Gaultheria / Bergthee / Wintergreen

Boxberry, Canada Tea, Checkerberry, Deerberry, Essence de Gaulthérie, Gaulteria, Gaultheria Oil, Gaulthérie Couchée, Ground Berry, Hilberry, Huile de Thé des Bois, Mountain Tea, Oil of Wintergreen, Partridge Berry, Petit Thé, Petit Thé des Bois, Spiceberry, Teaberry, Thé de Montagne, Thé de Terre-Neuve, Thé des Bois, Thé du Canada, Thé Rouge, Wax Cluster.

Scientific Name:
Gaultheria procumbens.
Family: Ericaceae.

Orally, wintergreen leaf is used for headache, stomachache, flatulence, fever, kidney disorders, asthma, neuralgia (particularly sciatica), pleurisy, ovarian pain, inflammation of the epididymis, inflammation of the diaphragm, gout, arthritis, and dysmenorrhea. Small doses of wintergreen oil have been used to stimulate gastric secretion and aid digestion.
Topically, wintergreen leaf is used as a wash for rheumatism, sore muscles, and lumbago. Wintergreen oil is used topically as a counterirritant, for musculoskeletal pain, and as an antiseptic.
In manufacturing, wintergreen is used as a flavoring agent in food, candies, teas, and in pharmaceutical products.

Wintergreen / Gaultheria procumbens
Family: Ericaceae

Wintergreen is a perennial that grows to 5 or 6 inches with white drooping flowers in June and July followed by bright red berries.1,2  Native to the eastern portion of North America, wintergreen is found from Canada, Newfoundland, and Minnesota to Georgia and Alabama.2,3  The oil is extracted from the leaves, but the berries and remaining portions of the plant are used as well.4  

History and Cultural Significance
Oil of wintergreen contains methyl salicylate which has anti-inflammatory properties and is closely related to the well-known medication aspirin.5  Wintergreen and the oil of wintergreen are used in topical pain relievers and products that produce a feeling of warmth for muscle and rheumatic pain relief.4,6  Oil of wintergreen has also been used for the treatment of cellulitis, a bacterial infection accompanied by inflammation of the skin.5  In the past, wintergreen was used internally to treat chronic mucous discharges, regulate hormones, and as a diuretic; due to its toxicity it is no longer used internally for medicinal purposes.1  Wintergreen is commonly used in very small amounts to adjust the flavor in candies, chewing gum, herbal teas, mouthwashes, toothpastes, and various beverages.2,4  It is also found in insect repellents and insecticidal products.2  

North American Indians chewed the leaves of the wintergreen plant for their distinct flavor, used them in the treatment of aches and pains, and to aid in breathing during hard work.3,5  French explorers used wintergreen leaves in hot infusions, thus leading to the term ‘Thé du Canada’, the tea of Canada.3  During the American war of independence, wintergreen leaves served as a replacement for Chinese tea.3  Folk remedies also used the wintergreen plant for body aches, cold symptoms, colic, headaches, inflammation, pain, skin diseases, sore throats, rheumatism, and tooth decay.2,4  

Modern Research
No current documented studies are available on the external or internal uses of wintergreen or wintergreen oil. However, methyl salicylate is tentatively is accepted by the U.S. Food and Drug Administration as an over-the-counter (OTC) external analgesic, and it is included in many OTC products intended to relieve mild muscle and joint pain. There are current studies on the active constituent of wintergreen, methyl salicylate, for use in topical creams in the treatment of pain relief, possible antimicrobial use in dental care, and the comparison of salicylate levels between the oil of wintergreen and synthetic methyl salicylate cream.7,8,9  

Future Outlook
Wintergreen oil production is on the decline due to the production of its replacement, synthetic methyl salicylate.10  Although the natural oil of wintergreen is available and in use by some manufacturers, it is very rare and most of what is labeled wintergreen oil on the market is actually synthetic methyl salicylate.11  

