2008

NPC Natural Product Communications Vol. 3

No. 7
1183 - 1192
Linalool – A Review of a Biologically Active Compound of
Commercial Importance
Guy P. P. Kamatou and Alvaro M. Viljoen*

Department of Pharmaceutical Sciences, Tshwane University of Technology, Private Bag X680,

Pretoria, 0001, South Africa

viljoenam@tut.ac.za

Received: May 10th, 2008; Accepted: May 31st, 2008

Since the earliest times fragrant materials have been used in rituals. Today, a lucrative industry has developed to produce and
deliver fragrances and aromatic chemicals with various applications in modern society. Linalool, a much sought after
compound in the flavor and fragrance industry is a monoterpene alcohol which occurs naturally in many aromatic plants.
Linalool and linalool-rich essential oils are known to exhibit various biological activities such as antimicrobial, anti-
inflammatory, anticancer, anti-oxidant properties and several in vivo studies have confirmed various effects of linalool on the
central nervous system. The applications of linalool are not confined to simply adding or enhancing a specific scent to domestic
products such as soaps, detergents and shampoos. Linalool also plays an import role in nature as a key compound in the
complex pollination biology of various plant species to ensure reproduction and survival. Linalool is also a key compound for
the industrial production of a variety of fragrance chemicals such as geraniol, nerol, citral and its derivatives, as well as a lead
compound in the synthesis of vitamins A and E. The repellent properties of linalool on various crop-destroying insects has been
well documented accentuating the application of this molecule in eco-friendly pest management. This review aims to highlight
the various biological properties of linalool and to emphasize the value of linalool and linalool-rich essential oils in
phytotherapy.

Keywords: Linalool, essential oils, aromatic plants, biological activities.

1. Introduction chemical intermediate in the biosynthesis of vitamin

E [2]. Linalool is also the principal component of
Fragrance-containing products are part of daily life.
many essential oils known to exhibit several
The majority of personal-care, household and laundry
biological activities such as antibacterial and
products on the market contain fragrances. In
antiplasmodial effects [4]. In addition, the anti-
cosmetic formulations, fragrances are commonly
inflammatory, antihyperalgesic and antinociceptive
used to give the consumer a feeling of well-being, to
effects of linalool in different animal models have
mask the odour of other chemical ingredients or to
been established [5-7]. Since its discovery, linalool
contribute a specific cosmeceutical property (e.g. a
has been widely studied, yet, most of the research is
soothing effect). It is estimated that approximately
fragmented and obscured in several broader studies.
3000 chemical substances (including essential oils
The purpose of this review is to coherently re-
and their constituents) are commonly used for this
assemble some of the most significant research
purpose [1].
findings specifically relating to linalool and to
highlight its importance in nature, industry and
Many plants produce linalool, with members of the
phytotherapy.
Lamiaceae (mints), Lauraceae (laurels, cinnamon,
rosewood) and Rutaceae (citrus), often accumulating
2. Chemical aspects
linalool in abundance [2]. Linalool is an unsaturated
monoterpene alcohol with the specific odour In comparison with other essential oil components
description; “light and refreshing, floral-woody, with linalool has an appreciable solubility in water.
a faint citrusy note” [3]. This volatile component is a Linalool exists in two enantiomeric forms, S-(+)- and
1184 Natural Product Communications Vol. 3 (7) 2008 Kamatou and Viljoen

OH OH the balance obtained from natural plant terpenes [2].

