Can I read Transport characteristics of 9-nitrocamptothecin in the human intestinal cell line Caco-2 and everted gut sacs on EtoBox?

Transport characteristics of 9-nitrocamptothecin in the human intestinal cell line Caco-2 and everted gut sacs by Xianyi Sha; Xiaoling Fang is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

What is Transport characteristics of 9-nitrocamptothecin in the human intestinal cell line Caco-2 and everted gut sacs about?

The intestinal absorptive characteristics and the efflux mechanisms of 9-nitrocamptothecin (9-NC), a novel water-insoluble camptothecin (CPT) derivative, were investigated. The Caco-2 cells and the everted gut sacs were used as models of the intestinal mucosa to assess transepithelial transport of 9-NC. The determination of 9-NC was performed by HPLC. In the Caco-2 cells, the absorptive transport of 9-NC was pH dependent and the transport was enhanced at weakly acidic pH on the apical side. No concentration dependence and saturation were observed for the absorptive transport of 9-NC at concentrations up to 250 M, while secretory transport were concentration dependent and saturable process (K m was 49.8 ± 1.2 M, V max was 38.28 ± 0.8 ng/cm 2 /min). In the presence of verapamil (100 M) and CsA (10 M), potent inhibitors of P-glyprotein (P-gp)/MRP2 (cMOAT), the P app BL-AP /P app AP-BL ratio was decreased from 3.4 to 1.4 and 1.3, respectively, and permeation of apical to basolateral was enhanced approximately two-fold. In the everted gut sacs, the absorption of 9-NC was passive diffusion and had no significant difference in different gut regions. Adding verapamil in the everted gut sac

Who reads Transport characteristics of 9-nitrocamptothecin in the human intestinal cell line Caco-2 and everted gut sacs?

Author

Xianyi Sha; Xiaoling Fang

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

2004

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)