In the late 1980s, the U.S. Food and Drug Administration (FDA) officially approved ursodeoxycholic acid as a treatment for liver disease. The drug's patent expired and it is now available as a generic.
On December 5, 2022, a research team from the University of Cambridge published a paper entitled "FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2" in the top international journal Nature. The study found that ursodeoxycholic acid, a liver disease drug that turns off ACE2 receptors and closes the door for viruses to enter cells, could be used to prevent COVID-19 infection, and since the drug targets host cells rather than the virus, it may prevent future new variants of the virus as well as other coronaviruses that may emerge.
Based on this evidence, the team is optimistic that ursodeoxycholic acid has the potential to be an important weapon in the fight against COVID-19.
Ursodeoxycholic acid supplied on the market at present is mostly synthetic, synthetic methods include chemical synthesis and bioenzyme method. Chemical synthesis of ursodeoxycholic acid is relatively complicated, requiring multiple steps of hydroxyl protection and deprotection, resulting in low total yield and high cost. Ursodeoxycholic acid (CDCA) as raw material is prepared by two-step enzymatic method, which has the advantages of short path and low cost, so it is more and more used in industrial production. Enzymatic synthesis of UDCA route:
