Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (3): 759-766.DOI: 10.6023/cjocx201607022 Previous Articles     Next Articles

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冬凌草甲素卟啉壳聚糖微球的制备及体外光动力抗肿瘤活性研究

何洁a, 曹泳a, 袁强b   

  1. a 浙江中医药大学生命科学学院 杭州 310053;
    b 浙江中医药大学药学院 杭州 310053
  • 收稿日期:2016-07-14 修回日期:2016-10-21 出版日期:2017-03-25 发布日期:2016-11-22
  • 通讯作者: 袁强,E-mail:yuanqiang0825@sina.com E-mail:yuanqiang0825@sina.com
  • 基金资助:

    2017年浙江省中医药科技计划(No.2017ZB027)资助项目.

Preparation and Photocytotoxicity in vitro of Oridonin-porphyrinchitosan Microspheres

He Jiea, Cao Yonga, Yuan Qiangb   

  1. a College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053;
    b College of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou 310053
  • Received:2016-07-14 Revised:2016-10-21 Online:2017-03-25 Published:2016-11-22
  • Contact: 10.6023/cjocx201607022 E-mail:yuanqiang0825@sina.com
  • Supported by:

    Project supported by the Zhejiang Science and Technology Program of Traditional Chinese Medicine (No. 2017ZB027).

A emulsion crosslinking method to prepare oridonin-porphyrin-chitosan microspheres with oridonin and 5-p-(6-bromohexylaminophenyl)-10,15,20-triphenylporphyrin-chitosan (BHP-CS) is reported, which in turn was synthesized from 5-p-(6-bromo-hexylaminophenyl)-10,15,20-triphenylporphyrin (BHP) and chitosan. The porphyrin grafting rate of BHP-CS reached 30.80% on average, the drug loading rate and entrapment rate of the prepared microspheres reached 12.41% and 8.72% measured by HPLC, and the accumulated release rate was 81.74% in 48 h in vitro. The thiazolyl blue tetrazolium bromide (MTT) method was used to evaluate the photocytotoxicities of these derivatives against MCF-7 cells. The results revealed that oridonin-porphyrin-chitosan microspheres showed high photocytotoxicity in concentrations of 25, 50 and 100 μmol/mL against MCF-7 cells, and the inhibit ratio of MCF-7 cells under light irradiation for 30 min were (31.55±1.70)%, (71.03±0.76)% and (82.74±0.38)%, respectively.

Key words: oridonin, porphyrin, microspheres, photocytotoxicity, antitumor