Newly discovered clouting interplay between matrix metalloproteinases structures and novel quaternary Ammonium K21: computational and in-vivo testing.

Aims And Objectives: To analyze anti-MMP mode of action of Quaternary Ammonium Silane (QAS, codenamed as k21) by binding onto specific MMP site using computational molecular simulation and Anti-Sortase A (SrtA) mode of action by binding onto specific site using computational molecular simulation.

Materials And Methods: In silico Molecular Dynamics (MD) was used to determine the interactions of K21 inside the pocket of the targeted protein (crystal structure of fibroblast collagenase-1 complexed to a diphenyl-ether sulphone based hydroxamic acid; PDB ID: 966C; Crystal structure of MMP-2 active site mutant in complex with APP-derived decapeptide inhibitor. MD simulations were accomplished with the Desmond package in Schrödinger Drug Discovery Suite.

Antimicrobial FiteBac® K21 promotes antimicrobial Potency and wound healing.

Objectives: Successful root canal therapy is dependent on the efficacy of complete instrumentation and adequate use of chemical irrigant to eliminate the biofilm from dentin surface. The aim of the study was to examine antibiofilm and antimicrobial effectiveness of newly formulated Quaternary ammonium silane (QAS/also codenamed K21; against and biofilm on radicular dentin with evaluation of the anti-inflammatory consequence .

Methods: Fourier Transform Infrared Spectroscopy (FTIR) was performed after complete hydrolysis of K21 solution.

Advancements in dextran-based nanocarriers for treatment and imaging of breast cancer.

Breast cancer is the most prevalent type of cancer worldwide,particularly among women, with substantial side effects after therapy. Despite the availability of numerous therapeutic approaches, particularly chemotherapy, the survival rates for breast cancer have declined over time. The therapies currently utilized for breast cancer treatment do not specifically target cancerous cells, resulting in significant adverse effects and potential harm to healthy cells alongside the cancer cells.

Cathepsin-K inhibition enhances anti-cancerous activity within oral squamous cell carcinoma cells: Uncloaking the potency of new K21 formulation.

Background: The ability of cancer cells to be invasive and metastasize depend on several factors, of which the action of protease activity takes center stage in disease progression.

Purpose/objective: To analyze function of new K21 molecule in the invasive process of oral squamous cell carcinoma (OSCC) cell line.

Materials & Methods: The Fusobacterium (ATCC 23726) streaks were made, and pellets were resuspended in Cal27 (ATCC CRL-2095) OSCC cell line spheroid cell microplate.

Swietenine Alleviates Nonalcoholic Fatty Liver Disease in Diabetic Mice via Lipogenesis Inhibition and Antioxidant Mechanisms.

Our previous studies have reported the effect of swietenine (a major bioactive component of Swietenia macrophylla seeds) in reversing and potentiating the effect of metformin in hyperglycemia and hyperlipidaemia in diabetic rats. Moreover, we reported that the anti-inflammatory effect of swietenine is mediated via the activation of nuclear factor erythroid 2-related factor 2 (Nrf2). This study evaluated the effect of swietenine and its mechanisms in nonalcoholic fatty liver disease (NAFLD) in high-fat diet/streptozotocin-induced diabetic mice.

In-vitro evaluation of the effectiveness of polyphenols based strawberry extracts for dental bleaching.

To formulate a dental bleaching agent with strawberry extract that has potent bleaching properties and antimicrobial efficacy. Enamel specimens (3 × 3 × 2 mm) were prepared. Quaternary Ammonium Silane (CaC2 enriched) was homogenized with fresh strawberries: Group 1: supernatant strawberry (10 g) extract < Group 2: supernatant strawberry (10 g) extract + 15%HA (Hydroxyapatite) < Group 3: supernatant strawberry (10 g) extract + 15% (HA-2%k21) < Group 4: supernatant strawberry (20 g) extract only (20 g strawberries) < Group 5: supernatant strawberry (20 g) extract + 15% HA < Group 6: supernatant strawberry (20 g) extract + 15% (HA-2%K21) < Group 7: In-office Opalescence Boost 35%.

Synthesis of New Shogaol Analogues as NRF2 Activators and Evaluation of Their Anti-Inflammatory Activity, Modes of Action and Metabolic Stability.

6-shogaol is a natural and the most potent bioactive vanilloid in dried rhizomes. Many scientific studies have reported the diverse biological activities of 6-shogaol. However, the major drawback of 6-shogaol is its instability at room temperature.

Quercetin and metformin synergistically reverse endothelial dysfunction in the isolated aorta of streptozotocin-nicotinamide- induced diabetic rats.

The antidiabetic effects of quercetin and metformin are well known. However, their synergistic effect in reversing the symptoms of diabetes-induced endothelial dysfunction remains unknown. In this study, we have investigated their synergistic effect in streptozotocin (STZ)-nicotinamide induced diabetic rats.

Anti-Inflammatory Effects of Auranamide and Patriscabratine-Mechanisms and In Silico Studies.

Auranamide and patriscabratine are amides from (L.) Smith. Their anti-inflammatory activity and nuclear factor erythroid 2-related factor 2 (NRF2) activation ability were evaluated using lipopolysaccharide (LPS)-stimulated murine macrophages (RAW264.

Effect of Sustained Systemic Administration of Ginger (Z officinale) Rhizome Extracts on Salivary Flow in Mice.

Objective: This study aimed to evaluate the effect of methanol (70% v/v), ethanol (80% v/v), dimethyl sulfoxide (DMSO; 100% v/v) extracts of ginger rhizome (GR), and 6-shogaol on the pilocarpine-stimulated salivary flow rate in C57BL/6 mice.

