hepatotoxicity

Datelliptium chloride hydrochloride is a DNA-intercalating agent derived from ellipticine, exhibiting anti-tumor activities.

Tienilic Acid is a uricosuric diuretic with certain hepatotoxicity

D(+)-Galactosamine hydrochloride (D-Galactosamine HCl) hepatotoxicity is associated with endotoxin sensitivity and mediated by lymphoreticular cells in mice.

Tacrine (CS 12602) is an indirect cholinergic agonist and centrally acting anticholinesterase. It is approved for the treatment of Alzheimer's disease.

Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.

2,4'-Dihydroxybenzophenone can effectively protect C57BL/6J mice from APAP-induced hepatotoxicity. Its mechanisms might be associated with its Antioxidant activity.

Cholesteryl Hemisuccinate Tris Salt is an acidic cholesteryl ester with hepatoprotective and anticancer activity.Cholesteryl hemisuccinate is a membrane stabilizer in dipalmitoylphosphatidylcholine liposomes containing Chaikosaponin-d, which enhances the anticancer efficacy of cisplatin.Cholesteryl hemisuccinate possesses antitumor activity, inhibits tumor Cholesteryl hemisuccinate has antitumor activity, inhibits tumor growth, inhibits the hepatotoxicity of acetaminophen (AAP) and prevents AAP-induced apoptosis of hepatocytes.Cholesteryl hemisuccinate protects rodents against the toxic effects of acetaminophen, adriamycin, carbon tetrachloride, chloroform, and galactosamine.

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I/R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1/2, p38, and JNK1/2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

UTL-5g (3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-) is a novel potential chemoprotective agent, TNF-α inhibitor that reduces cisplatin-induced side effects including nephrotoxicity, hepatotoxicity and hematotoxicity. It lowers elevated levels of AST, ALT, creatinine, BUN, and TNF-α, increases the reduced platelet count in mice, and acts as a novel chemo- and radioprotective agent.

1. Diosbulbin B exhibits potential hepatotoxicity. 2. Diosbulbin B has potential anti-tumor effects which may be related to influencing the immune system for the first time.

Trovafloxacin is a broad-spectrum fluoroquinolone antibiotic that inhibits the activity of DNA gyrase and topoisomerase IV, enzymes involved in DNA replication. It also acts as an effective and specific inhibitor of the pannexin 1 channel (PANX1, IC50 = 4 μM).

Trovafloxacin, a broad-spectrum quinolone antibiotic, exhibits potent activity against Gram-positive bacteria.

Meliasenin B may cause hepatotoxicity, it displays dose-dependent toxicity on HepG2 cells.

(E,Z)-2-propyl-2-Pentenoic acid is a bioactive metabolite of valproic acid that exhibits the same profile and potency of anticonvulsant activity in animal models as its parent compound without any observed teratogenicity and hepatotoxicity.

Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

Microcystin-WR, a hepatotoxic metabolite derived from cyanobacteria, has been demonstrated to induce hepatotoxicity in mice [1].

Anti-inflammatory agent 62 mitigates acetaminophen-induced hepatotoxicity in HepG2 cells by modulating inflammatory and oxidative stress pathways [1].

1. Alisol B 23-acetate (Alisol B Acetate) produces protective effect against ANIT-induced hepatotoxity and cholestasis, due to FXR-mediated regulation of transporters and enzymes. 2. Alisol B 23-acetate produces promotive effect on liver regeneration, due to FXR-mediated regulation of genes involved in hepatocyte proliferation and hepato-protection. 3. Alisol B 23-acetate produces a protective effect against CCl4-induced hepatotoxicity, due to FXR and STAT3-mediated gene regulation.

Ganodermanondiol exhibits potent cytoprotective effects on t-BHP-induced hepatotoxicity in human liver-derived HepG2 cells, presumably through Nrf2-mediated antioxidant enzymes and AMPK.

Compound 6, known as Heilaohuguosu F, is a tetrahydrofuranolignan demonstrating weak hepatoprotective properties. It exhibits a mild protective effect against acetaminophen (APAP)-induced hepatotoxicity in HepG2 cells.

Glomeratide A, a benzophenone C-glucoside, exhibits hepatoprotective properties and safeguards rat liver epithelial stem-like cells from d-galactosamine-induced hepatotoxicity.

