88 research outputs found
Dizajniranje i sinteza novih derivata tiofenkarbohidrazida, tienopirazola i tienopirimidina s antioksidativnim i antitumorskim djelovanjem
2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3a), 1-(5-amino-4-(4-chloro-3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3b), 1-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) pyrazolidine-3,5-dione (4), (Z)-N\u27-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) formohydrazonic acid (5a), (Z)-ethyl-N\u27-(4-methyl-2-amino-5-acetylthiophene-3-carbonylformo hydrazonate (5b), 6-acetyl-3-amino-2,5-dimethylthieno2,3-dpyrimidin-4(3H)-one (8), 5-methyl-3-amino-2-mercapto-6-acetylthieno2,3-dpyrimidin-4(3H)-one (10) and 5-methyl-6-acetyl-2-thioxo-2,3-dihydrothieno2,3-dpyrimidin-4(1H)-one (12) as potential antioxidant and antitumor agents. Pharmacological results showed that compounds 6a, 6b, 8, 10 and 12 exhibited promising antitumor and antioxidant activity.Etilni ester 2-amino-5-acetil-4-metil-tiofen-3-karboksilne kiseline (1) i 5-acetil-2-amino-4-metiltiofen-3-karbohidrazid (2) sintetizirani su i upotrebljeni kao reaktanti u sintezi novih spojeva 1-(5-amino-4-(3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3a), 1-(5-amino-4-(4-klor-3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3b), 1-(4-metil-2-amino-5-acetiltiofen-3-karbonil) pirazolidin-3,5-diona (4), (Z)-N\u27-(4-metil-2-amino-5-acetiltiofen-3-karbonil) formohidrazonske kiseline (5a), (Z)-etil-N\u27-(4-metil-2-amino-5-acetiltiofen-3-karbonilformo hidrazonata (5b), 6-acetil-3-amino-2,5-dimetiltieno2,3-dpirimidin-4(3H)-one (8), 5-metil-3-amino-2-merkapto-6-acetiltieno2,3-dpirimidin-4(3H)-ona (10) i 5-metil-6-acetil-2-tiokso-2,3-dihidrotieno2,3-dpirimidin-4(1H)-ona (12) kao potencijalnih antioksidansa i citostatika. Farmakološka ispitivanja ukazuju na to da spojevi 6a, 6b, 8, 10 i 12 imaju značajno antitumorsko i antioksidativno djelovanje
EPHA2 Is Associated with Age-Related Cortical Cataract in Mice and Humans
Age-related cataract is a major cause of blindness worldwide, and cortical cataract is the second most prevalent type of age-related cataract. Although a significant fraction of age-related cataract is heritable, the genetic basis remains to be elucidated. We report that homozygous deletion of Epha2 in two independent strains of mice developed progressive cortical cataract. Retroillumination revealed development of cortical vacuoles at one month of age; visible cataract appeared around three months, which progressed to mature cataract by six months. EPHA2 protein expression in the lens is spatially and temporally regulated. It is low in anterior epithelial cells, upregulated as the cells enter differentiation at the equator, strongly expressed in the cortical fiber cells, but absent in the nuclei. Deletion of Epha2 caused a significant increase in the expression of HSP25 (murine homologue of human HSP27) before the onset of cataract. The overexpressed HSP25 was in an underphosphorylated form, indicating excessive cellular stress and protein misfolding. The orthologous human EPHA2 gene on chromosome 1p36 was tested in three independent worldwide Caucasian populations for allelic association with cortical cataract. Common variants in EPHA2 were found that showed significant association with cortical cataract, and rs6678616 was the most significant in meta-analyses. In addition, we sequenced exons of EPHA2 in linked families and identified a new missense mutation, Arg721Gln, in the protein kinase domain that significantly alters EPHA2 functions in cellular and biochemical assays. Thus, converging evidence from humans and mice suggests that EPHA2 is important in maintaining lens clarity with age
Acyloxylation of Cyclic Enones: Synthesis of Densely Oxygenated Guaianolides
The α′-acyloxylation of cyclic enones with linear carboxylic acids is described. The reaction is promoted by KMnO4 in the presence of a carboxylic acid and its corresponding carboxylic anhydride. The optimization of the reaction has been carried out using the statistical methodology known as design of experiments. The optimized reaction conditions have been evaluated in terms of substrate scope and compatibility with different functional groups. The methodology has been applied to the synthesis of densely oxygenated guaianes and guaianolides
Genetic analysis of typical wet-type age-related macular degeneration and polypoidal choroidal vasculopathy in Japanese population
Age-related macular degeneration (AMD) is a common cause of blindness in the elderly. Caucasian patients are predominantly affected by the dry form of AMD, whereas Japanese patients have predominantly the wet form of AMD and/or polypoidal choroidal vasculopathy (PCV). Although genetic association in the 10q26 (ARMS2/HTRA1) region has been established in many ethnic groups for dry-type AMD, typical wet-type AMD, and PCV, the contribution of the 1q32 (CFH) region seem to differ among these groups. Here we show a single nucleotide polymorphism (SNP) in the ARMS2/HTRA1 locus is associated in the whole genome for Japanese typical wet-type AMD (rs10490924: \documentclass[12pt]{minimal}
