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1.
J Anim Sci ; 92(12): 5762-8, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25403190

ABSTRACT

The aim of this study was to evaluate effects of free ferulic acid (FA) supplementation on productive performance, some blood metabolite concentrations, and carcass characteristics of ewe lambs finished in a feedlot. Dorper×Pelibuey ewe lambs (n=20; BW=28.5±0.5 kg; age=5 mo) were individually housed in pens and assigned under a randomized complete block design to the following dietary treatments (n=10): daily feeding without (control) or with 300 mg of FA/animal. The feedlot feeding period lasted 34 d and then all ewe lambs were slaughtered. Free FA did not affect (P≥0.16) BW gain, ADG, DMI, and G:F during the first 17 d, but BW gain (P=0.10) and ADG (P=0.10) tended to decrease for FA from d 17 to 34 and from d 1 to 34 without affecting (P≥0.16) DMI and G:F in ewe lambs. Serum concentrations of glucose, cholesterol, triglyceride, total protein, and urea were not affected (P>0.05) by FA at d 1, 17, and 34 of the feeding period. Carcass characteristics were not affected (P>0.05) by FA. Stomach percentage tended (P=0.08) to decrease and leg yields increased (P=0.02) for FA. Other noncarcass components and wholesale cut yields were not affected (P>0.10) by FA. In conclusion, FA supplementation did not improve productive performance, metabolic status, and carcass characteristics of ewe lambs receiving a feedlot finishing diet.


Subject(s)
Animal Feed , Blood Glucose/metabolism , Body Composition/drug effects , Cholesterol/blood , Coumaric Acids/pharmacology , Dietary Supplements , Sheep/physiology , Animals , Antioxidants/administration & dosage , Antioxidants/pharmacology , Body Composition/physiology , Body Weight/drug effects , Body Weight/physiology , Coumaric Acids/administration & dosage , Diet/veterinary , Female , Meat , Proteins/metabolism , Sheep/growth & development , Triglycerides/blood , Urea/blood
2.
Bioorg Med Chem ; 20(18): 5658-67, 2012 Sep 15.
Article in English | MEDLINE | ID: mdl-22890009

ABSTRACT

The syntheses of stable isotope labelled internal standards of important CYP-isoform selective probes, like testosterone 1, diclofenac 3, midazolam 5, and dextromethorphan 7, as well as their corresponding hydroxylated metabolites 6ß-hydroxytestosterone 2, 4'-hydroxydiclofenac 4, 1'-hydroxymidazolam 6 and dextrorphan 8 are reported. Microwave-enhanced H/D-exchange reactions applying either acid, base, or homogeneous and heterogeneous transition metal catalysis, or combinations thereof proved to be highly efficient for direct deuterium labelling of the above mentioned probes. Compared to conventional stepwise synthetic approaches, the combination of H/D exchange and biotransformation provides the potential for considerable time- and cost savings, in particular for the synthesis of the stable isotope labelled internal standards of 4'-hydroxydiclofenac 4 and 1'-hydroxymidazolam 6.


Subject(s)
Diclofenac/analogs & derivatives , Isotope Labeling/methods , Midazolam/analogs & derivatives , Pharmaceutical Preparations/chemistry , Cytochrome P-450 Enzyme System/metabolism , Deuterium Exchange Measurement , Diclofenac/chemical synthesis , Diclofenac/chemistry , Diclofenac/metabolism , Microwaves , Midazolam/chemical synthesis , Midazolam/chemistry , Midazolam/metabolism , Molecular Structure , Pharmaceutical Preparations/metabolism , Reference Standards
4.
J Steroid Biochem ; 33(1): 119-24, 1989 Jul.
Article in English | MEDLINE | ID: mdl-2761260

ABSTRACT

The synthesis of new progesterone derivatives substituted at the 18 methyl group is described. These compounds are designed as 18-monooxygenase, cytochrome P-450-dependent potential kcat inhibitors. Preliminary results on the in vitro biological investigation of these modified progesterones are presented.


Subject(s)
Adrenal Glands/metabolism , Aldosterone/biosynthesis , Mineralocorticoid Receptor Antagonists/pharmacology , Progesterone/analogs & derivatives , Progesterone/pharmacology , Adrenal Glands/drug effects , Animals , Indicators and Reagents , Magnetic Resonance Spectroscopy , Mass Spectrometry , Progesterone/chemical synthesis , Rats , Rats, Inbred Strains , Structure-Activity Relationship
5.
J Steroid Biochem ; 30(1-6): 469-72, 1988.
Article in English | MEDLINE | ID: mdl-3386274

ABSTRACT

A new family of aldosterone biosynthesis inhibitors, designed as 18-mono-oxygenase, cytochrome-P450-dependent, potential Kcat inhibitors, is described. These compounds are progesterone derivatives substituted at the 18-methyl group. Preliminary results on the in vitro biological evaluation of these modified progesterones are presented. Aldosterone biosynthesis is completely inhibited by 18-vinyl progesterone 5 at a concentration of 0.8 microM and by 18-ethynyl progesterone 6 at 8 microM. It appears that products designed as alkylating agents for the prosthetic heme group are the most potent inhibitors in that series.


Subject(s)
Adrenal Glands/metabolism , Mineralocorticoid Receptor Antagonists/biosynthesis , Progesterone/analogs & derivatives , Progesterone/pharmacology , Adrenal Glands/drug effects , Animals , Kinetics , Progesterone/chemical synthesis , Rats , Rats, Inbred Strains , Structure-Activity Relationship
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