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新型腺嘌呤衍生物的研究:L 的体外乙酰胆碱酯酶抑制活性、抗菌活性和细胞毒性评价。

New Adenosine Derivatives from L.: In Vitro Anticholinesterase, Antimicrobial, and Cytotoxic Evaluation of Its Extracts.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza 11787, Egypt.

Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City, Sadat 32897, Egypt.

出版信息

Molecules. 2021 Feb 24;26(5):1198. doi: 10.3390/molecules26051198.

DOI:10.3390/molecules26051198
PMID:33668096
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7956659/
Abstract

Aizoaceae is a large succulent family characterized by many psychoactive species. L., a wild neglected plant traditionally used in gastrointestinal ailments, has been the subject of a limited number of phytochemical and biological studies. Therefore, herein, we investigated the in vitro cytotoxic, antimicrobial, and anticholinesteraseactivity of the aerial parts of L. and analyzed the phytochemical compositions of the lipoidal and alkaloidal fractions. Petroleum ether extract showed the presence of behenic and tricosylic acid, while an in-depth investigation of the alkaloidal fraction revealed the identification of new adenine based alkaloids (1-5), which were isolated and identified for the first time from L. Their structures were elucidated based on extensive spectroscopic analyses. The alkaloidal extract showed a powerful cytotoxic effect (IC 14-28 μg/mL), with the best effect against colon carcinoma, followed by liver and breast carcinomas. The alkaloidal extract also had a potent effect against and , with minimum inhibitory concentrations (MIC) values of 312.5 and 625 µg/mL. The in vitro anticholinesterase activity was potent, with IC < 200 ng/mL for the tested extracts compared with 27.29 ± 0.49 ng/mL for tacrine.

摘要

马齿苋科是一个大型肉质植物科,其特点是有许多具有精神活性的物种。马齿苋,一种野生的被忽视的植物,传统上用于治疗胃肠道疾病,已经成为少数植物化学和生物学研究的主题。因此,在这里,我们研究了 马齿苋地上部分的体外细胞毒性、抗菌和乙酰胆碱酯酶活性,并分析了脂类和生物碱部分的化学成分。石油醚提取物显示存在山嵛酸和二十三酸,而对生物碱部分的深入研究揭示了鉴定出的新型腺嘌呤基生物碱(1-5),这些生物碱首次从马齿苋中分离出来并鉴定出来。它们的结构是基于广泛的光谱分析来阐明的。生物碱提取物具有强大的细胞毒性作用(IC 14-28 μg/mL),对结肠癌的效果最好,其次是肝癌和乳腺癌。生物碱提取物对 和 也有很强的作用,最小抑菌浓度(MIC)值分别为 312.5 和 625 μg/mL。体外乙酰胆碱酯酶活性很强,与他克林的 27.29 ± 0.49 ng/mL 相比,测试提取物的 IC < 200 ng/mL。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6708/7956659/e5deeee3c10e/molecules-26-01198-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6708/7956659/ceec81f0e6bd/molecules-26-01198-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6708/7956659/e5deeee3c10e/molecules-26-01198-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6708/7956659/ceec81f0e6bd/molecules-26-01198-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6708/7956659/e5deeee3c10e/molecules-26-01198-g002.jpg

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