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PubMedDate not supplied

[Effect of hyperglycemia and hyperthermia on liver mitochondrial respiration and blood glucose content of rats during postnatal ontogenesis].

Correlation between glucose level in blood and liver mitochondrial energetics of 1, 10, 20-days rats under hyperglycemia and high environmental temperature (38 degrees C) has been studied. Glucose feeding led to a significant increase of glucose content in blood, this increase being less at hyperthermia. Glucose feeding strengthened the oxidation of such intermediates as succinate (Krebs cycle), pyruvate and malate (hydrocarbonates) and caprylate (lipid). High environmental temperature with hyperglycemia suppresses the liver mitochondria breathing, hydrocarbon and lipid intermediates being used; the suppression is less in the presence of succinate. It is found that liver mitochondria of growing rats at different experimental conditions oxidize different intermediates with various rates. These data can be explained in the light of ontogenetic evolution of the energetic apparatus. It is supposed that exogenic glucose is the factor which activates growing processes of animals and to certain extent diminishes the negative influence of hyperthermia on the organism.

Animals↗
PubMed2004

[Effect of casein and protamine on the enzymatic degradation and the orally hypoglycemic action of insulin].

AIM: To study the protection of casein and protamine against degradation of insulin (INS) by proteolysis enzymes and the effect of these two kinds of protein on the hypoglycemic action of INS solution and enteric-microspheres after administrated orally to rats. METHODS: HPLC was used to determine the remained INS in the solution of alpha-chymotrypsin and trypsin with or without casein or protamine; INS solution and enteric-microspheres were prepared and adiministrated orally to rats together with the absorption enhancer sodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC). At the same time, casein or protamine or both of these two kinds of protein were administrated together in order to study their influence on the hypoglycemic effect of INS and microspheres. RESULTS: Casein had a good protection against degradation of INS by alpha-chymotrypsin, but protamine had no protection effect. However, the degradation of INS by trypsin is concerned, the protection effect of protamine on INS was better that of casein. Both of protamine and casein can increase the hypoglycemic effect of INS solution and enteric-microspheres. Co-administrated these two kinds of protein had a better effect. In addition, co-administrated with SNAC, casein and protamine, INS enteric-microspheres had a longer and more potent hypoglycemic effect than that of the solution. CONCLUSION: Casein and protamine can increase the stability of INS in the intestinal fluid by the mechanism of competition and combine with proteolysis enzymes, which will benefit to INS oral administration.

Administration, Oral↗
PubMed1990

Effect of monoglycerides on the percutaneous absorption of papaverine hydrochloride.

The skin permeation enhancement of papaverine hydrochloride by free fatty acids (C3-C12), monoglycerides (side chains C5-C12) and caprylic acid (C8) esters was evaluated using the excised hairless rat skin. Enhancement was marked in the case of glyceryl monocaprylate; the cumulative amount of papaverine that permeated through skin over 28 hours from an aqueous suspension was 29.7 mg/cm2 with, and 26.9 micrograms/cm2 without glyceryl monocaprylate. The mechanism of enhancement was studied by measuring the effect the enhancers had on the diffusion and partition parameters of papaverine. Free fatty acids mainly affected the drug's diffusion, and monoglycerides mainly affected the drug's partition. For monoglyceride enhancers, a good linear relationship between the flux of papaverine and the amount of enhancer in skin was established. n-Octanol-water partition coefficients (log Pcal) of the enhancers were selected as indicators of their physicochemical properties, and related to their penetration-enhancing abilities. A parabolic relationship was found between the log of the flux of papaverine and log Pcal, for all types of enhancers. The relationship may be a good indicator in predicting enhancing effects.

1-Octanol↗
PubMed1989

The effect of octanoic fatty acid on the cardiovascular system of the guinea pig.

