دورية أكاديمية
أعرض في EDS

Anti-diarrheal therapeutic potential of diminazene aceturate stimulation of the ACE II/Ang-(1-7)/Mas receptor axis in mice: A trial study.

التفاصيل البيبلوغرافية
العنوان: Anti-diarrheal therapeutic potential of diminazene aceturate stimulation of the ACE II/Ang-(1-7)/Mas receptor axis in mice: A trial study.
المؤلفون: Souza LKM; The Northeast Biotechnology Network (RENORBIO), Federal University of Piauí, Teresina, PI 64049-550, Brazil; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (Lafidg), Federal University of Parnaíba Delta (UFDPar), Av. São Sebastião, n° 2819, CEP 64202-02 Parnaíba, PI, Brazil. Electronic address: luankelves11@gmail.com., Nogueira KM; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Araújo TSL; The Northeast Biotechnology Network (RENORBIO), Federal University of Piauí, Teresina, PI 64049-550, Brazil; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (Lafidg), Federal University of Parnaíba Delta (UFDPar), Av. São Sebastião, n° 2819, CEP 64202-02 Parnaíba, PI, Brazil., Sousa NA; The Northeast Biotechnology Network (RENORBIO), Federal University of Piauí, Teresina, PI 64049-550, Brazil; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (Lafidg), Federal University of Parnaíba Delta (UFDPar), Av. São Sebastião, n° 2819, CEP 64202-02 Parnaíba, PI, Brazil., Sousa FBM; The Northeast Biotechnology Network (RENORBIO), Federal University of Piauí, Teresina, PI 64049-550, Brazil; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (Lafidg), Federal University of Parnaíba Delta (UFDPar), Av. São Sebastião, n° 2819, CEP 64202-02 Parnaíba, PI, Brazil., Oliveira AP; The Northeast Biotechnology Network (RENORBIO), Federal University of Piauí, Teresina, PI 64049-550, Brazil; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (Lafidg), Federal University of Parnaíba Delta (UFDPar), Av. São Sebastião, n° 2819, CEP 64202-02 Parnaíba, PI, Brazil., Sales T; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Silva K; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Rocha TM; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Leal LKAM; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Magalhães PJC; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Souza MHLP; Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, CE 60430-275, Brazil., Medeiros JVR; The Northeast Biotechnology Network (RENORBIO), Federal University of Piauí, Teresina, PI 64049-550, Brazil; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (Lafidg), Federal University of Parnaíba Delta (UFDPar), Av. São Sebastião, n° 2819, CEP 64202-02 Parnaíba, PI, Brazil; Biotechnology and Biodiversity Center Research, BIOTEC, Federal University of Parnaíba Delta, Parnaíba, PI 64202-020, Brazil.
المصدر: Biochemical pharmacology [Biochem Pharmacol] 2021 Apr; Vol. 186, pp. 114500. Date of Electronic Publication: 2021 Mar 06.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Country of Publication: England NLM ID: 0101032 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-2968 (Electronic) Linking ISSN: 00062952 NLM ISO Abbreviation: Biochem Pharmacol Subsets: MEDLINE
أسماء مطبوعة: Publication: Oxford : Elsevier Science
Original Publication: Oxford, New York [etc.] Paragamon Press.
مواضيع طبية MeSH: Angiotensin I/*metabolism , Angiotensin II/*metabolism , Antidiarrheals/*therapeutic use , Diarrhea/*metabolism , Diminazene/*analogs & derivatives , Peptide Fragments/*metabolism , Proto-Oncogene Proteins/*metabolism , Receptors, G-Protein-Coupled/*metabolism, Animals ; Antidiarrheals/pharmacology ; Castor Oil/toxicity ; Diarrhea/chemically induced ; Diarrhea/drug therapy ; Diminazene/pharmacology ; Diminazene/therapeutic use ; Dose-Response Relationship, Drug ; Gastrointestinal Tract/drug effects ; Gastrointestinal Tract/metabolism ; Male ; Mice ; Proto-Oncogene Mas ; Renin-Angiotensin System/drug effects ; Renin-Angiotensin System/physiology
مستخلص: The angiotensin (Ang) II converting enzyme (ACE II) pathway has recently been shown to be associated with several beneficial effects on the body, especially on the cardiac system and gastrointestinal tract. ACE II is responsible for converting Ang II into the active peptide Ang-(1-7), which in turn binds to a metabotropic receptor, the Mas receptor (MasR). Recent studies have demonstrated that Diminazene Aceturate (DIZE), a trypanosomicide used in animals, activates the ACE II pathway. In this study, we aimed to evaluate the antidiarrheal effects promoted by the administration of DIZE to activate the ACE II/Ang-(1-7)/MasR axis in induced diarrhea mice models. The results show that activation of the ACE II pathway exerts antidiarrheal effects that reduce total diarrheal stools and enteropooling. In addition, it increases Na + /K + -ATPase activity and reduces gastrointestinal transit and thus inhibits contractions of intestinal smooth muscle; decreases transepithelial electrical resistance, epithelial permeability, PGE2-induced diarrhea, and proinflammatory cytokines; and increases anti-inflammatory cytokines. Enzyme-linked immunosorbent assay (ELISA) demonstrated that DIZE, when activating the ACE II/Ang-(1-7)/MasR axis, can still interact with GM1 receptors, which reduces cholera toxin-induced diarrhea. Therefore, activation of the ACE II/Ang-(1-7)/MasR axis can be an important pharmacological target for the treatment of diarrheal diseases.
(Copyright © 2021 Elsevier Inc. All rights reserved.)
فهرسة مساهمة: Keywords: ACE II; Angiotensin; Cholera; Diarrhea; Inflammation
المشرفين على المادة: 0 (Antidiarrheals)
0 (Peptide Fragments)
0 (Proto-Oncogene Mas)
0 (Proto-Oncogene Proteins)
0 (Receptors, G-Protein-Coupled)
11128-99-7 (Angiotensin II)
8001-79-4 (Castor Oil)
9041-90-1 (Angiotensin I)
IJ3FUK8MOF (angiotensin I (1-7))
JI8SAD85NO (diminazene aceturate)
Y5G36EEA5Z (Diminazene)
تواريخ الأحداث: Date Created: 20210308 Date Completed: 20210630 Latest Revision: 20211204
رمز التحديث: 20221213
DOI: 10.1016/j.bcp.2021.114500
PMID: 33684388
قاعدة البيانات: MEDLINE
الوصف
تدمد:1873-2968
DOI:10.1016/j.bcp.2021.114500