Genipin 是衍生自黄栀果实的天然交联剂，可抑制细胞中的 UCP2 (解偶联蛋白 2)。它有蛋白质调节、抗肿瘤、抗炎症、免疫抑制、抗血栓形成和对海马神经元保护的多种生物活性，可研究 2 型糖尿病。

Genipin, an active aglycone derived from an iridoid glycoside called geniposide, is found in the fruit of Gardenia jasminoides Ellis.

Genipin stimulats glucose uptake in a time- and dose-dependent manner. The maximal effect is achieved at 2?h with a concentration of 10?μM. In myotubes, genipin promotes glucose transporter 4 (GLUT4) translocation to the cell surface, which increases the phosphorylation of insulin receptor substrate-1 (IRS-1), AKT, and GSK3β. Meanwhile, genipin increases ATP levels, closed KATP channels, and then increases the concentration of calcium in the cytoplasm in C2C12 myotubes. Genipin-stimulated glucose uptake could be blocked by both the PI3-K inhibitor wortmannin and calcium chelator EGTA. Moreover, genipin increases the level of reactive oxygen species and ATP in C2C12 myotubes[1]. Genipin increases mitochondrial membrane potential, which then increases ATP levels and closes KATP channels, thereby stimulating insulin secretion in pancreatic β-cells. Genipin activates glucose-excited POMC neurons[2]. Cytochrome c content increases significantly in the cytosol of genipin-treated FaO cells. Activation of caspase-3 and caspase-7 is ultimately responsible for genipin-induced apoptotic process in hepatoma cells. ROS level notably increases in Hep3B cells treated with 200 μM genipin[3].

Briefly, the peptide substrate N-acetyl-Asp-Glu-Val-Asp-ρ-nitroanilide (Ac-DEVD-ρNA) is added to the cell lysates in assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 0.1% CHAPS, 10 mM dithiothreitol, 1 mM EDTA, 10% glycerol) and incubated at 37°C. The cleavage of the substrate is monitored at 405 nm.

6902-77-8

C11H14O5

226.228

(+)-Genipin;京尼平

H2O:1 mg/mL (4.42 mM)
Ethanol:45 mg/mL (198.91 mM)
DMSO:45 mg/mL (198.91 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years