Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Hymecromone”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 37 records · Page 2Linked to original sources
PubMed1997

[Pharmacologic modification of postprandial bile duct kinetics--ultrasound measurement of the lumen of the bile duct].

UNLABELLED: The physiological correlate of biliary colic is a rapid increase in pressure in the presence of biliary obstruction. The relaxing action of hymecromone on the biliary tract provides a pharmacotherapeutic approach. PURPOSE: Since the symptoms usually occur postprandially, we used ultrasonography to examine whether hymecromone could reverse the contraction of the common bile duct (CBD) after ingestion of a standardised test meal. METHOD: The study was designed as a prospective, double-blind randomised cross-over study versus placebo in 20 healthy volunteers. The width of the CBD was measured ultrasonographically in the fasting subjects and 1, 3, 5, 10, 15 and 20 minutes after ingestion of a test meal. The subjects were then given either 400 mg of hymecromone or placebo i.v. and the measurement series was repeated. RESULTS: After ingestion of the test meal the width of the CBD decreased by a maximum of 20% after 15 minutes. While there was only a slight increase in the width of the CBD after subsequent administration of placebo, a maximum increase of 36% was measured 10 minutes after administration of hymecromone. CONCLUSION: The postprandial contraction of the CBD can be reversed within a short time by i.v. administration of hymecromone. Sonography proved a suitable tool for examining the physiological changes.

Adult↗
PubMed1980

[Pharmacological effects on the motor activity of Oddi's sphincter. Postoperative electromanometric measurements of the bile ducts].

Besides the high diagnostical value of the electromanometric measurement, this method is especially useful for the registration of pharmacological effects upon the sphincter of Oddi. In this study the influence of hymecromon on sphincter function was tested in 138 patients. Hymecromon induced a significant decrease of pressure by prolonging the opening time (p < 0.001). In clinical experiments it could be shown that the increase of pressure induced by morphine in the common bile duct could be equalized by hymecromon within a short time. Depending significantly on the dosage (p < 0.01) there were identical results on the intravenous or intraductal application of hymecromon. An increase of activity of the liver-specific enzymes could not be seen after hymecromon treatment.

Ampulla of Vater↗
PubMed1996

Gallbladder dyskinesia in acalculous biliary colic.

AIMS: To test the hypotheses that: 1) postprandial gallbladder emptying might be abnormal in patients with acalculous biliary colic; and 2) that hymecromone, a drug that increases bile flow and relaxes biliary muscle might improve symptoms. METHODS: Twenty-four women were studied. Twelve patients presented recurrent biliary type of pain in the absence of gallstones, and persistence of contrast in the gallbladder, 24 hours after an oral cholecystogram, suggesting cholesterolosis. Twelve healthy volunteers used as controls had no symptoms and the gallbladder was not visible the day after an oral cholecystogram. Gallbladder emptying induced by an oral meal was studied with ultrasound in both groups before and after the administration of hymecromone. RESULTS: Gallbladder volumes were similar in both groups (23 +/- 10 ml vs. 31 +/- 11 ml; NS). Gallbladder emptying in the control group was simple exponential (R2 = 0.948 +/- 0.059) with a rate of 32 +/- 16 minutes. Gallbladder emptying was bimodal in patients. Gallbladder volume increased to 120% in the first 10 minutes, to empty exponentially thereafter (R2 = 0.964 +/- 0.040. Rate: 29 +/- 22 minutes). This resulted in a marked reduction in gallbladder volume emptied at 40 minutes when compared to controls (30% +/- 27% vs. 54% +/- 14%; p = 0.012). Pretreatment of controls with hymecromone induced an emptying pattern similar to that of patients. In patients, emptying after hymecromone did not change but symptoms were improved. CONCLUSIONS: An abnormal emptying pattern of the gallbladder was identified in patients with acalculous biliary colic, and hymecromone was partly effective to reduce pain, despite a minor effect on gallbladder emptying pattern.

Biliary Tract Diseases↗
PubMed1996

Heteroligation of a mouse monoclonal IgE antibody (La2) with small molecules, analysed by computer-aided automated docking.

