Optimization of hypocrellin B derivative amphiphilicity and biological activity
文献类型：期刊论文
| 作者 | Liu Xin1,2; Xie Jie1,2; Zhang LuYong3; Chen HongXia3; Gu Ying3; Zhao JingQuan1,2 |
| 刊名 | CHINESE SCIENCE BULLETIN
 |
| 出版日期 | 2009-06-01 |
| 卷号 | 54期号:12页码:2045-2050 |
| 关键词 | Hypocrellin Derivatives PhoTodynamic Therapy To Vas Capillary Diseases Drug Delivery Target Affinity Epr Spectra Phtotoxicity |
| ISSN号 | 1001-6538 |
| DOI | 10.1007/s11434-009-0036-3 |
| 英文摘要 | To satisfy the dual requirements of the fluent transportation in blood and the affinity to the target tissues of vascular diseases, hypocrellin derivatives with optimized amphiphilicity are expected. In this work, 3-amino-1-propanesulfonic acid and 4-amino-1-butanesulfonic acid substituted hypocrellin B, named compounds 1 and 2, were designed, synthesized in high yields and characterized. Besides greatly strengthened red absorption, the maximum solubility of compound 2 in phosphate buffered saline (PBS) is 4.2 mg/mL which is just enough to prepare an aqueous solution for intravenous injection in clinically acceptable concentration, while the partition coefficient between n-octanol and PBS, 5.6, benefits the cell-uptake and biological activity as well. Furthermore, EPR measurements reveal that the photosensitization activities of the two compounds to generate semiquinone anion radicals, superoxide anion radicals and singlet oxygen are a little bit higher than those of taurine substituted hypocrellin B (THB), but the photodynamic activities to human lung cancer A549 cells are several times that of THB, mainly due to increases in lipophilicity and cell-uptake. |
| 语种 | 英语 |
| WOS记录号 | WOS:000267145500011 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/66523]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Zhao JingQuan |
| 作者单位 | 1.Chinese Acad Sci, Inst Chem, BNLMS, Beijing 100080, Peoples R China 2.Chinese Acad Sci, Inst Chem, Key Lab Photochem, Beijing 100080, Peoples R China 3.Chinese Peoples Librat Army Gen Hosp, Dept Laser Med, Beijing 100853, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu Xin,Xie Jie,Zhang LuYong,et al. Optimization of hypocrellin B derivative amphiphilicity and biological activity[J]. CHINESE SCIENCE BULLETIN,2009,54(12):2045-2050. |
| APA | Liu Xin,Xie Jie,Zhang LuYong,Chen HongXia,Gu Ying,&Zhao JingQuan.(2009).Optimization of hypocrellin B derivative amphiphilicity and biological activity.CHINESE SCIENCE BULLETIN,54(12),2045-2050. |
| MLA | Liu Xin,et al."Optimization of hypocrellin B derivative amphiphilicity and biological activity".CHINESE SCIENCE BULLETIN 54.12(2009):2045-2050. |
入库方式： OAI收割
来源：化学研究所
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