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PubMed1978

Methanogenesis from acetate: a nonmethanogenic bacterium from an anaerobic acetate enrichment.

A methanogenic acetate enrichment was initiated by inoculation of an acetate-mineral salts medium with domestic anaerobic digestor sludge and maintained by weekly transfer for 2 years. The enrichment culture contained a Methanosarcina and several obligately anaerobic nonmethanogenic bacteria. These latter organisms formed varying degrees of association with the Methanosarcina, ranging from the nutritionally fastidious gram-negative rod called the satellite bacterium to the nutritionally nonfastidious Eubacterium limosum. The satellite bacterium had growth requirements for amino acids, a peptide, a purine base, vitamin B12, and other B vitamins. Glucose, mannitol, starch, pyruvate, cysteine, lysine, leucine, isoleucine, arginine, and asparagine stimulated growth and hydrogen production. Acetate was neither incorporated nor metabolized by the satellite organism. Since acetate was the sole organic carbon source in the enrichment culture, organism(s) which metabolize acetate (such as the Methanosarcina) must produce substrates and growth factors for associated organisms which do not metabolize acetate.

Acetates↗
PubMed1998

Leuprorelin acetate blood levels and dialysance after the administration of sustained-release leuprorelin acetate in a dialysis case complicated by prostate cancer.

BACKGROUND: The objective of this study is to determine whether in a dialysis patient with prostate cancer leuprorelin acetate blood levels were abnormally high or low due to kidney failure or because of dialysis. METHODS: Sustained-release leuprorelin acetate 3.75 mg was given every 4 weeks for prostate cancer in a 79-year-old dialysis patient. Changes in serum level of leuprorelin acetate in this patient were measured before and after dialysis. RESULTS: Leuprorelin acetate appeared to have a dialysance close to that of vitamin B12, which has a similar molecular weight. The amount dialyzed did not exceed 8.3% of the amount released per day. Mean blood levels of leuprorelin acetate, as measured in this patient, were higher (0.64 to 1.31 ng/ml) than those in prostate cancer patients with normal kidney function (mean +/- SD, 0.24 +/- 0.12 to 0.50 +/- 0.32 ng/ml). CONCLUSIONS: Sustained-release leuprorelin acetate can be used safely in dialysis patients with prostate cancer.

Aged↗
PubMed1989

Preparation and properties of (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl- (R)-(+)-alpha-hydroxy-alpha-(4-[125I]iodophenyl)-alpha-phenyl acetate and (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(S)-(-)-alpha-hydroxy-alpha- (4-[125I]iodophenyl)-alpha-phenyl acetate as potential radiopharmaceuticals.

rac-4-Nitrobenzilic acid was synthesized and resolved with quinidine and quinine to give the corresponding (R)- and (S)-salts. The resolved diastereomeric salts were converted to (R)- and (S)-4-nitrobenzilic acids and subsequent esterification gave their corresponding ethyl esters. Transesterification with (R)-(-)-3-quinuclidinol afforded (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(R)-(+)-alpha-hydroxy-alpha- (4-nitrophenyl)-alpha-phenyl acetate and (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(S)-(-)-alpha-hydroxy- alpha-(4-nitrophenyl)-alpha-phenyl acetate. After hydrogenation, the (R,R)- and (R,S)-amines were converted to the respective triazene derivatives. The triazene derivatives reacted with sodium [125I]iodide to give (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(R)-(+)- alpha-hydroxy-alpha-(4-[125I]iodophenyl)-alpha-phenyl acetate and (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(S)-(-)-alpha-hydroxy- alpha-(4-[125I]iodophenyl)-alpha-phenyl acetate. The evaluation of their affinities to muscarinic acetylcholine receptors (MAcChR) shows that (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(S)-(-)-alpha-hydroxy-alpha-(4- [125I]iodophenyl)-alpha-phenyl acetate exhibits an affinity for the MAcChR from corpus striatum that is approximately threefold lower than that of (R)-(-)-1-azabicyclo[2.2.2]oct-3-yl-(R)-(+)-alpha-hydroxy-alpha-(4- [125I]iodophenyl)-alpha-phenyl acetate.

Animals↗
PubMed1985

Ferric acetate-uranium acetate reagent in cholesterol estimations in plasma and high density lipoprotein fractions: comparison with existing methods.

