Anti-tumor and Anti-angiogenic Ergosterols from Ganoderma lucidum.
Anti-tumor and Anti-angiogenic Ergosterols from Ganoderma lucidum.
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DOI：
10.3389/fchem.2017.00085
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发表时间：
2017
影响因子：
5.5
通讯作者：
Xie Y
中科院分区：
文献类型：
--
作者：
Chen S;Yong T;Zhang Y;Su J;Jiao C;Xie Y
本研究从灵芝提取物的富脂部分分离化学成分，并评价其对肿瘤细胞和人脐静脉内皮细胞（HUVECs）的抗增殖作用。从茯苓脂质富集部位分离纯化麦角甾醇衍生物（1-14）。它们的化学结构是通过光谱分析或与先前报道的质量和核磁共振光谱数据进行比较确定的。其中化合物1经纯化，为新化合物。所有化合物的体外抗人肿瘤细胞和HUVECs的增殖作用进行了评价。化合物9 ~ 13对2种人肿瘤细胞和HUVECs均有抑制作用，表明这4个化合物具有抗肿瘤和抗血管生成的双重活性。化合物2对两种肿瘤细胞系有明显的选择性抑制作用，化合物3对HUVECs有明显的选择性抑制作用。通过3D-QASR技术揭示了抑制人HepG2细胞的构效关系。测定了灵芝原料和产品中不同部位麦角甾醇的含量。本研究为麦角甾醇衍生物作为天然营养保健品和功能性食品原料的进一步开发利用，或作为抗肿瘤、抗血管生成化疗药物的潜在来源提供了基础。
This study was carried out to isolate chemical constituents from the lipid enriched fraction of Ganoderma lucidum extract and to evaluate their anti-proliferative effect on tumor cells and human umbilical vein endothelial cells (HUVECs). Ergosterol derivatives (1–14) were isolated and purified from the lipid enriched fraction of G. lucidum. Their chemical structures were established by spectroscopic analyses or by comparison of mass and NMR spectral data with those reported previously. Amongst, compound 1 was purified and identified as a new one. All the compounds were evaluated for their anti-proliferative effect on human tumor cells and HUVECs in vitro. Compounds 9–13 displayed inhibitory activity against two types of human tumor cells and HUVECs, which indicated that these four compounds had both anti-tumor and anti-angiogenesis activities. Compound 2 had significant selective inhibition against two tumor cell lines, while 3 exhibited selective inhibition against HUVECs. The structure–activity relationships for inhibiting human HepG2 cells were revealed by 3D-QASR. Ergosterol content in different parts of the raw material and products of G. lucidum was quantified. This study provides a basis for further development and utilization of ergosterol derivatives as natural nutraceuticals and functional food ingredients, or as source of new potential antitumor or anti-angiogenesis chemotherapy agent.
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影响因子：
--
作者：
Li X;Wu Q;Xie Y;Ding Y;Du WW;Sdiri M;Yang BB
通讯作者：
Yang BB
影响因子：
4.6
作者：
Liang F;Han Y;Gao H;Xin S;Chen S;Wang N;Qin W;Zhong H;Lin S;Yao X;Li S
通讯作者：
Li S
影响因子：
2.5
作者：
Berz, David;Wanebo, Harold
通讯作者：
Wanebo, Harold
影响因子：
3.8
作者：
KAWAGISHI, H;KATSUMI, R;NAKAMURA, T
通讯作者：
NAKAMURA, T
DOI：
10.1615/interjmedicmush.v5.i4.60
发表时间：
2003-01-01
影响因子：
1.2
作者：
Kang, Jie;Wang, Hong-Qing;Chen, Ruo-Yun
通讯作者：
Chen, Ruo-Yun