[Prodrug structural modifications of cyclovirobuxine D and their biological activity].

Abstract

AIM:

To search for compounds for the treatment of cardiovascular diseases through prodrug structural modifications of cyclovirobuxine D, a single efficient composition distilled from Box plant in China, which was used to treat angina and myocardial infarction.

METHODS:

According to prodrug design principle, a series of cyclovirobuxine D analogues were prepared, suc as succinate, phosphate and amino acid ester, and their biological activities were tested.

RESULTS:

Seven new compounds were obtained and confirmed with 1H NMR, MS, and element analysis.

CONCLUSION:

In pharmacology experiment, for treating arrhythmia induced by aconitine, succinate and amino acid ester of cyclovirobuxine D (I and VII) showed better activities than that of cyclovirobuxine D. The normal rhythm of the heart duration of I and VII were ( 11.53 +/- 7.62) min and (12.68 +/- 9.25) min, compared with 0.9% NaCl solution and cyclovirobuxine D, (2.36 +/- 1.68) min and (10.25 +/- 6.59) min (P < 0.01), respectively. Another pharmacology experiment, for treating arrhythmia induced by chloroform, the negative ratio of I and VII were 80% and 82%, compared with 0.9% NaCl solution and cyclovirobuxine D, 43% and 52% (P < 0.05), respectively. The difference between new compounds and cyclovirobuxine D was distinct.

• Authors: Lan Deng, Heng Huang, Ming-Xia Xu, Shi-Qing Zhou, Fang Ren, Xing-Wen Wang, Dai-Qing Li
• Journal: Yao xue xue bao = Acta pharmaceutica Sinica (Yao Xue Xue Bao) Vol. 40 Issue 9 Pg. 820-4 (Sep 2005) ISSN: 0513-4870 [Print] China
• PMID: 16342684 (Publication Type: Journal Article)

Chemical References

• Anti-Arrhythmia Agents
• Drugs, Chinese Herbal
• Prodrugs
• cyclovirobuxine D
• Chloroform
• Aconitine

Topics

• Aconitine
• Animals
• Anti-Arrhythmia Agents (chemical synthesis, pharmacology)
• Arrhythmias, Cardiac (chemically induced, physiopathology)
• Buxus (chemistry)
• Chloroform
• Drugs, Chinese Herbal (chemical synthesis, pharmacology)
• Female
• Heart Rate (drug effects)
• Male
• Mice
• Plants, Medicinal (chemistry)
• Prodrugs (chemical synthesis, pharmacology)
• Random Allocation
• Rats
• Rats, Sprague-Dawley