Synthesis and Biological Activity of Cyclopropyl Δ7-Dafachronic Acids as DAF-12 Receptor Ligands

2021 ◽  
Author(s):  
Valentina Mancino ◽  
Giada Ceccarelli ◽  
Andrea Carotti ◽  
Laura Goracci ◽  
Roccaldo Sardella ◽  
...  
Keyword(s):  
Biological Activity ◽  
Bile Acid ◽  
Receptor Ligands ◽  
Hyodeoxycholic Acid ◽  
Chemical Tools

The four cyclopropyl stereoisomers of Δ7-dafachronic acids were prepared from the bile acid hyodeoxycholic acid and employed as chemical tools to exploit the importance of the orientation and spatial disposition...

Reporter cell lines are useful tools for monitoring biological activity of nuclear receptor ligands

Luminescence ◽  
2001 ◽  
Vol 16 (2) ◽  
pp. 153-158 ◽  
Author(s):  
Patrick Balaguer ◽  
Anne-Marie Boussioux ◽  
Ediz Demirpence ◽  
Jean-Claude Nicolas
Keyword(s):  
Biological Activity ◽  
Cell Lines ◽  
Nuclear Receptor ◽  
Receptor Ligands ◽  
Reporter Cell ◽  
Nuclear Receptor Ligands

scholarly journals Identification of bile acids in the serum and urine in cholestasis. Evidence for 6α-hydroxylation of bile acids in man

1976 ◽  
Vol 154 (2) ◽  
pp. 507-516 ◽  
Author(s):  
J A. Summerfield ◽  
B H. Billing ◽  
C H. L. Shackleton
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Acid Metabolism ◽  
Gas Chromatography Mass Spectrometry ◽  
Acid Mixture ◽  
Bile Acid Metabolism ◽  
Hyodeoxycholic Acid ◽  
Normal Man ◽  
Hyocholic Acid ◽  
Sulphate Conjugate

In this qualitative study of the pattern of bile acid excretion in cholestasis, methods are described for the isolation of bile acids from large volumes of urine and plasma. The bile acids were subjected to a group separation and identified by combined gas chromatography-mass spectrometry. The techniques were developed to allow identification of the minor components of the bile acid mixture. Four bile acids that have not previously been described in human urine and plasma were detected, namely 3β, 7α-dihydroxy-5β-cholan-24-oic acid, 3α, 6α-dihydroxy-5β-cholan-24-oic acid (hyodeoxycholic acid), 3α, 6α, 7α-trihydroxy-5β-cholan-24-oic acid (hyocholic acid) and 3α, 7β, 12α-trihydroxy-5β-cholan-24-oic acid. In addition three C27 steroids were found; 26-hydroxycholesterol and a trihydroxy cholestane, probably 5 β-cholestane-3α, 7α, 26-triol were found in the sulphate fraction of plasma and urine. In the plasma sample, a sulphate conjugate of 24-hydroxycholesterol was found. The presence of these compounds probably reflects the existence of further pathways for bile acid metabolism. It is not yet known whether this is a consequence of the cholestasis or whether they are also present in normal man, at much lower concentrations.

scholarly journals Epimeric Mixtures of Brassinosteroid Analogs: Synthesis, Plant Growth, and Germination Effects in Tomato (Lycopersicum esculentum Mill.)

Agronomy ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 808
Author(s):  
Nitza Soto ◽  
César González ◽  
Marco Mellado ◽  
Andrés F. Olea ◽  
Yamilet Coll ◽  
...  
Keyword(s):  
Biological Activity ◽  
Plant Growth ◽  
Potential Application ◽  
Growth And Development ◽  
Side Chains ◽  
Lycopersicum Esculentum ◽  
Good Level ◽  
Hyodeoxycholic Acid ◽  
Pure Compounds

Brassinosteroids (BRs) play an important role in the growth and development of plants. Herein, we describe the synthesis of epimeric mixtures of BR analogs with 24-norcholane type side chains, S/R configuration at C22 and A/B ring cis-type fusion. All epimeric mixtures were synthetized from hyodeoxycholic acid. The biological activity of mixtures was evaluated by using rice lamina inclination test and germination of tomato (Lycopersicum esculentum) seeds. The results show that these epimeric mixtures exhibit similar bioactivity to brassinolide in both bioassays. Thus, our results corroborate that the A/B junction has almost no effect on bioactivity and open the possibility of using epimeric mixtures instead of pure compounds. In this approach, the synthesized BR analogs maintain a good level of bioactivity, whereas the synthesis is shorter, cheaper and with higher yields. All these factors make this alternative very interesting for potential application.

scholarly journals Hyodeoxycholic acid derivatives as liver X receptor α and G-protein-coupled bile acid receptor agonists

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Simona De Marino ◽  
Adriana Carino ◽  
Dario Masullo ◽  
Claudia Finamore ◽  
Silvia Marchianò ◽  
...  
Keyword(s):  
Bile Acid ◽  
G Protein ◽  
Liver X Receptor ◽  
Acid Receptor ◽  
Receptor Agonists ◽  
Hyodeoxycholic Acid ◽  
Liver X Receptor Α ◽  
Bile Acid Receptor ◽  
G Protein Coupled

scholarly journals Synthesis and biological activity of adenophostin derivatives as IP3 receptor ligands

2002 ◽  
Vol 2 (1) ◽  
pp. 23-24 ◽  
Author(s):  
S. Shuto ◽  
T. Mochizuki ◽  
H. Abe ◽  
Y. Kondo ◽  
A. Matsuda
Keyword(s):  
Biological Activity ◽  
Ip3 Receptor ◽  
Receptor Ligands
Sign in / Sign up

Export Citation Format

Share Document