Polarity Directed Appraisal of Pharmacological Potential and HPLC-DAD Based Phytochemical Profiling of Polygonum glabrum Willd

The present study was designed to evaluate polarity-dependent extraction efficiency and pharmacological profiling of Polygonum glabrum Willd. Crude extracts of leaves, roots, stems, and seeds, prepared from solvents of varying polarities, were subjected to phytochemical, antioxidant, antibacterial, antifungal, antidiabetic, and cytotoxicity assays. Maximum extraction yield (20.0% w/w) was observed in the case of an acetone:methanol (AC:M) root extract. Distilled water:methanol (W:M) leaves extract showed maximum phenolic contents. Maximum flavonoid content and free radical scavenging potential were found in methanolic (M) seed extract. HPLC-DAD quantification displayed the manifestation of substantial quantities of quercetin, rutin, gallic acid, quercetin, catechin, and kaempferol in various extracts. The highest ascorbic acid equivalent total antioxidant capacity and reducing power potential was found in distilled water roots and W:M leaf extracts, respectively. Chloroform (C) seeds extract produced a maximum zone of inhibition against Salmonella typhimurium. Promising protein kinase inhibition and antifungal activity against Mucor sp. were demonstrated by C leaf extract. AC:M leaves extract exhibited significant cytotoxic capability against brine shrimp larvae and α-amylase inhibition. Present results suggest that the nature of pharmacological responses depends upon the polarity of extraction solvents and parts of the plant used. P. glabrum can be considered as a potential candidate for the isolation of bioactive compounds with profound therapeutic importance.

In vitro assessment of deworming potential of Guiera senegalensis in Nigerian ethnoveterinary industry using Caenorhabditis elegans

Background Although Guiera senegalensis is used as a dewormer in ethnoveterinary health care in Nigeria, its anthelmintic potential has not been validated. Hence, this work investigated the in vitro anthelmintic potential of G. senegalensis extracts on two Caenorhabditis elegans strains: Bristol N2 (wild type/ivermectin susceptible) and DA1316 (ivermectin resistant). Results Aqueous and methanol extracts of G. senegalensis were tested against the motility of the L4 larvae at two exposure periods of 24 and 48 h and found to be active against the C. elegans strains. Motility of C. elegans DA1316 was reduced to 18.6% and 8.3% by aqueous and methanol extracts, respectively, at 2.0 mg/ml after 48 h, whereas that of C. elegans DA1316 treated with ivermectin (0.02 µg/ml) remained above 95%. The motility of C. elegans Bristol N2 was reduced to 16.6% and 7.2% by aqueous and methanol extracts, respectively, at 2.0 mg/ml after 48 h and ≤ 2.7% by ivermectin (0.02 µg/ml). Activity of the plant extracts was concentration and time dependent. Conclusions This work confirms the anthelmintic activity of G. senegalensis and its effectiveness against ivermectin-resistant nematodes, thus validating its ethnoveterinary use as an animal dewormer in Nigeria and pharmacological potential as a source of anthelmintic compounds against ivermectin-resistant nematodes. There is, however, the need for in vivo studies to confirm the in vitro efficacy of the extracts.

Fine-tuning of the pharmacological potential of novel thiazolium ionic liquids by anion alteration

A novel series of thiazolium ionic liquids (TILs) bound to chloride (2a–c), tetrafluoroborate (BF4) (3a–c), and bis-(trifluoromethanesulfonimide) (Tf2N) anions (4a–c) was synthesized and their physicochemical characteristics were investigated.

Turmeric and Ginger as Health Protective Food Sources - An Integrative Review

Most of the medicinal plants utilized in traditional medicine are spices. Majority of those spices are widely used for aroma, flavour and colour in cuisine though they behave as appetizers, digestives, preventives and aphrodisiacs. Their antimicrobial properties are in a broad spectrum that provides a considerable immunity development within the human body. This review summarizes the beneficial characteristics of major active constituents in turmeric and ginger and their presumed pharmacological potential to safeguard human health.Keywords: Turmeric, Ginger, Curcumin, Human health, Active Ingredients, Nanotechnology

Potential of germanium-based compounds in coronavirus infection

The first germanium compounds which exhibited immunomodulatory and antiviral effects were sesquioxane-type germanates. To date, more than a dozen compounds containing germanium have been synthesized and are being actively studied. They include germanium carboxylates and citrates, complexes of germanium with resveratrol, daphnetin, mangiferin, chrysin, quercetin, ascorbic and nicotinic acids, amino acids, gamma-lactones, germanium-containing spirulina, yeast and others. Germanium-based compounds have shown the ability to influence the replication of various DNA/RNA viruses, stimulate the body’s natural resistance, prevent the development of metabolic intoxication of various origin, increase the efficacy of vaccines, and prevent the development of excessive accumulation of reactive oxygen species, which plays a decisive role in the development of inflammatory response caused by a viral infection. It seems reasonable to say that germanium-based complex compounds effectively contribute to the preservation of high--energy bonds in the form of ATP, optimize the activity of metabolic processes by re-oxygenation, and exhibit antimicrobial activity. The purpose of this review is to summarize the pharmacological potential of various germanium-based compounds studied nowadays, taking into account their mechanisms of action, and to analyze their prospects in the development of integrated approaches in the prevention and treatment of SARS-CoV-2 infection.

