Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.
Complement activation leads to membrane attack complex formation, which can lyse not only pathogens but also host cells. Histones can be released from the lysed or damaged cells and serve as a major type of damage-associated molecular pattern, but their effects on the complement system are not clear. In this study, we pulled down two major proteins from human serum using histone-conjugated beads: one was C-reactive protein and the other was C4, as identified by mass spectrometry. In surface plasmon resonance analysis, histone H3 and H4 showed stronger binding to C4 than other histones, with KD around 1 nM. The interaction did not affect C4 cleavage to C4a and C4b. Because histones bin
Introduction: The therapeutic efficacy of erythropoietin (EPO) may be diminished by the formation of anti-erythropoietin antibodies (AEAs), potentially resulting in therapy failure. Objectives: This retrospective study included 84 hemodialysis patients with end-stage renal disease (ESRD) treated with recombinant EPO and aimed to evaluate the association between serum AEA and treatment response. Patients and Methods: This cross-sectional study included eighty-four Iraqi patients with ESRD who had been on recombinant human EPO for more than 6 months and had hemoglobin levels below 11 g/dL. Serum AEA levels were measured in all patients to evaluate their association with treatment response and to investigate correlations with demograph
... Show MoreThe dried fruit peel of pomegranate in Punicaceae family was fractionated chromatographically on Sephadex-LH-20 column .Gallic acid (trihydroxybenzoic acid) and its related galloyl esters such as gallotannin(i.e. β-penta-O-galloyl–D-glucose) were obtained homogenously. Different concentrations of gallic acid and gallotannin were used to determine their inhibitory effect on human serum cholinesterase. The enzyme activity was measured according to the method reported by the WHO .The inhibitory effect of these compounds on the activity of human serum cholinesterase have been studied in vitro .The inhibitory effect was remarkably clear with increasing concentration of gallic acid .Whereas galloyl ester showed n
... Show MoreThe importance of algae as a natural source of various bioactive compounds continues to grow due to their diverse biological activities. One of such compounds is n-hexadecanoic acid, more commonly known as palmitic acid; it is more lipidous than many algal species. It is one of the most common saturated fatty acids in nature. One can find it in algal, animal, and plant oils and is extracted from numerous natural sources. Its chemical and biological attributes enable its widespread use in the pharmaceutical, food, and cosmetic industries. Numerous studies have found that palmitic acid is effective for fungal activities and does have pharmaceutical and environmental promising antioxidant capabilities.
Corrosion behavior of aluminum alloy 7025 was investigated in hydrochloric acid (pH=1) containing 0.6 mol.dm-3 NaCl in the existence and absence of diverse concentrations of sulphamethoxazole as environmentally friendly corrosion inhibitor over the temperature range (298-313)K. Electrochemical polarization method using potentiostatic technique was employed. The inhibition efficiency has been raised with increased sulphamethoxazole concentration but lessened at temperature increases. The highest efficiency value was 96.5 at 298 K and 2 x10-4 mol.dm-3 concentration of sulphamethoxazole. The sulphamethoxazole adsorption was agreed with Langmuir adsorption isotherm. Some thermodynamic parameter (△Gads) and activation energy (Ea) were determin
... Show MoreBackground: One of the unique prosthesis for tooth or teeth replacement is the dental implant. Our attempt is using a biomaterial system that is easily obtained and applicable and has the ability to provoke osteoinductive growth factor to enhance bone formation at the site of application. One of these natural polymers is hyaluronic acid. Material and methods: Sixty machined surface implants from commercially pure titanium rod inserted in thirty NewZealand rabbits. Two implants placed in both tibia of each rabbit. The animals scarified at 1, 2 and 4 weeks after implantation (10 rabbits for each interval). For all of animals the right tibia’s implant was control (uncoated) and the left one was experimental (coated with 0.1ml Hyaluro
... Show MoreEndoglucanase produced from Aspergillus flavus was purified by several steps including precipitation with 25 % ammonium sulphate followed by Ion –exchange chromatography, the obtained specific activity was 377.35 U/ mg protein, with a yield of 51.32 % .This step was followed by gel filtration chromatography (Sepharose -6B), when a value of specific activity was 400 U/ mg protein, with a yield of 48 %. Certain properties of this purified enzyme were investigated, the optimum pH of activity was 7 and the pH of its stability was 4.5, while the temperature stability was 40 °C for 60 min. The enzyme retained 100% of its original activity after incubation at 40 °C for 60 min; the optimum temperature for enzyme activity was 40 °C.
Abstract
The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibi
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