Coronarin A 是一种具有口服活性的天然物，可抑制mTORC1和S6K1增加 IRS1 活性。Coronarin A 具有抗炎活性，也可用于糖尿病的研究。
| 生物活性 | Coronarin A is an orally active natural compound that inhibitsmTORC1andS6K1to increase IRS1 activity. Coronarin A shows anti-inflammatory activity and can also be used for type 2 diabetes mellitus research[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Coronarin A (3-30 μM; 4 or 12 h) stimulates glycogen synthesis through activating PI3K/Akt/GSK3β signaling and inhibits gluconeogenesis by activating ERK-dependent Wnt/β-catenin/TCF7L2 pathway in rat primary hepatocytes[1].
Coronarin A (1-30 μM; 4 h) increases tyrosine phosphorylation of IRS1 through inhibiting mTOR/S6K1 signaling[1].
Western Blot Analysis[1] | Cell Line: | Primary rat hepatocytes | | Concentration: | 1, 3, 10 and 30 μM | | Incubation Time: | 4 h | | Result: | Increased the Akt and GSK3β phosphorylation dose-dependently. Dose-dependently stimulated the phosphorylation of both ERK1 and ERK2. Increased the phosphorylation of β-catenin and mitogen-activated protein kinase kinase (MEK). Dose-dependently enhanced the tyrosine phosphorylation of IRS1 at Tyr1222, whereas the serine phosphorylation of IRS1 was dose-dependently inhibited. Reduced the phosphorylation of mTOR, S6K1 and S6. |
Cell Viability Assay[1] | Cell Line: | Primary rat hepatocytes | | Concentration: | 1, 3, 10, 30, 100 and 300 μM | | Incubation Time: | 5.5 h or 12 h | | Result: | Showed no toxicity at 1-30 μM, decreased cell viability after 12 h incubation at 100 μM. |
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体内研究
(In Vivo) | Coronarin A (30 or 100 mg/kg; i.p. or p.o.; once daily for 22 days) ameliorates hyperglycemia in mice[1].
Coronarin A (100 mg/kg; p.o.; once daily for 22 days) inhibits the mTOR/S6K1 pathway to activate PI3K/Akt and ERK/β-catenin signaling in livers ofob/obmice[1].
Pharmacokinetic properties of Coronarin A after single administrationainob/obmice[1].
| Coronarin A | t1/2(h) | tmax(h) | Cmax(ng/mL) | AUC0-t(ng·h/mL) | AUC0-∞(ng·h/mL) | MRT (h) | | i.p. | 14.8 | 1.0 | 1073 | 4571 | 11045 | 21.7 | | p.o. | 3.01 | 1.0 | 388 | 1694 | 1856 | 4.88 |
Data are presented as the mean of three mice. aCoronarin A was intraperitoneally or orally administered at 30 mg/kg to ob/ob mice.
| Animal Model: | Maleob/obmice[1] | | Dosage: | 30 mg/kg (IP) or 100 mg/kg (PO) | | Administration: | Oral or intraperitoneal administration, once daily for 22 days | | Result: | Significantly decreased the non-fasting and fasting blood glucose. Significantly reduced the serum insulin concentration at 15 min after glucose loading, reduced the average daily food intake while the body weight was unaffected. Increased hepatic glycogen content and the expression levels of gluconeogenic genePck1andG6pcwere significantly decreased. |
| Animal Model: | Femaleob/obmice[1] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal or oral administration (Pharmacokinetic Analysis) | | Result: | Intraperitoneal injection exhibited higher plasma exposure than oral gavage at the same dose of 30 mg/kg, with Cmaxvalue of 1073 and 388 ng/mL, respectively. |
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| 来源 | - Plants
- Zingiberaceae
- Hedychium coronariumKoen.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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