The magical effects of Ganoderma lucidum triterpenoids

Mar 15 2024

Ganoderma lucidum triterpenes are a class of natural products with unique structures and diverse biological activities, mainly extracted from Ganoderma lucidum. Ganoderma lucidum is a medicinal fungus widely used in traditional Chinese medicine and is also known as “jelly grass” for its potential health benefits.

In recent years, with the development of modern analytical technology and the advancement of biotechnology, Ganoderma lucidum triterpenoids have attracted widespread attention from scientific researchers.

These compounds have been found to have a variety of biological activities, including anti-tumor, anti-hypertensive, immunomodulatory, anti-hepatitis B, antioxidant, anti-inflammatory, and antibacterial, making them important candidate molecules for the development of new drugs.

This article will take a closer look at its chemical structure and classification, review its inherent chemical properties, and systematically explore its biological activities.

Physical and chemical properties of Ganoderma lucidum triterpenes

Physical and chemical properties of Ganoderma lucidum triterpenes

The physical and chemical properties of Ganoderma lucidum triterpenes, including solubility and stability, have an important impact on its biological activity and medicinal value. Due to the structural diversity of Ganoderma triterpenoids, their physical and chemical properties also show corresponding diversity.

In terms of stability, the chemical structure of Ganoderma lucidum triterpenes determines its stability under different environmental conditions. Some Ganoderma triterpenes may undergo structural changes under light, heat or acid-base conditions, thus affecting their biological activity.

In addition, the interaction characteristics between Ganoderma lucidum triterpene molecules are also an important aspect of research. These interactions may affect their absorption, distribution, metabolism, and excretion (ADME) properties in the organism, thereby affecting their bioavailability and efficacy.

Main types of Ganoderma triterpenoids and their structural differences

Currently, more than 300 triterpenoids have been isolated from Ganoderma lucidum. The main extraction methods are: organic solvent extraction, ultrasonic extraction, enzyme extraction, microwave extraction, supercritical CO2 extraction, etc.

Ganoderma triterpenes can be divided into two categories through acid-base extraction: acidic triterpenes (ganoderma acid) and neutral triterpenes (ganoderma alcohol, ganoderma aldehyde, ganoderma ketone, etc.). Studies have found that the neutral triterpenes in Ganoderma lucidum can not only inhibit the growth of tumor cells in the proliferating phase, but also induce the apoptosis of dormant tumor cells.

Ganoderma triterpenoids can be divided into several main types, mainly distinguished based on their skeletal structure and functional groups. The most common types of Ganoderma triterpenoids include Ganoderma terpenoids, naphthenic types, and steroidal types.

These structural differences not only determine the chemical properties of individual Ganoderma triterpenes, such as solubility and stability but also have an important impact on their biological activities. For example, different types of Ganoderma triterpenes may exhibit different potencies and mechanisms in terms of anti-inflammatory, anticancer, or immunomodulatory activities.

Pharmacological effects on the immune system

Study on the biological activities of Ganoderma lucidum triterpenoids

The chemical structure of Ganoderma lucidum triterpenoids determines its diverse biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-viral, anti-aging, immunomodulatory function, metabolism regulation, and radiation protection. More and more studies have found that Ganoderma triterpenes exert pharmacological effects on the human immune, nervous, cardiovascular, digestive, urinary and other systems.

Pharmacological effects on the immune system

Ganoderma triterpenoids have significant immunomodulatory functions and can effectively regulate and enhance the body’s immune system. They improve the body’s defense against pathogens by affecting the activity of immune cells, such as enhancing the phagocytic ability of macrophages, activating T cells and B cells, and promoting the production of cytokines.

In addition, Ganoderma triterpenes can also regulate immune responses and reduce inflammatory damage caused by immune system overreaction, and have potential value in treating autoimmune diseases and alleviating chronic inflammatory states.

Pharmacological effects on the nervous system

Studies have shown that Ganoderma triterpenes can improve Alzheimer’s disease and are related to age-related methylation changes. Ganoderic acid Mk, ganoderic acid C6, lucidone A and other components screened out by molecular docking analysis are the main extracts involved in delaying the progression of AD.

The results show that ganoderic acid A reduces neuroinflammation in AD mice by regulating the imbalance of the Th17/Treg axis. The potential mechanism may be related to regulating Treg cells, inhibiting the Janus kinase (JAK)/activator (STAT) signaling pathway induced by Th17 cells, and enhancing mitochondrial oxidative phosphorylation, thereby improving mitochondrial dysfunction in AD mice.

Pharmacological effects on the cardiovascular system

Research has meticulously elucidated the impacts of Ganoderma triterpenoids, including but not limited to: Ganoderic Acid A, Ganoderic Acid B, Ganoderic Acid C6, Ganoderic Acid G, and Ganoderma Glycol on serious health conditions such as atherosclerosis and aortic calcification. Furthermore, these investigations have provided crucial insights into their corresponding mechanistic actions.

These Ganoderma triterpenoids enhance ABCA1/G1-mediated cholesterol efflux in LDLR-/- mice, inhibit macrophage inflammation, and attenuate RUNX2-regulated osteogenesis in vascular smooth muscle cells, ultimately reducing atherosclerosis and cardiovascular disease.

