This document discusses several classes of natural anticancer drugs derived from plants, including their plant sources, mode of action, and clinical uses. It describes vinca alkaloids from Catharanthus roseus that block microtubule assembly; podophyllotoxins from Podophyllum species that inhibit topoisomerase; taxanes from Taxus species that interfere with microtubule disassembly; and camptothecins from Camptotheca acuminata that inhibit topoisomerase I. The document concludes that plants have been a major source of effective anticancer drugs and that natural agents show promise as sources of new inhibitors for cancer treatment.

1. PRESENTED BY
Ravi R. Sharma
Gandaki Medical College THC
B.Pharm 2nd year

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
1.
CLASS
Vinca alkaloids
DRUGS
Vincristine
Vinblastine
PLANT SOURCE
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 DNAbases
* 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. Firstagentsthatwere clinicallyusedareVincaalkaloids,Vinblastine(VLB) &
Vincristine(VCR),isolatedfromMadagascarperiwinkle.
2. Two clinically active agents, etoposide (VM 26) & teniposide (VP 16-213),
semi syntheticderivativesofepipodophyllotoxinareusedincancertreatment.
3. The use of variouspartsof T.brevifoliaand otherTaxusspeciesis widelyused in
canertherapy.
4. Anti-cancer drug armamentariumis 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 Camptothecins Taxanes
Vinblastine
Vincristine
Vinorelbine
Teniposide
Etoposide
Irinotecan
Topotecan
Docetaxel
Paclitaxel

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
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.