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Cholesteryl hemisuccinate as a membrane stabilizer in dipalmitoylphosphatidylcholine liposomes containing saikosaponin-d

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单位: [1]Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100083, Peoples R China [2]China Japan Friendship Hosp, Dept Mat Med & Pharmacol, Beijing 100029, Peoples R China [3]Hoshi Univ, Inst Med Chem, Shinagawa Ku, Tokyo 1428501, Japan
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关键词: cholesteryl hemisuccinate saikosaponin-d saponin liposome differential scanning calorimetry Fourier transform infrared spectroscopy

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In the present study, cholesteryl hemisuccinate (CHEMS) was evaluated for use as a membrane stabilizer in dipalmitoylphos-phatidylcholine (DPPC) liposomes. Differential scanning calorimetry (DSC) and a calcein release study showed that CHEMS was more effective than cholesterol (CHOL) in increasing DPPC membrane stability. The findings of Fourier transform infrared spectroscopy (FT-IR) also suggested that CHEMS interacts with DPPC via both hydrogen bonding and electrostatic interaction. More importantly, CHEMS did not interact with saikosaponin-d (SSD), a triterpene saponin from Bupleurum species, unlike CHOL. SSD-containing liposomes with DPPC, CHEMS and DSPE-PEG could greatly decrease the hemolytic activity of SSD. This study demonstrated that CHEMS has more stabilization ability than CHOL since CHEMS may exhibit both hydrogen bond interaction and electrostatic interaction with DPPC membrane while CHOL only has hydrogen bond interaction, resulting in stable and low-hemolytic SSD-liposomes. (c) 2005 Elsevier B.V. All rights reserved.

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大类 | 2 区 医学
小类 | 2 区 药学
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出版当年[2003]版:
Q3 PHARMACOLOGY & PHARMACY
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Q1 PHARMACOLOGY & PHARMACY

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