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.
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
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.
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
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,
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,
Table 1: Some recent applications, observed activities and suggested mechanisms of actions for Ganoderma lucidum raw extracts (I), and its purified Ganoderic acids (II) on several types of cancer cells.