Synthesis and Biological Activity of a Bis-steroid-Methanocyclobutanaphthalene- dione Derivative against Ischemia/Reperfusion Injury via Calcium Channel Activation

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Author(s): Figueroa-Valverde Lauro*, Diaz-Cedillo Francisco, Rosas-Nexticapa Marcela, Mateu-Armand Virginia, Garcimarero-Espino E. Alejandra, Lopez-Ramos Maria, Hau-Heredia Lenin, Borges-Ballote Yaritza, Cabrera-Tuz Jhair.

Journal Name: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents)

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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 to differences in the chemical structure of each one of the steroid derivatives.

Objective: The aim of this study was synthesizing a new bis-steroid-methanocyclobuta-naphthalene-dione derivative using some tools chemical.

Methodology: The biological activity exerted by the bis-steroid-methanocyclobuta-naphthalene-dione derivative against ischemia/reperfusion injury was evaluated in an isolated heart model using noradrenaline, milrinone, dobutamine, levosimedan, 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 decrease the ischemia-reperfusion injury translated as decrease the infarct area in a similar manner that levosimedan drug; 2) both bis-steroid-methanocyclobuta-naphthalene-dione and Bay-K-8644 increase the left ventricular pressure and 3) the biological activity exerted by bis-steroid-methanocyclobuta-naphthalene-dione derivative against left ventricular pressure was inhibited by nifedipine.

Conclusion: The bis-steroid-methanocyclobuta-naphthalene-dione derivative decreases the area of infarction and increase left ventricle pressure via calcium channels activation; this phenomenon could constitute a new therapy for ischemia/reperfusion injury.

Keywords: steroid, ischemia, reperfusion, infarct, pressure, bis-steroid-methanocyclobuta-naphthalene-dione

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(E-pub Ahead of Print)
DOI: 10.2174/1871523018666191003152854

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