Abstract
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.
Highlights
Lamiaceae, called as the mint family, has a worldwide distribution and includes around 295 genus and 7,780 species (Stevens, 2001)
Rosmarinic acid was quantified in the crude ethanolic extract of Leptohyptis macrostachys by high-performance liquid chromatographic-diode array detection
In the investigation of this study, we evaluate the role of K+ channels in the spasmolytic action mechanism, toxicological and antidiarrheal activities of LM–EtOHAP, an extract that contains rosmarinic acid as a chemical marker (Figure 1)
Summary
Called as the mint family, has a worldwide distribution and includes around 295 genus and 7,780 species (Stevens, 2001) It has species with high economic importance used as cosmetics, condiments, medicines, among others (Sousa and Couri, 2013). A highlighter genus of this family, is composed by 400 species with broad distribution in America, Oceania, and Africa (Raja, 2012). This genus has different species that have therapeutic potential such as antifungal (Rocha et al, 2019), antinociceptive, anti-inflammatory (Anjos et al, 2017; Figueiredo et al, 2019), antiedematogenic (Barbosa et al, 2017), antibacterial (Andrade et al, 2017), among others. We developed a pharmacological screening with the crude ethanolic extract obtained from the aerial parts of L. macrostachys (LMEtOHAP) in different smooth muscles (rat aorta, rat uterus, and guinea pig trachea and ileum) and this preliminary study showed a selective spasmolytic effect of the extract on guinea pig ileum (Souza et al, 2013)
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