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LOGO
Learning Objectives
Learning Objectives are
1. to understand tumor, its types, causes and cell
cycle of normal cell.
2. To learn and comprehend the pharmacognostic
features of various plant and marine derived drugs
having anticancer activity.
3. To know the anti cancer mechanism of these
natural drugs.
4. To have knowledge of various foods increasing
cancer risk and also foods beneficial for health.
Abnormal activation of cellular genes that control
the cell growth and cell mitosis, characterized by
a rapid and uncontrolled formation of abnormal
cells that leads to the formation of mass growth
called tumor.
Abnormal genes are called oncogenes.
When these tumor cells spread though blood to
various organs leading to cancer.
 G1 = growth and preparation of the chromosomes for replication
 S = synthesis of DNA
 G2 = preparation for mitosis
 M = mitosis.
 Genetic factor
 Carcinogens. e.g. tobacco smoking (due to nitro pepridine
agent).
 Certain type of viruses.
 Radiations
 Alcohol
 Pollution
 Diet
LOGO
Catharanthus roseus
Periwinkle, Sadabahar
About 150 alkaloids have now been isolated . 30
indole alkaloids are seen – 20 of which are dimeric indole dihydro
indole type. Many are oncolytic in nature. E.g. Vincristine,
Vinblastine and Ajmalicine.
They are M-phase specific and block
mitosis in metaphase. They bind to microtubular protein, tubulin that
form the mitotic spindle during cell division and block the ability of
tubulin to polymerize. No cell division take place and cell death occur.
Antineoplastic agent which acts by arresting
mitosis at metaphase. Also used in children to
treat leukemia by IV route. In adults, for
treatment of Hodgkin’s disease, reticular cell
lymphosarcoma, myosarcoma etc.
Antineoplastic agents which also acts by stopping
mitosis at metaphase or by interfering with amino
acid metabolism. Suppresses immune mechanism.
Also used In the treatment of lymphomas,
choriocarcinomas, Hodgkin’s lymphoma.
Also exhibits hypotensive and antidiabetic action.
by IV route.
100μg/kg body
weight.
By IV route.
10 – 30 μg/kg by
body weight
Podophyllum peltatum
May apple root, Wild Mandrake.
The active principle is podophylotoxin which is a resin.
 These compounds possesses cytotoxic or antitumor activity, but activity is loss
on mild base treatment.
They are S-phase specific. They form complex
with enzyme Topoisomerase II, which results in single strand breakage of DNA
and thus cell death occur.
Lung cancer
Testicular cancer
Ovarian cell cancer
Leukemia
Brain tumor in children
Etoposide and Taniposide are
semi-synthetic products of
podophylotoxin which are
used in the treatment of
Taxus brevifolia
Pacific Yew.
The plant contains different diterpenoid
derivatives known as . Taxol is predominantly found
in the bark.
 Commercially Taxol is obtained by semisynthetic of
or by cell cultures of Taxus species. Substitution of side
chain has resulted in docetaxol which is more potent than
Taxol and has fewer side effects.
It binds to tubulin and promotes polymerization
and stabilization of polymer rather than disassembly.
 Thus stable microtubules are formed which are non-functional and results in cell
death.
The drug paclitaxel, used in treatment of;
 breast
 Ovarian
 lung cancer
 The cucurbitacins from Marah oreganus is the most
cytotoxic compound known but its narrow index makes
the compound unpromising as therapeutic agents.
 Colchicine from Colchicum autumnale is used as mitotic
poison in plant breeding and its anti-tumor activity are
closely related.
 Colchicine derivates e.g. Demecolcine are being used in
cancer treatment in some countries.
 The anti-tumor activity of Acronycine, an Acridone
alkaloid isolated from Achronychia baueri exhibited a
very broad anti-tumor spectrum.
LOGO
The two prominent US based institutes, namely
US National Cancer Institute(NCI) and US National
Sea Grant Office (NSGO) have discovered many
pure and semi-synthetic compounds derived from
the marine origin that distinctly exhibited
antineoplastic activities against both malignant
tumors and leukemias.
(a). Sinularin:
Sinularin and its derivatives are obtained from Sinularia flexibilis. (A kind of
sponge)
 It possesses anti-cancer activities.
(b). Crassin Acetate:
It is obtained from the Caribbean sponge Pseudoplexaura porose.
 Crassin acetate was observed very toxic to human leukemic cells.
(c). Cytarabine:
It is a synthetic compound based on the knowledge of
naturally occurring moieties found in the Caribbean sponges .
 It is indicated in both adult and childhood leukemia.
(d). Aplysistatin:
It is obtained from the Aplysia angasi. (Spotted sea hare)
 It is used as Antineoplastic agent.
Reading Material
1. Trease and Evans’ Pharmacognosy, William C. Evans,
George E. Trease, Daphne Evans, 16th ed., Illustrated
Elsevier Health Sciences Division Publisher (2009).
2. Tyler V.E., Brady E.R. and Robbers J.E. Pharmacognosy,
9th ed., Lea & Febiger, Philadelphia
3. Biologically Active Natural Products: Pharmaceuticals,
Horace G. Cutler, Eds., Illustrated
Edition, CRC Press Publisher, New York (2000).

