title: In vitro and in vivo antitumor activity of Macrothelypteris torresiana and its acute/subacute oral toxicity.
abstract: 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.
authors.affiliation: 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.
authors.forename: X H
authors.initials: XH
authors.lastname: Huang
authors.forename: P C
authors.initials: PC
authors.lastname: Xiong
authors.forename: C M
authors.initials: CM
authors.lastname: Xiong
authors.forename: Y L
authors.initials: YL
authors.lastname: Cai
authors.forename: A H
authors.initials: AH
authors.lastname: Wei
authors.forename: J P
authors.initials: JP
authors.lastname: Wang
authors.forename: X F
authors.initials: XF
authors.lastname: Liang
authors.forename: J L
authors.initials: JL
authors.lastname: Ruan
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D003512:Cyclohexanones / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D029624:Ferns / Q000737:chemistry* / Q000633:toxicity; D047309:Flavones / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D056945:Hep G2 Cells; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009369:Neoplasms / Q000188:drug therapy*; D008517:Phytotherapy; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D018517:Plant Roots; D012509:Sarcoma / Q000188:drug therapy*; D023041:Xenograft Model Antitumor Assays / Q000379:methods
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003512:Cyclohexanones; D047309:Flavones; D010936:Plant Extracts; C524112:protoapigenone