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PRESENTED BY
Nabeela Jabeen
DEFINITION
• CANCER:- Cancer is characterized by rapid and uncontrolled
formation of abnormal cells which may mass together to form a
growth or tumor, or proliferate throughout the body, initiating
abnormal growth at other sites.
* ANTI-CANCER DRUGS:- The Drugs that are used in inhibiting
the abnormal cell growth or killing the cancer cells.
CLASSIFICATION:-
S.No CLASS DRUGS PLANT SOURCE
1. Vinca alkaloids Vincristine
Vinblastine
Catharanthus
roseus
(Apocynaceae)
2. Taxanes Paclitaxel
Docetaxel
Taxus brevifolia
(Taxaceae)
3. Epipodophyllotoxin Etoposide Podophyllum
hexandrum
(Berberidaceae)
4. Camptothecin
analouges
Topotecan
Irinotecan
Camptotheca
acuminata
(Nyssaceae)
5. Colchicine Demecoline Cocus
cholchicum
Autumnale
(Liliaceae)
6. Maytansinoid Mcytanacine
Maytansine
Maytenus
buchananii,
M.Serrata
(Celastraceae)
7. Macrocyclic lactones Bryostanins Bryozoa Bugula
neritina
8. Quassinoids Bruceantin brusato Brucea javanica
(Simarubaceae)
9. Curcuma Curcumin Curcuma longa
(Zingiberaceae)
10. Flavonoids Vicenin
Orentin
Ocimum sanctum
(Labiatae)
11. Sesquiterpene Gossypal Gossypium
barbadense
(Gossypiaceae
)
12. Ellipticine Ellipticine Ochrosia eliptica
(Apocynaceae)
13. Pthalide isoquinoline
alkaloid
Noscapine Papaver
somniferum
(Papaveraceae)
14. Acetogenins Acetogenin Annona species
(Annonaceae)
MODE OF ACTION OF NATURAL ANTICANCER
DRUGS :
Purine synthesis Pyrimidine synthesis
Ribonucleotides
Deoxyribonucleotides
DNA
RNA
Enzymes Proteins Microtubules
Camptothecin
Etoposide
Block
topoisomerase
functions
Paclitaxel
Vinca
Cholchine
Inhibit the function
of microtubules
RECENT ADVANCES OF NATURAL ANTICANCER
AGENTS:-
1. Natural agents have low toxicity.
2.The MOA of recent natural agents are
* Acts on DNA bases
* Intercalation of DNA
* Inhibit topoisomerases & Proteinkinases
* Induction of Apoptosis (Cell suicide)
3. Many new species are investigated to find out new agents
for treatment of cancer.
4.Cell culture techniques are involved to produce new botanical
therapeutic agents to treat neoplasms
5. Development of QSAR modelling on anti- cancer agents also
produces good therapeutic agents with decreasing toxicity
PLANT-DERIVED ANTICANCER AGENTS IN CLINICAL
USE:-
1. First agents that were clinically used are Vinca alkaloids, Vinblastine(VLB) &
Vincristine(VCR),isolatedfromMadagascarperiwinkle.
2. Two clinically active agents, etoposide (VM 26) & teniposide (VP 16-213), semi
syntheticderivativesofepipodophyllotoxinareusedincancertreatment.
3. The use of various parts of T.brevifolia and other Taxus species is widely used in
canertherapy.
4. Anti-cancer drug armamentarium is the class of clinically- active agents derived
from camptothecin, which is isolated from chinese ornamental tree is widely
used.
5. Other plant-derived agents in clinical use are homoharringtonine (Cephalotaxus
harringtonia) and elliptinium, a derivative of ellipticine, isolated from species of
severalgeneraoftheApocynaceaefamily,includingBleekeriavitensisA.C.Sm.
PLANT-DERIVED ANTICANCER AGENTS IN CLINICAL
DEVELOPMENT:-
1.Vinblastine/Vincristine: Catharanthus roseus/Jamaica,
Philippines (originally from Madagascar)
2. Etoposide: Podophyllum species/ Eastern US, Himalayas
3. Paclitaxel/Docetaxel: Taxus species/NW US, Europe
4. Topotecan/Irinotecan: Camptotheca acuminata/China
5. Homoharringtonine: Cephalotaxus harringtonia/China
6. Flavopiridol: Synthetic based on rohutikine from
Dysoxylum binectariferum/India
7. Combretastatins: Combretum caffrum/S. Africa
Plant Alkaloids
Vinca Alkaloids Podophyllotoxins
Etoposide
Camptothecins
Topotecan
Taxanes
Paclitaxel
Vinblastine
Vincristine
Vinorelbine
Teniposide Irinotecan Docetaxel
Vinca alkaloids
B. source: Catharanthus roseus
Family: Apocynaceae
Part used: Dried whole plant
Chemical constituent:
 Vincristine
 Vinblastine
 Ajmalicine
 Vindesine
MODE OF ACTION OF VINCA
• These drugs block the
formation of mitotic spindle
by preventing the assembly
of tubulin dimers into
microtubules.
