ABSTRACT
Chemical modification was performed for improving the antioxidant activity of lead compound glycyrrhetinic acid (Ib). Two conjugated diene derivatives were prepared by reduction and dehydration reactions. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA probe, while evaluating the capacity to inhibit reactive oxygen species (ROS) formation. The initial result showed that the two homo- and heterocyclic diene derivatives--18beta-olean-11,13(18)-diene-3beta, 30-diol (IV) and 18beta-olean-9 (11), 12-diene-3beta, 30-diol (V) exhibited strong antioxidant activities, at a concentration of 1.0 mg x mL(-1), they inhibited free radical (ROS) formation by 45% and 41%, respectively. In the same conditions, the lead compound (Ib) and the reference vitamin E inhibited ROS activity by 31% and 32%. Our results suggest that the elimination of the 11-keto group and the chemical reduction of 30-carboxylic group into hydroxyl function can increase the antioxidant activity of Ib significantly.
Subject(s)
Animals , Male , Rats , Antioxidants , Pharmacology , Glycyrrhetinic Acid , Microsomes, Liver , Metabolism , Reactive Oxygen Species , Metabolism , Triterpenes , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To establish the HPLC fingerprint of Xuelian injection.</p><p><b>METHOD</b>HPLC with Diamonsil C18 (4.6 mm x 250 mm, 5 microm) column was used, the methanol-1% acetic acid as a mobile phase and detection wavelength at 270 nm.</p><p><b>RESULT</b>Indicating 11 peaks on HPLC fingerprint.</p><p><b>CONCLUSION</b>This method is simple and acurate with a good reproducibility and can be used as a quality control method for Xuelian injection.</p>
Subject(s)
Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Chemistry , Injections , Plants, Medicinal , Chemistry , Quality Control , Saussurea , ChemistryABSTRACT
<p><b>AIM</b>To prepare the target drug delivery systems(TDDS), albendazole polybutycyanocrylate nanoparticles (ABZ-PBCA-NP), its pharmaceutical characters and tissue distributions were simultaneously investigated.</p><p><b>METHODS</b>Albendazole nanoparticles were prepared with the emulsification-polymerization method and the drug-load mechanism of polybutycyanocrylate nanoparticles was studied with the equal-tempaerature adsorption principle. The dialyse dynamic of albendazole from ABZ-PBCA-NP was investigated in four formulations in vitro. The tissue distribution of albendazole in different drug vehicles was studied with isotope labelling experiment.</p><p><b>RESULTS</b>ABZ-PBCA-NP and ABZ-PVP-PBCA-NP fit to the Higuchi and bi-exponent function in vitro respectively. The drug loaded in nanoparticles was abide by the Langmuir adsorption equation. Targeting index of albendazole in liver and spleen in mice are 11.4 and 3.9 after ig 3H-ABZ-PBCA-NP. The bioavailability of albendazole nanoparticle and suspension are 76.0% and 36.9% respectively.</p><p><b>CONCLUSION</b>The absorptive capability of drug was enhance when 4% PVP was added into the nanoparticle, and its release time was lengthen. At the same time, the nanoparticles vehicles increase the albendazole bioavailability.</p>