The aim of the study was to clarify the role of octanoic acid (OA) in the development of cardiovascular disorders occurring in some liver diseases associated with high OA levels in blood serum. The effect of OA (caprylic acid) on the functional state of the cardiovascular system was studied in guinea pig by means of the thermodilution method and ultrasound Doppler echography. It was found that, as a result of its inotropic action, OA decreases arterial pressure and vascular resistance while increasing cardiac output. The effect of OA can be inhibited by the administration of indomethacin, a fact suggesting the prostaglandin system plays a role in the mechanism of cardiovascular action of OA. This hypothesis represents a new concept regarding the pathogenesis of the hyperdynamic cardiovascular syndrome in liver cirrhosis and hepatic encephalopathy.

Animals↗
PubMed1984

[Effect of the replacement of a part of the tallow in a milk supply with tricaprylin or coconut oil on the use of energy and nitrogen by the preruminant calf].

The advantages of using caprylic acid in the feed of preruminant calf have been investigated and compared to those of coconut oil. Two trials were carried out. Trial 1 studied the effect on the appetence and digestibility of a conventional milk replacer when tricaprylin ( TC8 ) was substituted for one-half of the tallow in the replacer. Trial 2 investigated diet digestibility and energy and nitrogen balances in 3 groups of 6 Friesian male preruminant calves each, using two open-circuit respiratory chambers. Group 1 was fed a control diet based on skim-milk powder and tallow (diet 1). In group 2, 2/3 of the tallow was replaced by coconut oil (diet 2). In group 3, 1/3 of the tallow was replaced by coconut oil and the other 1/3 by TC8 (diet 3). Apparent digestibility of energy (94.4 vs 90.7%; P less than 0.05) and nitrogen (93.2 vs 89.7%; P less than 0.10) and energy metabolizability , q (91.6 vs 88.1%, NS) were higher with diet 2 than with diet 1. TC8 intake also favoured a higher apparent digestibility of energy (98.0 vs 92.9%; P less than 0.01) and nitrogen (96.9 vs 93.0%; P less than 0.001) in trial 1 but not in trial 2 where diet 3 had only a slightly higher apparent digestibility than diet 1 (92.9% for energy and 90.7% for nitrogen; P less than 0.10). Adjusted protein gains observed in trial 2 were 52.3 +/- 3.4, 58. 9b +/- 5.3 and 56. 5ab +/- 5.4 kcal/d/kg W0 .75, respectively, for each of the 3 diets; adjusted lipid gains were 66. 8a +/- 4.0, 59.6b +/- 4.2 and 61. 2ab +/- 6.7 kcal/d/kg W0 .75; and adjusted energy gains were 119.2 +/- 6.2, 118.4 +/- 6.1 and 117.5 +/- 6.6 kcal/d/kg W0 .75 (a, b = data with different superscripts are significantly different; P less than 0.05). Metabolizable energy (EM) efficiency for tissue deposition was of the order of 0.67 +/- 0.14, and maintenance requirements amounted to an average of 95 kcal EM/d/kg W0 .75.

Amino Acids↗
PubMed1980

[Resolution of cholesterol-gallstone with a modified Capmul 8210-emulsion and with an EDTA solution (author's transl)].

Cholesterol stones in the bile duct may be resolved by applying Capmul 8210 (Cholesterol-caprylic acid ester) by way of T-drain or through a gastro-biliary tube. Results of in vitro experiments and a case reported do show, that an alternating irrigation with a specially prepared solution of glycerooctonate with bile salt-EDTA-solution will yield better results than Capmul 8210 alone. The advantage of this alternating therapy results from the fact, that calcium bilirubinate may be resolved in addition to the other components of the gallstones, and that side effects are rarer and less disturbing than side effects caused by Capmul 8210.

Anticholesteremic Agents↗
PubMed1977

Toxic fatty acid resistant mutant of Trichophyton rubrum.

A mutant of Trichophyton rubrum which could tolerate high concentration (110 microgram/ml) of undecanoic acid was isolated from undecanoic (27.5 microgram/ml) sensitive parent. The mutant showed cross resistance towards other fatty acids like propionic acid, caprylic acid and undecenoic acid which were toxic for the parent strain. Development of fatty acid resistance in the mutant strain was associated with increased pigment production. There was no difference in colony or cell morphology between fatty acid resistant mutant and fatty acid sensitive parent.

Caprylates↗
PubMed1995

Development and comparison of purification strategies for chicken antibodies from egg yolk.