Approximately 95% of synthetic linalool and
practically the entire volume extracted from natural
sources is used in formulations to contribute a
specific fragrance in cosmetics, soaps, perfumes,
(A) (B) household cleaners, while only approximately 1% is
Figure 1: The structure of linalool: A (S)-(+)-linalool and B (R)-(–)-
added to food and beverages for aroma and flavoring
linalool). [2]. Before the 1950s, nearly all linalool used in
perfumery was isolated from essential oils,
R-(−)-linalool (Figure1), which differ in their particularly from rosewood oil [10].
olfactory and physiological properties [5].
A FAO/WHO Joint Expert Committee on Food
R-(−)-Linalool has a fragrance reminiscent of Additives [11] estimated the amount of terpene
lavender, whereas S-(+)-linalool has more of a alcohols used in the flavoring of food and beverages
petitgrain fragrance [8]. Linalool may be isolated in the USA and Europe at approximately 75
from the essential oils of linalool-biosynthesizing tons/annum. The majority of these terpene alcohols
plants. It can be produced industrially by hemi- consist of linalool and its ester, linalyl acetate.
synthesis from natural pinene or through total
chemical synthesis. Isolation of linalool as a single Traditionally, linalool, has been (and still is) used in
compound from an essential oil mixture can be the form of natural products such as dried herbs, as a
achieved by using various chromatographic fumigant for the storage of cereals and as a deterrent
techniques such as column chromatography or against pests. However, this specific use cannot be
through fractional distillation. The partial synthesis accurately quantified [10].
of linalool is based either on α- or β-pinene [9]. α-
Pinene is hydrogenated to cis-pinane and 4. The role of linalool in pollination
subsequently oxidised to a cis/trans mixture of
Pollination is vital to ensure the existence and
pinane hydroperoxide, which is in turn reduced to the
continued survival of plants. It is hypothesized that
corresponding pinanols and the latter finally
floral heat and scent may have been key components
pyrolysed to the respective d- or l-linalools. The total
in the breeding systems of early angiosperms [12].
chemical synthesis of linalool is by way of 2-methyl-
The flowers of many plants attract pollinators by
2-hepten-6-one [2]. It may start from the reaction of
producing volatile aromatic compounds within the
acetylene with acetone resulting in 3-methyl-1-butyn-
various floral organs (e.g. stigma, style, ovary, petals,
3-ol, which is hydrogenated over a palladium catalyst
sepals) or in special glands called osmosphores [13].
to 3-methyl-1-buten-3-ol, that is in turn reacted with
Volatile compounds predominate in attracting
either diketene or acetic acid ester to the aceto-acetate
pollinators at night when visual cues become
and the latter thermally reacted to yield 2-methyl-2-
inadequate [14]. Certain compounds can be detected
hepten-6-one. Alternatively, 3-methyl-1-buten-3-ol is
by insects at a very low concentration, acting as
reacted with isopropenyl methyl ether to yield 2-
essential components for pollinator attraction in a
methyl-2-hepten-6-one. In this synthetic pathway,
complex scent or sometimes even as the most
isoprene hydrochloride is reacted with acetone in the
informative molecule [15]. Therefore, plant scent in
presence of either an alkaline agent or an organic
insect interactions cannot usually be reduced to the
base as catalysts to yield 2-methyl-2-hepten-6-one. 2-
effect of one major compound.
Methyl-2-hepten-6-one is finally reacted with
acetylene to dehydrolinalool, which is partially
Linalool is present in the floral fragrance of diverse
hydrogenated. The industrial methods for the
plant families (e.g. Lamiaceae, Lauraceae,
synthesis of linalool are through the pinene and the
Verbenaceae) and is attractive to a broad spectrum of
dehydrolinalool routes.
pollinators (e.g. bee and butterfly), herbivores and
parasitoids [16]. An investigation into the pollination
3. Linalool production
of Satyrium microrrhynchum, a rare South African
The industrial estimate for the worldwide production orchid revealed that this orchid is pollinated
of linalool in 2000 was 12,000 tons. Over half of this specifically by two insects; a cetoniid beetle
is estimated to be produced through synthesis, with (Atrichelaphinus tigrina) and a pompilid wasp
(Hemipepsis hilaris). The two insects have short
Linalool: A Review Natural Product Communications Vol. 3 (7) 2008 1185

