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6,7-脱氢洛里桉酮及其从(科德)A.J.帕顿中获得的衍生物的生物活性

Biological Activity of 6,7-Dehydroxyroyleanone and Derivatives Obtained from (Codd) A.J.Paton.

作者信息

Filipe Márcia S, Domínguez-Martín Eva M, Pires Tânia C S P, Finimundy Tiane C, Melgar Bruno, Mandim Filipa, Isca Vera M S, Pereira Raquel, Teixidó-Trujillo Silvia, Capote Natalia A, Nikolić Milan, Filipović Nenad, Díaz-Lanza Ana M, Figueiredo Ana Cristina, Barros Lillian, Rijo Patrícia

机构信息

CBIOS-Universidade Lusófona's Research Center for Biosciences & Health Technologies, Campo Grande 376, 1749-024 Lisbon, Portugal.

Departamento de Ciencias Biomédicas (Área de Farmacología, Nuevos agentes antitumorales, Acción tóxica sobre células leucémicas), Facultad de Farmacia, Universidad de Alcalá de Henares, 28805 Madrid, España.

出版信息

ACS Omega. 2024 Apr 8;9(16):18113-18118. doi: 10.1021/acsomega.3c10071. eCollection 2024 Apr 23.

Abstract

The genus (Lamiaceae) is known to be rich in abietane diterpenes. The bioactive 6,7-dehydroxyroyleanone (DHR, ) was previously isolated from var. and var. . This study aimed to explore the occurrence of DHR, , in and the potential bioactivities of new semisynthetic derivatives from DHR, . Several extraction methods were evaluated, and the hydrodistillation, using a Clevenger apparatus, afforded the highest yield (77.8 mg/g of in the essential oil). Three new acyl derivatives (-) were successfully prepared from (yields of 86-95%). Compounds - showed antioxidant activity, antibacterial effects, potent cytotoxic activity against several cell lines, and enhanced anti-inflammatory activity that surpassed dexamethasone (positive control). These findings encourage further exploration of derivatives - for potential mechanisms of antitumoral, antioxidant, and anti-inflammatory capabilities, studying both safety and efficacy.

摘要

唇形科植物已知富含松香烷二萜类化合物。具有生物活性的6,7 - 脱氢罗伊烷酮(DHR)先前已从[具体植物变种1]和[具体植物变种2]中分离出来。本研究旨在探究DHR在[具体植物]中的存在情况,以及DHR新半合成衍生物的潜在生物活性。对几种提取方法进行了评估,使用克莱文杰装置进行水蒸馏得到的产量最高(精油中每克[具体植物]含77.8毫克)。成功从[具体物质]制备了三种新的酰基衍生物([衍生物名称])(产率为86 - 95%)。化合物[具体化合物名称]表现出抗氧化活性、抗菌作用、对几种细胞系的强细胞毒性活性以及超过地塞米松(阳性对照)的增强抗炎活性。这些发现鼓励进一步探索衍生物[具体化合物名称]的抗肿瘤、抗氧化和抗炎能力的潜在机制,同时研究其安全性和有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fd4/11044231/b6de02075f5b/ao3c10071_0001.jpg

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