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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.

Aim: To search for new compounds for the treatment of cardiovascular diseases by structural modification of cyclovirobuxine D., Methods: According to rational drug design principle, a series of cyclovirobuxine D analogues were prepared, and their bioactivities were tested., Results: Ten new compounds were syntheized and confirmed by spectra., Conclusion: Endurance lacking oxygen activity and antiarrhythmia effects of some analogues of cyclovirobuxine D were tested. Some compounds showed better activity than cyclovirobuxine D.

The effects of vasoactive agents propranolol hydrochloride and angiotensin (AT-II) on improving the directed therapy of cancer with the use of conjugate of gastric cancer monoclonal antibody (3H11) and mitomycin C (MMC) were studied. The antibody activity of the conjugate (3H11-HSA-MMC) was retained with the molecular ratio of 1:2:60. In tests with tumor-bearing nude mice, the tumor inhibitory rate of the conjugate alone was found to be 50%, while in conjugate treated mice that also received propranolol or AT-II the tumor inhibitory rate were 79% and 60%, respectively. In tumor-bearing nude mice given 131I-3H11 both propranolol and AT-II increased the tumor uptake of 131I-3H11. These results indicate that these vasoactive agents can change the tissue perfusion ratio via the effect on tumor blood vessels and increase the access of the conjugate to tumor, thereby, enhancing the effectiveness of tumor directed therapy with the use of conjugates.

The compounds of quinolone class, which were studied extensively and developed very quickly in the last decades, showed high activity, low toxicity and broad antibacterial spectrum. About thirty new compounds of 1,7-disubstituted-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acids were synthesised and evaluated in vitro against S. aureus 25923, E. coli-25922 and P. aeruginosa. Their activities were low. The minimum inhibitory concentrations (MIC microgram/ml) of these compounds against Gram-positive bacteria were higher than those against Gram-negative bacteria. The relative in vitro activity contributed by 1-benzyl was: benzyl greater than p-chlorobenzyl greater than p-nitrobenzyl groups.