Deciphering the Pharmacological Properties of Methanol Extract of Psychotria calocarpa Leaves by In Vivo, In Vitro and In Silico Approaches.

Tahmina Akter Bristy,Md Arfin Ibn Aziz,Talha Bin Emran,A.S.M Ali Reza,Raffaele Capasso,Niloy Barua,Mifta Ahmed Jyoti,Elisabetta Caiazzo,Abu Montakim Tareq,Shahenur Alam Sakib,Kamrul Hasan Chowdhury,Saida Tasnim Etu,Barbara Romano,Syed Mohammed Tareq

doi:10.3390/ph13080183

Abstract

The present study explores the neuropharmacological, antinociceptive, antidiarrheal, antioxidant, thrombolytic and cytotoxic activity of methanol extract of Psychotria calocarpa leaves (MEPC). In anxiolytic activity testing of MEPC by elevated plus maze test, hole–board test and light–dark test, the extract exhibited a dose-dependent reduction of anxiety while the open field test observed a decreased locomotion. The administration of MEPC revealed a significant dose-dependent reduction of depressant behavior in forced swimming and tail suspension test. Additionally, the antinociceptive and antidiarrheal activity exposed a significant reduction of nociception and diarrheal behavior at the highest dose. In addition, a strong antioxidant activity was observed in DPPH-free radical-scavenging assay (IC50 = 461.05 μg/mL), total phenol content (118.31 ± 1.12 mg) and total flavonoid content (100.85 ± 0.97 mg). The significant clot–lysis activity was also observed with moderate toxicity (LC50 = 247.92 μg/mL) level in the lethality assay of brine shrimp. Moreover, in silico molecular docking study showed that the compound Psychotriasine could offer promising active site interactions for binding proteins. Furthermore, ADME/T and toxicological properties of the compound satisfied the Lipinski’s rule of five and Veber rules for drug-like potential and toxicity level. Overall, MEPC had a potential neuropharmacological, antinociceptive, antidiarrheal and antioxidant activity that warranted further investigation.

Highlights

Depressive disorders are common psychiatric disorders characterized by inflammatory conditions, oxidative stress, overproduction of nitric oxide and imbalance of antioxidant [1], whereas 121 million people affected by it [2]
In elevated plus maze (EPM), a significant activity in dose-dependent manner was observed for time spent in the open arm, whereas the methanol extract of Psychotria calocarpa leaves (MEPC) (400 mg/kg) exposed 44.89 ± 2.50% (p < 0.01) increased time spent in open arm compared with the control (30.33 ± 0.88%)
The Light and Dark Box Test (LDT) is likewise a favored model for assessing anxiolytic or anxiogenic drugs, where the animals revealed a strong tendency towards exploring the new condition

Summary

Introduction

Depressive disorders are common psychiatric disorders characterized by inflammatory conditions, oxidative stress, overproduction of nitric oxide and imbalance of antioxidant [1], whereas 121 million people affected by it [2]. Oxidative stress (OS) is only the imbalance of oxidants and antioxidants, whereas it framed as a typical result of aerobic metabolism [4]. The N-acetyl-cysteine (NAC) twice per day (1 g) is useful for bipolar disorder [18] and even in depression [13] Such investigations have likewise opened the potential roads of new treatment systems utilizing antioxidants as adjunctive treatment in the neuropsychiatric disorders and naturally derived food substances have been used as a great potential over the last two decades and numerous biologic activities demonstrating promising aspect on anti-inflammatory, anti-apoptotic and modulatory effects [19]

Objectives

Methods

Results

Conclusion