Title:Curcumin: A Natural Lead for Potential New Drug Candidates
Volume: 22
Issue: 36
Author(s): Ana Sofia Oliveira, Emília Sousa, Maria Helena Vasconcelos and Madalena Pinto
Affiliation:
关键词:
抗癌活性,Curcuma longa L.,姜黄素,细胞毒活性,多药耐药,P-糖蛋白抑制剂,构效关系,类似物合成。
摘要: Curcumin (1) is a secondary metabolite of turmeric, derived from Curcuma longa L. and was
shown to have many biological activities. One of the most interesting properties of curcumin (1) is the antitumour
activity allied with the ability to act as a multidrug resistance (MDR) modulator. Several curcumin derivatives
have been synthesized with the purpose of discovering more information about the mechanisms of
action, to establish structure-activity relationships (SAR), and to overcome pharmacokinetic problems. Over
the past few decades, more potent and more stable curcumin derivatives have emerged with potential as drug
candidates. Some important SAR studies pointed out that the unstable α,β-unsaturated diketone linker present
in curcumin (1) may not be necessary for the antitumour activity; generally, shorter linkers result in more potent
compounds than curcumin (1); the type of substituents and their substitution pattern are crucial regarding
the biological activities of interest. Overall, the structure of curcumin (1) may represent an important basis for
the development of more effective therapeutic agents, particularly in chemotherapy, as reflected by ongoing
clinical trials. This article aims to review the synthesis and biological activities of curcumin (1) and derivatives,
highlighting the MDR modulation properties of curcumin (1), since these effects makes this natural
product a promising lead compound for the development of new anticancer drugs.