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
收稿日期: 2016-07-14
修回日期: 2016-10-21
网络出版日期: 2016-11-22
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
Received date: 2016-07-14
Revised date: 2016-10-21
Online published: 2016-11-22
Supported by
Project supported by the Zhejiang Science and Technology Program of Traditional Chinese Medicine (No. 2017ZB027).
基于光-化联合抗肿瘤的目的，通过共价偶联将5-对（6-溴已氨基苯基）-10，15，20-三苯基卟啉（BHP）引入壳聚糖侧基制备复合物，卟啉枝接率平均达30.80%；采用乳化交联法制备了冬凌草甲素卟啉壳聚糖微球，经高效液相色谱（HPLC）测得微球载药量为12.41%，包封率为8.72%，48 h体外释放量达81.74%；采用噻唑蓝（MTT）法考察合成的系列化合物对人乳腺癌细胞MCF-7的光毒性.实验结果表明：浓度为25，50和100 μmol/mL的冬凌草甲素光敏微球光照30 min后对MCF-7细胞的光动力杀伤率的平均值分别达（31.55±1.70）%，（71.03±0.76）%和（82.74±0.38）%，光动力杀伤效果显著.
何洁 , 曹泳 , 袁强 . 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[J]. 有机化学, 2017 , 37(3) : 759 -766 . DOI: 10.6023/cjocx201607022
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
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