β-Sitosterol Mediates Gastrointestinal Smooth Muscle Relaxation Induced by <i>Coccoloba uvifera</i> via Muscarinic Acetylcholine Receptor Subtype 3

• Main Authors: Francisco J. Aguirre-Crespo (Author), José L. Aragón-Gastélum (Author), Eduardo J. Gutiérrez-Alcántara (Author), Pedro Zamora-Crescencio (Author), Diana L. Gómez-Galicia (Author), Diego R. Alatriste-Kurzel (Author), Guzman Alvarez (Author), Emanuel Hernández-Núñez (Author)
• Format: Book
• Published: MDPI AG, 2024-04-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

<i>Coccoloba uvifera</i> is a Mayan medicinal plant, and these leaves are used as antidiarrheal and diuretic agents. In the present work, we develop in-vitro, ex-vivo, in-vivo, and in-silico strategies to evaluate several aqueous extracts of <i>C. uvifera</i> leaves. In vitro tests showed that decoction extract (CuDe) presented the best yield and chlorophyll, phenol, and flavonoid content; however, CuDe showed low antioxidant activity (DPPH model). All aqueous extracts exert spasmolytic and vasorelaxant activity in a concentration-dependent manner (ex vivo), and in vivo tests showed that CuDe exerts the best antiperistaltic and diuretic effects. The in-silico analysis suggests that <i>C. uvifera</i> triterpenes act as a ligand of GPCR, and β-sitosterol could act as an antagonist of muscarinic acetylcholine receptor subtype 3 (m3AChR). In the context of aqueous extracts of <i>C. uvifera</i>, β-sitosterol and their heterosides were identified by FTIR and ¹H-NMR spectroscopy. The concerted binding of β-sitosterol and other triterpenes within the m3AChR binding site may be relevant for the induction of relaxant effects at the gastrointestinal smooth muscle level. In this context, <i>C. uvifera</i> is a high-value plant species that requires analytical and pharmacological studies to confirm traditional medicinal use.

Item Description

10.3390/scipharm92020019
2218-0532
0036-8709