Li Xiao, Wang Wei, Fan Yi, Wei Yue, Yu Li-Qin, Wei Ji-Fu, Wang Yi-Fen
Biotechnology Developing Center of Henan Academy of Sciences, Henan Academy of Sciences, Zhengzhou 450002, Henan, People's Republic of China.
State Key Laboratory of Photochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, Yunnan, People's Republic of China,
Cancer Manag Res. 2018 Dec 6;10:6715-6729. doi: 10.2147/CMAR.S185387. eCollection 2018.
The roots and rhizomes of Hsiao are commonly used as anti-inflammatory, antipyretic, and analgesic remedies and detoxification agents in traditional Chinese medicine (TCM). Although has been considered as supplementary medicine for several disorders, the antitumor effect of this herb and its key components has not been explored.
The rhizomes of were isolated by chromatographic techniques. Structures of isolated compounds were identified based on spectroscopic methods and comparison with published data. The in vitro anticancer activities of purified components were also performed by MTT experiments. The in vivo anticancer activities were examined by subcutaneous tumor model or a breast cancer liver metastasis model.
In this study, we aimed to identify and characterize the effective antitumor components from the rhizomes of . By bioassay-guided fractionation techniques and chemical characterization, 12 cycloartane triterpenes and four chromones were isolated, among them, 11 compounds were identified in this genus at first. The identified two compounds showed dramatic inhibitory activities against breast cancer cells: compound 4 (23-epi-26-deoxyactein) and compound (cimigenol). Then, we examined the antitumor effect of these two selective candidate chemicals on triple-negative breast cancer (TNBC) cells in vivo and found that they could reduce tumor growth in subcutaneous tumor model or breast cancer liver metastasis model.
These results suggested that the selective compounds isolated from Hsiao could be the promising new agents for TNBC treatment.
小(Hsiao)的根及根茎在传统中药中常被用作抗炎、解热、镇痛药物及解毒剂。尽管小已被视为多种疾病的辅助药物,但其抗肿瘤作用及其关键成分尚未得到研究。
通过色谱技术分离小的根茎。基于光谱方法并与已发表数据进行比较来鉴定分离化合物的结构。纯化成分的体外抗癌活性也通过MTT实验进行。通过皮下肿瘤模型或乳腺癌肝转移模型检测体内抗癌活性。
在本研究中,我们旨在从小的根茎中鉴定并表征有效的抗肿瘤成分。通过生物活性导向的分离技术和化学表征,分离出12种环阿尔廷烷三萜和4种色酮,其中11种化合物在该属中首次被鉴定。鉴定出的两种化合物对乳腺癌细胞显示出显著的抑制活性:化合物4(23-表-26-脱氧actein)和化合物(升麻醇)。然后,我们在体内检测了这两种选择性候选化学物质对三阴性乳腺癌(TNBC)细胞的抗肿瘤作用,发现它们可以在皮下肿瘤模型或乳腺癌肝转移模型中减少肿瘤生长。
这些结果表明,从小中分离出的选择性化合物可能是治疗TNBC的有前景的新药物。