期刊
MEDICINAL CHEMISTRY RESEARCH
卷 21, 期 8, 页码 1641-1646出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-011-9678-1
关键词
Berberine; Structural modification; Bioavailability; 9-O-glycosyl-berberine
资金
- Major Technologies R D Program [2010ZX09401-306-3-10, CSTC2008AA5021, 2010AC5007]
- Graduate School of Southwest University [kb2009017]
- National Science and Technology Pillar program of China [2011BAI13B02-1]
To increase the bioavailability of berberine, three new 9-O-glycosyl-berberine derivatives, 9-O-glucosyl-(4a), 9-O-arabinosyl-(4b), and 9-O-erythrol-(4c) were obtained and confirmed by UV, (HNMR)-H-1, (CNMR)-C-13, and MS. The pharmacokinetic profiles of these synthetic compounds have been evaluated compared with berberine (1) and 9-O-alkyl-berberine (5) derivatives, which showed that maximum concentration (C (max)) and area under concentration-time curve (AUC) of 9-O-glycosyl-berberine increased dramatically. The results indicated that hydrophilic modification could significantly improve the bioavailability of berberine; 9-O-glycosyl-berberine might be a promising prodrug.
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