mouthparts and collect nectar from the perianth hairs. inhibitory concentration) method [4] indicates that
In the orchids, nectar is secreted as droplets on long linalool exhibits some degree of activity against
floral hairs. The fragrance from plants in three Escherichia coli (MIC value: 51.9 µM) and C.
different populations, analyzed by gas albicans (MIC value: 38.9 µM).
chromatography coupled to mass spectrometry,
confirmed the dominance of linalool [17]. Like most chemotherapeutic agents, linalool exhibits
specificity for certain pathogens. Results from an in
A study was conducted to explore whether or not vitro assay (Ames with and without S9 activation) of
there are convergent patterns in floral scent linalool exposed to Salmonella thyphimurium strains
composition among plant species that rely (TA92, TA94, TA98, TA100, TA1535 and TA1537)
(completely or partially) on butterflies for pollination. showed that linalool was not capable of inhibiting the
Floral scent compounds were analyzed from 22 growth of this microbe [21-23].
flowering butterfly-pollinated plant species,
representing 13 families (originating mainly from The influence of (R)-(−)-linalool on airborne
temperate North Europe, tropical and temperate microbes when vaporized with an air washer has
America). It was postulated that the benzenoids been reported. The average reduction in germ count
phenylacetaldehyde and 2-phenylethanol, the was above 40% [24]. When water devoid of volatile
monoterpenes linalool and linalool oxide (furanoid) I compounds was applied, the colony forming units
and II serve as a signal to attract pollinating increased. These results show the positive effect of
butterflies, and these compounds may have evolved selected aromatic compounds (including linalool) on
in conjunction with the sensory capabilities of the reduction of airborne pathogens.
butterflies as a specific group of pollinators [18].
Various essential oils containing linalool have shown
5. The pharmacological properties of linalool promising activity against Plasmodium falciparum
[25,26]. However, the antiplasmodial activity of
5.1. Infectious diseases: Despite the progress in
linalool as a single compound exhibited poor activity
understanding the life cycle and control of many
when tested in vitro on P. falciparum FCR-3 strain
pathogens, the majority of diseases affecting millions
(IC50 value: 254.4 µM) using the 3[H]-hypoxanthine
of people in developing countries are caused by
incorporation assay [4]. Therefore it may be
micro-organisms. Although a plethora of papers are
postulated that linalool probably may act in a
available on the anti-infective properties of essential
synergistic manner with other essential oil
oils, very few studies have explored the activity of
components to inhibit the in vitro growth of the P.
individual oil constituents (e.g. linalool). The
falciparum FCR-3 strain.
essential oil of Bursera aloexylon which contains
high levels of linalool (96%) was shown to be
The in vitro leishmanicidal effects of Croton
effective against Rhodococcus equi (0.60 mg/mL)
cajucara rich in linalool was investigated against
and Staphylococcus epidermides (0.15 mg/mL) [19].
Leishmania amazonensis [27]. The LD50 values for
The essential oil of Croton cajucara (linalool-rich
promastigotes were 8.3 ng/mL for the linalool-rich
chemotype) inhibits the growth of Candida albicans,
essential oil and 4.3 ng/mL for purified linalool,
Lactobacillus casei, S. aureus, Streptococcus
respectively and the LD50 values for amastigotes
sobrinus, Porphyromonas gingivalis and
were 22.0 ng/mL, respectively for the essential oil
Streptococcus mutans cell suspensions. All of these
and 15.5 ng/mL for purified linalool. Morphological
pathogens are associated with oral cavity disease
changes in L. amazonensis promastigotes treated with
[20]. These results may provide some scientific
15 ng/mL of essential oil were observed by
evidence for the inclusion of linalool as an ingredient
transmission electron microscopy. Leishmanial
in several mouthwash and gargle products claimed to
nuclear and kinetoplast chromatin destruction,
provide symptomatic relief of sore throats, mouth
followed by cell lysis, was observed within 1 h.
ulcers and tender gums. The effects of linalool on the
Mouse peritoneal macrophages pretreated with 15
cell biology of C. albicans were further studied by
ng/mL of essential oil reduced the interaction
electron microscopy, which showed that linalool
between these macrophages and L. amazonensis by
induced a reduction in cell size and germination [20].
50% [27].
The antimicrobial activity of linalool against various
pathogens using the microtitre plate assay (minimum
1186 Natural Product Communications Vol. 3 (7) 2008 Kamatou and Viljoen

