| I- Ganoderma extracts |
Applications |
Observed Activities |
Suggested Mechanism(s) |
Refs |
Dried powder of G. lucidum
(dissolved in boiled water) |
Highly invasive breast cancer (MDA- MB-231) and prostate cancer (PC-3) cell lines. |
Downregulates transcription factors AP-1 and
NF-κB in breast and prostate cancer cells. |
Inhibition of uPA and uPAR reduces cell motility. |
[65] |
Dried powder of G. lucidum
(13.5% polysaccharides &
6% triterpenes) |
Human prostate cancer cells (PC-3), and human aortic endothelial cells (HAECs) |
Inhibits early
events in angiogenesis & capillary morphogenesis of HAECs, and
modulates the phosphorylation of Erk1/2 & Akt kinases in PC-3 cells,
potentially decreasing the activity of AP-1. |
Inhibition of AP-1 down-regulates the
secretion of VEGF and TGF-β1 from
PC-3 cells. Suppression of angiogenesis by modulating MAPK and Akt signaling. |
[66] |
Ethanol and water extract of
G. lucidum |
Human urothelial cells (HUC, bladder cancer ) consisting of two cell lines (HUC-PC cells and MTC-11 cells). |
Ethanol extracts
show a stronger growth inhibition than those of water extracts.
Induces growth arrest and reduces cell migration in vitro. |
Increased actin polymerization inhibits carcinogen 4-aminobiphenyl-induced cellular migration. |
[67] |
Methanolic G. lucidum
extract |
26 types of human
cancer cell lines including16 hematological cell lines
(lymphomas & multiple myelomas), and 10 other solid tumor cell
lines. |
Exhibits cytotoxicity to HL-60 (ED50 ≥26 μg/ml), U937 (ED50 ≥63μg/ml), K562 (ED50 ≥50μg/ml), Blin-1 (ED50 ≥38μg/ml), Nalm-6 (ED50 ≥30 μg/ml) and
RPMI8226 (ED50 ≥40 μg/ml) |
Induction of cell cycle arrest, mitochondrial dysfunction, and upregulation of p21/p27. |
[68] |
| G. lucidum polysaccharide extract |
In vivo treatment of ovarian cancer in rodents. |
Reduces MDA adducts
by increasing activity of serum antioxidant enzymes [superoxide
dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px)]. |
Reduction of malignant growth by modulation of serum antioxidant enzymes. |
[69] |
| Hot water G. lucidum extract |
Drug-sensitive (H69)
and multi-drug resistant (VPA) human SCLC cells. VPA was derived from
H69 cells selected in etoposide. |
Exhibits cytotoxicity and induces apoptosis in both drug-sensitive and drug-resistant cells. |
Induction of
apoptosis similar to the conventional chemotherapeutics (etoposide and
doxorubicin) via DNA fragmentation and caspase activation. |
[70] |
Semi-purified G. lucidum
(methanol extract) |
Human leukemic cell line NB4. |
Induces apoptosis in NB4 cells. |
Reduction and modulation of Bcl2/Bax,
p53, Akt, Erk; Inhibition of NF-κB. |
[71] |
| Ethanol extract of G. lucidum (GLe) |
Pre-cancerous human uroepithelial cell line (HUC-PC) . |
Induces apoptosis and upregulates IL-2, IL-6, and IL-8 in HUC-PC cells in a dose-dependent manner. |
Enhancement of cytokine expression by p50/p65 NF-κB activity. Migration of neutrophils via upregulation of IL-8. |
[72] |
| II-Ganoderic acid subtypes |
Applications |
Observed Activities |
Suggested Mechanism(s) |
Refs |
| Ganoderic acid X (GA-X) |
Hepatoma cells
(HuH-7), colorectal carcinoma (HCT-116), Burkitt’s lymphoma (Raji
cells), acute promyelocyte leukemia (HL-60). |
Inhibits topoisomerases I and IIa in vitro, resulting
in immediate inhibition of DNA synthesis as well as activation of
ERK and JNK mitogen-activated protein kinases. |
Induction of
apoptosis with degradation of chromosomal DNA; decreased levels of
Bcl-xL, disruption of mitochondrial membrane, release of cytochrome c
and activation of caspase-3. |
[73] |
| Ganoderic acid T (GA-T) |
Human metastatic
lung tumor (95-D), liver tumor (SMMC7721), epidermal cancer
(KB-A-1&KB-3-1), cervical cancer (HeLa), melanoma (A375), normal
lung (HLF), embryonic liver
(L-02), kidney (HEK293), and colon carcinoma (Ls174t) cell lines. |
Induces cytotoxicity
to cancer cells, but less toxic to normal cells. Induces cell cycle
arrest at G1 phase. Suppresses MMP-2 and MMP-9
gene expression through the inhibition of NF-κB
activation. |
Reduction of
mitochondrial membrane potential (Δψm), release of cytochrome c and
apoptotic activity in lung cancer cells. Induction of p53 and Bax, which
stimulates the activity of caspase-3 but not caspase-8. |
[50,
74] |
| Ganoderic acid ME (GA-Me) |
In vivo Lewis lung carcinoma
in C57BL/6 mice, human colon carcinoma cells (HCT-116), MDR
human colorectal carcinoma cell lines, and metastatic lung carcinoma
(95-D), p53-null lung cancer (H1299),HCT-
116 p53+/+ and HCT-116 p53 -/- colon cancer cells. |
Inhibits tumor
growth and lung metastasis in rodents (28 mg/kg i.p.), increases NK
activity with upregulation of NF-κB. Kills cancer cells via p53 and
mitochondria-mediated apoptosis. Reverses multidrug resistance of
HCT-116 cells enhancing chemosensitivity to anticancer agents. |
Induction of cell
cycle arrest. Induction of apoptosis in MDR cells via upregulation of
p-p53, p53, Bax, caspases-3/9 with downregulation of Bcl-2.
Upregulation of IL-2 and IFN-γ in vivo. |
[54,
55,
75,
76] |