1. Kamebakaurin (Kamebakaurine) has the ability to protect the liver from APAP-induced hepatotoxicity, presumably by both inhibiting the inflammatory response and oxidative stress. 2. Kamebakaurin inhibits the expression of hypoxia-inducible factor-1α and its target genes to confer antitumor activity. 3. Kamebakaurin has anti-cancer and anti-inflammatory activities through direct inhibition of DNA-binding activity of nuclear factor-kappa B (NF-κB) p50.4. Kamebakaurin has anti-neuroinflammatory activity via inhibition of c-Jun NH -terminal kinase and p38 mitogen-activated protein kinase pathway in activated microglial cells.

3-Cysteinylacetaminophen is an acetaminophen-protein adduct formed during the metabolism of acetaminophen.[1],[2] 3-Cysteinylacetaminophen has been found in isolated human serum following therapeutic and supratherapeutic doses of acetaminophen and in the presence and absence of hepatotoxicity.[3],[4] In mice, 3-cysteinylacetaminophen decreases renal glutathione (GSH) levels, an effect that can be blocked by the γ-glutamyl inhibitor acivicin.

Dibenamine hydrochloride is a competitive and irreversible blocker of the β-adrenergic receptor.

CAY10704 is a potent inhibitor of hepatitis C virus (HCV) infection (EC50 = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC50 = 21.3 μM). It displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without significant hepatotoxicity. CAY10704 is selective for HCV over dengue virus (EC50 = 4.62 μM).

Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) is a highly soluble cholesterol analogue often used in polar solutions for its hepatoprotective, anticancer and tumour growth inhibiting properties. Cholesteryl Hemisuccinate inhibits the hepatotoxicity of acetaminophen and prevents AAP-induced apoptosis and necrosis in hepatocytes. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase, thereby inhibiting DNA replication and repair as well as cell division.

CT1-3 is a potent anti-cancer agent. CT1-3 regulates the JNK/Bcl-2/Bax/XIAP pathway, which induces mitochondria-mediated apoptosis. CT1-3 regulates the E-cadherin/Snail axis to inhibit epithelial mesenchymal transition (EMT) potentials in human cancer cells (HCCs) and suppresses tumourigenesis. CT1-3 has anti-tumour effects in mouse models and does not show significant hepatotoxicity or nephrotoxicity.

Senkirkin is a pyrrolizidine alkaloid with hepatotoxicity.

CP-199330 is a cysteyl LT1 receptor antagonist with no hepatotoxicity and is equivalent to the commercially available CYSLT1 receptor antagonists Zafirlukast and Pranlukas.

Diosbulbin C has hepatotoxicity.

Ar-H047108 free base is an imidazopyridine potassium competitive acid blocker (P-CAB). This drug may be used to treat early stellate cell activation and veno-occlusive-disease (VOD)-like hepatotoxicity.

Saikosaponin D is a novel SERCA inhibitor by inhibiting NF-κB and STAT3 signaling to protect against acetaminophen-induced hepatotoxicity.

Akt1-IN-1 is a potent and selective inhibitor of Akt1, demonstrating an IC50 of 18.79 nM in MIA PaCa-2 cells, indicating its high efficacy in inhibiting this specific kinase. Notably, it shows no significant teratogenicity, hepatotoxicity, or cardiotoxicity (No Observed Adverse Effect Level > 100 µM), making it a viable candidate for anticancer research.

Taurohyodeoxycholic acid (THDCA) is a taurine-conjugated form of the secondary bile acid hyodeoxycholic acid .1THDCA decreases the size and weight of human gallstonesin vitro. It increases bile flow, biliary cholesterol secretion, and biliary lipid secretion in rats.2Co-administration of THDCA with taurochenodeoxycholic acid prevents TCDCA-induced hepatotoxicity, increasing bile flow as well as biliary acid and phospholipid secretion in rats.3THDCA also reduces myeloperoxidase activity, expression of TNF-α and IL-6, and colonic damage in a mouse model of TNBS-induced ulcerative colitis.4Taurohyodeoxycholic acid MaxSpec standard is a quantitative grade standard of taurohyodeoxycholic acid (sodium salt) that has been prepared specifically for mass spectrometry and related applications where quantitative reproducibility is required. The solution has been prepared gravimetrically and is supplied in a deactivated glass ampule sealed under argon. The concentration was verified by comparison to an independently prepared calibration standard. Verified concentration is provided on the certificate of analysis. This taurohyodeoxycholic acid MaxSpec standard is guaranteed to meet identity, purity, stability, and concentration specifications and is provided with a batch-specific certificate of analysis. Ongoing stability testing is performed to ensure the concentration remains accurate throughout the shelf life of the product.Note: The amount of solution added to the vial is in excess of the listed amount. Therefore, it is necessary to accurately measure volumes for preparation of calibration standards. Follow recommended storage and handling conditions to maintain product quality.

