Orlistat (Synonyms: Ro 18-0647/002, (–)-Tetrahydrolipstatin) |
| カタログ番号GC17318 |
オルリスタットは、膵臓と胃のリパーゼの不可逆的な阻害剤です。
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Cas No.: 96829-58-2
Sample solution is provided at 25 µL, 10mM.
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Orlistat is an irreversible inhibitor of lipases in the pancreas and stomach. It is a drug for the treatment of obesity. It suppresses the action of gastrointestinal lipases, thereby impairing the metabolism of lipids in the gastrointestinal lumen, which can prevent the absorption of 30% of the lipids in dietary fat[1,2]. Orlistat is very hydrophobic and binds covalently to the active serine residues of pancreatic lipase. Orlistat passes through cell membranes sufficiently and exerts intracellular effects[3].
Orlistat(0-25µM;32h) induced a pronounced antiproliferative effect in the PC-3 cell line[4]. Orlistat inhibits Jurkat cell growth and induces a perturbation of cell cycle along with a decline of FASN activity and protein levels[6]. Orlistat-mediated(0-50µM) FASN inhibition could overcome sorafenib resistance and enhance cell killing in HCC by changing cell metabolism[7].
Orlistat(10 mg/kg/day, p.o.) alleviates colon cancer promotion in WD-driven CAC mice by suppressing inflammation, especially by inhibiting STAT3 and NF-κB activation[5].Orlistat(240 mg/kg/day;3 weeks; i.p.) prevented the growth of PC-3 tumors. Animals exhibited no outward signs of toxicity, experienced no loss of weight, nor were there any effects of Orlistat on hematocrit or WBC levels[4].
References:
[1]. Chandra P, Enespa, et,al. Microbial lipases and their industrial applications: a comprehensive review. Microb Cell Fact. 2020 Aug 26;19(1):169. doi: 10.1186/s12934-020-01428-8. PMID: 32847584; PMCID: PMC7449042.
[2]. Bansal AB, Al Khalili Y. Orlistat. 2022 Nov 2. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-. PMID: 31194359.
[3]. Padwal, et,al. Drug treatments for obesity: Orlistat, sibutramine, and rimonabant. Lancet 2007, 369, 71-77.
[4]. Kridel SJ, Axelrod F, et,al. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity. Cancer Res. 2004 Mar 15;64(6):2070-5. doi: 10.1158/0008-5472.can-03-3645. PMID: 15026345.
[5]. Jin BR, Kim HJ, et,al. Anti-Obesity Drug Orlistat Alleviates Western-Diet-Driven Colitis-Associated Colon Cancer via Inhibition of STAT3 and NF-κB-Mediated Signaling. Cells. 2021 Aug 11;10(8):2060. doi: 10.3390/cells10082060. PMID: 34440829; PMCID: PMC8394553.
[6]. Cioccoloni G, Aquino A, et,al. Fatty acid synthase inhibitor orlistat impairs cell growth and down-regulates PD-L1 expression of a human T-cell leukemia line. J Chemother. 2020 Feb;32(1):30-40. doi: 10.1080/1120009X.2019.1694761. Epub 2019 Nov 28. PMID: 31775585.
[7]. Shueng PW, Chan HW, et,al. Orlistat Resensitizes Sorafenib-Resistance in Hepatocellular Carcinoma Cells through Modulating Metabolism. Int J Mol Sci. 2022 Jun 10;23(12):6501. doi: 10.3390/ijms23126501. PMID: 35742944; PMCID: PMC9223797.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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