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Anti-tumor drugs PPT Dr. Shahid Rasool.ppt

  • 2. Learning Objectives Learning Objectives are 1. to understand tumor, its types, causes and cell cycle of normal cell. 2. To learn and comprehend the pharmacognostic features of various plant and marine derived drugs having anticancer activity. 3. To know the anti cancer mechanism of these natural drugs. 4. To have knowledge of various foods increasing cancer risk and also foods beneficial for health.
  • 3. Abnormal activation of cellular genes that control the cell growth and cell mitosis, characterized by a rapid and uncontrolled formation of abnormal cells that leads to the formation of mass growth called tumor. Abnormal genes are called oncogenes. When these tumor cells spread though blood to various organs leading to cancer.
  • 4.  G1 = growth and preparation of the chromosomes for replication  S = synthesis of DNA  G2 = preparation for mitosis  M = mitosis.
  • 5.  Genetic factor  Carcinogens. e.g. tobacco smoking (due to nitro pepridine agent).  Certain type of viruses.  Radiations  Alcohol  Pollution  Diet
  • 8. About 150 alkaloids have now been isolated . 30 indole alkaloids are seen – 20 of which are dimeric indole dihydro indole type. Many are oncolytic in nature. E.g. Vincristine, Vinblastine and Ajmalicine. They are M-phase specific and block mitosis in metaphase. They bind to microtubular protein, tubulin that form the mitotic spindle during cell division and block the ability of tubulin to polymerize. No cell division take place and cell death occur.
  • 9. Antineoplastic agent which acts by arresting mitosis at metaphase. Also used in children to treat leukemia by IV route. In adults, for treatment of Hodgkin’s disease, reticular cell lymphosarcoma, myosarcoma etc. Antineoplastic agents which also acts by stopping mitosis at metaphase or by interfering with amino acid metabolism. Suppresses immune mechanism. Also used In the treatment of lymphomas, choriocarcinomas, Hodgkin’s lymphoma. Also exhibits hypotensive and antidiabetic action. by IV route. 100μg/kg body weight. By IV route. 10 – 30 μg/kg by body weight
  • 10. Podophyllum peltatum May apple root, Wild Mandrake.
  • 11. The active principle is podophylotoxin which is a resin.  These compounds possesses cytotoxic or antitumor activity, but activity is loss on mild base treatment. They are S-phase specific. They form complex with enzyme Topoisomerase II, which results in single strand breakage of DNA and thus cell death occur.
  • 12. Lung cancer Testicular cancer Ovarian cell cancer Leukemia Brain tumor in children Etoposide and Taniposide are semi-synthetic products of podophylotoxin which are used in the treatment of
  • 14. The plant contains different diterpenoid derivatives known as . Taxol is predominantly found in the bark.  Commercially Taxol is obtained by semisynthetic of or by cell cultures of Taxus species. Substitution of side chain has resulted in docetaxol which is more potent than Taxol and has fewer side effects.
  • 15. It binds to tubulin and promotes polymerization and stabilization of polymer rather than disassembly.  Thus stable microtubules are formed which are non-functional and results in cell death.
  • 16. The drug paclitaxel, used in treatment of;  breast  Ovarian  lung cancer
  • 17.  The cucurbitacins from Marah oreganus is the most cytotoxic compound known but its narrow index makes the compound unpromising as therapeutic agents.  Colchicine from Colchicum autumnale is used as mitotic poison in plant breeding and its anti-tumor activity are closely related.  Colchicine derivates e.g. Demecolcine are being used in cancer treatment in some countries.  The anti-tumor activity of Acronycine, an Acridone alkaloid isolated from Achronychia baueri exhibited a very broad anti-tumor spectrum.
  • 18. LOGO
  • 19. The two prominent US based institutes, namely US National Cancer Institute(NCI) and US National Sea Grant Office (NSGO) have discovered many pure and semi-synthetic compounds derived from the marine origin that distinctly exhibited antineoplastic activities against both malignant tumors and leukemias.
  • 20. (a). Sinularin: Sinularin and its derivatives are obtained from Sinularia flexibilis. (A kind of sponge)  It possesses anti-cancer activities.
  • 21. (b). Crassin Acetate: It is obtained from the Caribbean sponge Pseudoplexaura porose.  Crassin acetate was observed very toxic to human leukemic cells.
  • 22. (c). Cytarabine: It is a synthetic compound based on the knowledge of naturally occurring moieties found in the Caribbean sponges .  It is indicated in both adult and childhood leukemia.
  • 23. (d). Aplysistatin: It is obtained from the Aplysia angasi. (Spotted sea hare)  It is used as Antineoplastic agent.
  • 24.
  • 25.
  • 26.
  • 27. Reading Material 1. Trease and Evans’ Pharmacognosy, William C. Evans, George E. Trease, Daphne Evans, 16th ed., Illustrated Elsevier Health Sciences Division Publisher (2009). 2. Tyler V.E., Brady E.R. and Robbers J.E. Pharmacognosy, 9th ed., Lea & Febiger, Philadelphia 3. Biologically Active Natural Products: Pharmaceuticals, Horace G. Cutler, Eds., Illustrated Edition, CRC Press Publisher, New York (2000).