Study on the physicochemical properties and anti-inflammatory effects of paeonol in rats with TNBS-induced ulcerative colitis.

Paeonol, an active component from Paeonia suffruticosa Andr., has a variety of biological activities, such as vascular endothelial cell protection, anti-oxidation, and anti-inflammation. The aim of this study was to investigate the basic physicochemical properties of paeonol, including solubility, oil-water partition coefficient, and permeability. Then evaluated the anti-inflammatory effects of paeonol were evaluated on 2,4,6-trinitrobenzenesulfonic acid-induced ulcerative colitis in rats. The rats were divided randomly into 6 groups, namely, normal, model, paeonol-treated (100, 200, and 400mg/kg), and positive. Each group had 10 rats. Inhibition effects were evaluated by the disease activity index (DAI), colon weight/length ratio, as well as macroscopical and histological evaluations. Serum interleukin (IL)-17, IL-6 and transforming growth factor beta 1 (TGF-ß1) levels were determined by enzyme-linked immunosorbent assay. The solubility and oil-water partition coefficient of paeonol in different phosphate buffer solutions were 284.06-598.23 and 461.97-981.17µg/mL, respectively. The effective passive permeability value Pe was 23.49×10-6cm/s. In terms of anti-inflammatory results, compared with the model group, treatment with 200 and 400mg/kg doses of paeonol had significantly decreased DAI, colon weight/length ratio, and macroscopic and histopathological scores. Furthermore, the serum levels of IL-17 and IL-6 were significantly reduced, whereas the TGF-ß1 level was increased in the two paeonol-treated groups (medium- and high-dose group). Therefore, paeonol had poor water solubility, but oral absorption was good. In addition, paeonol had therapeutic effects on ulcerative colitis, and the therapeutic efficacy was dose dependent. The results presented in this study provide evidence for the development of a novel therapeutic agent in the treatment of UC. However, whether this agent could have therapeutic benefit or adverse effects in human IBD remains to be fully explored.

[Optimization of Ethanol Extraction and Water Extraction Technologies of Zuogui Pills by Orthogonal Test].

OBJECTIVE: To optimize the ethanol extraction and water extraction technologies of Luogui Pills. METHODS: An orthogonal test was used to study the influence of ethanol concentration, amount of ethanol and reflux time on hyperoside in Cuscutae Semen, ursolic acid in Corni Fructus and the yield of dry paste. Also, The effect of soaking time, amount of water and extraction time on acteoside in Rehmanniae Radix Praeparata and the yield of dry paste were investigated. All these factors were adopted as the indices for choosing the best ethanol extraction and water extraction technologies. RESULTS: The best ethanol extraction technology for Cuscutae Semen, Corni Fructus and Achyranthis Bidentatae Radix was reflux extracting for 1 h each time for two times with eight times of 70% ethanol. The best water extraction technology for the residue and the rest herbs after the ethanol extraction was soaking for 0. 5 h and then decocting for 0. 5 h each time for two times with twelve times of water. CONCLUSION: The optimal extraction technologies are stable and feasible, the extraction rate of the alcohol soluble and water soluble effective components is high, and it provides the reference basis for the secondary development of Zuogui Pills.