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1.
Acta Pharmaceutica Sinica B ; (6): 246-257, 2021.
Article in English | WPRIM | ID: wpr-881134

ABSTRACT

Nanotechnology has emerged as an ideal approach for achieving the efficient chemo agent delivery. However, the potential toxicity and unclear internal metabolism of most nano-carriers was still a major obstacle for the clinical application. Herein, a novel "core‒shell" co-assembly carrier-free nanosystem was constructed based on natural sources of ursolic acid (UA) and polyphenol (EGCG) with the EpCAM-aptamer modification for hepatocellular carcinoma (HCC) synergistic treatment. As the nature products derived from food-plant, UA and EGCG had good anticancer activities and low toxicity. With the simple and "green" method, the nanodrugs had the advantages of good stability, pH-responsive and strong penetration of tumor tissues, which was expected to increase tumor cellular uptake, long circulation and effectively avoid the potential defects of traditional carriers. The nanocomplex exhibited the low cytotoxicity in the normal cells

2.
Chinese Pharmacological Bulletin ; (12)1986.
Article in Chinese | WPRIM | ID: wpr-563388

ABSTRACT

Aim To investigate whether Rhizoma curcumaecould induce pregnane X receptor(PXR)-mediated transcriptional expression of CYP3A4 and study the modulatory effects on the enzyme activity and mRNA expression of CYP3A in the rat liver.Methods Transient cotransfection reporter gene assays were performed in HepG2 cells;the rat liver microsomal cytochrome P450 and CYP3A isoenzyme-erythromycin N-demethylase(ERD)activities were determined by UV chromatography;the mRNA expression level of CYP3A was detected by reverse transcriptase-polymerase chain reaction(RT-PCR).Results In vitroinvestigation showed Rhizoma curcumaeand its four selected constituents could induce the CYP3A4 transcriptional expression by activating PXR.In vivoinvestigation showed the CYP450 content of liver microsomes and enzyme activity of CYP3A were markedly increased and induced by Rhizoma curcumaeextract;at the mRNA level, the expression of CYP3A1 and CYP3A2 gene were markedly induced by Rhizoma curcumaeextract.Conclusions Rhizoma curcumaeand its four selected constituents could induce the expression of the CYP3A4 gene transcriptional expression through activating PXR;Rhizoma curcumaeextract could increase and induce the enzyme activity and mRNA expression of CYP3A.

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