• They act primarily on the M
phase of cancer cell cycle.
Uses of vinca
In Europe, folk remedy for
diabetes for centuries.
In China, an astringent,
diuretic and cough remedy.
In Central and South
America, homemade cold
remedy to ease lung
congestion and
inflammation and sore
throats
Throughout the Caribbean,
an flower extract to treat
eye irritation and infections
VinBlastine VinCristine
Uses :
Hodgkin’s disease
Lymphomas
Carcinoma Breast
Testicular tumors
Uses:
Childhood leukemias
Childhood tumors-Wilm’s
tumor, Neuroblastoma,
Hodgkin’s disease
Podophyllum
B. Source: Podophyllum
hexandrum
Family: Berberidaceae
Part used: dried rhizomes & roots
Uses:
• Used in treatment of small cell
carcinoma of lung, prostrate and
testicular carcinomas
Chemical constitutent:
• Podophyllotoxin
• Etoposide
• Teniposide
Podophyllotoxin
MOA of Podophyllum
• Acts by inhibiting
topoisomerase II
• These drugs are most active in
late S and early G2 phase
Taxanes
• B. source: Taxus brevifolia
• Family: Taxaceae
• Part used: Stem bark
Uses:
• Ovarian cancer
• Lung carcinoma
• Gastric & Cervical cancers
• Prostate & colon cancer
Chemical constituent:
• Taxol
• Paclitaxel
• Docetaxal
Taxol
TAXOL
MOA of Taxanes
• These drugs act by interfering with mitotic
spindle
• They prevent micotubule disassembly into
tubulin monomers
Camptothecin
B. source: Camptotheca acuminata
Family: Nyssaceae
Part used: Dried stem wood
Uses:
 Ovarian cancers
 Colorectal cancer
 Cancer of neck & head
 Liver cancer
Chemical constituent:
 Camptothecin
 Topotecan
 Irinotecan
Camptothecin
Topotecan
TOPOTECAN
Camptotecan
MOA of Camptothecin
• Camptothecin act by
inhibiting topoisomerase-I
CONCLUSION
• Plants have been a prime source of highly effective
conventional drugs for the treatment of many forms of
cancer.
• The actual compound isolated from the plant may not serve
as the drug but leads to the development of potential novel
agents.
• Natural agents are proving to be an important source of
novel inhibitors & have the potential for development into
selective anticancer agents.
Objectives
At the end of lecture student will able to understand
 What is cancer
 Classification of anticancer drug from plant
 Their mode of actions
 Also their pharmacognostic features
Anticancer drug from plant

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Anticancer drug from plant

  • 2. DEFINITION • CANCER:- Cancer is characterized by rapid and uncontrolled formation of abnormal cells which may mass together to form a growth or tumor, or proliferate throughout the body, initiating abnormal growth at other sites. * ANTI-CANCER DRUGS:- The Drugs that are used in inhibiting the abnormal cell growth or killing the cancer cells.
  • 3. CLASSIFICATION:- S.No CLASS DRUGS PLANT SOURCE 1. Vinca alkaloids Vincristine Vinblastine Catharanthus roseus (Apocynaceae) 2. Taxanes Paclitaxel Docetaxel Taxus brevifolia (Taxaceae) 3. Epipodophyllotoxin Etoposide Podophyllum hexandrum (Berberidaceae) 4. Camptothecin analouges Topotecan Irinotecan Camptotheca acuminata (Nyssaceae)
  • 4. 5. Colchicine Demecoline Cocus cholchicum Autumnale (Liliaceae) 6. Maytansinoid Mcytanacine Maytansine Maytenus buchananii, M.Serrata (Celastraceae) 7. Macrocyclic lactones Bryostanins Bryozoa Bugula neritina 8. Quassinoids Bruceantin brusato Brucea javanica (Simarubaceae) 9. Curcuma Curcumin Curcuma longa (Zingiberaceae) 10. Flavonoids Vicenin Orentin Ocimum sanctum (Labiatae)
  • 5. 11. Sesquiterpene Gossypal Gossypium barbadense (Gossypiaceae ) 12. Ellipticine Ellipticine Ochrosia eliptica (Apocynaceae) 13. Pthalide isoquinoline alkaloid Noscapine Papaver somniferum (Papaveraceae) 14. Acetogenins Acetogenin Annona species (Annonaceae)
  • 6. MODE OF ACTION OF NATURAL ANTICANCER DRUGS : Purine synthesis Pyrimidine synthesis Ribonucleotides Deoxyribonucleotides DNA RNA Enzymes Proteins Microtubules Camptothecin Etoposide Block topoisomerase functions Paclitaxel Vinca Cholchine Inhibit the function of microtubules
  • 7. RECENT ADVANCES OF NATURAL ANTICANCER AGENTS:- 1. Natural agents have low toxicity. 2.The MOA of recent natural agents are * Acts on DNA bases * Intercalation of DNA * Inhibit topoisomerases & Proteinkinases * Induction of Apoptosis (Cell suicide) 3. Many new species are investigated to find out new agents for treatment of cancer. 4.Cell culture techniques are involved to produce new botanical therapeutic agents to treat neoplasms 5. Development of QSAR modelling on anti- cancer agents also produces good therapeutic agents with decreasing toxicity
  • 8. PLANT-DERIVED ANTICANCER AGENTS IN CLINICAL USE:- 1. First agents that were clinically used are Vinca alkaloids, Vinblastine(VLB) & Vincristine(VCR),isolatedfromMadagascarperiwinkle. 2. Two clinically active agents, etoposide (VM 26) & teniposide (VP 16-213), semi syntheticderivativesofepipodophyllotoxinareusedincancertreatment. 3. The use of various parts of T.brevifolia and other Taxus species is widely used in canertherapy. 4. Anti-cancer drug armamentarium is the class of clinically- active agents derived from camptothecin, which is isolated from chinese ornamental tree is widely used. 5. Other plant-derived agents in clinical use are homoharringtonine (Cephalotaxus harringtonia) and elliptinium, a derivative of ellipticine, isolated from species of severalgeneraoftheApocynaceaefamily,includingBleekeriavitensisA.C.Sm.
