Discovery of the selective and nanomolar inhibitor of DPP-4 more potent than sitagliptin by structure-guided rational design.

Various therapeutic targets and approaches are commonly employed in the management of Type 2 Diabetes. These encompass diverse groups of drugs that target different mechanisms involved in glucose regulation. Inhibition of the DPP-4 enzyme has been proven an excellent target for antidiabetic drug design.

Draft genome sequence of 16 isolated from cashew nuts from coastal Kenya.

is a soil-borne fungus known for its aflatoxin contamination of agricultural products. Here, we report the draft genome sequences of 16 predicted aflatoxin-producing isolated from cashew nuts from coastal Kenya.

Expression patterns of candidate genes for the Lr46/Yr29 "slow rust" locus in common wheat (Triticum aestivum L.) and associated miRNAs inform of the gene conferring the Puccinia triticina resistance trait.

Leaf rust caused by Puccinia triticina (Pt) is one of the most impactful diseases causing substantial losses in common wheat (Triticum aestivum L.) crops. In adult plants resistant to Pt, a horizontal adult plant resistance (APR) is observed: APR protects the plant against multiple pathogen races and is distinguished by durable persistence under production conditions.

Mesenchymal stem cells derived from human adipose tissue exhibit significantly higher chondrogenic differentiation potential compared to those from rats.

Background: Osteoarthritis is a prevalent joint disease affecting both humans and animals. It is characterized by articular cartilage degeneration and joint surface eburnation. Currently, no effective pharmacological treatment is available to restore the original function and structure of defective cartilage.

Molecular detection of Coxiella burnetii in ticks infesting wild and domestic animals in the Eastern region of Punjab, Pakistan.

Tick-borne pathogens are significant for human, veterinary, and wildlife health. Coxiella burnetii is an example that is widely distributed across various hosts and can cross species boundaries. In Pakistan, there is a scarcity of data regarding C.

Bovine lactoferrin inhibits Plasmodium berghei growth by binding to heme.

Bovine lactoferrin (bLF) is a 77 kDa glycoprotein that is abundant in bovine breast milk and exerts various bioactive functions, including antibacterial and antiviral functions. Few studies have explored bLF activity against parasites. We found that bLF affects hemozoin synthesis by binding to heme, inhibiting heme iron polymerization necessary for Plasmodium berghei ANKA survival in infected erythrocytes, and also binds to hemozoin, causing it to disassemble.

Exploring Acyl Thiotriazinoindole Based Pharmacophores: Design, Synthesis, and SAR Studies with Molecular Docking and Biological Activity Profiling against Urease, α-amylase, α-glucosidase, Antimicrobial, and Antioxidant Targets.

A diminutive chemical library of acyl thiotriazinoindole (ATTI) based bioactive scaffolds was synthesized, instigated by taking the economical starting material Isatin, through a series of five steps. Isatin was first nitrated followed by the attachment of pentyl moiety via nucleophilic substitution reaction. The obtained compound was reacted with thiosemicarbazide to obtain thiosemicarbazone derivative, which was eventually cyclized using basic conditions in water as solvent.

Transcriptional expression of SLC16A7 as a biomarker of occult lymph node metastases in patients with head and neck squamous cell carcinoma.

Purpose: Glucose is the main energy substrate of tumor cells. This study aims to assess whether the transcriptional expression of glucose metabolism-related genes is associated with occult lymph node metastases in head and neck squamous cell carcinoma (HNSCC) patients.

Methods: We examined the transcriptional expression of a panel of glucose metabolism-related genes in a cohort of 53 patients with HNSCC without cervical lymph node involvement at the time of diagnosis (cN0) and subsequently treated with elective neck dissection.

A cocktail of histidine, carnosine, cysteine and serine reduces adiposity and improves metabolic health and adipose tissue immunometabolic function in ovariectomized rats.

Many women have sought alternative therapies to address menopause. Recently, a multi-ingredient supplement (MIS) containing L-histidine, L-carnosine, L-serine, and L-cysteine has been shown to be effective at ameliorating hepatic steatosis (HS) in ovariectomized (OVX) rats, a postmenopausal oestrogen deficiency model. Considering that HS frequently accompanies obesity, which often occurs during menopause, we aimed to investigate the effects of this MIS for 8 weeks in OVX rats.

The Influence of Chitosan Derivatives in Combination with Bacteria on the Development of Systemic Resistance in Potato Plants with Viral Infection and Drought.

Viral diseases of potatoes are among the main problems causing deterioration in the quality of tubers and loss of yield. The growth and development of potato plants largely depend on soil moisture. Prevention strategies require comprehensive protection against pathogens and abiotic stresses, including modeling the beneficial microbiome of agroecosystems combining microorganisms and immunostimulants.

Silybin-Functionalized PCL Electrospun Fibrous Membranes for Potential Pharmaceutical and Biomedical Applications.

