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JPH203 as a potential L-Type Amino Acid Transporter 1 (LAT 1) inhibitor in the development of cancer theragnostic compounds Yolanda Pertiwi; Driyanti Rahayu; Maula Eka Sriyani; Raden Bayu Indradi; Holis Abdul Holik
Jurnal Ilmiah Farmasi Vol. 16 No. 2 (2020): Jurnal Ilmiah Farmasi
Publisher : Universitas Islam Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20885/jif.vol16.iss2.art8

Abstract

AbstractBackground: Cancer has become a major cause of global health problems. Latest research currently focuses on an approach to cancer therapy that involves specific target molecules and theragnostic (therapy and diagnostic) agents. Among the specific target molecules in cancer therapy is LAT1, which is over expressed in cancer cells but under expressed in normal cells. Therefore, LAT1 inhibition can become an alternative to cancer therapy. A number of studies have shown that JPH203 specifically inhibits LAT1, thus reducing amino acid absorption into cancer cells and inhibiting cancer cell growth.Objective: The main objective of this literature study was to determine the potential of JPH203 as a LAT1 inhibitor to be developed into a novel theragnostic agent for cancer.Methods: Various studies were summarized to outline the development of JPH203 as a therapy targeting LAT1 and potential candidate of theragnostic compounds.Results: The results of the literature study showed that JPH203 as a selective LAT1 inhibitor was able to efficiently suppress the growth of cancer cells with a low IC50 value.Conclusion: The activity of LAT1 as an amino acid transporter of cancer cells could be selectively inhibited by JPH203, thereby allowing JPH203 to be reconsidered as a potential therapy in the development of theragnostic compounds against cancer.Keywords: JPH203, theragnostic, LAT1 inhibitorIntisariLatar belakang: Kanker telah menjadi penyebab masalah kesehatan utama di dunia. Saat ini penelitian terbaru berfokus pada pendekatan terapi kanker yang melibatkan molekul target yang spesifik dan menggunakan senyawa teranostik (terapi dan diagnostik). Salah satu molekul target spesifik dalam terapi kanker adalah LAT1 yang terekspresi berlebih pada sel kanker, namun sedikit pada sel normal. Oleh karena itu, inhibisi LAT1 dapat menjadi alternatif terapi kanker. Beberapa penelitian menunjukkan inhibitor yang secara spesifik menghambat LAT1 adalah JPH203, sehingga penyerapan asam amino ke dalam sel kanker dapat berkurang dan menghambat pertumbuhan sel kanker.Tujuan: Tujuan utama dari studi literatur ini adalah untuk mengetahui potensi JPH203 yang merupakan inhibitor LAT1 dalam perannya sebagai senyawa teranostik baru terhadap penyakit kanker.Metode: Berbagai penelitian dirangkum mengenai pengembangan JPH203 sebagai terapi pentarget-LAT1 dan potensinya sebagai kandidat senyawa teranostik.Hasil: Hasil studi literatur yang dilakukan menunjukkan bahwa JPH203 sebagai inhibitor selektif LAT1 mampu menekan pertumbuhan sel kanker secara efisien dengan didapatkan hasil IC50 yang rendah.Kesimpulan: Aktivitas LAT1 sebagai transporter asam amino sel kanker dapat dihambat secara selektif oleh JPH203, sehingga dapat dipertimbangkan kembali sebagai target terapi potensial yang dapat digunakan dalam pengembangan senyawa teranostik kanker.Kata kunci : JPH203, teranostik, inhibitor LAT1
REVIEW: 99mTEKNESIUM DAN KHELATOR DWIFUNGSINYA SEBAGAI AGEN RADIOFARMAKA TARGET SPESIFIK Arini Nurhaqiqi Aminudin; Holis Abdul Holik
Farmaka Vol 20, No 1 (2022): Farmaka (Maret)
Publisher : Fakultas Farmasi, Universitas Padjadjaran

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.24198/farmaka.v20i1.34612

Abstract

ABSTRAK99mTc adalah radioisotop pemancar sinar gamma yang memiliki karakteristik optimal untuk digunakan dalam kedokteran nuklir. Diketahui waktu paruhnya 6.02 jam dengan Еγ sebesar 140 keV, mode peluruhan IT 100%. Produksi 99mTc dilakukan menggunakan generator 99Mo/99mTc. 99mTc dielusi dari generator dalam bentuk larutan Na99mTcO4. Saat ini lebih dari 80% radiofarmaka diagnostik yang digunakan pada klinik di seluruh dunia mengandung 99mTc. Secara umum penggunaan 99mTc dilakukan pada diagnosis onkologi, kardiologi, dan scan tulang, serta imaging fungsi organ seperti ginjal, hati, otak, dan paru-paru. Pada aplikasinya, radiofarmaka 99mTc seringkali dikonjugasi dengan khelator dwifungsi dimana yang paling umum adalah dengan HYNIC, DTPA, dan MAG3. HYNIC lebih unggul dalam aspek biodistribusi dan efisiensi, sementara DTPA memiliki waktu penyerapan yang paling cepat diantara ketiganya.ABSTRACT99mTc is a gamma-emitting radioisotope that has optimal properties for use in nuclear medicine. Given a half-life of 6.02 hours with Еγ of 140 keV, 100% IT decay mode. 99mTc production is carried out using a 99Mo / 99mTc generator. 99mTc is eluted from the generator in the form of a Na99mTcO4 solution. Thus, more than 80% of the diagnostic radiopharmaceuticals used in clinics worldwide contain 99mTc. In general, the use of 99mTc is carried out in the diagnosis of oncology, cardiology, and bone scans, as well as imaging of organ functions such as kidneys, liver, brain, and lungs. In its application, 99mTc radiopharmaceuticals have been conjugated with a dual-function chelator, the most common of which are HYNIC, DTPA, and MAG3. HYNIC is superior in terms of biodistribution and efficiency, while DTPA has the fastest absorption time of the three.
Edukasi Hidup Sehat Tanpa Diabetes Dengan Pemanfaatan Tanaman Obat Bagi Masyarakat Desa Mekarjaya Banjaran Ida Musfiroh; Sandra Megantara; Holis Abdul Holik; Yasmiwar Susilawati; Gofarana Wilar
Journal of Community Development Vol. 3 No. 3 (2023): April
Publisher : Indonesian Journal Publisher

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47134/comdev.v3i3.113

Abstract

Diabetes mellitus in Indonesia now ranks 5th with the highest number of diabetes mellitus sufferers in the world. At present, the prevalence has increased from 6.2% compared to 2019. Diabetics need to get effective and safe drugs in order to avoid various complications. In addition to using pharmacological therapy, it is also necessary to carry out non-pharmacological therapy. One type of medicinal plant that is known to be effective in reducing sugar is ginger and cinnamon, but there has not been much reported on its processing other than in the form of a decoction or marinade. The purpose of carrying out this PPM activity is to increase the knowledge and understanding of the people of Mekarjaya Banjaran Village regarding the use of medicinal plants as anti-diabetics, and provide knowledge about making ginger-cinnamon instant powder drinks. The activity method is carried out in 3 stages, namely the planning, implementation, evaluation and follow-up stages. The results of this PPM activity show that the community has a better understanding of efforts to be healthy in preventing diabetes through the use of ginger-cinnamon medicinal plants, and how to process them through instant powders. The evaluation is carried out based on the results of the initial test and the final test as a method for measuring the achievements of this PPM activity.