ICCAS OpenIR
Novel Surfactant-like Hypocrellin Derivatives to Achieve Simultaneous Drug Delivery in Blood Plasma and Cell Uptake
Zhang, Yang1; Song, Liming1; Xie, Jie1; Qiu, Haixia2; Gu, Ying2; Zhao, Jingquan1
2010-05-01
Source PublicationPHOTOCHEMISTRY AND PHOTOBIOLOGY
ISSN0031-8655
Volume86Issue:3Pages:667-672
AbstractWater-soluble derivatives of hypocrellins can be safely delivered in blood plasma but lose their photodynamic activity in vivo due to poor cell uptake, while hydrophobic derivatives retaining their activity may aggregate in the blood plasma and block vascular networks. Considering both drug delivery and biological activity, surfactant-like hypocrellin B (HB) derivatives, sodium 12-2-HB-aminododecanoate (SAHB) and sodium 11,11'-5,8-HB-dimercaptoundecanoate (DMHB), were first designed and then synthesized in the current work. Both SAHB and DMHB were photoactive, generating free radicals and reactive oxygen species, as confirmed by EPR and chemical measurements. Most importantly, DMHB was not only readily soluble, allowing preparation of an intravenous injection solution at a clinically acceptable concentration, but it was also more photodynamic therapy (PDT) active to human breast carcinoma MCF-7 cells than its parent HB under irradiation. The photodynamic activity was exactly identical to the 1O(2) quantum yield and was not reduced by the improved water solubility, suggesting an independent hydrophilicity or lipophilicity. To our knowledge, this is a new strategy that possesses general significance for converting hydrophobic photosensitizers into clinically usable PDT drugs.
DOI10.1111/j.1751-1097.2010.00711.x
Indexed BySCI
Language英语
WOS IDWOS:000277301700027
PublisherWILEY-BLACKWELL
Citation statistics
Cited Times:14[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.iccas.ac.cn/handle/121111/69728
Collection中国科学院化学研究所
Corresponding AuthorZhao, Jingquan
Affiliation1.Chinese Acad Sci, Inst Chem, BNLMS, Key Lab Photochem, Beijing 100080, Peoples R China
2.Chinese Peoples Liberat Army Gen Hosp, Dept Laser Med, Beijing, Peoples R China
Recommended Citation
GB/T 7714
Zhang, Yang,Song, Liming,Xie, Jie,et al. Novel Surfactant-like Hypocrellin Derivatives to Achieve Simultaneous Drug Delivery in Blood Plasma and Cell Uptake[J]. PHOTOCHEMISTRY AND PHOTOBIOLOGY,2010,86(3):667-672.
APA Zhang, Yang,Song, Liming,Xie, Jie,Qiu, Haixia,Gu, Ying,&Zhao, Jingquan.(2010).Novel Surfactant-like Hypocrellin Derivatives to Achieve Simultaneous Drug Delivery in Blood Plasma and Cell Uptake.PHOTOCHEMISTRY AND PHOTOBIOLOGY,86(3),667-672.
MLA Zhang, Yang,et al."Novel Surfactant-like Hypocrellin Derivatives to Achieve Simultaneous Drug Delivery in Blood Plasma and Cell Uptake".PHOTOCHEMISTRY AND PHOTOBIOLOGY 86.3(2010):667-672.
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