Antipyrine (Phenazone) serves as both an antipyretic and an analgesic. It is commonly utilized as a probe agent for studying the metabolism of oxidative agents, playing a significant role in assessing hepatic oxidative capacity[1].[2].
体内研究
In dietary studies, lithocholic acid at a concentration of 0.6% in the diet over a period of 7 days leads to increased mRNA levels of TGFB1, TGFBR1, and TGFBR2 in the liver of male C57BL/6 mice, activates SMAD3, and results in biliary injury[4].
Additionally, an intraperitoneal dose of 125 mg/kg administered twice daily for four days results in liver damage in male C57BL/6 mice, marked by elevated levels of AST, ALT, and ALP[2].
体外研究
Lithocholic acid inhibits FXR activation induced by CDCA and GW4064, with IC50 values of 0.7 μM and 1.4 μM, respectively[5].
Lithocholic acid also suppresses GW4064-induced BSEP expression at concentrations of 10-30 μM over 24 hours in HepG2 cells[5].
Furthermore, lithocholic acid inhibits the proliferation of various neuroblastoma cell lines (BE(2)-M17, SK-n-SH, SK-n-MCIXC, and Lan-1) in a dose-dependent manner, up to 500 μM[3].
Lithocholic Acid/石胆酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
CD4+ T cells
100 μM
48 hours
To assess the ability of bacteria to convert LCA to 3-oxoLCA and isoLCA. Results showed that multiple bacterial strains could convert LCA to 3-oxoLCA and isoLCA.
Nature. 2022 Mar;603(7903):907-912.
Barrett’s cell lines (CP-C and CP-D)
15 μM
1 hour
To assess the effect of LCA and ATRA alone or in combination on p21 mRNA expression. Results showed that combined treatment with LCA and ATRA led to a threefold increase in p21 mRNA expression, indicating that LCA can augment the effect of local RA to stimulate RA signalling.
Gut. 2007 Jul;56(7):906-17.
IEC-6 cells
20 μM
5 days
To evaluate the effect of 7-keto-LCA on intestinal epithelial cells, results showed that 7-keto-LCA had anti-apoptotic and proliferative effects.
Cell Host Microbe. 2024 Feb 14;32(2):191-208.e9.
HT29 cells
20 μM
5 days
To evaluate the effect of 7-keto-LCA on intestinal stem cell function, results showed that 7-keto-LCA promoted the proliferation and differentiation of intestinal stem cells.
Cell Host Microbe. 2024 Feb 14;32(2):191-208.e9.
Lithocholic Acid/石胆酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
GF mice
Oral
0.3% w/w
Once daily for 7 days
To assess the effect of isoLCA on TH17 cell differentiation. Results showed that isoLCA significantly reduced TH17 cell differentiation.
Nature. 2022 Mar;603(7903):907-912.
C57BL/6 Il10–/– mice
C. jejuni infection model
Oral gavage
30 mg/kg body weight
Daily for 12 days
To evaluate the effect of lithocholic acid on C. jejuni-induced colitis. Results showed that lithocholic acid did not alleviate colitis.
Gastroenterology. 2018 May;154(6):1751-1763.e2
Mice
C57BL/6NCr mice and Fxr-null mice
Dietary supplementation
0.6% LCA-supplemented diet
7 consecutive days
To investigate the effect of LCA on phospholipid and sphingolipid metabolism, results showed that LCA significantly decreased serum LPC and SM levels, increased hepatic ceramide levels, and altered related gene expression through TGF-β-SMAD3 signaling.
Hepatology. 2011 Apr;53(4):1282-93.
C57BL/6J mice
Aspirin-induced intestinal injury model
Oral gavage
50 mg/kg/d
Once daily for 2 weeks
To evaluate the protective effect of 7-keto-LCA on aspirin-induced intestinal injury, results showed that 7-keto-LCA significantly alleviated intestinal injury and promoted the recovery of intestinal barrier function.
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