Green Coffee Bean Extract Normalize Obesity-Induced Alterations of Metabolic Parameters in Rats by Upregulating Adiponectin and GLUT4 Levels and Reducing RBP-4 and HOMA-IR.

Obesity is a serious public health issue worldwide. Finding safe and efficacious products to reverse obesity has proven to be a difficult challenge. This study showed the effects of Coffea arabica or green coffee bean extract (GCBE) on obesity disorders and the improvement of obesity-induced insulin resistance, dyslipidemia, and inflammation. The active constituents of GCBE were identified via high-performance liquid chromatography. Twenty-four male albino Wistar rats were divided into two groups. The first group (Group I) was fed a control diet, whereas the second group was fed a high-fat diet (HFD) for eight weeks till obesity induction. The second group was equally subdivided into Group II, which received HFD, and Group III, which received HFD + GCBE for another eight weeks. The body and organ weights of the animals were measured, and blood and adipose tissue samples were collected for analysis. The results indicated that the administration of GCBE significantly decreased the body and organ weights. Furthermore, it had an ameliorative effect on serum biochemical parameters. It dramatically reduced total cholesterol, triacylglycerol, low-density lipoprotein cholesterol, very low-density lipoprotein cholesterol, glucose, and insulin levels. In addition, an improvement in homeostasis model assessment-insulin resistance and an enhancement of high-density lipoprotein cholesterol levels were observed compared with the HFD group. In addition, the group treated with GCBE exhibited a marked increase in serum levels of adiponectin (an anti-inflammatory adipokine). In addition, a considerable reduction in adipocyte hypertrophy was found following GCBE treatment. Remarkably, the administration of GCBE resulted in a remarkable decrease in the expression of RBP4 (a pro-inflammatory cytokine), whereas an increase in GLLUT4 expression was observed in the adipose tissue. This improved insulin resistance in GCBE-administered HFD rats compared with other HFD rats. Our study showed that GCBE exhibits anti-obesity activity and may be used as a natural supplement to prevent and treat obesity and its associated disorders.

Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon.

Some new pyridinethione and thienopyridine derivatives have been synthesized and evaluated for their antiproliferative activity using the MTT assay. Nicotinamide derivatives 3 have been synthesized and used for the preparation of new condensed thieno [2,3-b]pyridines by their reactions with active halo compounds. Finally the synthesized thienopyridine underwent ring closure whenever possible through boiling in a solution of sodium ethoxide. The antiproliferative evaluation against (HCT-116, HepG-2, and MCF-7) human cancer cells and one human healthy cell line (BJ-1) revealed that compounds 3b, 4c-5d, 7b-12a, 10d, and 13b have interesting antitumor activity specifically as antihepatocellular and anticolon cellular carcinoma agents. Besides, the docking results for most active derivatives were in agreement with the in vitro antitumor results.

Synthesis of Some Novel Heterocyclic and Schiff Base Derivatives as Antimicrobial Agents.

Treatment of 2,3-diaryloxirane-2,3-dicarbonitriles 1a-c with different nitrogen nucleophiles, e.g., hydrazine, methyl hydrazine, phenyl hydrazine, hydroxylamine, thiosemicarbazide, and/or 2-amino-5-phenyl-1,3,4-thiadiazole, afforded pyrazole, isoxazole, pyrrolotriazine, imidazolothiadiazole derivatives 2-5, respectively. Reacting pyrazoles 2a-c with aromatic aldehydes and/or methyl glycinate produced Schiff's bases 7a-d and pyrazolo[3,4-b]-pyrazinone derivative 8, respectively. Treating 7 with ammonium acetate and/or hydrazine hydrate, furnished the imidazolopyrazole and pyrazolotriazine derivatives 9 and 10, respectively. Reaction of 8 with chloroacetic acid and/or diethyl malonate gave tricyclic compound 11 and triketone 12, respectively. On the other hand, compound 1 was reacted with active methylene precursors, e.g., acetylacetone and/or cyclopentanone producing adducts 14a,b which upon fusion with ammonium acetate furnished the 3-pyridone derivatives 15a,b, respectively. Some of newly synthesized compounds were screened for activity against bacterial and fungal strains and most of the newly synthesized compounds showed high antimicrobial activities. The structures of the new compounds were elucidated using IR, ¹H-NMR, (13)C-NMR and mass spectroscopy.

