Penandaan Falerin dengan Iodium-131 dan Uji Biodistribusi pada Mencit yang Diinduksi Inflamasi

Abstract

Phalerin is an active component of mahkota dewa (Phaleria macrocarpa (Scheff) Boerl) proven to have an anti-inflammation effect. The labeling of phalerin with gamma emitting radionuclides was aimed to study its pharmacokinetic behavior and particularly to trace its metabolites. The labeling with ¹³¹I was caried out using iodogen as oxidator. Radiolabeled compound was characterized by high performance liquid chromatography (HPLC) using C- 18 column eluted with methanol 70% and detected with UV detector (λ=291 nm) and by thin layer chromatography (TLC) using silica gel strips eluted with chloroform-methanol (9:2), and labeling efficiency was determined using the same TLC system. Purification of radiolabeled product Was carried out using size exclusion chromatography (Sephadex G-25 column) eluted with 0.05 M phosphate buffer pH 7.4. Biodistributions of ¹³¹l-phalerin in various organs of normal and inilammation-induced mice were observed at 1, 4, and 24 hours post-intravenous injection. Radiochemical purity of ¹³¹l-phalerin was 90.2 ± 2.8% and increased to 96.0 ± 0.4% after purification. Radioactivities in inflamed tissue at 1, 4, and 24 hours post-injection were respectively 1.6 times, 1.4 times, and 1.3 times higher than that in normal tissue, The results showed a significant uptake of radiolabeled phalerin in inflamed tissue.