Diabetes melitus tipe 2 dapat dikontrol dengan menghambat kerja enzim α-glukosidase. Sulokrin merupakan salah satu senyawa yang mempunyai potensi sebagai penghambat α-glukosidase. Senyawa sulokrin-I dan sulokrin-125I telah disintesa serta dipelajari ikatannya dengan metode Radioligand Binding Assay (RBA) dan penambatan molekuler. Sulokrin-I disintesa dengan rumus molekul C17H15O7I dan berat molekul 457,9940. Senyawa sulokrin-125I disintesa dari sulokrin-I menggunakan metode pertukaran isotop. Sulokrin-125I diperoleh dengan kemurnian radiokimia sebesar 82,3%. Dari hasil pengujian dengan metode RBA diperoleh Kd dan Bmax secara berturut turut 83,33 pM dan 1,2 x 10-6 pmol/mg reseptor. Penambatan molekuler sulokrin-I dilakukan terhadap α-glukosidase Saccharomyces cerevisiae dan α-glukosidase manusia. Sulokrin-I yang digunakan dalam proses penambatan molekuler adalah metil 2-(2,6-dihidroksi-3-iodo-4-metilbenzoil)-5-hidroksi-3-metoksibenzoat [A] dan metil 2-(2,6-dihidroksi-5-iodo-4-metilbenzoil)-5-hidroksi-3-metoksibenzoat [B]. Model senyawa A dan B berinteraksi dengan α-glukosidase Saccharomyces cerevisiae melalui pembentukan ikatan hidrogen dengan residu Arg213, Asp215, Glu277, Asp352. Nilai ΔG dan Ki yang diperoleh adalah -6,71 kkal/mol dan 12,03 µM untuk senyawa A, -5,82 kkal/mol dan 54,39 µM untuk senyawa B. Interaksi senyawa A, senyawa B dengan α-glukosidase manusia menghasilkan ΔG dan Ki sebesar -6,81 kkal/mol dan 10,3 µM untuk senyawa A, senyawa B mempunyai ΔG dan Ki sebesar -6,27 kkal/mol dan 25,4 µM.;Treatment type 2 diabetes melitus can be done by inhibiting α-glucosidase.

---

Sulochrin is one of the potential α-glucosidase inhibitor compound. Sulochrin-I and sulochrin-125I were synthesized and their binding were studied using Radioligand Binding Assay and molecular docking method. Sulochrin-I has been synthesized with molecular formula C17H15O7I and molecular weight 457.9940. Sulochrin-125I was synthesized from sulochrin-I by isotope exchange method. sulochrin-125I radiochemical purity was 82.3%. From the RBA method, Kd and Bmax were obtained 83.33 pM and 1.2 x 10-6 pmol / mg receptor respectively. Molecular docking of sulochrin-I was done in two macromolecules, Saccharomyces cerevisiae α-glucosidase and human α-glucosidase. Two ligands were used in this research, they are methyl 2 - (2,6-dihydroxy-3-iodo-4-methylbenzoil)-5-hydroxy-3-methoxibenzoate [A] and methyl 2 - (2,6-dihydroxy-5-iodo-4-methylbenzoil)-5-hydroxy-3-methoxybenzoat [B]. Compound A and B showed interaction with Saccharomyces cerevisiae α-glucosidase and showed hydrogen bound with Arg213, Asp215, Glu277, Asp352. ΔG and Ki values for compound A are -6.71 kcal / mol and 12.03 µM, whereas for compound B are - 5.82 kcal/mol and 54.39 µM respectively. Interaction study with human α-glucosidase gave ΔG -6.81 kcal/mol and Ki 10.3 µM for compound A, whereas compound B gave ΔG and Ki -6.27 kcal/mol and 25.4 µM respectively.