Cycloastragenol

Shaanxi Yuantai Biological Technology Co., Ltd. is one of the most reliable manufacturers and suppliers of cycloastragenol in China. With abundant experience, we warmly welcome you to wholesale bulk cycloastragenol for sale here from our factory. Quality products and reasonable price are available.

Cycloastragenol (also known as the triterpenoid cycloastragenol) is a cycloartane-type triterpenoid compound with a chemical formula of C₃₀H₅₀O₅, a molecular weight of 490.71, and a density of 1.20 g/cm³. It typically occurs as colorless, needle-shaped crystals. As the core nucleus of astragaloside saponins, it is primarily produced by the hydrolysis of astragaloside IV. Its industrial production can be achieved through two pathways: intestinal microbiota-mediated biotransformation and a β-glucosidase/xylosidase cascade catalytic process.

This compound exhibits significant biological activity and is the only known telomerase activator. It delays telomere shortening by enhancing telomerase activity, demonstrating significant potential in the anti-aging field. In 2022, a Peking University team achieved a breakthrough with the discovery of the key glycosyltransferase AmGT8 and its mutants. Using combinatorial biocatalytic techniques, they successfully synthesized 13 cycloastragenol derivatives with anti-COVID-19 activity. In addition, research has also shown that as a representative substance of triterpenoid saponin compounds, it has multiple application values in the medical field.

Physicochemical Properties

CAG is a cycloartanoid of the tetracyclic triterpenoid class, derived from the cleavage of two glycosidic bonds of AS-IV. Compared to AS-IV, CAG has enhanced lipid solubility, allowing for easier absorption across cell membranes. However, its water solubility is poor, resulting in lower oral bioavailability. Furthermore, CAG contains a cyclopropane group, which is less acidic and can be converted to astragenol (AG, 3) under acidic conditions.

Gut Microbial Transformation Pathway
Extracorporeal rat intestinal microbiota can hydrolyze astragaloside IV to cycloastragenol, which can then be further converted to its oxidized derivative. This transformation involves multiple enzymatic steps, including glycosidic bond cleavage and redox reactions.

Enzyme-Catalyzed Industrial Transformation
A cascade catalytic system consisting of β-glucosidase and β-xylosidase was constructed to efficiently transform astragaloside IV to cycloastragenol-6-O-β-D-glucoside (CMG) to cycloastragenol (CAG). Compared to traditional extraction methods, this method increased yield by 3.8-fold and has potential for industrial application.

Advances in Synthetic Biology (2022 Breakthrough by Peking University Team)

• The first cycloartenane-type glycosyltransferase, AmGT8, was discovered, catalyzing glycosylation of cycloastragenol at both the 3-OH and 2-OH sites. Site-directed mutagenesis generated the F395A mutant, which increased 2-OH glycosylation efficiency by 5.7-fold.
• Combining glycosyltransferases such as AmGT1 and AmGT9 with a mutant of AmGT8 enabled the synthesis of 13 cycloartane-type saponins. Among them, cycloastragenol-3-O-glucoside exhibited 17-fold increased inhibitory activity against SARS-CoV-2 compared to the parent compound.
• The catalytic mechanism of oxysqualene cyclase AmOSC3 was elucidated, revealing that its conserved DCTAE motif plays a crucial role in the formation of the cycloartane backbone.

1. Therapeutic Effects for Brain Injury

After OGD treatment, cell proliferation rates were significantly increased at 24 and 48 hours in the CAG groups at different concentrations.

Cycloastragenol (CAG) significantly promoted neural stem cell proliferation and reduced hypoxia-ischemia-induced cell death, suggesting that telomerase activators may be promising therapeutics for post-hypoxic-ischemic brain injury.

2. Ameliorative Effects for Liver Fibrosis

*After treatment with different doses of CAG, the degree of collagen deposition and fibrosis in mice in all dose groups was reduced compared with the model group, and the collagen volume fraction was significantly decreased.

*Immunohistochemistry revealed that the expression levels of collagen I and α-SMA proteins in the liver tissues of mice in all CAG dose groups were significantly decreased compared with the model group.

Cycloastragenol (CAG) ameliorates CCl4-induced liver fibrosis in mice and reduces the levels of key glycolytic enzymes and products.

3. Therapeutic Effects on Osteoporosis

*CAG significantly increased ALP staining in MC3T3-E1 cells at concentrations ranging from 0.01 to 50 μM, consistent with the ALP activity results (Figure 3A,C). CAG also enhanced mineralization in MC3T3-E1 cells. Calcium deposition in MC3T3-E1 cells was significantly increased at concentrations ranging from 0.01 to 50 μM (Figure 3B,D).

*CAG dose-dependently increased the mineralized area and IOD in DEX-induced zebrafish larvae at concentrations ranging from 25 to 100 μM, indicating that CAG can mitigate DEX-induced bone damage.

Cycloastragenol (CAG) alleviated salmethasone-induced inhibition of osteogenic differentiation both in vitro and in vivo. CAG may be a potential therapeutic agent for glucocorticoid-induced osteoporosis (GIOP).

4. Anti-aging effect

*Compared with the normal group, the MDA of the model group increased significantly, while T-SOD, T-AOC and HYP decreased significantly, indicating that the model was successfully established; compared with the model group, the cycloastragenol group could significantly reduce MDA and significantly improve T-SOD, HYP and T-AOC, and the results were similar to those of VE [5].

Cycloastragenol (CAG) can improve the antioxidant capacity of the whole body by increasing T-AOC, T-SOD and reducing MDA in mouse tissues, significantly improving or adjusting the metabolism of aging cells and improving cell vitality.

5. Anti-aging effect of cells

This study evaluated the therapeutic effect of cycloastragenol (CAG) on early age-related macular degeneration. Oral administration of cycloastragenol (CAG) significantly improved macular function in 38 patients. Microscopic observations revealed that CAG activated telomerase, adding telomeric DNA to the ends of retinal pigment epithelial chromosomes, thereby delaying cellular senescence and potentially treating macular degeneration.

6. Antiviral Effects

* TAT2 demonstrated a telomerase-enhancing effect, which was observed across a wide concentration range (Figure 1b). TAT2's telomerase-enhancing effect on pha-activated PBMCs from healthy adults was relatively modest, ranging from 1.5- to 2.5-fold (Figure 1c). In contrast, TAT2-induced increases in telomerase activity were more pronounced, ranging from 2.5- to 7-fold, in asymptomatic individuals chronically infected with HIV-1 or in individuals with AIDS (Figure 1c).

* Treatment of CD8 T lymphocytes with TAT2 significantly increased their ability to suppress HIV-1 replication in autologous CD4 T cells. TAT2 significantly enhanced CD8 T lymphocyte inhibition of HIV-1 replication (Figure 5, a and b). Notably, the TAT2-mediated enhancement of antiviral activity was almost completely abolished in the presence of a specific TI (Figure 5c).

The study found that telomerase activity in T lymphocytes of 21 subjects significantly increased after receiving cycloastragenol (CAG), thereby enhancing the cells' antiviral capacity and improving the subjects' immunity. The underlying signaling pathway was the MAPK pathway. The upregulation of telomerase activity by CAG was short-term and reversible, with no adverse effects on cell viability.

1. Pharmaceutical.

2. Functional food and food additive

3. Livestock products and poultry products.

4. Water-soluble beverages

5. In heart cerebrovascular aspect,it can inhibit platelet aggregation, reduce blood viscosity and coagulation, relax smooth muscle, expand of cerebrovascular, reduce vascular resistance, improve blood circulation, especially improve the microcirculation, can also inhibit the formation of arterial thrombosis.

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