Hyperlipidemia is one of the most important factors leading to atherosclerosis and heart disease, therefore, this study conducted to examine the effect of two newly synthesized compounds[3-(5(ethylthio)-1,3,4-thiadiazol-2-yl)-2,3-dihydro-2-(3-nitrophenyl)benzo[1-3-e] thiazin-4-one (I) and 5(4dimethyl amino) benzylidene amino)-1,3,4-thiadiazole-2-thiol(II)] on the activities of creatine kinase(CK) and 3-hydroxy-3-methylglutaryl- CoA reductase (HMGR) in male Wister mice . Also to determine the type of inhibition of these compounds on the above enzymes .The study was carried out on sixty male Wister mice aged seven to eight weeks their weight ranged(180-200 g) . The mice were grouped as: group(1): control group (12 mice).Group(2):consisted of 48 mice in which the mice were daily administered cholesterol (25mg/kg/day) in coconut oil 6% and creamy cheese for 28 days. Lipid profile was measured for 12 of mice chosen randomely from G2 to assure hyperlipidemia. Then group2 is subdivided into three groups as:group (2.A): (12 mice) positive control group in which the mice were daily administered simvastatin (40mg /day) as standard drug for hyperlipidemia for 20 days.Group(2.B):(12 mice) in which the mice were daily treated with (10-4)M of compound (I)via drinking water for 20 days. Group(2.C):(12 mice) in which the mice were daily treated with (10-5)M of compound II via drinking water for 20 days.Lipid profile(Tch, TG, HDL-c, LDL-c and VLDL-c) were determined in all groups.The activities of CK and HMGR were determined in all groups. Lineweaver-Burk plot was used for determination of Vmax, Km and type of inhibition for treated and untreated groups with compounds I and II. The results showed significant elevation in levels of Tch, TG, LDL and VLDL, while there are significant reduction in HDL-c levels in G2 comparing to control group(G1), after administration of fat rich diet. Simvastatin, compound I with concentration (10-4M) and compound I The results revealed that the levels of Tch, TG, LDL and VLDL were reduced while the levels of HDL-c was elevated after administration of simvastatin, compound I and II in G2A, G2B and G2C respectively. The results showed that the activities of CK reduced for group G2B and G2C while it is increased for G2A . The results also showed that the activities of HMGR were reduced in the three groups. The effect of compound I on CK activity was found to be noncompetitive inhibitor with Vmax values values(1000and 166.6) U/L respectively for the uninhibited and inhibited reactions and Km value (0.6)mmol/L for compound I and with Vmax values (1000 and 250)U/L and Km value(0.84)mmol/L respectively for the uninhibited and inhibited reactions for compound II. Compounds I and II were found to be noncompetitive inhibitors on HMGR with Vmax values (0.83 and 0.16)U and Km value (0.34)mmol/L respectively for the uninhibited and inhibited reactions for compound I and Vmax values (0.83 and 0.35) U and Km value(0.28)mmol/L respectively for the uninhibited and inhibited reactions for compound II. In conclusion the new compounds(I and II) showed different inhibitory effect on CK and HMGR activities that could be used in treatment of hyperlipidemia and related disease in future.
This work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring. The new 2-amino-1, 3, 4thiadiazole derivatives[IV] and [V]a, b were synthesized by cyclization reaction of 2-methyl1H-indole-carbothiosemicarbazide[III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone derivatives [XI]a, b were s
... Show MoreThis work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring. The new 2-amino-1, 3, 4-thiadiazole derivatives [IV] and [V] a, b were synthesized by cyclization reaction of 2-methyl-1H-indole-carbothiosemicarbazide [III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2-amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone derivatives [XI] a, b were synthesized from heati
... Show MoreThe protective effect of benfotiamine against doxorubicin-induced cardiotoxicity was evaluated in rabbits. Pretreatment of rabbits with 70mg/kg benfotiamine orally 7 days before induction of cardiotoxicity with I.V 15mg/kg doxorubicin. injection resulted in significant reduction of the activities of lactate dehydrogenase and creatine phosphokinase enzyme in the serum compared to doxorubicin treated animals; benfotiamine also improves the histological changes produced by doxorubicin in the cardiac muscle compared to control. In conclusion, benfotiamine when used concomitantly with doxorubicin protects the myocardium against the cardiotoxicity induced by this cytotoxic drug.
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تم في هذه الدراسة ، تزيين رقائق أكسيد الجرافين (GO) بجسيمات كوبلتيت النيكل النانوية NiCo2O4(NC) عن طريق الترسيب في الموقع ، وتم استخدام المتراكب المحضر (NC: GO) كسطح ماز لإزالة صبغة الميثيل الخضراء ( MG) من المحاليل المائية. تم التحقق من التغطية الناجحة لأوكسيد الجرافين بجزيئات كوبلتيت النيكل النانوية (NC) باستخدام دراسات FT-IR وحيود الأشعة السينية (XRD). كانت أحجام الجسيم
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Biomimicry, as a way of thinking to go back to nature for inspiration, has its impact on many contemporary technological achievements. Some of them are used to design and construct kinetic facades in architecture, because of the importance role of facades in reducing sun radiation, that enter the building through using shading systems and components. In light of this, research problem is determined: "Do technologies which are inspired by biomimicry effect shading in kinetic facades through its characteristics in materials and the mechanics. So the research identifies its goal as: "To identify the types of kinetic facades in buildings and their characteristics as materials and shading mechanism associated with the b
... Show MoreThe present study has conducted to investigate the effect of hot aqueous extract of seeds and leaves of fenugreek (Trigonella foenum-graecum) on embryonic development in Swiss albino mice morphologically , the results is showed throught dosage pregnant female orally after period 4, 8, 12days at the beginning of pregnancy by doses 100 , 200 , 300 mg/kg of body weight , the results showed normal period of pregnancy 21 days and abortion did not occur when the pregnant mice take the hot aqueous extract of leaves of fenugreek, but the pregnant mice that take the hot aqueous extract of seeds of fenugreek occurred abortion of embryos and showed some histopathological changes in ovaries and uterus such as congestion, hemorrhage, necrosis, odema,
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In this study the new azo compounds (3compounds) for nitrogen bases (Adenine and Cytosine) are synthesized through two reaction steps (formation of diazonium salt and coupling reaction). The compounds have been characterized by FTIR, melting point, and ultra-violate (UV) spectra. All synthesized compounds have been estimated in vitro for their antimicrobial activities against two species of bacteria(E.coli, S.aureus)and one kind of fungi ( Aspergillus flavus) .The results show that these compounds have very good antibacterial and antifungal activities especially compounds 1 and 3.To study the effect of these compounds were making some physiological tests on rats are made ,the results of hematological study showed decreasing level of
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