Hampannavar Girish A, Karpoormath Rajshekhar, Palkar Mahesh B, Shaikh Mahamadhanif S
Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
Bioorg Med Chem. 2016 Feb 15;24(4):501-20. doi: 10.1016/j.bmc.2015.12.049. Epub 2016 Jan 2.
Natural products serve as a key source for the design, discovery and development of potentially novel drug like candidates for life threatening diseases. Curcumin is one such medicinally important molecule reported for an array of biological activities. However, it has major drawbacks of very poor bioavailability and solubility. Alternatively, structural analogs and degradants of curcumin have been investigated, which have emerged as promising scaffolds with diverse biological activities. Dehydrozingerone (DZG) also known as feruloylmethane, is one such recognized degradant which is a half structural analog of curcumin. It exists as a natural phenolic compound obtained from rhizomes of Zingiber officinale, which has attracted much attention of medicinal chemists. DZG is known to have a broad range of biological activities like antioxidant, anticancer, anti-inflammatory, anti-depressant, anti-malarial, antifungal, anti-platelet and many others. DZG has also been studied in resolving issues pertaining to curcumin since it shares many structural similarities with curcumin. Considering this, in the present review we have put forward an effort to revise and systematically discuss the research involving DZG with its biological diversity. From literature, it is quite clear that DZG and its structural analogs have exhibited significant potential in facilitating design and development of novel medicinally active lead compounds with improved metabolic and pharmacokinetic profiles.
天然产物是设计、发现和开发针对危及生命疾病的潜在新型药物候选物的关键来源。姜黄素就是这样一种具有多种生物活性的重要药用分子。然而,它存在生物利用度和溶解度极低的主要缺点。另外,人们对姜黄素的结构类似物和降解产物进行了研究,它们已成为具有多种生物活性的有前景的骨架。脱氢姜酮(DZG)也称为阿魏酰甲烷,就是这样一种公认的降解产物,它是姜黄素的半结构类似物。它是从姜黄根茎中获得的一种天然酚类化合物,已引起药物化学家的广泛关注。已知DZG具有广泛的生物活性,如抗氧化、抗癌、抗炎、抗抑郁、抗疟疾、抗真菌、抗血小板等。由于DZG与姜黄素具有许多结构相似性,因此也对其在解决与姜黄素相关的问题方面进行了研究。考虑到这一点,在本综述中,我们努力对涉及DZG及其生物多样性的研究进行修订并系统地讨论。从文献中可以清楚地看出,DZG及其结构类似物在促进设计和开发具有改善代谢和药代动力学特征的新型药用活性先导化合物方面已展现出巨大潜力。