Linalool

Linalool is a naturally occurring monoterpenoid found in several aromatic plant species, such as Lavandula angustifolia Mill, Melissa officinalis L, Rosmarinus officinalis L and Cymbopogon citratus DC (1,2).

The strong antioxidant activity of linalool inhibits LDL oxidation: this inhibition enhances cholesterol uptake via macrophage scavenger receptors (3,4). Linalool has remarkable effects on the central nervous system (CNS), acting as a relaxant, pain reducer, and anti-stress agent (5,6,7,8).

Linalool was evaluated recently for its psychopharmacological activity in mice, revealing marked dose-dependent relaxant effects on the central nervous system (CNS) (9,10).

Pain reducing activity related to its effects on the nicotinic receptor ion-channel (11) and muscle relaxant effects (12) were also reported, as well as antimicrobial activity against several bacteria and fungi (13).

Linalool is also anti-proliferative via upregulation of apoptosis in deleterious cells (14,15,16), and has neuroprotective effects including protection of memory (17).

Linalool has also been demonstrated to protect teeth and gums against periodontopathic and cariogenic bacteria when used in combination with alpha terpineol (18).

Key references:

Anti-stress (5,6,7,8)
Reduced pain (5,6,7,8)
Antioxidant (3,4)
Relaxant (5,6,7,8)
Anti-proliferative (14,15,16)
Anti-microbial (13)
Tooth/gum health (18)

1 - Batista, PA., Werner, MF., Oliveira, E.C., Burgos, L., Pereira, P., Brum, L.F., Story, GM., Santos, AR.,2010. The antinociceptive effect of (-)-linalool in models of chronic inflammatory and neuropathic hypersensitivity in mice. J. Pain 11, 1222-1229.

2 - Elisabetsky, E., Marschner, J., Souza, D.O., 1995 Effects of linalool on glutamatergic system in the rat cerebral cortex. Neurochem. Res.20, 461-465.

3 - Cho, SY., Jun, H.J., Lee, J.H., Jia, Y., Kim, K, H., Lee, S.J., 2011. Linalool reduces the expression of 3-hydroxy-3-methylglutaryl CoA reductase via sterol regulatory element binding protein-2- and ubiquitin-dependant mechanisms. FEBS Lett.585, 3289-3296.

4 - Chung, M.J., Park, K.W., Kim, K.H., Kim, C.T., Baek, J.P., Bang, K.H., Choi, Y.M., Lee, S.J.,2008. Asian plantain (Plantago asiatica) essential oils supress 3-hydroxy-3-methyl-glutaryl-co-enzyme A reductase expression in vitro and in vivo and show hypocholesterolaemic properties in mice. Br. J. Nutr.99, 67-75.

5 - Batista, P.A., Werner, M.F., Oliveira, E.C., Burgos, L., Periera, P., Brum, L.F., Story, G.M., Santos, A.R., 2010. The antinociceptive effect of (-)-linalool in models of chronic inflammatory and neuropathic hypersensitivity in mice. J. Pain 11, 1222-1229.

6 - de Almeida, E.R., Rafael, K.R., Couto, G.B., Ishigami, A.B., 2009. Anxiolytic and anticonvulsant effects on mice of flavonoids, linalool and alpha tocopherol presents in the extract o of leaves of cissus sicyoides L. (Vitaceae). J. Biomed. Biotechnol.2009,274740.

7 - Elisabetsky, E., Brum L.F., Souza, D.O., 1999. Anticonvulsant properties of linalool in glutamate-related seizure models. Phytomedicine 6, 107-113.

8 - Linck, V.M., da Silva, A.L., Figueiro, M., Piato, A.L., Hermann, A.P., Dupont Birck, F., Caramao, E.B., Nunes, D.S., Moreno, P.R., Elisabetsky, E.,2009. Inhaled linalool-induced sedation in mice. Phytomedicine 16, 303-307.

9 - Jirovetz L, Jager W, Buchbauer G, Nikiforov A, Raverdino V (1991) Investigations of animal blood samples after fragrance drug inhalation by gas chromatography/mass spectrometry with chemical ionization and selected ion monitoring. Biol Mass Spectrom 20 (12):801-803

9 - Buchbauer G, Jirovetz L., Jager W, Dietrich H, Plank C (1991) Aromatherapy: evidence for sedative effects of the essential oil lavender after inhalation. Z Naturforsch 46 (11-12): 1067-1072

10 - Elisabetsky E, Coelho De Souza GP, Dos Santos MAC, Siquiera IR, Amador TA, Nunes DS (1995) Sedative properties of linalool. Fitoterapia LXVI (5):407-414

10 - Elisabetsky E, Brum LF, Souza DO (1999) Anticonvulsant properties of linalool in glutamate related seizure models, Phytomedicine,6: 107-113

11 - Ghelardini C, Galeotti N, Salvatore G, Mazzanti G (1999) Local anaesthetic activity of the essential oil of Lavandula angustifolia. Planta Med 65: 700-703

11 - Re L., Barocci S, Sonnino S, Mencarelli A, Vivani C, Paolucci G, Scarpantonio A, Rinaldi L, Mosca E (2000) Linalool modifies the nicotinic receptor-ion channel kinetics at the mouse neuromuscular junction. Pharmacol Res 42: 177-182

12 - Lis-Balchin M, Hart S (1999) Studies on the mode of action of the essential oil lavender (Lavandula angustifolia P. Muller). Phytother Res 23 (6): 540-542

13 - Carson CF, Riley TV (1995) Antimicrobial activity of the major components of the essential oil Melaleuca alternifolia. J Appl Bacteriol 78: 264-269

13 - Pattnaik S, Subramanyam VR, Bapaji M, Kole CR (1997) Antibacterial and antifungal activity of aromatic constituents of essential oils. Microbios 89: 39-46

13 - Peana AT, Moretti MDL. Juliano C (1999) Chemical composition and antimicrobial action of the essential oils of Salvia desoleana and S. sclarea. Planta Med 65: 752 -754

14 - Paik S.Y., Koh K.H., Beak S.M., Paek S.H., Kim J.A. The essential oils from Zanthoxylum schinofolium pericarp induce apoptosis of HepG2 human hepatoma cells through increased production of reactive oxygen species. Biol.Pharm.Bul.2005;28: 802-807.doi 10.1248/bpb.28.802

15 - Jana S., Patra K., Sarkar S., Jana J., Mukherjee G., Bhattacharjee S., Mandal D.P. Antitumorigenic potential of linalool is accompanied by modulation of oxidative stress: An in vivo study in sarcoma-180 solid tumor model. Nutr: Cancer 2014; 66:835-848. Doi 10.1080/01635581.2014.904906.

16 - Russo R., Ciociaro A., Berliocchi L., Cassiano M.G., Rombola L., Ragusa S., Bagetta G., Blandini F., Corasaniti M.T. Implication of limonene and linalyl acetate in cytotoxicity induced by bergamot essential oil in human neuroblastoma cells. Fitoterapia.2013;89:48-57 doi: 10.1016/j.fitote.2013.05.014

17 - Angelica Maria Sabogal-Guaqueta, Edison Osorio, Gloria Patricia Cardona-Gomez,2016. Linalool reverses neuropathological and behavioral impairments in old triple transgenic Alzheimer’s mice. Neuropharmacology 102, 111-120

18 - Park, S. N., Lim, Y. K., Freire, M. O., Cho, E., Jin, D., & Kook, J. K. (2012). Antimicrobial effect of linalool and α-terpineol against periodontopathic and cariogenic bacteria. Anaerobe, 18(3), 369-372.