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Studies on biotransformation of STS 557
Experimental and Clinical Endocrinology
|February 1, 1983
Summary
The 9-double bond in STS 557 hinders its transformation by rat liver microsomes compared to similar steroids. Microbial studies reveal this double bond prevents 5 alpha-hydrogenation but not 5 beta-hydrogenation.
Area of Science:
- Steroid metabolism
- Pharmacokinetics
- Biochemistry
Background:
- STS 557 is a steroid compound with a unique structure.
- Understanding steroid biotransformation is crucial for drug development and toxicology.
Purpose of the Study:
- To investigate the metabolic transformation pathways of STS 557 in vitro and in vivo.
- To compare the transformation rate of STS 557 with related steroid compounds.
Main Methods:
- Incubation of STS 557 with female rat liver microsomes.
- Microbial model investigations using hydrogenating microorganisms.
- Isolation and characterization of metabolites from urine of beagle dogs and rats administered with 3H-STS 557.
Main Results:
- STS 557 exhibited a lower transformation rate compared to 17 alpha-cyanomethyl-19-nortestosterone and 19-nortestosterone.
- Identified metabolites include hydroxylated and aromatized forms, as well as altered side chains.
- The 9-double bond in STS 557 was found to prevent 5 alpha-hydrogenation but not 5 beta-hydrogenation.
Conclusions:
- The 9-double bond significantly influences the biotransformation of STS 557.
- Multiple metabolic pathways, including hydroxylation, aromatization, and side-chain alteration, contribute to STS 557 biotransformation.
- These findings provide insights into the metabolic fate of STS 557 and related steroids.