Nanoparticles: Taking a Unique Position in Medicine.

The human nature of curiosity, wonder, and ingenuity date back to the age of humankind. In parallel with our history of civilization, interest in scientific approaches to unravel mechanisms underlying natural phenomena has been developing. Recent years have witnessed unprecedented growth in research in the area of pharmaceuticals and medicine. The optimism that nanotechnology (NT) applied to medicine and drugs is taking serious steps to bring about significant advances in diagnosing, treating, and preventing disease-a shift from fantasy to reality. The growing interest in the future medical applications of NT leads to the emergence of a new field for nanomaterials (NMs) and biomedicine. In recent years, NMs have emerged as essential game players in modern medicine, with clinical applications ranging from contrast agents in imaging to carriers for drug and gene delivery into tumors. Indeed, there are instances where nanoparticles (NPs) enable analyses and therapies that cannot be performed otherwise. However, NPs also bring unique environmental and societal challenges, particularly concerning toxicity. Thus, clinical applications of NPs should be revisited, and a deep understanding of the effects of NPs from the pathophysiologic basis of a disease may bring more sophisticated diagnostic opportunities and yield more effective therapies and preventive features. Correspondingly, this review highlights the significant contributions of NPs to modern medicine and drug delivery systems. This study also attempted to glimpse the future impact of NT in medicine and pharmaceuticals.

Identification of sustainable trypsin active-site inhibitors from Nigrospora sphaerica strain AVA-1.

Trypsin is a protein-digesting enzyme that is essential for the growth and regeneration of bone, muscle, cartilage, skin, and blood. The trypsin inhibitors have various role in diseases such as inflammation, Alzheimer's disease, pancreatitis, rheumatoid arthritis, cancer prognosis, metastasis and so forth. From 10 endophytic fungi isolated, we were able to screen only one strain with the required activity. The fungus with activity was obtained as an endophyte from Dendrophthoe falcata and was later identified as Nigrospora sphaerica. The activity was checked by enzyme assays using trypsin. The fungus was fermented and the metabolites were extracted and further purified by bioassay-guided chromatographic methods and the compound isolated was identified using gas chromatography-mass spectrometry. The compound was identified as quercetin. Docking studies were employed to study the interaction. The absorption, distribution, metabolism, and excretion analysis showed satisfactory results and the compound has no AMES and hepatotoxicity. This study reveals the ability of N. sphaerica to produce bioactive compound quercetin has been identified as a potential candidate for trypsin inhibition. The present communication describes the first report claiming that N. sphaerica strain AVA-1 can produce quercetin and it can be considered as a sustainable source of trypsin active-site inhibitors.

An updated patent review of therapeutic applications of chalcone derivatives (2014-present).

INTRODUCTION: Chalcone or benzylideneacetophenone or 1,3-diphenyl-2-propene-1-one is a natural product comprising of two aromatic rings connected together by a three-carbon α, ß unsaturated carbonyl bridge. It is one of the most privileged scaffolds in medicinal chemistry that can be synthesized in the laboratory and can be converted into several therapeutically active heterocyclic scaffolds. It exhibits multifarious pharmacological activities and also plays a key role in several non-pharmacological scientific applications. AREAS COVERED: The present article comprehensively focuses on the approved patents during the time duration 2014-2018 on various chalcone molecules with diverse pharmacological activities. EXPERT OPINION: The study puts forward the latest updated therapeutic applications of chalcone-based compounds as antiproliferative, antidiabetic, anti-infective, anti-inflammatory, antioxidant, antiaging, neuroprotective, and cardioprotective agents. The type, position, and the number of substituents present on the chalcone scaffold have been perceived to play an imperative function in interacting with molecular targets (receptor, enzyme, and/or channel) to express the biological responses. In the majority of the studies, the overall activity of the ligand administered as pharmaceutically acceptable salt is found to be better than that of standard marketed drug preparation. The article will certainly attract (medicinal)-chemists actively involved in the development of therapeutically active scaffolds.