HERBAL
MEDICINAL
PLANT
----------------------------------------
GENTIAN
Gentiana lutea L., Gentiana acaulis L. ++ (Gentianaceae)
by
RETTODWIKART THENU
GENTIAN
(jehn’shuhn)
Gentiana lutea L.,
Gentiana acaulis L.
++
SUMMARY
AND PHARMACEUTICAL COMMENT
The
major constituents of pharmacological importance in gentian are the bitter principles;
limited information is available on the other compounds present. The herbal
uses of gentian are supported by the known properties of the bitter principles
present in the root. Excessive doses should be avoided in view of the lack of
toxicity data.
DESCRIPTION
Medicinal Parts:
The
medicinal parts of the plant are the dried or fresh underground plant organs.
Flower and
Fruit: The
flowers are yellow, terminal, pedicled and axillary in cyme-like false whorls.
The calyx is deeply divided in 2. The corolla is rotate and divided almost to
the base into 5 or 6 lanceolate tips. There are 5 stamens with 8 mm long
anthers and 1 superior ovary. The fruit is 6 cm long and capsule shaped. The
numerous seeds are flat, oblong or round, with a membranous edge.
Leaves, Stem and
Root: Yellow
Gentian is a completely glabrous perennial plant that grows to 140 cm high. The
rhizome has a number of heads, and the top of the rhizome can attain the
thickness of an arm. The main root is a taproot, which grows up to 1 m long.
The stem is round, unbranched, hollow and grooved in the upper region to finger
thickness. The leaves are elliptical, bluish-green, have strongly curved ribs
and grow up to 30 cm long and 15 cm wide.
Characteristics:
The
drug has a weak, sweetish odor. It tastes metallic/sweet at first, then bitter.
Habitat: The plant is
indigenous to the mountainous regions of central and southern European, and
cultivated in many other regions.
Production: The roots are
collected from spring through October, cleaned and swiftly dried. Extended,
slower drying causes the roots to ferment. The roots become brittle through drying,
swollen and spongy through contact with moisture.
Not to be
Confused With: The
roots of Rumex alpinus or Gentiana asclepiadea
Other Names: Bitter Root.
Bitterwort, Gentian Root, Pale Gentian
Figure 1. Gentian
SPECIES
(FAMILY)
Gentiana lutea L.
(Gentianaceae)
SYNONYM(S)
Bitterwort, Bitter Root, Gentiana, Yellow Gentian
PART(S)
USED
Rhizome, root
PHARMACOPOEIAL
AND OTHER MONOGRAPHS
BHC 1992(G6)
BHP 1996(G9)
BP 2007(G84)
Complete German Commission E(G3)
ESCOP 2003(G76)
Martindale 35th edition(G85)
Ph Eur 2007(G81)
LEGAL
CATEGORY (LICENSED PRODUCTS)
GSL(G37)
CHEMICAL
COMPONENTS/CONSTITUENTS
The
following is compiled from several sources, including General References G2, G6
and G62.
Alkaloids Pyridine-type.
Gentianine 0.6–0.8%, gentialutine.
Bitters Major
component is secoiridoid glycoside gentiopicroside (also known as gentiamarin
and gentiopicrin) 2%, with lesser amounts of amarogentin (0.01–0.04%) and
swertiamarine.(1) Gentianose (a trisaccharide bitter principle). The glycosides
amaropanin and amaroswerin are reported to be present in the related species Gentiana
pannonica, Gentiana punctata and Gentiana purpurea, but are absent from Gentiana
lutea.
Xanthones Gentisein,
gentisin (gentianin), isogentisin and 1,3,7- trimethoxyxanthone.
Other constituents Carbohydrates (e.g.
gentiobiose, sucrose and other common sugars), pectin, tannin (unspecified), triterpenes
(e.g. b-amyrin, lupeol) and volatile oil (trace).
Secoiridoid
bitter glycosides, oligosaccharides, phenolic acids, phytosterols,
polysaccharides (inulin and pectin), tannin, lupeol, beta-amyrin triterpenes, xanthones
and essential oil. Analysis of several commercially available G. lutea samples
showed that gentiopicroside is the most prevalent bioactive compound (4.46–9.53%),
followed by loganic acid (0.10–0.76%), swertiamarin (0.21–0.45%) and the xanthone
glycosides. Gentisin and isogentisin were found in much lower concentrations
between 0.02 and 0.11%, respectively (Aberham et al 2007).