The use of ferric acetate-uranium acetate colour reaction for the estimation of cholesterol in the supernatants of plasma samples after precipitation of low density lipoprotein (LDL) and very low density lipoprotein (VLDL) cholesterol by heparin-MnCl2 was assessed and compared with the conventional method using the FeCl3 colour reaction and also with the method using o-phthalaldehyde as the colouring reagent. All three methods gave comparable values when total cholesterol in plasma samples was determined and also when high density lipoprotein (HDL) fractions were separated by ultracentrifugation and the cholesterol contents determined. But when heparin-MnCl2 precipitation was used for HDL separation, and the cholesterol content determined, the FeCl3 method gave significantly lower values. This could be due to interference of the cholesterol colour reaction with FeCl3, due to Mn2+ ions present in the supernatant. Addition of Mn2+ to cholesterol standards and subsequent colour development with ferric acetate-uranium acetate and FeCl3 reagents showed that Mn2+ decreased the absorbancy of the coloured complex at 560 nm only when FeCl3 was used. Percentage recovery of added cholesterol was also lower when the heparin-MnCl2 supernatant was treated with FeCl3 reagent for colour development. Use of ferric acetate-uranium acetate reagent provides a simpler and quicker method. It does not suffer from interference due to the presence of Mn2+ ions and gives results comparable to the o-phthalaldehyde method and those using ultracentrifugation as the separation procedure.

Chemical Precipitation↗
PubMed2005

Comparison of embryo implantation in Wistar rats that underwent ovarian stimulation using exogenous gonadotropins associated with cetrorelix acetate or leuprolide acetate.

OBJECTIVE: To compare embryo implantation in Wistar rats submitted to ovarian stimulation using recombinant FSH (rFSH) with cetrorelix acetate or leuprolide acetate. DESIGN: Experimental study. SETTING: Faculty of medicine animal facility. PATIENT(S): Fifty-six female Wistar rats with normal estrus cycles and 30 male. INTERVENTION(S): Ovarian stimulation and laparotomy (by the day 13 of gestation). MAIN OUTCOME MEASURE(S): Embryo implantation. RESULT(S): The female rats were subdivided into four groups: group 1, medicated with rFSH, hCG, and cetrorelix acetate; group 2, medicated with rFSH, hCG, and leuprolide acetate; group 3, medicated with rFSH and hCG; and group 4, in which only saline solution was administered. The female rats were mated with fertile male rats on the day of hCG administration with copulation confirmed through cytologic vaginal analysis. The females were killed on the 13th day of gestation. After laparotomy, comparison and identification was done regarding the numbers of corpora lutea and embryo implantations and gestation rates. Group 1 presented lower numbers of corpora lutea and embryo implantations in comparison to the other groups (P<.05). A difference was not found in the gestation rates between the groups. CONCLUSION(S): The number of embryo implantations in Wistar rats medicated with rFSH and cetrorelix acetate is lower than that of rats medicated with rFSH and leuprolide acetate.

Animals↗
PubMed1995

Subcutaneous low dose leuprolide acetate depot versus leuprolide acetate for women undergoing ovarian stimulation for in-vitro fertilization.

A total of 100 women undergoing ovarian stimulation with gonadotrophin-releasing hormone agonist (GnRHa) and a human menopausal gonadotrophin (HMG) for in-vitro fertilization (IVF) participated in this randomized comparative study. Leuprolide acetate at a dose of 0.5 mg/day s.c. (n = 52, group I), or low-dose leuprolide acetate depot at a dose of 1.88 mg s.c. (n = 48, group II), was started on days 21-23 of the cycle. Stimulation with 225 IU/day HMG was started after pituitary desensitization had been achieved. The luteal phase was supported by human chorionic gonadotrophin (HCG) i.m. injection. There were no statistical differences in baseline oestradiol (24.5 +/- 4.8 versus 21.9 +/- 4.5 pg/ml) and follicle stimulating hormone (FSH) concentrations (3.9 +/- 1.9 versus 3.2 +/- 1.8 mIU/ml), and concentrations on the day of HCG administration of oestradiol (1657 +/- 245 versus 1512 +/- 165 pg/ml), luteinizing hormone (LH; 6.2 +/- 4.8 versus 5.6 +/- 4.3 mIU/ml) and FSH (10.6 +/- 2.8 versus 10.8 +/- 3.6 mIU/ml). There were also no statistical differences in the HMG dosage (26.8 +/- 1.8 versus 28.5 +/- 1.5), the number of oocytes retrieved (7.6 +/- 3.0 versus 8.1 +/- 4.3), the number of oocytes fertilized (5.3 +/- 2.1 versus 5.6 +/- 3.0) and the number of embryos transferred (3.5 +/- 1.3 versus 3.4 +/- 1.6). There was no evidence of a premature LH surge in either group, but two patients appeared to have a poor response in the leuprolide acetate group (group I). There were 11 pregnancies (21.2%) after the use of leuprolide acetate and 12 pregnancies (25.0%) in those given leuprolide acetate depot; no statistical difference existed between these two groups. Thus, a s.c. low-dose leuprolide acetate depot injection may offer a useful alternative for pituitary suppression in ovarian stimulation for IVF.

