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UNDER THE GUIDENCE OF:
MRS. D. SANTHI KRUPA
Asst. Professor
DEPT OF PHARMACOLOGY
VIPW
PRESENTED BY:
MEHRAJ. MOHAMMAD
IV yr. B.PHARMACY
A-SECTION
147N1R0024
CONTENTS
INTRODUCTION
HISTORY OF ANTICANCER DRUGS SCREENING
DEFINITION OF CANCER
TYPES OF CANCER
SCREENING METHODS
In vitro methods
In vivo methods
 CONCLUSION
1. INTRODUCTION
Cancer is a group of diseases involving
abnormal cell growth with the potential to invade
or spread to other parts of the body.
Screening methods are important to find the
solid tumor causing specific agents.
Presently, the existing major anticancer drugs
are having both beneficial and cytotoxic effects.
So as to overcome the undesired effects, new
molecules are to be produced, using simple
cheap methods.
3
2. HISTORY OF ANTICANCER DRUG SCREENING
Initial screening and drug development
programs were small in scale.
Ehrlich and Warburg, studies were
conducted on the tumor growth.
In the early 1950s the program had
evaluated more than 300 chemicals and
several hundreds of plant extracts.
4
3. DEFINITION OF CANCER
Cancer is a group of diseases characterized by
uncontrolled growth and spread of abnormal cells. If the
spread is not controlled, it can result in death.
. Cancer is caused by both external factors and
internal factors
. Cancer is treated with surgery, radiation,
chemotherapy, hormone therapy, biological therapy,
and targeted therapy etc.
 
 
 
 
5
4. TYPES OF CANCERS
They are noncancerous
They are removed by
surgery and they don’t
reoccur once they
removed
They can be grown
very large and weigh
pounds sometimes
They are cancerous
and it can invade near
by tissues
They reoccur if they
are removed by surgery
These are more
dangerous than benign
tumors
6
7
ANTICANCER DRUGS GENERAL TARGETS
Directly damage the Pre-DNA molecules
Directly Damage the DNA in the nucleus of the cell
Effect the synthesis or breakdown of the mitotic Spindles
8
5.1TRYPHAN BLUE DYE EXCLUSION ASSAY
Live cells possess intact cell membranes that excludes the dye, where as
dead cells lost membrane integrity take up the dyes
PROCEDURE
Cells are incubated with different concentrations of test
compounds for 4 days.
Dead cells are stained with dyes colors.
Specimen is centrifuged, collected and
observed on microscopic slides.
9
5.2. LDH (LACTIC DEHYDROGENASE) ASSAY
10
5.3 MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium
bromide) ASSAY
11
5.4 XTT (2,3-bis[2-Methoxy-4-nitro-5-sulfophenyl]- 2H-
tetrazolium-5-carboxyanilide salt) ASSAY
12
5.5 SULFORHODAMINE-B ASSAY
13
14
6.6. IN VIVOIN VIVO METHODSMETHODS
6.1 INDUCTION OF EHRLICH ASCITES CARCINOMA
15
6.2 HOLLOW FIBER ASSAY
16
6.3 NEW XENOGRAFT
TUMORS FROM PATIENT TISSUES
Transplant of tumor tissue.
17
Injection of cell suspension
Agitate the cell suspension to prevent the cells from settling, and
withdraw from the sterile tube into a 1-cc TB syringe with the needle
removed.
Lift the skin of the mouse to separate it from the underlying
muscle and inject, with a 21 G needle, 0.1 ml of the cell suspension
(1 × 107
cells) subcutaneously.
Observation
The mice have to be sacrificed to measure tumor volume.
18
6.4 GENETICALLY ENGINEERED CANCER MODELS (GEM)
GEM models have increased understanding of the molecular
pathways responsible for the initiation and progression of human
cancer, and have highlighted the importance of specific oncogenes
and tumor suppressor genes (TSG) in particular types of cancer.
GEM models possess well-validated molecular/genetic
characteristics which ultimately facilitate the rational design of
small molecule therapeutics.
19
7. CONCLUSION
Anticancer drug screening is necessary to prioritize compounds for
further development. In the era of target oriented molecular cancer
therapeutics, screening procedures are tailored towards the specific area.
They however require, careful design and validation. So, knowledge on
this screening methods can lay a path for screening of the novel anticancer
drugs with more selectivity and specificity.
20
8. REFERENCES
•  Kumar V, Abbas AK, Aster JC. Robbins Basic Pathology. 9th ed.
Philadelphia, PA: Saunders. 2013. , Neoplasm; pp. 161–214.
• Talmadge JE, Singh RK, Fidler IJ, Raz A. Murine models to evaluate
novel and conventional therapeutic strategies for cancer. Am J Pathol.,
2007;170:793–804.
• Farber S. Some observations on the effect of folic acid antagonists on acute
leukemia and other forms of incurable cancer. Blood.,1949;4:160–7.
• Elion GB, Singer S, Hitchings GH. Antagonists of nucleic acid derivatives.
VIII. Synergism in combinations of biochemically related
antimetabolites. J Biol Chem., 1954;208:477–88.
21
.
22

