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Horm Metab Res 2012; 44(12): 879-884
DOI: 10.1055/s-0032-1312624
Original Basic
© Georg Thieme Verlag KG Stuttgart · New York

Stimulatory Effect of Allantoin on Imidazoline I1 Receptors in Animal and Cell Line

T. T. Yang
1   The School of Chinese Medicine for Post-Baccalaureate, I-Shou University, Yanchao, Kaohsiung City, Taiwan
,
N. H. Chiu
2   Department of Applied Cosmetology, Hwa Hsia Institute of Technology, Chung Ho, Taipei City, Taiwan
,
H. H. Chung
3   Institute of Basic Medical Sciences, College of Medicine, National Cheng Kung University, Tainan City, Taiwan
,
C. T. Hsu
4   Department of Pathology, Edah University Medical Center, Yanchao, Kaohsiung City, Taiwan
,
W. J. Lee
5   Department of Emergency Medicine and Medical Research, Chi-Mei Medical Center, Yong Kang, Tainan City, Taiwan
,
J.-T. Cheng
3   Institute of Basic Medical Sciences, College of Medicine, National Cheng Kung University, Tainan City, Taiwan
5   Department of Emergency Medicine and Medical Research, Chi-Mei Medical Center, Yong Kang, Tainan City, Taiwan
6   Institute of Medical Science, College of Health Science, Chang Jung Christian University, Guei-Ren, Tainan City, Taiwan
› Author Affiliations
Further Information

Publication History

received 26 March 2012

accepted 19 April 2012

Publication Date:
15 May 2012 (online)

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Abstract

Allantoin is known as the agonist of imidazoline receptor, especially the I2 subtype. Effect of allantoin on imidazoline I1 receptor (I1R) relating to reduction of blood pressure and its merit in steatosis are still obscure. Also, farnesoid X receptor (FXR) plays an important role in lipid homeostasis related to I1R activation. Thus, we administered allantoin into high fat diet (HFD)-fed mice showing hypertriglyceridemia and hypercholesterolemia. Allantoin significantly improved hyperlipidemia in HFD mice after 4 weeks of administration. Pretreatment with efaroxan, at a dose sufficient to inhibit I1R activation, attenuated the action of allantoin. In addition, in cultured HepG2 cells, allantoin increased the expression of farnesoid X receptor (FXR). The allantoin-induced FXR expression was blocked by efaroxan. Similar changes were observed in the expressions of FXR-targeted genes. Otherwise, allantoin also lowered systolic blood pressure (SBP) in HFD mice that can be blocked by efaroxan. Taken together, allantoin has an ability to activate I1R for improvement of metabolic disorders.

Key words

allantoin - blood pressure - efaroxan - farnesoid X receptor (FXR) - imidazoline receptor - steatosis
 

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