USES
Gentian has been used to stimulate the appetite and to
treat digestive disorders such as colitis, irritable bowel syndrome, colic,
gallstones, biliary pain, peptic ulcer, and heartburn. It is also used as a component
in alcoholic beverages (bitters).
Figure 2. Dried Gentian dan Tea Gentian
Figure 3. Dried Rhizoma Gentian
FOOD USE
Gentian
(root, herbs and preparations) is listed by the Council of Europe as a natural
source of food flavouring (category N4, with limits on xanthones) (see Appendix
3, Table 1).(G17) Previously, in the USA, gentian has been approved for food
use.(G41)
HERBAL USE
Gentian
is stated to possess bitter, gastric stimulant, sialogogue and cholagogue
properties. Traditionally, it has been used for anorexia, atonic dyspepsia,
gastrointestinal atony, and specifically for dyspepsia with anorexia. The
German Commission E approved use for digestive disorders such as loss of
appetite, fullness and flatulence.(G3) Gentian is used in combination with angelica
root and caraway fruit or with ginger and wormwood for loss of appetite and
peptic discomfort.(G3)
ACTIONS
Very little primary research is available for gentian.
It is typically used to stimulate the appetite and is usually mixed in
alcoholic products. However, no studies support this use. Several of the
chemical components, gentiopicroside, sweroside, and swertiamerine;
secoiridoids are responsible for the wound-healing properties of gentian (Ozturk
et al, 2006).
ACTIVITIES
Analgesic
(1; HHB); Antiemetic (1, BGB); Antiinflammatory (1; APA; CAN; PED); Antipyretic
(1; CRC; HHB); Antiseptic (f; CRC); Aperitif (1; CRC; PNC); Astringent (1;
APA); Bitter (2; KOM; PNC); Carminative (f; PH2); Cholagogue (1; CAN; PH2);
Choleretic (1; AOA; PNC); CNS Stimulant (1; HHB); Depurative (f; CRC);
Digestive (1; APA; CRC; SKY); Emmenagogue (f; CRC); Fungistat (1; PH2);
Gastrostimulant (1; CAN); Insecticide (1; CRC); Mutagenic (1; APA; CAN);
Roborant (2; KOM); Secretagogue (2; KOM; PIP); Sialagogue (2; APA; CAN; KOM;
PH2); Stimulant (f; CRC); Stomachic (f; CRC; HHB); Tonic (2; CRC; KOM; PIP);
Vermifuge (f; CRC; HHB; MAD).
INDICATIONS
Achlorhydria
(1; BGB; MAD); Anemia (f; MAD); Anorexia (2; APA; CAN; KOM; PH2; PNC);
Arthrosis (1; HHB; PED); Bite (f; CRC); Bronchosis (f; JAD); Atony (f; BGB);
Cancer (f; CRC); Cancer, liver (f; JLH); Cancer, spleen (f; JLH); Carcinoma (f;
CRC; JLH); Cardiopathy (f; MAD); Chlorosis (f; MAD); Cholecystosis (f; HHB);
Cold (f; CRC); Convulsion (f; CRC); Debility (f; CRC); Diarrhea (f; APA; CRC;
PNC); Dysmenorrhea (f; CRC); Dyspepsia (2; APA; CAN; KOM; PH2); Dysuria (f;
CRC); Edema (1; HHB); Enterosis (1; APA; HHB); Fever (1; CRC; HHB; MAD); Gas
(2; APA; KOM; PHR; PH2); Gastrosis (1; HHB; KOM; PED); Gastroenterosis (1; APA;
CAN); Gout (f; CRC; MAD); Headache (f; MAD); Heartburn (1; APA; PNC); Hepatosis
(f; CRC; JLH); Herpes (f; CRC); Hyperemia (f; HHB); Hysteria (f; MAD);
Induration (f; CRC); Inflammation (1; APA; CAN; PED); Jaundice (f; APA; CRC;
PED); Malaria (f; CRC; HHB); Nausea (f; PNC); Neurosis (f; MAD); Nicotinism (f;
APA; CRC); Pain (1; HHB); Rheumatism (f; MAD); Snakebite (f; CRC); Sore (f;
JLH); Sore Throat (f; APA; PED); Splenosis (f; CRC; JLH); Stomachache (1; CRC; PED);
Syncope (f; CRC); Typhus (1; HHB); Ulcer (1; APA; JLH); Vomiting (1, BGB); Worm
(f; CRC; HHB; MAD); Wound (1; APA).
