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Anti-inflammatory steroids, lysosomal stabilization and parachor
Canadian Journal of Biochemistry
|October 1, 1975
Summary
Parachor, a molecular property, correlates with steroid biological activities like enzyme release and anti-inflammatory potency. This structure-activity relationship offers insights for drug design.
Area of Science:
- Biochemistry
- Pharmacology
- Computational Chemistry
Background:
- Parachor is an additive molecular property linked to molar volume and surface tension.
- It reflects a molecule's ability to permeate hydrophobic cellular environments, particularly membranes.
Purpose of the Study:
- To investigate the correlation between steroid parachor values and various biological activities.
- To explore the utility of parachor as a structure-activity relationship parameter in drug design.
Main Methods:
- Calculation of parachor values based on molecular structure (atoms and bonds).
- Analysis of existing data correlating steroid parachor with biological effects like lysosomal enzyme release, anti-inflammatory potency, and mitochondrial effects.
- Evaluation of percutaneous absorption data in relation to parachor and partition coefficients.
Main Results:
- Steroid parachor is inversely related to lysosomal enzyme release and directly related to anti-inflammatory potency.
- Steroid parachor correlates with the uncoupling of oxidative phosphorylation and mitochondrial swelling.
- Percutaneous absorption of steroids correlates with parachor and specific partition coefficients.
Conclusions:
- Parachor is a valuable parameter for predicting steroid biological activity.
- The calculated parachor method offers a useful approach for drug design and structure-activity relationship studies.
- Understanding these correlations can guide the development of novel steroid-based therapeutics.
Keywords:
AndrogensAnimals, LaboratoryBiologyClinical ResearchContraceptionContraceptive Agents, Estrogen--analysisContraceptive Agents, Female--analysisContraceptive Agents, Progestin--analysisContraceptive Agents--analysisDiethylstilbestrol--analysisEndocrine SystemEstradiol--analysisEstrogensEthinyl Estradiol--analysisFamily PlanningHormonesIn VitroNorethindrone--analysisNorgestrel--analysisPhysiologyProgestational HormonesProgesterone--analysisResearch MethodologyTestosterone--analysis