Kim Keunyoung, Kim Jung-Jun, Jung Yeryeon, Noh Ji-Yoon, Syed Ahmed Shah, Kim Chul Young, Lee Moo-Yeol, Lim Kyung-Min, Bae Ok-Nam, Chung Jin-Ho
College of Pharmacy, Seoul National University , Seoul 08826, Korea.
College of Pharmacy, Hanyang University , Ansan 15588, Korea.
J Nat Prod. 2017 Jan 27;80(1):196-200. doi: 10.1021/acs.jnatprod.6b00331. Epub 2017 Jan 9.
Despite the increasing attention on the therapeutic potential of Curcuma longa (turmeric), the biological activities of curcuminoids other than curcumin are not well understood. Here, we investigated antivasoconstrictive activities of C. longa extract and its ingredients using freshly isolated rat aortic rings. C. longa extract significantly suppressed agonist-stimulated vasoconstriction, and cyclocurcumin was found to be the most potent (IC against phenylephrine-induced vasoconstriction: 14.9 ± 1.0 μM) among the 10 tested ingredients including four curcuminoids. Cyclocurcumin significantly inhibited contraction of vascular smooth muscle, which was mediated by the suppression of myosin-light-chain phosphorylation and calcium influx via the L-type calcium channel. The inhibitory effect of cyclocurcumin was observed to be reversible and without cytotoxicity. Taken together, we demonstrated that cyclocurcumin, a bioactive ingredient in C. longa, may have a therapeutic potential as a novel antivasoconstrictive natural product.
尽管姜黄(Curcuma longa)的治疗潜力日益受到关注,但除姜黄素外的姜黄素类化合物的生物活性尚未得到充分了解。在此,我们使用新鲜分离的大鼠主动脉环研究了姜黄提取物及其成分的抗血管收缩活性。姜黄提取物显著抑制激动剂刺激的血管收缩,并且在包括四种姜黄素类化合物在内的10种测试成分中,环姜黄素被发现是最有效的(对去氧肾上腺素诱导的血管收缩的IC:14.9±1.0μM)。环姜黄素显著抑制血管平滑肌收缩,这是通过抑制肌球蛋白轻链磷酸化和经由L型钙通道的钙内流介导的。观察到环姜黄素的抑制作用是可逆的且无细胞毒性。综上所述,我们证明环姜黄素作为姜黄中的一种生物活性成分,可能作为一种新型抗血管收缩天然产物具有治疗潜力。