ABSTRAK KARAKTERISTIK FISIKO-KIMIA SENYAWA BERTANDA 99m Tc-KUERSETIN. Berkembangnya ilmu pengetahuan dan informasi di bidang kesehatan membuat masyarakat meyakini bahwa mengkonsumsi makanan yang kaya antioksidan penting untuk mencegah berbagai penyakit degeneratif seperti penyakit jantung dan kanker. Kuersetin merupakan senyawa flavonoid yang banyak ditemukan pada buah dan sayur yang memiliki aktivitas antioksidan yang sangat kuat. Banyak penelitian yang telah membuktikan efektivitas kuersetin sebagai senyawa antikanker secara in-vitro, namun data pengujiannya secara in-vivo masih terbatas. 99m Tc-kuersetin diharapkan dapat dijadikan radiotracer untuk mengetahui efektivitas senyawa kuersetin sebagai senyawa antikanker pada pengujian in-vivo menggunakan hewan percobaan. Namun sebelum dilakukan pengujian in-vivo untuk menjamin aplikasinya perlu dilakukan pengujian karakteristik fisiko-kimia sediaan 99m Tc-kuersetin. Oleh karena itu tujuan dari penelitian ini adalah untuk mengetahui karakteristik fisiko-kimia dari senyawa 99m Tckuersetin. Hasil penelitian karakteristik fisiko-kimia 99m Tc-kuersetin menunjukkan bahwa kemurnian radiokimia sediaan 99m Tc-kuersetin adalah 98,94 ± 0,30%. Sediaan 99m Tc-Kuersetin ini bermuatan netral, memiliki nilai lipofilisitas dengan log (P) = 0,62 ± 0,05 dan dapat berikatan kuat dengan plasma darah dengan persentase sebesar 95,06 ± 1,34%. Berdasarkan nilai lipofilisitas sebesar 0,62 ± 0,05 diharapkan senyawa ini akan mudah terdistribusi kedalam jaringan organ sehingga diharapkan akan efektif sebagai senyawa bertanda penyidik kanker.Kata kunci : 99m Tc-kuersetin, karakteristik fisiko-kimia, antioksidan, antikanker, flavonoid ABSTRACT PHYSICOCHEMICAL CHARACTERISTIC OF LABELED COMPOUND 99m Tc-QUERCETIN. The science and information development in the field of health makes people believe that consumption foods with rich in antioxidants is importance to prevent various degenerative diseases such as heart disease and cancer. Quercetin is a flavonoid compound found in many fruits and vegetables that have very strong antioxidant activity. Many in-vitro studies have proven the effectiveness of quercetin as an anticancer compound, but the data from in-vivo study is still limited. 99m Tc-quercetin is expected to be used as a radiotracer to determine the effectiveness of quercetin compounds as anticancer agent on in-vivo study using animal model. However, before doing in-vivo study to assure its application, it is necessary to determine the physico-chemical characteristics of 99m Tc-quercetin. Therefore, the purpose of this study was to determine the physicochemical characteristics of the 99m Tc-quercetin. The results of the physicochemical characteristics of 99m Tc-quercetin showed that the radiochemical purity of 99m Tc-quercetin preparation was 98.94 ± 0.30%. The 99m Tc-quercetin is neutral charge, has a lipophilic value with log (P) = 0.62 ± 0.05 and can strongly bind with blood plasma with a percentage of 95.06 ± 1.34%. Based on the lipophilicity result of 0.62 ± 0.05, this compound will be e...
Kanamycin antibiotic was radiolabeled successfully with radioisotope technetium-99m for the potential use as radiopharmaceuticals for infection i maging. 99m Tc-kanamycin complexes was prepared 93 % radiochemical purities by direct labelling using 5 mg kanamycin and 30 µg SnCl2. The reaction occurred at alkaline condition (pH=9) and under room temperature for 30 min to achieve high radiochemical purity. Radiochemical purity and stability of 99m Tc-kanamycin was determined by ascending paper chromatography using Whatman 3 paper as the stationary phase, and acetone as the mobile phase to separate the radiochemical impurities in the form of 99m Tc-pertechnetate. While impurities in the form of 99m Tc-reduced were separated using the stationary phase ITLC-SG and 0.5 N NaOH as mobile phase. This study aimed to determine biological characteristic of 99m Tc-kanamycin radiopharmaceutical. In vitro cell studies showed that the change of kanamycin structure after labeling with technetium-99m did not give a specific influence to the potency of kanamycin as an antibiotic. In addition on uptake study, a significantly higher uptake of 99m Tc-kanamycin with S. aureus than E. coli. Biodistribution of 99m Tc-kanamycin complexes was studied on normal and infection mice at 15, 30, 60 and 120 min postinjections. The biodistribution of 99m Tc-kanamycin in infection mice showed that the complex accumulated in the infection sites. These results show that 99m Tc-Kanamycin radiopharmaceutical have a potential application for infection diagnosis.
Infectious diseases have become one of the leading cause of mortality around the world, including in the Southeast Asia. One of the microbial that cause infection is fungi. Occasionally, deep-seated fungal infection is difficult to detect using conventional diagnosis methods and therefore leads to inaccurate detection. Our previous research was conducted in order to obtain the labeled compound of <sup>99m</sup>Tc-DTPA-Ketoconazole with a high radiochemical purity (98.40 ± 0.86%). Moreover, the in-vitro assays showed that <sup>99m</sup>Tc-DTPA-Ketoconazole can potentially bind to Candida albicans. On the other hand, in clinical routine use, diagnostic kit should be safe for the patients. Consequently, this research was conducted to determine the biological safety parameters of <sup>99m</sup>Tc-DTPA-Ketoconazole on the animal study, including single dose and acute toxicity test, sterility, and apirogenicity test. The results showed that both the single dose at 34.6 μCi and dose until 149 times of the single dose did not stimulate the toxic response to the animals. In addition, the sterility data revealed that there was no microbial growth after 7 days of incubation at 37°C as well as fungal growth after 14 days of incubation at 25°C. Furthermore, the apirogenicity test using rabbits revealed that there was no increase in temperature more than 0.6°C for each animal and not more than 1.5°C of total increase of temperature for all the animals. It is concluded that the <sup>99m</sup>Tc-DTPA-Ketoconazole is satisfy the requirements of biological safety of a radiopharmaceutical and therefore was acceptable for fungal detection in nuclear medicine.
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