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Gentian

Scientific Name(s): Gentiana lutea L. Stemless gentian is derived from Gentiana acaulis L. Family: Gentianaceae

Common Name(s): Gentian , stemless gentian , yellow gentian , bitter root , bitterwort , pale gentian , gall weed

Clinical Overview

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Uses of Gentian

In traditional medicine, gentian is used in bitters to stimulate appetite, improve digestion, and treat GI complaints. It also has been used to treat wounds, sore throat, arthritic inflammation, and jaundice.

Gentian Dosing

Gentian root has been used as a bitter digestive tonic in doses from 1 to 4 g/day. However, there are no clinical studies substantiating this dose recommendation.

Contraindications

Contraindicated in gastric ulcer because of stimulant effect on gastric secretion.

Pregnancy/Lactation

May not be well tolerated by women who are pregnant. Documented adverse effects. Avoid use.

Gentian Interactions

None well documented.

Gentian Adverse Reactions

The extract may cause gastric irritation, resulting in nausea and vomiting.

Toxicology

Acute veratrum alkaloid poisoning has been reported in persons who prepared homemade gentian wine that had been accidentally contaminated by veratrum.

Botany

Native to the mountains of central and southern Europe, G. lutea is a perennial herb with erect stems and smooth, oval leaves, which grows to 1.8 m in height. The plant produces a cluster of fragrant orange-yellow flowers. The roots and rhizomes are nearly cylindrical, sometimes branched, varying in thickness from 5 to 40 mm. The root and rhizome portions are longitudinally wrinkled. The color of the rhizomes, ranging from dark brown to light tan, appears to be related to the content of bitter principles, because the darker roots have a more persistent, bitter taste. 1 The roots and rhizomes of G. lutea are the parts used medicinally.

G. acaulis is a smaller herb with a basal rosette of lance-shaped leaves and generally grows to only 10 cm in height. It is native to the European Alps at 914 to 1,524 m above sea level. The entire G. acaulis plant is used medicinally. Numerous species of Gentian native to China are used in Chinese traditional medicine.

History

The gentians have been used for centuries as bitters to stimulate the appetite, improve digestion, and treat a variety of GI complaints (eg, heartburn, vomiting, stomach ache, diarrhea). 2 , 3 Both gentian and stemless gentian generally are recognized as safe by the FDA for food use. Stemless gentian usually is consumed as a tea or alcoholic extract such as Angostura bitters. The extracts are used in a variety of foods, cosmetics, and some antismoking products. The plant has been used externally to treat wounds and internally to treat sore throat, arthritic inflammation, and jaundice.

Chemistry

The most characteristic aspect of gentian is its bitter taste. This is imparted by a number of bitter iridoid glycosides, primarily amarogentin, gentiopicrin (about 1.5% in fresh roots), gentiopicroside, and swertiamarin. 4 Amarogentin is one of the most bitter compounds known. The speed of drying of the roots affects their properties as a medicinal bitter. Slow drying permits enzymatic hydrolysis of gentiopicrin into gentiogenin and glucose, thus reducing the bitter nature of the product. 5 Gentian extract is used in concentrations of about 0.02% in nonalcoholic beverages. The iridoids have been analyzed by thin-layer chromatography 6 micellar electrokinetic capillary chromatography, 7 and by high-performance liquid chromatography mass spectrometry. 8

In addition to iridoids, the plant contains xanthones 9 and triterpenes. 10 , 11 The reported pyridine alkaloids gentianine and gentialutine are thought to be artifacts of basic extraction derived from the iridoids. Stemless gentian also contains the xanthone glycoside gentiacauloside. The flowers and leaves of G. lutea contain iridoids, flavonoids, and xanthones. 12 The dye, gentian violet, is not derived from this plant.



Gentian Uses and Pharmacology

The pharmacokinetics and tissue distribution of gentiopicroside after oral and parenteral administration have been studied in mice. 13 It was rapidly absorbed with low bioavailability and rapidly cleared.

Appetite stimulant

Bitter substances ingested before meals are reputed to improve the appetite and aid digestion by stimulating the flow of gastric juices and bile. However, because gentian is most often consumed in an alcoholic beverage, it is difficult to distinguish the effects of gentian from those of alcohol.

Animal/Clinical data

Research reveals no animal or clinical data regarding the use of gentian for stimulation of appetite.

Anti-inflammatory

Gentianine has been shown to exert a measurable anti-inflammatory effect in animals. Extracts of G. lutea were active in carageenan-induced rat paw edema, xylol-induced mouse ear edema, and cotton-pellet granulatoma models. In addition, the extracts were active in several wound-healing models. 14

Other uses

Gentiopicroside relaxes smooth muscle, 15 promotes bile secretion, and protects the liver against chemical insults. 16 Amarogentin and 2 other iridoids inhibited topoisomerase I of Leishmania. 17 Isogentisin and several other compounds from gentian inhibited monoamine oxidase. 18 , 19 Gentian extracts have been shown to have hydroxy radical scavenging activity, 20 and to prolong swimming endurance in mice. 21

Dosage

Gentian root has been used as a bitter digestive tonic in doses of 1 to 4 g/day. There are no clinical studies to substantiate this dose recommendation.

Pregnancy/Lactation

The extract may cause gastric irritation and may not be tolerated by pregnant women. Documented adverse effects. Avoid use.

