Genipin (Synonyms: 京尼平; (+)-Genipin)
Genipin ((+)-Genipin) 是衍生自 Gardenia jasminoides Ellis 果實的天然交聯(lián)劑。Genipin 抑制細胞中的 UCP2 (解偶聯(lián)蛋白 2)。Genipin 具有多種生物活性，包括蛋白質(zhì)調(diào)節(jié)，免疫抑制，抗血栓形成和對海馬神經(jīng)元的保護。Genipin 也可用于 2 型糖尿病研究。
生物活性
Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research[1][2].
體外研究(In Vitro)
Genipin increases mitochondrial membrane potential, increased ATP levels, closed KATP channels, and stimulated insulin secretion in pancreatic islet cells. Genipin causes suppression of insulin signal transduction through hyperactivation of c-Jun N-terminal kinase (JNK) and subsequent serine phosphorylation of insulin receptor substrate-1 (IRS-1), thus impairing insulin-stimulated glucose uptake in 3T3-L1 adipocytes[1].
Genipin activates IRS-1, PI3-K, and downstream signaling pathway and increases concentrations of calcium, resulting in glucose transporter 4 (GLUT4) translocation and glucose uptake increase in C2C12 myotubes[1].
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[2].
分子量：226.23
性狀：Solid
Formula：C11H14O5
CAS 號：6902-77-8
中文名稱：京尼平
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
In Vitro:
DMSO : ≥ 100 mg/mL (442.03 mM)
H2O : 4 mg/mL (17.68 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.4203 mL | 22.1014 mL | 44.2028 mL |
| 5 mM | 0.8841 mL | 4.4203 mL | 8.8406 mL |
| 10 mM | 0.4420 mL | 2.2101 mL | 4.4203 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨?。以下溶解方案都請先按?In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： PBS
Solubility: 9.09 mg/mL (40.18 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
- 2.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (11.05 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (11.05 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (11.05 mM); Clear solution
參考文獻
[1]. Ma C, et al. Genipin stimulates glucose transport in C2C12 myotubes via IRS-1 and calcium- dependent mechanism. J Endocrinol. 2012 Dec 20. [Content Brief]
[2]. Kim BC, et al. Genipin-induced apoptosis in hepatoma cells is mediated by reactive oxygen species/c-Jun NH2-terminal kinase-dependent activation of mitochondrial pathway. Biochem Pharmacol. 2005 Nov 1;70(9):1398-407.
[3]. Ye D, et al. Genipin normalizes depression-like behavior induced by prenatal stress through inhibiting DNMT1. Epigenetics. 2018 Mar 9:1-22. [Content Brief]
注：產(chǎn)品僅用于科研
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