Synthesis and Biological Activity of a Bis-steroid-methanocyclobutanaphthalene- dione Derivative against Ischemia/Reperfusion Injury via Calcium Channel Activation
| Autor: | Díaz-Cedillo Francisco, Mateu-Armand Virginia, Cabrera-Tuz Jhair, Rosas-Nexticapa Marcela, Figueroa-Valverde Lauro, Garcimarero-Espino E. Alejandra, Borges-Ballote Yaritza, Hau-Heredia Lenin, Lopez-Ramos Maria |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Male
Cardiotonic Agents Infarct Immunology Ischemia Myocardial Reperfusion Injury ischemia Pharmacology 01 natural sciences Ventricular Function Left Article pressure Nifedipine Ventricular Pressure medicine Animals Immunology and Allergy Rats Wistar 010405 organic chemistry Chemistry Calcium channel steroid Biological activity General Medicine Levosimendan medicine.disease reperfusion 0104 chemical sciences Calcium Channel Agonists 010404 medicinal & biomolecular chemistry Ventricular pressure Milrinone calcium channel Reperfusion injury Naphthoquinones medicine.drug |
| Zdroj: | Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry |
| ISSN: | 1871-5230 |
| DOI: | 10.2174/1871523018666191003152854 |
| Popis: | Background: There is some experimental data on the effect exerted by some steroid derivatives against ischemia/reperfusion injury; however, the molecular mechanism is very confusing, perhaps this phenomenon could be due to the protocols used and/or differences in the chemical structure of each one of the steroid derivatives. Objective: The aim of this study was to synthesize a new bis-steroid-methanocyclobutanaphthalene- dione derivative using some tools chemical. Methodology: The biological activity exerted by the bis-steroid-methanocyclobutanaphthalene- dione derivative against ischemia/reperfusion injury was evaluated in an isolated heart model using noradrenaline, milrinone, dobutamine, levosimendan, and Bay-K- 8644 as controls. In addition, other alternative experiments were carried out to evaluate the biological activity induced by the bis-steroid-methanocyclobuta-naphthalene-dione derivative against left ventricular pressure in the absence or presence of nifedipine. Results: The results showed that 1) the bis-steroid-methanocyclobuta-naphthalene-dione derivative significantly decreases the ischemia-reperfusion injury translated as a decrease in the the infarct area in a similar manner to levosimendan drug; 2) both bis-steroidmethanocyclobuta- naphthalene-dione and Bay-K-8644 increase the left ventricular pressure and 3) the biological activity exerted by bis-steroid-methanocyclobuta-naphthalenedione derivative against left ventricular pressure is inhibited by nifedipine. Conclusion: In conclusion, the bis-steroid-methanocyclobuta-naphthalene-dione derivative decreases the area of infarction and increases left ventricle pressure via calcium channels activation; this phenomenon could constitute a new therapy for ischemia/reperfusion injury. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|