Pharmacological effects on the urinary system

Experiments have found that ganoderic acid can significantly reduce the expression of renal mesenchymal cell markers α-smooth muscle actin (α-SMA) and Vimentin, and upregulate the expression of E-cadherin, suggesting that ganoderic acid inhibits TGF-β/Smad and MAPK . ERK, JNK, p38) signaling pathway partially inhibits renal tubular epithelial-to-mesenchymal transition (EMT).

Ganoderic acid also directly reduces the deposition of extracellular matrix (EMC) proteins such as fibronectin by inhibiting the activation of TGF-β/Smad2/3 signaling. These studies suggest that ganoderic acid may be a potential treatment for renal fibrosis.

Pharmacological effects on the digestive system

Ganoderma lucidum triterpenoids have a very good hepatoprotective effect and have good therapeutic effects on liver damage caused by various different inducements. According to biological indicators and liver histopathological studies, the ideal hepatoprotective dose of Ganoderma lucidum triterpene extract is 180 mg/kg.

Studies have found that oral administration of Ganoderic Acid A can play a beneficial role in reducing alcohol-induced liver damage by improving liver lipid metabolism disorders and oxidative stress in alcohol-exposed mice and regulating intestinal flora.

Secondly, Ganoderma triterpenes have a protective effect on acetaminophen-induced acute liver injury. Compared with the model group, Ganoderma triterpenoids can reduce serum ALT, AST and LDH levels, reduce liver MDA levels, and increase liver GSH and SOD contents and HO-1 protein expression.

Pharmacological effects on metabolic diseases

Ganoderma triterpenes help prevent and improve diseases related to metabolic disorders, such as hyperlipidemia. Modulating intestinal flora is considered a new direction in preventing and treating hyperlipidemia.

Studies have found that Ganoderma triterpenes have an effective therapeutic effect on non-alcoholic fatty liver disease. Histopathological examination found that the degree of fatty liver and liver cell necrosis was significantly reduced after intervention with Ganoderma lucidum triterpenoids.

In addition, intervention of ganoderic acid A contributes to structural changes in the intestinal microbial ecosystem, mainly regulating the relative abundance of some health-promoting microbiota. It can be seen that the intervention of ganoderic acid A has a positive effect on improving intestinal flora imbalance and alleviating lipid metabolism disorders.

Anti-tumor pharmacological effects

Research has found that Ganoderma lucidum triterpenoids can play anti-tumor effects in different tissues and organs through different mechanisms. Ganoderma triterpenes have a protective effect on the spleen and thymus, and improve lipid peroxidation caused by increased free radicals. Ganoderma triterpenoids also down-regulated the B-cell lymphoma/leukemia (Bcl)-2 gene, up-regulated Bax, and improved intestinal microbiota richness.

Ganoderic acid A has antioxidant potential in the STAT3 pathway in prostate cancer. Molecular docking revealed the binding effect of ganoderic acid A and the STAT3 signaling pathway. In cell experiments, it was found that ganoderic acid A inhibited the proliferation, vitality and reactive oxygen species of PC-3 cells.

Anti-ageing pharmacological effects

Triterpenoids extracted from Ganoderma lucidum can increase the levels of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX) and glutathione (GSH) in various tissues. levels, including but not limited to those found in the liver, brain, and brain tissue.

This ability allows them to protect these vital tissues from the effects of protein and lipid peroxidation that may be triggered by oxidative stress. Additionally, these triterpenoids stimulate the body’s immune mechanisms. The above properties highlight the potential use of Ganoderma triterpenes as anti-aging therapeutics.

Decline in male fertility can be largely attributed to the natural aging process. Extensive research has shown that triterpenoids in Ganoderma significantly improve testicular structure and function in middle-aged male mice. Beneficial effects are primarily seen in reducing oxidative stress, maintaining mitochondrial balance, and minimizing cell death or apoptosis.

Antiviral pharmacological effects

Two compounds, ganoderic acid B and ganoderol B, exhibit anti-HIV properties by inhibiting essential proteases associated with HIV infection. In addition, Ganoderma alcohol F and Ganoderma mannitol have effective inhibitory effects on the activity of HIV-1 protease. In addition, several other substances include ganoderma alcohol B, ganoderic acid C1, 3-5α-dihydroxy-6β-methoxykerosyl-7,22-diene, and three types of ganoderic acid-α, H, and A- , showing a moderate effect on inhibition. This particular HIV-1 enzyme.

Radiation protection

Test results show that Ganoderma triterpenes can effectively reduce lipid peroxidation and protein oxidation levels in liver and brain tissue, and successfully restore antioxidant enzyme activity and GSH (glutathione) levels in the liver and brain of irradiated mice.

Relieve chemotherapy fatigue

Chemotherapy-related fatigue (CRF) is considered to be one of the serious symptoms of chemotherapy patients, which not only reduces the patient’s quality of life to a great extent, but also weakens the patient’s physical and social abilities. Ganoderic acid can downregulate the expression of IL-6, iNOS and COX2 in hippocampal tissue by inhibiting the TLR4/Myd88-κB pathway, and delay central fatigue induced by 5-FU.

Relieve chemotherapy fatigue

Conclusion

Extensive research demonstrates the potential of Ganoderma triterpenoids to improve immune function, reduce inflammation and support various aspects of cardiovascular health.

Additionally, these triterpenoids have been found to have anti-cancer properties and show potential in treating diabetes and liver disease. To experience the wonders of reishi triterpenoids for yourself, consider incorporating products containing this powerful compound into your daily routine.

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