Nialamide monohydrochloride is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class that was used as an antidepressant. It was withdrawn by Pfizer several decades ago due to the risk of hepatotoxicity.

Anti-NASH Agent 1 (Compound 3d), derived from Elafibranor, serves as a strong PPAR-α/δ agonist aimed at treating nonalcoholic steatohepatitis (NASH). At dosages of 3-10 mg/kg over four weeks, this compound ameliorates hyperlipidemia, liver fat degeneration, and inflammation in a methionine-choline deficiency (MCD)-induced NASH mouse model, exhibiting minimal hepatotoxicity while providing substantial hepatic protection [1].

Zederone has anti-bacterial activity,it inhibits gram-positive bacteria activity. Zederone induces hepatotoxicity implicated the induction of Cyps, which leads to the formation of biological reactive metabolites and that cause the oxidative stress and liver cell injuries.

Celosin H, celosin I, and celosin J could be used as chemical markers for the quality control of C. argentea seeds. Celosin I exhibited significant hepatoprotective effect on carbon tetrachloride-induced and N,N-dimethylformamide-induced hepatotoxicity in

9-Oxo-10,11-dehydroageraphorone has acaricidal activity. It induces hepatotoxicity and cholestasis in rats. 9-Oxo-10,11-dehydroageraphorone also effectively inhibits the proliferation of HeLa cells by arresting the cell cycle transition from S to G2/M pha

Metamizol (Methamizole) blocks thyroid hormone production from the thyroid gland which is an anti-thyroid agent. However, Metamizol has hepatotoxicity as adverse effect [1].

AChE-IN-9, a Tacrine glycoconjugate connected to acetylated β-Glucose, acts as an AChE inhibitor, demonstrating an IC 50 value of 0.4 μM and exhibiting reduced hepatotoxicity in healthy cells. This compound finds use in Alzheimer's research [1].

1. Toosendanin possesses hepatotoxicity. 2. Toosendanin has effects on the growth, cell cycle arrest, induction of apoptosis and the involved signaling pathway in human promyelocytic leukemia HL-6 cells. 3. Toosendanin is an effective insecticide for Ae.

N-Nitrosofenfluramine is a compound that is thought to cause hepatotoxicity in subjects.

Celosin L, a triterpenoid saponin, demonstrates hepaprotective activity and exerts protective effects against APAP-induced hepatotoxicity in HepG2 cells [1].

Andrographiside shows protective effects on hepatotoxicity induced in mice by carbon tetrachloride or tert-butylhydroperoxide (tBHP) intoxication, the effects could be due to its glucoside groups which may act as strong antioxidants.

12-Hydroxynevirapine (12-hydroxy-NVP; 12-OH-NVP), a significant oxidative metabolite of Nevirapine—an antiviral drug for HIV-1 infections known for potential idiosyncratic hepatotoxicity and skin rashes—undergoes bioactivation through sulphotransferases (SULTs) in the liver and skin to form the reactive species 12-Sulphoxy-nevirapine [1] [2].

Anticancer agent 12 shows cytotoxic activity in malignant cells with no hepatotoxicity.

L-Cysteine-glutathione disulfide, a glutathione derivative endogenous to mammalian cells, is comprised of the oxidized form of free glutathione tripeptide linked via a disulfide bond to L-cysteine. It has been shown to protect mice against acetaminophen-induced hepatotoxicity.

Dihydroisotanshinone I has protective action against menadione-induced hepatotoxicity, attributed to its antioxidant properties including the free radical scavenging activity and inhibition of lipid peroxidation.