With regard for animal welfare as well as cost, antibodies purified from the egg yolk of immunized chickens are an attractive alternative to antibodies raised in serum of mammals. Various purification strategies based on initial purification by a freeze-and-thaw method followed by one of three precipitation methods--ammonium sulfate, polyethylene glycol 6000, or caprylic acid--were compared. Ammonium sulfate precipitation (25 to 40%) was found to give the best combination of high purity and yield (58%). Moreover, this method is inexpensive and well suited for standard purification of egg yolk antibodies in large scale production facilities.

Ammonium Sulfate↗
PubMed2003

Management of venous thromboembolism: past, present, and future.

Venous thromboembolism, including deep vein thrombosis and pulmonary embolism, represents a significant source of morbidity and mortality in the United States and worldwide. The pharmacologic management of venous thromboembolic disease has witnessed significant advances since oral anticoagulant and heparin therapies began to gain widespread use more than 50 years ago. Cumulative clinical experience gained from using these 2 classes of antithrombotic agents for the prevention and treatment of venous thromboembolism in high-risk patients pointed to a number of efficacy and safety limitations. This prompted further research and the eventual introduction, in the 1980s, of low-molecular-weight heparin(s) as a potentially superior therapeutic modality. Within the last decade the pace of development of newer classes of antithrombotic agents for venous thromboembolism prevention and treatment (as well as other indications) has accelerated. Among agents at late stages of investigation are ximelagatran (a direct thrombin inhibitor), nematode anticoagulant peptide c2 (a tissue factor VIIa inhibitor), and sodium N-[8(2-hydroxylbenzoyl)amino]caprylate (SNAC)/heparin (a heparin derivative). The most recently approved agents for venous thromboembolism indications include the heparinoid, danaparoid sodium, and the newly introduced selective factor Xa inhibitor, fondaparinux.

Anticoagulants↗
PubMed1998

A novel esterase from Saccharomyces carlsbergensis, a possible function for the yeast TIP1 gene.

An extracellular esterase was isolated from the brewer's yeast, Saccharomyces carlsbergensis. Inhibition by diisopropyl fluorophosphate shows that the enzyme has a serine active site. By mass spectrometry, the molecular weight of the enzyme was 16.9 kDa. The optimal pH for activity was in the range of four to five. Esterase activity was found in beer before pasteurization, and a low level of activity was still present after pasteurization. Caprylic acid, which is present in beer, competitively inhibited the esterase. The substrate preference towards esters of p-nitrophenol indicated that the enzyme prefers esters of fatty acids from four to 16 carbon atoms. The esterase has lipolytical activity; olive oil (C-18:1), which is a classical substrate for lipase, was hydrolysed. N-terminal sequence analysis of the esterase yielded a sequence which was identical to the deduced amino acid sequence of the S. cerevisiae TIP1 gene. The esterase preparation did not appear to contain significant amounts of other proteins than Tip1p, indicating that the TIP1 gene is the structural gene for the esterase.

Amino Acid Sequence↗
PubMed1998

Quantitative enzymatic production of 6-O-acylglucose esters

Selective production of emulsifiers from glucose and fatty acids has been achieved using an immobilized Candida antarctica lipase. Optimization of process selectivity considers the solubilities of the sugar and its monoesters in acetone at different temperatures, the percentage of this organic solvent in the reaction mixture, and the reaction temperature. The solvent (acetone) is both easily eliminated and accepted by the European Community for use in the manufacture of foods and/or food additives. Different fatty acids with a longer length chain than that of caprylic acid may be employed. For saturated fatty acids longer than lauric acid, continuous precipitation of the monoester as it is formed at 40 degrees C permits nearly complete conversion (98%) of glucose to the monoester within 2-3 days. The procedure does not require total dissolution of the sugar, and precipitation of the monoester permits selective conversion of charges of glucose higher than 100 mg/mL solvent. A scaleup of the process under the optimum conditions gives high yields of 6-O-lauroyl glucose, which may be readily prepared on a gram scale. Copyright 1998 John Wiley & Sons, Inc.

