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Bitter Glycosides
In general, bitters are the edible natural products
mostly consumed before any normal meals to
stimulate as well as enhance the appetite.
However, the bitter glycosides as a class do possess
almost similar activities like the bitters such as:
digestive, stomachic and febrifuge.
Therapeutically, the bitters have been found to
exert their stimulant effects on the gustatory (i.e.;
related to the sense of taste) nerves located in the
mouth and ultimately give rise to an improved
gastric juice secretion in the stomach.
The bitter glycosides have been found not confined
to the same chemical class, but the most important
ones amongst them essentially possess the pyran
cyclopentane ring.
A number of bitter glycosides isolated from natural
plants have been put into actual therapeutic
practice, namely: Picrorhiza, Gentian, and Chirata,
which shall be discussed in the sections that follow.
 Picrorhiza -:
 Synonyms Indian Gentian; Katki.
 Biological Source It is the dried rhizome
of Picrorhiza kurroa Royle ex Benth., belonging
to family Serophulariaceae.
 GeographicalSourcesIt is a perennial herb
grown abundantly and distributed on the
Alpine Himalayas extended from Kashmir to
Sikkim at an altitude between 3000 to 5000
meters. It is also found in China.
 Preparation The plant is either propogated
by seeds or by rhizomes. The rhizomes are
collected from the cultivated and naturally
growing plants washed dried and packed.
 Description
 Colour : Externally—Dark Greyish brown
Internally—White blackish
 Odour : Slight and unpleasant
 Taste : Bitter
 Size : Length = 3-5 cm; Diameter = 0.5-1 cm
 Shape : Mostly cylindrical small fragments
having longitudinal wrinkled and annulations
at the tip.
 Special Features : The stems and conical
buds along with the drugs usually form a part
of the drug itself. The roots are invaribaly
wrinkled in the longitudinal fashion having
transverse cracks. They are greyish to brown in
appearance, while the fracture is tough.
 Chemical Constituents : The
therapeutically potent constituents of the drug
essentially comprises of three vital bitter
glycosides, namely: Picroside I, Picroside
II and Kutkoside as given below:
In fact, chemically
both Picroside and Kutkoside are C-9
monoterpene iridoid glycosides having an epoxy
moiety present in the cyclopentane ring. Besides,
it also contains organic acids, resin, sugar and
tannins.
 Uses
1. It is mostly employed as a vital bitter tonic
2. It is also used as a stomachic and febrifuge.
3. In large doses it exerts its action as a laxative
4. It also finds its usefulness in the treatment of
jaundice.
5. Its alcohlic extract exhibits remarkable
antibacterial effect.
Gentian :
 Synonyms Yellow Gentian; Pale Genetian;
Bitter Root; Gentian Root; Radix; Radix
Gentianae; Gentiana.
 Biological Source Gentian is the dried
rhizomes and roots of Gentiana lutea L.,
belonging to family Gentianaceae.
 Geographical Source It is perennial
herbaceous tree which is found to be native to
the hilly zones in Central and Southern Europe.
It is also grown on Vosges mountains,
Yugoslavia (now known as Serbia and Crotia)
and Jura.
 Preparation The long rhizomes and fully
grown fleshly roots of 2 to 5 year aged plants
are dug up carefully and collected preferably in
autumn. The roots and rhizomes are washed
thoroughly to get rid of the adhered soil and
then sliced into a longitudianal fashion. The
freshly sliced pieces of roots and rhizomes
generally appear white in colour and do not
have any odour. However, during the process
of gradual drying in small heaps at a controlled
temperature of 50-60o
C fermentation
commences which eventually turns them into
dark or yellow coloured product that have a
characteristc odour.
 Description The description of root and
rhizome of gentian are summarised below:
 ChemicalConstituents The principal bitter
glycosides of common gentians, which was
isolated in 1862 from G. lutea, is gentiopicrin,
also known as gentiopicroside. It is present
upto 2%.
It is a highly water soluble crystalline
substance having a bitter value to the extent
of 12, 000.
The process of drying and fermentation helps
in the cleavage of the above glycoside
to gentiogenin and glucose.
The drug also contains amarogenin, which is
considerd to be a strongly bitter
glucoside that even imparts a distinct bitter
taste at 580 thousand time dilutions.
Besides,it
contains amaroswerin and gentioside;
and gentinin which is a mixture
of gentiopicrin and gentinin. It also contains a
flavonoid alkaloid commonly known
as gentisin (Syn: Gentianic acid; Gentianin;
Gentin) and gentisic acid.
