UGT

Mycophenolic acid (Mycophenolate) is an inosine monophosphate dehydrogenase(IMPDH) inhibitor with anti-proliferative activity.

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

α-Angelica lactone has cardiotonic activity, may exert their effects by providing an increased contraction-dependent calcium pool to be released upon systolic depolarization.

Bakuchiol possesses anti-tumor,and anti-helmenthic properties. It has cytotoxic activity, mainly due to its DNA polymerase1 inhibiting activity. Bakuchiol has anti-bacterial activity against oral pathogens, has great potential for use in food additives and mouthwash for preventing and treating dental caries.

Demethylzeylasteral (T-96), isolated from Tripterygium wilfordii, has anti-inflammatory, immunosuppressive and anti-tumor activities. It inhibits the invasion of triple-negative breast cancer by blocking the TGF-β signaling pathway, and it can significantly reduce atherosclerosis.

Licochalcone A is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch with obvious anti-cancer effects.

1. Gitogenin, tigogenin, and solasodine are novel selective inhibitors of UGT1A4, and do not inhibit the activities of major human CYP isoforms. 2. Gitogenin and (25S)-5α-furastan-3β, 22, 26-triol are the inhibitors of enzyme α-glucosidase with IC50 value

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug/ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.

1. Schisanhenol (Schizanhenol) can protect against adriamycin induced heart mitochondrial toxicity. 2. Schisanhenol has antioxidative effect on human LDL oxidation, may be through scavenging free radicals. 3. Schisanhenol has anti-apoptosis effect on BACSs, may be related to its inhibition of ROS generation.

Ophiopogonin D' can activate SIRT1 in a dose-dependent manner. Ophiopogonin D' also noncompetitively inhibits UGT1A6 and UGT1A10.

1,2,3,6-Tetragalloylglucose (TeGG) has antioxidative activity, it also shows the most potent anticomplement activity (IC50 = 34 microM). 1,2,3,6-Tetragalloylglucose is also a potent inhibitor of UDP glucuronosyltransferase 1 A1 (UGT1A1, Ki = 1.68 μM).

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

(Rac)-Hesperetin, the racemate form of Hesperetin, is a natural flavanone compound exhibiting potent inhibitory effects against human UGT activity, making it a broad-spectrum inhibitor. Additionally, Hesperetin induces apoptosis through the activation of p38 MAPK.

Propofol β-D-Glucuronide is the major inactive metabolite of isoproterenol sulfate (a short-acting anesthetic), mediated by UDP-glucuronosyltransferase (UGT), and can be used to study sleep deprivation (SD).

Silydianin (Silidianin) exerts inhibition of UGT in human liver. Silydianin exerts inhibition of OATP1B1, OATP1B3 (unknown origin) expressed in HEK293 cells. Silydianin exerts inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells.

Naringenin-7-O-β-D-glucuronide, a metabolite of the flavonoid naringenin, is predominantly synthesized through the action of UDP-glucuronosyltransferase (UGT) isoforms UGT1A1, UGT1A3, UGT1A6, and UGT1A9.