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At least 289 records · Page 16Linked to original sources
PubMed1995

Catabolism of indole-3-acetic acid and 4- and 5-chloroindole-3-acetic acid in Bradyrhizobium japonicum.

Some strains of Bradyrhizobium japonicum have the ability to catabolize indole-3-acetic acid. Indoleacetic acid (IAA), 4-chloro-IAA (4-Cl-IAA), and 5-Cl-IAA were metabolized to different extents by strains 61A24 and 110. Metabolites were isolated and analyzed by high-performance liquid chromatography and conventional mass spectrometry (MS) methods, including MS-mass spectroscopy, UV spectroscopy, and high-performance liquid chromatography-MS. The identified products indicate a novel metabolic pathway in which IAA is metabolized via dioxindole-3-acetic acid, dioxindole, isatin, and 2-aminophenyl glyoxylic acid (isatinic acid) to anthranilic acid, which is further metabolized. Degradation of 4-Cl-IAA apparently stops at the 4-Cl-dioxindole step in contrast to 5-Cl-IAA which is metabolized to 5-Cl-anthranilic acid.

Chromatography, High Pressure Liquid↗
PubMed1994

Morphological diversity of Blastocystis hominis in sodium acetate-acetic acid-formalin-preserved stool samples stained with iron hematoxylin.

The objective of this investigation was to study the morphological characteristics of Blastocystis hominis in sodium acetate-acetic acid-Formalin-preserved stool samples. Routinely processed samples were examined for morphological detail, including size, shape, nuclear detail, and central body characteristics. Morphological findings revealing the importance of recognizing B. hominis in the diagnostic laboratory are described.

Animals↗
PubMed1999

Octreotide acetate long-acting formulation versus open-label subcutaneous octreotide acetate in malignant carcinoid syndrome.

PURPOSE: Subcutaneous (SC) octreotide acetate effectively relieves the diarrhea and flushing associated with carcinoid syndrome but requires long-term multiple injections daily. A microencapsulated long-acting formulation (LAR) of octreotide acetate has been developed for once-monthly intramuscular dosing. PATIENTS AND METHODS: A randomized trial compared double-blinded octreotide LAR at 10, 20, and 30 mg every 4 weeks with open-label SC octreotide every 8 hours for the treatment of carcinoid syndrome. Seventy-nine patients controlled with treatment of SC octreotide 0.3 to 0.9 mg/d whose symptoms returned during a washout period and who returned for at least the week 20 evaluation constituted the efficacy-assessable population. RESULTS: Complete or partial treatment success was comparable in each of the four arms of the study (SC, 58.3%; 10 mg, 66.7%; 20 mg, 71.4%; 30 mg, 61.9%; P> or =.72 for all pairwise comparisons). Control of stool frequency was similar in all treatment groups. Flushing episodes were best controlled in the 20-mg LAR and SC groups; the 10-mg LAR treatment was least effective in the control of flushing. Treatment was well tolerated by patients in all four groups. CONCLUSION: Once octreotide steady-state concentrations are achieved, octreotide LAR controls the symptoms of carcinoid syndrome at least as well as SC octreotide. A starting dose of 20 mg of octreotide LAR is recommended. Supplemental SC octreotide is needed for approximately 2 weeks after initiation of octreotide LAR treatment. Occasional rescue SC injections may be required for possibly 2 to 3 months until steady-state octreotide levels from the LAR formulation are achieved.

Carcinoid Tumor↗
PubMed1984

Pulmonary and percutaneous absorption of 2-propoxyethyl acetate and 2-ethoxyethyl acetate in beagle dogs.

A comparison was made of the absorption and elimination rates of 2-propoxyethyl acetate (PEA) and 2-ethoxyethyl acetate (EEA) following inhalation, dermal application or IV administration. Male beagle dogs were exposed to 50 ppm PEA or EEA for 5 hr, and breath samples were collected during the exposure and a 3-hr recovery period. Both compounds were rapidly absorbed through the lungs. After 10 min of exposure, the concentrations of the parent compounds in the expired breath were 5 to 10 ppm (80-90% absorption) and reached plateau values at about 3 hr of 13 ppm for PEA (74% absorption) and 16 ppm for EEA (68% absorption). Post-exposure breath samples declined exponentially to 0.5 ppm and 2 ppm after 3 hr for PEA and EEA, respectively. Expired concentrations of PEA were slightly, but significantly (p less than 0.025), lower than those of EEA at corresponding times during the exposure. After IV dosing with 1 mg/kg [ethyl-1,2-14C]PEA, the urine contained 61% and 88% of the dose in 4 and 24 hr, respectively. [14C]EEA was eliminated more slowly, with 20% and 61% of the dose appearing in the urine in 4 and 24 hr, respectively. Blood elimination half-lives were 1.6 hr for [14C]PEA and 7.9 hr for [14C]EEA. Only trace amounts of 14CO2 (less than 1%) or volatile materials (less than 0.1%) were detected in the expired air with either compound. For studies of percutaneous absorption, [14C]PEA or [14C]EEA was added to undiluted compound and applied in a glass cell to a shaved area on a dog's thorax for 30 or 60 min.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Topical↗
PubMed1977

