In vitro and in vivo antitumor activity of Macrothelypteris torresiana and its acute/subacute oral toxicity

In vitro and in vivo antitumor activity of Macrothelypteris torresiana and its acute/subacute oral toxicity
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托雷西毛毛蕨的体内外抗肿瘤活性及其急性/亚急性口服毒性

DOI:
10.1016/j.phymed.2010.03.006
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发表时间:
2010-10-01
期刊:
影响因子:
7.9
通讯作者:
Ruan, J. L.
Ruan, J. L.
中科院分区:
医学1区
文献类型:
--
作者:
Huang, X. H.;Xiong, P. C.;Ruan, J. L.

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本研究的目的是通过研究原芹菜酮的体外抗肿瘤活性以及M根总黄酮部分的体内抗肿瘤活性和急性/亚急性口服毒性来评价大针蕨的抗肿瘤潜力。torresiana。认为原芹菜酮是总黄酮部位的主要成分,可能在抗肿瘤活性中起关键作用。torresiana中,MIT测定用于研究原芹菜酮的体外抗肿瘤活性。我们的研究表明,M. torresiana对Hep G2、Tca-8113、MCF-7、M5和K562显示出显著的抗肿瘤活性,IC 50值分别为2.3、0.6、0.8、0.3和0.9 μ g/ml。使用制剂1、2和3评价总黄酮级分的抗肿瘤潜力,所述制剂1、2和3分别由用无菌盐水直接稀释的总黄酮级分、用羧甲基纤维素钠(CMC-Na)溶解和用羟丙基-β-环糊精包合而制备。在完成肿瘤接种24小时后,在BALB/c小鼠中使用小鼠肉瘤S-180进行体内研究。在制剂2和3的处理组中观察到显著的抗肿瘤活性,特别是高剂量和中剂量显示出非常高的肿瘤生长抑制率(>50%)。与阳性对照组(5-氟尿嘧啶)相比,未观察到显著差异。进行急性/亚急性经口毒性试验,急性经口毒性结果表明,制剂2和3的LD 50值分别为2.76和0.87 g/kg体重,分别亚急性经口毒性试验结果表明,总黄酮部位毒性较低。本研究的总体结果表明,从M。torresiana显示出显著的抗肿瘤活性,并且代表了治疗癌症的潜在药物来源。(C)2010年Elsevier GmbH。All rights reserved.
The aim of this study was to evaluate the antitumor potential of Macrothelypteris torresiana by studying in vitro antitumor activity of the protoapigenone, as well as in vivo antitumor activity and acute/subacute oral toxicity of the total flavonoid fraction from the roots of M. torresiana. Considering that the protoapigenone is a main constituent of the total flavonoid fraction and it might play a key role in the antitumor activity of M. torresiana, the MIT assay was used to investigate the in vitro antitumor activity of the protoapigenone. Our study revealed that the protoapigenone of M. torresiana showed significant antitumor activity towards Hep G2, Tca-8113, MCF-7, M5 and K562 with IC50 values of 2.3, 0.6, 0.8, 0.3 and 0.9 mu g/ml, respectively. The antitumor potential of the total flavonoid fraction was evaluated using preparations 1, 2 and 3, which were prepared by total flavonoid fraction directly diluted with sterile saline, dissolved using sodium carboxymethyl cellulose (CMC-Na) and included by hydroxypropyl-beta-cyclodextrin, respectively. These were investigated in vivo using mouse sarcoma S-180 in BALB/c mice after completing tumor inoculation for 24 h. Pronounced antitumor activity was observed in the treated groups for preparations 2 and 3, and the high and medium doses in particular showed very high inhibition ratio of tumor growth (>50%). No significant difference was observed when compared to the positive control group (5-fluorouracil). The acute/subacute oral toxicity test was performed, and the results of acute oral toxicity showed that the LD50 values of preparations 2 and 3 were 2.76 and 0.87 g/kg body wt., respectively. According to the results of the subacute oral toxicity study, the total flavonoid fraction had low toxicity. The overall results of this study suggest that the total flavonoid fraction from the roots of M. torresiana shows significant antitumor activity and represents a potential source of medicine for the treatment of cancer. (C) 2010 Elsevier GmbH. All rights reserved.