Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2020-08-31 , DOI: 10.2174/1570180817999200421144007 Sudip Kumar Mandal 1 , Utsab Debnath 2 , Amresh Kumar 3 , Sabu Thomas 4 , Subhash Chandra Mandal 5 , Manabendra Dutta Choudhury 3 , Partha Palit 6
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Background and Introduction: Sesquiterpene lactones are a class of secondary metabolite that contains sesquiterpenoids and lactone ring as pharmacophore moiety. A large group of bioactive secondary metabolites such as phytopharmaceuticals belong to this category. From the Asteraceae family-based medicinal plants, more than 5,000 sesquiterpene lactones have been reported so far. Sesquiterpene lactone-based pharmacophore moieties hold promise for broad-spectrum biological activities against cancer, inflammation, parasitic, bacterial, fungal, viral infection and other functional disorders. Moreover, these moiety based phytocompounds have been highlighted with a new dimension in the natural drug discovery program worldwide after the 2015 Medicine Nobel Prize achieved by the Artemisinin researchers.
Objective: These bitter substances often contain an α, β-unsaturated-γ-lactone as a major structural backbone, which in recent studies has been explored to be associated with anti-tumor, cytotoxic, and anti-inflammatory action. Recently, the use of sesquiterpene lactones as phytomedicine has been increased. This study will review the prospect of sesquiterpene lactones against inflammation and cancer. Methods: Hence, we emphasized on the different features of this moiety by incorporating its structural diversity on biological activities to explore structure-activity relationships (SAR) against inflammation and cancer. Results: How the dual mode of action such as anti-inflammatory and anti-cancer has been exhibitedby these phytopharmaceuticals will be forecasted in this study. Furthermore, the correlation of anti-inflammatory and anti-cancer activity executed by the sesquiterpene lactones for fruitful phytotherapy will also be revealed in the present review in the milieu of pharmacophore activity relation and pharmacodynamics study as well. Conclusion: So, these metabolites are paramount in phytopharmacological aspects. The present discussion on the future prospect of this moiety based on the reported literature could be a guide for anti-inflammatory and anti-cancer drug discovery programs for the upcoming researchers.中文翻译：
天然倍半萜内酯在预防和治疗炎性疾病和癌症中的应用：基于化学和药理学方面的这种新兴治疗方法的系统研究
背景与简介：倍半萜内酯是一类次生代谢产物，含有倍半萜类和内酯环作为药效团部分。一大类具有生物活性的次生代谢物，例如植物性药物，属于这一类。迄今为止，从菊科家族的药用植物中已经报道了5,000多种倍半萜烯内酯。基于倍半萜内酯的药效基团部分有望在广谱的生物活性中抵抗癌症，炎症，寄生虫，细菌，真菌，病毒感染和其他功能性疾病。此外，在青蒿素研究人员获得2015年诺贝尔医学奖之后，这些基于基团的植物化合物在全球天然药物发现计划中得到了新的强调。
目的：这些苦味物质通常含有α，β-不饱和-γ-内酯作为主要结构骨架，在最近的研究中已发现其与抗肿瘤，细胞毒性和抗炎作用有关。近来，倍半萜内酯作为植物药的使用已经增加。这项研究将审查倍半萜内酯抗炎症和癌症的前景。 方法：因此，我们通过将其结构多样性纳入生物学活性中来强调该部分的不同特征，以探索针对炎症和癌症的构效关系（SAR）。 结果：本研究将预测这些植物药物如何表现出抗炎和抗癌等双重作用方式。此外，在有关药效基团活性关系和药效学研究的环境中，倍半萜烯内酯执行的用于有效植物疗法的抗炎和抗癌活性的相关性也将在本综述中得到揭示。结论：因此，这些代谢物在植物药理学方面至关重要。基于所报道的文献，关于该部分的未来前景的当前讨论可以为即将到来的研究人员的抗炎和抗癌药物发现计划提供指导。
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