Substances tested

What has been given to the hepatocyte, and what the hepatocyte did. Research reference, not medical advice.

All substances 10

Clofibrate fibrate, peroxisome proliferator

acts on PPAR-alpha driven peroxisomal beta-oxidation

Raises the peroxisome volume fraction in hepatocytes from 1.05 percent to 6.26 percent and the mitochondrial volume fraction from 22 percent to 29.5 percent. Also protected the animals against the toxic, hypoglycaemic and hypothermic effects of hypoglycin and pent-4-enoate, and completely prevented the ultrastructural damage hypoglycin caused.

dose: 0.5 percent clofibrate in the diet for 1 to 2 months · rat, male adult · ultrastructural morphometry with biochemical assay · Van Hoof F 1985, Biochem J · source

Hypoglycin plant toxin, inhibitor of beta-oxidation

acts on mitochondrial fatty acid beta-oxidation

Doubles the mitochondrial volume fraction in hepatocytes, from 22 percent to 44 percent, and cuts the peroxisome volume fraction from 1.05 percent to 0.26 percent. Hypoglycaemic and hypothermic.

dose: injected; the amount is not stated in the abstract · rat · ultrastructural morphometry · Van Hoof F 1985, Biochem J · source

Phenobarbital barbiturate, classical CYP inducer

acts on cytochrome P-450, mixed function oxygenase system

Increases hepatocyte size: the average volume of the largest sedimenting cell fraction rose to 16,725 um3 from 10,500 um3 previously reported in untreated animals, and the number of cells in the fast-sedimenting fractions also increased. Cytochrome P-450 was raised, and a gradient of P-450 concentration across cell sizes persisted, with a 6.8-fold range in cytochrome per cell. Density fell in cells of all sizes.

dose: 40 mg/kg intraperitoneally, twice daily, for 3 days · rat · sedimentation velocity analysis with electronic cell sizing and P-450 assay · Sweeney GD 1978, J Lab Clin Med · source

3-Methylcholanthrene polycyclic aromatic hydrocarbon, CYP1A inducer

acts on aryl hydrocarbon hydroxylase, CYP1A1 and P1-450

Unlike phenobarbital, caused no significant increase in the size or number of cells in the fast-sedimenting fractions, but made the discontinuity in density and volume characteristics markedly more pronounced. The P-450 gradient across cell sizes was less steep, 4.62-fold against phenobarbital's 6.8-fold.

dose: 50 mg/kg as a single injection · rat · sedimentation velocity analysis with enzyme assay · Sweeney GD 1978, J Lab Clin Med · source

Ketoconazole azole antifungal, CYP3A4-selective inhibitor

acts on CYP3A4

Concentration-dependent inhibition of CYP3A4-mediated luciferin-isopropyl acetal metabolism in human hepatocytes, with more than 50 percent inhibition already at the lowest concentration evaluated.

dose: more than 50 percent inhibition at 0.78 uM, the lowest concentration tested · human, cryopreserved hepatocytes · luminescent substrate assay · Li AP 2009, Drug Metab Dispos · source

1-Aminobenzotriazole (ABT) non-specific cytochrome P450 inhibitor

acts on cytochrome P450, broadly

Concentration-dependent inhibition of the same CYP3A4 reaction, more than 50 percent at the lowest concentration evaluated. Used here as the non-selective comparator that establishes the reaction is P450-dependent.

dose: more than 50 percent inhibition at 7.8 uM, the lowest concentration tested · human, cryopreserved hepatocytes · luminescent substrate assay · Li AP 2009, Drug Metab Dispos · source

Rifampicin rifamycin antibiotic, PXR agonist and CYP3A inducer

acts on CYP3A, measured as 6beta-hydroxytestosterone formation

Induced CYP3A activity 2.8-fold in cryopreserved human hepatocytes, from 57.2 to 157.7 pmol per well per minute, against 2.3-fold in non-frozen cells, from 115.8 to 269.1. Note the basal activity in cryopreserved cells is about half that of fresh cells, so the larger fold-change starts from a lower floor.

dose: not stated in the abstract · human, cryopreserved and fresh hepatocytes on collagen gel · enzyme induction assay in culture · Kafert-Kasting S 2006, Toxicology · source

Acetaminophen (paracetamol) analgesic, dose-dependent hepatotoxin

acts on covalent protein binding; a 50-kDa microsomal protein comigrating with CYP2E1

Covalent binding was confined to the centrilobular hepatocytes, which is the area of the ensuing necrosis. The zonal restriction of the binding, not the binding alone, is what matches the injury pattern: the regioisomer 3'-hydroxyacetanilide binds proteins at similar levels without causing toxicity.

dose: 250 mg/kg intraperitoneally · mouse · immunochemical staining with Western blot · Salminen WF Jr 1998, Drug Metab Dispos · source

Colchicine microtubule depolymerising agent

acts on microtubules, and through them polarised membrane protein traffic

Scrambles the hepatocyte's membrane domains. The antigen A39 moved from the sinusoidal membrane to the lateral and canalicular membranes while B10 was displaced from the canalicular to the sinusoidal and lateral, ending in almost equal labelling of all three domains with both antibodies. Evidence that the hepatocyte's three-domain polarity is maintained by microtubule-dependent traffic rather than being structurally fixed.

dose: 0.25 mg per 100 g body weight; effect read at 8 hours · rat · light and electron microscopy immunolocalisation · Durand-Schneider AM 1987, Hepatology · source

Phalloidin actin filament stabiliser

acts on the pericanalicular actin cytoskeleton

Studied alongside colchicine in the same work as the second drug known to interfere with hepatocyte secretory processes, to separate microtubule-dependent from actin-dependent maintenance of membrane domain identity.

dose: not stated in the abstract · rat · light and electron microscopy immunolocalisation · Durand-Schneider AM 1987, Hepatology · source

Every row rests on a PubMed abstract read in full by hepato.site on 2026-09-13. A dose not stated in the abstract is written as such and never guessed. Doses were read off the abstract by hand rather than taken from the extracted rows, because the sweep's list handling was wrong until extractor 1.7 and a solidus fraction is still parsed as its denominator, so "1/2 mg/kg" reads as 2 mg/kg. Research reference, not medical advice.