Design and synthesis of two new steroid derivatives with biological activity on heart failure via the M2-muscarinic receptor activation
| Autor: | Figueroa-Valverde Lauro, Diaz Cedillo Francisco, Garcimarero-Espino E. Alejandra, Ortiz-Ake Yazmin, Rosas-Nexticapa Marcela, Lopez-Gutierrez Tomas, Mateu-Armand Virginia, Lopez-Ramos Maria, García-Martínez Rolando |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Pharmacology
medicine.medical_treatment Organic Chemistry Clinical Biochemistry Ischemia 030209 endocrinology & metabolism Biological activity medicine.disease Biochemistry Yohimbine Steroid 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Endocrinology chemistry 030220 oncology & carcinogenesis Heart failure Muscarinic acetylcholine receptor medicine Methoctramine Ventricular pressure Molecular Biology medicine.drug |
| Zdroj: | Steroids. 158:108620 |
| ISSN: | 0039-128X |
| DOI: | 10.1016/j.steroids.2020.108620 |
| Popis: | Several drugs have been prepared to treat of heart failure using some protocols which require dangerous reagents and specific conditions. The aim of this study was to synthesize a series of steroid derivatives (compounds 2 to 18) using some chemical strategies. The biological activity of steroid derivatives against heart failure was evaluated using an ischemia/reperfusion model. In addition, the effect exerted by compounds 4 or 5 on left ventricular pressure was evaluated in the absence or presence of yohimbine, butaxamine and methoctramine. The results showed that 1) both compounds 4 or 5 significantly decrease the heart failure (translated as infarct area) compared with the compounds 2, 3 and 6–18. In addition, the compound 4 and 5 decreased the left ventricular pressure in a dose-dependent manner and this effect was significantly inhibited in the presence of methoctramine (p = 005). In conclusion, the compounds 4 or 5 decrease both the infarct area and left ventricular pressure via M2-muscarinic receptor activation. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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