A mouse monoclonal anti-TNP IgE antibody (IgE-La2) was screened by a competitive-binding ELISA with a random pool of over 2000 small molecules, mostly drugs, drug derivatives and metabolites. Thirteen of these (naproxene, beta-carboxy-chi-naphthol, oxolinic acid, hymecromone, 8-aminoquinoline, beta-naphthylamine, chi-nitrilo-cinnamic acid, 1,5-diaminonaphthaline, prolonium iodide, diaspirin, 3,4,5-trimethoxy-cinnamic acid, cycrimine, hemimellitic acid) were found to bind as strongly, or stronger, to the antibody as the immunizing hapten. We have used a Monte Carlo search technique for simulated docking of the DNP and non-DNP ligands to a model of the Fv region of IgE(La2). The validity of structural predictions made by the AutoDock program were tested on IgG(ANO2), the three-dimensional structure of which had been obtained previously by X-ray crystallography and 2D-NMR. The rms differences between the experimentally determined and auto-docked complexes in the energetically most favored binding modes were 0.31-0.44 A. Evaluation of structures of IgE(La2)-ligand complexes [including 2,4-dinitrophenol (DNP), 16 DNP amino acids, and the 13 non-DNP ligands listed above] obtained by computer-aided automated docking, suggested the existence of two subsites within an approximately 12 x 18 A2 groove extending between the H and L CDRs. Some of the ligands (DNP-Glu, 8-aminoquinoline, prolonium-I, beta-naphthylamine) were found to bind exclusively to subsite 1, others (DNP-Ala, chi-nitrilo-cinnamic acid, hemimellitic acid, beta-carboxy-chi-naphthol) to subsite 2. The majority of DNP amino acids and other ligands (oxolinic acid, 3,4,5-trimethoxy-cinnamic acid, diaspirin, [R]-cycrimine) were found to occupy an overlapping area including subsites 1 and 2, while some of the compounds (DNP-Asn, DNP-Pro, hymecromone, 1,5-naphthylenediamine) were predicted to interact with either of these subsites with comparable probabilities. When all of the docked La2-ligand complexes were taken into account, five tyrosine residues (H33, L32, L91, L92, L96) were found to provide the majority (53.4%) of all observed contact points. Thus, a multitude of interactions with aromatic residues, and a combinatorial type of interaction within the binding region, seem to be the major factors to explain the mechanism of heteroligation by IgE(La2).

Amino Acid Sequence↗
PubMed2001

New metal complexes of 4-methyl-7-hydroxycoumarin sodium salt and their pharmacological activity.

Complexes of copper (II), zinc (II), nickel (II), cobalt (II) and iron (III) with 4-methyl-7-hydroxycoumarin sodium salt (Mendiaxon, Hymecromone) were synthesized by mixing of equimolar amounts of the respective metal nitrates and 4-methyl-7-hydroxycoumarin sodium salt in water. The complexes were characterized and identified by elemental analysis, conductivities, IR, 1H NMR spectroscopy and mass spectral data. DTA and TGA have been applied to study the compositions of the compounds. Thermal analysis of the complexes indicate the formation of compounds which correspond to the compositions Met(HL)2 x nH2O, where Met = Cu, Zn, Ni, Co; n = 2, 3 or 4 and Fe(HL)3 x 5H2O. The newly synthesized compounds were assayed for acute intraperitoneal and per oral toxicity, influence on blood clotting time and the most active complex was investigated for spasmolytic activity.

Administration, Oral↗
PubMed1987

[The liver and aging. The effect of age on liver function and drug metabolism].

Theophylline (oxidative phase I metabolism) is biotransformed by the liver at an increasingly delayed rate with advancing age. Hymecromone (phase II metabolism) does not display any dependence of glucuronidisation on age. The indocyanine green half-life and the galactose elimination capacity show a highly significant dependence on age. Drugs with flow-limited elimination or mainly oxidative phase I biotransformation should be administered with reduced dosage level while monitoring the serum concentration levels. Drugs that are transformed via phase II reactions usually do not require dosage adjustment.

Adult↗
PubMed1980

[The dynamics of the drug release from tablets. Part 7: Comparison of three liberation models on Cholestil tablets (author's transl)].

The liberation of hymecromone from Cholestil tablets (0.2 g) has been determined by three procedures; half-change method, stationary-basket method, and rotating-basket method. The release rate was highest when determined by the rotating-basket method. The other two methods yielded comparable, but considerably lower values. Artificial gastric and intestinal juices according to the Polish Pharmacopoeia IV have been used in this study.

