Abstract
The therapeutic effect of cardiac glycosides lies in their reversible inhibition on the membrane-bound Na+/K+-ATPase in human myocardium. Unfortunately, the utilization of steroidal cardiac glycosides suffers some severe adverse side effects. Magnesium lithospermateB (MLB), a derivative of caffeic acid tetramer found in Danshen (Salvia miltiorrhiza), is suggested to provide a comparable cardiac therapeutic effect by effectively inhibiting Na+/K+-ATPase via the same molecular mechanism triggered by cardiac glycosides. Molecular modeling suggests that ouabain, a cardiac glycoside, and MLB presumably bind to the same extracellular pocket of the Na+/K+-ATPase. Moreover, MLB outperforms ouabain in cell toxicity, and thus has a great potential, with extensive clinical trials, to become a safe substitute for cardiac glycosides. Neuroprotective effects of cardiac glycosides and MLB against ischemic stroke have been observed, and cumulative data suggest that effective inhibitors of Na+/K+-ATPase in the brain may be potential drugs for the treatment of ischemic stroke. Taken together, recent studies on MLB seem to promote a paradigm shift of searching potential drugs for the treatment of cardiac diseases from steroid-like compounds to non-steroid ones.
Keywords: Cardiac glycoside, Danshen, magnesium lithospermate B, Na+/K+-ATPase, ouabain, Salvia miltiorrhiza, MLB, Cell toxicity, Plausible biosynthetic pathway, Rosmarinic acid
Mini-Reviews in Organic Chemistry
Title:Magnesium Lithospermate B Extracted from Salvia Miltiorrhiza, A Potential Substitute for Cardiac Glycosides
Volume: 9 Issue: 2
Author(s): Tse-yu Chung, Feng-yin Li, Wen-Hua Chiou and Jason T.C. Tzen
Affiliation:
Keywords: Cardiac glycoside, Danshen, magnesium lithospermate B, Na+/K+-ATPase, ouabain, Salvia miltiorrhiza, MLB, Cell toxicity, Plausible biosynthetic pathway, Rosmarinic acid
Abstract: The therapeutic effect of cardiac glycosides lies in their reversible inhibition on the membrane-bound Na+/K+-ATPase in human myocardium. Unfortunately, the utilization of steroidal cardiac glycosides suffers some severe adverse side effects. Magnesium lithospermateB (MLB), a derivative of caffeic acid tetramer found in Danshen (Salvia miltiorrhiza), is suggested to provide a comparable cardiac therapeutic effect by effectively inhibiting Na+/K+-ATPase via the same molecular mechanism triggered by cardiac glycosides. Molecular modeling suggests that ouabain, a cardiac glycoside, and MLB presumably bind to the same extracellular pocket of the Na+/K+-ATPase. Moreover, MLB outperforms ouabain in cell toxicity, and thus has a great potential, with extensive clinical trials, to become a safe substitute for cardiac glycosides. Neuroprotective effects of cardiac glycosides and MLB against ischemic stroke have been observed, and cumulative data suggest that effective inhibitors of Na+/K+-ATPase in the brain may be potential drugs for the treatment of ischemic stroke. Taken together, recent studies on MLB seem to promote a paradigm shift of searching potential drugs for the treatment of cardiac diseases from steroid-like compounds to non-steroid ones.
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Chung Tse-yu, Li Feng-yin, Chiou Wen-Hua and T.C. Tzen Jason, Magnesium Lithospermate B Extracted from Salvia Miltiorrhiza, A Potential Substitute for Cardiac Glycosides, Mini-Reviews in Organic Chemistry 2012; 9 (2) . https://dx.doi.org/10.2174/157019312800604715
DOI https://dx.doi.org/10.2174/157019312800604715 |
Print ISSN 1570-193X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6298 |
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