Quantitative and Site-Directed Chemical Modification of Hypocrellins toward Direct Drug Delivery and Effective Photodynamic Activity

doi:10.1021/jm2017368

CORC > 化学研究所 > 中国科学院化学研究所

	Quantitative and Site-Directed Chemical Modification of Hypocrellins toward Direct Drug Delivery and Effective Photodynamic Activity
	Deng, Hong 1; Liu, Xin 1; Xie, Jie 1; Yin, Rong 2; Huang, Naiyan 2; Gu, Ying 2; Zhao, Jingquan 1
刊名	JOURNAL OF MEDICINAL CHEMISTRY
	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
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000301170000011
内容类型	期刊论文
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.