5.2. Anti-oxidant activity: The anti-oxidant (51%, P = 0.03 and 38%, P = 0.02) and 5 h (45%, P =
properties of essential oils have been of great interest 0.01 and 34%, P = 0.04).
in recent years. Their possible use as natural additives
has emerged from a growing tendency to replace 5.4. Anticancer activity: Cancer is a worldwide
synthetic anti-oxidants with natural compounds [28]. public health concern, with more than 11 million
Cinnamomum osmophloeum (Lauraceae) oil people being diagnosed with the disease every year.
displayed the ability to scavenge the DPPH radical It is estimated that by 2020, there will be 16 million
(IC50 value: 29.7 µg/mL) and this activity was new cases annually [33]. Plants and plant products
correlated to the major compound, linalool (73%) (including essential oils) have a long and established
[29]. Although, the anti-oxidant activity of essential use to prevent or treat symptoms associated with
oils has mainly been correlated with the presence of cancer. Studies were conducted on cancer cells
the major compounds in some plants (e.g. linalool), derived from eight human organs, using ten related
van Zyl et al [4] demonstrated that linalool as a pure compounds from common vegetables and fruits
single component has little anti-oxidant activity (IC50 including linalool and flavonoids (e.g. luteolin) [34].
value > 648 µM) against the DPPH radical. Linalool showed the strongest activity against a broad
range of cancer cells, such as carcinoma of the cervix
5.3. Anti-inflammatory activity: Inflammation is the (IC50: 0.37 μg/mL), stomach (IC50: 14.1 μg/mL), skin
normal physiological response which occurs when (IC50: 14.9 μg/mL), lung (IC50: 21.5 μg/mL) and bone
the body is exposed to infective agents or to physical, (IC50: 21.7 μg/mL). In another study, the effects of
or chemical change [30]. Some essential oils are linalool on tumor cells were investigated [35]. The
used in aromatherapy for their therapeutic benefits results obtained confirmed that linalool inhibited
such as their anti-inflammatory, anticancer and tumor cells (CD50 = 82.3, 90.7 and 113.6 μ g/mL for
antiplasmodial properties. A number of linalool and A-549, HeLa e HT-29 cell lines, respectively), while
linalyl acetate-producing species are used in linalool did not exhibit any cytotoxicity against non-
traditional medicine systems to relieve symptoms and tumor cells.
cure a variety of ailments, both acute and chronic [5].
Linalool-producing species have been reported to The chemopreventive activity of linalool was also
possess good anti-inflammatory activity and exhibit a studied using the 7,12-dimethylbenz[a]anthracene
peripheral analgesic effect [31,32]. These (DMBA) induced rat mammary carcinogenesis
pharmacological activities were attributed to the model. Rats were fed with a diet containing 1%
content of alcohols such as linalool and its linalool for a period of 20 weeks. A fortnight after the
corresponding ester (linalyl acetate) [32]. Linalyl initiation of the dietary regimen, a single dose of 65
acetate is mentioned here as it is considered a pro- mg/kg DMBA in 0.5 mL sesame oil was
drug in the sense that this ester is metabolized to the administered to each rat by gastric intubation. Results
alcohol. The inhibitory effect of (–) linalool, (±) showed no significant reduction in the total number
linalool and linalyl acetate, on carrageenin-induced of tumors and no significant extension of the tumors
edema in rats was studied. (–) Linalool at a dose of when compared to the controls [36,37]. The ability of
25 mg/kg body (wt), did not exhibit any activity 1 h linalool to inhibit large bowel and duodenal tumor
after administration of carrageenin, but after 3 and 5 formation using the azoxymethane-induced neoplasia
h, a significant inhibition of oedema (28%, P = 0.008 in rats produced no significant decrease in
and 25%, P = 0.0004, respectively) was observed. adenocarcinomas of the duodenum [38].
The administration of higher doses (50 and 75 mg/kg Furthermore, no epidemiological or case reports
body wt.) resulted in the higher inhibitory effect investigating the association of exposure to linalool
against oedema, which appeared 1 h after the and cancer risk in humans have been identified [10].
carrageenin injection (58%, P = 0.008 and 60%, P =
0.006, respectively) [5]. (±)-Linalool at 12.5 mg/kg Linalool has been examined for potential
failed to produce any effect and exhibited a antimutagenic and antitumorigenic activity. It was
significant anti-oedematous effect (55%, P = 0.03) 1 not effective against the activity of 4-nitroquinoline
h after carrageenin administration. At 50 and 75 1-oxide in Escherichia coli strain WP2s at 200
mg/kg body wt the racemate however failed to ng/mL [39]. In Drosophila melanogaster, linalool
produce any obvious effect 1 h after carrageenin had no effect on tumour expression in the melanotic
induction, but displayed a positive effect after 3 h strain, tu bw; +s-tu, but it caused retardation in
development [40].
Linalool: A Review Natural Product Communications Vol. 3 (7) 2008 1187

