The in Vitro and in Vivo Antitumor Activities of Tetracyclic Triterpenoids Compounds Actein and 26-Deoxyactein Isolated from Rhizome of Cimicifuga foetida L.
Wu, Desong1,2,3; Yao, Qi3; Chen, Yajuan1,2; Hu, Xiaodong4; Qing, Chen1,2; Qiu, Minghua5
2016-08-01
Source PublicationMOLECULES
Volume21Issue:8Pages:1001
AbstractAims: This work aims to study the in vitro and in vivo antitumor activities of tetracyclic triterpenoids compounds actein and 26-deoxyactein. Further, the mechanism is investigated. Methods: In vitro, a modified MTT method was used to assay the cytotoxicities of actein and 26-deoxyactein in 12 human tumor cell lines. In vivo, mouse sarcoma S180 and human lung cancer A549 cells were respectively implanted subcutaneously in ICR mice and nude mice to establish implanted tumor models. Flow cytometry (FCM) was used to assay the cycle distribution of the tumor cells. Immunohistochemistry was used to measure CD31-positive expression in the xenogrft tumor by analyzing microvessel density (MVD). In addition, acute toxicities of actein and 26-deoxyactein were also evaluated. Results: Actein and 26-deoxyactein inhibited the proliferation of the 12 human cancer cell lines tested with the values of 50% inhibitory concentrations (IC50) between 12.29 and 88.39 mu g/mL. In vivo, both actein (3-27 mg/kg) and 26-deoxyactein (3-27 mg/kg) significantly inhibited the growth of the implanted sarcoma S180 in a dose-dependent manner. Actein (10, 30 mg/kg) and 26-deoxyactein (10, 30 mg/kg) markedly inhibited the xenograft growth with T/C (%) values of 38%, 55% for actein, and 35%, 49% for 26-deoxyactein. Compared with the vehicle control, actein (10, 30 mg/kg) and 26-deoxyactein (10, 30 mg/kg) significantly reduced the MVD in the xenograft tumor. The FCM result showed that human leukemia HL-60 cells were arrested at G1 phase after treated with either actein (6.25-25 mu g/mL) or 26-deoxyactein (6.25-25 mu g/mL) for 48 h. A limited trial in mice showed that both of the minimal lethal doses (MLDs) of actein and 26-deoxyactein were over 5 g/kg. Conclusions: Both actein and 26-deoxyactein have low toxicities. Importantly, both these two tetracyclic triterpenoids compounds isolated from rhizome of Cimicifuga foetida L. have significant antitumor activities in vitro and in vivo, which is associated with cell cycle arrest and angiogenesis inhibition.
KeywordActein 26-deoxyactein Antitumor Activity Ic50 Cell Cycle
DOI10.3390/molecules21081001
Indexed BySCI
Language英语
WOS IDWOS:000382334600040
Citation statistics
Cited Times:10[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/33608
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.Kunming Med Univ, Sch Pharmaceut Sci, Kunming 650500, Peoples R China
2.Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Kunming 650500, Peoples R China
3.Yunnan Inst Mat Med, Dept Pharmacol, Kunming 650111, Peoples R China
4.Bengbu Med Coll, Dept Histol & Embryol, Bengbu 233030, Peoples R China
5.Chinese Acad Sci, Kunming Inst Bot, Kunming 650201, Peoples R China
Recommended Citation
GB/T 7714
Wu, Desong,Yao, Qi,Chen, Yajuan,et al. The in Vitro and in Vivo Antitumor Activities of Tetracyclic Triterpenoids Compounds Actein and 26-Deoxyactein Isolated from Rhizome of Cimicifuga foetida L.[J]. MOLECULES,2016,21(8):1001.
APA Wu, Desong,Yao, Qi,Chen, Yajuan,Hu, Xiaodong,Qing, Chen,&Qiu, Minghua.(2016).The in Vitro and in Vivo Antitumor Activities of Tetracyclic Triterpenoids Compounds Actein and 26-Deoxyactein Isolated from Rhizome of Cimicifuga foetida L..MOLECULES,21(8),1001.
MLA Wu, Desong,et al."The in Vitro and in Vivo Antitumor Activities of Tetracyclic Triterpenoids Compounds Actein and 26-Deoxyactein Isolated from Rhizome of Cimicifuga foetida L.".MOLECULES 21.8(2016):1001.
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