Blood Pressure Correlates with Serum Leptin and Body Mass Index in Overweight Male Saudi Students.

The precise association of serum leptin (Lep) with the body mass index (BMI) and blood pressure (BP) is not well known for understanding their involvement in health and disease. Hence, the present study was conducted to investigate the association of BP, BMI and serum Lep levels in young normal-weight (NW) and overweight (OW) male Saudi students. The NW (n: 198) and OW (n: 192) male subjects in the age range of 18-20 years were consulted. The BP was measured with a mercury sphygmomanometer. Leptin Human ELISA Kits were employed for the determination of the serum Lep levels. The mean ± SD values of BMI (kg/m2), Lep (ng/mL), systolic BP (SBP; mmHg), and diastolic BP (DBP; mmHg) all showed significant differences for young OW vs. NW subjects as: 27.52 ± 1.42 vs. 21.49 ± 2.03; 10.70 ± 4.67 vs. 4.68 ± 1.91; 121.37 ± 2.59 vs. 118.51 ± 1.54 and 81.44 ± 1.97 vs. 78.79 ± 1.44, respectively. All associations (among BMI, Lep, SBP and DBP) showed a positive linear and significant correlation, except the nonsignificant correlation of BMI and SBP for the NW group. Other variables showing significant variation for NW vs. OW subjects were: interleukin-6, high sensitivity C-reactive protein, apelin (APLN) and resistin. Serum APLN correlated significantly with Lep, BMI, SBP and DBP in lower and higher levels of BMI, with considerable progressive patterns in both the NW and OW groups and subgroups. The present study in young Saudi male students presents significant variations for BP and serum leptin levels, and a significant positive linear association among serum leptin, BMI and BP.

3-Substituted-2,3-Dihydrothiazole as a promising scaffold to design EGFR inhibitors.

The overexpression of EGFR has been recognized as the driver mechanism in the development of several human malignancies and the clinical use of EGFR inhibitors currently constitutes the standard of care for a wide range of malignancies, including colorectal cancer. However, the clinical efficacy of EGFR targeted inhibitors is limited by the development of intrinsic or acquired resistance, requiring the discovery of new compounds with different structural characteristics from those already developed. In this context, we explored the replacement of the aminoquinazoline pharmacophore of several FDA-approved EGFR inhibitors by its bioisosteric hydrazinothiazole moiety. A series of 14 new compounds were designed, synthesized, and evaluated as potential EGFR inhibitors. Compound 5i was active against 12 different cell lines in the NCI-60 cell line panel and showed an IC50 of 6.9 ± 0.013 µM against HCT-116 cells, with no significant toxicity against normal human fibroblasts (WI-38). Further studies showed that this compound showed submicromolar activity against EGFR and was able to induce tumor cell cycle arrest and cell apoptosis. Additionally, docking experiments, molecular dynamics and binding free energy calculations were performed and confirmed the potential of 2-hydrazino-2,3-dihydrothiazole derivatives as new EGFR inhibitors.

Biochemical Reactions and Their Biological Contributions in Honey.

Honey is known for its content of biomolecules, such as enzymes. The enzymes of honey originate from bees, plant nectars, secretions or excretions of plant-sucking insects, or from microorganisms such as yeasts. Honey can be characterized by enzyme-catalyzed and non-enzymatic reactions. Notable examples of enzyme-catalyzed reactions are the production of hydrogen peroxide through glucose oxidase activity and the conversion of hydrogen peroxide to water and oxygen by catalase enzymes. Production of hydroxymethylfurfural (HMF) from glucose or fructose is an example of non-enzymatic reactions in honey.

Identification of Some Promising Heterocycles Useful in Treatment of Allergic Rhinitis: Virtual Screening, Pharmacophore Mapping, Molecular Docking, and Molecular Dynamics.

Rhinitis is an allergic disease that causes troubles and restlessness for patients. In this research work we will focus on finding promising organic molecules with potential ability to target histamine receptor with no sedative side effect. Phalazines and their isosteres, pyrimidines and pyridines have been reported to target H1 receptors, for this reason we have searched for library of these basic scaffolds, this library which has 184 organic molecules will be subjected for further explorations through computer aided drug design techniques. Swiss ADMET will be used to gather these compounds in clusters. Cluster with low potential to penetrate BBB is selected for virtual screening through pharmacophore model. Then molecular docking that revealed the stability of the complex formed between the investigated molecules and H1 receptor. ADMET profile showed three compounds (XVIII), (XX), and (XXI) with no toxicity on liver and no effect on CYP2D6, these three compounds were subjected to molecular dynamic simulations and compound (XVIII) showed the most stable complex with the target protein (H1). Finally, we can say this work helped us to find new compounds with promising potential to target H1 without ability to penetrate BBB, so they can be used as useful candidates in treatment of rhinitis and deserve to be subjected for preclinical and clinical investigations. Supplementary Information: The online version contains supplementary material available at 10.1134/S1068162022330019.