European Brain Research Institute (EBRI) Rita Levi Montalcini Foundation, Viale Regina Elena 295, 00161 Rome, Italy.
Department of Biotechnology and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.
Int J Mol Sci. 2020 Sep 10;21(18):6619. doi: 10.3390/ijms21186619.
Among the extensive public and scientific interest in the use of phytochemicals to prevent or treat human diseases in recent years, natural compounds have been highly investigated to elucidate their therapeutic effect on chronic human diseases including cancer, cardiovascular disease, and neurodegenerative disease. Curcumin, an active principle of the perennial herb , has attracted an increasing research interest over the last half-century due to its diversity of molecular targets, including transcription factors, enzymes, protein kinases, growth factors, inflammatory cytokines, receptors, and it's interesting pharmacological activities. Despite that, the clinical effectiveness of the native curcumin is weak, owing to its low bioavailability and rapid metabolism. Preclinical data obtained from animal models and phase I clinical studies done in human volunteers confirmed a small amount of intestinal absorption, hepatic first pass effect, and some degree of intestinal metabolism, might explain its poor systemic availability when it is given via the oral route. During the last decade, researchers have attempted with new pharmaceutical methods such as nanoparticles, liposomes, micelles, solid dispersions, emulsions, and microspheres to improve the bioavailability of curcumin. As a result, a significant number of bioavailable curcumin-based formulations were introduced with a varying range of enhanced bioavailability. This manuscript critically reviews the available scientific evidence on the basic and clinical effects and molecular targets of curcumin. We also discuss its pharmacokinetic and problems for marketing curcumin as a drug.
近年来,人们对利用植物化学物质预防和治疗人类疾病产生了浓厚的兴趣,天然化合物也受到了广泛的研究,以阐明其对癌症、心血管疾病和神经退行性疾病等慢性人类疾病的治疗作用。姜黄素是一种多年生草本植物的活性成分,由于其分子靶点的多样性,包括转录因子、酶、蛋白激酶、生长因子、炎症细胞因子、受体等,以及其有趣的药理学活性,在过去半个世纪引起了越来越多的研究兴趣。尽管如此,由于其生物利用度低和代谢迅速,天然姜黄素的临床疗效较弱。来自动物模型的临床前数据和在人类志愿者中进行的 I 期临床研究证实,少量的肠道吸收、肝脏首过效应和一定程度的肠道代谢可能解释了其经口服途径给药时的全身利用率低。在过去的十年中,研究人员尝试了新的药物方法,如纳米粒子、脂质体、胶束、固体分散体、乳液和微球,以提高姜黄素的生物利用度。结果,推出了大量具有不同生物利用度增强的基于姜黄素的可生物利用的配方。本文批判性地回顾了关于姜黄素的基础和临床作用及其分子靶点的现有科学证据。我们还讨论了其药代动力学问题以及将姜黄素作为药物推向市场的问题。