Abstarct

Development of NSAIDS based on inhibiting cyclooxygenase activity. However, the different physiological consequences arrised by appearance of new drugs with different selectivity to COX-2 enzyme upon their administration with their relevant affects on some cardiovascular risk factors. To study the potential effects of relatively diclofenac and highly specific celecoxib COX-2 inhibitors on lipid profile and serum C-reactive protein in type 2 diabetes, whom have hyperlipidemia to be compared by their effects with normolipidemic patients. A total number of 34 type 2 diabetics (14 normolipidemics and 20 hyperlipidemics) treated with either diclofenac 100mg/day or celecoxib 200mg/day for eight weeks. Analysis of results indicated that diclofenac increased serum triglycerides (TG) whereas; celecoxib group exerted a significant reduction in total cholesterol (TC), triglycerides (TG) levels in hyperlipidemic patients. Normolipidemic diabetics showed a significant elevation in serum total cholesterol, triglycerides and low density lipoprotein-cholesterol (LDL) with significant reduction in high density lipoprotein-cholesterol (HDL) in those treated with diclofenac , whilst those treated with celecoxib exhibited no modification of serum lipids. The results of the present study indicated that the net effect of treatment of hyperlipidemic type 2 diabetics by diclofenac was mostly qualitative as indicated by elevated TG/HDL ratio, to be a marker of atherogenic- small dense LDL particles in diabetics, whereas celecoxib exerted no such effect in this group but produced a beneficial reduction in LDL/HDL ratio. Meanwhile, diclofenac in normolipidemic diabetics exert a significant qualitative and quantitative modulation of their serum lipid components presented by net elevation in both LDL/HDL and TG/HDL ratios. As a conclusion the administration of relatively selective COX-2 inhibitors ( diclofenac ) to normolipidemic type 2 diabetics could adversely affect lipid metabolism by producing undesirable qualitative as well as , quantitative changes in serum lipid components, more than that observed in the hyperlipidemic diabetics.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

Summary:Background: The development of non steroidal anti-inflammatory drugs (NSAIDs) was based principally on inhibiting cyclooxygenases (COX) activity. However, the identification of two COX- isoforms (i.e., COX-1 and COX-2) with different physiological effects has led to the development of COX-2 specific NSAIDs, with fewer adverse effects than traditional NSAIDs. Therefore, They are expected to produce anti-inflammatory activity with minimal adverse effects on GI mucosa, as well as, other structures and cells such as platelets. The aim of this study is to evaluate the effect of selectivity of COX-2 inhibitors on many organs and systems function such as the hepatobiliary system, platelets function, as well as, serum uric acid levels. Patients and methods: Thirty six patients with osteoarthritis participated in this study. Twenty –four of them were treated with 400 mg celecoxib/day. The remainder received 15 mg meloxicam daily for 3 months .In addition to twelve apparently healthy subjects as a control . Measurement of serum alanine transaminase , serum alkaline phosphatase activity ,total serum protein, and serum albumin to evaluate hepatobiliary system . In addition to the estimation of bleeding time to evaluate the effect of selectivity of inhibitors to COX-2 on platelets function. Results: The results showed minor variations in their effects on liver function tests. However, meloxicam, the relatively selective COX-2 inhibitor affects bleeding time more than does celecoxib, the purely COX-2 selective. Whereas, celecoxib elevated serum levels of uric acid more than meloxicam.Conclusion: We could conclude that selectivity to COX-2 enzyme has different odds of risks on platelets function, such effects that could add more risk factors to patients due to their pharmacological action.Key words: Hepatobiliary, COX-2 inhibitors, Platelet function.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

Cell proliferation characteristics may reflect the aggressiveness of gastric cancer and their eventual prognosis. The aim of this study was to evaluate whether the proliferative activities determined by Ki-67 labeling index (LI) could be used as a predictor in patients with gastric cancer, and examine the relation between COX-2 and Ki-67 expression and gastric cancer. The expression of COX-2 and Ki-67 were detected in 40 patients with gastric cancer and 30 healthy individuals were assessed by immunohistochemistry. The biopsies were fixed in 10% buffered formaldehyde solution, embedded in paraffin and stained immunohistochemically with anti-human COX-2 and Ki-67 antibodies. Expression of Ki-67 andCOX-2was significantly higher in tumor compared with control samples.A significant correlation was found between COX-2 and Ki-67 protein expression. In conclusion,the expression of COX-2 and Ki-67 proteins was closely connected with gastric cancer.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to ل-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

