Recapitulating Antioxidant and Antibacterial Compounds into a Package for Tissue Regeneration: Dual Function Materials with Synergistic Effect.

Oxidative damage and infection can prevent or delay tissue repair. Moreover, infection reinforces reactive oxygen species (ROS) formation, which makes the wound's condition even worse. Therefore, the need for antioxidant and antibacterial agents is felt for tissue regeneration. There are emerging up-and-coming biomaterials that recapitulate both properties into a package, offering an effective solution to turn the wound back into a healing state. In this article, the principles of antioxidant and antibacterial activity are summarized. The review starts with biological aspects, getting the readers to familiarize themselves with tissue barriers against infection. This is followed by the chemistry and mechanism of action of antioxidant and antibacterial materials (dual function). Eventually, the outlook and challenges are underlined to provide where the dual-function biomaterials are and where they are going in the future. It is expected that the present article inspires the designing of dual-function biomaterials to more advanced levels by providing the fundamentals and comparative points of view and paving the clinical way for these materials.

Benzimidazole analogues as efficient arsenals in war against methicillin-resistance staphylococcus aureus (MRSA) and its SAR studies.

Small molecule based inhibitors development is a growing field in medicinal chemistry. In recent years, different heterocyclic derivatives have been designed to counter the infections caused by multi-drug resistant bacteria. Indeed, small molecule inhibitors can be employed as an efficient antibacterial agents with different mechanism of action. Methicillin-resistant Staphylococcus aureus (MRSA) is becoming lethal to mankind due to easy transmission mode, rapid resistance development to existing antibiotics and affect difficult-to-treat skin and filmsy diseases. Benzimidazoles are a class of heterocyclic compounds which have capability to fight against MRSA. High biocompatibility of benzimidazoles, synergistic behaviour with antibiotics and their tunable physico-chemical properties attracted the researchers to develop new benzimidazole based antibacterial agents. The present review focus on recent developments of benzimidazole-hybrid molecules as anti MRSA agents and the results of in-vitro and in-vivo studies with possible mechanism of action and discussing structure-activity relationship (SAR) in different directions. Benzimdazoles act as DNA binding agents, enzyme inhibitors, anti-biofilm agents and showed synergistic effect with available antibiotics to achieve antibacterial activity against MRSA. This cumulative figures would help to design new benzimidazole-based MRSA growth inhibitors.

Dual Role of MoS2 Quantum Dots in a Cross-Dehydrogenative Coupling Reaction.

Modern day research focuses on the development of greener and eco-friendlier protocols to fabricate biologically relevant targets with minimal waste generation. C-C bond formation reactions are of prime importance in this regard. In a typical photocatalytic hydrogen evolution reaction, three components are used, viz, catalyst, photosensitizer, and sacrificial amine donor. Among these, the photosensitizer and sacrificial amine donors are wasted at the end of the reaction. Considering these drawbacks, in this work, we have developed a methodology targeted at the utilization of sacrificial amine donors for C-H functionalization with MoS2 quantum dots (QDs) as the catalyst as well as the photosensitizer. QDs indeed emerged to be an active participant in the heterogeneous electron transfer process. This concept opens up new possibilities in the field of nanomaterial-based photomediated organic transformations without the aid of any external photosensitizers via a clean and sustainable protocol with no side product.

Pyrazole-based analogs as potential antibacterial agents against methicillin-resistance staphylococcus aureus (MRSA) and its SAR elucidation.

Methicillin-resistant Staphylococcus aureus (MRSA) is becoming lethal to humanity due to easy transmission and difficult-to-treat skin and flimsy diseases. The most threatening aspect is the rapid resistance development of MRSA to any approved antibiotics, including vancomycin. The development of new, efficient, and nontoxic drug candidate to fight against MRSA isolates is the need of the hour. The intriguing molecular structure and versatile bioactive pyrazole core attracting to development required novel antibiotics. This review presents the decade developments of pyrazole-containing derivatives with a broad antibacterial movement against diverged bacterial strains. In specific, we correlated the efficacy of structurally diversified pyrazole analogs against MRSA and discussed different angles of structure-activity relationship (SAR). The current survey highlights pyrazole hybrids' present scenario on MRSA studies, covering articles published from 2011 to 2020. This collective information may become an excellent platform to plan and develop new pyrazole-based small MRSA growth inhibitors with minimal side effects.

Employing siRNA tool and its delivery platforms in suppressing cisplatin resistance: Approaching to a new era of cancer chemotherapy.

Although chemotherapy is a first option in treatment of cancer patients, drug resistance has led to its failure, requiring strategies to overcome it. Cancer cells are capable of switching among molecular pathways to ensure their proliferation and metastasis, leading to their resistance to chemotherapy. The molecular pathways and mechanisms that are responsible for cancer progression and growth, can be negatively affected for providing chemosensitivity. Small interfering RNA (siRNA) is a powerful tool extensively applied in cancer therapy in both pre-clinical (in vitro and in vivo) and clinical studies because of its potential in suppressing tumor-promoting factors. As such oncogene pathways account for cisplatin (CP) resistance, their targeting by siRNA plays an important role in reversing chemoresistance. In the present review, application of siRNA for suppressing CP resistance is discussed. The first priority of using siRNA is sensitizing cancer cells to CP-mediated apoptosis via down-regulating survivin, ATG7, Bcl-2, Bcl-xl, and XIAP. The cancer stem cell properties and related molecular pathways including ID1, Oct-4 and nanog are inhibited by siRNA in CP sensitivity. Cell cycle arrest and enhanced accumulation of CP in cancer cells can be obtained using siRNA. In overcoming siRNA challenges such as off-targeting feature and degradation, carriers including nanoparticles and biological carriers have been applied. These carriers are important in enhancing cellular accumulation of siRNA, elevating gene silencing efficacy and reversing CP resistance.

Crystallography, in Silico Studies, and In Vitro Antifungal Studies of 2,4,5 Trisubstituted 1,2,3-Triazole Analogues.

A series of 2,4,5 trisubstituted-1,2,3-triazole analogues have been screened for their antifungal activity against five fungal strains, Candida parapsilosis, Candida albicans, Candida tropicalis, Aspergillus niger, and Trichophyton rubrum, via a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) microdilution assay. Compounds GKV10, GKV11, and GKV15 emerged as promising antifungal agents against all the fungal strains used in the current study. One of the highly active antifungal compounds, GKV10, was selected for a single-crystal X-ray diffraction analysis to unequivocally establish its molecular structure, conformation, and to understand the presence of different intermolecular interactions in its crystal lattice. A cooperative synergy of the C-H···O, C-H···N, C-H···S, C-H···π, and π···π intermolecular interactions was present in the crystal structure, which contributed towards the overall stabilization of the lattice. A molecular docking study was conducted for all the test compounds against Candida albicans lanosterol-14α-demethylase (pdb = 5 tzl). The binding stability of the highly promising antifungal test compound, GKV15, from the series was then evaluated by molecular dynamics studies.