Interactions

None well documented.

Adverse Reactions

Although the extract usually is taken in very small doses that do not appear to cause adverse effects, it has been suggested that gentian may not be well tolerated by people with hypertension or by women who are pregnant. The extract may cause gastric irritation, resulting in nausea and vomiting.

Toxicology

The highly toxic white hellebore ( Veratrum album L.) often grows in close proximity to gentian. At least 5 cases of acute veratrum alkaloid poisoning have been reported in people who prepared homemade gentian wine that had been accidentally contaminated by veratrum. 22

Bibliography

1. Meyer JE. The Herbalist . Hammond, IN: Hammond Book Co.; 1934.
2. Leung AY. Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics . New York, NY: John Wiley and Sons; 1980.
3. DerMarderosian A, Liberti L. Natural Product Medicine . Philadelphia, PA: G.F. Stickley Co.; 1988.
4. Bricout J. Identification and determination of the bitter constituents of Gentiana lutea roots [in French]. Phytochemistry . 1974;13:2819-2823.
5. Tyler VE, Brady LR, Robbers, JE. Pharmacognosy . 9th ed. Philadelphia, PA: Lea & Febiger; 1988.
6. VanHaelen M, Vanhaelen-Fastre R. Quantitative determination of biologically active constituents in medicinal plant crude extracts by thin-layer chromatography-densitometry. I. Aesculus hippocastaneum L., Arctostaphylos uva-ursi Spreng., Fraxinus excelsior L., Gentiana lutea L., Glyccyrhiza glabra L., Hamamelis virginiana L., Hypericum perforatum L., Olea europea L., Salix alba L., and Silybum marianum Gaertn. J Chromatogr . 1983;281:263-271.
7. Glatz Z, Pospisilova J, Musil P. Determination of gentiopicroside in extracts of Centaurium erythreae and Gentiana lutea by micellar electrokinetic capillary chromatography. J Liq Chromatogr Relat Technol . 2000;23:1831-1839.
8. Szucs Z, Danos B, Nyiredy S. Comparative analysis of the underground parts of Gentiana species by HPLC with diode-array and mass spectrometric detection. Chromatographia . 2002;56:S19-S23.
9. Hayashi T, Yamagishi T. Two xanthone glycosides from Gentiana lutea . Phytochemistry . 1988;27:3696-3699.
10. Toriumi Y, Kakuda R, Kikuchi M, Yaoita Y, Kikuchi M. New triterpenoids from Gentiana lutea . Chem Pharm Bull . 2003;51:89-91.
11. Kakuda R, Machida K, Yaoita Y, Kikuchi M, Kikuchi M. Studies on the constituents of Gentiana species. II. A new triterpenoid, and (S)-(+)- and (R)-(-)-gentiolactones from Gentiana lutea . Chem Pharm Bull . 2003;51:885-887.
12. Menkovic N, Savikin-Fodulovic, Savin K. Chemical composition and seasonal variations in the amount of secondary compounds in Gentiana lutea leaves and flowers. Planta Med . 2000;66:178-180.
13. Wang CH, Wang ZT, Bligh SW, White KN, White CJ. Pharmacokinetics and tissue distribution of gentiopicroside following oral and intravenous administration in mice. Eur J Drug Metab Pharmacokinet . 2004;29:199-203.
14. Mathew A, Taranalli AD, Torgal SS. Evaluation of anti-inflammatory and wound healing activity of Gentiana lutea rhizome extract in animals. Pharm Biol . 2004;42:8-12.
15. Rojas A, Bah M, Rojas JI, Gutiérrez DM. Smooth muscle relaxing activity of gentiopicroside isolated from Gentiana spathacea . Planta Med . 2000;66:765-767.
16. Liu ZW, Chen C, Jin R, Shi G, Song C, Hu Z. Studies on liver-protecting and bile secretion-promoting effects of gentiopicroside. Zhong Cao Yao . 2002;33:47-50.
17. Ray S, Majumder, Chakravarty AK, Mukhopadhyay S. Amarogentin, a naturally occurring secoiridoid glycoside and a newly recognized inhibitor of topoisomerase I from Leishmania donovani . J Nat Prod . 1996;59:27-29.
18. Suzuki O, Katsumata Y, Oya M. Inhibition of monoamine oxidase by isogentisin and its 3-O-glucoside. Biochem Pharmacol . 1978;27:2075-2078.
19. Haraguchi H, Tanaka Y, Kabbash A, Fujioka T, Ishizu T, Yagi A. Monoamine oxidase inhibitors from Gentiana lutea . Phytochemistry . 2004;65:2255-2260.
20. Calliste CA, Trouillas P, Allais DP, Simon A, Duroux JL. Free radical scavenging activities measured by electron spin resonance spectroscopy and B16 cell antiproliferative behaviors of seven plants. J Agric Food Chem . 2001;49:3321-3327.
21. Öztürk N, Baser KH, Aydin S, Öztürk Y, Calis I. Effects of Gentiana lutea ssp. symphyandra on the central nervous system in mice. Phytother Res . 2002;16:627-631.
22. Garnier R, Carlier P, Hoffelt J, Savidan A. Acute dietary poisoning by white hellebore ( Veratrum album L.). Clinical and analytical data. A propos of 5 cases [in French]. Ann Med Interne (Paris) . 1985;136:125-128.



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