Small molecule additive enhances cell uptake of 5-aminolevulinic acid and conversion to protoporphyrin IX.
Small molecule additive enhances cell uptake of 5-aminolevulinic acid and conversion to protoporphyrin IX.
复制标题
DOI：
10.1039/c6pp00151c
复制
发表时间：
2016-11-02
期刊：
影响因子：
--
通讯作者：
Smith BD
中科院分区：
文献类型：
--
作者：
Harmatys KM;Musso AJ;Clear KJ;Smith BD
Administration of exogenous 5-aminolevulinic acid (5-ALA) to cancerous tissue leads to intracellular production of photoactive protoporphyrin IX, a biosynthetic process that enables photodynamic therapy and fluorescence-guided surgery of cancer. Cell uptake of 5-ALA is limited by its polar structure and there is a need for non-toxic chemical additives that can enhance its cell permeation. Two zinc-bis(dipicolylamine) (ZnBDPA) compounds were evaluated for their ability to promote uptake of 5-ALA into Chinese Hamster Ovary (CHO-K1) cells and produce protoporphyrin IX. One of the ZnBDPA compounds was found to be quite effective, and a systematic comparison of cells incubated with 5-ALA (100 μM) for 6 hours showed that the presence of this ZnBDPA compound (10 μM) produced 3-fold more protoporphyrin IX than cells treated with 5-ALA alone. The results of mechanistic studies suggest that the ZnBDPA compound does not interact strongly with the 5-ALA. Rather, the additive is membrane active and transiently disrupts the cell membrane, permitting 5-ALA permeation. The membrane disruption is not severe enough to induce cell toxicity or allow passage of larger macromolecules like plasmid DNA. Cells incubated with an admixture of 5-ALA (100 μM) and a zinc(II)-bis(dipicolylamine) compound (10 μM) produced 3-fold more protoporphyrin IX than cells treated with 5-ALA alone.
登录
查看更多内容
DOI：
10.1016/j.jphotobiol.2009.06.001
发表时间：
2009-08-03
影响因子：
5.4
作者：
Di Venosa, Gabriela;Hermida, Laura;Batlle, Alcira
通讯作者：
Batlle, Alcira
影响因子：
10.3
作者：
Casas, A;Fukuda, H;Batlle, AMD
通讯作者：
Batlle, AMD
影响因子：
6.6
作者：
Kriegmair, M;Baumgartner, R;Hostetter, A
通讯作者：
Hostetter, A
影响因子：
5.7
作者：
Battah, Sinan;Balaratnam, Sherina;MacRobert, Alexander J.
通讯作者：
MacRobert, Alexander J.
影响因子：
8
作者：
Chung CW;Chung KD;Jeong YI;Kang DH
通讯作者：
Kang DH