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Synthesis and biological evaluation of the codrug of Leonurine and Aspirin as cardioprotective agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Oct 01; Vol. 26 (19), pp. 4650-4654. Date of Electronic Publication: 2016 Aug 21. - Publication Year :
- 2016
-
Abstract
- The novel codrugs of Leonurine and Aspirin, compounds 545 and 503 have been synthesized and evaluated on their cardioprotective effects. Preliminary pharmacological studies showed that both compounds 545 and 503 were able to increase cell viability of hypoxia-induced H9c2 cells, and compound 545 exhibited at least ten fold potency than 503 and their parent drugs (Leonurine and Aspirin). Further mechanisms studies indicated that the cardioprotective effect of 545 due to its (1) anti-oxidative ability by increasing SOD and CAT enzymes activity and decreasing MDA content and LDH leakage rate, (2) anti-apoptosis activity by regulating apoptosis-associated proteins expression during hypoxia, (3) anti-inflammatory effect by suppression of pro-inflammatory mediators. All of these results demonstrate that compound 545 as a new class of Leonurine analogue could be a drug candidate in our further drug development studies.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Apoptosis drug effects
Catalase metabolism
Cell Line
Gallic Acid pharmacology
Humans
Inflammation Mediators antagonists & inhibitors
Inflammation Mediators metabolism
L-Lactate Dehydrogenase metabolism
Oxidative Stress drug effects
Reactive Oxygen Species metabolism
Superoxide Dismutase metabolism
Aspirin pharmacology
Cardiotonic Agents chemical synthesis
Cardiotonic Agents pharmacology
Gallic Acid analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 26
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 27575471
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.08.058