title: Study on the physicochemical properties and anti-inflammatory effects of paeonol in rats with TNBS-induced ulcerative colitis.
abstract: 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-β1) 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-β1 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.
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China; School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: zongsy114@163.com.
authors.forename: Shi-Yu
authors.initials: SY
authors.lastname: Zong
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: puyiq@163.com.
authors.forename: Yi-Qiong
authors.initials: YQ
authors.lastname: Pu
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: xbl2004000@126.com.
authors.forename: Ben-Liang
authors.initials: BL
authors.lastname: Xu
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China; School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: zhangtdmj@hotmail.com.
authors.forename: Tong
authors.initials: T
authors.lastname: Zhang
authors.affiliation: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China; School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: annabel_cn@163.com.
authors.forename: Bing
authors.initials: B
authors.lastname: Wang
mesh_terms: D000098:Acetophenones / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000627:therapeutic use*; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy*; D003106:Colon / Q000187:drug effects* / Q000473:pathology; D004195:Disease Models, Animal; D006801:Humans; D020381:Interleukin-17 / Q000097:blood; D015850:Interleukin-6 / Q000097:blood; D008297:Male; D029596:Paeonia / Q000276:immunology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D053773:Transforming Growth Factor beta1 / Q000378:metabolism; D014302:Trinitrobenzenesulfonic Acid
chemical_list: D000098:Acetophenones; D000893:Anti-Inflammatory Agents; D020381:Interleukin-17; D015850:Interleukin-6; D053773:Transforming Growth Factor beta1; C013638:paeonol; D014302:Trinitrobenzenesulfonic Acid
keywords: 2,4,6-trinitrobenzene sulfonic acid; Paeonol; Physicochemical properties; Ulcerative colitis