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新型水溶性姜黄素衍生物介导勃起信号。

Novel water-soluble curcumin derivative mediating erectile signaling.

机构信息

Faculty of Medicine, Cairo University-Medical Biochemistry, Unit of Molecular Biology, Cairo, Egypt.

出版信息

J Sex Med. 2010 Aug;7(8):2714-22. doi: 10.1111/j.1743-6109.2009.01543.x. Epub 2009 Oct 19.

Abstract

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.

摘要

简介

姜黄素是血红素加氧酶-1(HO-1)的诱导剂,通过提高环鸟苷酸(cGMP)水平参与勃起信号传导。

目的

评估口服水溶性长效姜黄素衍生物对勃起信号的影响。

方法

将 236 只雄性白化大鼠分为四组;第 1 组(N=20)包括对照组。第 2 组(N=72)分为四小组;第 1 小组接受纯姜黄素(10mg/kg),第 2 小组接受长效姜黄素衍生物(2mg/kg),第 3 小组接受长效姜黄素衍生物(10mg/kg),第 4 小组接受西地那非(4mg/kg)。各亚组在第 1、2、3 小时后处死。第 3 组(N=72)分为上述四个小组,同样在 24 小时、48 小时和 1 周后处死。第 4 组(N=72)在口服相同剂量后 1 小时进行海绵体内压(ICP)测量。

主要观察指标

海绵体组织 HO 酶活性、cGMP 和 ICP。

结果

第 2 组第 3、4 小组从第 1 小时开始,HO 活性和 cGMP 组织水平呈持续升高趋势,而其他小组则从第 2 小时开始升高。西地那非的作用在 3 小时后减弱。第 3 组所有接受两种姜黄素的大鼠亚组,HO 活性和 cGMP 组织水平均持续升高,持续至 1 周,与对照组相比有显著差异。第 4 组,与对照组和纯姜黄素相比,长效姜黄素衍生物更显著地增强了海绵体内压。

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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