Silybin is a natural flavonolignan with potential anticancer, antioxidant, and hepatoprotective properties. In the present study, various loadings of silybin (1, 3, and 5 wt%) were encapsulated in poly-ε-caprolactone (PCL) fibers by electrospinning, in order to produce new pharmaceutical composites with improved bioactive and drug delivery properties. The morphological characteristics of the composite fibrous structures were evaluated by scanning electron microscopy (SEM), and the encapsulation efficiency and the release rate of silybin were quantified using a UV-Vis spectrophotometer.

Enhancing Antibiotic Efficacy and Combating Biofilm Formation: Evaluating the Synergistic Potential of Essential Oil against Multidrug-Resistant Gram-Negative Bacteria.

Multidrug-resistant (MDR) Gram-negative bacteria remain a global public health issue due to the barrier imposed by their outer membrane and their propensity to form biofilms. It is becoming imperative to develop new antibacterial strategies. In this context, this study aims to evaluate the antibacterial efficacy of essential oil (OEO), alone and in combination with antibiotics, as well as its antibiofilm action against multidrug-resistant Gram-negative strains.

Green Synthesis of Silver Nanoparticle from Extract and Its Antimicrobial Action against ESKAPEE Group Bacteria.

Given the urgent need for novel methods to control the spread of multidrug-resistant microorganisms, this study presents a green synthesis approach to produce silver nanoparticles (AgNPs) using the bark extract from (Vell.) Brenan var. colubrina.

Chemical Composition Analysis and Assessment of Antioxidant and Anti-Inflammatory Activities of Crude Extract of on Carrageenan-Induced Paw Edema in Wistar Albino Rats.

A member of the Phyllanthaceae family, is a well-known plant in the tribal areas of Sri Lanka, India's Shaurastra region, Australia, and Malaysia. This study provides information about , a plant with a wide range of therapeutic uses in India. Different extracts from the leaves and roots of were evaluated for their physical and chemical properties, preliminary phytochemical parameters, and pharmacological activities in the current study, followed by their fourier transform infrared spectroscopy (FTIR), gas chromatography-mass spectrometry (GC-MS), antioxidant, and anti-inflammatory properties.

Engineering proteins with catechol chemistry for biotechnological applications.

Developing proteins with increased chemical space by expanding the amino acids alphabet has been an emerging technique to compete for the obstacle encountered by their need in various applications. 3,4-Dihydroxyphenylalanine (L-DOPA) catecholic unnatural amino acid is abundantly present in mussels foot proteins through post-translational modification of tyrosine to give a strong adhesion toward wet rocks. L-DOPA forms: bidentate coordination, H-bonding, metal-ligand complexes, long-ranged electrostatic, and van der Waals interactions a pair of donor hydroxyl groups.

Dietary plants for oral cancer prevention and therapy: A review of preclinical and clinical studies.

Oral cancer is a disease with high mortality and rising incidence worldwide. Although fragmentary literature on the anti-oral cancer effects of plant products has been published, a comprehensive analysis is lacking. In this work, a critical and comprehensive evaluation of oral cancer preventative or therapeutic effects of dietary plants was conducted.

Bioactive plant waste components targeting oral bacterial pathogens as a promising strategy for biofilm eradication.

The significance of this study lies in its exploration of bioactive plant extracts as a promising avenue for combating oral bacterial pathogens, offering a novel strategy for biofilm eradication that could potentially revolutionize oral health treatments. Oral bacterial infections are common in diabetic patients; however, due to the development of resistance, treatment options are limited. Considering the excellent antimicrobial properties of phenolic compounds, we investigated them against isolated oral pathogens using and models.

Development and evaluation of methotrexate-loaded nanoemulsion formulation for topical treatment of psoriasis.

Psoriasis is a chronic inflammatory disease that is becoming widespread and is associated with many kinds of additional severe diseases. The present study aimed to develop a methotrexate-loaded almond oil-based nanoemulsion formulation (MTX NE) for topical administration. The drug-loaded nanoemulsion formulation was prepared by high shear homogenization technique.

Ca-dependent lipid preferences shape synaptotagmin-1 C2A and C2B dynamics: Insights from experiments and simulations.

Signal transmission between neurons requires exocytosis of neurotransmitters from the lumen of synaptic vesicles into the synaptic cleft. Following an influx of Ca, this process is facilitated by the Ca sensor synaptotagmin-1. The underlying mechanisms involve electrostatic and hydrophobic interactions tuning the lipid preferences of the two C2 domains of synaptotagmin-1; however, the details are still controversially discussed.

Phosphofructokinase-1 in Cancer: A Promising Target for Diagnosis and Therapy.

Tumor cells have distorted enzymatic houses, which change the metabolic state from oxidative phosphorylation to glycolysis with high lactate levels in a hypoxic environment. Redrafting the metabolic profile is an emerging hallmark of cancer. Glycolytic enzyme amplification occurs in about 70% of all malignancies.