PRODUCT
AVAILABILITY
Fluid extract, infusion, root,
tea, tincture
Plant
Parts Used: Rhizome, roots
DOSAGES
DOSAGE
·
Adult PO fl uid extract: 2-4 g
daily (Blumenthal, 1998)
·
Adult PO infusion: no dosage
consensus
·
Adult PO root: 2-4 g daily
(Blumenthal, 1998)
·
Adult PO tea: Place 1⁄2 tsp in
4 oz water, boil and strain, take tid before meals
·
Adult PO tincture: 1-3 g daily
(Blumenthal, 1998); 2 ml tid (1:5 dilution) (Mills, Bone, 2000)
DOSAGE
Dosages
for oral administration (adults) for traditional uses recommended in standard
herbal reference texts are given below.
·
Dried rhizome/root 0.6–2 g as an infusion or decoction three times
daily.(G6)
·
Tincture 1–4mL (1 : 5 in 45% alcohol) three times daily.(G6)
DOSAGE
General guide
·
Cut
root or dried extract: 2–4 g/day.
·
Fluid
extract (1:1): 1–2 mL taken 1 hour before meals up to three times daily.
·
Tincture
(1:5): 3–12 mL/day.
·
Infusion:
1–2 g in 150 mL boiled water taken 1 hour before meals and up to three times
daily.
DOSAGE
·
0.5–1 tsp fresh root (PED); 0.25–0.5 g dry root (PED); 0.5 g dry
root:3 ml alcohol/2 ml water (PED); 0.6–2 g root, or in tea, 3 ×/day (CAN);
0.3–2 g root/day (HHB); 2–4 g root/day (KOM; PIP); 0.5–2 g powdered root (PNC);
1 tsp powdered root/3 cups water, take 1 tbsp 30 minutes before meals (APA);
·
1 g herb/cup water, or 1–4 ml tincture 3 ×/day (PH2); 1–3 g root
tincture/day (KOM; PIP); 20–40 drops tincture (APA); 10 drops tincture 2–3 ×/day
(MAD); up to 20 drops tincture before meals (SKY);
·
2–5 ml tincture (PNC); 1–4 ml herbal tincture (1:5 in 45%
ethanol) 3 ×/day (CAN); 0.5–4 g extract/day (APA); 2–4 g fluid extract (KOM;
PIP); 1.5–4 ml herb infusion (PNC).
DOSAGE
Mode of
Administration: Comminuted
drug and dried extracts for infusions and teas. Forms of commercial pharmaceutical
preparations include digestives, drops and coated tablets.
Preparation: Tea is prepared
by pouring boiling water over 1/2 teaspoon of the drug (1 to 2 g) and allowing
it to steep for 5 to 10 minutes. The tea may be sweetened with honey to alleviate
the bitter taste. Decoctions are made using 1 g of the drug to 1 cup boiled
water.
Daily Dosage: The average single
dose is 1 g of the drug; daily dose is 2 to 4 g. The average daily dose of
tincture is 1 to 4 ml 3 times daily. Liquid extract: 2 to 4 g; root: 2 to 4 g. A
one-cup dose of cold or lukewarm tea is taken several times a day, including
1/2 hour before meals.
Homeopathic
Dosage: 5 drops,
1 tablet or 10 globules every 30 to 60 minutes (acute) or 1 to 3 times daily
(chronic); parenterally: 1 to 2 ml sc acute, 3 times, daily: chronic: once a
day (HAB1)
Storage: The drug must be
stored away from light sources.
PHARMACOLOGICAL
ACTIONS
IN VITRO AND ANIMAL STUDIES
The
pharmacological activites of gentian root have been reviewed.(G52) A summary of
this information is provided below. Root extracts have antifungal activity, and
are reported to stimulate phagocytic activity of human lymphocytes, indicating immunostimulant
activity.(G52) Choleretic properties have been documented for gentian,(G41) and
gentianine has been reported to possess anti-inflammatory activity.(G22) The
bitter principles stimulate secretion of gastric juices and bile, thus aiding
appetite and digestion. Elevation of gastric secretion by up to 30% has been
reported following the administration of gentian tincture to dogs. An infusion
given orally to sheep as a single daily dose (5 g) stimulated enzyme secretion
in the small intestine. A root extract (12 mg/kg/day) applied by gavage to rats
for three days elevated bronchosecretion. A standardised extract perfused into
the stomachs of anaesthetised rats increased gastric secretion in a dose-dependent
manner. Lower doses caused no changes in gastric pH, whereas higher doses
increased pH from 4.25 to 4.85. A dose of 0.5 mL/kg did not affect the
incidence of gastric ulceration in rats.
