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一种从兰花中提取的新型春药化合物,可激活一氧化氮合酶。

A novel aphrodisiac compound from an orchid that activates nitric oxide synthases.

机构信息

Department of Phytopharmacology, Tropical Botanic Garden and Research Institute (TBGRI), Palode, Thiruvananthapuram, India.

出版信息

Int J Impot Res. 2013 Nov-Dec;25(6):212-6. doi: 10.1038/ijir.2013.18. Epub 2013 Apr 18.

Abstract

Nitric oxide (NO) is known to have roles in several crucial biological functions including vasodilation and penile erection. There are neuronal, endothelial and inducible NO synthases that influence the levels of NO in tissues and blood. NO activates guanylate cyclase and thereby increases the levels of cyclic GMP (cGMP). Viagra (sildenafil), a top selling drug in the world for erectile dysfunction, inhibits phosphodiesterase-5, which hydrolyses cGMP to GMP. Thus, it fosters an NO-mediated increase in the levels of cGMP, which mediates erectile function. Here, we show the aphrodisiac activity of a novel chemical isolate from the flowers of an epiphytic orchid, Vanda tessellata (Roxb.) ex Don, which activates neuronal and endothelial, but not inducible, NO synthases. The aphrodisiac activity is caused by an increase in the level of NO in corpus cavernosum. The drug increases blood levels of NO as early as 30 min after oral administration. The active compound was isolated by column chromatography. Based on the spectral data, the active compound is found to be a new compound, 2,7,7-tri methyl bicyclo [2.2.1] heptane. We anticipate that our findings could lead to the development of a commercially viable and valuable drug for erectile dysfunction.

摘要

一氧化氮(NO)在多种关键的生物学功能中发挥作用,包括血管舒张和阴茎勃起。有神经元型、内皮型和诱导型一氧化氮合酶影响组织和血液中的 NO 水平。NO 激活鸟苷酸环化酶,从而增加环鸟苷酸(cGMP)的水平。伟哥(西地那非)是世界上治疗勃起功能障碍最畅销的药物,它抑制磷酸二酯酶-5,后者将 cGMP 水解为 GMP。因此,它促进了由 NO 介导的 cGMP 水平增加,从而介导勃起功能。在这里,我们展示了一种从附生兰花 Vanda tessellata(Roxb.)ex Don 的花朵中分离出的新型化学物质的催情活性,它能激活神经元型和内皮型,但不能激活诱导型,NO 合酶。催情活性是由海绵体中 NO 水平的增加引起的。该药物在口服后 30 分钟内即可增加血液中的 NO 水平。活性化合物通过柱层析进行分离。根据光谱数据,活性化合物被发现是一种新化合物,2,7,7-三甲基双环[2.2.1]庚烷。我们预计我们的发现可能会导致开发出一种用于治疗勃起功能障碍的商业可行且有价值的药物。

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