Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P06889 (Mol)
 630,302 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The interaction of Cd(II) with the non-steroidal anti-inflammatory drug diclofenac sodium (Dic) leads to the formation of the complex [Cd2(L)41.5(MeOH)2(H2O)]n(L = Dic), 1, which has been isolated and structurally characterized by X-ray crystallography. Diclofenac sodium and its metal complex 1 have also been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The results of cytotoxic activity in vitro expressed as IC50 values indicated the diclofenac sodium and cadmium chloride are non active or less active than the metal complex of diclofenac (1). Complex 1 was also found to be a more potent cytotoxic agent against T-24 and MCF-7 cancer cell lines than the prevalent benchmark metallodrug, cisplatin, under the same experimental conditions. The superoxide dismutase activity was measured by Fridovich test which showed that complex 1 shows a low value in comparison with Cu complexes. The binding properties of this complex to biomolecules, bovine or human serum albumin, are presented and evaluated. Antibacterial and growth inhibitory activity is also higher than that of the parent ligand compound.
Spectrochim Acta A Mol Biomol Spectrosc 2015 Feb 05
PMID:Synthesis, crystal structure and spectroscopy of bioactive Cd(II) polymeric complex of the non-steroidal anti-inflammatory drug diclofenac sodium: antiproliferative and biological activity. 2531 20

A novel method was developed for spectral resolution and further determination of five-component mixture including Vitamin B complex (B1, B6, B12 and Benfotiamine) along with the commonly co-formulated Diclofenac. The method is simple, sensitive, precise and could efficiently determine the five components by a complementary application of two different techniques. The first is univariate second derivative method that was successfully applied for determination of Vitamin B12. The second is Multivariate Curve Resolution using the Alternating Least Squares method (MCR-ALS) by which an efficient resolution and quantitation of the quaternary spectrally overlapped Vitamin B1, Vitamin B6, Benfotiamine and Diclofenac sodium were achieved. The effect of different constraints was studied and the correlation between the true spectra and the estimated spectral profiles were found to be 0.9998, 0.9983, 0.9993 and 0.9933 for B1, B6, Benfotiamine and Diclofenac, respectively. All components were successfully determined in tablets and capsules and the results were compared to HPLC methods and they were found to be statistically non-significant.
Spectrochim Acta A Mol Biomol Spectrosc 2015 Apr 05
PMID:A novel spectral resolution and simultaneous determination of multicomponent mixture of Vitamins B1, B6, B12, Benfotiamine and Diclofenac in tablets and capsules by derivative and MCR-ALS. 2564 31

Transition metal complexes containing tri-dentate NSN donor ligands i.e., 5-((1(aminomethyl)cyclohexyl)methyl)-1,3,4-thiadiazol-2-amine (AMTA) (2) and 5-(2-aminophenyl)-1,3,4-thiadiazol-2-amine (ATA) (4i-ii) have been synthesized. The newly synthesized ligands and their respective complexes were characterized by elemental analysis, molar conductance measurement and various spectral studies [infrared (IR), electronic, and NMR (for ligands only)]. Metal complexes are like [M(AMTA)2], [M(ATA)2] type, where M=Mn(II), Co(II) and Cu(II). The proposed geometries of the complexes are octahedral in nature. The synthesized ligands and their complexes were exhibits effective anti-inflammatory, analgesic and DNA binding activities. All the tested compounds exhibited significant analgesic activity, whereas the compound 4i, 4(ia) and 4(iib) is equipotent with Diclofenac sodium.
Spectrochim Acta A Mol Biomol Spectrosc 2015 Apr 15
PMID:DNA binding, anti-inflammatory and analgesic evaluation of metal complexes of N/S/O donor ligands; synthesis, spectral characterization. 2566 28

Diclofenac sodium (DS) was the third generation non-steroidal drugs with analgesic and antipyretic properties. Owing to taking action faster, long lasting potency, good efficacy and low side effects, DS was widely used in the pharmaceutical industry. To further ensure animal food safety and consumer health, the rational usages regulations of DS and DS withdrawal time should be provided. In the present study, a new high performance liquid chromatography tandem mass spectrometry (HPLC/MS) method was first established for extracting and validating diclofenac sodium levels in edible porcine tissues. Meanwhile, the pharmacokinetics characteristics and residue elimination of intramuscular DS administration in pigs were also studied. We found DS eliminated quickly and the distribution was poor in vivo. After a single dose of 2.5 mg/kg body weight per day for continuous 3 days, the withdrawal time in the tissues of liver, kidney, sebum, muscle and administration site were 9.892 days, 5.116 days, 14.205 days, 5.444 days and 8.818 days, respectively. According to the double-sided 95% confidence interval, DS withdrawal period should be 15 days. These experiment evidences lay a good foundation on the rational usages regulations of DS and DS withdrawal time, which will be helpful for the animal food safety and consumer health.
Cell Mol Biol (Noisy-le-grand) 2019 Jan 31
PMID:Pharmacokinetics and residues elimination of diclofenac sodium administration in pigs by a new HPLC/MS method. 3078 91

Supersaturable active pharmaceutical ingredients (sAPI), such as salts, cocrystals, and amorphous solids, can form supersaturated solutions after dissolving in the gastrointestinal fluids. However, there are cases in which supersaturation is not observed in an in vitro nonsink dissolution test. The purpose of the present study was to investigate the mechanisms of supersaturation suppression in the dissolution process of acidic drug salts. Diclofenac sodium (DCF Na, p Ka = 4.0) was employed as a model drug. DCF Na APIs and tablets (25 mg, 0.08 mmol) showed little or no supersaturation at pH 1.2 (compendial paddle apparatus, 500 mL, 50 rpm). However, marked supersaturation was observed at pH 2.0 and 3.0. The liquid-liquid phase separation (LLPS) of DCF free acid (FA) was observed in the surrounding of the DCF Na particles immediately after contact with acidic media. Particularly at pH 1.2, the surface of DCF Na was immediately covered with the liquid (oil) layer of DCF FA. The DCF FA liquid layer started to crystallize within several minutes. The LLPS concentration of DCF FA (0.30 mM) was twice as high as the theoretical maximum concentration after the complete dissolution of DCF Na in the dissolution test (0.16 mM). In addition, in the bulk phase precipitation test at 0.16 mM, rapid concentration reduction was not observed within 1 h in the bulk media. Taken together, these results suggest that the LLPS (and subsequent crystallization) of DCF FA on the surface of DCF Na particles rather than in the bulk medium is more likely to have suppressed the supersaturation from DCF Na.
Mol Pharm 2019 04 01
PMID:Mechanism of Supersaturation Suppression in Dissolution Process of Acidic Drug Salt. 3079 20