The present study aimed to produce a novel biocompatible, stable and biodegradable exopolysaccharide (EPS) from endophytic bacteria to deliver drugs into malignant cells effectively. EPS-producing endophytic bacteria, Pseudomonas otitidis was isolated and identified from the roots of the medicinal plant Tribulus terrestris L. The ice-cold ethanol precipitation method was used to isolate EPS from an endophytic bacterial culture. The isolated EPS was partially characterized by FTIR, NMR spectroscopy, and the presence of reducing sugar and protein contents were also measured. The isolated EPS contained 26.665±1.302% of reducing sugar and 0.912±0.023% of proteins. Further, EPS-based quercetin-loaded nanoparticles (NPs) were formulated through the precipitation method to deliver quercetin into breast cancer cells. The fabricated nanoparticles size, shape, physical nature, drug release and release kinetics properties were studied and confirmed. EPS-based nanoparticles could cause the highest release of quercetin in an acidic medium at pH 5.0, and they had high biocompatibility in a physiological medium. In addition, the NPs showed significant free radicals (DPPH* and ABTS*) scavenging and ferric ion reducing potentials and concentration-dependent cytotoxic effects against breast cancer cell lines (MCF-7 cells) after 24 h treatment with IC50 value of 14.313 μg ml−1. The obtained results demonstrated that the isolated EPS from endophytic bacteria can positively applied as a drug delivery vehicle and enhanced the activity of the loaded drug.
Tropical, vector-borne, and neglected diseases with a limited number of medication therapies include Leishmaniasis, Malaria, Chagas and Human African Trypanosomiasis (HAT). Chromones are a large class of heterocyclic compounds with significant applications. This heterocycle has long aroused the interest of scientists and the general public from biosynthetic and synthetic points of view owing to its interesting pharmacological activities. Chromones and their hybrids and isomeric forms proved to be an exciting scaffold to investigate these diseases. The in vitro activities of Chromone, Chromane, and a panel of other related benzopyran class compounds against Trypanosoma brucei rhodesiense, Trypanosoma brucei gambiense, Trypanosoma cruzi, and numerous Leishmanial and Malarial species were investigated in our previous studies. The current article briefly describes the neglected diseases and the current treatment. This review aims to attempt to find better alternatives by scrutinizing natural and synthetic derivatives for which chromones and their analogues were discovered to be a new and highly effective scaffold for the treatment of neglected diseases, including compounds with dual activity or activity against multiple parasites. Additionally, the efficacy of other new scaffolds was also thoroughly examined. This article also discusses prospects for identifying more unique targets for the disease, focusing on flavonoids as drug molecules that are less cytotoxic and high antiprotozoal potential. It also emphasizes the changes that can be made while searching for potential therapies—comparing existing treatments against protozoal diseases and the advantages of the newer chromone analogues over them. Finally, the structure-activity relationship at each atom of the chromone has also been highlighted.
The novel coronavirus disease 19 (COVID-19) has resulted in an estimated 20 million excess deaths and the recent resurgence of COVID-19 in China is predicted to result in up to 1 million deaths over the next few months. With vaccines unable to halt transmission it is important to continue our quest for safe, effective, affordable drugs that will be available to all countries. Drug repurposing is one of the strategies being explored in this context. Recently, out of 7,817 approved drugs, 214 candidates were systematically down-selected using a combination of 11 filters including approval status, assay data against SARS-CoV-2, pharmacokinetic, pharmacodynamic and toxicity profiles. These drugs were subjected in this study to virtual screening against various targets of SARS-CoV-2 followed by molecular dynamic studies of the best scoring ligands against each target. The chosen molecular targets were Spike receptor binding domain, Nucleocapsid protein RNA binding domain, and key non-structural proteins 3, 5, 12, 13 and 14. Four drugs approved for other indications — alendronate, cromolyn, natamycin and treprostinil — look sufficiently promising from our in silicostudies to warrant further in vitro and in vivo investigations as appropriate to ascertain their extent of anti-viral activities.
The present study aimed to produce a novel biocompatible, stable and biodegradable exopolysaccharide (EPS) from endophytic bacteria to deliver drugs into malignant cells effectively. EPS-producing endophytic bacteria, Pseudomonas otitidis was isolated and identi ed from the roots of the medicinal plant Tribulus terrestris L. The ice-cold ethanol precipitation method was used to isolate EPS from an endophytic bacterial culture. The isolated EPS was partially characterized by FTIR, NMR spectroscopy, and the presence of reducing sugar and protein contents were also measured. The isolated EPS contained 26.665±1.302% of reducing sugar and 0.912±0.023% of proteins. Further, EPS-based quercetinloaded nanoparticles (NPs) were formulated through the precipitation method to deliver quercetin into breast cancer cells. The fabricated nanoparticles size, shape, physical nature, drug release and release kinetics properties were studied and con rmed. EPS-based nanoparticles could cause the highest release of quercetin in an acidic medium at pH 5.0, and they had high biocompatibility in a physiological medium. In addition, the NPs showed signi cant free radicals (DPPH* and ABTS*) scavenging and ferric ion reducing potentials and concentration-dependent cytotoxic effects against breast cancer cell lines (MCF-7 cells) after 24 h treatment with IC50 value of 14.313 μg ml−1. The obtained results demonstrated that the isolated EPS from endophytic bacteria can positively applied as a drug delivery vehicle and enhanced the activity of the loaded drug.
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