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.
Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehy
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This study included effect of polyherbs mixture treatment of diabetic patients type II for two months. The polyherbs mixture contains Nigella sativa seeds, Boswellia carterri gum, Citrus aurantifolia fruits, Elettaria cardamomum fruits. Also this study included estimation of some biochemical parameters in the serum Diabetes Mellitus (D.M.) patients-type II and knowing the relationship of these parameters with this disease. The parameters are glucose, cholesterol ,High density , Low density lipoproteins( HDL-C, LDL-C) respectively , Triglycerides TG, urea, total protein , albumin , Alkaline phosphatase ALP,Transaminase GOT, GPT enzymes . Take (77) samples of diabetic patients serum type II which included (47) samples for group one: herbs
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Condensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-
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In the present research synthesis and study of biological activity a series of new polymers modified of chitosan with compounds containing azo group. Beginning diazonium salt produced from 3,3'-dimethyl-[1,1'-biphenyl]-4,4'-diamine reacted with concentrated HCl acid and sodium nitrite. The coupling reaction between diazonium salt with substituted aromatic aldehyde to produce Azo derivatives )1-6(. Azo Schiff bases Chitosan )7-12( were synthesized by condensation of Chitosan with Azo derivatives )1-6( in ethanol with some drops of glacial acetic acid. The structural modifications of Chitosan ring (linked to a bioactive azo moiety) were expected to give new derivatives )7-12( with a diverse range of biological functions. These compounds' st
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Identifying phenolic compounds in some genera belonging in the Amaranthaceae family by HPLC technique
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This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [4-(1,3-dioxoisoindolin-2-yl)benzoic acid] was synthesized by reaction p-aminobenzoic acid and phthalic anhydride in presence of (gla. CH3COOH). Reaction of compound (V) with thionyl chloride produced [4-(1,3-dioxoisoindoli
... Show MoreAn experiment was carried out on the fields of the college of Agriculture - Abu Ghraib, of a silty clay loam soil that has moisture of 15-16%, to study the effect of plowing and pulverization systems on some plant indicators of onion. The experiment included plowing systems with three levels (plowing with a moldboard plow, plowing by chisel plow and zero tillage plowing) as a primary factor. The second factor was that pulverization for only one time and repeating the pulverization twice through the use of the rotary tiller. The plant indicators of onion that are studied: plant length, onion diameter, onion weight and onion neck diameter. The experiment has carried out according to SPLIT PLOT design according to RCBD design by three replicat
... Show MoreBackground: The restoration of bone continuity and bone union are complex processes, and their success is determined by the effectiveness of osteosynthesis. The use of plants for healing purposes predates human history and forms the source of current modern medicine The aim of this study: It was histological evaluation of effect of topical application of flavonoid on healing of induced bone defect in rabbit tibia. Material and method: Twenty-four Adult New Zealand rabbits used in this study, they were divided into four groups for the healing periods (3days, 1,2, and 4weeks) Two holes were induced in rabbit tibia one on the left side and has been left to heal normally as control. While, the other hole made on the right side filled with flavo
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