Synthesis of sulochrin-125I and its binding affinity as α-glucosidase inhibitor using Radioligand Binding Assay (RBA) method

W. Lestari, V. Y. Susilo, S. Setiyowati, Triningsih, A. Ariyanto, P. Widayati, L. B.S. Kardono, A. Yanuar

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Abstract

Most of diabetics patients have type 2 diabetes mellitus or non insulin dependent diabetes mellitus. Treatment type 2 diabetes mellitus can be done by inhibiting α-glucosidase enzyme which converts carbohydrates into glucose. Sulochrin is one of the potential compounds which can inhibit the function of α-glucosidase enzyme. This study was carried out to obtain data of sulochrin binding with α-glucosidase enzyme as α-glucosidase inhibitor using Radioligand Binding Assay (RBA) method. Primary reagent required in RBA method is labeled radioactive ligand (radioligand). In this study, the radioligand was sulochrin-125I and prior to sulochrin-125I synthesis, the sulochrin-I was synthesized. Sulochrin-I and sulochrin-125I were synthesized and their bindings were studied using Radioligand Binding Assay method. Sulochrin-I was synthesized with molecular formula C17H15O7I and molecular weight 457.9940. Sulochrin-125I was synthesized from sulochrin-I by isotope exchange method. From the RBA method, dissociation constant (Kd) and maximum binding (Bmax) were obtained 26.316 nM and Bmax 9.302 nM respectively. This low Kd indicated that sulochrin was can bind to α-glucosidase.

Original languageEnglish
Pages (from-to)22-26
Number of pages5
JournalAtom Indonesia
Volume40
Issue number1
DOIs
Publication statusPublished - 1 Jan 2014

Keywords

  • Radioligand binding assay
  • Sulochrin
  • Sulochrin-125I
  • Sulochrin-I
  • α-glukosidase inhibitor

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    Lestari, W., Susilo, V. Y., Setiyowati, S., Triningsih, Ariyanto, A., Widayati, P., Kardono, L. B. S., & Yanuar, A. (2014). Synthesis of sulochrin-125I and its binding affinity as α-glucosidase inhibitor using Radioligand Binding Assay (RBA) method. Atom Indonesia, 40(1), 22-26. https://doi.org/10.17146/aij.2014.261