دورية أكاديمية
أعرض في EDS

Antileishmanial activity of 2-amino-thiophene derivative SB-200.

التفاصيل البيبلوغرافية
العنوان: Antileishmanial activity of 2-amino-thiophene derivative SB-200.
المؤلفون: Sousa JPA; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil., Sousa JMS; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil., Rodrigues RRL; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil., Nunes TAL; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil., Machado YAA; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil., Araujo AC; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil., da Silva IGM; Microscopy and Microanalysis Laboratory, Department of Cell Biology, Institute of Biological Sciences, University of Brasília, Brasília, Brazil., Barros-Cordeiro KB; Microscopy and Microanalysis Laboratory, Department of Cell Biology, Institute of Biological Sciences, University of Brasília, Brasília, Brazil., Báo SN; Microscopy and Microanalysis Laboratory, Department of Cell Biology, Institute of Biological Sciences, University of Brasília, Brasília, Brazil., Alves MMM; Laboratory of Antileishmania Activity, Medicinal Plants Research Center, Federal University of Piauí, Teresina 64049-550, Brazil., Mendonça-Junior FJB; Molecular Synthesis and Vectorization Laboratory, Department of Biological Sciences, State University of Paraíba, 58071-160 João Pessoa, PB, Brazil., Rodrigues KADF; Infectious Disease Laboratory, Campus Ministro Reis Velloso, Federal University of Parnaíba Delta, 64202-020 Parnaíba, PI, Brasil. Electronic address: klinger@ufpi.edu.br.
المصدر: International immunopharmacology [Int Immunopharmacol] 2023 Oct; Vol. 123, pp. 110750. Date of Electronic Publication: 2023 Aug 01.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Country of Publication: Netherlands NLM ID: 100965259 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1878-1705 (Electronic) Linking ISSN: 15675769 NLM ISO Abbreviation: Int Immunopharmacol Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Amsterdam ; New York : Elsevier Science, c2001-
مواضيع طبية MeSH: Antiprotozoal Agents*/pharmacology , Antiprotozoal Agents*/therapeutic use , Leishmaniasis*/drug therapy , Leishmania infantum*, Animals ; Chlorocebus aethiops ; Mice ; Vero Cells ; Thiophenes/pharmacology ; Thiophenes/therapeutic use ; Mice, Inbred BALB C
مستخلص: Leishmaniasis, presenting the highest number of cases worldwide is one of the most serious Neglected Tropical Diseases (NTDs). Clinical manifestations are intrinsically related to the host's immune response making immunomodulatory substances the target of numerous studies on antileishmanial activity. The currently available drugs used for treatment present various problems including high toxicity, low efficacy, and associated drug resistance. The search for therapeutic alternatives is urgent, and in this context, thiophene derivatives appear to be a promising therapeutic alternative (many have shown promising anti-leishmanial activity). The objective of this study was to investigate the antileishmanial activity of the 2-amino-thiophenic derivative SB-200. The thiophenic derivative was effective in inhibiting the growth of Leishmania braziliensis, Leishmania major, and Leishmania infantum promastigotes, obtaining respective IC 50 values of 4.25 μM, 4.65 μM, and 3.96 μM. For L. infantum, it was demonstrated that the antipromastigote effect of SB-200 is associated with cell membrane integrity losses, and with morphological changes observed during scanning and transmission electron microscopy. Cytotoxicity was performed for J774.A1 macrophages and VERO cells, to obtain a CC 50 of 42.52 μM and a SI of 10.74 for macrophages and a CC 50 of 39.2 μM and an SI of 9.89 for VERO cells. The anti-amastigote activity of SB-200 revealed an IC 50 of 2.85 μM and an SI of 14.97 against macrophages and SI of 13.8 for VERO cells. The anti-amastigote activity of SB-200 is associated with in vitro immunomodulation. For acute toxicity, SB-200 against Zophobas morio larvae permitted 100% survival. We conclude that the 2-amino-thiophenic derivative SB-200 is a promising candidate for in vivo anti-leishmania drug tests to evaluate its activity, efficacy, and safety.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier B.V. All rights reserved.)
فهرسة مساهمة: Keywords: 2-Amino-thiophene derivative; Immunomodulation; Leishmaniasis; Visceral leishmaniasis
المشرفين على المادة: 0 (Thiophenes)
0 (Antiprotozoal Agents)
تواريخ الأحداث: Date Created: 20230803 Date Completed: 20230922 Latest Revision: 20230922
رمز التحديث: 20240628
DOI: 10.1016/j.intimp.2023.110750
PMID: 37536181
قاعدة البيانات: MEDLINE
الوصف
تدمد:1878-1705
DOI:10.1016/j.intimp.2023.110750