Cedars-Sinai Medical Center, Department of Neurology, Davis Research Building, D-2091, 110 N. George Burns Road, Los Angeles, CA 90048, USA.
Expert Opin Investig Drugs. 2011 Jan;20(1):13-22. doi: 10.1517/13543784.2011.542410.
Curcumin has been investigated in preclinical and translational stroke models because of its pleiotropic 'neuroprotective' activities. Since curcumin has poor blood-brain barrier (BBB) penetration following acute administration, creative medicinal chemistry has been used to modify the parent curcumin molecule, resulting in second generation curcuminoids, which have enhanced BBB penetration, improved pharmacokinetics and interact with multiple viable targets to treat stroke.
This review covers epidemiological, preclinical and translational data published between 2002 and 2010.
There are two main goals: First, epidemiological data comparing the incidence of stroke in North America to that of India, a country where curcumin is a main-stay of the diet is presented. Second, the pharmacological characteristics of curcuminoids are detailed to determine if they should be further studied in translational stroke models for safety and efficacy prior to initiating clinical trials.
Curcumin and curcuminoids are neuroprotective in a variety of preclinical stroke models. The novel multi-target curcuminoid, CNB-001, has a superior safety and pharmacokinetic profile and should be further developed as an acute monotherapy or to be used in conjunction with thrombolytics for acute ischemic stroke.
姜黄素因其多效的“神经保护”作用，已在临床前和转化性中风模型中进行了研究。由于姜黄素在急性给药后穿透血脑屏障（BBB）的能力较差，因此创造性的药物化学已被用于修饰母体姜黄素分子，从而产生第二代姜黄素，其增强了 BBB 穿透性，改善了药代动力学，并与多个可行的靶点相互作用，以治疗中风。
本综述涵盖了 2002 年至 2010 年期间发表的流行病学、临床前和转化数据。
有两个主要目标：首先，提出了比较北美和印度中风发病率的流行病学数据，印度是一个将姜黄作为饮食主要成分的国家。其次，详细介绍了姜黄素类化合物的药理学特性，以确定在开始临床试验之前，它们是否应在转化性中风模型中进一步研究安全性和疗效。
姜黄素和姜黄素类化合物在多种临床前中风模型中具有神经保护作用。新型多靶点姜黄素 CNB-001 具有优越的安全性和药代动力学特性，应进一步开发为急性单药治疗或与溶栓剂联合用于急性缺血性中风。