AbstractBackground: Cyclooxygenase-2 (Cox-2) is a central mediator in inflammation and cancer. Expression of the Cox-2 gene is up-regulated in the gastric mucosa during H. pylori infection.Vascular endothelial growth factor (VEGF) has a potent angiogenic activity and cyclooxygenase-2 (COX-2) promotes angiogenesis by modulated production of angiogenic factors including VEGF.Aim: investigate the distribution and intensity of COX-2 and VEGF expression in premalignant and malignant gastric lesions with H. pylori.Material and Methods: Gastric biopsies from patients with chronic active gastritis and gastric adenocarcinoma, and control group were studied. Immunohistochemical analysis was used to examine the expression of COX-2 and VEGF in 81 cases of patients, including 30 cases with chronic gastritis infected with H. pylori, 51 cases of gastric cancer, 42 cases from GC have H. pylori and 30 cases with normal mucosa and none infected with H. pylori as control group.Results: In H. pylori-infected patients, COX-2 expression was predominantly found in the epithelium and, to a lesser extent, in the lamina propria. In the non infected group, few cases demonstrated weak COX-2 expression. Intensity of COX-2 was significantly different between the chronic active gastritis, gastric adenocarcinoma groups and control group. The positive rate of COX-2 was increased from chronic gastritis (60%), to gastric cancer (88.09%) in patients with H. pylori, compared with negative ones (22.58%). COX-2 was expressed in 23 of 24 intestinal types and in 14 of 18 diffuse types' carcinomas. The negative VEGF carcinomas have turned positive for COX-2 only for 76.92% of the cases. Different from those, the positive VEGF carcinomas have associated COX-2 immunoreactivity in 93.10% of the cases. Conclusions: These results suggest that COX-2 may play an important role in carcinogenesis by stimulating tumor angiogenesis. Also, show a relation between the expressions of COX-2 and VEGF in gastric carcinomas and the value significantly higher in the positive COX-2 carcinomas, suggesting an intense angiogenesis activity in that group of tumors.Keywords: Gastric cancer, Cox-2, H. pylori, tumor angiogenesis, VEGF

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

The aim of this study was identify the effect of (coxibs) on renal function in comparison to the traditional (NSAIDs) to provide more insight on this issue. Particular emphasis has been paid to the possible acute renal toxicities such as acute decline in renal function, hyperkalaemia, hypertension and sodium and water retension, the study was conducted during the period from (February –August) 2018 , Rheumatological out-patient clinic in Ibn-Sina Teaching Hospital in Mosul. patients and methods : Eighty patients with different rheumatological disorders who have no history of pre-existing renal disease. They were divided into 2 groups: Group A (40 patients): Treated with diclofenac sodium and Group B (40 patients): Who were treated with celeecoxib. Twenty healthy subjects, group C were taken as a control group. They have all undergone clinical examination including measurement of their body weights and blood pressure at the start of the study and repeated a month later.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

This study includes design and synthesis of new non-steroidal anti inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects.Two mefenamic acid derivatives were designed and synthesized as potential NSAIDs. In vivo acute anti-inflammatory effect of the synthesized agents (compound 2and 3) was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 2and 3 produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group), moreover compound 2 exhibited comparable anti-inflammatory effect to that of aspirin after 120 and 210 minutes and compound 3 has less anti-inflammatory effect, which encourages the continuation of the search to identify their selectivity toward COX-2 isoenzymes.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

This study includes design and synthesis of new non-steroidal anti-inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects. Two series of compounds have been designed and synthesized as potential NSAIDs,these are: Salicylamide derivatives (compounds 3,4,5 ) and Diflunisal derivatives (compounds 10&11). In vivo acute anti-inflammatory effect of one of the synthesized agents (compound 3) was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 3 exhibited less anti-inflammatory effect compared to that of aspirin after 120 and 210 minutes, which encourage the continuation of the search to demonstrate or identify the preliminary pharmacological activity for the synthesized compounds and to identify their selectivity toward COX-2 isoenzymes.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex

Abstarct

Inflammation is the complex biological response to a protective attempt to remove the injurious stimuli, most strongly implicated are prostaglandins (PGs), leukotrienes (LTs), histamine, bradykinin, platelet activity factor (PAF) and interleukins. The Phenytoin is a drug used for the treatment of antiepileptic. Phenytoin acts to suppress the abnormal brain activity seen in seizure by reducing electrical conductance among brain cells by stabilizing the inactive state of voltage gated sodium channels, Phenytoin (5,5-diphenylimidazolidine-2,4-dione) were prepared from benzil and urea with sodium hydroxide in absolute ethanol. The derivative of phenytoin was prepared from a histidine acidifies with hydrochloric acid in absolute ethanol and phenytoin to give phenytoin-3-histdine IUPAC name is (S)-3-(2-amino-3-(1H-imidazol-4-yl) propanoyl)-5,5-diphenylimidazolidine-2,4-dione.

Keywords

Export bibliographic record

Choose an application

• Reference Manager
• EndNote
• BibTex