Quantitative and Site-Directed Chemical Modification of Hypocrellins toward Direct Drug Delivery and Effective Photodynamic Activity
文献类型：期刊论文
| 作者 | Deng, Hong1; Liu, Xin1; Xie, Jie1; Yin, Rong2; Huang, Naiyan2; Gu, Ying2; Zhao, Jingquan1 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-03-08 |
| 卷号 | 55期号:5页码:1910-1919 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/jm2017368 |
| 英文摘要 | For photodynamic therapy (PDT) treatment of microvascular diseases, drugs are delivered via blood circulation and the targets are vasculature endothelial cells, for which the contradictory requirements of hydrophilicity and lipophilicity of the drugs have been achieved by liposome preparations. Herein, it is demonstrated that the drug delivery and target affinity are achieved by a single chemical compound, hypocrellin B (HB) derivative 6 selected from three novel aminoalkanesulfonic acid HB derivatives, 5-7. 6 exhibits a much higher PDT activity (IC50 = 22 nM) on human gastric carcinoma BGC823 cells than HB, while it has no cellular toxicity in the dark. On the basis of estimation of the clinically required concentration according to relative PDT activity and clinical criteria, it can be predicted that 6 is directly deliverable to and PDT effective on target cells. The enhanced red absorption and superhigh photoactivity suggest that 6 is more powerful for PDT of tumors than HB. |
| 语种 | 英语 |
| WOS记录号 | WOS:000301170000011 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/48423]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Xie, Jie |
| 作者单位 | 1.Chinese Acad Sci, Beijing Natl Lab Mol Sci BNLMS, Key Lab Photochem, Inst Chem, Beijing 100080, Peoples R China 2.Chinese Peoples Liberat Army Gen Hosp, Dept Laser Med, Beijing 100853, Peoples R China |
| 推荐引用方式 GB/T 7714 | Deng, Hong,Liu, Xin,Xie, Jie,et al. Quantitative and Site-Directed Chemical Modification of Hypocrellins toward Direct Drug Delivery and Effective Photodynamic Activity[J]. JOURNAL OF MEDICINAL CHEMISTRY,2012,55(5):1910-1919. |
| APA | Deng, Hong.,Liu, Xin.,Xie, Jie.,Yin, Rong.,Huang, Naiyan.,...&Zhao, Jingquan.(2012).Quantitative and Site-Directed Chemical Modification of Hypocrellins toward Direct Drug Delivery and Effective Photodynamic Activity.JOURNAL OF MEDICINAL CHEMISTRY,55(5),1910-1919. |
| MLA | Deng, Hong,et al."Quantitative and Site-Directed Chemical Modification of Hypocrellins toward Direct Drug Delivery and Effective Photodynamic Activity".JOURNAL OF MEDICINAL CHEMISTRY 55.5(2012):1910-1919. |
入库方式： OAI收割
来源：化学研究所
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