Product name: Ganoderic Acid A
Synonym name:
Catalogue No.: BP0615
Cas No.: 81907-62-2
Formula: C30H44O7
Mol Weight: 516.675
Botanical Source: Ganoderma lucidum (reishi)
Physical Description: Powder
Type of Compound: Triterpenoids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams, up to kilograms
Inquire for bulk scale.
Descriptions:
Ganoderic acid A is a lanostane triterpene isolated from Ganoderma lucidum. It exhibits antitumor activity, which is mainly mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1, it promotes cisplatin-induced cell death by enhancing the sensitivity of HepG2 cells to cisplatin mainly via the signal transducer and activator of transcription 3 suppression. [1]
Ganoderic acid A induces a remarkable cytotoxicity in various leukemia and lymphoma cell lines and primary tumors, with a minor toxicity to nonmalignant B-cells, can upregulate pro-apoptotic protein Bax proteins while downregulating anti-apototic proteins Bcl-2 and survivin, it may play dual roles in inducing apoptosis and enhancing HLA class II Ag presentation, and could be used as novel adjunctive therapy for the treatment of hematological malignancies.[2]
Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human osteosarcoma HOS and MG-63 cells, down-regulate the expression level of phosphorylated STAT3 and increase the phosphorylation level of p38 and NF-κB1 expression in both cells. [3]
References:
[1] Yao X, Li G, Xu H, et al. Planta Medica, 2012, 78(16):1740-8.
[2] Haque A, Radwan F F Y, Hossain A, et al. Cancer Res, 2012, 72(8 Supplement):5641.
[3] Shao J, Li Z, Jiao G, et al. Journal of Southern Medical University, 2015, 35(5):619-24.
[4] Duan-Ping L U, Chen S, Wang Y, et al. Modern Chinese Medicine, 2013, 15(06):496-9.
HPLC of Ganoderic Acid A
HNMR of Ganoderic Acid A
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Ganoderma lucidum, as a highly representative medicinal fungus in traditional Chinese medicine, has attracted much attention for its extensive pharmacological activity and remarkable clinical efficacy. Ganoderic Acid A (CAS No.: 81907-62-2) is one of the important triterpenoid active components in Ganoderic lucidum. In recent years, it has become a hot topic in pharmacological research of natural products due to its potential for various biological functions such as immune regulation and anti-tumor effects. Ganodermic acid A not only inhibits the JAK-STAT3 signaling pathway, regulating cell proliferation and survival, but also significantly reduces intracellular reactive oxygen species (ROS) levels, demonstrating excellent anti-inflammatory and antioxidant properties. This paper will systematically review the chemical structure and physicochemical properties of Ganoderma Acid A, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, pharmacokinetic characteristics, and clinical application prospects, aiming to provide theoretical basis and research directions for subsequent drug development and clinical translation.
Ganodermic acid A belongs to the triterpene class of compounds, with the molecular formula C_30H_44O_7 and a molecular weight of 516.6750. Its structural feature is a typical pentacyclic triterpene skeleton, containing multiple hydroxyl and carboxyl functional groups, which give it certain water solubility and biological activity. The LogP value of Ganodermic acid A is 3.0501, indicating moderate lipid solubility, which facilitates cell membrane penetration without being overly hydrophobic, balancing its bioavailability and distribution in vivo. The polar surface area (TPSA) was 128.97 Ų, indicating high polarity that may limit its ability to cross the blood-brain barrier, meeting the criteria for low blood-brain barrier penetration. Its low water solubility (0.0328 mg/mL) limits its oral absorption efficiency to some extent. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity; The Ames mutagenic test result was 0.0, indicating an extremely low genotoxicity risk and a solid safety foundation.
Ganoderma Acid A is mainly found in the fruiting body and mycelium of Ganoderma. As a fungi of the Polypore family, Ganoderma is widely distributed across many regions of Asia, especially occupying an important position in traditional medicinal resources in China, Japan, and South Korea. The content of Ganoderma acid A is greatly influenced by factors such as variety, harvest time, cultivation conditions, and treatment techniques.
Traditional methods for extracting Ganoderma acid A mostly use organic solvent extraction methods, such as ethanol, methanol, or ethyl acetate, combined with ultrasound-assisted extraction or reflux extraction technologies, which can effectively improve extraction efficiency. Common extraction processes include: crushing the dried Ganoderma lucidum, performing multiple extraction cycles with 70% ethanol, concentrating the filtrate, and separating and purifying it by silica gel column chromatography or high-performance liquid chromatography (HPLC), ultimately obtaining high-purity Ganoderma acid A. In recent years, supercritical CO_2 extraction and microwave-assisted extraction technologies have also been applied to the extraction of Ganoderma acid A, offering advantages such as fast extraction speed, minimal solvent residue, and environmental friendliness, gradually becoming a trend in research and industrial production.
Pharmacological activity studies of Ganodermic acid A cover multiple aspects including immunomodulatory, anti-tumor, anti-inflammatory, and antioxidant properties, reflecting its multi-target and multi-mechanism effects.
Immunomodulatory effects
Ganodermic acid A demonstrates significant immune regulation by regulating various immune-related signaling pathways and cytokines. It can regulate the expression and activity of key immune targets such as TLR4, STAT3, IL2, NFKB1, TGFB1, CTLA4, STAT4, IL10, FOXP3, and IFNG, promoting the recovery of immune cell function and the maintenance of immune balance. For example, Ganodermic acid A inhibits the STAT3 signaling pathway, reduces the secretion of immunosuppressive cytokines, and enhances the activity of effector T cells, thereby improving the body's immune response to pathogens and tumor cells.