 Uses :
1. It is invariably used as a bitter tonic in
anorexia and dyspepsia.
2. It appreciably improves the relatively dull
appetite.
Chirata-:
 Synonyms Bitter stick; Chiretta; Chirayita;
East Indian Balmony.
 Biological Source It is the dried plant
of Swerlia (Ophelia) chirata (Roxb) Buch-Ham;
belonging to family Gentianaceae.
 Geographical Source It is found in India
from Himalaya to the mountainous regions in
Kashmir, Bhutan, Meghalaya and Khasi Hills at
an altitude ranging between 1200-1500
meters. It is also grown in Nepal.
 Preparation The plant usually flowers from
July to October. It is collected for medicinal
utilities as and when the capsuls are fully
formed. The dried plants are tied into bundles
weighting approximately 1-1.25 kg.
 Description
 Colour : Leaves, flowers and fruits-yellowish
shade; stem-yellowish brown to purple
 Odour : Odourless
 Taste : Extremely bitter
 Size : Stems = Length: 1.0 meter; Breadth = 6
mm
 Shape : Stems are mostly cylindrical, glabrous
and quandrangular at the appex hawing a large
pith.
 Chemical Constituents : It invariably
contains bitter principles, namely: ophelic
acid; bitter glycosides:
amarogentin and chiratin; alkaloids;
gentianine and gentiocrucine.
 Substituents/Adulterants In fact, there
are three widely known substituents
for chirata, namely:
(a) Swertia paniculata Wall: The plant grows in
the temperate climate of Western Himalaya, from
Kashmir to Nepal at an attitude of 2000-3000
meters;
(b) Swertia angustifolia Buch-Ham: The plant is
found in the subtropical region of Himalaya at an
altitude ranging between 300 to 2000 meters from
the Chenab to Bhutan; and
(c) Sweritia densifolia: It grows in the Konkan
region and usually attains a height of about 30 to
90 cm.
 Uses :
1. It is invariably used as a bitter tonic.
2. It also finds its use as a febrifuge.
3. It is employed in dyspepsia.
4. It has been recommended as a diuretic and in
epilepsy.
5. Industrially, it is extensively used in dyeing
cotton cloth.

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Bitter glycosides ll

  • 1.
  • 2. Bitter Glycosides In general, bitters are the edible natural products mostly consumed before any normal meals to stimulate as well as enhance the appetite. However, the bitter glycosides as a class do possess almost similar activities like the bitters such as: digestive, stomachic and febrifuge. Therapeutically, the bitters have been found to exert their stimulant effects on the gustatory (i.e.; related to the sense of taste) nerves located in the mouth and ultimately give rise to an improved gastric juice secretion in the stomach. The bitter glycosides have been found not confined to the same chemical class, but the most important ones amongst them essentially possess the pyran cyclopentane ring. A number of bitter glycosides isolated from natural plants have been put into actual therapeutic practice, namely: Picrorhiza, Gentian, and Chirata, which shall be discussed in the sections that follow.
  • 3.  Picrorhiza -:  Synonyms Indian Gentian; Katki.  Biological Source It is the dried rhizome of Picrorhiza kurroa Royle ex Benth., belonging to family Serophulariaceae.  GeographicalSourcesIt is a perennial herb grown abundantly and distributed on the Alpine Himalayas extended from Kashmir to Sikkim at an altitude between 3000 to 5000 meters. It is also found in China.  Preparation The plant is either propogated by seeds or by rhizomes. The rhizomes are collected from the cultivated and naturally growing plants washed dried and packed.
  • 4.  Description  Colour : Externally—Dark Greyish brown Internally—White blackish  Odour : Slight and unpleasant  Taste : Bitter  Size : Length = 3-5 cm; Diameter = 0.5-1 cm  Shape : Mostly cylindrical small fragments having longitudinal wrinkled and annulations at the tip.  Special Features : The stems and conical buds along with the drugs usually form a part of the drug itself. The roots are invaribaly wrinkled in the longitudinal fashion having transverse cracks. They are greyish to brown in appearance, while the fracture is tough.  Chemical Constituents : The therapeutically potent constituents of the drug essentially comprises of three vital bitter glycosides, namely: Picroside I, Picroside II and Kutkoside as given below:
  • 5. In fact, chemically both Picroside and Kutkoside are C-9 monoterpene iridoid glycosides having an epoxy moiety present in the cyclopentane ring. Besides, it also contains organic acids, resin, sugar and tannins.  Uses 1. It is mostly employed as a vital bitter tonic 2. It is also used as a stomachic and febrifuge. 3. In large doses it exerts its action as a laxative 4. It also finds its usefulness in the treatment of jaundice. 5. Its alcohlic extract exhibits remarkable antibacterial effect.
