Phytochemical characterization and phospholipase A inhibitory effect of Vitex negundo L. root extracts.

Ethnopharmacological Relevance: Snake bites are a critical health issue in many parts of the world particularly in Asian countries lacking efficient health facilities in rural areas. Cobra is the most common snake type in Asia and is responsible for a large number of mortalities particularly in rural areas. Plants are usually considered the most effective and easy-to-approach treatment for snake bites in rural areas of various countries.

A novel synthetic derivative of biaryl guanidine as a potential BACE1 inhibitor, to treat Alzheimer's disease: In-silico, in-vitro and in-vivo evaluation.

BACE1 enzyme has been known a potential target involved in Alzheimer's disease (AD). Present research was focused on the principles of virtually screening, chemical synthesis and protease inhibitory effect of BACE1 enzyme via biaryl guanidine derivatives. In-silico based paradigm (ligand binding interaction within active domain of BACE 1 enzyme i.

PEGylated Protamine Letrozole Nanoparticles: A Promising Strategy to Combat Human Breast Cancer via MCF-7 Cell Lines.

The objective of the study was to develop PEGylated protamine letrozole nanoparticles to combat human breast cancer by modifying the release pattern of letrozole. Breast cancer is amongst the most prevalent diseases in women due to overactivity of human epidermal growth factor receptor 2 (HER2). PEG-protamine letrozole nanoparticle formulation was designed and optimized to alter the release pattern of the drug.

Molecular Docking, Synthesis, and Tyrosinase Inhibition Activity of Acetophenone Amide: Potential Inhibitor of Melanogenesis.

Tyrosinase and its related proteins are responsible for pigmentation disorders, and inhibiting tyrosinase is an established strategy to treat hyperpigmentation. The carbonyl scaffolds can be effective inhibitors of tyrosinase activity, and the fact that both benzoic and cinnamic acids are safe natural substances with such a scaffolded structure, it was speculated that hydroxyl-substituted benzoic and cinnamic acid derivatives may exhibit potent tyrosinase inhibitory activity. These moieties were incorporated into new chemotypes that displayed in vitro inhibitory effect against mushroom tyrosinase with a view to explore antimelanogenic ingredients.

Formulation, Optimization, and Evaluation of Saxagliptin-Loaded Lipospheres for an Improved Pharmacokinetic Behavior.

The development and optimization of controlled release lipospheres (LS) from safe biocompatible behenic acid (BA) was performed for not only enhancing patient's compliance against highly prevailed chronic diabetes but also to vanquish the insufficiencies of traditional methods of drug delivery. The Box-Bhenken design (BBD) was utilized to statistically investigate the impact of formulation variables on percentage yield ( ), entrapment efficiency ( ), and SG-release ( ) from saxagliptin- (SG-) loaded LS, and the chosen optimized LS were subjected to a comparative pharmacokinetic analysis against commercially available SG brand. The compatibility analysis performed by DSC and FTIR established a complete lack of interaction of formulation components with SG, while p-XRD suggested a mild transformation of crystalline drug to its amorphous form during encapsulation process.

Diagnostic Performance and Appropriate Cut-Offs of Different Anthropometric Indicators for Detecting Children with Overweight and Obesity.

In the clinical settings, different anthropometric indicators like neck circumference (NC), waist circumference (WC), midupper arm circumference (MUAC), waist-to-height ratio (WHtR), and arm-to-height ratio (AHtR) have been suggested for evaluating overweight and obesity in children. The comparative ability of these indicators in Pakistan is yet unknown. This study is aimed at examining the validity of different anthropometric indicators of overweight and obesity simultaneously and at determining their superlative cut-off values that would correctly detect overweight and obesity in children.

Investigation of Husk as Pharmaceutical Excipient for Solid Dosage Form (Orodispersible Tablets).

The objective of the study was to investigate the suitability of the (PO) husk as a pharmaceutical excipient. Various phytoconstituents of the husk were determined according to the standard test procedures. The husk was evaluated for various pharmaceutical parameters related to flow, swelling index, and compressibility index.

Vicissitudes in polyphenolic extract-based high internal phase creams (HIPCs)- effect of storage temperature dependent characteristics.

The purpose of this investigation was to evaluate the vicissitudes in polyphenolic extract- based high internal phase creams (HIPCs) and effect of storage temperature dependent characteristics. Rheological parameters, that is, power law and IPC analysis with its physical characteristics were exploredat different storage temperatures (8°, 25°, 40° and 40° with 75% relative humidity- RH) with different time intervals up to 2 months of newly formulated poly-phenolic extract- based high internal phase cream and its comparison with base. Polyphenolic- based HIPCs showed non-Newtonian-pseudo plastic tendencies in vicissitudes with time and storage temperatures.

Fabrication of Carbamazepine Cocrystals: Characterization, and Comparative Evaluation.

Carbamazepine (CBZ) is an antiepileptic drug having low bioavailability due to its hydrophobic nature. In the current study, efforts are made to investigate the effect of dicarboxylic acid coformer spacer groups (aliphatic chain length) on physicochemical properties, relative humidity (RH) stability, and oral bioavailability of CBZ cocrystals. Slurry crystallization technique was employed for the preparation of CBZ cocrystals with the following coformers: adipic (AA), glutaric (GA), succinic (SA), and malonic acid (MA).

Antihyaluronidase and Alkaline Phosphatase (ALP) Activities of Medicinal Plants to Combat Venom-Induced Toxicities.

