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新型合成姜黄素类似物及其潜在抗癌特性的观点。

Perspectives on new synthetic curcumin analogs and their potential anticancer properties.

机构信息

ISTRA, Department of Chemistry, Abeda Inamdar College, University of Pune, Pune 411001, India.

出版信息

Curr Pharm Des. 2013;19(11):2047-69.

Abstract

Curcumin is the active component of dried rhizome of Curcuma longa, a perennial herb belonging to ginger family, cultivated extensively in south and southeastern tropical Asia. It is widely consumed in the Indian subcontinent, south Asia and Japan in traditional food recipes. Extensive research over last few decades has shown that curcumin is a potent anti-inflammatory agent with powerful therapeutic potential against a variety of cancers. It suppresses proliferation and metastasis of human tumors through regulation of various transcription factors, growth factors, inflammatory cytokines, protein kinases and other enzymes. It induces apoptotic cell death and also inhibits proliferation of cancer cells by cell cycle arrest. Pharmacokinetic data has shown that curcumin undergoes rapid metabolism leading to glucuronidation and sulfation in the liver and excretion in the feces, which accounts for its poor systemic bioavailability. The compound has, therefore, been formulated and administered using different drug delivery systems such as liposomes, micelles, polysaccharides, phospholipid complexes and nanoparticles that can overcome the limitation of bioavailability to some extent. Attempts to avoid rapid metabolism of curcumin until now have been met with limited success. This has prompted researchers to look for new synthetic curcumin analogs in order to overcome the drawbacks of limited bioavailability and rapid metabolism, and gain efficacy with reduced toxicity. In this review we provide a summarized account of novel synthetic curcumin formulations and analogs, and the recent progress in the field of cancer prevention and treatment.

摘要

姜黄中的活性成分是姜黄素,它是姜科多年生草本植物姜黄的干燥根茎,广泛种植于南亚和东南亚的热带地区。姜黄素在印度次大陆、南亚和日本的传统食品配方中被广泛食用。过去几十年的广泛研究表明,姜黄素是一种有效的抗炎剂,具有强大的治疗多种癌症的潜力。它通过调节各种转录因子、生长因子、炎症细胞因子、蛋白激酶和其他酶来抑制人类肿瘤的增殖和转移。它诱导细胞凋亡,通过细胞周期阻滞抑制癌细胞增殖。药代动力学数据表明,姜黄素在肝脏中迅速代谢,导致葡萄糖醛酸化和硫酸化,并从粪便中排出,这导致其全身生物利用度较差。因此,该化合物已通过不同的药物传递系统进行配方和给药,例如脂质体、胶束、多糖、磷脂复合物和纳米粒子,这些系统在一定程度上可以克服生物利用度的限制。迄今为止,人们试图避免姜黄素的快速代谢,但收效甚微。这促使研究人员寻找新的合成姜黄素类似物,以克服生物利用度有限和代谢迅速的缺点,并在降低毒性的同时提高疗效。在这篇综述中,我们提供了对新型合成姜黄素配方和类似物的总结,并介绍了癌症预防和治疗领域的最新进展。

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