Journal Article↗
PubMed1998

Quantitative enzymatic production of 1,6-diacyl sorbitol esters

The enzymatic synthesis of several sorbitol diesters whose HLB values are similar to those of monoglycerides (the largest single type of food-grade emulsifiers) has been studied. The procedure is carried out by the simple addition of the polyol to a solution of the fatty acid and is based on continuous precipitation of the diester formed at a low temperature. A solvent of relatively low toxicity (acetone) was used. Pure fatty acids of different chain lengths (lauric and caprylic acids) were employed. The procedure was also tested using the acids obtained from total hydrolysis of olive oil, as an example of industrial feedstocks of fatty acids. This synthesis strategy gave complete conversion of sorbitol and >95% yields of the corresponding 1,6-diesters. In addition, a strategy to reduce the reaction time is reported. The enzymatic procedure permits minimization of the solvent/sugar ratio because it does not require complete dissolution of the sugar in the organic solvent. Copyright 1998 John Wiley & Sons, Inc.

Journal Article↗
PubMed2002

A comparison of lipase-catalysed ester and lactone synthesis in low-water systems: analysis of optimum water activity.

We investigated the effects of the lyophilisation medium (enzyme plus buffer salt and additives) and of water activity (a(w)) on the catalytic properties of lipase from Chromobacterium viscosum (lipase CV) in organic solvents; catalysis of ester and lactone synthesis were compared and, despite the similarities of the reactive groups involved in these reactions, some interesting differences were observed. Including 2-[N-morpholino]ethanesulfonic acid (MES) buffer in the lyophilisation medium of lipase CV increased its catalytic activity in transesterification and lactonisation, although the buffer salt requirement for maximal activity differed between the two reactions. Sorbitol, glucose, lactose, 18-crown-6 (crown ether 18-C-6), beta-cyclodextrin and bovine serum albumin were employed as alternative additives in the transesterification reaction, but were not as effective as MES buffer. Salt hydrates were used to investigate the effect of a(w) on esterification and lactonisation reactions catalysed by lipase CV. The maximum rate of hexadecanolide synthesis in toluene occurred at a(w) = 0.48. The optimum a(w) for the transesterification reaction in heptane/alcohol mixtures depended on the alcohol substrate employed (1-heptanol, 2-heptanol, or 3-methyl-3-hexanol) but not on the acyl donor (p-NP acetate or caprylate). The optimum a(w) values for both reactions were unchanged when a common solvent system (toluene/1-heptanol) was employed, indicating that the dependence of enzyme activity on a(w) is an intrinsic property of the enzyme-catalysed reaction and not a function of the solvent or other additives.

Biotechnology↗
PubMed2004

Preparation of tripeptide-bridged dicatechol ligands and their macrocyclic molybdenum(VI) complexes: fixation of the RGD sequence and the WKY sequence of urotensin ii in a cyclic conformation.

Dicatechol ligands were prepared with caprylic acid (6-H(4)) or the naturally occurring RGD (23-H(4)) or WKY sequences (32-H(4)) as spacers. 6-H(4) was prepared by solution-phase amide coupling chemistry, while 16, the precursor of 23-H(4), was obtained by solution-phase and solid-phase preparation. In the latter case, a polystyrene resin with a hydrazine benzoate linker was used as the solid support. The last coupling step was performed simultaneously with cleavage of the peptide from the resin. The protecting groups of 16 were all removed in one step to yield the free ligand 23-H(4). The WKY-bridged derivative 32-H(4) was obtained by a similar solid-phase synthesis followed by deprotection. The reaction of all three ligands with dioxomolybdenum(VI) bis(acetylacetonate) afforded 19-membered metallamacrocycles in which the short peptides are conformationally fixed in a turn-type structure. Hereby, the side-chain functionalities of the peptides do not interfere in the metal complexation.

Amino Acid Sequence↗
PubMed1982

Wetting characteristics and blood clotting on surfaces of acylated chitins.

