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PubMed1981

Tolfenamic acid. Detection and structure of urinary metabolites.

N-(2-Methyl-3-chlorophenyl)anthranilic acid (tolfenamic acid) and its metabolites in serum and urine were analyzed by a reversed-phase ion-pair HPLC method. The major metabolites were N-(2-methyl-3-chloro-4-hydroxyphenyl)anthranilic acid, and one of the minor metabolites was N-(2-formyl-3-chlorophenyl)anthranilic acid, i.e., products resulting from hydroxylation in either the methyl group or the methylchlorophenyl group of tolfenamic acid, and further oxidation of the hydroxymethyl group to a formyl group.

Adult↗
PubMed1999

Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors.

Eight small molecules were synthesized to evaluate the structure activity relationships (SAR) of N-substituted anthranilic acids. The molecules were synthesized by benzylation or arylation of methyl anthranilate. A light scattering-based amyloid fibril formation assay was used to evaluate potential inhibitors of transthyretin (TTR) amyloid fibril formation in vitro. The m-carboxyphenylated and o-trifluoromethylphenylated anthranilic acids are potent inhibitors that will be subjected to further SAR and structural analysis.

Amyloid↗
PubMed1989

Drug binding to alpha 1-acid glycoprotein studied by circular dichroism.

The interactions of acidic and basic drugs with alpha 1-acid glycoprotein (alpha 1-AGP) were investigated using circular dichroism (CD) measurements. Extrinsic Cotton effects were generated by the binding of drugs to alpha 1-AGP. The CD data suggested the presence of a single binding site on the alpha 1-AGP molecule. The induced ellipticities of the acidic drug-alpha 1-AGP system decreased with increasing pH, while the ellipticities for the basic drugs increased with pH. The ellipticities for all drugs were reduced by the addition of fatty acids. Furthermore, the induced ellipticities decreased in the presence of cesium chloride for basic drugs bound to alpha 1-AGP. The extrinsic Cotton effects therefore appear to result from hydrophobic interaction with alpha 1-AGP for the acidic drugs and from hydrophobic and electrostatic interactions for the basic drugs.

Acenocoumarol↗
PubMed1979

Effects of some anti-rheumatic agents on copper-catalyzed thermal aggregation of gamma globulin.

Gerber has shown that specific anti-rheumatics, D-penicillamine and aurothiomalate, inhibit copper(II)-catalyzed thermal aggregation of human gamma globulin. Various anti-rheumatics were tested for the activity. Steroidal and non-steroidal anti-inflammatory agents were almost ineffective, while a new non-steroidal anti-inflammatory agent, TAI-284 (6-chloro-5-cyclohexyl-1-indancarboxylic acid), was found to be one half as active as aurothiomalate. The structure-activity relationship of TAI-284 derivatives and the mode of action of TAI-284 were investigated.

Anti-Inflammatory Agents↗
PubMed1977

[Nonsteroid antirheumatic agents].

It is given a short, oriented to practice survey on the at present internationally most usual non-steroidal antirheumatic drugs. Picture of effect and efficiency, side-effects, indications and contraindications of these remedies are described and compared. The description comprises salicylates, phenylbutazone, indomethacin, flufenamine acid and mefenamine acid, ibuprofene as well as new substances (benorylate, clofezone, nuflumine acid, azapropazone, bumadizone calcium, naproxene and others). In their qualitities of effect the new drugs do not essentially differ from the classical antirheumatic drugs. However, they partly reveal a more favourable relation between desirable and undesirable effects.

Anti-Inflammatory Agents↗
PubMed1988

Induction of fibrinolysis by polyanions in human plasma.

The fibrinolytic potency of several polyanions was comparatively investigated. Fibrinolytic activity was measured in a whole plasma assay using H-D-Val-Leu-Lys-pNA (S-2251) as chromogenic substrate and by a fibrin plate assay using plasminogen rich fibrin plates. In the chromogenic substrate assay potent fibrinolytic polyanions comprised dextran sulfate, GAGPS, pentosan polysulfate, polyanethol sulfate, l-carrageenan and i-carrageenan. Chondroitin sulfates A, B, C, keratan sulfate, ribonucleic acid, k-carrageenan and heparin were weakly fibrinolytic. Hyaluronic acid and lipopolysaccharide from E. coli were inactive. Similar results were obtained when fibrinolytic activity was measured by a fibrin plate assay. All polyanions except lipopolysaccharide produced lysis zones. Induction of fibrinolytic activity in human plasma was shown to be at least partially dependent on Hageman factor. In factor XII deficient plasma no fibrinolysis was induced by any of the polyanions when measured in the fibrin plate assay. In the chromogenic substrate assay corn Hageman factor inhibitor (CHFI) inhibited the activation of S-2251 cleaving enzyme by GAGPS, pentosan polysulfate, polyanethol sulfate, heparin, and ribonucleic acid near completely. The activation by dextran sulfate was inhibited by 45%. Heparin, pentosan polysulfate and GAGPS, three polyanions of therapeutic interest were separately compared. In both assays GAGPS proved the most potent activator, while pentosan polysulfate exhibited 83% and 44% and heparin 32% and 14% of GAGPS fibrinolytic activity in the chromogenic substrate test and the fibrin plate assay, respectively.

