intercalants

In phamacology, intercalants are compounds with intercalative properties. In addition to cytostatics, these include polyaromatic hydrocarbons and phenanthridine-type dyes such as ethidium bromide or the proflavin type (Falbe and Regitz, 1992; Mutschler 1996). Indirubin derivatives also intercalate into the DNA.

In biochemistry, intercalation (from the Latin intercalare = to insert) refers to a special interaction between small molecules and DNA. The small molecule moves into the space between two neighboring base pairs of the DNA double helix. As a result, the geometry of the DNA strand is distorted at these points. This disrupts transcription and consequently also replication. Intercalation is attributed to this effect for the chemotherapeutic effect of antibiotics or cytostatics such as actinomycin or anthracyclines (e.g. doxorubicin, daunorubicin).

Intercalation is therefore held responsible for the mutagenic effect of many representatives of this substance class, and the chemotherapeutic effect of antibiotics or cytostatics such as actinomycin or anthracyclines, such as daunorubicin, is also attributed to intercalation.

1. Graefe KH et al. Unselective cytotoxic chemotherapeutics (cytostatics) In: Graefe KH et al. (Eds) Pharmacology and Toxicology. Georg Thieme Publishers Stuttgart S 672-673