1  Grieve M. A Modern Herbal. Volume II. New York: Dover Publications, 1981.
2  Wintergreen. Purdue University Center for New Crops and Plant Products website. December 6, 1997. Available at: Accessed October 6, 2004.
3  Guenther E. The Essential Oils. Volume VI. Huntington, NY: Robert E. Krieger Publishing Company, 1952.
4  DerMarderosian A, Beutler JA (editors). The Review of Natural Products: The Most Complete Source of Natural Product Information. 3rd edition. St. Louis, Mo: Facts and Comparisons, 2002.
5  Plants for a Future: Database Search Results: Gaultheria procumbens. ibiblio website. Available at: Accessed October 6, 2004.
6  Williamson EM. Potter’s Herbal Cyclopaedia. Saffron Walden, UK: C.W. Daniel Company, 2003.
7  Lobo SL, Mehta N, Forgione AG, et al. Use of Theraflex-TMJ topical cream for the treatment of temporomandibular joint and muscle pain. Cranio. April 2004;22(2):137-144.
8  Charles CH, Vincent JW, Borycheski L, et al. Effect of an essential oil-containing dentifrice on dental plaque microbial composition. Am J Dent. September 2000;13:26C-30C.
9  Wolowich WR, Hadley CM, Kelley MT, Walson PD, and Casavant MJ. Plasma salicylate from methyl salicylate cream compared to oil of wintergreen. J Toxicol Clin Toxicol. 2003;41(4):355-358.
10  Arctander S. Perfume and Flavor Materials of Natural Origin. Carol Stream , IL: Allured Publishing Corporation, 1994.
11  Tisserand R, Balacs T. Essential Oil Safety: A Guide for Health Care Professionals. New York: Churchill Livingstone, 1995.

Molecules. 2011 May 9;16(5):3875-84. doi: 10.3390/molecules16053875.
Anti-inflammatory activity of methyl salicylate glycosides isolated from Gaultheria yunnanensis (Franch.) Rehder.
Zhang D1, Liu R, Sun L, Huang C, Wang C, Zhang DM, Zhang TT, Du GH.
Gaultheria yunnanensis (Franch.) Rehder is a kind of traditional Chinese herbal medicine used for the treatments of rheumatoid arthritis, swelling and pain. Two methyl salicylate glycosides, namely methyl benzoate-2-O-β-D-xylopyranosyl(1-6)-O-β-D-gluco-pyranoside (J12122) and methyl benzoate-2-O-β-D-xylopyranosyl(1-2)[O-β-D-xylopyranosyl(1-6)]-O-β-D-glucopyranoside (J12123), are natural salicylic derivatives isolated from Gaultheria yunnanensis. In this study, we investigated the anti-inflammatory activity of J12122 and J12123 on LPS-induced RAW264.7 macrophage cells by measuring the production of pro-inflammatory cytokines, accumulation of nitric oxide (NO), and level of reactive oxygen species (ROS). The results showed that both methyl salicylate glycosides dose-dependently inhibited the production of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6, respectively. Consistent with these observations, J12122 and J12123 significantly suppressed the accumulation of NO, with an inhibitory rate of 56.20% and 51.72% at 3.0 μg/mL concentration, respectively. Furthermore, the two methyl salicylate glycosides reduced the level of ROS induced by LPS. These results showed that the isolated compounds possess anti-inflammatory properties through inhibition the production pro-inflammatory cytokines, NO, and ROS.

Biol Pharm Bull. 2007 Mar;30(3):465-9.
Analgesic and anti-inflammatory activities of a fraction rich in gaultherin isolated from Gaultheria yunnanensis (FRANCH.) REHDER.
Zhang B1, Li JB, Zhang DM, Ding Y, Du GH.
The analgesic and anti-inflammatory activities of a salicylate derivatives fraction (SDF) isolated from Gaultheria yunnanensis (FRANCH.) REHDER and the mechanisms of actions were investigated in the present study. The major constituent of SDF, which represented around 50% of this fraction, was a methyl salicylate diglycoside named gaultherin. SDF showed a significant inhibition on the hind paw edema in rats (200, 400 mg/kg body wt., p.o.) and ear swelling in mice (200, 400, 800 mg/kg body wt., p.o.) caused by carrageenin and croton oil, respectively. In addition, SDF (400, 800 mg/kg body wt., p.o.) inhibited only the second phase (inflammatory) in the formalin test, and showed no effect in the hot-plate test in mice. The antinociceptive activity of SDF was predominantly peripheral and independent of the opioid system. These findings demonstrate that SDF from Gaultheria yunnanensis (FRANCH.) REHDER possesses analgesic and anti-inflammatory activities, which may be mediated, at least partly, through the suppression of inflammatory mediators or their release suggested by the animal experiment. The observed effects of SDF are probably due to the presence of high content of salicylate derivatives (80%), including gaultherin, MSTG-A and MSTG-B.

