β-glucuronidase Inhibitor

D-Saccharic acid 1,4-lactone hydrate is an orally active β-glucuronidase inhibitor (IC₅₀=48.4 μM). D-Saccharic acid 1,4-lactone hydrate can be used as a standard agent compared with novel β-glucuronidase inhibitors. D-Saccharic acid 1,4-lactone hydrate possesses anticarcinogenic, detoxifying, and antioxidant properties.

Saccharic acid is a competitive and potent inhibitor of β-glucuronidase. Saccharic acid inhibits glucuronide synthesis. Saccharic acid as an efficient iron chelate to enhance photo-Fenton
degradation of organic contaminants.

Saccharolactone is a potent orally active β-glucuronidase inhibitor. Saccharolactone markedly lowers biliary endogenous β-glucuronidase activity in the rat bile. Saccharolactone can stabilize glucuronide metabolites in vitro. Saccharolactone is also a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms (IC₅₀ < 4 mM).

β-Glucuronidase-IN-5 (Compound 19; Compound 5c) is a β-glucuronidase inhibitor with an IC₅₀ of 39.8 μM. β-Glucuronidase-IN-5 does not show significant cytotoxicity towards PC-3 cells, with its IC₅₀ > 30 μM. β-Glucuronidase-IN-5 shows no affinity for adenosine receptors (A₁ and A₂A receptors). β-Glucuronidase-IN-5 can be used to study diseases related to excessive expression of β-glucuronidase (such as colon cancer, arthritis, and AIDS complications).

β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC₅₀ and a K_i of 283 nM and 164 nM, respectively.

UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC₅₀ value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide (HY-126373) processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.

2′-Hydroxydaidzein is a metabolite. 2′-Hydroxydaidzein inhibits the release of chemical mediator from inflammatory cells. 2′-Hydroxydaidzein significantly inhibits lysozyme and β-glucuronidase release from rat neutrophils, which is stimulated with fMLP/CB, respectively.

3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC₅₀ value of 0.74 μM, an K_i value of 0.58 μM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies.

2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC₅₀ values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively.

Ganoderenic acid A is a lanostane-type triterpene. Ganoderenic acid A is a potent inhibitor of β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury.

Siastatin B is an effective broad-spectrum glycosidase inhibitor that can effectively inhibit the activities of sialidase, β-D-glucuronidase, N-acetyl-glucosaminidase, β-glucuronidase, and human heparinase.

Garcinoic acid is an orally active anti-inflammatory agent that crosses the blood-brain barrier. Garcinoic acid also enhances efferocytosis and enzyme/receptor regulation, and selectively inhibits human COX-2, porcine α-amylase, Saccharomyces cerevisiae α-glucosidase and human DNA polymerase β (IC₅₀=11 μM), as well as activates human PXR. Garcinoic acid enhances macrophage efferocytosis via receptors such as MerTK and LRP-1, and promotes the production of pro-resolving lipid mediators. Garcinoic acid inhibits NF-κB activation and pro-inflammatory cytokine secretion, interferes with Aβ aggregation, downregulates NLRP3 inflammasome activity, and binds to targets including CD44 and EGFR to inhibit leukemia cell proliferation. The pharmacological activities of Garcinoic acid, such as antioxidant, anti-inflammatory and lipid metabolism-regulating effects, are widely used in studies related to various diseases including atherosclerosis, Alzheimer's disease, type 2 diabetes, inflammatory bowel disease and viral pneumonia.

β-Glucuronidase/hCAII-IN-2 (Compound 12e) is a potent β-glucuronidase and hCA II inhibitor with an IC₅₀ of 440.1 μM and 4.91 μM, respectively.

Ilicicolin C exhibits antibacterial activity against Pseudomonas syringae with IC₅₀ of 28.5 µg/mL. Ilicicolin C exhibits weak inhibitory activities against acetylcholinesterase (AChE) and β-glucuronidase with IC₅₀ of 30-43 µg/mL. Ilicicolin C exhibits weak cytoxicity in human lung fibroblasts with IC₅₀ of 64-120 µg/mL. Ilicicolin C affects seed germination and root tip growth of lettuce.

Carbidopa (monohydrate) (Standard) is the analytical standard of Carbidopa (monohydrate). This product is intended for research and analytical applications. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.

Foryshiyanine A is a triterpenoid alkaloid. Foryshiyanine A possesses anti-inflammatory activity, inhibiting the release of β-glucuronidase from rat polymorphonuclear leukocytes. Foryshiyanine A exhibits antiviral activity, with an EC₅₀ of 4.5 μM against respiratory syncytial virus (RSV) and an IC₅₀ of 7.3 μM against influenza A virus (H1N1). Foryshiyanine A reduces viral load by disrupting viral replication and entry. Foryshiyanine A may be used for the researches of inflammation and infection.

Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC₅₀s of 2.07 μM and 3.05 μM, respectively.

CH-123 is an orally active lipid-lowering agent. CH-123 inhibits the elevated activities of β-glucuronidase, β-galactosidase, N-acetyl-β-glucosaminidase and acid phosphatase in aortic smooth muscle cells and hepatocytes. CH-123 reduces serum total lipid and cholesterol levels, as well as intracellular cholesterol content in aortic smooth muscle cells. CH-123 significantly inhibits lysosomal enzyme activity. CH-123 can be used in the research of atherosclerosis.

6-Keto-PGE1 (6-keto-Prostaglandin E1) is a biologically active derivative of PGE1. 6-Keto-PGE1 inhibits adenosine diphosphate-induced platelet aggregation. 6-Keto-PGE1 reduces cardiac afterload, decreases the accumulation of plasma myocardial depressant factor (MDF), lowers arterial blood pressure, dilates vascular beds, inhibits the vasoconstrictive response of vascular smooth muscle, and increases pulmonary compliance. 6-Keto-PGE1 directly stabilizes isolated cat liver lysosomes and significantly reduces the release of β-glucuronidase and cathepsin D. 6-Keto-PGE1 prolongs the survival time of traumatized rats and exerts protective effects through hemodynamic and cytoprotective actions. 6-Keto-PGE1 reduces central airway resistance. 6-Keto-PGE1 can be used in studies related to traumatic shock.

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.