02551nas a2200241 4500008004100000245011700041210006900158260001800227300001000245490000600255520178200261653002102043653002102064653003702085653002302122653001402145100001902159700001902178700001602197700001602213700001602229856006402245 2016 eng d00aThe Effect of Ultrafine Process on the Dissolution, Antibacterial Activity, and Cytotoxicity of Coptidis rhizoma0 aEffect of Ultrafine Process on the Dissolution Antibacterial Act cDecember 2015 a71-770 v83 a

Background: The dosage of herb ultrafine particle (UFP) depended on the increased level of its dissolution, toxicity, and efficacy. Objective: The dissolution, antibacterial activity, and cytotoxicity of Coptidis rhizoma (CR) UFP were compared with those of traditional decoction (TD). Materials and Methods: The dissolution of berberine (BBR) of CR TD and UFP was determined by high‑performance liquid chromatography. The antibacterial activity of CR extract was assayed by plate‑hole diffusion and broth dilution method; the inhibitory effect of rat serums against bacteria growth was evaluated after orally given CR UFP or TD extract. The cytotoxicity of CR extract was evaluated by 3‑(4,5‑dimethylthiazol‑2‑Yl)‑2,5‑diphenyltetrazolium bromide assay. Results: The dissolution amount of BBR from CR UFP increased 6–8‑folds in comparison to TD at 2 min, the accumulative amount of BBR in both UFP and TD group increased in a time‑dependent manner. The minimal inhibitory concentrations and minimal bactericidal concentrations of CR UFP extract decreased to 1/2~1/4 of those of TD extract. The inhibitory effect of rat serums against bacteria growth decreased time‑dependently, and no statistical difference was observed between two groups at each time point. The 50% cytotoxic concentrations of UFP extract increased 1.66~1.97 fold than those of TD. Conclusions: The antibacterial activity and cytotoxicity of CR UFP increased in a dissolution‑effect manner in vitro, the increased level of cytotoxicity was lower than that of antibacterial activity, and the inhibitory effect of rat serums containing drugs of UFP group did not improve.

10aCoptidis rhizoma10aDissolution rate10aMinimal inhibitory concentration10aSerum pharmacology10aUltrafine1 aJiang, Zhen-Yu1 aDeng, Hai-Ying1 aYu, Zhi-Jun1 aNi, Jun-Yan1 aKang, Si-He uhttps://phcogres.com/article/2016/8/1/1041030974-8490171097