Studies on Secondary Metabolites and In Vitro and In Silico Anticholinesterases Activities of the Sea Urchin Echinometra Mathaei Crude Venoms from the Persian Gulf-Bushehr

IF 0.7 Q4 CHEMISTRY, MEDICINAL Natural Products Journal Pub Date : 2023-06-22 DOI:10.2174/2210315514666230622144244
G. Mohebbi, Hamideh Dehghani, M. Rashedinia, A. Vazirizadeh
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Abstract

Echinoderms are a unique source of amazing secondary metabolites with a wide spectrum of biological activities. Several species of sea urchins contain various toxins and biologically active metabolites. One of the most attractive approaches to treating Alzheimer's disease is searching for effective marine natural products with cholinesterase inhibitory activities. The current study is designed to investigate the in vitro and in silico acetylcholinesterase and butyrylcholinesterase inhibitory activities of the Persian Gulf echinoderm sea urchin Echinometra mathaei venom and related chemical compounds. The experiments for LD50, total protein, protein bands, in vitro cholinesterase inhibitory activities, the identity of secondary metabolites, and the in silico evaluations, respectively, were performed by Spearman-Karber, Lowry, SDS-PAGE, Ellman's spectroscopic method, GC-MS, and docking methods. The LD50 (IV rat) of the spine, gonad, and coelomic fluid from sea urchin samples were 2.231 ± 0.09, 1.03 ± 0.05, and 1.12 ± 0.13 mg/ml, respectively. The SDS-PAGE and total protein studies showed that at least a portion of the venom is protein in nature. GC-MS analysis of the identified samples revealed 12, 23, and 21 compounds with different chemical types, including alkaloids, terpenes, and steroids, respectively. According to the results, all samples act as significant inhibitors of both enzymes. In silico data for the identified compounds also confirmed the experimental results. The alkaloid compound 6H-Indolo[3,2,1-de] [1,5] naphthyridine-6-one,1,2,3a,4,5-hexahydro-8-hydroxy-3-methyl (C7) had the highest affinity for both enzymes. Further research is needed to determine whether C7 could be a therapeutic candidate for Alzheimer's disease.
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波斯湾-布什尔海胆粗毒液次生代谢物及体外、体内抗胆碱酯酶活性研究
棘皮动物是一种独特的次级代谢产物来源,具有广泛的生物活性。几种海胆含有各种毒素和生物活性代谢产物。治疗阿尔茨海默病最有吸引力的方法之一是寻找具有胆碱酯酶抑制活性的有效海洋天然产物。本研究旨在研究波斯湾棘皮动物海胆(Echinometramathaei)毒液及其相关化合物的体外和体外乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性。分别采用Spearman-Karber、Lowry、SDS-PAGE、Ellman光谱法、GC-MS和对接法对LD50、总蛋白、蛋白带、体外胆碱酯酶抑制活性、次级代谢产物的鉴定和计算机评价进行了实验。来自海胆样品的脊椎、性腺和体腔液的LD50(IV大鼠)分别为2.231±0.09、1.03±0.05和1.12±0.13 mg/ml。SDS-PAGE和总蛋白研究表明,毒液中至少有一部分是天然蛋白质。对已鉴定样品的GC-MS分析显示,分别有12、23和21种化合物具有不同的化学类型,包括生物碱、萜烯和类固醇。根据结果,所有样品都是这两种酶的重要抑制剂。鉴定化合物的计算机数据也证实了实验结果。生物碱化合物6H-吲哚[3,2,1-de][1,5]萘啶-6-酮,1,2,3a,4,5-六氢-8-羟基-3-甲基(C7)对这两种酶的亲和力最高。需要进一步的研究来确定C7是否可以作为阿尔茨海默病的候选治疗药物。
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来源期刊
Natural Products Journal
Natural Products Journal CHEMISTRY, MEDICINAL-
CiteScore
1.70
自引率
0.00%
发文量
91
期刊介绍: The Natural Products Journal a peer reviewed journal, aims to publish all the latest and outstanding developments in natural products. The Natural Products Journal publishes original research articles, full-length/mini reviews, letters and guest edited issues on all aspects of research and development in the field including: isolation, purification, structure elucidation, synthesis and bioactivity of chemical compounds found in nature.
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