title: Effect of chito-oligosaccharide on the oral absorptions of phenolic acids of Flos Lonicerae extract.
abstract: Phenolic acids, the main active ingredients in Flos Lonicerae extract possess strong antibacterial, antioxidant and antiviral effects, and their contents was higher largely than that of other ingredients such as flavones, but the absolute bioavailability orally was significantly low, which is significant low influencing clinical efficacies of its oral preparations. In the present study, in vitro Caco-2 cell, in situ single-pass intestinal perfusion and in vivo pharmacokinetics study were performed to investigate the effects of COS on the intestinal absorption of phenolic acids. The pharmacological effects such as antiviral activity improvement by COS were verified by MDCK cell damage inhibition rate after influenza virus propagation. The observations from in vitro Caco-2 cell showed that the absorption of phenolic acids in Flos Lonicerae extract could be improved by COS. Meanwhile, COS at the same low, medium and high concentrations caused a significant, concentration-dependent increase in the Papp-value for phenolic acids compared to the control group (p<0.05), and was all safe for the Caco-2 cells. The observations from single-pass intestinal perfusion in situ model showed that the intestinal absorption of phenolic acids can be enhanced by COS. Meanwhile, the absorption enhancing effect of phenolic acids might be saturable in different intestine sites. In pharmacokinetics study, COS at dosage of 25 mg/kg improved the bioavailability of phenolic acids in Flos Lonicerae extract to the greatest extent, and was safe for gastrointestine from morphological observation. Besides, treatment with Flos Lonicerae extract with COS at dosage of 25 mg/kg prevented MDCK cell damage upon influenza virus propagation better than that of control. All findings above suggested that COS at dosage of 25 mg/kg might be safe and effective absorption enhancer for improving the bioavailability of phenolic acids and the antiviral activity in vitro in Flos Lonicerae extract.
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, PR China; Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhou
authors.affiliation: First Medicine College, Nanjing University of Chinese Medicine, Nanjing 210046, PR China.
authors.forename: Jinjun
authors.initials: J
authors.lastname: Shan
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Meteria Medica, Jiangsu Provinical Academy of Chinese Medicine, PR China.
authors.forename: Xiaobin
authors.initials: X
authors.lastname: Tan
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, PR China; Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, PR China.
authors.forename: Jiashuang
authors.initials: J
authors.lastname: Zou
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China.
authors.forename: Ailing
authors.initials: A
authors.lastname: Yin
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China.
authors.forename: Baochang
authors.initials: B
authors.lastname: Cai
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, PR China; Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, PR China. Electronic address: diliuqing@hotmail.com.
authors.forename: Liuqing
authors.initials: L
authors.lastname: Di
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D018938:Caco-2 Cells; D048271:Chitosan / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D035264:Flowers; D006801:Humans; D062385:Hydroxybenzoates; D007408:Intestinal Absorption; D031239:Lonicera / Q000737:chemistry*; D009844:Oligosaccharides / Q000494:pharmacology*; D010636:Phenols / Q000493:pharmacokinetics*; D010936:Plant Extracts / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D062385:Hydroxybenzoates; D009844:Oligosaccharides; D010636:Phenols; D010936:Plant Extracts; D048271:Chitosan; C017616:phenolic acid
keywords: Antiviral activity; Chito-oligosaccharide; Flos Lonicerae extract; Phenolic acids; Tight junction
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