Adult↗
PubMed1994

A prospective randomized comparison of two gonadotrophin-releasing hormone agonists, nafarelin acetate and buserelin acetate, in in-vitro fertilization-embryo transfer.

We tested the efficacy of a new gonadotrophin-releasing hormone agonist (GnRHa), nafarelin acetate, in in-vitro fertilization (IVF), and compared the results with those of another widely used GnRHa, buserelin acetate; both were in the form of nasal spray. Therapy was used in a long protocol in the luteal phase in two groups of women with similar aetiology of infertility. There was no significant difference in patient response, measured by cycle cancellation, number of oocytes retrieved, fertilization rate and cleavage rate. Pregnancy rates were similar in nafarelin acetate and buserelin acetate treated women, namely 22% and 24% pregnancies per cycle, and 28.8% and 32.1% pregnancies per transfer, respectively. Side-effects were few and comparable in both groups. The only difference noted was that women receiving nafarelin acetate required significantly fewer ampoules of human menopausal gonadotrophin, making a significant difference in the expense involved. We conclude that on the basis of our experience, nafarelin acetate is an efficient and safe gonadotrophin-releasing hormone agonist, effective in IVF therapy.

Administration, Intranasal↗
PubMed2002

Melaminium acetate acetic acid solvate monohydrate.

The crystals of the title new melaminium salt, 2,4,6-triamino-1,3,5-triazin-1-ium acetate acetic acid solvate monohydrate, C(3)H(7)N(6)(+).CH(3)COO(-).CH(3)COOH.H(2)O, are built up from singly protonated melaminium residues, acetate anions, and acetic acid and water molecules. The melaminium residues are interconnected by N-H...N hydrogen bonds to form chains along the [010] direction. These chains of melaminium residues form stacks aligned along the a axis. The acetic acid molecules interact with the acetate anions via the H atom of their carboxylic acid groups and, together with the water molecules, form layers that are parallel to the (001) plane. The oppositely charged moieties interact via multiple N-H...O hydrogen bonds that stabilize a pseudo-two-dimensional stacking structure.

Journal Article↗
PubMed1992

Structure-activity relationships for substituted 9-oxo-9,10-dihydroacridine-4-acetic acids: analogues of the colon tumour active agent xanthenone-4-acetic acid.

A series of 9-oxo-9,10-dihydroacridine-4-acetic acids (acridone-4-acetic acids) were prepared by Jourdan-Ullmann condensation of 2-halobenzoic acids with 2-aminophenylacetic acids, followed by H2SO4-induced cyclodehydration of the resulting 2-[2-(carboxymethyl)phenylamino]benzoic acids. These were evaluated for their ability to induce haemorrhagic necrosis in transplanted colon 38 tumours in mice, using a short-term histology assay. The results broadly paralleled those seen previously for xanthenone-4-acetic acids, with 1-, 2- and 7-substitution being dystherapeutic, and substitution at the 5- and 6-positions by lipophilic groups increasing activity. While some analogues were as active as xanthenone-4-acetic acids in the histology assay and gave significant growth delays against colon 38 tumours in vivo, as a class the 9-oxo-9,10-dihydroacridine-4-acetic acids were generally less potent than the xanthenone-4-acetic acids.

Animals↗
PubMedDate not supplied

Reverse-phase liquid chromatographic determination of dexamethasone acetate and cortisone acetate in bulk drug substance and dosage forms: collaborative study.

A reverse-phase liquid chromatographic method for determination of dexamethasone acetate and of cortisone acetate was subjected to an interlaboratory study by 8 collaborators for each steroid acetate. Bulk drug substance, suspensions, and tablets were assayed. Bulk drug or dosage form is dissolved in an acetonitrile-buffer mixture and analyzed by an external standard method. The steroid acetate is resolved from extraneous components by reverse-phase chromatography and detected at 254 nm. The sample solutions are stable for at least 72 h. For dexamethasone acetate, coefficients of variation were 0.9 and less than or equal to 3.1% for the bulk drug substance and the suspensions, respectively. For cortisone acetate, coefficients of variation were 0.7% for bulk material, less than or equal to 2.0% for suspensions, and less than or equal to 2.5% for tablets. All dosage forms were commercial formulations. The 2 methods have been adopted official first action.

