Experimental analysis of isolated compounds of Borreria hispida (L) in the context of antioxidant.

Borreria hispida comprises an effective potential source of natural antioxidant, which might be helpful in preventing the progress of various oxidative stresses. This study aimed to gain information by molecular docking of biologically active compounds of Borreria hispida with Glutathione reductase (GR), Urate oxidase(UO), Protein-tyrosine kinase 2-β (PTK-2β) and Peroxiredoxin-5(PRDX5) proteins target that are responsible for antioxidant activity and also correlate the relation by previous literature in vitro antioxidant analysis. Molecular docking analysis of the compounds was done by Schrodinger. Furthermore ADME properties of the isolated compounds were evaluated with QikProp. A mixed range of docking score was found during molecular docking by Schrodinger where the in vitro study showed moderate antioxidant activity. They also satisfy the Lipinski rule to sow the drug-like properties. Due to its superior docking score, it could be an effective GR, UO, PTK-2β and PRDX5 inhibitors. Furthermore studies are required to detect GR, UO, PTK-2β and PRDX5 inhibitory activity of isolated compounds from Borreria hispid

IN VIVO AND IN VITRO EVALUATION OF PHARMACOLOGICAL ACTIVITIES OF Hedychium coccineum RHIZOMES EXTRACT

The study reports the in vivo antidiarrheal and in vitro anthelmintic, cytotoxic, and thrombolytic activity of methanol extract of Hedychium coccineum rhizomes (MEHC). The antidiarrheal activity was determined using Castor oil-induced diarrhea and Gastrointestinal motility test in mice at the doses of 200 and 400 mg/kg body weight, whereas an aquarium worm, Tubifex tubifex, was used to determine the anthelmintic activity. The cytotoxic and thrombolytic activity of MEHC was performed by Brine shrimp lethality bioassay and clot lysis method respectively. In antidiarrheal, castor oil-induced diarrhea and gastrointestinal motility exhibited a significant reduction in diarrhea and defecation and an extremely significant inhibition in intestinal motility and peristalsis index by 200 and 400 mg/kg of MEHC. The MEHC (5, 10, and 20 mg/mL) showed a significant dose-dependent manner paralysis time and times to death in multiple comparisons to the different levamisole concentrations (0.5, 0.8, and 1 mg/mL) at in vitro anthelmintic activity. The brine shrimp lethality bioassay exhibited a weak LC50 (681.95 µg/mL; R² = 0.951) while in thrombolytic a significant percentage of clot lysis (32.70%, P < 0.05) demonstrated. The findings demonstrate that H. coccineum rhizomes could be potential sources for biological activity

Ethnomedicinal Value of Antidiabetic Plants in Bangladesh: A Comprehensive Review

The use of conventional drugs to treat metabolic disorders and the pathological consequences of diabetes further increases the complications because of the side effects, and is sometimes burdensome due to relatively higher costs and occasionally painful route of administration of these drugs. Therefore, shifting to herbal medicine may be more effective, economical, have fewer side effects and might have minimal toxicity. The present review amasses a list of ethnomedicinal plants of 143 species belonging to 61 families, from distinctive domestic survey literature, reported to have been used to treat diabetes by the ethnic and local people of Bangladesh. Leaves of the medicinal plants were found leading in terms of their use, followed by fruits, whole plants, roots, seeds, bark, stems, flowers, and rhizomes. This review provides starting information leading to the search for and use of indigenous botanical resources to discover bioactive compounds for novel hypoglycemic drug development

Anti-inflammatory, thrombolytic and hair-growth promoting activity of the n-hexane fraction of the methanol extract of Leea indica leaves

The anti-inflammatory, thrombolytic, and hair growth-promoting activity of the n-hexane fraction from the methanol extract of Leea indica (NFLI) leaves was investigated. NFLI showed significant inhibition of hemolysis and protein denaturation, and exhibited a concentration-dependent thrombolytic activity. When applied topically to mice at concentrations of 10, 1, 0.1%, NFLI demonstrated a significant increase in average hair length (p < 0.001) compared with untreated animals. NFLI (1% concentration) exhibited the highest percentage of hair regrowth on day 7, 14 and 21 (81.24, 65.60, and 62.5%, respectively). An in silico study was further conducted to predict the binding affinity of phytochemicals previously reported in L. indica towards PGD2 synthase (PDB ID: 2VD1), an enzyme that catalyses the isomerisation of prostaglandin H2 to PGD2 which is involved in hair loss. Phthalic acid, farnesol, n-tricosane, n-tetracosane, and n-heptacosane showed the best ligand efficiencies towards PGD2 synthase and their intermolecular interactions were visualised using BIOVIA Discovery Studio Visualizer. Our results indicate that L. indica could represent a promising natural alternative to tackle alopecia

In vivo anxiolytic and in vitro anti-inflammatory activities of water-soluble extract (WSE) of Nigella sativa (L.) seeds

The WSE is a highly polar, gummy and mucilaginous bioactive content of the Nigella sativa (L.) seeds. This study reports the anxiolytic and anti-inflammatory effects of WSE investigated using Elevated Plus Maze (EPM) and Hole-Board Test (HBT) in adult mice and human RBCs haemolysis inhibition and protein denaturation respectively. The oral WSE treatment (100 & 200 mg/kg b.w/day) for 72 hours has exhibited slightly better anxiolytic effect (p < 0.05) through the time span (92.33 & 93.33 s) spent in the opened arms of EPM vs. diazepam (1 mg/kg b.w i.p/day; 69.33 s). In HBT, only WSE (200 mg/kg b.w/day) has shown a promising number of mean head pokes (13.27 times/min) vs. diazepam (12.87 times/min). The WSE (62.5-500 mg/mL) exposure has exhibited 40.14-72.18% protection against lysis of RBCs vs. aspirin (57.04-71.48%) whilst 62.67-67.66% inhibition of protein denaturation vs. diclofenac sodium (43.11-80.64%). The current findings suggested WSE has promising anxiolytic and anti-inflammatory activities

