癌变·畸变·突变 ›› 2016, Vol. 28 ›› Issue (2): 81-90,96.doi: 10.3969/j.issn.1004-616x.2016.02.001

• 论著 •    下一篇

华卟啉钠的光漂白性质研究

刘汉清1, 姜智焕2, 吴文涛3, 魏金峰1,2, 靳洪涛1,2, 王爱平1,2   

  1. 1. 中国医学科学院北京协和医学院药物研究所, 北京 100050;
    2. 北京协和建昊医药技术开发有限责任公司, 北京 100176;
    3. 奥溪利亚医药科技有限公司, 天津 300384
  • 收稿日期:2015-07-10 修回日期:2015-12-19 出版日期:2016-03-31 发布日期:2016-03-31
  • 通讯作者: 靳洪涛,E-mail:jinhongtao@imm.ac.cn;王爱平,E-mail:wangaiping@imm.ac.cn E-mail:jinhongtao@imm.ac.cn;wangaiping@imm.ac.cn
  • 作者简介:刘汉清,E-mail:hanqingl@163.com
  • 基金资助:
    国家重大新药创制资助项目(2013ZX09302302,2012ZX09J12203,2012ZX09301002-001-009)

Research on photobleaching characters of sinoporphyrin sodium

LIU Hanqing1, JIANG Zhihuan2, WU Wentao3, WEI Jinfeng1,2, JIN Hongtao1,2, WANG Aiping1,2   

  1. 1. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050;
    2. Beijing Union-Genius Pharmaceutical Technology Development Co., Ltd., Beijing 100176;
    3. Ocelean Pharmaceutical Technology Company, Tianjin 300384, China
  • Received:2015-07-10 Revised:2015-12-19 Online:2016-03-31 Published:2016-03-31

摘要: 目的: 观察华卟啉钠(DVDMS)在不同溶液中及动物皮肤中的光漂白性质。方法: 采用微量分光光度计,测量不同浓度DVDMS(10、20、40 μg/mL)在生理盐水(NS)、RPMI-1640培养基(RPMI-1640)、含10%胎牛血清的RPMI-1640培养基(RPMI-FBS)和HaCaT细胞悬液中的吸收峰;设置DVDMS浓度1、2.5、5、10、20、40 μg/mL,采用酶标仪分别检测在激光照射3、6、10、20、40、50、60、120、180 min后DVDMS在上述4种溶液中的光漂白;正常和银屑病裸鼠均尾静脉注射DVDMS 2 mg/kg,采用小动物活体成像仪观察DVDMS在皮肤组织中的分布及激光照射后在银屑病模型动物皮肤组织中的漂白现象。结果: DVDMS 10、20、40 μg/mL在本实验设置的4种溶液中特征吸收峰明显;在前期药效学研究的条件下(激光照射3 min),DVDMS在4种溶液中发生了光漂白;在180 min内,DVDMS的光漂白呈现先快后慢的二相过程;DVDMS在正常和银屑病模型动物组织中分布均匀,在9.6 J/cm2激光照射后,DVDMS在银屑病模型动物皮肤组织中发生了明显光漂白。结论: DVDMS体外光漂白受光剂量、初始浓度、溶剂种类的影响,符合二级动力学模型,在银屑病模型动物皮肤组织中被激光照射后可发生光漂白。

关键词: 华卟啉钠, 激光, 光漂白, 银屑病

Abstract: OBJECTIVE: To observe the photobleaching characters of sinoporphyrin sodium (DVDMS) in different solutions and skins of animal. METHODS: Absorption peaks of DVDMS (10, 20, 40 μg/mL) in normal saline (NS), RPMI-1640 medium (RPMI-1640), RPMI-1640 medium containing 10% fetal calf serum (RPMI-FBS) and suspension of HaCaT cells were measured using micro-spectrophotometer. Using DVDMS solutions with concentrations of 1, 2.5, 5, 10, 20 and 40 μg/mL in the 4 solvents above, photobleaching of DVDMS after laser radiation for 3, 6, 10, 20, 40, 50, 60, 120, 180 min was observed using microplate reader. In vivo image acquisition system was used to study the distribution of DVDMS in animal skins, and the bleaching after irradiation in psoriasis-like animal skins were also observed. RESULTS: DVDMS with concentrations 10, 20 and 40 μg/mL showed obvious characteristic absorption peaks in the 4 solutions. Photobleaching occurred in the 4 solutions under the irradiation conditions used in previous pharmacodynamics studies (laser radiation was 3 minutes). Two-phase processes photobleaching (fast first phase and second slow phase) of DVDMS were observed in 180 min. The distributions of DVDMS in skins of normal and psoriasis-like animal were uniform, obvious photobleaching occurred in skins of psoriasis-like animal after laser irradiation with dose of 9.6 J/cm2. CONCLUSION: In vitro photobleaching of DVDMS was influenced by light dose, initial concentrations and solvents. Secondary-dynamic model was suitable to describe the photobleaching progress. Photobleaching occurred in skins of psoriasis-like animal after laser irradiation.

Key words: sinoporphyrin sodium, laser, photobleaching, psoriasis

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