β-glucuronidase Inhibitor

hCAII-IN-4 (Compound 12j) is a potent hCA II inhibitor with an IC₅₀ of 7.78 μM. hCAII-IN-4 also inhibits β-glucuronidase with an IC₅₀ of 773.9 μM.

Aceglatone, an antineoplastic agent, is a β-glucuronidase inhibitor. Aceglatone is a compound that inhibits colon carcinogenesis and prevents the induction of colon cancer by inhibiting the hydrolysis of glucuronides. Aceglatone reduces cell proliferation, induces apoptosis and inhibits DNA synthesis in human colon cancer cells.

β-Glucuronidase-IN-6 is an Escherichia coli β-glucuronidase (EcGUS) inhibitor with an IC₅₀ of 0.39 μM, K_i of 0.60 μM, selectivity over bovine liver β-glucuronidase, and oral effectiveness. β-Glucuronidase-IN-6 preferentially binds the enzyme-substrate complex, interacts with residues Asp163, Glu413, and Trp549 to stabilize the binding complex. β-Glucuronidase-IN-6 does not inhibit Escherichia coli growth and exhibits low cytotoxicity toward human epithelial cells. β-Glucuronidase-IN-6 attenuates irinotecan-induced weight loss, diarrhea, and colonic injury in mice. β-Glucuronidase-IN-6 can be used for the research of irinotecan-induced gastrointestinal toxicity.

β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric β-glucuronidase inhibitor. β-Glucuronidase-IN-3 has potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) (IC₅₀: 12.9 nM). β-Glucuronidase-IN-3 exerts its inhibitory effect by reversibly covalently modifying the cysteine residues (Cys28, Cys443, and Cys197) of EcGUS. β-Glucuronidase-IN-3 can be used in the study of intestinal microbiota-related diseases, especially to alleviate the toxic side effects of Irinotecan (HY-16562) and nonsteroidal anti-inflammatory drugs (NSAIDs).

4'',5''-Dehydroisopsoralidin is a β-glucuronidase inhibitor (IC₅₀: 6.3 μM). 4'',5''-Dehydroisopsoralidin has anti-inflammatory and anti-oxidative effects. 4'',5''-Dehydroisopsoralidin can be used in the research of inflammation and cancners.

Sanggenol A acts as a dual inhibitor of nitrofuranone reduction mediated by the intestinal microbial nitrification reductases EcNfsA and EcNfsB. In addition, Sanggenol A is also an effective inhibitor of intestinal bacterial β-glucuronidase.

EcGUS-IN-1 (Compound E-9) is a non-competitive β-glucuronidase inhibitor, with an IC₅₀ of 2.68 μM and a K_i value of 1.64 μM. EcGUS-IN-1 can improve gastrointestinal adverse events (GIAE) caused by Escherichia coli infection by inhibiting E. coli β-glucuronidase activity.