In vitro photodynamic therapy and quantitative structure-activity relationship studies with stable synthetic near-infrared-absorbing bacteriochlorin photosensitizers.
In vitro photodynamic therapy and quantitative structure-activity relationship studies with stable synthetic near-infrared-absorbing bacteriochlorin photosensitizers.
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DOI：
10.1021/jm901908s
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发表时间：
2010-05-27
影响因子：
7.3
通讯作者：
Hamblin, Michael R.
中科院分区：
文献类型：
--
作者：
Huang, Ying-Ying;Mroz, Pawel;Zhiyentayev, Timur;Sharma, Sulbha K.;Balasubramanian, Thiagarajan;Ruzie, Christian;Krayer, Michael;Fan, Dazhong;Borbas, K. Eszter;Yang, Eunkyung;Kee, Hooi Ling;Kirmaier, Christine;Diers, James R.;Bocian, David F.;Holten, Dewey;Lindsey, Jonathan S.;Hamblin, Michael R.
光动力疗法（PDT）是一种快速发展的治疗癌症的方法，其将无害的可见光和近红外光与无毒的光活化染料相结合，所述光活化染料在遇到分子氧时产生对癌细胞有毒的活性氧物质。细菌绿素是在大环中具有两个还原吡咯环的四吡咯化合物。这些分子的特征在于从700至>800 nm的强吸收特征，这使得能够深入渗透到组织中。本报告描述了12个新的稳定的合成菌绿素PDT活性的测试。这12个化合物具有多种外围取代基，并且在体外光照后对癌细胞具有非常强的杀伤作用。定量构效关系推导，并确定亚细胞定位。最具活性的化合物具有低的暗毒性和高的光毒性。这种结合与近红外吸收一起给予这些细菌绿素作为用于治疗癌症的光敏剂的巨大潜力。
Photodynamic therapy (PDT) is a rapidly developing approach to treating cancer that combines harmless visible and near-infrared light with a nontoxic photoactivatable dye, which upon encounter with molecular oxygen generates the reactive oxygen species that are toxic to cancer cells. Bacteriochlorins are tetrapyrrole compounds with two reduced pyrrole rings in the macrocycle. These molecules are characterized by strong absorption features from 700 to >800 nm, which enable deep penetration into tissue. This report describes testing of 12 new stable synthetic bacteriochlorins for PDT activity. The 12 compounds possess a variety of peripheral substituents and are very potent in killing cancer cells in vitro after illumination. Quantitative structure–activity relationships were derived, and subcellular localization was determined. The most active compounds have both low dark toxicity and high phototoxicity. This combination together with near-infrared absorption gives these bacteriochlorins great potential as photosensitizers for treatment of cancer.
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影响因子：
3
作者：
Lobner, D
通讯作者：
Lobner, D
影响因子：
3.3
作者：
HOLTEN, D;GOUTERMAN, M;ROCKLEY, MG
通讯作者：
ROCKLEY, MG
影响因子：
3.6
作者：
Krayer, Michael;Ptaszek, Marcin;Lindsey, Jonathan S.
通讯作者：
Lindsey, Jonathan S.
影响因子：
3.3
作者：
Mazor, O;Brandis, A;Scherz, A
通讯作者：
Scherz, A
影响因子：
3.3
作者：
Kee, Hooi Ling;Kirmaier, Christine;Hoten, Dewey
通讯作者：
Hoten, Dewey