5.5. The effects of linalool on the central nervous Methods used to control insect pests include chemical
system (CNS): The psychopharmacological activity and biological treatment [49,50]. Essential oils
of linalool in mice, showed marked dose-dependent contain a variety of compounds which are known to
sedative effects on the central nervous system. This aid the plants’ defense mechanisms against plant
includes protection against pentylenetetrazol, enemies [51]. Herbs and their constituents as a source
picrotoxin and transcorneal electroshock-induced of alternative fumigants have been suggested by
convulsions, hypnotic and hypothermic effects [41- many contributors [52,53] and the insecticidal
45]. A study was conducted using 40 different properties of numerous essential oils and some
extracts including 9 essential oils, to observe their monoterpenes have been extensively studied on
ability to decrease the motility of test animals [46]. various insects [54,55].
Results showed that linalool decreased the motor
activity (more than 60%) of 6-8 week old mice after Ecologically, insects (e.g. mosquitoes) are important
inhalation (1 h). components of the aquatic and terrestrial food chain.
With respect to human well-being, mosquitoes pose a
Several plant species rich in linalool are used as potential health risk as they may cause skin allergies,
anticonvulsants by practitioners of traditional and are vectors of a number of serious diseases, such
medicine in the Brazilian Amazon [42]. Thus, it is as malaria, yellow fever, dengue and West Nile Fever
not surprising that CNS depressant activity was [56,57]. Despite prevention and protection measures
observed with linalool. Various mental disorders to curb diseases transferred by mosquitoes, disastrous
have traditionally been treated with plant-derived outbreaks still occur in Africa and the rest of the
natural products [47]. Using the Vogel and Geller world often resulting in a humanitarian crisis.
conflict tests, Umezu et al [47] tested linalool which
produced significant anticonflict effects in both the Several aromatic plants are used as natural repellents
Geller and Vogel tests at 400 mg/kg. Thus, although in many African countries where traditional practices
linalool alone could not completely account for the remain the first option of health [58]. In most of the
anticonflict effects of lavender oil, it nevertheless aromatic plants studied, linalool, eugenol, geraniol
could be a major contributor to the observed effects. and terpineol have been identified as contributing
positively to the repellent action. Larvicidal assays
Studies have demonstrated that people with were conducted to evaluate the LC50 and LC90 after
Alzheimer’s disease have decreased brain levels of 24 and 48 h of the essential oils and some of their
acetylcholine. The inhibition of the major constituents against the seaside mosquito
acetylcholinesterase enzyme favors the accumulation Ochlerotatus caspius. All tested oils proved to have
of acetylcholine. Therefore, an increase in the amount strong larvicidal activity (LC50: 15–156 ppm), with
of acetylcholine may reduce mental decline in people coriander fruit oil (which is rich in linalool) as one of
with Alzheimer’s disease and related conditions. The the most potent oils [59].
in vitro anticholinesterase activity of terpenes
including linalool was examined and results indicated An experiment to determine the fumigant toxicities of
that linalool inhibited the acetylcholinesterase 10 monoterpenes against the mature mushroom
enzyme in a dose-dependent manner with 18% sciarid, Lycoriella mali was conducted. The results
inhibition of the enzyme at a concentration of 0.5 indicated that the monoterpene linalool (LD50 value:
mg/mL, while the inhibition by 1,8-cineole, α-pinene 21.15 µg/mL) exhibited the highest toxicity [53].
and β-pinene was higher than 50% at the same Oxygenated monoterpenes (e.g. linalool), were also
concentration [48]. toxic to the rice weevil, Sitophilus oryzae [60].

