Calycosin 7-O-Glucoside for Antioxidant, Anti-Inflammatory & Cardiovascular Health Support

1. Description

Calycosin 7-O-Glucoside is a natural isoflavone glycoside compound extracted and isolated from the dried roots of the leguminous plants Astragalus mongholicus and Astragalus membranaceus. Its chemical name is Calycosin-7-O-β-D-glucoside, and it is one of the most bioactive characteristic components of Astragalus. It appears as a white to pale yellow powder. It is soluble in dimethyl sulfoxide (solubility ≥ 100 mg/mL) and methanol, but has low solubility in cold water. Storage conditions: The powder can be stored for 3 years at -20°C and for 2 years at 4°C; when dissolved in a solvent, it can be stored for 6 months at -80°C. This compound exhibits a variety of biological activities, including neuroprotection, cardioprotection, anti-inflammatory, antioxidant, antitumor, antiviral, melanin formation inhibition, and immunosuppressive effects.

2. Application

(1) Ischemic stroke studies: Used in animal models of middle cerebral artery occlusion and reperfusion. Studies have shown that intraperitoneal of 26.8 mg/kg morin (for 14 days) significantly reduces cerebral infarct volume, alleviates histopathological damage, and decreases blood-brain barrier permeability. In the microvasculature of the ischemic rat cortex, treatment with 2 μM for 6 hours significantly inhibited the expression and activity of matrix metalloproteinases and protected the expression of Cav-1 and tight junction proteins.

(2) Neuroprotection Studies: Used in studies of superoxide anion-induced damage in PC12 cells. Mao-Rui isoflavone glycoside exerts neuroprotective effects by enhancing the activity of endogenous antioxidant enzymes (superoxide dismutase and glutathione peroxidase), with a half-maximal effective concentration (EC₅₀) of approximately 0.05 μg/mL. Its half-maximal inhibitory concentration (IC₅₀) for xanthine oxidase activity is approximately 50 μg/mL.

(3) Oncology Research: Studies on chemotherapeutic sensitization for malignant tumors such as ovarian cancer. In human epithelial ovarian cancer SK-OV-3 cells, the combination of 50 μM morin with 10 μM cisplatin for 48 hours resulted in a cell proliferation inhibition rate of 46.7%, significantly higher than the 23.2% observed in the cisplatin monotherapy group. The mechanism involves enhancing cisplatin-induced apoptosis via the p53 pathway, upregulating the expression of caspase-3, caspase-9, and Bax, while downregulating Bcl-2 expression.

(4) Asthma and Airway Inflammation Studies: Used in research on allergic asthma. In an ovalbumin-induced mouse asthma model, morin reduced airway hyperresponsiveness, suppressed airway inflammation, decreased the number of inflammatory cells in alveolar lavage fluid, inhibited chemokine secretion, promoted Th1 cell differentiation, suppressed IL-17A, promoted IFN-γ and IL-10 secretion, and inhibited NF-κB activation.

(5) Cardiovascular Protection Studies: Research on cardiovascular diseases such as myocardial ischemia. Studies indicate that morin can induce angiogenesis in human umbilical vein endothelial cells and may have potential therapeutic effects on myocardial infarction. It also exhibits vasodilatory effects on the thoracic aorta of rats.

(6) Antioxidant and Anti-inflammatory Studies: Research into the mechanisms of free radical scavenging, inhibition of lipid peroxidation, and alleviation of inflammatory responses.

3. Main Efficacy

(1) Neuroprotective effects: By enhancing the activity of endogenous antioxidant enzymes (superoxide dismutase, glutathione peroxidase), it protects neurons from oxidative stress damage, rather than acting through direct inhibition of xanthine oxidase or scavenging of free radicals.

(2) Anti-ischemic brain injury effects: In a cerebral ischemia-reperfusion model, it protects the expression of tight junction proteins (ZO-1 and occludin) by inhibiting the expression and activity of matrix metalloproteinases, thereby maintaining the integrity of the blood-brain barrier and reducing cerebral infarct volume and tissue damage.

(3) Chemotherapy sensitization and antitumor activity: By activating the p53 signaling pathway, it enhances cisplatin-induced apoptosis in ovarian cancer cells. When used in combination, it upregulates the expression of caspase-3, caspase-9, and Bax, downregulates Bcl-2 expression, and reduces the toxic side effects caused by cisplatin monotherapy.

(4) Anti-asthmatic and anti-inflammatory effects: By inhibiting NF-κB activation, it regulates the Th1/Th2/Th17 immune balance, promotes the secretion of IFN-γ and IL-10, and suppresses IL-17A production, thereby alleviating airway inflammation and hyperreactivity.

(5) Antioxidant effects: It possesses free radical scavenging and lipid peroxidation inhibitory activities, which can mitigate oxidative stress-induced cellular damage.

(6) Cardiovascular protective effects: It induces angiogenesis, increases vascular endothelial growth factor (VEGF) expression, and has potential therapeutic effects on myocardial infarction; it also exhibits vasodilatory effects.

(7) Inhibition of melanin formation: It possesses melanin-inhibiting activity and has potential applications in the field of skin whitening.

(8) Immunomodulatory effects: It exhibits immunosuppressive activity, regulates immune cell function, and has potential therapeutic value in autoimmune diseases.