Biological source, Chemical constituents and Therapeutic efficacy of the following category of crude drugs: Cinchona and Artemisia

1. ANTI-MALARIALS
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Prepared By: Ms. Divya Kanojiya
Assistant Professor in Pharmacognosy
Department of Pharmacy, Sumandeep Vidyapeeth
Deemed to be University, Piparia, Vadodara.

2. Content:
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 B i o l o g ic a l s o u rc e , C h e m ic a l c o ns t i t u e nt s
a n d T h e ra p e u t i c ef f ic a c y o f t h e f o l l ow i n g
c ate go r y of c rude drugs :
 C inc h o na
 A rte mis ia

3. • Synonyms: Cortex Cinchonae, Countess, Peruvian or Jesuit’s bark, Cinchona
• Biological Source: Cinchona is the dried bark of the stem or of the root of
Cinchona calisaya Wedd., Cinchona ledgeriana Moens., Cinchona officinalis Linn.,
and Cinchona succirubra Pavon., or hybrids of any of the first two species with
any of the last two species, belonging to family Rubiaceae.
• Geographical Source: Tropical valleys of the Andes. Bolivia and Southern Peru.
Cinchona is a native of South America, occurring wild there. At present, it is
mainly cultivated in Indonesia (Java), Zaire, India, Guatemala, Bolivia, Ceylon etc.
CINCHONA
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4. 4
Figure: Cinchona bark

5. Morphology
Size 30 cm long and 2–7 mm thick.
Shape Curved, quill or double quill.
Colour The outer surface is yellowish to brown, with short fractures and the inner
surface varies in all the four species; like Cinchona calisaya and Cinchona
ledgeriana is yellowish, Cinchona officinalis is slightly brown and Cinchona
succilubra is reddish brown
Odour Distinctive
Taste Highly bitter and astringent.
Extra
features
The outer surface consist of longitudinal and transverse cracks, fissures,
ridges 5

6. • T.S. shows a well developed periderm, a wide cortex and a large secondary phloem.
• PERIDERM
• Cork consists of several layers of radially arranged rows of thin walled cells with dark
brown contents. The cork cells are impregnated with suberin.
• Phellogen
• 2-3 layers of thin walled rectangular cells without any cell contents.
• Phelloderm
• 6-8 layers of thin walled rectangular cells without any cell contents, like cork, they are
arranged at times in radial rows.
Microscopy
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7. • CORTEX
• Several layers of thin walled and tangentially elongated cells containing yellowish
brown matter. Some of the cortical cells are filled with micro sphenoidal crystals of
calcium oxalate and the rest with minute starch grains. Besides, isolated secretion
cells (latex ducts) are also found in the cortical parenchyma.
• SECONDARY PHLOEM
• This region comprises of phloem parenchyma, phloem fibres and medullary rays.
Microscopy
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8. • Phloem fibres, characteristic of Cinchona bark occur intermingled with
phloem parenchyma and in between medullary rays. Fibres are numerous,
mostly isolated, at times in groups of 2 or 3, rounded to oval, in various sizes,
yellow in colour, thick walled, strongly lignified with a small lumen and
stratifications.
• MEDULLARY RAYS
• It is traverse radially the phloem parenchyma; 1-3 cells wide, extend upto
cortex, cells radially elongated and contain starch grains.
Microscopy
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Figure: T.S of Cinchona bark