Bupleurum turcicum: A Rich Source of Saikosaponin A and D with Potential Use as Adjunct for the Management of Acute Respiratory Diseases: A Meta Review

COVID-19 pandemic caused by SARS-CoV-2 has resulted in unprecedented havoc worldwide with significant morbidity and mortality. Till now, no effective antivirals are at disposal prompting researchers to explore potential lead molecules including from bioactive phytochemicals. An extensive literature search was carried out utilizing online resources; Google Scholar and PubMed to collect published reports on pharmacological potential of saikosaponin particularly in underexplored Bupleurum species. A number of molecular docking studies have reported promising antiviral effects of saikosaponins particularly of saikosaponin A, D, U and V with tremendous potential to be developed as anti-SARS-CoV-2 therapy. The search for potential sources of saikosaponin A and D led to the identification of Bupleurum turcicum; an unexplored, underutilized and endemic Bupleurum species. The observation that B. turcicum root extract contains highest amount of SSa and SSd among endemic Bupleurum species found in Turkey (Bupleurum sulphureum, Bupleurum lycaonicum, Bupleurum turcicum, Bupleurum heldreichii, Bupleurum pauciradiatum) and presence of significant amounts of antioxidant compounds led to the proposition of using B. turcicum extracts as adjust therapy in the management of COVID-19. The proposal also relies on the evidence of SSa and SSd being effective against a number of viruses including SARS-CoV. This review discusses phytochemical composition of B. turcicum root, antiviral, immunomodulatory and anti-inflammatory potential of saikosaponins in view of its plausible usefulness in the management of COVID-19. B. turcicum is an underutilized species rich in saikosaponin A and D with potential antiviral properties which could be effective alternative therapy in COVID-19 management.

Green by Design: Convergent Synthesis, Computational Analyses, and Activity Evaluation of New FXa Inhibitors Bearing Peptide Triazole Linking Units

Green chemistry implementation has led to promising results in waste reduction in the pharmaceutical industry. However, the early sustainable development of pharmaceutically active compounds and ingredients remains a considerable challenge. Herein, we wish to report a green synthesis of new pharmaceutically active peptide triazoles as potent factor Xa inhibitors, an important drug target associated with the treatment of diverse cardiovascular diseases. The new inhibitors were synthesized in three steps, featuring cycloaddition reactions (high atom economy), microwave-assisted organic synthesis (energy efficiency), and copper nanoparticle catalysis, thus featuring Earth-abundant metals. The molecules obtained showed FXa inhibition, with IC50-values as low as 17.2 μM and no associated cytotoxicity in HEK293 and HeLa cells. These results showcase the environmental potential and chemical implications of the applied methodologies for the development of new molecules with pharmacological potential.

The Diversity, Metabolomics Profiling, and the Pharmacological Potential of Actinomycetes Isolated from the Estremadura Spur Pockmarks (Portugal)

The Estremadura Spur pockmarks are a unique and unexplored ecosystem located in the North Atlantic, off the coast of Portugal. A total of 85 marine-derived actinomycetes were isolated and cultured from sediments collected from this ecosystem at a depth of 200 to 350 m. Nine genera, Streptomyces, Micromonospora, Saccharopolyspora, Actinomadura, Actinopolymorpha, Nocardiopsis, Saccharomonospora, Stackebrandtia, and Verrucosispora were identified by 16S rRNA gene sequencing analyses, from which the first two were the most predominant. Non-targeted LC-MS/MS, in combination with molecular networking, revealed high metabolite diversity, including several known metabolites, such as surugamide, antimycin, etamycin, physostigmine, desferrioxamine, ikarugamycin, piericidine, and rakicidin derivatives, as well as numerous unidentified metabolites. Taxonomy was the strongest parameter influencing the metabolite production, highlighting the different biosynthetic potentials of phylogenetically related actinomycetes; the majority of the chemical classes can be used as chemotaxonomic markers, as the metabolite distribution was mostly genera-specific. The EtOAc extracts of the actinomycete isolates demonstrated antimicrobial and antioxidant activity. Altogether, this study demonstrates that the Estremadura Spur is a source of actinomycetes with potential applications for biotechnology. It highlights the importance of investigating actinomycetes from unique ecosystems, such as pockmarks, as the metabolite production reflects their adaptation to this habitat.