Chemistry, Pharmaceutical↗
PubMed2001

New lanthanide complexes of 4-methyl-7-hydroxycoumarin and their pharmacological activity.

Complexes of cerium(III), lanthanum(III) and neodymium(III) with 4-methyl-7-hydroxycoumarin (Mendiaxon, Hymecromone) were synthesized by the mixing of equimolar amounts of the respective metal nitrates and 4-methyl-7-hydroxycoumarin sodium salt in water. The complexes were characterized and identified by elemental analysis, conductivities, IR, (1)H and (13)C NMR spectroscopies and mass spectral data. DTA and TGA have been applied to study the compositions of the compounds. The newly synthesized compounds were assayed for acute intraperitoneal and per oral toxicity, influence on blood clotting time and the most active complex was investigated for spasmolytic activity. The complexes of cerium(III) and neodymium(III) showed marginal cytotoxic activity against transformed leukemic cell lines (P3HR1 and THP-1) as compared to the inorganic salts.

Administration, Oral↗
PubMed1988

Pharmacology of the sphincter of Oddi.

The sphincter of Oddi is the smooth muscle connection between the bile duct and the duodenum. Its physiological function is associated with a regular motility characterized by phasic contractions superimposed on the sphincter of Oddi baseline pressure. Recently introduced ERCP-manometry permits further studies of sphincter of Oddi pharmacology. A number of drugs have so far been studied. Sedatives of the diazepam type had no effect on the sphincter, while butylscopolaminium bromide, a typical neurotropic agent, brings about cessation of the sphincter motility for 3-8 minutes. Hymecromon lowered the sphincter baseline pressure from 9.8 to 7.8 mmHg. A 1.2 mg sublingual dose of nitroglycerin, a typical musculotropic agent, caused significant relaxation of the sphincter, and decreased baseline pressure from 8.9 mmHg to 2.9 mmHg; Sphincter motility was not affected. Morphine-like analgetics, in particular pentazocine, elevated sphincter baseline pressure, but buprenorphine and tramadol did not. Pharmacological doses of gastrointestinal hormones also affect the sphincter; CCK octapeptide, glucagon and secretin are able to decrease sphincter of Oddi baseline pressure, and CCK octapeptide abolishes sphincter motility. Sphincter of Oddi pharmacology is of clinical interest. The administration of sphincter-relaxing agents, in particular nitroglycerin and butylscopolaminium bromide, enables the endoscopist to extract small common bile duct stones without previous papillotomy. Analgetics that induce sphincter contraction and thus hinder the flow of bile and pancreatic juice, may be helpful for the treatment of pain in patients with pancreatico-biliary disease. Investigations into the effect of CCK on the healthy and diseased sphincter permit us to identify patients with sphincter dysfunction using a special CCK-provocation test.

Ampulla of Vater↗
PubMed2003

[Effect of vegetotropic pharmacologic preparations of the motor-evacuatory function of the gallbladder in patients with chronic biliary tract pathology].

We examined 74 patients at the age of 18-54 with a chronic bilary pathology, including 50 patients with chronic non-calculous cholecystitis, 16 patients with a gallbladder dysfunction, and 8 patients with cholelithiasis. The differentiated correction of the motor gallbladder dysfunction can be carried out on the basis of the analysis of heart rate variability parameters and results of the gallbladder dynamic sorbite echography against the background of the action of vegetotropic pharmacological preparations (Atropine, Propranolol, Metoclopramide, Hymecromone, Cisapride, Amitriptyline).

Adolescent↗
PubMed1994

[Stenosis of the papilla of Vater--clinical picture and possibilities of therapy].

Stenosis of the ampulla of Vater is encountered in as many as 10% of patients with biliary diseases. In general it is classified as tumourous, inflammatory of functional stenosis. In the clinical picture biliary dyspepsia associated with cholestasis predominates. The cause of functional stenosis of the ampulla of Vater is not known. In the development of inflammatory stenosis most frequently iatrogenic damage of the ampulla during revision of the biliary pathways participates or repeated passage of concrements in cholecystolithiasis. Treatment of tumours of the ampulla of Vater is surgical, treatment of inflammatory stenosis is endoscopic by endoscopic papillotomy. In the treatment of functional stenosis a useful drug is hymecromon, as a rule combined with metoclopramide.

Ampulla of Vater↗
PubMed2000

Cytotoxic activity of cerium complexes with coumarin derivatives. Molecular modeling of the ligands.

