A study of anti-diabetic activity of gensinoside by assessing sodium-glucose symporter blocking effect in silico and in rat intestinal model

American Journal of BioMedicine  Volume 2, Issue 8, pages 984-991, August 2014


Sahar A. majeed; Heider S Qassam; Karrar Kareem Gaen; Khalida Kadhim; Fadhaa Abdul Ameer; Ikhlas Hassan; Hussein Abdul Kadhim

Abstract

Diabetes mellitus has repeatedly attracted attention of researchers to design different therapeutic approaches to achieve an optimal treatment for this serious health challenge. The purpose of the study is to evaluate treatment option for controlling hyperglycemia at site of glucose absorption through designing computerized and in vivo models to test a sodium-glucose symporter based drug design. In silico protein data bank (pdb) model of SGLUT was processed and analyzed for docking with edited test glycoside. Another model included determination of the dose-response relationship in rat intestinal glucose/saline perfusion with test glycoside. Our result showed that Ginsenoside revealed a dose dependent SGLUT blocking activity in a saturation kinetics curve, which was agreed with in silico model results.

Keywords: SGLUT; Gensinoside; Perfusate glucose; ICM docking


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References

1. Wild S, Roglic G, Green A, Sicree R, King H. Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes care 2004; 27(5): 1047-1053. [PubMed]

2. Dyck R, Osgood N, Lin TH, Gao A, Stang MR. Epidemiology of diabetes mellitus among First Nations and non-First Nations adults. CMAJ 2010;182(3):249-56. [PubMed]

3. Wild S, Roglic G, Sicree R, Green R,  King H. Global burden of diabetes mellitus in the year 2000. Global Burden of Disease 2000.1-28.

4. Anthony J, Kelkar A, Wilankar C, Ranjith V, Bhumra SK, Mutt S, Deka N. Discovery of p1736, a novel antidiabetic compound that improves peripheral insulin sensitivity in mice models. PLoS One 2013;8(10):e77946. [PubMed]

5. Yang W, Liu J, Shan Z, Tian H, Zhou Z, Ji Q. Acarbose compared with metformin as initial therapy in patients with newly diagnosed type 2 diabetes: an open-label, non-inferiority randomised trial. Lancet Diabetes Endocrinol 2014 ;2(1):46-55. [PubMed]

6. Shirazi-Beechey SP, Moran AW, Bravo D, Al-Rammahi M. Nonruminant Nutrition Symposium: intestinal glucose sensing and regulation of glucose absorption: implications for swine nutrition. J Anim Sci 2011;89(6):1854-62. [PubMed]

7. Dyer J, Daly K, Salmon KS, Arora DK, Kokrashvili Z, Margolskee RF, Shirazi-Beechey SP. Intestinal glucose sensing and regulation of intestinal glucose absorption. Biochem Soc Trans 2007;35(Pt 5):1191-4. [PubMed]

8. Andrei A. Gruzdkov, Liudmila V. Gromova, Nadezhda M. Grefner, Yan Yu. Komissarchik. Kinetics and mechanisms of glucose absorption in the rat small intestine under physiological conditions. JBPC 2012;3(2): 191-200. [Abstract/Full-Text]

9. Jolla L. Molsoft ICM Workshop – Protein Structure and Drug Discovery. Molsoft ICM 2006; 29:14:46.

10. Jessing K, Ehrenkrantz J. Quantitation of Phlorizin and Phloretin in Human Plasma and Urine. Web WWW.Tandemlabs.com.

11. Buller CL. Role of GLUT1 in the Mammalian Target of Rapamycin  Pathway: Mechanisms of Regulation. [website]

12. Lee CH, Kim JH. A review on the medicinal potentials of ginseng and ginsenosides on cardiovascular diseases. Journal of Ginseng Research 2014; 38(3): 161–166. [Abstract/Full-Text]

13. Hwang CR, Lee SH, Jang GY, Hwang IG, Kim HY, Changes in ginsenoside compositions and antioxidant activities of hydroponic-cultured ginseng roots and leaves with heating temperature. Journal of Ginseng Research 2014; 38:180–186. [Abstract/Full-Text]

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