Front Plant Sci. 2014 Sep 23;5:477. doi: 10.3389/fpls.2014.00477. eCollection 2014.
Foliar treatments with Gaultheria procumbens essential oil induce defense responses and resistance against a fungal pathogen in Arabidopsis.
Vergnes S1, Ladouce N1, Fournier S1, Ferhout H2, Attia F3, Dumas B1.
Essential oil from Gaultheria procumbens is mainly composed of methylsalicylate (MeSA) (>96%), a compound which can be metabolized in plant tissues to salicylic acid, a phytohormone inducing plant immunity against microbial pathogens. The potential use of G. procumbens essential oil as a biocontrol agent was evaluated on the model plant Arabidopsis thaliana. Expression of a selection of defense genes was detected 1, 6, and 24 h after essential oil treatment (0.1 ml/L) using a high-throughput qPCR-based microfluidic technology. Control treatments included methyl jasmonate and a commercialized salicylic acid (SA) analog, benzo(1,2,3)-thiadiazole-7carbothiolic acid (BTH). Strong induction of defense markers known to be regulated by the SA pathway was observed after the treatment with G. procumbens essential oil. Treatment induced the accumulation of total SA in the wild-type Arabidopsis line Col-0 and analysis of the Arabidopsis line sid2, mutated in a SA biosynthetic gene, revealed that approximately 30% of MeSA sprayed on the leaves penetrated inside plant tissues and was demethylated by endogenous esterases. Induction of plant resistance by G. procumbens essential oil was tested following inoculation with a GFP-expressing strain of the Arabidopsis fungal pathogen Colletotrichum higginsianum. Fluorescence measurement of infected tissues revealed that treatments led to a strong reduction (60%) of pathogen development and that the efficacy of the G. procumbens essential oil was similar to the commercial product BION(®). Together, these results show that the G. procubens essential oil is a natural source of MeSA which can be formulated to develop new biocontrol products.

Polyphenolic Profile, Antioxidant and Anti-Inflammatory Activity of Eastern Teaberry (Gaultheria procumbens L.) Leaf Extracts
Piotr Michel 1,  Anna Dobrowolska 1,  Agnieszka Kicel 1,  Aleksandra Owczarek 1,  Agnieszka Bazylko 2, Sebastian Granica 2,  Jakub P. Piwowarski 2 and  Monika A. Olszewska 1,* 
1 Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszyńskiego St., Lodz 90-151, Poland
2 Department of Pharmacognosy and Molecular Basis of Phytotherapy, Faculty of Pharmacy, Warsaw Medical University, 1 Banacha St., Warsaw 02-097, Poland
Dry leaf extracts of eastern teaberry (Gaultheria procumbens L.) were evaluated as a source of bioactive phytocompounds through systematic activity testing and phytochemical profiling. The antioxidant efficiency was tested using five complementary in vitro models (DPPH; FRAP; linoleic acid (LA) peroxidation assay; O2•− and H2O2 scavenging tests) in parallel with standard antioxidants. The 75% methanol extract and its diethyl ether, ethyl acetate (EAF), n-butanol and water fractions exhibited the dose-dependent responses in all assays, with the highest capacities found for EAF (DPPH EC50 = 2.9 μg/mL; FRAP = 12.8 mmol Fe2+/g; IC50 for LA-peroxidation = 123.9 μg/mL; O2•− SC50 = 3.9 μg/mL; H2O2 SC50 = 7.2 μg/mL). The EAF had also the highest anti-inflammatory activity in the inhibition tests of lipoxygenase and hyaluronidase (60.14% and 21.83% effects, respectively, at the concentration of 100 μg/mL). Activity parameters of the extracts correlated strongly with the levels of total phenolics (72.4–270.7 mg GAE/g), procyanidins, and phenolic acids, whereas for flavonoids only moderate effects were observed. Comprehensive UHPLC-PDA-ESI-MS3 and HPLC-PDA studies led to the identification of 35 polyphenols with a procyanidin A-type trimer, quercetin 3-O-glucuronide, isomers of caffeoylquinic acids, and (‒)-epicatechin being the dominant components. Significant activity levels, high phenolic contents and high extraction yields (39.4%–42.5% DW for defatted and crude methanol extracts, respectively) indicate the value of eastern teaberry leaves as bioactive products.