6. The fumigant and insect repellent properties of Several monoterpenes (e.g. carvacrol, linalool,
linalool eugenol, thymol, cinnamaldehyde, α-pinene,
camphor) when tested against Acanthoscelides
There is growing evidence that many biological
obtectus (bean weevil) showed that linalool (log IC50
pesticides can adversely affect the environment and
value: 0.5 mg/L) was the most toxic of all the
the identification of safer means of pest management
compounds investigated [61]. Linalool was found to
has become crucial. Therefore, the use of safe, low
be highly effective and produced 100% mortality of
toxicity botanical pesticides is now emerging as one
Rhyzopertha dominica (lesser grain borer) and 85%
of the prime means to protect crops, their products
mortality on the rice weevil (Sitophilus oryzae) after
and the environment from pesticide pollution.
1188 Natural Product Communications Vol. 3 (7) 2008 Kamatou and Viljoen

24 h exposure at a concentration of 0.1 µl/720 mL enhance the permeability of a number of drugs

[62]. Furthermore, studies demonstrated the toxicity through biological tissues like skin or mucus
of linalool towards Tribolium castaneum (rust-red membranes [70-72].
flour beetle) and the saw-toothed grain beetle
(Oryzaephilus surinamensis) in a dose-dependent 8. Toxicity, irritancy and allergenicity of linalool
manner [63].
In vitro studies have shown that linalool exhibited
negligible toxicity against the kidney epithelial cells
Repellent effects of several pure compounds against
(Graham cells) (IC50 value: 128.5 µM) [4]. An
the false powder post beetle (Dinoderus bifloveatus)
investigation was conducted to assess the general
were investigated and further experiments were
toxicity of linalool in an immuno-toxicity assay
carried out to isolate the toxic principles from the
[73,74], no toxic effects were recorded when female
combined compounds. Linalool was one of the most
mice were given 94, 188 or 375 mg/kg of linalool for
toxic compounds to D. bifloveatus, resulting in mean
five days. A combination of linalool and citronellol
mortality values > 50% within 24 h. Increasing the
(1:1) added to the diet of rats showed a slight
exposure period to 48 h led to higher mortality,
retardation of growth (only in males) after 90 days
particularly for less toxic compounds. The direct
and the measurements of haematology, clinical
contact of linalool was largely responsible for the
chemistry and urinalysis showed no significant
toxicity of this compound against D. bifloveatus [64].
differences between the test and the control groups.
In another study, five monoterpenoids (terpinen-4-ol,
The conclusion drawn from the study was that the
1,8-cineole, linalool, R-(+)-limonene and geraniol)
retardation of the growth in the male mice was
were tested in vapour form against different stages of
biologically insignificant [75].
the confused flour beetle, Tribolium confusum (eggs,
larvae and adults) [65]. Linalool (LC50 values ranging
Linalool was evaluated for skin irritation in humans
between 8.6 and 183.5 mL/L air [65] was among the
(approximately 380 male and female volunteers). No
most toxic to all the stages tested.
irritation was observed with the application of 20%
linalool, however, mild irritation was observed with
7. Percutaneous absorption and penetration
32% linalool [76,77]. Studies have shown that,
enhancement of linalool
undiluted linalool was severely irritating to rabbits
Lavender oil was used to measure the transdermal and slightly irritating to guinea pigs [40]. Linalool is,
absorption of its main components (linalool: 24.8% at most, a moderate eye irritant and does not cause
and linalyl acetate: 29.6%) in a male subject. any eye irritation at 320 ppm to approximately a third
Lavender oil (1500 mg) was softly massaged for 10 of human trial participants [2]. Therefore, linalool
