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Following numerous experimental observations that various non-steroidal anti-inflammatory drugs have antitumor potentials, a series of fenoprofenamides (1a-g) and ketoprofenamides (2a-c) was tested on proliferation of different human tumor cell lines and normal human fibroblasts in vitro. Fenoprofen and ketoprofen showed modest antiproliferative activity, whereas the growth inhibitory activity of the tested amides clearly demonstrates that the substituents linked by an amide bond are essential for the significantly stronger cytostatic activity, probably because of a greater lipophilicity and/or better cell uptake. Additionally, it was shown that the most active derivatives (1d and 2a) induced cell cycle arrest at the G1 phase, as well as apoptosis.

By using HPLC/UV-VIS, Croatian barberry (Berberis croatica Horvat) was found to be a new source of the bioactive alkaloid berberine. Comparison of berberine content in roots, leaves, and twigs between wild specimens of B. croatica and B. vulgaris collected in Croatia showed that the roots of both species contained the highest berberine content (B. croatica 1.120-1.217%; B. vulgaris 0.805-1.424%), followed by twigs (B. croatica 0.049-0.216%; B. vulgaris 0.077-0.112%). While the berberine content in the leaves of both species was very low (between 0.002% and 0.044%), they were found to be rich in phenols and flavonols. The Student's t-test showed a significant difference at P \ 0.05 for phenol and flavonol content in the plant organs, both between species and within species. Leaf samples were most variable, while root samples were the least. Extracts from the roots of both barberry species expressed antimicrobial activity against Bacillus subtilis NCTC 8236, Staphylococcus aureus ATCC 6538, Escherichia coli ATCC 10535, Pseudomonas aeruginosa ATCC 27853 and Candida albicans ATCC 10231. Antimicrobial activity of leaf extracts was species-dependent. Root extracts of both species also showed lower MIC values than other extracts (MIC B 87.5 mg/ml).

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An improved method of piroxicam benzoate synthesis was described, and an isocratic reversed-phase high-performance liquid chromatography method for its determination was developed and fully validated. The method was found to be specific, precise (relative standard deviation 0.3%), accurate (mean recovery 99.9%), and robust. Limit of detection was estimated at 0.055 microg mL(-1) and limit of quantification at 0.185 microg mL(-1). The kinetics of piroxicam benzoate hydrolysis in aqueous buffer solutions (pH 1.1 and 10), simulated gastric and intestinal fluids was studied. The hydrolysis followed first-order kinetics. The following rate constants were obtained at pH 10: k = 1.8 x 10(-3) hr(-1) at 37 degrees C and k = 3.4 x 10(-2) hr(-1) at 60 degrees C. In acidic media, no significant hydrolysis was observed after 24 hr. During the 24-hr period in simulated intestinal fluid, only 10.9% of the starting ester was hydrolyzed.

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