Methods: Three extracts of ginger (Zingiber officinale) rhizome prepared by maceration using the respective solvents and 6-shogoal were reconstituted in normal saline with 0.2% DMSO.

Light-responsive polyurethanes: classification of light-responsive moieties, light-responsive reactions, and their applications.

Stimuli responsiveness has been an attractive feature of smart material design, wherein the chemical and physical properties of the material can be varied in response to small environmental change. Polyurethane (PU), a widely used synthetic polymer can be upgraded into a light-responsive smart polymer by introducing a light-sensitive moiety into the polymer matrix. For instance, azobenzene, spiropyran, and coumarin result in reversible light-induced reactions, while -nitrobenzyl can result in irreversible light-induced reactions.

Microarray Analysis of the Genomic Effect of Eugenol on Methicillin-Resistant .

is a highly adaptive human pathogen responsible for serious hospital- and community-acquired infectious diseases, ranging from skin and soft tissue infections, to complicated and life-threatening conditions such as endocarditis and toxic shock syndrome (TSS). The rapid development of resistance of this organism to available antibiotics over the last few decades has necessitated a constant search for more efficacious antibacterial agents. Eugenol (4-allyl-2-methoxyphenol) belongs to the class of chemical compounds called phenylpropanoids.

PH Responsive Polyurethane for the Advancement of Biomedical and Drug Delivery.

Due to the specific physiological pH throughout the human body, pH-responsive polymers have been considered for aiding drug delivery systems. Depending on the surrounding pH conditions, the polymers can undergo swelling or contraction behaviors, and a degradation mechanism can release incorporated substances. Additionally, polyurethane, a highly versatile polymer, has been reported for its biocompatibility properties, in which it demonstrates good biological response and sustainability in biomedical applications.

Biochemical changes and macrophage polarization of a silane-based endodontic irrigant in an animal model.

Silane-based/fully hydrolyzed, endodontic irrigant exhibiting antimicrobial properties, is prepared, and is hypothesized to control macrophage polarization for tissue repair. Albino wistar rats were injected with 0.1 ml root canal irrigant, and bone marrow cells procured.

var. : Red Ginger's Medicinal Uses.

var. (red ginger) is widely used in traditional medicine in Asia. Unlike other gingers, it is not used as a spice in cuisines.

Synthesis and Incorporation of Quaternary Ammonium Silane Antimicrobial into Self-Crosslinked Type I Collagen Scaffold: A Hybrid Formulation for 3D Printing.

Novel 3D-biomaterial scaffold is constructed having a combination of a new quaternary ammonium silane (k21) antimicrobial impregnated in 3D collagen printed scaffolds cross linked with Riboflavin in presence of d-alpha-tocopheryl poly(ethyleneglycol)-1000-succinate. Groups of "0.1% and 0.

The role of DMPK science in improving pharmaceutical research and development efficiency.

The successful regulatory authority approval rate of drug candidates in the drug development pipeline is crucial for determining pharmaceutical research and development (R&D) efficiency. Regulatory authorities include the US Food and Drug Administration (FDA), European Medicines Agency (EMA), and Pharmaceutical and Food Safety Bureau Japan (PFSB), among others. Optimal drug metabolism and pharmacokinetics (DMPK) properties influence the progression of a drug candidate from the preclinical to the clinical phase.

Concentration-Dependent Multi-Potentiality of L-Arginine: Antimicrobial Effect, Hydroxyapatite Stability, and MMPs Inhibition.

This study's objective was to examine L-arginine (L-arg) supplementation's effect on mono-species biofilm (/) growth and underlying enamel substrates. The experimental groups were 1%, 2%, and 4% arg, and 0.9% NaCl was used as the vehicle control.

Success stories of AI in drug discovery - where do things stand?

Introduction: Artificial intelligence (AI) in drug discovery and development (DDD) has gained more traction in the past few years. Many scientific reviews have already been made available in this area. Thus, in this review, the authors have focused on the success stories of AI-driven drug candidates and the scientometric analysis of the literature in this field.

In vitro methods used for discovering plant derived products as wound healing agents - An update on the cell types and rationale.

Wounds still pose a huge burden on human health and healthcare systems in many parts of the world. Phytomedicines are being used to heal the wounds since ancient times. Now-a-days also many researchers are exploring the wound healing activity of phytomedicines.

Antibacterial and antibiofilm efficacy of k21-E in root canal disinfection.

Objectives: The aim of the current project was to study the antimicrobial efficacy of a newly developed irrigant, k21/E against E. faecalis biofilm.

Methods: Root canals were instrumented and randomly divided into the following groups: irrigation with saline, 6% NaOCl (sodium hypochlorite), 6% NaOCl+2% CHX (Chlorhexidine), 2% CHX, 0.

Swietenine potentiates the antihyperglycemic and antioxidant activity of Metformin in Streptozotocin induced diabetic rats.

Diabetes mellitus or type-2 diabetes, commonly referred as diabetes, is a metabolic disorder that results in high blood sugar level. Despite the availability of several antidiabetic drugs in the market, they still do not adequately regulate blood sugar levels. Thus, in general people prefer to use herbal supplements/medicines along with antidiabetic drugs to control blood sugar levels.

A Critical Review on Emerging Trends in Dry Powder Inhaler Formulation for the Treatment of Pulmonary Aspergillosis.

Pulmonary aspergillosis (PA), a pulmonary fungal infection caused by spp., is a concern for immunocompromised populations. Despite substantial research efforts, conventional treatments of PA using antifungal agents are associated with limitations such as excessive systemic exposure, serious side effects and limited availability of the therapeutics in the lungs for an adequate duration.