Cerium complexes of Umbellipherone, Mendiaxon, Warfarin, Coumachlor, and Niffcoumar have been synthesized by reaction of the ligands with cerium nitrate in a stoichiometric ratio of 1:2. The formation of the complexes has been proved on the basis of elemental analysis, conductivities, IR spectroscopy, and 1H-NMR spectroscopy. The molecules of the ligands were optimized by means of the semiempirical quantum mechanical method PM3 to the energetically most stable conformers. All the ligands were characterized by molecular and submolecular electronic indices and the putative donor centers are proposed. It is concluded that the lactone- and the keto-carbonyl groups of Warfarin, Coumachlor, and Niffcoumar are bonded to the metal ion as bidentate ligands. The other two coumarins are bonded as monodentate ligands. Conductivity measurements show the non-electrolytic nature of the complexes. Cytotoxic screening by MTT assay was carried out. The cerium complexes were found to be more active than the inorganic salts.

4-Hydroxycoumarins↗
PubMed2001

Synthesis, physicochemical characterization, and cytotoxic screening of new zirconium complexes with coumarin derivatives.

Zirconium complexes of mendiaxon, warfarin, coumachlor, and niffcoumar have been synthesized by reaction of the ligands with zirconium chloride in stoichiometric ratio 1:2. The formation of the complexes has been proved on the basis of elemental analysis, IR-spectroscopy, 1H-NMR spectroscopy, and thermal studies. Differential thermal analyses and thermogravimetric analyses have been applied to study the compositions of the new complexes. It is concluded that the lactone- and the keto-carbonyl groups of warfarin, coumachlor, and niffcoumar are bonded to the metal ion as bidentate ligands, but mendiaxon is bonded as monodentate ligand. Cytotoxic screening by MTT-assay was carried out. Among these compounds the zirconium complex of mendiaxon showed highest cytotoxic activity against human promyelocytic leukemic HL-60 cells. The inorganic salt was found to be active against this cell line.

Antineoplastic Agents↗
PubMed2001

A fluorogenic assay using pressure-driven flow on a microchip.

A fluorogenic assay for human T-cell phosphatase (TCPTP) was conducted on an etched glass microchip using pressure driven flow. The TCPTP enzyme catalyzes the removal of a phosphate group from 6,8-difluoro-4-methylumbelliferyl/phosphate (DiFMUP) to produce the fluorogenic product 6,8-difluoro-4-methylumbelliferone (DiFMU). Enzyme assays with real-time on-chip dilution were performed in both low-viscosity (1 cP) buffer and an enzyme solution containing 50% glycerol (6 cP). Single side channels connect a series of reagent wells to a main channel where the fluorescent product of the enzyme reaction passes the detector region. Flow regulation of mixed viscosity fluids requires a pressure control on each arm of the chip contributing to the overall flow. An 8-channel pressure controller was built to regulate the air pressure above all wells feeding channels of the chip, thereby controlling the dilution ratios of buffer, substrate and enzyme. Well pressures maintained a constant concentration of enzyme in the detector channel while adjusting the flow contribution of substrate and buffer. The substrate concentration was stepped over two orders of magnitude while verifying fluid dilutions using marker dyes. The kinetic parameters, Km, Vmax, and Kcat, showed good agreement with the values determined using a standard well plate and fluorometer.

Chromogenic Compounds↗
PubMed1985

The "muscular variant" of Pompe disease: clinical, biochemical and histologic characteristics.

We report on a 2-yr-old boy with progressive muscular weakness and respiratory failure. There was no clinical evidence of heart muscle involvement. Autopsy showed marked intralysosomal glycogen deposition in skeletal muscle and liver with no histological evidence of glycogen deposition in cardiac muscle. The activity of the lysosomal enzyme alpha-1,4-glucosidase was deficient in skin fibroblasts, skeletal muscle, cardiac muscle, and liver; however, the enzymatic activity in peripheral blood leukocytes was in the low normal range. The child's mother had normal enzymatic activity in leukocytes but heterozygote levels in skin fibroblasts.

Child, Preschool↗
PubMed1987

Gaucher disease: accurate identification of asymptomatic French-Canadian carrier using nonlabeled authentic sphingolipid substrate N-palmitoyl dihydroglucocerebroside.