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\begin{document}\end{document}, OR = 2.72) followed by CFH (rs800292: \documentclass[12pt]{minimal}
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\begin{document}\end{document}, OR = 2.08; \documentclass[12pt]{minimal}
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\begin{document}\end{document}, OR = 2.00), which differs from previous studies in Caucasian populations. Moreover, a SNP (rs2241394) in complement component C3 gene showed significant association with PCV (\documentclass[12pt]{minimal}
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\begin{document}\end{document}, OR = 3.47). We conclude that dry-type AMD, typical wet-type AMD, and PCV have both common and distinct genetic risks that become apparent when comparing Japanese versus Caucasian populations
Insights into the Genetic Architecture of Early Stage Age-Related Macular Degeneration: A Genome-Wide Association Study Meta-Analysis
10.1371/journal.pone.0053830PLoS ONE81
Constituents of plants growing in Qatar XVII anti-inflammatory and cytotoxic activities of extracts of thirty indigenous species
Thirty plants, indigenous to Qatar, were extracted separately with hexane, chloroform and ethanol. The dried extracts were examined for potential anti-inflammatory activities both in vitro by their ability to inhibit agonist-induced platelet aggregation and in vivo by a topical antierythema test. The same extracts were also tested for cytotoxicity to mononuclear cells. Fourteen extracts were found to exhibit significant antiaggregatory activity when DOP (Phorbol ester) was used as agonist in human platelets, five extracts inhibited PAF-acether induced rabbit platelet aggregation and four extracts inhibited ADP-induced aggregation of human platelets. Three plant extracts demonstrated a significant inhibition of phorbol ester-induced erythema of mouse skin in vivo. An in vitro cytotoxicity test showed that twenty-four of the species investigated exhibited significant toxic effects on human mono-nuclear cells at a dose of 5 μg dry weight of extract/ml. © 1990 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted
دراسة المكونات الكيميائية لبعض الطحالب البحرية التي تنمو على سواحل قطر
The most dominant twenty three algal species representing the main three groups of benthic macroalgae, Chlorophyceae, Phaeophyceae and Rhodophyceae were collected from the coastal zones of the Qatar peninsula. These algae were screened for alkaloids, coumarins, flavonoids, saponins and tannins. The moisture, ash, protein, lipid, carbohydrate, minerals and trace elements content of the investigated algal species were determined.يشمل البحث المسح الكيميائي لثلاثة وعشرين طحلبا تمثل أكثر الأنواع انتشارا على سواحل دولة قطر وذلك لتحديد نسبة ما تحتويه من بروتين -كربوهيدرات -معادن وكذلك الكشف عن وجود القلويدات - الكومارينات - الفلافونيدات - السابونينات والتانينات
المركبات الحلقية غير المتجانسة لأسترات الأكريل الأمينية ذوات النشاط البيولوجي المتوقع
This work describes the synthesis of N-substituted piperidyl 2-benzoxazole acrylates (la-d); 2-benzothiazole acrylates (2a-d); 2-furyl acrylates (3a-d) and 2-thiophene acrylates (4a-d). The esters of 3-quinuclidyl (Ie, 2e, 3e, 4e) and N, N-dimethylaminoethyl - (If, 2f, 3f, 4f) and of N, N-diethylaminoethyl - (Ig, 2g, 3g, 4g) of the respective acids have been also synthesized.
The psychotopathic properties of the prepared compounds will be published elsewhere.يشمل هذا البحث نتيجة تفاعلات أحماض بنزاوكسازول - 2 - أكريليك ، بنزوثيازول - 2 - أكريليك ، فيوران - 2 - أكريليك ، ثيوفين - 2 - أكريليك أو مشتقاتها مع الببريدينول أو مشتقاته ، ثنائي ميثيل وثنائي ايثيل ايثاثول أمين لتحضير استرات هذه الأحماض للكحولات المذكورة . والغرض من تحضير هذه الاسترات اختبار فعاليتها البيولوجية على الجهاز العصبي
مكونات نبات السيمبوبوجن
A comprehensive review of the Cymbopogon species including the essential oils and their constituents is given. An account of the other components viz. non volatile terpenoids and phenolic compounds is also given. The biological activities of the studied Cymbopogon species are also reported.نباتات السيمبوبوجن تشتهر باحتوائها على زيوت عطرية ( طيارة ) والكثير من زيوتها أو مكوناتها له استخدامات عديدة في صناعة العطور ، ويتناول هذا البحث عرضا لمكونات الزيوت الطيارة للأنواع المختلفة التي تنتمي إلى جنس السيمبوبوجن وكذا المركبات الأخرى مثل التربينات الثلاثية والمواد الفينولية ( الفلافونيدات ، الكومارينات وغيرها ) كما يتناول البحث استعراضا للاستخدامات الطبية لهذه النباتات والخواص البيولوجية لسواد المفصولة منها
Evidence for some prostaglandins in Allium sativum extracts
Homogenized garlic (Allium sativum Linn.) was extracted successively with organic solvents and the prostaglandin-rich fraction separated. Fractionation of the extract with column chromatography was performed. TLC of the extract indicated that prostaglandin like materials could be present. GC analysis detected prostaglandins A2 and F1? in the extract. This conclusion was confirmed by enrichment procedures using GC
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