Cancer Science Institute of Singapore, National University of Singapore, Singapore 117599; Department of Pharmacy, National University of Singapore, Singapore 117543.
Department of Pharmacy, National University of Singapore, Singapore 117543.
Cancer Lett. 2015 Jun 28;362(1):8-14. doi: 10.1016/j.canlet.2015.03.019. Epub 2015 Mar 18.
Garcinol is the main medicinal component of the dried fruit rind of Garcinia indica (G. indica), which has traditionally been extensively used to treat gastric ailments and skin irritation. In vitro studies of garcinol revealed its potential therapeutic effects, such as its anti-oxidative, anti-inflammatory and anti-cancer properties. Similarly, in vivo studies in animal models also demonstrated the efficacy of garcinol for the treatment of various inflammatory and cancerous conditions. Despite being well tolerated in preclinical studies, the toxicological profile of garcinol remains elusive. More importantly, systematic pharmacokinetics (PK) studies of garcinol to establish an appropriate route of administration and its effective concentration range under physiological conditions have not yet been performed. PK studies play an essential role in translating the preclinical findings of garcinol from cell line models and animal species to humans, thereby facilitating dose selection, the characterization of the therapeutic index, identification of a metabolic pathway, and the determination of garcinol's potency and tolerability. This paper reviews the current studies of garcinol as a potential anti-oxidant, anti-inflammatory and anti-cancer agent and highlights the importance of performing preclinical PK and toxicological studies on garcinol for its development pipeline.
姜黄素是藤黄（Garcinia indica）干果皮的主要药用成分，传统上被广泛用于治疗胃病和皮肤刺激。体外研究表明姜黄素具有抗氧化、抗炎和抗癌特性。类似地，动物模型的体内研究也证明了姜黄素治疗各种炎症和癌症的功效。尽管在临床前研究中具有良好的耐受性，但姜黄素的毒理学特征仍然难以捉摸。更重要的是，尚未对姜黄素进行系统的药代动力学（PK）研究，以确定在生理条件下合适的给药途径和有效浓度范围。PK 研究在将姜黄素的临床前发现从细胞系模型和动物物种转化为人类方面发挥着重要作用，从而有助于选择剂量、描述治疗指数、确定代谢途径以及确定姜黄素的效力和耐受性。本文综述了姜黄素作为一种潜在的抗氧化、抗炎和抗癌剂的研究现状，并强调了对姜黄素进行临床前 PK 和毒理学研究的重要性，以推进其开发进程。