 Gaultheria fragrantissima Wall of G. ovalifolia

Deze kleine heester wordt niet meer dan 20 cm hoog (bodembedekker). Hij bloeit tijdens de zomer (witte bloemen tijdens de maanden juni en juli) en produceert in het najaar rode ronde bessen, die lijken op kleine kersen. Doordat de heester zijn bladeren niet verliest en steeds groen blijft, wordt hij in het Engels ook wel 'Wintergreen' genoemd. Bij het kneuzen van de bladeren komt een heel kenmerkende geur vrij (methylsalicylaat).
Canada, Midden-Amerika, Azië, Nepal.
Gebruikte delen
De essentiële olie van de bladeren.
Aktieve bestanddelen
Essentiële olie (methylsalicylaat): ontstekingsremmende, krampstillende en pijnstillende werking.
De bladeren van de Gaultheria fragrantissima, die sterk naar kamfer ruiken, worden soms gebruikt om een kruideninfuus te bereiden. Het sap van de bladeren wordt gebruikt als hoestbehandeling. Het sap en de bladeren worden gebruikt als wormafdrijvend middel.
Ondanks hun sterke smaak kunnen de rijpe bessen gegeten worden. Erop kauwen helpt bij maagproblemen.

De essentiële olie verkregen uit de bladeren is antiseptisch, aromatisch, carminatief en stimulerend. De olie bevat methylsalicylaat, een natuurlijke voorloper van aspirine, en wordt gebruikt voor de topische behandeling van reumatische aandoeningen. 1-4 Door de aromatische geur wordt deze essentiële olie gebruikt als ingrediënt in snoepgoed, kruidenthee, tandpasta, parfum enz.

Bibliographic References
1 Involvement of transient receptor potential vanilloid subtype 1 in analgesic action of methylsalicylate.
Ohta T, Imagawa T, Ito S.
Mol Pharmacol. 2009 Feb;75(2):307-17.
Molecular Pharmacology:

2 Antiinflammatory and analgesic activity of topical administration of Siegesbeckia pubescens.
Wang J, Cai Y, Wu Y.
Pak J Pharm Sci. 2008 Apr;21(2):89-91.

3Anti-inflammatory and analgesic activity of the topical preparation of Verbena officinalis L.
Calvo MI.
J Ethnopharmacol. 2006 Oct 11;107(3):380-2.

4Self promotion of deep tissue penetration and distribution of methylsalicylate after topical application.
Cross SE, Megwa SA, Benson HA, Roberts MS.
Pharm Res. 1999 Mar;16(3):427-33.

De gezondheidsclaims voor planten die in onze producten voorkomen, staan op een lijst van gezondheidsclaims in afwachting van een definitief standpunt van Brussel (cf. website van de Europese Commissie: Ten gevolge van hun behandeling door de nationale overheden, kunnen hierin wijzigingen optreden.
De gezondheidsclaims van andere voedingsmiddelen of bestanddelen in onze producten zijn conform aan het Reglement N° 432/2012 van de Commissie van 16 mei 2012, die een lijst opmaakt van de toegelaten gezondheidsclaims ivm voedingsmiddelen, die niet verwijzen naar de vermindering van ziekterisico’s, de ontwikkeling van ziektes en de gezondheid van kinderen (cf. website van de Europese Commissie:

Gebruik van wintergreen etherische olie:
  • Bij onzuivere huid: 2 tot 4 druppels Wintergreen in een glas gekookt, afgekoeld water en hiermee de huid deppen of afspoelen
  • Bij reumatische klachten en spierpijn; 15 tot 20 druppels Wintergreen mengen met een eetlepel plantaardige olie en hiermee de pijnlijke plaatsen masseren. Eventueel nog een paar druppels pepermunt etherische olie toevoegen om de werking van Wintergreen te versterken.
  • Ook kan je een badzout maken van 2 eetlepels badzout en 10 druppels Wintergreen en 5 druppels pepermunt etherische olie. Wel oppassen, uittesten voor allergische reactie.
  • Verdampen: 8 druppels Wintergreen in de aromalamp zorgen voor een frisse atmosfeer en activeren de geest.