Phanginin A 是一种有效的具有口服活性的SIK1激活剂。Phanginin A 抑制糖异生。Phanginin A 增加 p-SIK1 的表达并降低 p-CREB 的表达。Phanginin A 可降低血糖水平并改善葡萄糖耐量和血脂异常。Phanginin A 具有用于 2 型糖尿病研究的潜力。
| 生物活性 | Phanginin A is a potent and orally activeSIK1(salt-induced kinase 1)activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Phanginin A (2.5, 5, 10 μM) 以剂量依赖性方式抑制原代小鼠肝细胞中的糖异生[1]。
Phanginin A (5, 10 μM) 降低 G6P 和 PEPCK 的 mRNA 表达，并减少细胞内 cAMP 的积累[1]。
Phanginin A (5, 10 μM; 0-120 min) 以时间和剂量依赖的方式抑制原代小鼠肝细胞中 CREB 磷酸化的表达[1]。
Phanginin A (2.5, 5, 10 μM; 0-120 min) 以时间和剂量依赖的方式增加原代小鼠肝细胞中 p-SIK1 的表达[1]。
Phanginin A (5, 10 μM) 增加 PDE4 活性[1]。
RT-PCR[1] | Cell Line: | Primary mouse hepatocytes | | Concentration: | 5, 10 μM | | Incubation Time: | | | Result: | Significantly decreased PEPCK mRNA expression by 25% and 43% under basal conditions and 45% and 67% under forskolin-stimulated conditions, The G6P mRNA expression was also significantly reduced, with 5 and 10 μM of phanginin A resulting in a decrease of 30% and 46% under basal conditions and 38% and 57% under forskolin-stimulated conditions, respectively. |
Western Blot Analysis[1] | Cell Line: | Primary mouse hepatocytes | | Concentration: | 0-120 min | | Incubation Time: | | | Result: | Inhibited CREB phosphorylation in a time and dose-dependent manner. |
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体内研究
(In Vivo) | Phanginin A (100 mg/kg; p.o.; once) 在 2 型糖尿病 ob/ob 小鼠中表现出抗糖异生活性[1]。
Phanginin A (100 mg/kg; p.o.; once daily for 26 days) 改善 ob/ob 小鼠的代谢紊乱[1]。
| Animal Model: | Type 2 diabetic ob/ob mice[1] | | Dosage: | 100 mg/kg | | Administration: | P.o.; once | | Result: | Significantly reduced the blood glucose, increased the phosphorylation of SIK1 in the liver by 119%, PDE4 activity in the liver was elevated by 74%, decreased in the cAMP concentration along with a 46% decrease in the CREB phosphorylation level in the liver, decreased the mRNA levels of PEPCK and G6P. |
| Animal Model: | Male ob/ob mice[1] | | Dosage: | 100 mg/kg | | Administration: | P.o.; once daily for 26 days | | Result: | Showed an average reduction rate of 29% and 32% in random and fast blood glucose, exhibited a marked improvement in glucose tolerance, significantly reduced by 20% in HbA1c level, showed no effect on food intake and body weight. |
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| 来源 | - Plants
- Leguminosae
- Caesalpinia sappanL.
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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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