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liposome intracellular delivery of Salvia miltiorrhiza Bge. deprivative DS-201 improves its BK_(Ca) channel-activating and vasorelaxing effects

引用

Science Bulletin 2016年第8期61卷 622-631页

作者： Lei Yu Jun Cheng Wen-Jun Huang Xiao-Qiu Tan Liang Mao Zhi-Fei Liu Xiao-Rong Zeng Yan Yang Key Laboratory of Medical Electrophysiology Ministry of Education of China Institute of Cardiovascular ResearchSichuan Medical University

Some drugs exert curative effects intracellu- larly, but their hydrophilic property prohibits the mem- brane-penetrating process and thus limits the curative efficacies, although this property guarantee their solubility in aqueous phase. An example is sodium tanshinone II-A sulfonate （DS-201）, a derivative of Chinese medical herb Danshen （Salvia miltiorrhiza） which is a BKc~ channel opener and a vasodilator. This study established and opti- mized a liposome delivery system which could pack and deliver DS-201 into HEK293 cells transfected with BKca channels, and DS-201 given this way significantly increased the open probability of BKca channel from baseline 0.013 ~ 0.004 to 0.036 -4- 0.011 at -t-40 mV membrane potential （P 〈 0.05） in single-channel attached study, and also increased the current density from baseline 23.2 ＋ 4.4 to 66.0 4- 15.2 pA/pF at ＋40 mV membrane potential （P 〈 0.05）, compared with the direct extracellular administration of this drug. Moreover, showing a ~ 60 % inhibition of the PE or PGF2a induced vascular constric- tion, the DS-201 liposomes did posses significantly enhanced vasorelaxant effect on rat mesenteric artery, compared with 20 % inhibition of the directly administration of this drug （P 〈 0.05）, suggesting that DS-201 delivered by liposomes significantly improved the drug＇s vasorelaxing effect. Taken together, the optimized DS-201 liposomes in our study successfully delivered DS-201 into cells and thus significantly activated BKca channels to reverse the contraction induced by PE and PGF2a, attesting the enhanced bioavailability.

关键词： drug delivery system - liposome Sodium tanshinone II-A sulfonate BKca channelVasodilatation

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