摘要
倍半萜烯是已经广泛研究其生物活性的天然产物,证明了它们作为药物开发有用支架的潜力。考虑到不同的衍生物,倍半萜内酯已被评估,特别是在体内研究中的癌细胞和抗肿瘤效力。它们的生物活性与反应性α-亚甲基-γ-内酯基团(αMγL)的存在严格相关。尽管如此,还缺少αMγL的其他几种倍半萜是已知的,并且已经研究了它们在新药开发中的生物效应和潜在用途。在这篇综述中,我们关注了几种倍半萜烯,它们不呈现αMγL部分,并且可能具有作为新药开发支架的未来潜力,即属于carotane型(daucanes)的双环化合物,其显示出抗增殖和雌激素代理商。单环藿烷衍生物与Zerumbone相关,并且双环化合物β-石竹烯及其衍生物已被考虑用于癌症和炎症领域。值得注意的是,在本综述中报道的关于倍半萜的已发表研究集中于日益重要的疾病,如雌激素,抗增殖,骨质流失,免疫缺陷和抗肿瘤活性。一些天然的“旧”倍半萜可以考虑它们在药物发现和抵消这些“新”挑战中的可能作用。
关键词: α-亚甲基-γ内酯,内酯组,倍半萜烯,抗肿瘤剂,肿瘤,治疗剂,疾病。
Current Medicinal Chemistry
Title:New Drugs from Old Natural Compounds: Scarcely Investigated Sesquiterpenes as New Possible Therapeutic Agents
Volume: 25 Issue: 10
关键词: α-亚甲基-γ内酯,内酯组,倍半萜烯,抗肿瘤剂,肿瘤,治疗剂,疾病。
摘要: Sesquiterpenes are natural products that have been extensively studied for their bioactivities, evidencing their potentiality as useful scaffolds for the development of drugs. Considering the different derivatives, the sesquiterpene lactones have been evaluated, especially on cancer cell and antineoplastic efficacy in in vivo studies. Their bioactivity is strictly related to the presence of the reactive α-methylene-γ-lactone group (αMγL). Nevertheless, several other sesquiterpenes lacking αMγL are known and have been studied for their biological effects and potential usefulness in the development of new drugs. In this review, we focused on several sesquiterpenes that are not presenting the αMγL moiety and may have future potential as scaffold for the development of new drugs, namely the bicyclic compounds belonging to the carotane type (daucanes) that present significant effects as antiproliferative and estrogenic agents. The monocyclic humulane derivatives correlated to zerumbone, and the bicyclic compound beta-caryophyllene and its derivatives that have been considered in the field of cancer and inflammation. It is noteworthy that published studies on sesquiterpenes, reported in this review, focus on pathologies of increasing importance, like estrogen, anti-proliferative, bone loss, immunity deficiency and anti-tumour activities. Some of the natural “old” sesquiterpenes can be considered for their possible role in drug discovery and in counteracting these “new” challenges.
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Cite this article as:
New Drugs from Old Natural Compounds: Scarcely Investigated Sesquiterpenes as New Possible Therapeutic Agents, Current Medicinal Chemistry 2018; 25 (10) . https://dx.doi.org/10.2174/0929867324666170404150351
DOI https://dx.doi.org/10.2174/0929867324666170404150351 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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