Gaucher disease is an autosomal recessive sphingolipidosis associated with deficient glucocerebroside beta-glucosidase activity. It is a panethnic metabolic disorder, but the carrier frequency is particularly high among Ashkenazi Jews (estimated between 1:12-1:25). In order to establish a reliable and convenient biochemical assay method for differentiating asymptomatic Gaucher carriers from normal individuals, glucocerebroside beta-glucosidase activity was determined in peripheral blood lymphocytes and cultured skin fibroblasts of 11 Gaucher obligate heterozygotes using the authentic nonlabeled sphingolipid substrate N-palmitoyl dihydroglucocerebroside and the artificial fluorogenic substrate 4-methylumbelliferyl-beta-D-glucopyranoside (4MUGP). The level of lymphocyte beta-glucosidase activity on the glucocerebroside substrate was observed to range from 42-65% of that of the control mean, and there was no overlap of enzyme activity between the Gaucher heterozygotes and controls. However, when the artificial fluorogenic substrate 4MUGP was used, the level of beta-glucosidase activity in 2 of the Gaucher obligate heterozygotes was noted to overlap with that of the control individuals. Contrary to findings in the lymphocytes, cultured skin fibroblasts appear to be a reliable enzyme source for Gaucher carrier detection even when the artificial fluorogenic 4MUGP substrate was used, as the level of beta-glucosidase activity in all of the Gaucher obligate heterozygotes tested was intermediate and distinctly separated from that of the control persons. Using the lymphocyte glucocerebroside beta-glucosidase assay and fibroblast 4MUGP beta-glucosidase assay methods, we identified the carrier status in 3 other relatives and ruled it out in 4 others. These data suggest that nonlabeled glucocerebroside is a reliable and highly specific substrate for either lymphocyte or fibroblast beta-glucosidase activity assay in identifying asymptomatic Gaucher carriers. Use of the 4MUGP substrate for differentiating Gaucher heterozygotes from control persons, on the other hand, should be restricted to the fibroblast enzyme assay method, as considerable overlap of enzyme activity was noted in lymphocytes.

Adult↗
PubMed1980

The role of epithelial collagen and proteoglycan in the initiation of osteogenesis by avian neural crest cells.

Osteogenesis was inhibited when mandibular processes from 3 1/2-day-old embryos were cultured in BUdR, LACA, alpha, alpha'-Dipyridyl, 4-Methylumbelliferone, and 4-Methylumbelliferyl-beta-D-glucoside or beta-D-xyloside. Mandibular processes were then cultured in the test substances for 3 days, enzymatically separated into their epithelial and ectomesenchymal components, combined with mandibular components from untreated embros, and either organ-cultured or grafted to chorioallantoic membranes of host embryos. Osteogenesis was inhibited when treated epithelium, but not when treated ectomesenchyme, was present in the tissue recombinations. Analysis of the known action of these inhibitors indicates that proliferation, hydroxylation of collagen, and synthesis of proteoglycans by epithelial cells are all necessary components of this osteogenic epithelial-ectomesenchymal interaction.

2,2'-Dipyridyl↗
PubMed2004

Effects of beta-estradiol and propofol on the 4-methylumbelliferone glucuronidation in recombinant human UGT isozymes 1A1, 1A8 and 1A9.

The effects of beta-estradiol and propofol on human UGT1A1, 1A8 and 1A9 activities were investigated using 4-methylumbelliferone (4-MU) as a substrate for glucuronidation. The formation of 4-MU glucuronide (4-MUG) from 4-MU, in recombinant human UGT 1A1, 1A8 and 1A9 was determined using HPLC with fluorescence detection. The glucuronidation activity of 4-MU was the highest in UGT1A9 with an apparent K(m) value of 8.3 microM, while that in UGT1A1 and 1A8 was linear to at least 100 microM. beta-estradiol had potent inhibitory effects on UGT1A9 as well as on UGT1A1 with IC(50) values of 2.1 and 7.2 microM, respectively. Propofol inhibited UGT1A9 activity with an IC(50) of 55 microM, while the IC(50) value was much higher for UGT1A8. In contrast, beta-estradiol and propofol activated 4-MU glucuronidation in UGT1A1 and 1A8, respectively. This study therefore indicates that the use of beta-estradiol as a specific inhibitor for UGT1A1 should be used with care in the identification of UGT isozymes responsible for glucuronidation in human liver microsomes.

Cells, Cultured↗