Bithionol is an aryl sulfide and anti-parasitic compound and has been found to have in vitro anti-cancer properties with ovarian cancer cell lines. It is an algaecide. Bithionol was formerly used in soaps and cosmetics until the U.S. FDA withdrew it from the market due to its photosensitizing properties.
Bithionol is soluble in DMSO but practically insoluble in water.
| Mechanism of Action |
The mechanism of action for antiparasitic properties is via competitive inhibition of electron transfer, resulting in impaired anaerobic energy metabolism and trematode death. Its parasite specificity is due to its unique target in the parasite respiratory chain. Bithionol is a potent inhibitor of soluble adenylyl cyclase, in intracellular enzyme important in the catalysis of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). The mechanism of action of Bithionol is not completely understood but is thought to inhibit cancer cell growth by reactive oxygen species generation, cell cycle arrest, NF-kB inhibition and autotaxin inhibition. |
| Spectrum | Activity against parasites including tnematodes (flatworms) including F. hepatica and Paragonimus spp. Trematodes are commonly known as flukes and are obligate internal parasites. It also has activity against tapeworms. |
| Molecular Formula | C12H6Cl4O2S |
| Cancer Applications |
The cytotoxic effects of Bithionol against a panel of ovarian cancer cell lines exhibiting varying sensitivities to cisplatin were determined via cell viability assay. Markers of apoptosis were assessed using microscopic, FACS and immunoblotting. Authors found it inhibited all tested ovarian cancer cell lines with IC50 values from 19 µM to 60 µM. It exhibited its cytotoxic effects on the cell lines regardless of their sensitivities to cisplatin. Thus, Bithionol may be useful in halting ovarian cancer cell growth (Vijayalakshmi A and Brard, 2014). |
| References | Vijayalakshmi A and Brard L (2014) Bithionol inhibits ovarian cancer cell growth in vitro - Studies on mechanism(s) of action. BMC Cancer 14 (1):61 PMID 24495391 |