Changes in insulin receptor concentration in rat fat cells following treatment with the gestagens clomegestone acetate and cyproterone acetate.

Specific insulin receptors were measured in isolated fat cells of rats after treatment with clomegestone acetate. Under conditions when peripheral insulin insensitivity was observed, the number of insulin receptors was simultaneously reduced. A similar though smaller decrease in insulin receptor concentration was seen in rats after treatment with cyproterone acetate, a compound which did not cause insulin resistance. It is concluded that the gestagenic compounds tested decrease insulin receptor concentration. Only drastic reduction of the number of binding sites results in significant perturbations of carbohydrate metabolism.

Adipose Tissue↗
PubMed1983

Metabolism of the anti-tumour drugs N2-methyl-9-hydroxyellipticinium acetate (NSC 264137) and N2-methyl-9-hydroxyolivacinium acetate in the rat: preliminary identification of biliary 9-(O)-glucuronide and 10-(S)-glutathione conjugates.

The metabolites of the two anti-tumour drugs, N2-methyl-9-hydroxyellipticinium acetate (9-OH-NME, NSC 264137) and N2-methyl-9-hydroxyolivacinium acetate (9-OH-NMO), in bile of i.v.-treated rats have been studied. Three products have been identified in the bile: the unmetabolized drug (17% excreted products for ellipticinium, 3% for olivacinium derivative); a major metabolite, the corresponding 9-(O)-glucuronide (80 and 96%, respectively) and a minor metabolite, a possible 10-(S)-glutathione conjugate (3 and 1%). The elimination yield of these three products excreted over a period of 12 h represents 36% (ellipticinium) and 74% (olivacinium) of the administered dose. The detection of glucuronide and glutathione conjugates of these pyridinium derivatives was possible by direct injection of bile on to h.p.l.c. without prior extraction with organic solvents, in which these polar metabolites are poorly soluble. Metabolites were tentatively identified by the comparison of h.p.l.c. behaviour (retention times and u.v. absorption ratios) with those of reference samples. Reference conjugates have been prepared by chemical synthesis for the 9-(O)-glucuronides and by biosynthesis for the 10(S)-glutathione derivatives. The detection of the GSH conjugates in bile can be considered as the first experimental evidence of the involvement of oxidative activation in vivo of these ellipticine and olivacine derivatives.

Alkaloids↗
PubMed1979

Analysis of some older Scandinavian formulations of 2,4-dichlorophenoxy acetic acid and 2,4,5-trichlorophenoxy acetic acid for contents of chlorinated dibenzo-p-dioxins and dibenzofurans.

Ten samples of older formulations of 2,4,5-trichlorophenoxy acetic acid and 2,4-dichlorophenoxy acetic acid used in Sweden were analyzed for chlorinated dibenzo-p-dioxins and dibenzofurans. The analyses were performed with gas chromatography/mass spectrometry with a high resolution glass capillary column for maximum isomeric separation and sensitivity. The detection limit was 0.01-0.05 ppm. The amounts of contaminants were of the same order of magnitude as that found earlier in European samples with later production dates (late 1960s and 1970s).

2,4,5-Trichlorophenoxyacetic Acid↗
PubMed2000

[Treatment of pelvic endometriosis with goserelin acetate or nafarelin acetate. Comparative study].

The medical treatment of the pelvic endometriosis includes the hormonal therapy that attacks directly to the endometriosis lesions or indirectly it inhibits the endometrial proliferation and it induces atrophy through the estrogenic deprivation, or to inclination of a combination of these effects. The objective of the present study was to evaluate the effects of two gonadotrophin release analogs in the treatment of the endometriosis. 15 patients were studied in who the diagnosis settled down of endometriosis by means of laparoscope; these were formed two groups in aleatory form and there were administered to each one them nafarelin acetate in dose of 200 or 400 micrograms each 12 hours or goserelin acetate in dose of 3.6 mg every 21 days; the serum levels of the stimulating follicle, luteinizing, estradiol and prolactin hormones were determined at intervals of four weeks and the secondary effects of these drugs were reported. There were carried out a second look laparoscope in 10 patients. The statistical analysis was carried out by means of the test of hypothesis of Wilcoxon and X2. Inside those results were found that as much the nafarelin as the Goserelin are able to diminish the gonadotropins and estradiol serum levels. Both analogs are effective for the control of the endometriotic lesions. The secondary symptoms are smaller and better supported by the patients using nafarelin. In conclusion as much the nafarelin as the goserelin are appropriate medications for the treatment of the pelvic endometriosis and the election between one or another one can settle down for the comfort of application, secondary effects and cost.

