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Enhancement by adrenaline of ginsenoside Rg1 transport in Caco-2 cells and oral absorption in rats

2009; Oxford University Press; Volume: 61; Issue: 3 Linguagem: Inglês

10.1211/jpp/61.03.0009

2042-7158

Jing Xiong, Minjie Sun, Zhixiong Guo, Luosheng Huang, Shujing Wang, Boyu Meng, Qineng Ping,

Adenosine and Purinergic Signaling

Journal of Pharmacy and PharmacologyVolume 61, Issue 3 p. 347-352 Enhancement by adrenaline of ginsenoside Rg1 transport in Caco-2 cells and oral absorption in rats Jing Xiong, Jing Xiong Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorMinjie Sun, Minjie Sun Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorJianxin Guo, Jianxin Guo Technology Department, Talecris Biotherapeutics, Clayton, North Carolina, USASearch for more papers by this authorLuosheng Huang, Luosheng Huang Department of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorShujing Wang, Shujing Wang Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorBoyu Meng, Boyu Meng Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorQineng Ping, Corresponding Author Qineng Ping Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaCollege of Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009 China. E-mail: [email protected]Search for more papers by this author Jing Xiong, Jing Xiong Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorMinjie Sun, Minjie Sun Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorJianxin Guo, Jianxin Guo Technology Department, Talecris Biotherapeutics, Clayton, North Carolina, USASearch for more papers by this authorLuosheng Huang, Luosheng Huang Department of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorShujing Wang, Shujing Wang Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorBoyu Meng, Boyu Meng Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaSearch for more papers by this authorQineng Ping, Corresponding Author Qineng Ping Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. ChinaCollege of Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009 China. E-mail: [email protected]Search for more papers by this author First published: 08 January 2010 https://doi.org/10.1211/jpp.61.03.0009Citations: 9Read the full textAboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat Abstract Objectives The purpose of this research was to evaluate the ability of adrenaline (epinephrine) to stimulate the uptake of ginsenoside Rg1 (Rg1) by Caco-2 cells. Methods Rg1 uptake was measured using Caco-2 cell monolayers. The Rg1 uptake medium with adrenaline at different concentrations was added to each well and incubated for different time intervals. Adrenergic antagonists such as phentolamine and propranolol were added to the incubation medium to investigate their effects on Rg1 uptake. The Rg1 concentration in the monolayers was determined by high-performance liquid chromato-graphy. Transport of Rg1 across Caco-2 cells was also studied and an oral bioavailability study of Rg1 was carried out in rats. Key findings The incubation medium with adrenaline remarkably increased the amount of Rg1 uptake by Caco-2 cells. Adrenaline-induced Rg1 transport increased in a dose- and time-dependent manner. The effect of adrenergic antagonists on adrenaline-induced uptake of Rg1 was investigated and it was found that the enhancement effect was attenuated by the co-treatment with propranolol but not phentolamine. The transport amount of Rg1 by Caco-2 cells increased in response to 1 mM adrenaline, isoproterenol or salbutamol. In contrast, 1 mM phenylephrine had no effect on Rg1 transport in Caco-2 cells. The effect of adrenaline on the absorption of Rg1 was further investigated in vivo in rats. The co-administration with adrenaline in rats showed that the oral bioavailability was increased remarkably relative to the aqueous solution. The area under the plasma concentration-time curve of Rg1 after co-administration with 1 mM adrenaline was 79.1 ± 31.04 μg/ml/h compared with 2.81 ± 1.13 μg/ml/h for its aqueous solution. Conclusions Adrenaline is effective for the stimulation of intestinal absorption of Rg1 and the enhanced absorption is mediated mainly by the interaction of adrenaline with β2-adrenoceptors. Citing Literature Volume61, Issue3March 2009Pages 347-352 RelatedInformation