Zhang Henan, Shao Qian, Wang Wenhan, Zhang Jingsong, Zhang Zhong, Liu Yanfang, Yang Yan
Institute of Edible Fungi, Shanghai Academy of Agricultural Sciences, National Engineering Research Center of Edible Fungi, Key Laboratory of Edible Fungi Resources and Utilization (South), Ministry of Agriculture, Shanghai 201403, China.
Molecules. 2017 Apr 27;22(5):698. doi: 10.3390/molecules22050698.
The inhibition of tumor-cell proliferationbyan organicsolvent extract from the solid-state fermentation of mycelia inoculated in rice medium was investigated in vitro. The active compounds inhibiting tumor-cell proliferation were characterized. Results revealed that all (petroleum ether, chloroform, ethyl acetate, and butanol) fractions inhibited tumor-cell proliferation in a dose-dependent fashion. The ethyl acetate extract had the highest inhibitory effecton tumor-cell proliferation, and the butanol fraction had the lowest. Six compounds were isolated and purified from the ethyl acetate extract of mycelia by the tandem application of silica-gel column chromatography (SGCC), high-speed countercurrent chromatography (HSCCC), and preparative HPLC. These compounds were identified by NMR and electrospray ionization-mass spectrometry (ESI-MS) spectroscopic methods as ergosterol (RF1), ergosta-7,22-dien-3β-yl pentadecanoate (RF3), 3,4-dihydroxy benzaldehyde(RF6), inoscavinA (RF7), baicalein(RF10), and 24-ethylcholesta-5,22-dien-3β-ol (RF13). To further clarify the activity of these compounds, the cell-proliferation-inhibition tests of these compounds on various tumor cells were carried out and evaluatedin vitro. Results suggested that compounds RF6, RF7, and RF10 had potent inhibition effects on the proliferation of a series of tumor cell lines, including K562, L1210, SW620, HepG2, LNCaP, and MCF-7cells. These findings indicated that mycelia produced by solid-state fermentation in rice canbe used to obtain active compounds with the ability to inhibittumor-cell proliferation.
体外研究了接种于大米培养基上的菌丝体固态发酵所得有机溶剂提取物对肿瘤细胞增殖的抑制作用。对抑制肿瘤细胞增殖的活性化合物进行了表征。结果显示,所有(石油醚、氯仿、乙酸乙酯和正丁醇)馏分均以剂量依赖性方式抑制肿瘤细胞增殖。乙酸乙酯提取物对肿瘤细胞增殖的抑制作用最强,正丁醇馏分的抑制作用最弱。通过硅胶柱色谱(SGCC)、高速逆流色谱(HSCCC)和制备型高效液相色谱(HPLC)串联应用,从菌丝体的乙酸乙酯提取物中分离并纯化出6种化合物。通过核磁共振(NMR)和电喷雾电离质谱(ESI-MS)光谱法将这些化合物鉴定为麦角甾醇(RF1)、麦角甾-7,22-二烯-3β-基十五烷酸酯(RF3)、3,4-二羟基苯甲醛(RF6)、肌醇甲素A(RF7)、黄芩素(RF10)和24-乙基胆甾-5,22-二烯-3β-醇(RF13)。为进一步阐明这些化合物的活性,对这些化合物在各种肿瘤细胞上的细胞增殖抑制试验进行了体外开展和评估。结果表明,化合物RF6、RF7和RF10对一系列肿瘤细胞系的增殖具有显著抑制作用,包括K562、L1210、SW620、HepG2、LNCaP和MCF-7细胞。这些发现表明,大米固态发酵产生的菌丝体可用于获得具有抑制肿瘤细胞增殖能力的活性化合物。