Antitumor activity
Ganodermic acid A demonstrates good anti-tumor potential by inhibiting tumor cell proliferation and promoting apoptosis. It can block the JAK-STAT3 pathway, reduce tumor cell survival and proliferation capacity, while lowering ROS levels, alleviating cellular damage caused by oxidative stress, and inhibiting tumor invasion and metastasis. Multiple in vitro cell experiments and animal model studies have confirmed that Ganodermic Acid A has inhibitory effects on various tumor types, especially in solid tumors such as lung, liver, and breast cancer.
Anti-inflammatory and antioxidant effects
Ganodermic acid A can significantly inhibit the release of inflammatory mediators and reduce inflammatory responses. By inhibiting the NF-κB signaling pathway, it reduces the expression of pro-inflammatory cytokines such as TNF-α and IL-6, thereby alleviating tissue inflammatory damage. At the same time, Ganodermic acid A reduces intracellular ROS production, enhances antioxidant enzyme activity, protects cells from oxidative stress damage, and exerts its protective function.
The mechanism of action of Ganoderma A mainly revolves around its regulation of the JAK-STAT3 signaling pathway and its impact on immune-related targets. The JAK-STAT3 pathway plays a central role in cell proliferation, differentiation, and immune regulation, with abnormal activation closely linked to various diseases, especially cancer and immune disorders. Ganodermic acid A directly or indirectly inhibits JAK kinase activity, blocks STAT3 phosphorylation and nuclear translocation, suppresses its transcriptional activity, and thereby regulates downstream gene expression, suppresses tumor cell proliferation, and forms an immunosuppressive environment.
Additionally, Ganodermic acid A regulates the TLR4 signaling pathway, influences innate immune responses, modulates NFKB1 activity, and reduces the release of inflammatory factors. Regulation of cytokines IL2, IL10, and TGFB1 promotes functional recovery of immune cells and balance of immune tolerance. Regulation of CTLA4 and FOXP3 affects the activity of regulatory T cells (Treg), modulates immunosuppression, and enhances anti-tumor immune responses. Enhanced IFNG expression promotes cellular immune activity, synergistically exerting immune regulation and anti-tumor effects.
Druggability evaluation of Ganodermic acid A indicates that it has certain development potential. Although the molecular weight of 516.6750 is slightly above the 500 Da threshold recommended by Lipinski's rules, its moderate LogP (3.05) and high TPSA (128.97 Ų) indicate good membrane permeability and bioactivity. Low water solubility (0.0328 mg/mL) is a limiting factor for oral bioavailability and needs to be improved through pharmaceutical techniques such as nanocarriers, liposomes, or solid dispersions.
The low penetration of the blood-brain barrier suggests its limited application in treating central nervous system diseases, but it also reduces the potential risk of CNS toxicity. Negative hERG channel inhibitory results and negative Ames test results indicate low cardiotoxicity and genotoxicity risks and good safety.
In terms of pharmacokinetics, current research is relatively limited. Preliminary in vivo metabolic experiments indicate that Ganodermic acid A is metabolized in the liver via the CYP450 enzyme system, with main metabolic pathways including hydroxylation and glucuronic acid binding. Its half-life is moderate, and plasma protein binding is relatively high, suggesting it is widely distributed in the body but cleared slowly. Further systematic pharmacokinetic and toxicological studies are needed in the future to improve the foundation for clinical development.
Ganodermic acid A, with its multi-target, multi-mechanism immunomodulatory and antitumor activity, shows broad clinical application prospects. Currently, its potential is particularly prominent in immune-related diseases such as autoimmune diseases, chronic inflammation, and adjuvant therapy for tumors. By regulating key immune factors and signaling pathways, Ganodermic Acid A is expected to become a novel immunomodulator, improving immune imbalance and enhancing immune function.
In tumor treatment, Ganodermic acid A not only directly inhibits tumor cell proliferation but also improves the tumor microenvironment, enhances the anti-tumor activity of immune cells, and helps improve the efficacy of traditional radiotherapy and chemotherapy and reduce side effects. In the future, by combining modern drug delivery systems with precision medicine strategies, Ganodermic Acid A is expected to achieve more efficient clinical translation.
However, the clinical application of Ganodermic Acid A still faces many challenges, including limited bioavailability due to low water solubility, lack of systematic clinical pharmacokinetics and safety data, and insufficient in-depth analysis of its mechanism of action. In the future, multidisciplinary collaboration should be strengthened, standardized preclinical and clinical research conducted, formulation processes optimized, and combined drug strategies explored to promote the conversion of Ganoderma A into clinical drugs.
As an important triterpene active component in Ganoderma lucidum, Ganodermic acid A, with its unique chemical structure and multi-target pharmacological properties, demonstrates significant potential in immunomodulatory and antitumor fields. Its ability to inhibit the JAK-STAT3 signaling pathway, regulate multiple immune-related targets, and reduce cell proliferation and ROS levels provides a valuable example for pharmacological research of natural products. Although its druggability and clinical application still need further improvement, with advances in extraction and purification techniques, pharmaceutical improvements, and mechanistic research, Ganodermic acid A is expected to become an important candidate for new immunomodulatory and antitumor drugs in the future. We look forward to more high-quality basic and clinical research in the future, promoting the scientific development and clinical application of Ganodermic Acid A, contributing the power of natural medicines to human health.
