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Biomedical subjects

V Petrow

Publications and source records attributed to V Petrow.

At least 55 records · Page 3Linked to original sources
PubMed1981

Prostatic cancer. I. 6-Methylene-4-pregnen-3-ones as irreversible inhibitors of rat prostatic delta 4-3 ketosteroid 5 alpha-reductase.

Some derivatives of 6-methylene-4-pregnen-3-one were studied as inhibitors of delta 4-3-ketosteroid 5 alpha-reductase. Maximum inhibitory activity was shown by 17-acetoxy-6-methylene-4-pregnene-3,20-dione (AMPD). Irreversible inactivation was observed following preincubation of the enzyme with NADPH and AMPD. This inactivation was found to occur only in the presence of NADPH. As such enzyme inactivation was not due to the formation of a more inhibitory metabolic product, or to the formation of superoxide via a cytochrome P-450/NADPH pathway, it seemed likely that the observed inactivation was derived from an irreversible combination of the enzyme with AMPD. That this was probably the case was established by kinetic studies which revealed a pattern compatible with a kcat type of mechanism.

5-alpha Reductase Inhibitors↗
PubMed1980

Growth and lipemic activity of 19-oxo-androstenedione: a potential growth stimulant for poultry.

A metabolite of androstenedione, 19-oxo-androstene-3,17-dione (19-oxo-A), was evaluated for its effects upon growth, oviductal weight, and plasma lipids of young chicks; estradiol benzoate (EB) was used as reference standard. Ten-day-old Leghorn pullets were treated subcutaneously with either olive oil vehicle, EB at .05 to 1.35 mg/kg/day, or 19-oxo-A at 1 to 30 mg/kg/day at 1/2-log dose concentrations for six days. At the highest dose levels of each compound, the relative potency for these biological responses was compared with EB equated to 100. The 19-oxo-A was 100% of EB for body weight gain, 1.4% for oviductal growth, and 10.1%, 2.6%, and 6.2% in elevation of plasma lipids for cholesterol, triglycerides, and phospholipids, respectively. In an antiogonadotropin assay using the hemicastrate rat, only 19-oxo-A suppressed ovarian weight without significant increase in uterine weight. Additionally, this compound did not bind with androgen, estrogen and progesterone cytosol receptor preparation. 19-oxo-A resembles estrogen in inducing growth of poultry, but differs markedly from estradiol benzoate in being essentially devoid of systemic estrogenicity. Thus, 19-oxo-A represents a new and unique steroid for stimulating growth and fat deposition in commercial meat poultry.

Androstenedione↗
PubMed1979

The synthesis of diazo, halo, and sulfoxy bile acid derivatives: potential affinity labels.

Bile acid derivatives, with and without C-3 sulfate groups, and having either the diazo- or halomethylketone moieties, have been synthesized in good yield and purity. The synthetic sequence, COOH leads to COC1 leads to COCHN2 leads to COCH2X, was used with deoxycholic and cholic acids, which requires carefully controlled quench, work-up, and purification procedures, especially for the 3-sulfate esters (made from deoxycholic acid derivatives only). The pure title compounds are anticipated to be useful chemical probes (affinity labels), especially the completely water soluble sulfates, toward our studies of ileal active transport of bile salts. A new use for Sephadex LH-20 as a sulfate ester protecting group is reported. Also developed were the use of acetamide hydrochloride complex as a mild hydrochlorination reagent and a neutral desalting method for sulfate esters of deoxycholic acid derivatives.

Affinity Labels↗
PubMed1977

5-(Tetradecyloxy)-2-furancarboxylic acid and related hypolipidemic fatty acid-like alkyloxyarylcarboxylic acids.

5-(Tetradecyloxy)-2-furancarboxylic acid (91, RMI 14514) was found to lower blood lipids and to inhibit fatty acid synthesis with minimal effects on liver weight and liver fat content. This fatty acid-like compound represents a new class of hypolipidemic agent; it is effective in rats and monkeys. The compound resulted from discovery of hypolipidemic activity in certain beta-keto esters, postulation and confirmation of the corresponding benzoic acids as active metabolites, and systematic exploration of the structure--activity relationships.

Animals↗
PubMed1976

Antiprogestational agents. The synthesis of 7-alkyl steroidal ketones with anti-implantational and antidecidual activity.

A series of 7alpha- and 7beta- alkyl derivatives of steroidal 4-en- and 5-en-3-ones were prepared by 1,6-conjugate addition of organocopper reagents to various steroidal 4,6-dien-3-ones of the androstane, estrane and gonane series. Biological study of these and related compounds revealed that 17beta-hydroxy-7alpha-methyl-5-androsten-3-one (2), 17beta-hydroxy-7alpha-methyl-5-estren-3-one acetate and 17beta-hydroxy-7alpha-methyl-4-estren-3-one acetate had significant anti-implantational and antidecidual activities. The contragestative effects were associated with the latter anti-hormonal properties, and not with the androgenicity of these compounds.

Androstenols↗