华蟾素注射液中酯蟾毒配基的分离及体内外抗肿瘤活性筛选

高波; 魏晓露; 韩玲玉; 边宝林

doi:10.13422/j.cnki.syfjx.2017160078

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华蟾素注射液中酯蟾毒配基的分离及体内外抗肿瘤活性筛选

化学与分析 | 更新时间：2024-01-04

- 华蟾素注射液中酯蟾毒配基的分离及体内外抗肿瘤活性筛选
- Research on Isolation of Bufadienolides from Cinobufacin Injection and Its Activity Screening of Anti-cancer and
- 中国实验方剂学杂志 2017年23卷第16期页码：78-84
- 作者机构：
- 作者简介：
- 基金信息：
  
  国家“重大新药创制”科技重大专项（2013ZX09102025）;国家中药标准化项目（ZYBZH-C-AH-01）
- DOI：10.13422/j.cnki.syfjx.2017160078
  中图分类号： R285;R286.0
- 纸质出版日期：2017
- 稿件说明：
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高波, 魏晓露, 韩玲玉, 等. 华蟾素注射液中酯蟾毒配基的分离及体内外抗肿瘤活性筛选[J]. 中国实验方剂学杂志, 2017,23(16):78-84.

GAO Bo, WEI Xiao-lu, HAN Ling-yu, et al. Research on Isolation of Bufadienolides from Cinobufacin Injection and Its Activity Screening of Anti-cancer and [J]. Chinese journal of experimental traditional medical formulae, 2017, 23(16): 78-84.
高波, 魏晓露, 韩玲玉, 等. 华蟾素注射液中酯蟾毒配基的分离及体内外抗肿瘤活性筛选[J]. 中国实验方剂学杂志, 2017,23(16):78-84. DOI： 10.13422/j.cnki.syfjx.2017160078.

GAO Bo, WEI Xiao-lu, HAN Ling-yu, et al. Research on Isolation of Bufadienolides from Cinobufacin Injection and Its Activity Screening of Anti-cancer and [J]. Chinese journal of experimental traditional medical formulae, 2017, 23(16): 78-84. DOI： 10.13422/j.cnki.syfjx.2017160078.

摘要

目的：通过观察华蟾素注射液中酯蟾毒配基体内外抗肿瘤的作用效果和对部分酯蟾毒配基类单体体外抗胰腺癌细胞的药效筛选，以明确酯蟾毒配基抗胰腺癌的物质基础。方法：运用现代色谱技术分离华蟾素注射液，得到酯蟾毒配基类成分，采用HPLC-DAD-FT-ICR-MS分析并鉴定酯蟾毒配基类化合物的主要单体。通过体外细胞筛选酯蟾毒配基抗肿瘤的活性，在体内建立胰腺癌荷瘤裸鼠模型以评价酯蟾毒配基药效，在体外将分离所得酯蟾毒配基的主要活性单体进行抗胰腺癌活性筛选。结果：华蟾素注射液中的酯蟾毒配基在体外对肝癌BEL7402细胞，胃癌BGC823细胞和胰腺癌SW1990，MIA PaCa-2细胞的半数抑制浓度（IC50）分别为（0.47±0.03），（0.06±0.01），（0.06±0.02），（0.11±0.03） g·L-1，酯蟾毒配基的半数致死量（LD50）为20 mg·kg-1，体内对SW1990荷瘤裸鼠的治疗效果接近化疗药物吉西他滨，从酯蟾毒配基中分离并鉴定的12个活性物质体外抗胰腺癌的活性筛选出日蟾毒它灵、沙蟾毒精和嚏根草苷元对SW1990和BxPC-3细胞具有明显抑制作用。结论：华蟾素注射液中酯蟾毒配基在体外对胰腺癌细胞的抑制率与胃癌几乎相同，在体内对胰腺癌荷瘤裸鼠有明显治疗效果，同时酯蟾毒配基中的单体成分日蟾毒它灵、沙蟾毒精和嚏根草苷元在体外对胰腺癌细胞有明显的抑制作用。

Abstract

Objective: According to observation of the anti-cancer effect of bufadienolides from cinobufacin injection in vivo and in vitro and the anti-pancreatic cancer cells of bufadienolide monomers in vitro

to indentify the foundation of bufadienolides on anti-pancreatic cancer. Method: Modern chromatographic separation technology was adopted to obtain bufadienolides from cinobufacin injection

HPLC-DAD-FT-ICR-MS was employed to analysis and identify the main monomers of bufadienolides.Anti-cancer activity of bufadienolides was screened by in vitro cells

then setting up the pancreatic cancer animal model in nude mice in vivo for evaluating the efficacy of bufadienolides

the anti-pancreatic cancer activity of the main bufadienolide monomers in vitro was screened. Result: IC50 of bufadienolides from cinobufacin injection on hepatocellular carcinoma cells(BEL7402)

gastric carcinoma cells(BGC823) and pancreatic cancer cells (SW1990 and MIA PaCa-2) in vitro were (0.47±0.03)

(0.06±0.01)

(0.06±0.02)

(0.11±0.03) g· L-1

respectively.LD50 of bufadienolides was 20 mg·kg-1 and the treatment effect on SW1990 nude mice in vivo was close to gemcitabine.Gamabufotalin

arenobufagin and hellebrigenin had obvious inhibitory effect on SW1990 and BxPC-3 cells

which were isolated and identified from bufadienolides. Conclusion: Bufadienolides from cinobufacin injection shows almost the same inhibition rate on pancreatic cancer cells as gastric cancer in vitro

and it has apparently treatment effect on human pancreatic cancer bearing xenograft nude mice in vivo.Gamabufotalin

arenobufagin and hellebrigenin from bufadienolides show significantly inhibition on pancreatic cancer cells in vitro.

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