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Piplartine Synthetic Analogs: In Silico Analysis and Antiparasitic Study against Trypanosoma cruzi

التفاصيل البيبلوغرافية
العنوان: Piplartine Synthetic Analogs: In Silico Analysis and Antiparasitic Study against Trypanosoma cruzi
المؤلفون: Rayanne H. N. Silva, Emanuel P. Magalhães, Rebeca C. Gomes, Yunierkis Perez-Castillo, Alice M. C. Martins, Damião P. de Sousa
المصدر: Applied Sciences, Vol 13, Iss 20, p 11585 (2023)
بيانات النشر: MDPI AG, 2023.
سنة النشر: 2023
المجموعة: LCC:Technology
LCC:Engineering (General). Civil engineering (General)
LCC:Biology (General)
LCC:Physics
LCC:Chemistry
مصطلحات موضوعية: piperlongumine, cytotoxicity, natural products, trypanocide, alkaloid, Trypanosoma, Technology, Engineering (General). Civil engineering (General), TA1-2040, Biology (General), QH301-705.5, Physics, QC1-999, Chemistry, QD1-999
الوصف: Neglected tropical diseases (NTDs) cause thousands of deaths each year. Among these diseases, we find Chagas disease, whose etiologic agent is Trypanosoma cruzi. Piplartine is an alkamide present in various species of the genus Piper that possess trypanocidal activity. In this study, the antiparasitic potential of a collection of 23 synthetic analogs of piplartine against Trypanosoma cruzi was evaluated in vitro. The compounds were prepared via amidation and esterification reactions using 3,4,5-trimethoxybenzoic acid as starting material. The products were structurally characterized using 1H and 13C nuclear magnetic resonance, infrared spectroscopy, and high-resolution mass spectrometry. Of the twenty-three compounds tested in the cytotoxic activity assays, five presented good activity in the trypomastigote, epimastigote, and amastigote forms of T. cruzi, showing IC50 values ranging from 2.21 to 35.30 µM, 4.06 to 34.30 µM, and 1.72 to 5.72 µM, respectively. N-iso-butyl-3,4,5-trimethoxybenzamide (17) presented potent trypanocidal activity with an IC50 = 2.21 µM and selectively caused apoptosis (SI = 298.6). Molecular modeling experiments suggested the inhibitions of the histone deacetylase (HDAC) enzyme as the main trypanocidal mechanism of action of compound 17 in T. cruzi.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 13201158
2076-3417
Relation: https://www.mdpi.com/2076-3417/13/20/11585; https://doaj.org/toc/2076-3417
DOI: 10.3390/app132011585
URL الوصول: https://doaj.org/article/241f6e5e19cf40b58a3eb1caf6a69517
رقم الأكسشن: edsdoj.241f6e5e19cf40b58a3eb1caf6a69517
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:13201158
20763417
DOI:10.3390/app132011585