期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 22, 页码 5524-5527出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.10.008
关键词
Ursolic acid; Prodrug; Anticancer; Pancreatic cancer; Bioavailability
资金
- Small and Medium Business Administration (SMBA) in Korea [S2321935]
- Korea Technology & Information Promotion Agency for SMEs (TIPA) [S2321935] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
The aim of our study was to develop ursolic acid (UA) prodrugs in order to overcome UA's weakness, which has an extremely low bioavailability. UA-medoxomil (NX-201), one of our UA prodrugs, showed an improved bioavailability about 200 times better than UA in rodent model. According to in vivo test performed with PANC-1 xenograft SCID mouse model, tumor growth rate decreased dose-dependently and 100 mg/kg dose of NX-201 had an anticancer effect comparable to gemcitabine. Most of all the combination of NX-201 (50 mg/kg, po, daily) and gemcitabine (40 mg/kg, iv, 2 times per week) even reduced tumor size after three weeks. (C) 2016 Elsevier Ltd. All rights reserved.
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