Abstract
Triterpenoids isolated from Ganoderma lucidum (GLTs) exhibit a broad spectrum of anti-cancer properties, including anti-proliferative, anti-metastatic and anti-angiogenic activities. Current research studies revealed the role by GLTs in inducing apoptosis and suppression of telomerase activity of cancer cells with much lower toxicity to healthy cells. Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or downregulate the oncogenes and may act as anti-cancer agents. Targeting human telomeric G-quadruplex DNA could be one of the mechanisms by which these GLTs exert anti-cancer activity. In this study, 208 GLTs were screened for ligands with high binding affinity and selectively to stabilize the pG4DNA by using the docking tool AutoDock4. The results showed that ganoderic acid A and ganoderic acid Df exhibit high binding affinity and selectively bind to the lateral groove of pG4DNA. Based on our findings, we suggest that the triterpenoid represents a new class of G-quadruplex groove binding ligands and thus act as potential anti-cancer agents.
Highlights
Triterpenoids isolated from Ganoderma lucidum (GLTs) exhibit a broad spectrum of anti-cancer properties, including anti-proliferative, anti-metastatic and anti-angiogenic activities
Cancer cell growth properties, which are documented in the ancient reports inhibition induced by GL extract (GLE) is mediated via apoptosis associated where GL is praised for its effects on the promotion of health and with suppression of telomerase activity and oxidative DNA
Most G4 ligands, such as triterpenoids, structurally highly oxidized lanostanes, have been BRACO19, PIPER, quercetin, RHPS4, telomestatin and TmTyP4, isolated and characterized with ganoderic acids (GAs) such as are planar molecules, which comprise a planar p-rich rings ganoderic acid A (GA A), GA D, GA Df, GA T [3,4]
Summary
Triterpenoids isolated from Ganoderma lucidum (GLTs) exhibit a broad spectrum of anti-cancer properties, including anti-proliferative, anti-metastatic and anti-angiogenic activities. Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or downregulate the oncogenes and may act as anti-cancer agents. 208 GLTs were screened for ligands with high binding affinity and selectively to stabilize the pG4DNA by using the docking tool AutoDock. The compounds those selectively binds to and than 400 bioactive compounds have been isolated and identified stabilize G4 complex structures could inhibit the telomerase and from GL [2]. The aims of the present work were to search for novel GLT ligands with high binding affinity and selectivity for the pG4DNA, which may lead to the discovery of novel natural molecules as lead, compounds having potential anti-cancer activity
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