GC-MS Analysis, Bioactivity-based Molecular Networking and Antiparasitic Potential of the Antarctic Alga Desmarestia antarctica

P. Colepicolo-Neto, H. Debonsi, Gustavo Souza dos Santos, K. C. Rangel, Thaiz Rodrigues Teixeira, L. R. Gaspar, Péricles Gama Abreu-Filho, L. M. Pereira, A. P. Yatsuda, M. E. Gallon, L. Gobbo-Neto, Leandro da Costa Clementino, M. Graminha, Laís Garcia Jordão, A. Pohlit
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引用次数: 3

Abstract

Abstract Leishmaniasis, malaria, and neosporosis are parasitic diseases that affect humans and animals, causing public health problems and billions in economic losses. Despite the advances in the development of new drugs, the severe side effects of available leishmaniasis treatments, the Plasmodium spp. resistance to antimalarial drugs, and the lack of a specific treatment against neosporosis lead us to the search for new anti-protozoan molecules from underexplored sources such as the Antarctic marine environment. Herein, we describe for the first time the chemical profile of Desmarestia antarctica crude extract and fractions using GC-MS and LC-MS/MS (molecular networking) approaches, and evaluate their antiparasitic activity against Leishmania amazonensis, Neospora caninum, and multi-drug-resistant Plasmodium falciparum. Furthermore, the cytotoxicity in 3T3 BALB/c fibroblasts and Vero cells was evaluated. D. antarctica fraction E ( IC50 of 53.8±4.4 μg mL− 1 and selectivity index of 3.3) exhibited anti-promastigote activity and was fourfold more selective to L. amazonensis rather than to the host cells. D. antarctica fraction D (IC50 of 1.6±1.3 μg mL− 1 and selectivity index of 27.8), D. antarctica fraction F (IC50 of 3.1±2.1 μg mL− 1 and selectivity index of 23.1), and D. antarctica fraction H (IC50 of 3.1±2.0 μg mL− 1 and selectivity index of 12.9) presented the highest antiparasitic effects against N. caninum with no cytotoxic effects. Also, D. antarctica fraction D presented a significant antiplasmodial inhibitory effect (IC50 of 19.1±3.9 μg mL− 1 and selectivity index of 6.0). GC-MS analysis indicated palmitic acid, myristic acid, fucosterol, phthalic acid, di(2-methylbutyl) ester, loliolide, and neophytadiene as the main components in the active fractions. In addition, this is the first report of a biological screening of macroalgae secondary metabolites against N. caninum parasites.
南极藻的气相色谱-质谱分析、生物活性分子网络及抗寄生潜力
利什曼病、疟疾和新孢子虫病是影响人类和动物的寄生虫病,造成公共卫生问题和数十亿美元的经济损失。尽管在开发新药方面取得了进展,但现有利什曼病治疗方法的严重副作用、疟原虫对抗疟疾药物的耐药性以及缺乏针对新孢子虫病的特异性治疗方法导致我们从未充分开发的来源(如南极海洋环境)寻找新的抗原生动物分子。本研究首次采用GC-MS和LC-MS/MS(分子网络)方法对南极德马提亚粗提物及其组分进行化学分析,并评价其对亚马逊利什曼原虫、犬新孢子虫和多重耐药恶性疟原虫的抗寄生活性。此外,还评估了3T3 BALB/c成纤维细胞和Vero细胞的细胞毒性。D. antarctica提取物E (IC50为53.8±4.4 μ mL−1,选择性指数为3.3)具有抗promastigote活性,对亚马逊乳杆菌的选择性比对宿主细胞的选择性高4倍。其中,南极D组分(IC50为1.6±1.3 μ mL−1,选择性指数为27.8)、南极F组分(IC50为3.1±2.1 μ mL−1,选择性指数为23.1)和南极H组分(IC50为3.1±2.0 μ mL−1,选择性指数为12.9)对犬蜱的抗寄生作用最强,无细胞毒作用。此外,南极草提取物D具有显著的抗疟原虫抑制作用(IC50为19.1±3.9 μ mL−1,选择性指数为6.0)。GC-MS分析表明,棕榈酸、肉豆蔻酸、木甾醇、邻苯二甲酸、二(2-甲基丁基)酯、油橄榄内酯和新茶树烯为活性部位的主要成分。此外,本文还首次报道了大型藻类次生代谢物的生物筛选。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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