姜辣素：一类新型的香草酸受体（VR1）激动剂。
Gingerols: a novel class of vanilloid receptor (VR1) agonists.
作者信息
Dedov Vadim N, Tran Van H, Duke Colin C, Connor Mark, Christie MacDonald J, Mandadi Sravan, Roufogalis Basil D
机构信息
Faculty of Pharmacy, University of Sydney, Sydney, N.S.W. 2006, Australia.
出版信息
Br J Pharmacol. 2002 Nov;137(6):793-8. doi: 10.1038/sj.bjp.0704925.
Abstract
- Gingerols, the pungent constituents of ginger, were synthesized and assessed as agonists of the capsaicin-activated VR1 (vanilloid) receptor. 2. [6]-Gingerol and [8]-gingerol evoked capsaicin-like intracellular Ca(2+) transients and ion currents in cultured DRG neurones. These effects of gingerols were blocked by capsazepine, the VR1 receptor antagonist. 3. The potency of gingerols increased with increasing size of the side chain and with the overall hydrophobicity in the series. 4. We conclude that gingerols represent a novel class of naturally occurring VR1 receptor agonists that may contribute to the medicinal properties of ginger, which have been known for centuries. The gingerol structure may be used as a template for the development of drugs acting as moderately potent activators of the VR1 receptor.
摘要
- 姜辣素是生姜中的辛辣成分，已被合成并作为辣椒素激活的VR1（香草酸）受体的激动剂进行评估。2. [6]-姜辣素和[8]-姜辣素在培养的背根神经节（DRG）神经元中诱发了类似辣椒素的细胞内Ca(2+)瞬变和离子电流。姜辣素的这些作用被VR1受体拮抗剂辣椒平所阻断。3. 姜辣素的效力随着侧链长度的增加以及该系列中整体疏水性的增加而增强。4. 我们得出结论，姜辣素代表了一类新型的天然存在的VR1受体激动剂，这可能有助于解释生姜几个世纪以来为人所知的药用特性。姜辣素结构可作为开发作为VR1受体适度有效激活剂的药物的模板。
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