Back كالسيتريول Arabic کلسیتریول AZB Kalcitriol BS Calcitriol Catalan Kalcitriol Czech Calcitriol Welsh Calcitriol German ކެލްސިޓްރިއޯލް DV Calcitriol English Calcitriol Spanish
| |
|---|---|
| Nama sistematis (IUPAC) | |
| (1R,3S)- 5-[2-[(1R,3aR,7aS)-1- [(2R)-6-hydroxy-6-methyl-heptan-2-yl]- 7a-methyl-2,3,3a,5,6,7-hexahydro-1H- inden-4-ylidene]ethylidene]- 4-methylidene-cyclohexane-1,3-diol | |
| Data klinis | |
| Kat. kehamilan | B3 (Au), C (U.S.) |
| Status hukum | S4 (Au), POM (UK) |
| Rute | Oral, IV, topical |
| Data farmakokinetik | |
| Metabolisme | Renal |
| Waktu paruh | 5–8 hours |
| Ekskresi | Renal |
| Pengenal | |
| Nomor CAS | 32222-06-3 |
| Kode ATC | A11CC04 D05AX03 |
| PubChem | CID 134070 |
| DrugBank | APRD00246 |
| ChemSpider | 4941667 |
| UNII | FXC9231JVH 
|
| Data kimia | |
| Rumus | C27H44O3 |
| Massa mol. | 416.64 g/mol |
| SMILES | eMolecules & PubChem |
Kalsitriol (bahasa Inggris: 1,25-dihydroxycholecalciferol, 1,25-dihydroxyvitamin D3, 1,25-(OH)2D3) adalah hormon pleitrofik yang merupakan bentuk aktif vitamin D setelah proses konversi oleh ginjal,[1] terhadap kalsidiol yang disekresi oleh hati,[2] dengan katalis berupa enzim sitokrom P450 hidroksilase 1-alfa.[3]
Kalsitriol memiliki sifat anti-proliferatif, pro-apoptotik dan pro-diferensiasi terhadap berbagai jenis sel tubuh, dan sifat anti-kanker, seperti kanker prostat, kanker usus besar,[4] kanker indung telur, kanker payudara, leukemia,[5] oleh kapasitas regulasi terhadap metabolisme kalsium dan fosfat,[6][7] serta modulasi sistem kekebalan dan fungsi sistem saraf pusat.[4]
Kalsitriol akan dikonversi menjadi asam kalsitroat sebelum diekskresi melalui empedu,[8] atau urin.[9]
- ^ (Inggris) "Analysis of SNPs and Haplotypes in Vitamin D Pathway Genes and Renal Cancer Risk". Core Genotyping Facility at the Advanced Technology Center of the National Cancer Institute, Division of Cancer Epidemiology and Genetics, National Cancer Institute, National Institutes of Health (NIH), Department of Health and Human Services, International Agency for Research on Cancer, Department of Cancer Epidemiology and Genetics, Masaryk Memorial Cancer Institute, Institute of Public Health, Institute of Carcinogenesis, Cancer Research Centre, Department of Preventive Medicine, Faculty of Medicine, Palacky University, Institute of Hygiene and Epidemiology, First Faculty of Medicine, Charles University, Department of Epidemiology, Institute of Occupational Medicine, Ohio State University Medical Center; Sara Karami, Paul Brennan, Philip S. Rosenberg, Marie Navratilova, Dana Mates, David Zaridze, Vladimir Janout, Helena Kollarova, Vladimir Bencko, Vsevolod Matveev, Neonila Szeszenia-Dabrowska, Ivana Holcatova, Meredith Yeager, Stephen Chanock, Idan Menashe, Nathaniel Rothman, Wong-Ho Chow, Paolo Boffetta, dan Lee E. Moore. Diakses tanggal 2010-12-10.
- ^ (Inggris) "Vitamin D Deficiency and Liver Disease". Medicine Medical Director of Liver Transplantation University of Tennessee Health Science Center; Satheesh Nair. Diakses tanggal 2010-12-10.
The liver produces 25-hydroxy (25-OH) vitamin D, also known as calcidiol, the immediate precursor to the metabolically active 1,25 dihydroxyvitamin D 1-25 vitamin D, also known as calcitriol.
- ^ (Inggris) "Expression of 25-hydroxyvitamin D3-1alpha-hydroxylase in the human kidney". Division of Medical Sciences, University of Birmingham, Queen Elizabeth Hospital;Zehnder D, Bland R, Walker EA, Bradwell AR, Howie AJ, Hewison M, Stewart PM. Diakses tanggal 2010-12-10.
- ^ a b (Inggris) "The pleiotropic actions of vitamin D". Department of Physiology, McGill University; Lin R, White JH. Diakses tanggal 2010-12-10.
- ^ (Inggris) "Vitamin D and Human Health: Lessons from Vitamin D Receptor Null Mice". Katholieke Universiteit Leuven, Laboratory of Experimental Medicine and Endocrinology, Massachusetts General Hospital, Endocrine Unit; Roger Bouillon, Geert Carmeliet, Lieve Verlinden, Evelyne van Etten, Annemieke Verstuyf, Hilary F. Luderer, Liesbet Lieben, Chantal Mathieu, dan Marie Demay. Diakses tanggal 2010-12-10.
To gain more insight into the antiproliferative and prodifferentiating effect of 1,25-(OH)2D, genomic profiling has been performed in malignant cells such as prostate (127,128,129,130,131,132,133), breast (134,135,136), leukemia (137,138), colon (139), and ovarian cancer (140) cells, and squamous cell carcinoma cells (141). Since then, the antineoplastic activity of 1,25-(OH)2D was shown both in vitro and in vivo in a wide variety of malignancies, such as leukemia (266,267) and colon (268,269), breast (270,271,272), and prostate cancer (273,274).
- ^ (Inggris) "Vitamin D and cancer: an update of in vitro and in vivo data". Instituto de Investigaciones Biomedicas, Consejo Superior de Investigaciones Cientificas, Universidad Autonoma de Madrid; Ordonez-Moran P, Larriba MJ, Pendas-Franco N, Aguilera O, Gonzalez-Sancho JM, Munoz A. Diakses tanggal 2010-12-10.
- ^ (Inggris) "Vitamin D and colon carcinogenesis". UCLA Center for Human Nutrition, University of California at Los Angeles; Harris DM, Go VL. Diakses tanggal 2010-12-10.
- ^ (Inggris) "Target cell metabolism of 1,25-dihydroxyvitamin D3 to calcitroic acid, Evidence for a pathway in kidney and bone involving 24-oxidation" (PDF). Department of Biochemistry, Queen's University, Human Nutrition Research Center on Aging, Tufts University; Guy MAKIN, David LOHNES, Valarie BYFORD, Rahul RAY dan Glenville JONES. Diakses tanggal 2010-12-10.
- ^ (Inggris) "Vitamin D Metabolism: New Concepts and Clinical Implications". Hanson Institute, Adelaide, SA 5000 and School of Molecular and Biomedical Science, University of Adelaide; PH Anderson, BK May, dan HA Morris. Diakses tanggal 2010-12-10.