffeic acid, gallic acid, and zingerone on delayed rectifier potassium current (IK) in human prostate cancer cells LNCaP and PC-3. Among the tested compounds, zingerone blocked IK in a concentration-dependent manner in LNCaP cells and estimated the IC50 value of 141 μM and Emax was 81.3%. Further analysis of KV channel activation kinetics showed that zingerone induces a positive shift in the activation curve in LNCaP cells, whereas the inhibitory effect of gallic acid on IK was significantly less potent than the inhibition caused by zingerone. However, chrysin, naringenin, and caffeic acid did not modulate the KV channel conductance in LNCaP or PC-3 cells. Our findings confirmed that not all the tested phytochemicals to be effective modulators of IK and suggested that IK inhibitory effect of zingerone and gallic acid may be responsible for their anticancer effects in prostate cancer cells.

中文翻译：

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所选饮食植物化学物质对人前列腺癌细胞中延迟整流器K +电流的调节作用。

植物化学物质在天然饮食元素中无处不在，在包括癌症在内的各种病理性疾病中均表现出不同的药理特性。质膜中的电压门控K +（KV）通道有助于广泛的细胞过程，包括癌症进展。因此，KV通道的调节被认为是癌症治疗的新的潜在靶标。使用全细胞膜片钳技术来记录菊花链，柚皮苷，咖啡酸，没食子酸和姜油酮对人前列腺癌细胞LNCaP和PC-3中延迟整流钾电流（IK）的调节作用。在测试的化合物中，姜油酮以浓度依赖的方式阻断LNCaP细胞中的IK，估计IC50值为141μM，Emax为81.3％。对KV通道激活动力学的进一步分析表明，姜油酮在LNCaP细胞中诱导了激活曲线的正向移动，而没食子酸对IK的抑制作用远不如姜油酮引起的抑制作用强。但是，在LNCaP或PC-3细胞中，Chrysin，naringenin和咖啡酸不能调节KV通道电导。我们的发现证实并非所有测试过的植物化学物质都是IK的有效调节剂，并表明姜油酮和没食子酸的IK抑制作用可能是其对前列腺癌细胞的抗癌作用。咖啡酸不会调节LNCaP或PC-3细胞中的KV通道电导。我们的发现证实并非所有测试过的植物化学物质都是IK的有效调节剂，并表明姜油酮和没食子酸的IK抑制作用可能是其对前列腺癌细胞的抗癌作用。咖啡酸不会调节LNCaP或PC-3细胞中的KV通道电导。我们的发现证实并非所有测试过的植物化学物质都是IK的有效调节剂，并表明姜油酮和没食子酸的IK抑制作用可能是其对前列腺癌细胞的抗癌作用。