Snakebite is one of the most neglected diseases of developing countries. Deaths due to snakebite envenoming are quite high in Pakistan, and many deaths are caused by envenomation. Traditional use of medicinal plants against snakebites is a common practice in Pakistan due to countless benefits.

Anti-5'-Nucleotidases (5'-ND) and Acetylcholinesterase (AChE) Activities of Medicinal Plants to Combat Venom-Induced Toxicities.

is one of the highly venomous snakes of Pakistan that is responsible for numerous cases of envenomation and deaths. In Pakistan, medicinal plants are commonly used traditionally for snakebite treatment because of their low cost and easy availability in comparison with antivenom. The current research is aimed at evaluating the inhibitory activity of Pakistani medicinal plants against acetylcholinesterase and 5'-nucleotidases present in venom.

Effect of varying quantities of polymer on preparation and stability evaluation of carbamazepine cocrystals with dicarboxylic acid coformers.

The current study is an attempt to explore the effect of varying quantities of hydroxypropyl cellulose (HPC) polymer on carbamazepine (CBZ) cocrystal formation with dicarboxylic acid coformers i.e., malonic acid (MA), succinic acid (SA), glutaric acid (GA), and adipic acid (AA).

Enzyme Inhibitory Kinetics and Molecular Docking Studies of Halo-Substituted Mixed Ester/Amide-Based Derivatives as Jack Bean Urease Inhibitors.

A series of halo-substituted mixed ester/amide-based analogues have been prepared as jack bean urease inhibitor, which showed good to excellent inhibition of enzyme activity. The role of halo-substituted benzoyl moieties and alkyl substituted anilines in urease inhibitory kinetics was also investigated. The alkyl-substituted anilines reacted with chloroacetyl chloride to afford intermediates , which were then reacted with different halo-substituted benzoic acids to prepare the title compounds .

Preparation and Nanoencapsulation of Lectin from on Chitosan-Tripolyphosphate Nanoparticle and Their Cytotoxicity against Hepatocellular Carcinoma Cells (HepG2).

Lectins are the oligomeric sugar-specific glycoprotein of nonimmune origin, are involved in the multiple biological recognition process, and have the capacity to perform a wide variety of physiological functions including antifungal, antiviral, antitumor, and cell agglutination. The main objective of the current study was to prepare lectin protein-loaded chitosan-TPP nanoparticles via ionic gelation methods with different CS/TPP ratios and to investigate anticancer potential against HepG2 cells. The best ratio showed the mean particle size (298.

The impact of airborne pollution and exposure to solar ultraviolet radiation on skin: mechanistic and physiological insight.

For several decades air pollution has been recognized to hit drastically the skin of human body. Air pollutants predominantly accountable for aging, oxidative damage, and inflammatory allergic reactions led to psoriasis, dermatitis, acne, and skin cancer owing to the impaired functions of DNA, proteins, and lipid biomolecules. Elevated air pollution and its detrimental effects along with variations in physiological parameters of the skin are verily the scaffold for anti-pollution assertions and could be recognized as markers.

The improvement on the skin surface by a new type of dermocosmetic loaded plant extract: A split face skin topographic study.

Various extrinsic and intrinsic origins slant skins and pledge evident vicissitudes of the skin surface. We explored the effects of dermocosmetic loaded medical Cannabis seed extract and evaluate the improvement on the skin surface in Asian and male volunteers in a split face topographic study. Dermocosmetic and base (without extract) fabricated were directed to apply by volunteers (Asian male) on their right and left cheek, respectively, in the split face skin topographic study up to three months.

Sulfonamide-Based Azaheterocyclic Schiff Base Derivatives as Potential Carbonic Anhydrase Inhibitors: Synthesis, Cytotoxicity, and Enzyme Inhibitory Kinetics.

A series of sulfonamide-bearing azaheterocyclic Schiff base derivatives were synthesized as carbonic anhydrase inhibitors. The substituted benzene sulfonyl chlorides were reacted with NH to get aromatic sulfonyl hydrazides . The intermediate hydrazides were treated with substituted aldehydes to afford azaheterocyclic sulfonamide Schiff bases .

Synthesis, characterization and docking studies of amide ligands as anti-leishmanial agents.

Aim of this study was to synthesize new inhibitors on the basis of active site of aspartic protease enzyme and to evaluate their intended biological activity. A3D model of an enzyme was generated via homology modeling and series of novel amide ligands were synthesized by using a short high yield process, subsequently, analyzed in-silico and in-vitro anti-leishmanial activities. Characterization and identification was accomplished via NMR (H& C), infrared and mass spectroscopic techniques.

Evaluation of different Pakistani medicinal plants for inhibitory potential against Echis carinatus induced Phospholipase A2 toxicity.

Medicinal plants of Pakistan are known for their curative properties against snake bite as rural people have been using natural herbs for such injuries for hundreds to thousands of years. People of rural areas of Pakistan are prone to snakebite, and on the whole death due to snakebite has been increasing worldwide. The objective of this study was to test the neutralizing potential of 17 Pakistani medicinal plant extracts against phospholipase A2 activity in Echis carinatus venom.

Glycemic and Insulinemic Responses of Vegetables and Beans Powders Supplemented Chapattis in Healthy Humans: A Randomized, Crossover Trial.

Vegetables and beans are nutrient-dense foods with innate potential to mediate diabetes in a variety of cultures. The present study aims at evaluating vegetables and beans for assessing their glycemic index and response in raising glucose levels in human model. Powdered formulations of vegetables and beans were designed to modulate glycemic response of carbohydrate-rich staples.