Plant-based indole alkaloids: a comprehensive overview from a pharmacological perspective

Plant-based indole alkaloids are very rich in pharmacological activities, and the indole nucleus is considered to contribute greatly to these activities. This review’s fundamental objective is to summarize the pharmacological potential of indole alkaloids that have been derived from plants and provide a detailed evaluation of their established pharmacological activities, which may contribute to identifying new lead compounds. The study was performed by searching various scientific databases, including Springer, Elsevier, ACS Publications, Taylor and Francis, Thieme, Wiley Online Library, ProQuest, MDPI, and online scientific books. A total of 100 indole compounds were identified and reviewed. The most active compounds possessed a variety of pharmacological activities, including anticancer, antibacterial, antiviral, antimalarial, antifungal, anti-inflammatory, antidepressant, analgesic, hypotensive, anticholinesterase, antiplatelet, antidiarrheal, spasmolytic, antileishmanial, lipid-lowering, antimycobacterial, and antidiabetic activities. Although some compounds have potent activity, some only have mild-to-moderate activity. The pharmacokinetic profiles of some of the identified compounds, such as brucine, mitragynine, 7-hydroxymitragynine, vindoline, and harmane, were also reviewed. Most of these compounds showed promising pharmacological activity. An in-depth pharmacological evaluation of these compounds should be performed to determine whether any of these indoles may serve as new leads

The genus curcuma and inflammation: overview of the pharmacological perspectives

The Curcuma genus has been extensively used for therapeutic purposes in traditional or folk medicine worldwide, including for its anti-inflammatory activity. Curcuma spp.’s active constituents, such as alkaloids, flavonoids, and terpenoids, can act on various targets in the signaling pathway, restrain pro-inflammatory enzymes, lower the production of inflammatory cytokines and chemokines, and reduce oxidative stress, which subsequently suppresses inflammatory processes. Preclinical and clinical studies have reported the predominant anti-inflammatory activity of several Curcuma species. This review provides an overview of the anti-inflammatory effects of different extracts, preparations, and bioactive components in this genus. This analysis may provide a scientific basis for developing new and alternative methods for the isolation of a single entity from this genus to attenuate inflammatory conditions. The Curcuma genus is waiting for researchers interested in developing safe and efficient anti-inflammatory agents for further investigation

Drug repurposing approach against novel Coronavirus disease (COVID-19) through virtual screening targeting SARS-CoV-2 main protease

Novel coronavirus disease (COVID-19) was identified from China in December 2019 and spread rapidly through human-to-human transmission, affecting so many people worldwide. Until now, there has been no specific treatment against the disease and repurposing of the drug. Our investigation aimed to screen potential inhibitors against coronavirus for the repurposing of drugs. Our study analyzed sequence comparison among SARS-CoV, SARS-CoV-2, and MERS-CoV to determine the identity matrix using discovery studio. SARS-CoV-2 Mpro was targeted to generate an E-pharmacophore hypothesis to screen drugs from the DrugBank database having similar features. Promising drugs were used for docking-based virtual screening at several precisions. Best hits from virtual screening were subjected to MM/GBSA analysis to evaluate binding free energy, followed by the analysis of binding interactions. Furthermore, the molecular dynamics simulation approaches were carried out to assess the docked complex’s conformational stability. A total of 33 drug classes were found from virtual screening based on their docking scores. Among them, seven potential drugs with several anticancer, antibiotic, and immunometabolic categories were screened and showed promising MM/GBSA scores. During interaction analysis, these drugs exhibited different types of hydrogen and hydrophobic interactions with amino acid residue. Besides, 17 experimental drugs selected from virtual screening might be crucial for drug discovery against COVID-19. The RMSD, RMSF, SASA, Rg, and MM/PBSA descriptors from molecular dynamics simulation confirmed the complex’s firm nature. Seven promising drugs for repurposing against SARS-CoV-2 main protease (Mpro), namely sapanisertib, ornidazole, napabucasin, lenalidomide, daniquidone, indoximod, and salicylamide, could be vital for the treatment of COVID-19. However, extensive in vivo and in vitro studies are required to evaluate the mentioned drug’s activity

Current State and Promising Opportunities on Pharmaceutical Approaches in the Treatment of Polymicrobial Diseases

In recent years, the emergence of newly identified acute and chronic infectious disorders caused by diverse combinations of pathogens, termed polymicrobial diseases, has had catastrophic consequences for humans. Antimicrobial agents have been clinically proven to be effective in the pharmacological treatment of polymicrobial diseases. Unfortunately, an increasing trend in the emergence of multi-drug-resistant pathogens and limited options for delivery of antimicrobial drugs might seriously impact humans’ efforts to combat polymicrobial diseases in the coming decades. New antimicrobial agents with novel mechanism(s) of action and new pharmaceutical formulations or delivery systems to target infected sites are urgently required. In this review, we discuss the prospective use of novel antimicrobial compounds isolated from natural products to treat polymicrobial infections, mainly via mechanisms related to inhibition of biofilm formation. Drug-delivery systems developed to deliver antimicrobial compounds to both intracellular and extracellular pathogens are discussed. We further discuss the effectiveness of several biofilm-targeted delivery strategies to eliminate polymicrobial biofilms. At the end, we review the applications and promising opportunities for various drug-delivery systems, when compared to conventional antimicrobial therapy, as a pharmacological means to treat polymicrobial diseases