Antineoplastic Agents, Hormonal↗
PubMed1992

Compared kinetics of 2-(2,3-dihydro-5-acetoxy-4,6,7-trimethylbenzofuranyl) acetic acid (IRFI 016) and its active metabolite 2-(2,3-dihydro-5-hydroxy-4,6,7-trimethylbenzofuranyl) acetic acid (IRFI 005) in plasma and bronchial alveolar liquid in mice.

The concentration of 2-(2,3-dihydro-5-acetoxy-4,6,7-trimethylbenzofuranyl) acetic acid (IRFI 016) and its active metabolite 2-(2,3-dihydro-5-hydroxy-4,6,7-trimethylbenzofuranyl) acetic acid (IRFI 005) in bronchial alveolar liquid (BAL) and plasma of mice were studied. IRFI 016 and its active metabolite IRFI 005 are both present in BAL and plasma after oral administration of IRFI 016. In BAL no delay times were noted, in comparison with plasma, regarding Cmax time nor significant variation of t1/2 and the elimination constant (Kel). IRFI 016, orally administered, is very rapidly absorbed and, both in unaltered form and as its active metabolite, reaches the anatomic site where it carries out its principal pharmacological activity, according to the same kinetic course observed in plasma.

Administration, Oral↗
PubMed1992

[Effects of valerian root oil, borneol, isoborneol, bornyl acetate and isobornyl acetate on the motility of laboratory animals (mice) after inhalation].

The aromatherapeutical use of commercial valerian root oil (Chinese origin) and of pure fragrance compounds--borneol, isoborneol, bornyl acetate (main constituent of the proved valerian root oil) and isobornyl acetate--as potentially drugs with sedative effects after inhalation was investigated in an animal experiment (mice). In additional analyses the mice were treated i.p. by caffeine and distinct sedative effects were observed only by inhalation of the cited substances.

Animals↗
PubMed1990

Evidence for the production of nitric oxide by activated macrophages treated with the antitumor agents flavone-8-acetic acid and xanthenone-4-acetic acid.

Activated peritoneal macrophages, obtained from mice pretreated with Bacillus Calmette-Guérin, after exposure in vitro to flavone-8-acetic acid (FAA; NSC 347512) at a concentration of 890 microM, produce nitrite (3.7 nmol/10(6) cells), as measured 20 h later by the Griess reaction. Stimulation of nitrite production was inhibited at least 90% by NG-monomethylarginine (125 microM), suggesting that nitrite was formed via nitric oxide as a product of arginine metabolism. Stimulation was only partially inhibited by dexamethasone (0.1 microM). The ability of xanthenone-4-acetic acid (XAA) and three of its analogues to stimulate nitrite production was also investigated. 5,6-Dimethyl-XAA stimulated nitrite production (12.6 nmol/10(6) cells) at an optimal concentration of 80 microM, 8-methyl-XAA was without effect, and XAA and 5-methyl-XAA showed intermediate activity. The optimal in vitro drug concentrations for stimulation by FAA, XAA, and active XAA analogues correlated with the optimal in vivo dose required for the induction of either hemorrhagic necrosis or growth delay of s.c. Colon 38 tumors. These results strongly imply that FAA and active XAA derivatives function as low molecular weight stimulators of nitric oxide formation in macrophages, possibly acting on the same differentiation pathway as do endotoxin and tumor necrosis factor alpha. We suggest that nitric oxide, which is known to be toxic to tumor cells, contributes to the cytotoxic action of FAA and its analogues.

Animals↗
PubMed1979

Studies on the derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. I. Syntheses and pharmacological analysis of acylderivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

A number of new acyl and imidoderivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid (II) and its methyl ester (VII) were synthesized. Methyl ester VII heated in benzene solution with acid anhydrides was transformed into adequate acyl derivatives (VIII, IX, X, XIII, XVI). Some of them (X, XIII, XVII) by heating with acetic anhydride underwent cyclization and were transformed into the imido derivatives (XI, XIV, XVIII). Compounds XI, XIV and XVI heated with diluted aqueous solution of sodium hydroxide underwent selective hydrolysis giving the respective dicarboxylic acids XII, XV, XVII. Pharmacological analysis revealed that some of the synthesized preparations exert an anti-inflammatory effect and allow to draw limited relations between chemical structure and pharmacological activity in this group of compounds.