  • 6. Gentian :  Synonyms Yellow Gentian; Pale Genetian; Bitter Root; Gentian Root; Radix; Radix Gentianae; Gentiana.  Biological Source Gentian is the dried rhizomes and roots of Gentiana lutea L., belonging to family Gentianaceae.  Geographical Source It is perennial herbaceous tree which is found to be native to the hilly zones in Central and Southern Europe. It is also grown on Vosges mountains, Yugoslavia (now known as Serbia and Crotia) and Jura.  Preparation The long rhizomes and fully grown fleshly roots of 2 to 5 year aged plants are dug up carefully and collected preferably in autumn. The roots and rhizomes are washed thoroughly to get rid of the adhered soil and then sliced into a longitudianal fashion. The freshly sliced pieces of roots and rhizomes generally appear white in colour and do not have any odour. However, during the process of gradual drying in small heaps at a controlled temperature of 50-60o C fermentation
  • 7. commences which eventually turns them into dark or yellow coloured product that have a characteristc odour.  Description The description of root and rhizome of gentian are summarised below:  ChemicalConstituents The principal bitter glycosides of common gentians, which was isolated in 1862 from G. lutea, is gentiopicrin,
  • 8. also known as gentiopicroside. It is present upto 2%. It is a highly water soluble crystalline substance having a bitter value to the extent of 12, 000. The process of drying and fermentation helps in the cleavage of the above glycoside to gentiogenin and glucose. The drug also contains amarogenin, which is considerd to be a strongly bitter
  • 9. glucoside that even imparts a distinct bitter taste at 580 thousand time dilutions. Besides,it contains amaroswerin and gentioside; and gentinin which is a mixture of gentiopicrin and gentinin. It also contains a flavonoid alkaloid commonly known as gentisin (Syn: Gentianic acid; Gentianin; Gentin) and gentisic acid.  Uses : 1. It is invariably used as a bitter tonic in anorexia and dyspepsia. 2. It appreciably improves the relatively dull appetite. Chirata-:  Synonyms Bitter stick; Chiretta; Chirayita; East Indian Balmony.  Biological Source It is the dried plant of Swerlia (Ophelia) chirata (Roxb) Buch-Ham; belonging to family Gentianaceae.
  • 10.  Geographical Source It is found in India from Himalaya to the mountainous regions in Kashmir, Bhutan, Meghalaya and Khasi Hills at an altitude ranging between 1200-1500 meters. It is also grown in Nepal.  Preparation The plant usually flowers from July to October. It is collected for medicinal utilities as and when the capsuls are fully formed. The dried plants are tied into bundles weighting approximately 1-1.25 kg.  Description  Colour : Leaves, flowers and fruits-yellowish shade; stem-yellowish brown to purple  Odour : Odourless
  • 11.  Taste : Extremely bitter  Size : Stems = Length: 1.0 meter; Breadth = 6 mm  Shape : Stems are mostly cylindrical, glabrous and quandrangular at the appex hawing a large pith.  Chemical Constituents : It invariably contains bitter principles, namely: ophelic acid; bitter glycosides: amarogentin and chiratin; alkaloids; gentianine and gentiocrucine.  Substituents/Adulterants In fact, there are three widely known substituents for chirata, namely: (a) Swertia paniculata Wall: The plant grows in the temperate climate of Western Himalaya, from Kashmir to Nepal at an attitude of 2000-3000 meters; (b) Swertia angustifolia Buch-Ham: The plant is found in the subtropical region of Himalaya at an altitude ranging between 300 to 2000 meters from the Chenab to Bhutan; and (c) Sweritia densifolia: It grows in the Konkan region and usually attains a height of about 30 to 90 cm.
  • 12.  Uses : 1. It is invariably used as a bitter tonic. 2. It also finds its use as a febrifuge. 3. It is employed in dyspepsia. 4. It has been recommended as a diuretic and in epilepsy. 5. Industrially, it is extensively used in dyeing cotton cloth.