METABOLISM AND MODE OF ACTION OF ANDROGENS IN TARGET TISSUES OF MALE RATS

1975 ◽  
Vol 80 (3) ◽  
pp. 592-602 ◽  
Author(s):  
R. Szalay ◽  
M. Krieg ◽  
H. Schmidt ◽  
K. D. Voigt
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Mode Of Action ◽  
Cyproterone Acetate ◽  
Biologically Active ◽  
Male Rats ◽  
Adult Rats ◽  
Target Organs ◽  
Layer Chromatography

ABSTRACT In order to get more information on the mode of action of anti-androgens, two series with low but biologically active doses of cyproterone acetate were started. In the first experiments 12 μg of [3H] cyproterone acetate was injected intravenously into adult rats castrated 3 days before treatment. Thirty min after injection the radioactivity uptake in the target organs and other tissues was measured. The metabolites were separated by thin layer chromatography. A large pool of radioactivity could be shown in the liver. Thin layer chromatography revealed that in this pool cyproterone acetate had been converted by more than 80% to one metabolite. In blood plasma, too, the metabolite accounted for the major part of radioactivity. When compared to skeletal muscle, the prostate, seminal vesicles, and m. bulbocavernosus and m. levator ani accumulated more radioactivity. Within 30 min unchanged cyproterone acetate was retained selectively thus showing its relative high affinity to target organs. In a second experimental series, adult castrated male rats were given 10 μg of cyproterone acetate intravenously 30 min before the injection of [3H] testosterone or [3H]5α-dihydrotestosterone. Under this condition androgen uptake in target tissues was reduced to about 70 % of the control values. The data parallel the results of in vivo studies on cytosol receptor displacement of androgens by cyproterone acetate. In agreement with previous investigators no significant influence of the anti-androgen on androgen metabolism was observed. The importance of the findings concerning the mode of anti-androgen action is discussed.

Phytochemical, Analytical and Medicinal Studies of Holoptelea integrifolia Roxb. Planch - A Review

2019 ◽  
Vol 5 (4) ◽  
pp. 270-277 ◽  
Author(s):  
Vijay Kumar ◽  
Simranjeet Singh ◽  
Ragini Bhadouria ◽  
Ravindra Singh ◽  
Om Prakash
Keyword(s):  
Liquid Chromatography ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
High Performance ◽  
Biologically Active ◽  
Toxicological Studies ◽  
Wide Range ◽  
Layer Chromatography

Holoptelea integrifolia Roxb. Planch (HI) has been used to treat various ailments including obesity, osteoarthritis, arthritis, inflammation, anemia, diabetes etc. To review the major phytochemicals and medicinal properties of HI, exhaustive bibliographic research was designed by means of various scientific search engines and databases. Only 12 phytochemicals have been reported including biologically active compounds like betulin, betulinic acid, epifriedlin, octacosanol, Friedlin, Holoptelin-A and Holoptelin-B. Analytical methods including the Thin Layer Chromatography (TLC), High-Performance Thin Layer Chromatography (HPTLC), High-Performance Liquid Chromatography (HPLC) and Liquid Chromatography With Mass Spectral (LC-MS) analysis have been used to analyze the HI. From medicinal potency point of view, these phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, and anti-tumor. In the current review, it has been noticed that the mechanism of action of HI with biomolecules has not been fully explored. Pharmacology and toxicological studies are very few. This seems a huge literature gap to be fulfilled through the detailed in-vivo and in-vitro studies.

scholarly journals Application of the thin-layer chromatography method for analysis of plant antioxidant activity

Food systems ◽  
2021 ◽  
Vol 4 (1) ◽  
pp. 26-30
Author(s):  
N. V. Kupaeva ◽  
E. R. Vasilevskaya ◽  
L. V. Fedulova ◽  
E. A. Kotenkova
Keyword(s):  
Antioxidant Activity ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
High Performance ◽  
Biologically Active ◽  
Chromatography Method ◽  
Physicochemical Methods ◽  
Ethanol Extracts ◽  
Layer Chromatography ◽  
Active Substances

Plants are a rich source of effective non-toxic biologically active substances. Various physicochemical methods of analysis are used for evaluation of plant antioxidant activity. Composition of ethanol extracts of red, yellow and white onion husks, dried rosemary, basil, and chaga were studied by high performance thin layer chromatography (HPTLC) method. The antioxidant activity of the obtained fractions on a chromatographic plate was assessed by subsequent DPPH screening. The extracts red and yellow onion husk and rosemary demonstrated the highest antioxidant activity, variability of the qualitative composition and similarity of antioxidant profiles, while extract of white onion husks did not contain any antioxidant classes. Intensive spots with Rf of 0.13-0.97 were observed along the whole chromatogram track corresponding to red onion husks. It was also found that all tested extract, excepting white onion husk and chaga, contained spots with varying degrees of intensity in the Rf range of 0.96-0.98, which corresponded quercetin Rf value.

scholarly journals Assessment of the quality of peppermint leaves by thin-layer chromatography in some objects of plant origin

