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硫代萜类化合物作为潜在的抗血栓药物:分子对接、抗聚集、抗凝和抗氧化活性。

Thioterpenoids as Potential Antithrombotic Drugs: Molecular Docking, Antiaggregant, Anticoagulant and Antioxidant Activities.

机构信息

G.A. Krestov Institute of Solution Chemistry of the Russian Academy of Sciences, 1 Akademicheskaya Street, 153045 Ivanovo, Russia.

Biologically Active Terpenoids Laboratory, Institute of Fundamental Medicine and Biology, Kazan Federal University, 18 Kremlevskaya Street, 420008 Kazan, Russia.

出版信息

Biomolecules. 2022 Oct 30;12(11):1599. doi: 10.3390/biom12111599.

Abstract

Natural monoterpenes and their derivatives are widely considered as effective ingredients for the design and production of new biologically active compounds with high antioxidant, antimicrobial and anti-protozoa properties. In this study, we synthesized two series of thiotherpenoids "sulfide-sulfoxide-sulfone", with different bicyclic monoterpene skeleton (bornane and pinane) structures. The effect of the obtained compounds on platelet aggregation was investigated by using the molecular docking technique. The obtained data revealed that all the synthesized compounds may act as potential inhibitors of platelet aggregation. Moreover, the studied sulfides have shown high antioxidant activity as revealed by lipid peroxidation (LPO) process inhibition in a non-cellular substrate containing animal lipids. The sulfides were able to inhibit erythrocyte oxidative hemolysis, to reduce the accumulation of secondary LPO products in cells and to prevent the oxidation of native oxyhemoglobin. Additionally, the corresponding sulfones and sulfoxides exhibited insignificant antioxidant activity. However, the sulfides were found to exhibit significant antiaggregant and anticoagulant effects. These findings suggest as well that the sulfides could serve as a leader compound for future research and possible practical applications.

摘要

天然单萜及其衍生物被广泛认为是设计和生产具有高抗氧化、抗菌和抗原生动物特性的新型生物活性化合物的有效成分。在这项研究中,我们合成了两个系列的硫代萜类化合物 "硫醚-亚砜-砜",具有不同的双环单萜骨架(莰烷和蒎烷)结构。通过分子对接技术研究了获得的化合物对血小板聚集的影响。获得的数据表明,所有合成的化合物都可能作为血小板聚集的潜在抑制剂。此外,研究表明,所研究的硫醚在含有动物脂质的非细胞基质中通过抑制脂质过氧化(LPO)过程显示出高抗氧化活性。硫醚能够抑制红细胞氧化溶血,减少细胞内次级 LPO 产物的积累,并防止天然氧合血红蛋白的氧化。此外,相应的砜和亚砜表现出不显著的抗氧化活性。然而,硫醚被发现具有显著的抗聚集和抗凝作用。这些发现表明,硫醚可以作为未来研究和可能的实际应用的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/97cd/9687754/d4b46689a1d6/biomolecules-12-01599-g001.jpg

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