Nerolidol

Nerolidol is a sesquiterpene alcohol present in many essential oils, particularly high in niaouli chemotypes, cabreuva and siam wood. The compound is non-irritating, non-allergenic and non-toxic.

Skin. In a modified Draize procedure on guinea pigs, nerolidol was non-sensitizing at 20 percent. Undiluted nerolidol was non-irritating to rabbit skin, and at 4 percent on 25 volunteers it caused no irritation and no sensitization. Among 102 dermatitis patients sensitive to Peru balsam, 3 reacted positively to 1 percent nerolidol.

Acute toxicity. Acute oral LD50 in rats exceeded 5 g/kg. Acute dermal LD50 in rabbits exceeded 5 g/kg.

Reproductive. In an ex vivo assay, nerolidol did not bind to estrogen receptors in female rat uterus tissue.

Mutagenicity. Neither (Z)-nerolidol nor mixed-isomer nerolidol was mutagenic in S. typhimurium strains TA98 and TA100. Nerolidol was weakly genotoxic in mouse peripheral blood leucocytes and hepatocytes, and genotoxic in a mouse micronucleus test.

Cancer. Shows significant anticancer activity, inhibiting azoxymethane-induced colon cancer in male F344 rats. Moderately cytotoxic in vitro against two human carcinoma cell lines.

In an uptake study using human skin, 39.6 percent of the applied nerolidol was found in the stratum corneum.

Nerolidol has several optical and geometric isomers. In nature, (E)-nerolidol dominates niaouli oils while (Z)-nerolidol is characteristic of cabreuva.

Nerolidol is an effective skin permeation enhancer and has been studied for improving transdermal drug delivery.