Analgesia↗
PubMed1983

Liquid-chromatographic determination of indole-3-acetic acid and 5-hydroxyindole-3-acetic acid in human plasma.

We describe a "high-performance" reversed-phase liquid-chromatographic method for determination of indole-3-acetic acid (I) and 5-hydroxyindole-3-acetic acid (II) in human plasma. I is eluted at 1.0 mL/min with a mixture of 1-pentanesulfonic acid (pH 3.1), methanol, and water. It is detected by fluorometry. A mixture of citric acid/sodium phosphate solution (pH 4.8) and methanol, at 1.5 mL/min, is used to elute II, which is detected with an electrochemical cell. Platelet-poor plasma samples were pretreated with HCl, perchloric acid, and trichloroacetic acid for protein precipitation. Best results were obtained with the last (protein precipitation is incomplete with HCl, while recoveries of I are concentration dependent with perchloric acid). Analytical recoveries were 58% (SD 3.1%, CV 5.3%, n = 12) and 79% (SD 3.3%, CV 5.3%, n = 9) for I and II, respectively. Concentrations of I and II in plasma ranged from 0.61 to 3.32 (mean 1.54, SD 0.59, n = 15) mumol/L and from 33.0 to 102.6 (mean 51.8, SD 20.1, n = 16) nmol/L, respectively.

Adult↗
PubMedDate not supplied

The efficacy of nafarelin acetate versus leuprolide acetate in conjunction with human menopausal gonadotropins for superovulation/intrauterine insemination.

OBJECTIVE: To compare the use of two gonadotropin-releasing hormone agonists, nafarelin acetate (NA) and leuprolide acetate (LA), in conjunction with human menopausal gonadotropins (hMG)/human chorionic gonadotropin (hCG) and intrauterine insemination (IUI). DESIGN: Retrospective analysis of selected patient records. Patients were assigned to treatment groups systematically, but not randomly. Fixed rules were used for selection of medical records, but the study was not blinded. SETTING: University medical center ovulation induction program. PATIENTS AND INTERVENTIONS: Fifteen NA/hMG/IUI cycles were analyzed in comparison with 15 contemporary LA/hMG/IUI cycles. RESULTS: There were no differences in: the number of days to ovarian suppression, the number of ampules of hMG required, the number of 17-mm preovulatory follicles, or the mean peak estradiol levels. However, the minimum estradiol levels at the height of ovarian suppression by GnRH agonist were lower in the LA group than in the NA group. Furthermore, 4/15 NA cycles resulted in pregnancy compared with 0/15 LA cycles. CONCLUSIONS: NA is, at the least, comparable to LA in effecting pregnancy after superovulation/IUI.

Adult↗
PubMed1994

Induction of tumor necrosis factor-alpha messenger RNA in human and murine cells by the flavone acetic acid analogue 5,6-dimethylxanthenone-4-acetic acid (NSC 640488).

The investigational antitumor agent, 5,6-dimethylxanthenone-4-acetic acid (5,6-MeXAA; NSC 640488) induced greater expression of tumor necrosis factor-alpha (TNF-alpha) mRNA in murine spleen cells in vivo at its optimal dose of 27.5 mg/kg than flavone acetic acid (FAA; NSC 347512) at its optimal dose of 220 mg/kg. Up-regulation of TNF-alpha mRNA was obtained using 5,6-MeXAA in vitro in cultures of murine splenocytes, the murine J774 macrophage cell line, and the human HL-60 myelomonocytic leukemia cell line. Maximal induction occurred at a 5,6-MeXAA concentration of 200 micrograms/ml for both murine J774 and human HL-60 cells. A direct comparison of FAA and 5,6-MeXAA (100-600 micrograms/ml) to stimulate TNF-alpha mRNA in HL-60 cells showed activity by 5,6-MeXAA at all doses but minimal activity with FAA. The results demonstrate that 5,6-MeXAA is equally potent in up-regulating TNF-alpha mRNA in human and murine cells of the monocyte/macrophage lineage, whereas FAA has demonstrable activity in murine cells only. The results suggest that 5,6-MeXAA would be a more active clinical agent than FAA because TNF-alpha induction appears to be a critical factor in the antitumor effects of this class of compounds.

Animals↗