Chromogenic Compounds↗
PubMed1990

Anti-oxidative profile of lobenzarit disodium (CCA).

The effects of lobenzarit disodium (CCA) on various species of activated oxygen were investigated in chemiluminescence experiments. CCA showed a quenching effect against hydroxyl radicals generated by Fenton reaction. The inhibition of CCA was much more intense than that of mefenamic acid which is an anti-inflammatory drug and an analogous compound to CCA. CCA also showed a quenching effect against singlet oxygen generated in enzymatic systems. However, CCA had no effect against superoxide anion radicals generated in the xanthine oxidase-hypoxanthine system. As a model of lipid peroxidation and protein alteration induced by activated oxygen, we examined the auto-oxidation of linolenic acid and the UV irradiation of immunoglobulin G (IgG). CCA inhibited the production of lipid peroxide; however CCA did not show a direct quenching action against lipid radicals which had been previously generated. CCA also inhibited the IgG alteration induced by UV irradiation. These results indicate that CCA has anti-oxidative actions with specificity for activated oxygen species and that CCA protects against lipid and protein damage induced by activated oxygen.

Antioxidants↗
PubMed1998

Discovering transthyretin amyloid fibril inhibitors by limited screening.

Insoluble protein fibrils, resulting from the self-assembly of a conformational intermediate are implicated to be the causative agent in several human amyloid diseases including familial amyloid polyneuropathy (FAP) and senile systemic amyloidosis (SSA). These diseases are associated with transthyretin (TTR) amyloid fibrils, which appear to form in the acidic partial denaturing environment of a lysosome or endosome. Here we identify several structural classes of small molecules that are capable of inhibiting the TTR conformational changes facilitating amyloid fibril formation. A small molecule inhibitor that stabilizes the normal conformation of a protein is desirable as a promising approach to treat amyloid diseases and to rigorously test the amyloid hypothesis, the apparent causative role of amyloid fibrils in amyloid disease.

Amyloid↗
PubMed1978

Glaucoma implants. Their use in difficult cases of glaucoma.

Implants with a regime of fibrosis suppression (prednisolone 30 mg daily plus fluphenamic acid 200 mg three times a day for 6 to 8 weeks) controlled the intraocular pressure (applanation tonometry (AT) less than 21 mm Hg) in seven out of ten patients with different types of glaucoma. One implant was removed after erosion of the conjunctiva and sclera; there were no other serious complications. Use of the implant is indicated after failed drainage operations or as a primary procedure in glaucoma associated with aphakia, chronic uveitis, vitreous in the anterior chamber, and scarring of the conjunctiva.

Adult↗
PubMed1975

Preliminary investigations of intrinsic and extrinsic optical activity as purity criterion for human serum albumins.

Induced circular dichroism measurements were made to follow the binding of four acidic drugs to two lots of crystalline and two lots of fraction V human serum albumins. The magnitude of the induced circular dichroism varied with all lots of albumin, suggesting a strong sensitivity of the phenomenon to small changes in purity or secondary structure of the albumins. The circular dichroism of the albumins themselves showed much less variation. The more classical analytical techniques of UV absorption, measurement of absorption following methyl orange binding, gel electrophoresis, and ultracentrifugation were also performed on the albumins for comparison.

Blood Protein Electrophoresis↗
PubMed1983

[Therapy of activated gonarthrosis with etofenamate cream (Rheumon cream)].

In a multicenter single-blind study on 60 patients with unilateral gonarthrosis the efficacy and tolerance of etofenamate cream were compared to a commonly used ointment containing salicylic acid and other ingredients. With respect to therapeutic success etofenamate was superior to the control medication. Mobility and circumference of the knee joint as well as pain parameters improved more rapidly in the etofenamate group, whereby the difference between both groups frequently was statistically significant. With the control medication therapy failed in three cases, with etofenamate cream clinical symptoms improved in all patients. With the exception of a transient local reddening of the skin in one patient of the etofenamate group no adverse drug reactions were observed.