  • 9. PLANT-DERIVED ANTICANCER AGENTS IN CLINICAL DEVELOPMENT:- 1.Vinblastine/Vincristine: Catharanthus roseus/Jamaica, Philippines (originally from Madagascar) 2. Etoposide: Podophyllum species/ Eastern US, Himalayas 3. Paclitaxel/Docetaxel: Taxus species/NW US, Europe 4. Topotecan/Irinotecan: Camptotheca acuminata/China 5. Homoharringtonine: Cephalotaxus harringtonia/China 6. Flavopiridol: Synthetic based on rohutikine from Dysoxylum binectariferum/India 7. Combretastatins: Combretum caffrum/S. Africa
  • 10. Plant Alkaloids Vinca Alkaloids Podophyllotoxins Etoposide Camptothecins Topotecan Taxanes Paclitaxel Vinblastine Vincristine Vinorelbine Teniposide Irinotecan Docetaxel
  • 11. Vinca alkaloids B. source: Catharanthus roseus Family: Apocynaceae Part used: Dried whole plant Chemical constituent:  Vincristine  Vinblastine  Ajmalicine  Vindesine
  • 12. MODE OF ACTION OF VINCA • These drugs block the formation of mitotic spindle by preventing the assembly of tubulin dimers into microtubules. • They act primarily on the M phase of cancer cell cycle.
  • 13. Uses of vinca In Europe, folk remedy for diabetes for centuries. In China, an astringent, diuretic and cough remedy. In Central and South America, homemade cold remedy to ease lung congestion and inflammation and sore throats Throughout the Caribbean, an flower extract to treat eye irritation and infections
  • 14. VinBlastine VinCristine Uses : Hodgkin’s disease Lymphomas Carcinoma Breast Testicular tumors Uses: Childhood leukemias Childhood tumors-Wilm’s tumor, Neuroblastoma, Hodgkin’s disease
  • 15. Podophyllum B. Source: Podophyllum hexandrum Family: Berberidaceae Part used: dried rhizomes & roots Uses: • Used in treatment of small cell carcinoma of lung, prostrate and testicular carcinomas Chemical constitutent: • Podophyllotoxin • Etoposide • Teniposide Podophyllotoxin
  • 16. MOA of Podophyllum • Acts by inhibiting topoisomerase II • These drugs are most active in late S and early G2 phase
  • 17. Taxanes • B. source: Taxus brevifolia • Family: Taxaceae • Part used: Stem bark Uses: • Ovarian cancer • Lung carcinoma • Gastric & Cervical cancers • Prostate & colon cancer Chemical constituent: • Taxol • Paclitaxel • Docetaxal Taxol TAXOL
  • 18. MOA of Taxanes • These drugs act by interfering with mitotic spindle • They prevent micotubule disassembly into tubulin monomers
  • 19. Camptothecin B. source: Camptotheca acuminata Family: Nyssaceae Part used: Dried stem wood Uses:  Ovarian cancers  Colorectal cancer  Cancer of neck & head  Liver cancer Chemical constituent:  Camptothecin  Topotecan  Irinotecan Camptothecin Topotecan TOPOTECAN Camptotecan
  • 20. MOA of Camptothecin • Camptothecin act by inhibiting topoisomerase-I
  • 21. CONCLUSION • Plants have been a prime source of highly effective conventional drugs for the treatment of many forms of cancer. • The actual compound isolated from the plant may not serve as the drug but leads to the development of potential novel agents. • Natural agents are proving to be an important source of novel inhibitors & have the potential for development into selective anticancer agents.
  • 22. Objectives At the end of lecture student will able to understand  What is cancer  Classification of anticancer drug from plant  Their mode of actions  Also their pharmacognostic features