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用于寻找抗癌先导分子的 spp. 提取物的初步生物活性筛选

Preliminary Biological Activity Screening of spp. Extracts for the Search of Anticancer Lead Molecules.

作者信息

Ntungwe Epole, Domínguez-Martín Eva María, Teodósio Catarina, Teixidó-Trujillo Silvia, Armas Capote Natalia, Saraiva Lucilia, Díaz-Lanza Ana María, Duarte Noélia, Rijo Patrícia

机构信息

CBIOS-Universidade Lusófona Research Center for Biosciences & Health Technologies, Universidade Lusófona de Humanidades e Tecnologias, Campo Grande 376, 1749-024 Lisboa, Portugal.

Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá de Henares, Ctra. A2, Km 33.100-Campus Universitario, 28805 Alcalá de Henares, Spain.

出版信息

Pharmaceuticals (Basel). 2021 Apr 23;14(5):402. doi: 10.3390/ph14050402.

DOI:10.3390/ph14050402
PMID:33922685
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8146581/
Abstract

species (Lamiaceae) have been employed in traditional medicine and this is now validated by the presence of bioactive abietane-type diterpenoids. Herein, sixteen acetonic extracts were prepared by ultrasound-assisted extraction and their biological activity was screened. The antimicrobial activity of each extract was screened against yeasts, and Gram-positive and Gram-negative bacteria. The and extracts possessed significant activity against and (microdilution method). Moreover, all extracts showed antioxidant activity using the DPPH method, with and extracts having the highest scavenging activities. Selected by the model, and possessed low micromolar anti-proliferative activities in human colon, breast, and lung cancer cell lines. Furthermore, the most bioactive extract of leaves and the known abietane diterpene, 7α-acetoxy-6β-hydroxyroyleanone isolated from this plant, were tested against the aggressive type triple negative breast cancer (MDA-MB-231S). extract reduced the viability of MDA-MB-231S cancer cell line cells, showing an IC value of 25.6 µg/mL. The IC value of 7α-acetoxy-6β-hydroxyroyleanone was 5.5 µM (2.15 µg/mL), suggesting that this lead molecule is a potential starting tool for the development of anti-cancer drugs.

摘要

唇形科植物已被用于传统医学,现在生物活性枞酸型二萜类化合物的存在证实了这一点。在此,通过超声辅助提取制备了16种丙酮提取物,并对其生物活性进行了筛选。针对酵母、革兰氏阳性菌和革兰氏阴性菌筛选了每种提取物的抗菌活性。[提取物名称1]和[提取物名称2]提取物对[细菌名称1]和[细菌名称2]具有显著活性(微量稀释法)。此外,所有提取物使用DPPH法均显示出抗氧化活性,其中[提取物名称3]和[提取物名称4]提取物具有最高的清除活性。通过[模型名称]模型筛选,[提取物名称5]和[提取物名称6]在人结肠、乳腺和肺癌细胞系中具有低微摩尔级的抗增殖活性。此外,对[植物名称]叶的生物活性最强的提取物以及从该植物中分离出的已知枞酸二萜7α - 乙酰氧基 - 6β - 羟基罗勒烯酮,针对侵袭性三阴性乳腺癌(MDA - MB - 231S)进行了测试。[提取物名称7]提取物降低了MDA - MB - 231S癌细胞系细胞的活力,IC值为25.6 µg/mL。7α - 乙酰氧基 - 6β - 羟基罗勒烯酮的IC值为5.5 µM(2.15 µg/mL),表明这种先导分子是开发抗癌药物的潜在起始工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d801/8146581/88e23ca843c9/pharmaceuticals-14-00402-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d801/8146581/88e23ca843c9/pharmaceuticals-14-00402-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d801/8146581/88e23ca843c9/pharmaceuticals-14-00402-g001.jpg

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