Chromatography, Liquid↗
PubMed1994

Identification and characterization of the ackA (acetate kinase A)-pta (phosphotransacetylase) operon and complementation analysis of acetate utilization by an ackA-pta deletion mutant of Escherichia coli.

The pta gene encoding phosphotransacetylase was cloned on a high copy plasmid with or without the ackA gene encoding acetate kinase in Escherichia coli. The acetate kinase and phosphotransacetylase were overproduced in cells harboring the plasmid possessing both genes. Nucleotide sequencing of the pta gene revealed that it is able to produce a polypeptide comprising 714 amino acid residues, which starts at 70 base pairs downstream from the stop codon of the ackA gene. The 77-kDa protein band of overproduced phosphotransacetylase was observed on SDS-polyacrylamide gel electrophoresis, of which the amino terminal sequence corresponds to that of the deduced polypeptide without the amino terminal methionine. Two transcripts of pta of different sizes were found in the cells. A 3,700 nucleotide transcript, which covers the ackA and pta genes, seemed to be produced by the first promoter in the operon and a 2,300 nucleotide transcript, which covers just pta, seemed to be produced by the second promoter. In a synthetic medium containing acetate as the sole carbon source, the growth of an ackA-pta double mutant was greatly impaired. Complementation analyses revealed that both the acetate kinase and phosphotransacetylase were required for the rapid growth in the acetate medium.

Acetate Kinase↗
PubMed1989

Capillary gas-liquid chromatographic/mass spectrometric measurement of plasma acetate content and (2-13C) acetate enrichment.

In studies where (2-13C)acetate is employed as isotopic tracer in vivo, we have reported a selected ion monitoring gas-liquid chromatographic/mass spectrometric method which allows plasma tracer enrichment as well as plasma acetate content to be determined in the same 200-500 microliters sample through the use of methacrylic acid as the assay internal standard. For standard solutions in the range equivalent to plasma acetic acid concentrations of 10-200 microM, assay precision was +/- 4.3%. For plasma samples in the physiological range (approximately 20-300 microM acetate) assay precision averaged better than +/- 5%. The use of the method is illustrated by measuring acetate turnover in a young adult.

Acetates↗
PubMed1990

Measurement of stable isotopic enrichment of underivatized acetate by gas chromatography/mass spectrometry: application to in vivo estimation of acetate production.

In order to assess endogenous and colonic production of acetate, we have developed an assay for determining the isotopic enrichment of plasma acetate using gas chromatography/mass spectrometry (GC/MS). Acidified, deproteinized plasma (200 microliters) was extracted into ethyl ether, and the ether phase was then injected into a gas chromatograph/mass spectrometer fitted with a 30 m x 0.252 mm i.d. capillary column (temperature program 50-245 degrees C at 10 degrees C min-1). Using electron impact GC/MS and selected ion monitoring, peak areas of ions with m/z 60 and 61 (M + 1) were determined. Triplicate extractions of enriched plasma samples (mol.% excess 1.38-1.5%) resulted in a coefficient of variation of 1.6-5.9%. Unenriched plasma samples were found to have an enrichment close to theoretical natural abundance, and analysis of our (1-13C)acetate tracer (99 at.% excess) revealed an ion at m/z 61 and no ion at m/z 60. To verify accuracy, we conducted an in vivo isotope dilution study. In a 1-month-old piglet, fasted for 24 h, changing the rate of a 4 h infusion (mmol h-1) of (1-13C)acetate from 0.141 to 0.282 doubled the isotope enrichment (2.08 x) of the second plateau. The rate of appearance of acetate was 26.0 mumols kg-1 min-1, which is comparable to that reported in fasting sheep.

Acetates↗
PubMed1977

Comparison of the biological activity of the tumor promotor phorbol myristate acetate and a metabolite, phorbolol myristate acetate, in the cell culture.

Phorbolol myristate acetate, a metabolite of the tumor promotor phorbol muristate acetate in mouse skin, has one-fiftieth the potency of the parent molecule for the induction of cell division in stationary cultures of BALB/c-3T3 mouse embryo cells. Similarly, in a mixed cell culture assay devised for detection of tumor-promoting agents, phorbolol myristate acetate exhibited only a small fraction of the activity of unmetabolized phorbol ester. The results indicate that the biological activity of phorbol esters either does not require metabolic conversion or is converted by the cells used in this system and that phorbolol myristate acetate would be a tumor promotor of low potency for mouse skin compared to phorbol myristate acetate.

3T3 Cells↗
PubMed2003

Fermentation of cellulose to acetic acid by Clostridium lentocellum SG6: induction of sporulation and effect of buffering agent on acetic acid production.