10. • More than 30 alkaloids have been reported in cinchona. The
chiefly identified alkaloids are quinidine, quinine, cinchonine
and cinchonidine. These constituents are the stereoisomers of
each other like quinine is stereoisomer of quinidine and
cinchonine is stereoisomer of cinchonidine.
Chemical constituents
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11. • The other constituents available are quiniarnine, cinchotine,
hydroquinine, hydrocinchonidine, cinchotannic acid, etc.
Quinine and quinidine has a methoxy group in it but
cinchonine and cinchonidine do not have a methoxy group.
• Other than these it also consist of bitter glycoside, starch
grains, calcium oxalate crystals and crystalline acid like quinic
acid.
Chemical constituents
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13. 1. Thalleioquin test: To the extract of cinchona powder add one drop of dilute sulphuric
acid and 1 ml of water. Add bromine water drop wise till the solution acquires permanent
yellow colour and add 1 ml of dilute ammonia solution, emerald green colour is
produced.
2. The powdered drug when heated with glacial acetic acid in dry test tube, evolves red
fumes, which con dense in the top portion of the tube.
3. Cinchona bark, when moistened with sulphuric acid and observed under ultraviolet light
shows a blue fluorescence due to the methoxy group of Quinine and quinidine.
Chemical test
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14. • It is mainly employed as antimalarial drug, but it is also used as
analgesic, antipyretic, protoplasmic, bitter stomachic and tonic.
• Quinidine is cardiac depressant and Cinchonidine is used in
rheumatism and neuralgia.
Uses
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15. • Cuprea Bark (Remijia pedupiculato); Family: Rubiaceae, it differs in
its morphological character with cinchona but consist of
constituents like Quinine, quinidine, cinchonine, cinchonamine,
etc., the other species of Remijia, that is, R. purdieana (false Cuprea
bark) does not contain quinine.
Substitutes
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16. • It is one of the ingredients of the
preparations known as Herbipyrin
tablet, M.P. 6 Capsules (Vasu
Healthcare).
Marketed products
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17. ARTEMISIA
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18. • Synonym: Mugwort, wormwood, sagebrush is a plant of the daisy, Santonica
and Worm seeds.
• Biological Source: Artemisia consists of unexpanded flower-head obtained
from the plant Artemisia annua, Artemisia apiacea, Artemisia lancea,
Artemisia brevifolia, Artemisia maritima.
• Family: Asteraceae.
• Geographical Source: Artemisia plant is found in the Kurran valley regions of
Pakistan, Turkey, and widespread from Kashmir to Kumaon in Himalayas, and
in West Tibet. The plant is also cultivated in the states of Punjab, Uttar
Pradesh, and Haryana.
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19. • Colour: Flowers are yellow in colour, while other parts are
whitish-grey.
• Odour: Aromatic and sweet.
• Taste: Bitter and camphoraceous.
• It contains yellowish or brownish, oval -shaped flower-heads.
• The flowers are fertile in presence of tubular corolla and short
cylindrical tube and narrow limb. It lacks calyx.
Morphology
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20. • The major active constituent of Artemisia annua, Artemisia apiacea,
and Artemisia lancea is Sesquiterpene with an internal peroxide
linkage Artemisinin.(The aerial parts of Artemisia annua contain 0.01-
0.8% of artemisinin per dry weight).
• Derivatives of this compound include arteether, artemether,
artemotil, artenimol, artesunate, and dihydroartemisinin, which,
along with artemisin, are currently being used to treat drug- resistant
and non-drug resistant malaria.
Chemical constituents
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21. • Other constituents of Artemisia annua include Santonin(Sesquiterpene
lactone), deoxyartemisinin, artemisinic acid, arteannuin-B, stigmasterol,
friedelin, friedelan-3 beta-ol, artemetin, and quercetagetin 6,7,3',4'-
tetramethyl ether.
• The essential oil of Artemisia annua aerial parts contains 44% camphor, 16%
germacrene D, 11% trans-pinocarveol, 9% beta- selinene, 9% beta-
caryophyllene, and 3% artemisia ketone.
Chemical constituents
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22. Chemical test
The colour of liquid
appears red.
Sodium hydroxide is
added to the filtrate
and the mixture is
heated.
1gm of finely
powdered drug is
mixed with 10ml
alcohol and filtered.
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23. • The plant can be substituted by a tall aromatic shrub of
Artemisia vulgaris Linn. (belonging to family Compositae)
distributed in all mountainous regions of India.
Substituents
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24. • Artemisia annua extracts have antimalarial properties.
• A combination of Artemisia annua and chloroquine was more effective in fever subsidence
and disappearance of malarial symptoms.
• Qinghaosu (QHS), also known as artemisinin and arteannuin, is a novel type of
sesquiterpene with a peroxide linkage isolated from the Chinese herb Artemisia annua L.
• Since its discovery as an antimalarial with low toxicity, hundreds of derivatives have been
synthesized; artesunate (ATS), artemether (ATM), and dihydroartemisinin (DHQHS) were
found to be more active than QHS itself.
• Santonin is a strong anthelmintic acting against roundworm infections.
Uses
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25. Marketed products
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