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Camptothecin-20(s)-O-[N-(3'α,12'α-dihydroxy-24'-carbonyl-5'β-cholan)]-lysine (B2) is a novel camptothecin analogue. Our previous study had shown that it displayed higher cytoxicity activity towards hepatocellular carcinoma SMMC-7721 cells than camptothecin (CPT) in vitro. In this paper, the underlying mechanism of anti-proliferation of B2 towards SMMC-7721(More)
A novel conjugate of camptothecin and artesunate (C-Q) was prepared and its cytotoxicity was evaluated using the MTT assay. In addition, the antitumour activity and toxicity of C-Q were investigated in mice, and interaction between transferrin (TF) and C-Q was investigated to evaluate its interaction with biological macromolecules. In the MTT assay, C-Q(More)
The purpose of this work is to prepare a formulation using mannitol coupling Camptothecin (CPT) nanoparticles (CPT-NPs) to circumvent the difficult solubilization practice based on central composite experimental statistical design. CPT-NPs were prepared with a high-pressure homogenization technique method. The independent variables considered for the(More)
A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to identify and quantify the camptothecin quaternary derivative CPT8 for application in pharmacokinetics and tissue distribution studies. Rat plasma and tissue samples were extracted with methanol by using camptothecin as the internal standard (IS). Chromatographic separation(More)
In this study, the binding interactions of the water-soluble camptothecin derivatives hydroxycamptothecin (10-HCPT), topotecan (TPT), and camptothecin quaternary salt (CPT8), to bovine serum albumin (BSA) were determined using fluorescence spectra and UV-vis spectra. The results revealed that the fluorescence of BSA was strongly quenched by the binding of(More)
Abstract Camptothecin-20(s)-O-glycine ester-[N-(3'α, 12'α-dihydroxy-24'-carbonyl-5'β-cholan)] (A2), 10-(3'α,12'α-dihydroxy-5'β-cholan-24'-carboxyl)-(20 s)-camptothecin (C2), and 10-O-(3-O-(3'α, 12'α-dihydroxy-24'-carbonyl-5'β-cholan)-propyl)-(20S)-camptothecin (D2) are novel camptothecin-deoxycholic acid analogues. MTT assays were performed to assess the(More)
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