scholarly journals Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro

2009 ◽  
Vol 30 (9) ◽  
pp. 1344-1350 ◽  
Author(s):  
Xu Zhang ◽  
Yang Zhou ◽  
Yu Shen ◽  
Li-li Du ◽  
Jun-hua Chen ◽  
...  
Keyword(s):  
Biological Activities ◽  
Hydroxysteroid Dehydrogenase ◽  
Derivatives Of

An in vitro microdialysis methodology to study 11β-hydroxysteroid dehydrogenase type 1 enzyme activity in liver microsomes

2007 ◽  
Vol 370 (1) ◽  
pp. 26-37 ◽  
Author(s):  
Li Sun ◽  
Julie A. Stenken ◽  
Amy Y. Yang ◽  
Jamie J. Zhao ◽  
Donald G. Musson
Keyword(s):  
Enzyme Activity ◽  
Liver Microsomes ◽  
Hydroxysteroid Dehydrogenase

scholarly journals 17β-Hydroxysteroid Dehydrogenase Type 1, 2, 3, and 4 Expression and Enzyme Activity in Human Anterior Pituitary Adenomas

1999 ◽  
Vol 84 (4) ◽  
pp. 1340-1345
Author(s):  
V. L. Green ◽  
V. Speirs ◽  
A. M. Landolt ◽  
P. M. Foy ◽  
S. L. Atkin
Keyword(s):  
Gene Expression ◽  
Enzyme Activity ◽  
Pituitary Adenomas ◽  
Anterior Pituitary ◽  
Estrogenic Activity ◽  
Hydroxysteroid Dehydrogenase ◽  
Messenger Ribonucleic Acid ◽  
Human Anterior Pituitary

17β-Hydroxysteroid dehydrogenase (17βHSD) isoforms reversibly catalyze the final step in the formation of estradiol (E2) from estrone (E1) and the formation of testosterone from androstenedione. We have investigated 17βHSD type 1, 2, 3, and 4 gene expression and 17βHSD estrogenic activity in human anterior pituitary adenomas. 17βHSD messenger ribonucleic acid (mRNA) expression was studied by RT-PCR in 42 pituitary tumors and 3 normal pituitaries, 17βHSD activity was studied in 11 tumors and 17βHSD type 1 was immunolocalized in vitro in 6 tumors. 17βHSD type 1 gene expression was detected in 34 of 42 adenomas in all tumor subtypes; 17βHSD type 2 mRNA was detected in 18 of 42 adenomas, but not in prolactinomas; 17βHSD type 3 mRNA was detected in 12 of 42 adenomas, but not in corticotropinomas; 17βHSD type 4 was expressed in 20 of 42 adenomas by all adenoma subtypes. Reversible 17βHSD activity was found in 9 of 11 adenomas, and 17βHSD type 1 immunopositivity was cytoplasmically distributed in all 6 adenomas in vitro. All 4 17βHSD isoforms are variably expressed in human anterior pituitary adenomas, which also show 17βHSD enzyme activity, suggesting that 17βHSD may play an important role in regulating the local cellular levels of estradiol.

scholarly journals Comparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17β-hydroxysteroid dehydrogenase type 1

2016 ◽  
Vol 31 (sup3) ◽  
pp. 61-69 ◽  
Author(s):  
Bianka Edina Herman ◽  
Johanna Szabó ◽  
Ildikó Bacsa ◽  
János Wölfling ◽  
Gyula Schneider ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Comparative Investigation

scholarly journals Direct antiproliferative effect of nonsteroidal 17β-hydroxysteroid dehydrogenase type 1 inhibitors in vitro

2012 ◽  
Vol 28 (4) ◽  
pp. 695-703 ◽  
Author(s):  
Ágnes Berényi ◽  
Martin Frotscher ◽  
Sandrine Marchais-Oberwinkler ◽  
Rolf W. Hartmann ◽  
Renáta Minorics ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Antiproliferative Effect

scholarly journals Emodin, an 11β-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts anti-diabetic effect in ob/ob mice

2012 ◽  
Vol 33 (9) ◽  
pp. 1195-1203 ◽  
Author(s):  
Yue-jing Wang ◽  
Su-ling Huang ◽  
Ying Feng ◽  
Meng-meng Ning ◽  
Ying Leng
Keyword(s):  
Hydroxysteroid Dehydrogenase

scholarly journals Insights on the Effects of Resveratrol and Some of Its Derivatives in Cancer and Autoimmunity: A Molecule with a Dual Activity

