Laboratory of Theoretical and Computational Biophysics, Ton Duc Thang University, Ho Chi Minh City-700000, Vietnam.
Department of Pharmacy, Faculty of Biological Sciences, Jahangirnagar University, Savar (Dhaka)-1342, Bangladesh.
Cell Mol Biol (Noisy-le-grand). 2020 Jun 25;66(4):243-249.
Phytol (PHY), a chlorophyll-derived diterpenoid, exhibits numerous pharmacological properties, including antioxidant, antimicrobial, and anticancer activities. This study evaluates the anti-diarrheal effect of phytol (PHY) along with its possible mechanism of action through in-vivo and in-silico models. The effect of PHY was investigated on castor oil-induced diarrhea in Swiss mice by using prazosin, propranolol, loperamide, and nifedipine as standards with or without PHY. PHY at 50 mg/kg (p.o.) and all other standards exhibit significant (p < 0.05) anti-diarrheal effect in mice. The effect was prominent in the loperamide and propranolol groups. PHY co-treated with prazosin and propranolol was found to increase in latent periods along with a significant reduction in diarrheal section during the observation period than other individual or combined groups. Furthermore, molecular docking studies also suggested that PHY showed better interactions with the α- and β-adrenergic receptors, especially with α-ADR1a and β-ADR1. In the former case, PHY showed interaction with hydroxyl group of Ser192 at a distance of 2.91Å, while in the latter it showed hydrogen bond interactions with Thr170 and Lys297 with a distance of 2.65 and 2.72Å, respectively. PHY exerted significant anti-diarrheal effect in Swiss mice, possibly through blocking α- and β-adrenergic receptors.
植物醇(PHY)是一种叶绿素衍生的二萜,具有多种药理作用,包括抗氧化、抗菌和抗癌活性。本研究通过体内和体外模型评估了植物醇(PHY)的抗腹泻作用及其可能的作用机制。用普萘洛尔、心得安、洛哌丁胺和硝苯地平作为标准,用或不用 PHY 研究 PHY 对蓖麻油诱导的瑞士小鼠腹泻的影响。PHY 在 50mg/kg(po)时,所有其他标准均对小鼠表现出显著的(p < 0.05)抗腹泻作用。洛哌丁胺和心得安组的效果更为显著。与普萘洛尔和心得安联合治疗的 PHY 被发现潜伏期延长,在观察期内腹泻段显著减少,比其他单独或联合组都要好。此外,分子对接研究还表明,PHY 与 α-和 β-肾上腺素能受体表现出更好的相互作用,特别是与 α-ADR1a 和 β-ADR1。在前一种情况下,PHY 与 Ser192 的羟基相互作用,距离为 2.91Å,而在后一种情况下,它与 Thr170 和 Lys297 表现出氢键相互作用,距离分别为 2.65 和 2.72Å。PHY 对瑞士小鼠表现出显著的抗腹泻作用,可能是通过阻断 α-和 β-肾上腺素能受体。