1. A novel H2S releasing-monastrol hybrid (MADTOH) inhibits L-type calcium channels
- Author
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Taniris Cafiero Braga, Cristiane J. da-Silva, Leonardo da Silva Neto, José Evaldo Rodrigues De Menezes Filho, Silvia Guatimosim, Itamar Couto Guedes de Jesus, Ângelo de Fátima, Luzia V. Modolo, Paula Rhana, Jader S. Cruz, and Kathleen Viveiros Soares
- Subjects
0303 health sciences ,Chemistry ,Positive control ,chemistry.chemical_element ,General Chemistry ,Calcium ,010402 general chemistry ,01 natural sciences ,Catalysis ,0104 chemical sciences ,03 medical and health sciences ,chemistry.chemical_compound ,Monastrol ,Nifedipine ,Materials Chemistry ,medicine ,Biophysics ,L-type calcium channel ,030304 developmental biology ,medicine.drug - Abstract
A new alleged monastrol-H2S releasing hybrid, named MADTOH, was designed based on the structure of monastrol (M) and 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione (ADTOH) and synthesized in 7.8% overall yield. MADTOH was shown to be an H2S donor under physiological conditions. In addition, the hybrid causes a decrease in global calcium transient in cardiomyocytes similar to nifedipine (NIFE), taken as a positive control. Whole-cell voltage-clamp showed that MADTOH decreases L-type Ca2+ current in isolated ventricular cardiomyocytes.
- Published
- 2021