min into a 376 cm2 area on the abdomen of a male should be seen as only mildly irritant to man [2].
volunteer and the blood samples were drawn at Various oral dosages of linalool (0, 250, 500 and
regular time intervals over a period of 90 min. The 1000 mg/kg/day) were administered to pregnant rats
results indicated that linalool was absorbed quickly [78]. The results showed no maternal deaths, clinical
and trace amounts of linalool could be detected in the signs or lesions as a result of linalool intake and it
blood 5 min after the massage had been completed could be concluded that linalool exhibits no
[66]. However, most of the linalool disappears from developmental toxicant effects in pregnant rats [78].
the blood in 90 min [67]. The concentration of
linalool, one of the main constituents of this oil, was Studies were carried out in order to determine
found to be about 130 ng/mL of plasma 20 min. after whether the use of linalool has sensitization effects,
completion of the massage [68]. using the lymph node assay [79]. The results
indicated that linalool was not a protein-reactive
The effect of linalool as a skin-penetration enhancing compound, suggesting low sensitization potency of
agent in excised guinea pig skin was evaluated by linalool [79]. In another sensitization study on guinea
assessing the depth to which Rhodamine B (active pigs [80], linalool of high purity produced no adverse
principle) penetrated the skin in the presence of 50% reactions, while linalool that had been oxidized for a
linalool. After 2 h, Rhodamine B was not detected in long period (10 weeks) sensitized the animals. Based
the epithelium and hair follicles and the conclusion on in vivo studies on mousse and rats, linalool
drawn from the study was that linalool did not presents low acute toxicity, orally and through the
enhance skin penetration [69]. However, other skin [2].
studies have demonstrated that linalool could
Linalool: A Review Natural Product Communications Vol. 3 (7) 2008 1189

Clinical studies have demonstrated that linalool and enantiomeric forms. A solid body of evidence has
specifically its oxidation products may be potential been generated to corroborate the various biological
allergens [81]. For this reason the European Union properties of linalool with the in vitro and in vivo
legislation requires a labeling obligation for any results, with the proof of CNS effects providing most
product containing linalool at certain concentrations. promising potential for treatment of disorders. The
repellent properties of linalool together with
9. Concluding comments negligible toxicity and low tendency to
bioaccumulation, justifies further research to
Due to the abundance of linalool in nature and its
investigate the feasibility of linalool as a
occurrence as a major constituent in plants with an
phytobiocide. Despite the positive results obtained in
established history of use (e.g. lavender), this
the various assays, the mechanism of action by which
monoterpene alcohol has been extensively studied.
linalool (and essential oils in general) exert their
Although it is the tendency to ascribe the biological
specific action remains poorly explored and may
activity of a complex mixture (such as an essential
prove to be a rewarding challenge to future
oil) to the main constituents this should be done with
researchers in this field of study.
caution, as the role of minor constituents and the
possible synergistic interaction between molecules
Acknowledgements - We appreciate the financial
cannot be ignored. Several studies have however
support from Tshwane University of Technology and
confirmed the activity of linalool specifically and
the National Research Foundation (South Africa) and
future investigations should explore the possible
Dr Gill Enslin is thanked for editing the manuscript.
effect of stereochemistry, as linalool exists in two

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