Age Factors↗
PubMed1993

The isolated perfused bovine udder as an in vitro model of percutaneous drug absorption. Skin viability and percutaneous absorption of dexamethasone, benzoyl peroxide, and etofenamate.

Using udders from slaughtered cows as a new in vitro model of percutaneous drug absorption, the tissue viability and the percutaneous absorption of dexamethasone, benzoyl peroxide, and etofenamate were studied. The organ was perfused with gassed tyrode solution for up to 6 hr. As shown by measurement of glucose consumption, lactate production, lactate dehydrogenase activity, and pH in the perfusate, the tissue was viable over a 6-hr period. This was confirmed by a histological examination. Determination of the udder skin-fold thickness demonstrated that no edema developed within the perfusion period. A maximum skin penetration of dexamethasone was found after administration of dexamethasone dissolved in acetone with dimethyl sulfoxide, followed by ointment with salicylic acid, ointment without salicylic acid, and acetone solution. Experiments with benzoyl peroxide and etofenamate demonstrated that the perfused udder skin was capable of metabolizing drugs in vitro. In conclusion, the isolated perfused bovine udder is a new in vitro model, which maintains bovine udder skin with an isolated vasculature in a viable state. Using this in vitro model, we note it is possible to compare the dermal penetration, metabolism, and absorption of substances after topical administration of different drug formulations.

Animals↗
PubMed1977

[On the chemistry of etofenamate, a novel anti-inflammatory agent from the series of N-arylanthranilic acid derivatives (author's transl)].

Etofenamate is 2-(2-hydroxyethoxy)ethyl-N-(a,a,a,-trifluorom-tolyl)anthranilate and has been selected as an antiphlogistic agent for percutaneous therapy. Its characteristic alcohol-ether-ester structure brings about an increase in lipophilia and in its ability to penetrate through the intact skin. Furthermore, its oily consistency renders it ideal for pharmaceutical formulation in gels. The physico-chemical material constants, partition coefficients (RM values) as a measure for lipophilia, spectra and molecular models of etofenamate are described. Various methods of synthesis of etofenamate and of its intermediates are described. Structural identification is made of by-products simultaneously obtained in the reaction. Pure etofenamate is obtained through repeated molecular distillation. The synthesis is carried out uniformly with protected reaction components and, after splitting off the protective groups, extremely pure etofenamate is obtained.

Administration, Oral↗
PubMed1986

The stimulation of human synovial fibroblast plasminogen activator activity. Involvement of cyclic AMP and cyclooxygenase products.

The plasminogen activator activity of human synovial fibroblasts is raised by a monocyte-derived polypeptide, synovial activator and also by all-trans retinoic acid. The elevation of the synovial cell plasminogen activator activity by the two stimuli is potentiated both by agents which can raise cellular cyclic AMP levels, namely prostaglandin E2, cholera toxin and 3-isobutyl-1-methylxanthine, and also by exogenous 8-bromocyclic AMP. These findings suggest that there might be a substrate, which is phosphorylated by a cyclic AMP-dependent protein kinase and which is important in the modulation of the synovial cell plasminogen activator activity by the two stimuli. Prostanoids can be important in the stimulation of the synovial fibroblast plasminogen activator activity by mononuclear cell supernatants, since indomethacin can inhibit the increase in proteinase activity.

1-Methyl-3-isobutylxanthine↗
PubMed1987

Enzymatic hydrolysis of haloperidol decanoate and its inhibition by proteins.

When [14C]haloperidol decanoate, a long-acting neuroleptic and an ester of haloperidol and decanoic acid, was incubated in human whole blood and plasma and in rat plasma and homogenates of rat brain, lung, liver, kidney, pancreas and muscle, no hydrolysis of the ester was seen. Although the decanoate was hydrolyzed by partially purified carboxylesterase, addition of rat plasma or liver homogenate to the enzymic reaction mixture resulted in marked inhibition of hydrolysis, whereas addition of the defatted residues of plasma or liver produced only partial inhibition. The enzymic hydrolysis was inhibited also by beta-lipoprotein and albumin, depending on their concentrations. The assumption that interaction between haloperidol decanoate and protein resulted in inhibition of the hydrolytic reaction mediated by the enzyme was validated by kinetic models and experimental data. The kinetics were apparently competitive. Based on the kinetic analysis, the interaction between the decanoate and albumin or beta-lipoprotein was investigated by measuring their equilibrium constants and extent of protein binding. Haloperidol decanoate appeared to interact with several proteins; this was exemplified by other measures of protein binding, an increasing effect of proteins on the solubility, and the partition ratio of the ester. The interaction between haloperidol decanoate and proteins caused marked stabilization of this ester against enzymatic hydrolysis and, thereby, influenced its metabolism.

Animals↗