Various acylated chitins, including formyl, acetyl, propionyl, butyryl, caproyl, capryl, lauroyl, and benzoylchitin, were evaluated as materials for blood contact surfaces by means of contact angle and blood-clotting time measurements. Critical surface tensions of acylated chitins varied within the range of 20-30 dyn cm-1 and were dependent on the length of the acyl side chains. Furthermore, the dispersion and nondispersion components of the surface tension show remarkable differences which are dependent on the type of acyl group attached to chitin. The chitin derivative with 2.0 acetyl groups per N-acetylglucosamine residue gave values of the dispersive and nondispersive components of the surface tension that are very close to those obtained for glutaraldehyde-treated umbilical cord vessels. All of the acylated chitin surfaces show longer clotting times than the original chitin surface.

Acylation↗
PubMed1976

Induction by short-chain fatty acids of alkaline phosphatase activity in cultured mammalian cells.

Short-chain fatty acids, such as propionic, n-butyric, n-butyric, n-valeric, isovaleric, n-caproic, and n-caprylic acids, induce alkaline phosphatase activity in cultured mammalian cells. Long-chain fatty acids have no similar effects. With B-6 cells (mouse X Chinese hamster cell hybrids), n-butyrate at 2 to 5 mM exhibits the greatest activity. Induction begins exponentially about 24 hours after addition of the fatty acid and continues over 48 hours. Studies on the inducing activity-structure relationship revealed the necessity of a carboxyl and an ethyl or longer alkyl group. n-Butyrate shows a marked synergistic action of induction when added along with other types of inducers: adenosine 3':5'-cyclic monophosphate (cAMP) or 5-bromodeoxyuridine (BrdU). Treatment of other cell lines with either n-buryrate, cAMP, or BrdU revealed a cell-type specific response pattern of alkaline phosphatase. The biological significance of this effect of short-chain fatty acids is discussed.

Acid Phosphatase↗
PubMed1977

[Physiology and biochemistry of streptomycetes. VIII. Esterase activity and production of turimycin in cultures of Streptomyces hygroscopicus JA 6599].

Esterase in cell-free extracts of Streptomyces hygroscopicus JA 6599 has a temperature-optimum of 35 degrees C, a pH-optimum with p-nitrophenylacetate as substrate at pH 7.7--8.1, with alpha-naphthylacetate at pH 7--9. Michaelis constants in cell-free extracts: with alpha-naphthylacetate Km = = 0.71 mM, with p-nitrophenylacetate Km = 0.21 mM. Phenylesters were better hydrolyzed than naphthylesters, phenylacetate was best hydrolyzed; beta-naphthylacetate was better hydrolyzed than alpha-naphthylacetate. Among the naphthylesters the ester of propionic acid was hydrolyzed best. Caprylate, stearate, and 0,0-diethyl-0-(p-nitrophenyl)-phosphate inhibit the splitting of alpha-naphthylacetate. A comparison with esterases of other biological origin shows that the enzyme studied can be a carboxylesterase (E.C.3.1.1.1.). In cultures of JA 6599 V13 and JA 6599-6 the change of esterase activity during the fermentation was determined. We found a carrelation between the enzymatic activity and the antibiotic-concentration in the culture medium.

Acetates↗
PubMed2007

Quantitation of crystalline material within a liquid vehicle using 1H/19F CP/MAS NMR.

A method to detect and quantify a small amount crystalline material within a liquid solution of solubilized material is described. 19F CP-MAS ssNMR was investigated as a technique to detect low levels (0.2 mg/g) of crystalline sodium (2R)-7-{3-[2-chloro-4-(2,2,2-trifluoroethoxy)phenoxy]propoxy}-2-methyl-3,4-dihydro-2H-chromane-2-carboxylate (I) within a solid mixture (with microcrystalline cellulose) and a slurry with a liquid vehicle (capric and caprylic acid triglycerides). The results demonstrate that the area of the 19F CP/MAS signal obtained in 25 min at 25 degrees C is linearly dependent (R2=0.997) on the mass of I within the ssNMR rotor. Slopes of CP-MAS peak area versus mass of I in the rotor were nearly identical for the solid mixture and slurry suspension. Signal-to-noise ratio for the low potency slurry suggest detection and quantitation of 0.1 mg of crystalline I in the rotor, corresponding to 2 mg/g of crystalline material within the slurry suspension.

Benzopyrans↗