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香豆素类骨架作为环氧化酶抑制剂

Coumarins scaffolds as COX inhibitors.

作者信息

Revankar Hrishikesh Mohan, Bukhari Syed Nasir Abbas, Kumar Gajjela Bharath, Qin Hua-Li

机构信息

School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan 430070, China.

School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan 430070, China; Department of Pharmaceutical Chemistry, College of Pharmacy, Aljouf University, Aljouf, Sakaka 2014, Saudi Arabia.

出版信息

Bioorg Chem. 2017 Apr;71:146-159. doi: 10.1016/j.bioorg.2017.02.001. Epub 2017 Feb 9.

Abstract

The discovery of COX enzymes has led to a better understanding of inflammation and its related biological pathways. Apart from being related to inflammation and pain, it has also been associated with cancer and neuropsychiatric diseases such as schizophrenia. Proverbially speaking, study of these enzymes has been crucial as they happen to "have fingers in many pies". Non-steroidal anti-inflammatory drugs (NSAID) that act specifically as COX-2 inhibitors have been known for a while; however these are also associated with severe side effects such as cardiac problems. Several heterocylic molecules have been tested for their anti-inflammatory activity specifically as COX-inhibitors. Coumarins also known as benzopyrans are widely found in nature, and are routinely employed as herbal remedies since early days. Over 1300 coumarins have been identified, principally as secondary metabolites in green plants, fungi and bacteria. Recently the use of natural and synthetic coumarins has garnered a lot of attention for their anti-inflammatory activities. In this review we delve further into the study of natural and synthetic coumarins as COX-inhibitors. Although the study is still in its nascent stage, we believe there is scope for a lot of development.

摘要

环氧化酶(COX)的发现使人们对炎症及其相关生物学途径有了更深入的了解。除了与炎症和疼痛相关外,它还与癌症以及精神分裂症等神经精神疾病有关。俗话说,对这些酶的研究至关重要,因为它们“涉足诸多领域”。作为COX-2特异性抑制剂的非甾体抗炎药(NSAID)已问世一段时间;然而,这些药物也与心脏问题等严重副作用有关。几种杂环分子已被测试其作为COX抑制剂的抗炎活性。香豆素又称苯并吡喃,在自然界中广泛存在,从早期就常被用作草药。已鉴定出1300多种香豆素,主要作为绿色植物、真菌和细菌中的次生代谢产物。最近,天然和合成香豆素因其抗炎活性而备受关注。在本综述中,我们将进一步深入研究天然和合成香豆素作为COX抑制剂的情况。尽管该研究仍处于初期阶段,但我们相信有很大的发展空间。

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