Studies on flavonoids from Derris eriocarpa / 中国中药杂志

Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before. In our further research on the ethyl acetate of this plant, nine flavone compounds were obtained by column chromatography on silica gel, Sephadex LH-20, semi-prep HPLC, polyamide column chromatography and recrystallization for separation and purification. The structures were determined on the basis of extensive spectroscopic analysis, including MS, NMR experiments and comparison with spectroscopic data in the literature, respectively, as diosmetin (1), 3, 3'-di-O-methylquercetin (2), afromosin (3), 6, 3'-dihydroxy-7, 4'-dimethoxyisoflavone (4), odoratin (5), 7, 3'-dihydroxy-8, 4'-dimethoxyisoflavone (6), 6, 4'-dihydroxy-7, 3'-dimethoxyisoflavone (7), 5, 7, 4'-trihydroxy-3, 3', 5'-trimethoxyflavone (8), and alpinumisoflavone (9). All these compounds were isolated from Derris eriocarpa How for the first time. And the in vitro assays showed that compound 2 possessed moderate inhibitory activity against human cancer cells K562 and HEL.

Study on skin toxicology and penetration enhancement of skin absorption of volatile oil extracted from tender branchers of Camellia oleifera / 中国中药杂志

<p><b>OBJECTIVE</b>To study the toxicity on skin and penetration effect of volatile oil from tender branchers of Camellia oleifera on nitrendipine, baicalin, nimesulide for percutaneous obsorption.</p><p><b>METHOD</b>Acute skin toxicity, irritation and allergy on rats were tested, and mouse skin in vitro was applied for studying the effects of different concentrations of volatile oil in nitrendipine, baicalin, nimesulide on drug permeation.</p><p><b>RESULT</b>Different dosage volatile oil had no acute toxicity, irritation or hypersensitive effects. Compared to azone, more powerful enhancement effects of volatile oil at different concentration on nitrendipine, baicalin, nimesulide were very obvious.</p><p><b>CONCLUSION</b>This paper firstly reported the results of experiment about the toxicity to skin and penetr-ation effect of volatile oil from tender branches of C. oleifera.</p>

Structure-activity relationships of salicylic acid and its analogs in the inhibitory action on beta-lactamase / 药学学报

<p><b>AIM</b>Nineteen compounds related to salicylic acid were evaluated for their in vitro activity of inhibiting beta-lactamase isolated from a resistant strain of Pseudomonas aeruginosa, and their structure-activity relationships were examined.</p><p><b>METHODS</b>Nitrocefin method was used.</p><p><b>RESULTS</b>The 50% inhibitory concentration (IC50) of salicylic acid inhibiting beta-lactamase was 22 mmol x L(-1); four analogs had IC50 lower than that of salicylic acid; fifteen analogs had IC50 higher than that of salicylic acid.</p><p><b>CONCLUSION</b>Examination of the structure-activity relationships of the compounds revealed that carboxyl group and adjoining hydroxyl group were active group, and replacement of adjoining hydroxyl by carboxyl increased activity nearly 4-fold. Moreover, addition of a sulfonic group at C-5 and nitro group at C-3, 5 of benzenoic ring of salicylic acid resulted in a 2-fold to 3-fold increase in activity, addition of a amino group at C-5 of benzenoic ring of salicylic acid decreased activity, add addition of -Cl or -F at C-2,4 position of benzenoic ring of benzoic acid did not show activity.</p>