CLINICAL STUDIES
There
is a lack of clinical research assessing the effects of gentian and rigorous
randomised controlled clinical trials are required. In an open, uncontrolled
study, a single dose of an alcoholic extract of gentian (equivalent to 0.2 g),
given to 10 healthy volunteers, was reported to result in a stimulation of
gastric juice secretion.(2) Gall-bladder emptying was increased and prolonged whilst
protein and fat digestion was enhanced. Nineteen patients with inflammatory conditions
of the gastrointestinal tract (colitis, Crohn's disease, non-specific inflammation)
and elevated secretory immunoglobulin A (IgA) concentrations and eight healthy individuals
were treated with gentian tincture (3 _ 20 drops/day) for eight days.(G52) IgA
concentrations decreased in both groups.(G52) However, the methodological
limitations of these studies do not allow the observed effects to be attributed
to administration of gentian.
CONTRAINDICATIONS,
INTERACTIONS, AND SIDE EFFECTS,TOXICITY
Class
2d. Root contraindicated in acid stomach, gastrosis, heartburn, and duodenal
and gastric ulcers (AHP; KOM; SKY). May cause headache (KOM; PIP). Reportedly
contraindicated in hypertension (CAN). Gentian has documented mutagenic
activity and is reputed to affect the menstrual cycle, its use in pregnancy and
lactation is to be avoided (CAN). Mutagenic activity in the AMES test has been
documented for gentian with gentisin and isogentisin identified as mutagenic
components. Gentian root is reported to contain 1000 ppm total mutagenic
compounds, of which 760 were gentisin and isogentisin (CAN). Blumenthal et al.,
(1998) caution re dandelion, but not gentian, that, “As with all drugs
containing bitter substances, discomfort due to gastric hyperacidity may occur”
(KOM). Do I need to write out this caveat for all the bitter herbs (Pedersen,
1998, classifies nearly half of his herbs as bitter)? Warning: may cause
hyperacidity and gastric distress. In general, bitter substances stimulate
gastric secretion.
CONTRAINDICATIONS
Pregnancy category is 3; breastfeeding category is 2A. Gentian
should not be given to children. It should not be used by persons with hypersensitivity
to this herb, those with stomach irritability or infl ammation, or those with
stomach or duodenal ulcers.
SIDE
EFFECTS/ADVERSE REACTIONS,TOXICITY
CNS: Headache
GI: Nausea, vomiting, anorexia
INTEG: Hypersensitivity reactions
INTERACTIONS
Drug
Antacids, H2-blockers,
proton pump inhibitors: Gentian
may decrease the action of these agents (theoretical) (Jellin et al, 2008).
Iron salts: Gentian may interfere with absorption of iron salts;
separate by at least 2 hours.
Extracts
of gentian are considered to be non-toxic, and are generally well-tolerated,(G52)
although clinical safety and toxicity data for gentian are limited and further
investigation of these aspects is required.
PRECLINICAL DATA
An
acute oral LD50 value in mice was reported to be 25 mL/kg of extract (37%
ethanol, bitterness value: 200 Swiss Pharmacopoeia units/g), and was the same
as that of 37% ethanol. Rabbits treated with gentian extract (12.6 mg/day for
three days) showed no toxic or abnormal concentration of serum parameters, with
the
exception
of slightly higher erythrocyte concentrations in treated animals. Gentian may
occasionally cause headache in some individuals.(G3) Mutagenic activity in the
Ames test (Salmonella typhimurium TA100 with S9 mix) has been documented for gentian,
with gentisin and isogentisin identified as mutagenic components.(3) Gentian root
100 g was reported to yield approximately 100 mg total mutagenic compounds, of
which gentisin and isogentisin comprised approximately 76 mg.(3)
CONTRA-INDICATIONS, WARNINGS
Gentian
is stated to be contra-indicated in individuals with high blood pressure,(G60) although
no rationale is given for this statement, and in individuals with hyperacidity,
gastric or duodenal ulcers.(G52,G3) Drug interactions None documented. However,
the potential for preparations of gentian to interact with other medicines administered
concurrently, particularly those with similar or opposing effects, should be
considered.
