Regular ArticleInhibitory Effect of Zinc on the Absorption of JBP485 via the Gastrointestinal Oligopeptide Transporter (PEPT1) in Rats
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2021, Advances in Protein Chemistry and Structural BiologyCitation Excerpt :The transport and uptake of antimetabolite drug floxuridine was shown to be enhanced upon conjugation with dipeptides (Phe-Gly, Phe-Tyr and Ile-Gly) (Tsume, Hilfinger, & Amidon, 2008). Generally, cyclic peptides are low affinity and poor substrates for PepT1 such as JP845 (Miao et al., 2011). Pseudo-tripeptidization of JP485 improved the transport and affinity toward PEPT1 (Jiang et al., 2019).
Dioscin protects against ANIT-induced cholestasis via regulating Oatps, Mrp2 and Bsep expression in rats
2016, Toxicology and Applied PharmacologyCitation Excerpt :Then, dioscin uptake study using isolated rat hepatocytes indicated that compared to control group, the Vmax value was decreased, without affecting Km in ANIT-induced cholestasis (Fig. 3C). As we know, Km value represents the transport function of transporter, while Vmax value means the expression of transporter (Ashida et al., 2004; Miao et al., 2011). In other words, the reduction of Vmax value for dioscin indicated the expression of Oatps might be decreased in ANIT-induced cholestasis.
Intestinal drug transporters: An overview
2013, Advanced Drug Delivery ReviewsOAT1 and OAT3: Targets of drug-drug interaction between entecavir and JBP485
2013, European Journal of Pharmaceutical SciencesCitation Excerpt :JBP485 (cyclo-trans-4-L-hydroxyprolyl-L-serine) is one type of dipeptide, and animal experiments have demonstrated that JBP485 exhibits a liver protective effect via oral administration (Liu et al., 2000; Yang et al., 2009; Wu et al., 2008). Our previous studies have shown that JBP485 is a substrate of OAT1, OAT3 (Zhang et al., 2010; Zhu et al., 2012; Guo et al., 2012a,b; Ye et al., 2012), and PEPT1 (Guo et al., 2012a,b; Cang et al., 2010; Liu et al., 2011; Miao et al., 2011). Owing to the complex pathology, the treatment programs for hepatitis B not only work on against hepatitis B virus, but also need to protect liver cells.
Inhibitory effect of 1α,25-dihydroxyvitamin D<inf>3</inf> on excretion of JBP485 via organic anion transporters in rats
2013, European Journal of Pharmaceutical SciencesCitation Excerpt :The substrates of Oat1 include various drugs, such as p-Aminohippurate (PAH), antiviral drugs, β-lactam antibiotics, anti-inflammatory agents, methotrexate and endogenous organic anions, whereas the major substrates of Oat3 include benzylpenicillin (PCG), cimetidine, estrone sulfate, pravastatin, and ochratoxin A (Deguchi et al., 2004; Uwai et al., 1998). JBP485 (cyclo-trans-4-L-hydroxyprolyl-L-serine) is a dipeptide (Liu et al., 2000) that was first isolated from Laennec (a trade name for the hydrolysate of human placenta), and has been synthesized by chemical means (Miao et al., 2011). Animal experiments have indicated that JBP485 exhibits obvious liver (Liu et al., 1998; Wu et al., 2008; Yang et al., 2009) and gastrointestinal (Wang et al., 2011) protective effects.
Benzylpenicillin inhibits the renal excretion of acyclovir by OAT1 and OAT3
2013, Pharmacological ReportsCitation Excerpt :All experiments were conducted in accordance with the National Institutes of Health Guide for the Care and Use of Laboratory Animals. In all cases, we used diethyl ether to anesthetize the rats [15]. Acyclovir and PCG were soluble in normal saline or buffer solution and were administered intravenously via the jugular vein to rats in aqueous solution.