Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle

Leptohyptis macrostachys, previously known as Hyptis macrostachys Benth., is used in folk medicine to relieve the symptoms of asthma, cough, and bronchitis. Recently, we showed that the ethanol extract obtained from Leptohyptis macrostachys has selective spasmolytic activity on guinea pig ileum. The...

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Main Authors: Iara Leão Luna de Souza, Maria Allynne de Vasconcelos, Anne Dayse Soares da Silva, Polyana Cristina Barros Silva, Carlos Arthur Gouveia Veloso, Diego Igor Alves Fernandes de Araújo, Vicente Carlos de Oliveira Costa, Hilzeth Luna Freire Pessôa, Josean Fechine Tavares, Marcelo Sobral da Silva, Bagnólia Araújo da Silva, Fabiana de Andrade Cavalcante
Format: Article
Language:English
Published: Frontiers Media S.A. 2020-07-01
Series:Frontiers in Pharmacology
Subjects:
Online Access:https://www.frontiersin.org/article/10.3389/fphar.2020.01042/full
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author Iara Leão Luna de Souza
Maria Allynne de Vasconcelos
Anne Dayse Soares da Silva
Polyana Cristina Barros Silva
Carlos Arthur Gouveia Veloso
Diego Igor Alves Fernandes de Araújo
Vicente Carlos de Oliveira Costa
Hilzeth Luna Freire Pessôa
Josean Fechine Tavares
Josean Fechine Tavares
Marcelo Sobral da Silva
Marcelo Sobral da Silva
Bagnólia Araújo da Silva
Bagnólia Araújo da Silva
Fabiana de Andrade Cavalcante
Fabiana de Andrade Cavalcante
author_facet Iara Leão Luna de Souza
Maria Allynne de Vasconcelos
Anne Dayse Soares da Silva
Polyana Cristina Barros Silva
Carlos Arthur Gouveia Veloso
Diego Igor Alves Fernandes de Araújo
Vicente Carlos de Oliveira Costa
Hilzeth Luna Freire Pessôa
Josean Fechine Tavares
Josean Fechine Tavares
Marcelo Sobral da Silva
Marcelo Sobral da Silva
Bagnólia Araújo da Silva
Bagnólia Araújo da Silva
Fabiana de Andrade Cavalcante
Fabiana de Andrade Cavalcante
author_sort Iara Leão Luna de Souza
collection DOAJ
description Leptohyptis macrostachys, previously known as Hyptis macrostachys Benth., is used in folk medicine to relieve the symptoms of asthma, cough, and bronchitis. Recently, we showed that the ethanol extract obtained from Leptohyptis macrostachys has selective spasmolytic activity on guinea pig ileum. Therefore, the aim of this study was to characterize the spasmolytic mechanism of this extract, investigated whether it presents toxicological and antidiarrheal activities. Therefore, the crude ethanolic extract of Leptohyptis macrostachys was analyzed by high-performance liquid chromatographic-diode array detection (HPLC–DAD). The spasmolytic effect was evaluated on guinea pig ileum, toxicological activity using rats and antidiarrheal activity using male and female mice. In HPLC-DAD analysis, Rosmarinic acid (5.44%) was the most abundant phenolic compound, being considered as a chemical marker. The spasmolytic potency of the extract on histamine-induced contraction was reduced in the presence of 1 mM TEA+, a selective big–conductance K+ channels blocker (BKCa). The extract produces a dose–dependent antidiarrheal activity, inhibiting equipotently defecation frequency and liquid stool formation. In addition, the extract has inhibited in a dose–dependent manner both castor oil–induced intestinal transit and intestinal fluid content. Thus, the spasmolytic activity of the extract involves positive modulation of BKCa and its antidiarrheal activity is related to inhibition of intestinal motility and secretion.
