Geniposide is an iridoid glucoside extracted from Gardenia jasminoides Ellis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.

Geniposide exhibits a variety of activities, such as on antithrombosis, anti-inflammation, anti-diabetes, anti-atherosclerosis, antidepression, healing Alzheimer’s disease (AD), anti-hypertension, toxicology, and untoward reaction are summarized^[1]. Geniposide markedly declines the production of IL-8, IL-1β and MCP-1 in OGD-induced brain microvascular endothelial cells, the expression of P2Y14 receptor is significantly down-regulated, the phosphorylation of RAF-1, MEK1/2, ERK1/2 are suppressed^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Geniposide (200 and 400 mg/kg) significantly decreases the blood glucose, insulin and TG levels in diabetic mice in a dose-dependent manner. This compound also decreases the expression of GP and G6Pase at mRNA and immunoreactive protein levels, as well as enzyme activity^[3]. Geniposide (20.0, 40.0, or 80 mg/kg) significantly reverses the excessive, alcohol-induced elevation in both serum ALT/AST and hepatic LPO levels. Geniposide upregulates the expression of heme oxygenase-1 (HO-1) to attenuate the cell apoptosis induced by 3-morpholinosydnonimine hydrochloride (SIN-1) in primary cultured hippocampal neurons^[4]. Geniposide inhibits photochemistry-induced thromboembolism model in vivo. Geniposide are very effective depressants on NF-κB by interrupting IκB degradation^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

388.37

C₁₇H₂₄O₁₀

24512-63-8

京尼平苷；京尼平甙；栀子甙；去羟基栀子甙；栀子苷

Room temperature in continental US; may vary elsewhere.

Powder	-20deg;C	3 years
	4deg;C	2 years
In solvent	-80deg;C	6 months
	-20deg;C	1 month

In Vitro:;

DMSO : 100 mg/mL (257.49 mM; Need ultrasonic)

H₂O : 50 mg/mL (128.74 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

  Solubility: ≥ 2.75 mg/mL (7.08 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (7.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.75 mg/mL (7.08 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (7.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.75 mg/mL (7.08 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (7.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Liu H, et al. Fructus Gardenia (Gardenia jasminoides J. Ellis) phytochemistry, pharmacology ofcardiovascular, and safety with the perspective of new drugs development. J Asian Nat Prod Res. 2013;15(1):94-110.

  [2]. Li F, et al. Geniposide attenuates inflammatory response by suppressing P2Y14 receptor and downstream ERK1/2 signaling pathway in oxygen and glucose deprivation-induced brain microvascular endothelial cells. J Ethnopharmacol. 2016 Jun 5;185:77-86.

  [3]. Wu SY, et al. Effect of geniposide, a hypoglycemic glucoside, on hepatic regulating enzymes in diabetic mice induced by a high-fat diet and streptozotocin. Acta Pharmacol Sin. 2009 Feb;30(2):202-8.

  [4]. Wang J, et al. Geniposide protects against acute alcohol-induced liver injury in mice via up-regulating the expression of the main antioxidant enzymes. Can J Physiol Pharmacol. 2015 Apr;93(4):261-7.

The third passages of brain microvascular endothelial cells (BMECs) are used for the experiment. The BMECs are divided into four groups: (1)normal control group: the normal cultured BMECs without treatment; (2)OGD group: the BMECs injured by OGD according to the above method; (3) geniposide group: the OGD-injured BMECs treated with 33.2 μg/mL geniposide for 6 h; (4)PTX group: the OGD-injured BMECs administrated with 100 ng/mL PTX. PTX, known as an inhibitor of G_i-coupled receptor is used to assess the activation of P2Y₁₄ receptor induced by OGD in this experiment^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Mice: Type 2 diabetic mice, induced by a high-fat diet and streptozotocin injection, are treated with or without geniposide for 2 weeks. Blood glucose levels are monitored by a glucometer. Insulin concentrations are analyzed by the ELISA method. Total cholesterol (TC) and triglyceride (TG) levels are measured using Labassay kits. Activities of hepatic GP and G6Pase are measured by glucose-6-phosphate dehydrogenase-coupled reaction. Real-time RT-PCR and Western blotting are used to determine the mRNA and protein levels of both enzymes^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Liu H, et al. Fructus Gardenia (Gardenia jasminoides J. Ellis) phytochemistry, pharmacology ofcardiovascular, and safety with the perspective of new drugs development. J Asian Nat Prod Res. 2013;15(1):94-110.

  [2]. Li F, et al. Geniposide attenuates inflammatory response by suppressing P2Y14 receptor and downstream ERK1/2 signaling pathway in oxygen and glucose deprivation-induced brain microvascular endothelial cells. J Ethnopharmacol. 2016 Jun 5;185:77-86.

  [3]. Wu SY, et al. Effect of geniposide, a hypoglycemic glucoside, on hepatic regulating enzymes in diabetic mice induced by a high-fat diet and streptozotocin. Acta Pharmacol Sin. 2009 Feb;30(2):202-8.

  [4]. Wang J, et al. Geniposide protects against acute alcohol-induced liver injury in mice via up-regulating the expression of the main antioxidant enzymes. Can J Physiol Pharmacol. 2015 Apr;93(4):261-7.