Geniposidic acid (GA) is an iridoid glucoside isolated from Gardeniae jasminoides Ellis (Rubiaceae) that has long been used to treat inflammation, jaundice and hepatic disorders. Geniposidic acid alleviates GalN/LPS-induced liver injury by enhancing antioxidative defense system and reducing apoptotic signaling pathways[3]. GPA (Geniposidic Acid) treatment significantly improved the spatial learning and memory abilities and also decreased cerebral amyloid-β deposition in APP/PS1 mice[4]. The relative IC50 of geniposidic acid on SMC inhibition was 87.73 μg/ml. Geniposide acid also showed promotion effect on ECs proliferation, and the related ED50 of geniposidic acid was 86.05 μg/ml. Besides, only 50 and 100 μg/ml geniposidic acid showed obvious inhibition on SMC migration from the upper chamber. The effects of geniposidic acid on protecting vascular endothelium and reversing plaque formation in an atherosclerotic model were demonstrated[5]. Geniposidic acid could improve bile acid hepatointestinal circulation and play a liver protection and cholagogu role in cholestasis rats induced by ANIT. The mechanism may be that Geniposidic acid activated FXR by regulating Sirt1, a key regulator of oxidative stress injury,and then the activated FXR could regulate protein of bile acid hepato-enteric circulation[6].
Geniposidic acid/京尼平苷酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
K6001 yeast
1 µM
Significantly prolonged the replicative lifespan of yeast
Antioxidants (Basel). 2021 Jun 21;10(6):987
Mouse bone marrow mononuclear cells (BMMCs)
100 or 1000 µg/mL
48 hours
GPA suppressed sRANKL and M-CSF-induced osteoclast differentiation of BMMCs (56.7% suppression) and inhibited mRNA expression of OSCAR, NFATc1, c-Fos, cathepsin K, and DC-STAMP.
Biomedicines. 2022 Dec 1;10(12):3096
Human gingival epithelial cells (HGECs)
100 µg/mL
12 hours
GPA suppressed P. gingivalis-induced IL-6 mRNA expression (33.8% suppression) and IL-6 protein production (69.2% suppression), and inhibited TLR2 expression and MAPK phosphorylation.
Biomedicines. 2022 Dec 1;10(12):3096
bone marrow-derived monocytes (BMDM)-differentiated macrophages
25-100 μM
24 hours
GPA pretreatment significantly inhibited the mRNA levels of NLRP3, NFκB1 and IL-1β
Redox Biol. 2022 Sep;55:102404
THP-1 monocyte-derived macrophages
25-100 μM
24 hours
GPA pretreatment significantly inhibited the mRNA levels of NLRP3, NFκB1 and IL-1β
Redox Biol. 2022 Sep;55:102404
mouse chondrocytes
12.5, 25, 50 μM
24 hours
GPA markedly inhibited IL-1β-induced inflammatory mediator and MMPs production and NF-κB activation.
J Cell Mol Med. 2024 Apr;28(8):e18228
BY4741 yeast
1 µM
24 hours
Improved the survival rate of yeast under oxidative stress and reduced the levels of ROS and MDA
Antioxidants (Basel). 2021 Jun 21;10(6):987
mouse chondrocytes
12.5, 25, 50 μM
24 hours
GPA significantly inhibited IL-1β-induced inflammatory mediators and MMPs production, and inhibited IL-1β-induced ferroptosis.
J Cell Mol Med. 2024 Apr;28(8):e18228
Geniposidic acid/京尼平苷酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
OVA-induced asthma model
Intraperitoneal injection
12.5, 25, 50 mg/kg
Once daily for the last three days
GPA protects mice against OVA-induced asthma by suppressing inflammation and regulating gut microbiota.
Front Immunol. 2025 Feb 25;16:1549459
C57BL/6J Jcl mice
P. gingivalis-induced periodontitis model
Oral inoculation
50 mg/50 µL
Twice per week for six weeks
GPA inhibited P. gingivalis-induced alveolar bone resorption (25.6% suppression) and reduced IL-6 and TLR2 levels in serum and gingiva.
Biomedicines. 2022 Dec 1;10(12):3096
C57 mice
Destabilization of the medial meniscus (DMM) model
Intraperitoneal injection
50 mg/kg
GPA could alleviate DMM-induced OA in mice, significantly increase the thickness of cartilage and reduce the number of fibrocartilage.
J Cell Mol Med. 2024 Apr;28(8):e18228
C57BL/6 mice
ANIT-induced cholestatic liver injury
Oral
100, 50, 25 mg/kg
Once daily for seven days
GPA pretreatment effectively improved ANIT-induced cholestatic liver injury as evidenced by decreased liver weight index, serum levels of biochemical parameters, including ALT, AST, TBA, and TBIL
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