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spelling doaj.art-da61ceaa6a8a469eb4c1438ad662e9982022-12-21T20:12:21ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122020-07-011110.3389/fphar.2020.01042563147Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth MuscleIara Leão Luna de Souza0Maria Allynne de Vasconcelos1Anne Dayse Soares da Silva2Polyana Cristina Barros Silva3Carlos Arthur Gouveia Veloso4Diego Igor Alves Fernandes de Araújo5Vicente Carlos de Oliveira Costa6Hilzeth Luna Freire Pessôa7Josean Fechine Tavares8Josean Fechine Tavares9Marcelo Sobral da Silva10Marcelo Sobral da Silva11Bagnólia Araújo da Silva12Bagnólia Araújo da Silva13Fabiana de Andrade Cavalcante14Fabiana de Andrade Cavalcante15Departamento de Ciências Biológicas e Saúde, Universidade Estadual de Roraima, Boa Vista, BrazilInstituto de Ciências Biológicas e da Saúde, Universidade Federal de Alagoas, Maceió, BrazilPrograma de Pós-graduação em Química e Biotecnologia, Instituto de Química, Universidade Federal de Alagoas, Maceió, BrazilInstituto de Ciências Biológicas e da Saúde, Universidade Federal de Alagoas, Maceió, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilDepartamento de Biologia Molecular, Centro de Ciências Exatas e da Natureza, Universidade Federal da Paraíba, João Pessoa, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilDepartamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal da Paraíba, João Pessoa, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilDepartamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal da Paraíba, João Pessoa, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilDepartamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal da Paraíba, João Pessoa, BrazilInstituto de Pesquisa em Fármacos e Medicamentos, Universidade Federal da Paraíba, João Pessoa, BrazilDepartamento de Fisiologia e Patologia, Centro de Ciências da Saúde, Universidade Federal da Paraíba, João Pessoa, BrazilLeptohyptis macrostachys, previously known as Hyptis macrostachys Benth., is used in folk medicine to relieve the symptoms of asthma, cough, and bronchitis. Recently, we showed that the ethanol extract obtained from Leptohyptis macrostachys has selective spasmolytic activity on guinea pig ileum. Therefore, the aim of this study was to characterize the spasmolytic mechanism of this extract, investigated whether it presents toxicological and antidiarrheal activities. Therefore, the crude ethanolic extract of Leptohyptis macrostachys was analyzed by high-performance liquid chromatographic-diode array detection (HPLC–DAD). The spasmolytic effect was evaluated on guinea pig ileum, toxicological activity using rats and antidiarrheal activity using male and female mice. In HPLC-DAD analysis, Rosmarinic acid (5.44%) was the most abundant phenolic compound, being considered as a chemical marker. The spasmolytic potency of the extract on histamine-induced contraction was reduced in the presence of 1 mM TEA+, a selective big–conductance K+ channels blocker (BKCa). The extract produces a dose–dependent antidiarrheal activity, inhibiting equipotently defecation frequency and liquid stool formation. In addition, the extract has inhibited in a dose–dependent manner both castor oil–induced intestinal transit and intestinal fluid content. Thus, the spasmolytic activity of the extract involves positive modulation of BKCa and its antidiarrheal activity is related to inhibition of intestinal motility and secretion.https://www.frontiersin.org/article/10.3389/fphar.2020.01042/fullLeptohyptis macrostachysLamiaceaespasmolytic activityantidiarrheal activitypotassium channel
spellingShingle Iara Leão Luna de Souza
Maria Allynne de Vasconcelos
Anne Dayse Soares da Silva
Polyana Cristina Barros Silva
Carlos Arthur Gouveia Veloso
Diego Igor Alves Fernandes de Araújo
Vicente Carlos de Oliveira Costa
Hilzeth Luna Freire Pessôa
Josean Fechine Tavares
Josean Fechine Tavares
Marcelo Sobral da Silva
Marcelo Sobral da Silva
Bagnólia Araújo da Silva
Bagnólia Araújo da Silva
Fabiana de Andrade Cavalcante
Fabiana de Andrade Cavalcante
Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle
Frontiers in Pharmacology
Leptohyptis macrostachys
Lamiaceae
spasmolytic activity
antidiarrheal activity
potassium channel
title Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle
title_full Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle
title_fullStr Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle
title_full_unstemmed Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle
title_short Toxicological and Pharmacological Activities of Leptohyptis macrostachys (Benth.) Harley and J.F.B.Pastore (Lamiaceae) on Intestinal Smooth Muscle
title_sort toxicological and pharmacological activities of leptohyptis macrostachys benth harley and j f b pastore lamiaceae on intestinal smooth muscle
topic Leptohyptis macrostachys
Lamiaceae
spasmolytic activity
antidiarrheal activity
potassium channel
url https://www.frontiersin.org/article/10.3389/fphar.2020.01042/full
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