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Novel Water-soluble Curcumin Derivative Mediating Erectile Signaling

机译:新型水溶性姜黄素衍生物介导勃起信号

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Introduction. Curcumin is an inducer of heme oxygenase enzyme-1 (HO-1) that is involved in erectile signaling via elevating cyclic guanosine monophosphate (cGMP)levels. Aim. To assess the effect of oral administration of a water-soluble long-acting curcumin derivative on erectile signaling. Methods. Two hundred and thirty six male white albino rats were divided into four groups; group 1 (N = 20) includes control. Group 2 (N = 72) was equally divided into four subgroups; subgroup 1 received pure curcumin (10 mg/kg), subgroup 2 received the long-acting curcumin derivative (2 mg/kg), subgroup 3 received the long-acting curcumin derivative (10 mg/kg), and subgroup 4 received sildenafil (4 mg/kg). Subgroups were sacrificed after the first, second, and third hour. Group 3 (N = 72) was equally divided into the same four subgroups already mentioned and were sacrificed after 24 hours, 48 hours, and 1 week. Group 4 (N = 72) was subjected to intracavernosal pressure (ICP) measurements 1 hour following oral administration of the same previous doses in the same rat subgroups. Main Outcome Measure. Cavernous tissue HO enzyme activity, cGMP, and ICP. Results. In group 2, there was a significant progressive maintained elevation of HO activity and cGMP tissue levels starting from the first hour in subgroups 3 and 4, whereas, the rise in HO activity and cGMP started from second hour regarding the other rat subgroups. Sildenafil effect decreased after 3 hours. In group 3, there was a significant maintained elevation of HO activity and cGMP tissue levels extended to 1 week as compared to controls for all rat subgroups that received both forms of curcumin. In group 4, long-acting curcumin derivative exhibited more significant potentiation of intracavernosal pressure as compared to control and to the pure curcumin. Conclusion. Water-soluble long-acting curcumin derivative could mediate erectile function via upregulating cavernous tissue cGMP.z
机译:介绍。姜黄素是血红素加氧酶-1(HO-1)的诱导剂,它通过提高环状鸟苷单磷酸(cGMP)水平参与勃起信号传导。目标。评估口服长效姜黄素水溶性衍生物对勃起信号的影响。方法。将236只雄性白色白化病大鼠分为4组;第1组(N = 20)包括对照。第2组(N = 72)被平均分为四个子组。第1组接受纯姜黄素(10 mg / kg),第2组接受长效姜黄素衍生物(2 mg / kg),第3组接受长效姜黄素衍生物(10 mg / kg),第4组接受西地那非( 4 mg / kg)。在第一,第二和第三小时之后,将亚组处死。将第3组(N = 72)分为已经提到的相同的四个亚组,并在24小时,48小时和1周后处死。在相同大鼠亚组中以相同先前剂量口服后1小时,对第4组(N = 72)进行海绵体内压(ICP)测量。主要结果指标。海绵组织的HO酶活性,cGMP和ICP。结果。在第2组中,从亚组3和4开始的第一小时开始,HO活性和cGMP组织水平显着持续维持升高,而在其他大鼠亚组中,从第二小时开始,HO活性和cGMP升高。 3小时后西地那非作用降低。在第3组中,与接受两种形式姜黄素的所有大鼠亚组的对照组相比,HO活性均显着维持升高,并且cGMP组织水平延长至1周。在第4组中,长效姜黄素衍生物与对照和纯姜黄素相比,显示出更强的海绵体腔内压增强作用。结论。水溶性长效姜黄素衍生物可通过上调海绵体组织cGMP介导勃起功能。

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