Bromination and diazo-coupling of pyridinethiones; microwave assisted synthesis of isothiazolopyridine, pyridothiazine and pyridothiazepines.

Isothiazolopyridines, pyridothiazines and pyridothiazepines are important compounds that possess valuable biological activities. This paper reports on the synthesis of these compounds using both conventional chemical methods and modern microwave techniques. 3-Bromo-6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-carboxamide, 5-arylazo-6-hydroxy-4-methyl-2-thioxo-1,2-dihydropyridine-3-carboxamides, 3,5-bis-arylazo-6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-caboxamide, 4-methyl-2,3,6,7-tetra-hydroisothiazolo[5,4-b]-pyridine-3,6-dione, 2,2'-(methylene-bis-(sulfanediyl))bis(4-methyl-6-oxo-1,6-dihydropyridine-3-carboxamide), 2-hydroxy-5-methyl-4H-pyrido[3,2-e][1,3]-thiazine-4,7(8H)-dione and 2-arylmethylene-8-hydroxy-6-methyl-2,3,4,5-tetrahydropyrido-[3,2-f][1,4]thiazepine-3,5-diones have been prepared from 6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-carboxamide. Some of these compounds were prepared using microwave-assisted reaction conditions, that provided higher yields in shorter times than the conventional methods.

Magnetic resonance imaging as a sole method for the morphological and functional evaluation of live kidney donors.

OBJECTIVE: To evaluate gadolinium-enhanced dynamic magnetic resonance imaging (MRI) as the sole method for the anatomical and functional assessment of potential live-kidney donors. SUBJECTS AND METHODS: The study included 50 consecutive kidney donors; in addition to routine donor evaluation, the kidney was imaged with Gd-enhanced dynamic MRI, which was also used for selectively determining the glomerular filtration rate (GFR) of each kidney. All donors had a m99Tc-mercaptoacetyltriglycine (MAG3) renal scan as the reference standard to measure GFR. The anatomical results of MRI were compared with the findings at donor nephrectomy, and the GFR estimated from MRI compared with that from MAG3 scintigraphy. RESULTS: MR angiography had 100% sensitivity, 94% specificity and 96% overall accuracy for detecting the number of renal arteries, and 100% sensitivity, 98% specificity and 98% overall accuracy for the number of renal veins. There was a close correlation (r = 0.54, P < 0.01) between the GFR of each kidney estimated by MRI or MAG3. For the right and left kidneys the mean isotope clearance was not significantly different from that of mean MRI clearance. MR urography allowed visualization of the urinary tract and the detection of any abnormality. CONCLUSION: Gd-enhanced dynamic MRI can provide accurate information about the anatomy of the urinary tract and vasculature of the kidney, and can be used to accurately estimate the selective GFR of each kidney. Therefore, we recommend MRI as a single imaging diagnostic method for assessing potential live kidney donors.

Studies on thiazolopyridines--a novel synthesis of bis-thiazolopyridines as promising antimicrobial agents.

A variety of novel bis-thiazolopyridine derivatives 4a-e were synthesized via the reaction of bis-thiazolinone 3 with different arylcinnamonitrile derivatives (1:2 molar ratio), whereas the reaction of bis-compounds 7a-e with malononitrile in ethanol solution containing a few drops of piperidine afforded the novel bis-thiazolopyridines 8a-e. The structures of the synthesized compounds were established by elemental analyses and spectral data. Some of the newly synthesized compounds show moderate to high antimicrobial activity.