2. ARTEMISININ
SYNONYM: SWEET WORMWOOD, SWEET ANNIE, ANNUAL
WORMWOOD,SWEET SAGEWORT
BIOLOGICAL SOURCE: IT IS A SEMISYNTHETIC
DERIVATIVE OF SESQUITERPENE LACTONE AND
SITUATED IN GLANDULAR TRICHOME OF LEAVE AND
EXTRACTED FROM THE PLANT OF ARTEMISIA ANNUA
(SWEET WORMWOOD).
FAMILY:ASTERACEAE/COMPOSITAE
IT IS MAINLY USED IN CHINESE SYSTEM
OF MEDICINE
GEOGRAPHICAL SOURCE: IT IS
MAINLY DISTRIBUTED IN MILD
LATITUDE OF FOUR CONTINENTS:
1. WESTERN AND CENTRAL
EUROPE
2. SOUTHEASTERN ASIA
3. SOUTHEASTERN NORTH
AMERICA
3. 4. SOUTHEASTERN SOUTH AMERICA
BUT IN INDIA IT IS MAINLY
CULTIVATED IN LUCKNOW AND
SRINAGAR WHICH IS EXTRACTED
BY PETROLEUM ETHER.
CHEMISTRY OF ARTEMISININ:
1. TETRACYCLIC STRUCTURE
WITH TRIOXANE RING AND A
LACTONE RING
2. TRIOXANE RING CONTAIN A
PEROXIDE BRIDGE WHICH IS
ACTIVE MOIETY OF MOLECULE.
ACTIVE CONSTITUENT OF
ARTEMISININ:
ARTEMISININ,DIHYDROARTEMISI
NIN, ARTEMISIN
4. MECHANISM OF ACTION OF
ARTEMISININ:
1. ARTEMISININS ARE PRODRUGS OF THE
BIOLOGICALLY ACTIVE
METABOLITE DIHYDROARTEMISININ
WHICH IS ACTIVE DURING
THE STAGE WHEN THE PARASITE IS
LOCATED INSIDE RBC.
2. SEVERAL LINE OF EVIDENCE INDICATE
THAT ARTEMISININS
EXERT THEIR ANTIMALARIAL ACTION BY
RADICAL
FORMATION THAT
DEPEND ON THEIR ENDOPEROXIDE BRIDGE.
3. WHEN THE PARASITE THAT CAUSES
MALARIA INFECT A RBC, IT
CONSUMES HEMOGLOBIN WITHIN ITS
DIGESTIVE VACUOLE, A
PROCESS THAT GENERATES OXIDATIVE
STRESS.
5. INDUSTRIAL PREPARATION OF ARTEMISININ:
TAKE A DRIED POWDER SAMPLE OF ARTEMISIA ANNUA
MIXED WITH METHANOL FOR 1 HOUR IN SOXHLET APPARATUS
EVAPORATED THE SOLUTION UNDER VACUUM UPTO 100 ML
AND MIXED WITH OR PARTITIONED WITH n-hexane
AFTER MIXING WITH n-hexane COLLECTED THE METHANOL LAYER AND
THAN ADD WATER
AGAIN PARTITIONED WITH ETHYL ACETATE
AFTER THIS 2 LAYER ARE SEPERATED 1. SEMIPOLAR LAYER (ETHYL
ACETATE LAYER) AND 2. POLAR LAYER(METHANOL WATER LAYER)
ETHYL ACETATE LAYER EVAPORATE TO GET CRUDE ARTEMISININ
6. CHEMICAL TEST
1. SAMPLE+fecl3+naI DEEP VIOLET COLOUR
2. SAMPLE+TRIPHENYLPHOSPHINE TRIPHENYLPHOSPHINE
OXIDE(INDICATE THE PRESENCE OF OR EXISTENCE OF AN
OXIDATIVE GROUP)
ESTIMATION AND IDENTIFICATION OF ARTEMISININ:
1. TLC METHOD:
a. PLATE: PRECOATED SILICA GEL 60F254
b. MOBILE PHASE: hexane(n):diethyl ether(6:4v/v)
c. SPRAYING REAGENT: ACETIC ACID : SULPHURIC ACID
:ANISALDEHYDE(100:2:1)
d. Rf: 0.20 ( PINK SPOT)
SAMPLE PREPARATION: 1mg IS EXTRACTED IS DISSOLVED IN 50 ML OF
MOBILE PHASE AND APPLIED IT ON PLATE.
7. STANDARD PREPARATION: 1mg OF STANDARD ARTEMISININ IS
DISSOLVED IN 100ml OF MOBILE PHASE AND APPLIED ON PLATE.
2. HPLC METHOD:
A. EQUIPMENT NAME: WATER C501
B. COLUMN: WATER C18
C. MOBILE PHASE: ACETONITRILE:WATER(85:15V/V)
D. FLOW RATE: 1.0 ml/min
E. DETECTION WAVELENGTH: 216nm-260nm
F. INJECTION VALUE: 20 µl
G. PUMP MODE: ISOCRATIC
H. RUN TIME: 4.68min
SAMPLE PREPARATION: 10mg ARTEMISININ DISSOLVED IN
MOBILE PHASE TO PRODUCE 10 ml
STANDARD PREPARATION: 1. 5g POWDER ARTEMISIA AND MIXED
WITH nhexane FOR 6hr AT 60+-2. AND AMBERED COLOURED FLASK
8. 2.COOLED AT ROOM TEMPERATURE AND FILTER THROUGH WHATMAN
NO 41 AND COLLECTED IN 250 ML AMBER COLOURED VOLUMETRIC
FLASK
3. MARC AGAIN REFLUX WITH 100 ml 0F nhexane FOR 1 HR
4. CONTENT WAS FILTERED AND EVAPORATED TO DRYNESS AT WATER
BATH AT 70 DEGREE CELSIUS
5. RESIDUE DISSOLVED AND DILUTED WITH MOBILE PHASE TO GET
PRODUCT
USE:
1. IT IS USED IN ANTIMALARIAL
2. IT IS USED IN GASTRIC INFECTION
3. IT IS USED IN TREATMENT OF SCHIZOPHRENIA
4. IT IS USED IN COLON AND HUMAN LEUKEMIA
5. IT IS USED IN SEVERAL BLOOD PARASITIC PROTOZOANS DISEASE