期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 94, 期 -, 页码 363-371出版社
ELSEVIER
DOI: 10.1016/j.ejpb.2015.06.012
关键词
Triptolide; Fragment peptide; Renal targeting; Conjugate; Human serum albumin
资金
- National Natural Science Foundation of China [81202489]
We have previously demonstrated that peptide fragments (PFs) of the human serum albumin could be developed as potential renal targeting carriers, in particular, the peptide fragment, PF-A(299-585) (A(299-585) representing the amino acid sequence of the human serum albumin). In this paper, we conjugated triptolide (TP), the anti-inflammatory Chinese traditional medicine, to PF-A(299-585) via a succinic acid spacer to give TPS-PF-A(299-585) (TP loading 2.2% w/w). Compared with the free TP, TPS-PF-A(299-585) exhibited comparable anti-inflammatory activity in the lipopolysaccharide stimulated MDCK cells, but was significantly less cytotoxic than the free drug. Accumulation of TPS-PF-A(299-585) in the MDCK cells in vitro and in rodent kidneys in vivo was demonstrated using FITC-labeled TPS-PF-A(299-585). Renal targeting was confirmed in vivo in a membranous nephropathic.(MN) rodent model, where optical imaging and analyses of biochemical markers were combined to show that TPS-PF-A(299-585) was capable of alleviating the characteristic symptoms of MN. The collective data affirm PF-A(299-585) to be a useful carrier for targeting TP to the kidney. (C) 2015 Elsevier B.V. All rights reserved.
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