Key Laboratory of Natural Medicinal Chemistry and Resources Evaluation of Hubei Province, College of Pharmacy, Tongji Medical College of Huazhong, University of Science and Technology, 13# Hangkong Road, Wuhan 430030, PR China.
Phytomedicine. 2010 Oct;17(12):930-4. doi: 10.1016/j.phymed.2010.03.006. Epub 2010 Apr 9.
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 MTT 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 IC(50) values of 2.3, 0.6, 0.8, 0.3 and 0.9 μg/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-β-cyclodextrin, respectively. These were investigated in vivo using mouse sarcoma S-180 in BALB/c mice after completing tumor inoculation for 24h. 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 LD(50) 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.
本研究旨在评估Macrothelypteris torresiana 的抗肿瘤潜力,研究其原花青素的体外抗肿瘤活性,以及其根总黄酮部位的体内抗肿瘤活性和急性/亚急性口服毒性。考虑到原花青素是总黄酮部位的主要成分,并且可能在 M. torresiana 的抗肿瘤活性中发挥关键作用,因此我们使用 MTT 法研究了原花青素的体外抗肿瘤活性。我们的研究表明,M. torresiana 的原花青素对 Hep G2、Tca-8113、MCF-7、M5 和 K562 具有显著的抗肿瘤活性,IC50 值分别为 2.3、0.6、0.8、0.3 和 0.9 μg/ml。总黄酮部位的抗肿瘤潜力通过直接用无菌生理盐水稀释总黄酮部位制备的制剂 1、2 和 3 进行评估,分别用羧甲基纤维素钠(CMC-Na)溶解和羟丙基-β-环糊精包合。在接种肿瘤 24 小时后,在 BALB/c 小鼠的肉瘤 S-180 中进行体内研究。制剂 2 和 3 的治疗组表现出明显的抗肿瘤活性,特别是高剂量和中剂量表现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,没有观察到显著差异。进行了急性/亚急性口服毒性试验,急性口服毒性试验结果表明,制剂 2 和 3 的 LD50 值分别为 2.76 和 0.87 g/kg 体重。根据亚急性口服毒性研究的结果,总黄酮部位的毒性较低。本研究的总体结果表明,M. torresiana 根的总黄酮部位具有显著的抗肿瘤活性,是治疗癌症的潜在药物来源。