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Neuroprotective and neurotrophic curcuminoids to treat stroke: a translational perspective

  作者 Lapchak, PA  
  选自 期刊  Expert opinion on investigational drugs;  卷期  2011年20-1;  页码  13-22  
  关联知识点  
 

[摘要]Importance of the field: 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. Areas covered in this review: This review covers epidemiological, preclinical and translational data published between 2002 and 2010. What the reader will gain: 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. Take home message: 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.

 
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