As a species of pharmaceutical substances, triterpenes contribute to the health benefits of Ganoderma lucidum. Its commercial products include ganoderma lucidum spore oil softgel (reishi spore oil softgel), reishi spore powder. It has been proven that many of these triterpenoids, especially the ganoderic acids (GAs), are bioactive components responsible for several beneficial effects, including anti-inflammatory, anti-tumorigenic, anti-HIV and hypolipidemic effects. So far, more than 150 triterpenes have been identified from the fruiting bodies, spores and mycelia of Ganoderma lucidum.

Antitumor Activity
Ganoderic acids are the typical triterpenes of Ganoderma lucidum, which play a key role in their bio-activity. The activity of ganoderic acids could be mainly related to the hydroxylation of their lanostane triterpene structure. The active ganoderic acid A (GA-A) is hydroxylated at positions 7 and 15, while ganoderic acid H (GA-H) is hydroxylated at C-3, and the non-active ganoderic acid F (GA-F) is not hydroxylated. Additional triterpenes with hydroxyl or acetoxy groups at locations 3, 7 and/or 15, such as ganoderic acid C1 (GA-C1), ganoderic acid C2 (GA-C2), ganoderic acid D (GA-D), ganoderic acid T (GA-T), ganoderic acid X (GA-X), ganoderic acid Y (GA-Y), ganoderiol A, ganoderol B, lucidumol B and ganodermadiol

Ganoderic acid T inhibited the proliferation of some cancer cells. It had higher cytotoxicity towards the 95-D lung cancer cell line than to normal cell lines. And the effects of GA-T on human hepatoma SMMC-7721 cell lines and hepatic leukaemia factor (HLF) are similar. This indicates that GA-T has different cytotoxic potency against different tumor cells. The cytoactive of 95-D cells was suppressed by 70% at 50 μg/mL at 24 h by GA-T. Ganoderic acid T could also effectively inhibit the formation of cell colonies of 95-D at low concentrations.

In our study of the influence of ganoderic acid Me on tumor invasion, the results showed the anti-metastasis effects of ganoderic acid Me (GA-Me), which was proven by inhibition of cell adhesion and motility, as well as suppression of MMP2 and MMP9 gene expression. Therefore, GA-Me could be a promising new anti-metastatic agent. Ganoderic acid DM is a lanostane-type triterpene extracted from Ganoderma lucidum which shows cytotoxicity to cancer cell lines.

After investigating the impact of lucidenic acids (A, B, C and N) on cell growth inhibition and apoptosis in human leukaemia cells HL-60, It was discovered that lucidenic acid B reduced the cell activity of some tumor cell lines and encouraged apoptosis in HL-60 cells.
The in vivo antitumor effects of the ganoderma alcohol and ganoderiol F were also investigated, which exhibited the strongest activity in a cytotoxicity assay. At three doses of 5, 10, and 20 mg/kg/day. Ganoderiol F obviously inhibited the tumor growth of Lewis lung carcinoma cell (LLC)-bearing mice. And no obvious toxic or side effects were perceived.

Also, ganodermanontriol blocked proliferation and development of invasive, metastatic, and therapy-resistant human breast cancer cells. Ganodermanontriol blocked countenance of the cell cycle regulatory protein CDC20.

Anti-Oxidation Activity
Free radicals and reactive oxygen species, which are produced as side-products of several metabolic processes, can seriously harm cells through oxidation processes. Ganoderma lucidum extract increases the activity of super oxide dismutase and catalase and enzymes, which can eliminate damaging reactive oxygen species.

Ganoderic acids A, B, C and D, lucidenic acid B and ganodermanontriol showed important antioxidant activity against several antioxidant systems in vitro. Consumption of Ganoderma lucidum extract can increase the activity of some enzymes like superoxide dismutase, catalase, glutathione peroxidase in the sera, liver and brain.

Anti-HIV Activity
HIV is a highly contagious virus affecting millions of people all over the world. It causes acquired immunodeficiency syndrome. It has been exhibited that various compounds from Ganoderma lucidum exhibit inhibitory effects on HIV progression. Ganderma lucidum triterpenoids (ganoderic acid beta, lucidumol B, ganodermanondiol, ganodermanontriol and ganolucidic acid A) have significant anti-human immunodeficiency virus (anti-HIV)-1 protease activity. In one of the earliest studies, it was found thirteen compounds from Ganoderma lucidum that had strong inhibitory activity against HIV-1 proteases. Laccases, present in Ganoderma lucidum have been proven to inhibit HIV-1 reverse transcriptase.

Neuro-Protective Effect
Oxidative stress is one reason for the progression of many neurodegenerative illnesses, like Parkinson’s disease, Huntington’s disease, amyotrophic lateral sclerosis and Alzheimer’s disease (AD). One of the approaches for treating AD is to control the function of the neurotransmitter acetylcholine in the brain through the inhibition of acetylcholinesterase (AChE). Triterpenoid compounds in Ganoderma lucidum promote neuronal survival and reduced fatigue. The potential use of Ganoderma lucidum for neurological disease treatment has been studied, the result showed that continuous intake of Ganoderma lucidum could cut the progression of Alzheimer’s disease.