Pregnancy
and lactation Gentian is reputed to affect the menstrual cycle,(G22, G60) and it
has been stated that gentian should not be used in pregnancy.(G60) In view of
this and the documented mutagenic activity, gentian is best avoided in pregnancy
and lactation.
CLIENT
CONSIDERATIONS
Assess
·
Assess the reason the client is
using gentian.
·
Assess for hypersensitivity
reactions. If present, discontinue use of this herb and administer an
antihistamine or other appropriate therapy.
Administer
·
Instruct the client to store
gentian products in a cool, dry place, away from heat and moisture.
Teach
Client/Family
·
Inform the client that
pregnancy category is 3 and breastfeeding category is 2A.
·
Caution the client not to give
gentian to children.
PRACTICE
POINTS/PATIENT COUNSELLING
·
Gentian
root and its preparations are extremely bitter.
·
Gentian
preparations stimulate salivation, gastric juice and bile secretion.
·
They
are used to improve digestion, relieve flatulence and stimulate appetite.
·
Little
clinical investigation has been undertaken with the herb, so evidence of
efficacy relies on traditional and animal studies.
·
It
should not be used in cases of gastric or duodenal ulcer or hyperacidity.
PATIENTS’
FAQs
What will this
herb do for me?
Gentian preparations
stimulate taste buds when taken orally, and increase gastric juice secretion, thereby
improving digestion.
When will it
start to work?
Effects are expected
within several minutes of ingestion.
Are there any
safety issues?
It should not be
used by people with gastric or duodenal ulcers or with gastric hyperacidity.
PREPARATIONS
Proprietary
single-ingredient preparations
Germany:
Enziagil Magenplus.
Proprietary
multi-ingredient preparations
Australia:
Calmo; Digest; Digestaid; Digestive Aid; Extralife Sleep-Care; Pacifenity;
Relaxaplex. Austria: Abdomilon N; Brady's-Magentropfen; China-Eisenwein;
Mariazeller; Montana; Montana N; Original Schwedenbitter; Sigman-Haustropfen; Sinupret.
Brazil: Digestar; Estomafitino; Gotas Digestivas; Xarope Iodo-Suma. Canada: Herbal
Laxative; Herbal Nerve. Czech Republic: Biotussil; Dr Theiss Schweden Krauter;
Dr Theiss Schwedenbitter; Naturland Grosser Swedenbitter; Sinupret. France: Elixir
Grez; Quintonine. Germany: Abdomilon; Abdomilon N; Amara-Pascoe; Amara-Tropfen;
Gallexier; Gastrosecur; Klosterfrau Melisana; Schwedentrunk Elixier; Sedovent;
Sinupret; Solvopret; ventri-loges N. Hong Kong: Sinupret. Hungary: Sinupret. Italy:
Amaro Medicinale; Caramelle alle Erbe Digestive. Russia: Herbion Drops for the Stomach
(Гербион Желудочные Капли); Original Grosser Bittner Balsam (Оригинальный Большой
Бальзам Биттнера); Sinupret (Синупрет). South Africa: Amara; Enzian Anaemodoron
Drops; Helmontskruie; Lewensessens; Versterkdruppels; Wonderkroonessens. Singapore:
Sinupret. Spain: Depurativo Richelet. Switzerland: Demonatur Gouttes pour le
foie et la bile; Gastrosan; Padma-Lax; Padmed Laxan; Sinupret; Strath Gouttes
pour l'estomac. Thailand: Pepsitase; Sinupret. UK: Acidosis; Appetiser Mixture;
DigestAid; Indigestion Mixture; Kalms; Quiet Tyme; Scullcap & Gentian
Tablets; Stomach Mixture.
REFERENCE
Barnes, J., Anderson, L. A., and Phillipson, J. D. 2007. Herbal Medicines Third Edition. Pharmaceutical Press. Auckland and London.
Braun, L and Cohen, M. 2010. Hebs and Natural Supplements An Evidence Based Guide 3R D Edition
Duke, J. A. with Mary Jo Bogenschutz-Godwin, Judi duCellier, Peggy-Ann K. Duke. 2002. Handbook of Medicinal Herbs 2nd Ed. CRC Press LLC. USA.
Gruenwald, J., Brendler, T., Jaenicke, Ch. 2000. PDR for Herbal Medicines. Medical Economics Company, Inc. at Montvale, NJ 07645-1742. USA
Linda S-Roth. 2010. Mosby’s Handbook Of Herbs & Natural Supplements, Fourth Edition. Mosby Elsevier. USA
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