Abstract
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.
Highlights
Tumor, characterized by abnormal cell proliferation and metastasis, is one of the most attracted chronic diseases and remains the leading cause of death worldwide
It was observed that G. lucidum extract (GL) samples (p < 0.05) inhibited the proliferation of three tumor cell lines compared to the blank control
Fourteen ergosterol derivatives including a new one were isolated from the lipids enriched fraction of G. lucidum
Summary
Tumor, characterized by abnormal cell proliferation and metastasis, is one of the most attracted chronic diseases and remains the leading cause of death worldwide. Angiogenesis plays a key role in tumor formation, growth, invasion, and metastasis. Inhibiting the angiogenesis of tumors can cut off the supply of nutrients such as, oxygen and nutrients needed for tumor growth, and cut the way of tumor cell metastasis (Folkman, 1971; Papetti and Herman, 2002; McDougall et al, 2006; Berz and Wanebo, 2011). Inhibitors of tumor angiogenesis are considered to be an effective strategy for the treatment of cancer. Edible or medicinal fungi have attracted more and more attention due to their extensive pharmacological effect for chronic diseases (Loria-Kohen et al, 2014), especially for preventing or complementary treating cancer. The anti-cancer of G. lucidum research is very popular in recent decades. Steroids and other kinds of compounds were found in
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