2020 ◽  
Vol 19 (5-6) ◽  
pp. 148-154
Author(s):  
Vali A. Sahratov ◽  
Tamara L. Malkova ◽  
Ludmila N. Karpova ◽  
Anna A. Pospelova
Keyword(s):  
Medicinal Plant ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Biologically Active ◽  
Mentha Piperita ◽  
Plant Origin ◽  
Plant Materials ◽  
Layer Chromatography ◽  
Active Substances

The State Pharmacopoeia of the XIV edition defines the approach for the assessment of the quality of medicinal plant materials, it deals with the identification of the main groups of biologically active substances by thin layer chromatography. According to this approach, the analysis of some types of medicinal plant materials as a part of some objects of plant origin was carried out. The article presents the quality assessment algorithm as examplified by peppermint leaves (Mentha piperita L.), which are part of a variety of plant object.

scholarly journals STUDYING OF THE LIPOPHILICITY AND TOXICITY OF DIPHENYLACETAMIDE DERIVATIVES

2018 ◽  
Vol 9 (1) ◽  
Author(s):  
Suzana Apostolov ◽  
Đenđi Vaštag ◽  
Borko Matijević ◽  
Gorana Mrđan
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Reversed Phase ◽  
Biologically Active ◽  
Log P ◽  
Organic Modifiers ◽  
Modern Approach ◽  
Software Packages ◽  
Test Organisms ◽  
Layer Chromatography

Modern approach in the study of biologically active compounds includes the establishment of relationships between molecular structure, physicochemical properties and the behavior which studied compound can manifest in the biological medium. These examinantions are performed in the early stages of the design of future bioactive agent and require the knowledge of molecular descriptors that can point to its biological activity, including lipophilicity which occupies a key position. For the series of diphenylacetamide derivatives, lipophilicity is determined experimentally by thin-layer chromatography on reversed phase (RP TLC18 F254s), in mixtures of water and various organic modifiers and computationally, by using the relevant software packages. In order to estimate the potential acute toxicity of the tested diphenylacetamide derivatives, their effective concentrations, EC50, on the selected test organisms have been determined. Experimentally determined lipophilicity (RM 0 and m) is correlated with a standard measure of lipophilicity (log P), as well as with the selected parameters of toxicity. Thus it has been found that thin-layer chromatography on reversed phase can be used reliably for describing the lipophilicity and for the evaluation of the toxic effects of diphenylacetamide derivatives.

scholarly journals Synthesis of new 6-hydroxypyrimidine-4(3Н)-onе derivatives

2020 ◽  
Vol 62 (6) ◽  
pp. 40-43
Author(s):  
Elena V. Kuvaeva ◽  
◽  
Denis A. Kolesnik ◽  
Ksenia E. Kirpikova ◽  
Igor P. Yakovlev ◽  
...  
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Elemental Analysis ◽  
Physicochemical Analysis ◽  
Reaction Mass ◽  
Biologically Active ◽  
Resonance Spectroscopy ◽  
Sedative Drugs ◽  
Layer Chromatography ◽  
Phenobarbital Sodium

In this paper, 6-hydroxypyrimidine-4 (3Н)-one derivatives are considered as promising syntones for the creation of new biologically active substances. This is useful since the pyrimidine fragment is a structural component of nucleic acid bases (cytosine, thymine, uracil), uric and orotic acids, coenzymes (flavins and xanthins), a number of vitamins (folic acid, thiamine, pyridoxine, riboflavin). It is worth noting that the pharmaceutical market is widely represented with antitumor (methotrexate, imatinib, tegafur); antiviral (stavudine, zalcitabine, lamivudine, zidovudine, acyclovir, idoxuridine); immunostimulatory (isophone) and sedative drugs (phenobarbital, sodium ethaminal) based on compounds including the pyrimidine cycle. The purpose of the present work is to develop a method for producing new 2,3-diphenyl-5-(alkyl/ phenyl)-6-hydroxypyrimidin-4(3Н)-ones, proving their structure and individuality by NMR spectroscopy and mass spectrometry, elemental analysis and thin-layer chromatography. As a method of producing new 6-hydroxypyrimidin-4(3Н)-ones, a method of condensing N-phenyl-benzenecarboxymidamide with 2-substituted propanedioyldichlorides in the medium of an aprotic non-polar solvent – o-xylene is proposed. The desired products are isolated from the reaction mass using solvent distillation and a reprecipitation method. It was found that maximum yields are achieved with constant stirring of a suspension of N-phenylbenzenecarboxymidamide with a solution of 2-substituted propanedioyl dichloride in o-xylene and further heating of the reaction mass at 144 °C for 4 hours. The individuality of the synthesized compounds was confirmed by thin layer chromatography on Sorbfil® plates in the methanol-dichloroethane (1:9) system, and their structure was proved using modern physicochemical analysis methods: proton magnetic resonance spectroscopy, NMR С13 spectroscopy, mass spectroscopy and elemental analysis.

Sign in / Sign up

Export Citation Format

Share Document