AIMS: To determine the growth, correlation between sporulation and acetic acid production and effect of buffering agent at high substrate cellulose concentrations of the strain Clostiridium lentocellum SG6. METHODS AND RESULTS: The strain SG6 was grown in cellulose mineral salt medium containing cellulose (Whatman No. 1 filter paper, Whatmore International Ltd., Maidstone, UK) or cellobiose. The strain fermented cellulose even after several transfers on cellobiose medium. The formation of endospores on third day onwards indicated the lowering of pH in the medium because of the formation of acetic acid. Maintaining the pH 7.2 at higher substrate concentrations resulted in increase of biomass, cellulose fermentation, acetic acid production, etc. CONCLUSIONS: The strain SG6, with its high fermentation yields and sporulating character can become a potential strain for acetic acid production and also as a probiotic strain in animal nutrition. SIGNIFICANCE AND IMPACT OF THE STUDY: The direct conversion of cellulosic biomass to acetic acid can eliminate expensive three-step saccharification, fermentation processes. The strain SG6 can ferment cellulose at high substrate concentrations.

Acetic Acid↗
PubMedDate not supplied

Cyclophosphamide, methotrexate and fluorouracil (CMF) versus hormonal ablation with leuprorelin acetate as adjuvant treatment of node-positive, premenopausal breast cancer patients: preliminary results of the TABLE-study (Takeda Adjuvant Breast cancer study with Leuprorelin Acetate).

PURPOSE: The objective of this study was to evaluate the efficacy and tolerability of leuprorelin acetate in adjuvant treatment in comparison to standard chemotherapy with CMF in premenopausal, estrogen-receptor-positive or unknown, node-positive patients with early breast cancer. PATIENTS AND METHODS: The patients were randomly assigned to receive either 2 years of hormone ablation with leuprorelin acetate 11.25 mg as a subcutaneous injection every three months or six courses of CMF (cyclophosphamide 500 mg/m2, methotrexate 40 mg/m2, fluorouracil 600 mg/m2, days 1 and 8, q 4 weeks). The primary study end-point was recurrence-free survival (RFS) after 2 years. Secondary end-points included overall survival, adverse events and hormonal suppression. RESULTS: Between 1995 and 1999, a total of 589 patients with breast cancer were randomized to treatment with leuprorelin acetate or CMF. The data of 227 patients were available for this first interim analysis. One hundred and ten and 117 patients were assigned to leuprorelin acetate and chemotherapy, respectively. Both treatment arms were well balanced for baseline characteristics. So far, no difference between the groups has emerged with respect to recurrence-free or overall survivaL Suppression of serum estradiol levels and menstruation was less marked in the CMF-group compared to the leuprorelin arm. The most common adverse events were low-grade hot flushes, weight gain and increased sweating in the leuprorelin-treated patients and alopecia, nausea and vomiting in the CMF-group. CONCLUSION: According to these preliminary results, ovarian suppression with leuprorelin acetate was as effective as standard chemotherapy for premenopausal women with hormone-sensitive, node-positive early breast cancer.

Adult↗
PubMed1992

Direct effects of medroxyprogesterone acetate, danazol, and leuprolide acetate on endometrial stromal cell proliferation in vitro.

OBJECTIVE: To assess the direct effects of three endometriosis chemotherapeutic agents (medroxyprogesterone acetate [MPA], danazol, and leuprolide acetate [LA]) on endometrial cell proliferation. DESIGN: Analysis of cell proliferation in vitro. SETTING: Proliferative phase endometrial stromal cells isolated from biopsy specimens and grown in short-term culture served as a model for stromal components of endometriotic implants. PATIENTS: Biopsies obtained from volunteers with regular cycles and without endometriosis or endometrial pathology. INTERVENTIONS: Medroxyprogesterone acetate, danazol, and LA were added to nutrient media with the following supplements: 2.5% calf serum (CS) only; 2.5% CS+estradiol (E2) 110 pmol/L; 2.5% CS+E2 550 pmol/L; 10% preovulatory serum (net E2 624 pmol/L). MAIN OUTCOME MEASURES: Cumulative [3H]-thymidine incorporation as a reflection of cell proliferation. RESULTS: Medroxyprogesterone acetate and danazol exerted significant antiproliferative effects on stromal cell proliferation (P less than 0.05), effects that were enhanced by an absence of exogenous E2. Leuprolide acetate exerted no consistent effects. CONCLUSIONS: These data imply that MPA and danazol but not LA exert direct effects, suppressing growth of endometriotic implants.

Adult↗