| Description: |
Geniposidic acid is an effective anticancer and radioprotection agent, used to treat inflammation, jaundice and hepatic disorders. It has anti-atherosclerotic effects, can protect vascular endothelium and reverse plaque formation in an atherosclerotic model. Geniposidic acid has effects on the expression of MRP2 and BSEP in BRL-3A cells after FXR gene silencing mediated by si RNA. |
| Targets: |
HO-1 | IL Receptor | Caspase | FXR | MRP2 | BSEP |
| In vitro: |
| China Journal of Traditional Chinese Medicine & Pharmacy, 2016,5. | | Effects of geniposidic acid on the expression of MRP2 and BSEP in BRL-3A cells after FXR gene silencing mediated by si RNA[Reference: WebLink] | To investigate the effects of Geniposidic acid(GPA) on the protein expression of multidrug resistance protein 2(MRP2) and bile salt export pump(BSEP) in BRL-3A cells, which was mediated by small interfering RNA(si RNA) farnesoid X receptor(FXR) gene silencing.
METHODS AND RESULTS:
RT-PCR was used to detect the result of FXR gene silencing and the gene levels of FXR, MRP2 and BSEP in BRL-3A cells affected by GPA, and Western blot was used to detect whether FXR gene silencing in BRL-3A cells or not by GPA and the protein expressions of FXR, MRP2 and BSEP in BRL-3A cells induced by Geniposidic acid. Compared with control group, the levels of m RNA and protein expressions of FXR, MRP2 and BSEP in BRL-3A cells were significantly increased in GPA group with the concentration of 4mmol/L and 1mmol/L(P0.01, P0.05). GPA with concentration of 4mmol/L and 1mmol/L could significantly reverse the levels of m RNA and protein expression of FXR, MRP2 and BSEP in BRL-3A cells(P0.01, P0.05), which was mediated by si RNA-FXR.
CONCLUSIONS:
: FXR gene silencing could down-regulate the levels of m RNA and protein expression of MRP2 and BSEP, and the GPA could up-regulate FXR to upregulate the levels of m RNA and protein expression of MRP2 and BSEP. |
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| In vivo: |
| Cancer Lett. 1997 Feb 26;113(1-2):31-7. | | Comparisons of geniposidic acid and geniposide on antitumor and radioprotection after sublethal irradiation.[Pubmed: 9065798] | The antitumor effects of two iridoid compounds, geniposidic acid (GA) and geniposide (GP), were investigated in mice along with their possible effects on radioprotection after sublethal X-irradiation.
METHODS AND RESULTS:
Decreases in the growth of the implanted tumor by ascitic cells were a result of intraperitoneal administration of GA and GP at high concentrated levels.
This result was achieved by exerting the levels of dosage in a dose-dependent manner. Except on the 12th day after treatment by the dosage of 500 mg/kg, reduced radiation effects of mice treated with the drugs in the 30 min preirradiated period by GA and GP on peripheral leukocytes were not observed significantly by the sublethal whole-body X-irradiation. And except on the 7th day after treatment, when these two compounds were administered i.p. to mice 30 min before 4 Gy irradiation, neither GA nor GP enhanced significantly the postirradiation responses of splenic blastogenesis by PHA. In addition, GA might be a more potent tumor growth inhibitor than GP when combined with the X-irradiation, though there was no significant synergetic effect on their combined antitumor activity.
CONCLUSIONS:
The preliminary results of GA and GP on hematological and blastogenic observations in this study suggested that they may very well, partially, play a role in an effective anticancer product with the ability to decrease undesirable radiation damage to the hematologic tissue after high dose irradiation. | | J Ethnopharmacol. 2013 Mar 7;146(1):271-7. | | Geniposidic acid protects against D-galactosamine and lipopolysaccharide-induced hepatic failure in mice.[Pubmed: 23298456] | 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.
This study examined the cytoprotective properties of GA against D-galactosamine (GalN)/lipopolysaccharide (LPS)-induced fulminant hepatic failure.
METHODS AND RESULTS:
Mice were given an intraperitoneal injection of GA (12.5, 25, 50 mg/kg) 1h before receiving GalN (800 mg/kg)/LPS (40 μg/kg). Liver and blood samples were collected 1 and 8 h after GalN/LPS injection.
The survival rate of the GA group was significantly higher than the control. GalN/LPS increased serum aminotransferase activity, serum tumor necrosis factor-α level and hepatic lipid peroxidation and decreased hepatic glutathione content. These changes were attenuated by GA. GA augmented increases in serum interleukin-6 level, heme oxygenase-1 and NF-E2-related factor 2 protein expression. Mice treated with GA decreased cleaved caspase-8 and caspase-3 protein expression and showed significantly fewer apoptotic cells. GA increased Bcl-xL protein expression and decreased Bax protein expression. Moreover, GA treatment enhanced phosphorylation of signal transducer and activator of transcription 3.
CONCLUSIONS:
Our findings suggest that geniposidic acid alleviates GalN/LPS-induced liver injury by enhancing antioxidative defense system and reducing apoptotic signaling pathways. |
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