UDCA

Description

Ursodeoxycholic Acid UDCA promotes the secretion of endogenous bile acids and reduces reabsorption.

1. Cytoprotective effect: Ursodeoxycholic AcidUDCA conjugate significantly reduced the cytolysis of hepatocytes induced by hydrophobic bile acid and reduced apoptosis induced by toxic bile acid in cultured murine and human hepatocytes.
2. Membrane stabilization: Ursodeoxycholic AcidUDCA can prevent bile acid-induced changes in mitochondrial membrane permeability, which means it can prevent toxic bile acid-induced damage to the mitochondrial membrane, basement membrane, and small bile duct membrane through membrane stabilization.
3. Antioxidant effect: Ursodeoxycholic AcidUDCA can inhibit the activation of blastocytes induced by toxic bile acids, and increase the level of glutathione and thiol-containing protein in hepatocytes to prevent the oxidative damage of hepatocytes.
4. Immunomodulatory effects: Ursodeoxycholic AcidUDCA inhibits indirectly by reducing the stimulatory impact of hydrophobic bile acids and directly inhibits the expression of histocompatibility complex (MHC) class I and class II genes by activating glucocorticoid receptors.
5. Ursodeoxycholic AcidUDCA could reduce SARS-Cov-2 entry into cells, which means it can be anti-Covid-19 to some extent, as reported by NATURE recently.

Introduction to UDCA Powder

Ursodeoxycholic acid (UDCA), also known as bear bile acid, is a naturally occurring secondary bile acid. UDCA has been used to treat liver disease for decades, with its first use in traditional medicine dating back over a hundred years. The earliest characterization of UDCA was from the bile of Chinese black bears, and it is formed by the epimerization of 7β-dehydroxylated chenodeoxycholic acid, a primary bile acid. Due to its hydrophilicity, UDCA is less toxic than cholic acid or chenodeoxycholic acid. In 1987, UDCA was first approved by the FDA for the dissolution of gallstones and for primary biliary cholangitis in 1996. UDCA works by replacing hydrophobic or more toxic bile acids from the bile acid pool.

Pharmacology of UDCA

UDCA is a secondary bile acid with intricate protective, immunomodulatory, and choleretic effects. It reduces the cholesterol portion of bile. One UDCA inhibits the absorption of cholesterol in the intestine and separates cholesterol into the bile, lowering the cholesterol content and saturation of bile. UDCA increases bile acid flow and promotes the fractionation of entering bile acids. Endogenous hydrophobic bile acids such as deoxycholic acid and chenodeoxycholic acid can cause intestinal toxicity. UDCA is a hydrophilic bile acid that can introduce its biological effects through multiple mechanisms. UDCA protects hepatocytes and cholangiocytes from bile acid-induced injury, such as inflammation and mitochondrial dysfunction induced by reactive oxygen species (ROS). UDCA has been shown to protect small liver tissue and stimulate anti-apoptotic pathways. It has also been demonstrated to prevent resident Kupffer cells from generating ROS in small muscles and the liver, thus alleviating oxidative stress in the liver. One UDCA can also alter the mild hydrophilic index of the bile acid pool. After oral administration, UDCA constitutes the major portion of the human bile acid pool and competitively replaces hydrophobic or more toxic bile acids. It increases the uptake of hydrophilic bile acids. UDCA’s choleretic effects have several modulating mechanisms: UDCA increases intracellular calcium levels and stimulates transport proteins and vesicular cell exocytosis in bile-stagnant liver cells. UDCA can also upregulate the expression of transport proteins such as the anion exchanger 2 (AE2). It separates from bile and is frequently observed in primary biliary cholangitis…

Introduction

Ursodeoxycholic Acid (UDCA), also known as Ursodiol, is a naturally occurring bile acid that has been used for the treatment of liver disease for decades. Its first use in traditional medicine can be traced back to more than a hundred years ago. UDCA was first characterized in the bile of Chinese black bears and is formed by the 7β-epimerization of Chenodeoxycholic Acid (CDCA), a primary bile acid. Due to its hydrophilicity, UDCA is less toxic than Cholic Acid or CDCA.

Medical Uses

In 1987, UDCA was first approved by the FDA for the dissolution of gallstones and for primary biliary cholangitis in 1996. UDCA works by replacing hydrophobic or more toxic bile acids from the bile acid pool. UDCA is a secondary bile acid with detailed hepatoprotective, immunomodulatory, and choleretic effects. It lowers the cholesterol fraction of bile quality by inhibiting the absorption of cholesterol in the intestine and its separation into bile, thereby reducing cholesterol levels in the bile. It also increases bile acid flow and promotes the fractionation of entering bile acids.

Mechanism of Action

Endogenous hydrophobic bile acids such as Deoxycholic Acid and CDCA can cause intestinal toxicity. UDCA is a hydrophilic bile acid that can introduce its biological effects through multiple mechanisms. UDCA protects liver cells and cholangiocytes from bile acid-induced damage, such as inflammation and mitochondrial dysfunction caused by reactive oxygen species (ROS). It has been shown to protect small liver tissue and stimulate the anti-apoptotic pathway. It also prevents resident macrophages in small muscles and the liver from generating ROS, thereby reducing oxidative stress in the liver. After oral administration, UDCA becomes the major component of the human bile acid pool and competes with hydrophobic or more toxic bile acids. It increases the uptake of hydrophilic bile acids and enhances bile flow by increasing intracellular calcium levels in hepatocytes and stimulating the transporters and vesicular exocytosis of bile-acid accumulated hepatocytes. It also regulates the expression of bile acid transporters, such as Anion Exchanger 2 (AE2).

Conclusion

In summary, UDCA has a detailed hepatoprotective, immunomodulatory, and choleretic effect. It has been used to treat liver diseases such as primary biliary cholangitis, non-alcoholic fatty liver disease, and drug-induced liver injury. UDCA is a safe and effective treatment for many liver diseases and is an important therapy option in clinical practice.

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