The "secondary" bile acid, lithocholic acid, is produced in humans in small quantities from the salts of glycochenodeoxycholic and taurochenodeoxycholic acid by bacteria resident in the colon. Once formed, some of the lithocholic acid is absorbed by the intestine and returned to the liver where it is conjugated and/or sulfated and released into the gall bladder as a minor component of bile.
It has been implicated in human and experimental animal carcinogenesis. Conversely, preliminary in vitro research suggests that LCA selectively kills neuroblastoma cells, while sparing normal neuronal cells and is cytotoxic to numerous other malignant cell types at physiologically relevant concentrations.
Recently lithocholic acid derivatives have been identified as potent agonists for the TGR5 receptor and the VDR receptor.
There is now a considerable body of knowledge describing the agonist activity of bile acids on the FXR receptor. LCA, especially as the tauro-conjugate, has been shown to be one of the agonists and while there might be evidence of its toxicity in some animal models, the functional toxicity in humans is in question, as a consequence of efficient human detoxification biology. This indicates that with the ready availability of Dextra-NZP’s lithocholic acid, growth in research about the possibilities of using LCA derivatives in drug development becomes a strong possibility.
Lithocholic acid is used in small quantities in photoresists. More recently, it has attracted attention in drug development.