白山毛桃根抗脑胶质瘤活性成分及其纳米胶束的制备

doi:10.7503/cjcu20180507

高等学校化学学报 ›› 2019, Vol. 40 ›› Issue (3): 468.doi: 10.7503/cjcu20180507

白山毛桃根抗脑胶质瘤活性成分及其纳米胶束的制备

唐霖¹, 蒋振奇², 李娟²(), 吴爱国²()

1. 浙江医药高等专科学校, 宁波 315100
2. 中国科学院宁波材料技术与工程研究所, 宁波 315201

收稿日期:2019-07-17 出版日期:2019-01-12 发布日期:2019-01-12
作者简介:
联系人简介: 吴爱国, 男, 博士, 研究员, 博士生导师, 主要从事纳米材料的制备与应用研究. E-mail: aiguo@nimte.ac.cn; 李娟, 女, 博士, 副研究员, 主要从事抗肿瘤纳米药物研究. E-mail: lij@nimte.ac.cn
基金资助:
浙江省教育厅科研项目(批准号: Y201636812)、国家自然科学基金(批准号: 81871411, U143211)和浙江省公益技术应用研究项目(批准号: 2016C33093)资助.

Anti-glioma Active Compounds and Their Nanomicelles Preparation of the Root of Actinidiaeriantha Benth^†

TANG Lin¹, JIANG Zhenqi², LI Juan^2,^*(), WU Aiguo^2,^*()

1. Zhejiang Pharmaceutical College, Ningbo 315100, China
2. Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo 315201, China

Received:2019-07-17 Online:2019-01-12 Published:2019-01-12
Contact: LI Juan,WU Aiguo E-mail:lij@nimte.ac.cn;aiguo@nimte.ac.cn
Supported by:
† Supported by the Scientific Research Fund of Zhejiang Provincial Education Department, China(No.Y201636812), the National Natural Science Foundation of China(Nos.81871411, U143211) and the Fund of the Science and Technology Department of Zhejiang Province, China(No.2016C33093).

摘要/Abstract

摘要：

采用溶剂提取和萃取方法得到白山毛桃根乙酸乙酯、正丁醇和水层萃取物. 通过噻唑蓝(MTT)比色法考察了各萃取物对脑胶质瘤细胞U87MG活性的抑制作用. 采用高效液相色谱(HPLC)指纹图谱法比对确认活性部位的主要化学成分为2α,3α,24-三羟基-12-烯-28-乌苏酸. 采用溶剂挥发法制备了2α,3α,24-三羟基-12-烯-28-乌苏酸纳米胶束, 对其包封率、粒径及ζ电位等进行了表征, 并考察了其抗肿瘤活性. 体外细胞实验结果表明, 白山毛桃根乙酸乙酯萃取物对脑胶质瘤细胞U87MG具有抑制作用, 通过与标准品比对确认2α,3α,24-三羟基-12-烯-28-乌苏酸为乙酸乙酯部位的主要成分, 且该成分对脑胶质瘤细胞活性具有较强抑制作用. 通过溶剂挥发法制备的2α,3α,4-三羟基-12-烯-28-乌苏酸纳米胶束包封率为64.7%, 粒径为20 nm, 粒径分布宽度(PDI)为0.246, ζ电位为-5.7 mV. 细胞实验结果进一步证明, 与单体化合物相比, 2α,3α,24-三羟基-12-烯-28-乌苏酸纳米胶束对脑胶质瘤细胞活性具有更强的抑制作用, 为白山毛桃根在脑胶质瘤治疗中的应用提供了实验依据.

关键词: 白山毛桃根, 2α;, 3α;, 24-三羟基-12-烯-28-乌苏酸, 脑胶质瘤, 活性成分, 纳米胶束

Abstract:

Actinidiaeriantha Benth was extracted by ethyl acetate, n-butyl alcohol and water, and three fractions were obtained. The in vitro cell experiments showed that ethyl acetate was the anti-glioma active fraction of the root of Actinidiaeriantha Benth. The high performance liquid chromatographic fingerprint confirmed that main compound of ethyl acetate fraction was 2α,3α,24-trihydroxyurs-12-en-28-oic acid, and it could significantly inhibit the glioma cell activity. The prepared 2α,3α,24-trihydroxyurs-12-en-28-oic acid loaded nanomicelles was with high loading efficiency of 64.7%, average diameter of 20 nm with polydispersity index(PDI) of 0.246 and ζ potential of -5.7 mV. Further cell experiment demonstrated the 2α,3α,24-trihydroxyurs-12-en-28-oic acid loaded nanomicelles through solvent evaporation with better inhibitory effects on the glioma cells than free one. Taken together, the ethyl acetate fractions from the root of Actinidiaeriantha Benth were confirmed with the anti-glioma activity, and 2α,3α,24-trihydroxyurs-12-en-28-oic acid was the main active compound. The prepared 2α,3α,24-trihydroxyurs-12-en-28-oic acid loaded nanomicelles was with good water dispersity and anti-glioma activity, providing solid experimental base for the application of the root of Actinidiaeriantha Benth in glioma therapy.

Key words: Root of Actinidiaeriantha Benth, 2α;, 3α;, 24-Trihydroxyurs-12-en-28-oic acid, Glioma, Active compound, Nanomicelle

TrendMD:

唐霖, 蒋振奇, 李娟, 吴爱国. 白山毛桃根抗脑胶质瘤活性成分及其纳米胶束的制备. 高等学校化学学报, 2019, 40(3): 468.

TANG Lin,JIANG Zhenqi,LI Juan,WU Aiguo. Anti-glioma Active Compounds and Their Nanomicelles Preparation of the Root of Actinidiaeriantha Benth^†. Chem. J. Chinese Universities, 2019, 40(3): 468.

图/表 4

Fig.1 Cell viability of U87 MG cells after incubation with different extracts for 24 h n-Butanol extraction layer; ethyl acetate extraction layer; water extraction layer.

Fig.2 High performance liquid chromatogram of the standard sample(a), the n-butanol layer extract(b), the ethyl acetate layer extract(c) and the aqueous layer extract(d)

Fig.3 TEM image of 2α,3α,24-trihydroxy-12-en-28-oic acid-loaded nanomicelles

Fig.4 Cell inhibition effect of 2α,3α,24-trihydroxyurs-12-ene-28-olic acid() and its nanomicelles() on U87MG cell for 24 h

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白山毛桃根抗脑胶质瘤活性成分及其纳米胶束的制备

Anti-glioma Active Compounds and Their Nanomicelles Preparation of the Root of Actinidiaeriantha Benth^†

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白山毛桃根抗脑胶质瘤活性成分及其纳米胶束的制备

Anti-glioma Active Compounds and Their Nanomicelles Preparation of the Root of Actinidiaeriantha Benth†

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Anti-glioma Active Compounds and Their Nanomicelles Preparation of the Root of Actinidiaeriantha Benth^†