Tumour Inhibitors From Plants
Tumour Inhibitors From Plants
Tumour Inhibitors From Plants
Plants
Dr. Najam-us-Sahar
TUMOR
• A mass of excess tissue that results from abnormal cell
division.
• Tumors perform no useful body function.
• They may be benign (not cancerous) or malignant
(cancerous).
CANCER
• A term for diseases in which abnormal cells divide
without control.
• Cancer cells can invade nearby tissues and can spread
through the bloodstream and lymphatic system to other
parts of the body.
CANCER
Botanical Source:
The Madagascan periwinkle, is the dried entire plant of
Catharunthus roseus has been variously designated Vinca
rosea and Lochnera rosea.
Family:
Apocynaceae
Vincristine & Vinblastine
• Leurocristine (Vincristine)
• Vinca leukoblastine (Vinblastine)
• First clinically used theraputic drug
• Used for treating a variety of cancers including leukaemia,
lymphomas, advanced testicular cancer, breast and lung
cancer
• Vincristine effective for treating acute childhood leukemia
• Vinblastine has been especially effective for treating
Hodgkin's disease
Uses:
• Mayapple
• Podophyllum peltatum
• Perennial plant in the barberry family (Berberidaceae)
• Well known poisonous plant
• Traditional uses of mayapple:
• Rhizomes dried and ground to a powder
• Powerful purgative
• Also used to treat warts and tumorous growths on the skin
Podophyllotoxin
• Isolated from rhizome of
Podophyllum peltatum
Podophyllum emodi
Its semi synthetic derivatives are used
in the cancer treatment .
• Etoposide :cancer, lymphomas and
leukaemias
• Teniposide: paediatric cancer,
neuroblastoma, brain tumours
• Use in cancer chemotherapy:
• Resin from mayapple rhizomes used in cream to treat cancerous tumors,
polyps and granulations in traditional medicine
• Active Compounds in Rhizome
• Podophyllum peltatum rhizome contains
high concentrations of anticancer lignans and other cmpds
• podophyllotoxin
• a and b peltatin
• Another species - Podophyllum emodii
• podophyllotoxin
• a and b peltatin
• berberine an alkaloid which can be used to treat fevers
(including malaria) and as an antibiotic
• Mode of action of podophyllotoxin:
• Podophyllotoxin acts as a cell poison for cells undergoing mitosis
• Too toxic for chemotherapy use
• Used in creams as treatment for genital warts
• Genital warts caused by HPV (human papillomavirus) associated with
cancers of the genitals (squamous cell carcinomas)
• Side effects of podophyllotoxin:
• Adverse reactions to topical applications include burning,
inflammation
• When the drug was being investigated as a chemotherapy agent, it
caused nausea, vomiting, fever, mouth ulcers, diarrhea, nervous
system problems, seizures, kidney damage, etc.
• Semi-synthetic derivatives:
• Etoposide and teniposide are derivatives of phyllotoxin that are much less toxic and
are safely used in chemotherapy
• Etoposide is much more widely used
• Both compounds block the cell cycle in at least two specific places
• Etoposide Marketed as VePesid or VP-16
• Administered intravenously or orally as liquid capsules
• Widely used to treat various types of cancer
• Testicular cancer which hasn't responded to other treatment
• First-line treatment for small-cell lung cancers
• Used for lymphomas and malignant melanomas
• Side effects of etoposide:
• Major side effects include hair loss, nausea, anorexia, diarrhea, and low leukocyte and
platelet counts
• Some people have severe allergic reactions to the drug
• Can cause genetic damage and may increase a patient's risk of developing leukemia
• Causes fetal damage and birth defects
Harringtonine and Homoharringtonine
•Colchicine
•Demecolcine
•Cholchicoresin
•Fixed oils
•Glucose
•Starch
Uses
•In treatment of gout
•Antirheumatic
•Cathartic
•Analgesic
•In Treatnent of Leukaemia
•Osteoarthritis of knee
• Although colchicine is not clinically used to treat cancer
because of toxicity, it exerts antiproliferative effects
through the inhibition of microtubule formation by
blocking the cell cycle and triggering apoptosis.
• Colchicine can still be used as a lead compound for the
generation of potential anticancer drugs.
• Thus, numerous analogues of colchicine have been
synthesized in the hope of developing novel, useful drugs
with more favourable pharmacological profiles.
• Several colchicine semisynthetics are less toxic than
colchicine and research is being carried out on effective,
less toxic colchicine semisynthetic formulations with
potential drug-delivery strategies directly targeting
multiple solid cancers.
• Colchicine is a plant secondary metabolite extracted
from Colchicum autumnale.
• Several analogs of colchicine were designed and
synthesized namely, 3-demethyl colchicine,
colchicoside, thiocolchicocide that displayed improved
anticancer activity in comparison to native drug against
certain leukemic cells and solid tumors.
• Mechanistically, colchicine inhibits microtubule
polymerization by binding to tubulin, one of the main
constituents of microtubules.
• In another sense, availability of tubulin is necessary to
mitosis; hence colchicine effectively works as a “mitotic
poison” or spindle poison.
Rifamycin antibiotics
• Rifamycins are microbial-derived macrolides that were
isolated in 1957 from the actinomycete Streptomyces
mediterranei, obtained from the soil of the pine forests of
southern France
• Many natural and semisynthetic rifamycins inhibit the
virion RNA-dependent DNA polymerase (RT).
• Rifamycin B was reported active against murine sarcoma
virus (MSV) due to its RT, focus formation and cell
transformation inhibitory activities.
• Rifamycin antibiotics also inhibit the RT of Rauuscher
leukemia virus, preventing its leukomogenic activity
Macrolide antibiotics
• Withanolides
• Present in the whole plant.
• They are believed to be immuno modulators having
anticancer activity
DNA Inhibitors
• Camptothecin
• Inhibit DNA synthesis and replication through enzyme
topoisomerase I
Alkylating agent
• A large number of natural tumor inhibitor acts as
alkylating agent become they posses highly electrophilic
centers and their action is through alkylation of
nucleophilic group in the enzyme that control cell
division.
• Eg; Cucurbitacin, Bruceantin, Triptolide, Elephantopin
• Most of these compounds are cytotoxic killing both
normal and cancer cell.
Some food materials with anti
cancerous property
Green Tea
Strawberry