Antioxidants ◽  
2020 ◽  
Vol 9 (2) ◽  
pp. 91 ◽  
Author(s):  
Elena Gianchecchi ◽  
Alessandra Fierabracci
Keyword(s):  
Lupus Erythematosus ◽  
Biological Activities ◽  
Systemic Autoimmune Diseases ◽  
Organ Specific ◽  
Inflammatory Bowel ◽  
Autoimmune Hepatitis Type 1

In recent years, the interest in natural compounds exerting immunoregulatory effects has enormously increased. Among these, the polyphenol resveratrol, found in a variety of foods and beverages, including red grapes and red wine, has been demonstrated to exert both in vitro and in vivo biological activities. More specifically, it has antiaging, cardioprotective, antioxidant, immunomodulatory, anti-inflammatory and chemopreventive activities. Due to its anti-proliferative, pro-apoptotic and immunoregulatory effects, resveratrol has gained substantial attention for the treatment of cancer or autoimmunity, which represent frequently diagnosed diseases with important consequences for the health of the patients affected. The aim of the present review is to focus on the role of resveratrol in the modulation of cancer as well as of several organ-specific or systemic autoimmune diseases, including autoimmune hepatitis, type 1 diabetes mellitus, inflammatory bowel disease, rheumatoid arthritis, systemic lupus erythematosus and multiple sclerosis.

scholarly journals Functional Effects of Polymorphisms in the Human Gene Encoding 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1): A Sequence Variant at the Translation Start of 11β-HSD1 Alters Enzyme Levels

Endocrinology ◽  
2010 ◽  
Vol 151 (1) ◽  
pp. 195-202 ◽  
Author(s):  
Elise L. V. Malavasi ◽  
Val Kelly ◽  
Nikita Nath ◽  
Alessandra Gambineri ◽  
Rachel S. Dakin ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Hydroxysteroid Dehydrogenase ◽  
In Vitro Translation ◽  
Metabolic Phenotype ◽  
Sequence Variant ◽  
Gene Encoding ◽  
Functional Consequences

Abstract Regeneration of active glucocorticoids within liver and adipose tissue by the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) may be of pathophysiological importance in obesity and metabolic syndrome and is a therapeutic target in type 2 diabetes. Polymorphisms in HSD11B1, the gene encoding 11β-HSD1, have been associated with metabolic phenotype in humans, including type 2 diabetes and hypertension. Here, we have tested the functional consequences of two single nucleotide polymorphisms located in contexts that potentially affect tissue levels of 11β-HSD1. We report no effect of allelic variation at rs846910, a polymorphism within the 5′-flanking region of the gene on HSD11B1 promoter activity in vitro. However, compared with the common G allele, the A allele of rs13306421, a polymorphism located two nucleotides 5′ to the translation initiation site, gave higher 11β-HSD1 expression and activity in vitro and was translated at higher levels in in vitro translation reactions, possibly associated with a lower frequency of “leaky scanning.” These data suggest that this polymorphism may have direct functional consequences on levels of 11β-HSD1 enzyme activity in vivo. However, the rs13306421 A sequence variant originally reported in other ethnic groups may be of low prevalence because it was not detected in a population of 600 European Caucasian women.

scholarly journals Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4960
Author(s):  
Olalla Barreiro-Costa ◽  
Gabriela Morales-Noboa ◽  
Patricio Rojas-Silva ◽  
Eliana Lara-Barba ◽  
Javier Santamaría-Aguirre ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
In Silico ◽  
Potential Application ◽  
Mammalian Cells ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Therapeutic Use ◽  
Derivatives Of

This work focuses on the search and development of drugs that may become new alternatives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We then characterized their potential application in therapeutic use. For this, the in vitro biological activities against three eukaryotic models—S. cerevisiae, five cancer cell lines, and the parasite L. mexicana—were evaluated. In addition, cytotoxicity against non-cancerous mammalian cells has been evaluated and other properties of interest have been characterized, such as genotoxicity, antioxidant properties and, in silico predictive adsorption, distribution, metabolism, and excretion (ADME). The results that we present here represent a first screening, indicating two derivatives of bis(spiropyrazolone)cyclopropanes as good candidates for the treatment of leishmaniasis. They have good specificity against parasites with respect to mammalian cells.

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