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Mehraj

  • 1. UNDER THE GUIDENCE OF: MRS. D. SANTHI KRUPA Asst. Professor DEPT OF PHARMACOLOGY VIPW PRESENTED BY: MEHRAJ. MOHAMMAD IV yr. B.PHARMACY A-SECTION 147N1R0024
  • 2. CONTENTS INTRODUCTION HISTORY OF ANTICANCER DRUGS SCREENING DEFINITION OF CANCER TYPES OF CANCER SCREENING METHODS In vitro methods In vivo methods  CONCLUSION
  • 3. 1. INTRODUCTION Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. Screening methods are important to find the solid tumor causing specific agents. Presently, the existing major anticancer drugs are having both beneficial and cytotoxic effects. So as to overcome the undesired effects, new molecules are to be produced, using simple cheap methods. 3
  • 4. 2. HISTORY OF ANTICANCER DRUG SCREENING Initial screening and drug development programs were small in scale. Ehrlich and Warburg, studies were conducted on the tumor growth. In the early 1950s the program had evaluated more than 300 chemicals and several hundreds of plant extracts. 4
  • 5. 3. DEFINITION OF CANCER Cancer is a group of diseases characterized by uncontrolled growth and spread of abnormal cells. If the spread is not controlled, it can result in death. . Cancer is caused by both external factors and internal factors . Cancer is treated with surgery, radiation, chemotherapy, hormone therapy, biological therapy, and targeted therapy etc.         5
  • 6. 4. TYPES OF CANCERS They are noncancerous They are removed by surgery and they don’t reoccur once they removed They can be grown very large and weigh pounds sometimes They are cancerous and it can invade near by tissues They reoccur if they are removed by surgery These are more dangerous than benign tumors 6
  • 7. 7 ANTICANCER DRUGS GENERAL TARGETS Directly damage the Pre-DNA molecules Directly Damage the DNA in the nucleus of the cell Effect the synthesis or breakdown of the mitotic Spindles
  • 8. 8
  • 9. 5.1TRYPHAN BLUE DYE EXCLUSION ASSAY Live cells possess intact cell membranes that excludes the dye, where as dead cells lost membrane integrity take up the dyes PROCEDURE Cells are incubated with different concentrations of test compounds for 4 days. Dead cells are stained with dyes colors. Specimen is centrifuged, collected and observed on microscopic slides. 9
  • 10. 5.2. LDH (LACTIC DEHYDROGENASE) ASSAY 10
  • 11. 5.3 MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) ASSAY 11
  • 12. 5.4 XTT (2,3-bis[2-Methoxy-4-nitro-5-sulfophenyl]- 2H- tetrazolium-5-carboxyanilide salt) ASSAY 12
  • 14. 14 6.6. IN VIVOIN VIVO METHODSMETHODS
  • 15. 6.1 INDUCTION OF EHRLICH ASCITES CARCINOMA 15
  • 16. 6.2 HOLLOW FIBER ASSAY 16
  • 17. 6.3 NEW XENOGRAFT TUMORS FROM PATIENT TISSUES Transplant of tumor tissue. 17
  • 18. Injection of cell suspension Agitate the cell suspension to prevent the cells from settling, and withdraw from the sterile tube into a 1-cc TB syringe with the needle removed. Lift the skin of the mouse to separate it from the underlying muscle and inject, with a 21 G needle, 0.1 ml of the cell suspension (1 × 107 cells) subcutaneously. Observation The mice have to be sacrificed to measure tumor volume. 18
  • 19. 6.4 GENETICALLY ENGINEERED CANCER MODELS (GEM) GEM models have increased understanding of the molecular pathways responsible for the initiation and progression of human cancer, and have highlighted the importance of specific oncogenes and tumor suppressor genes (TSG) in particular types of cancer. GEM models possess well-validated molecular/genetic characteristics which ultimately facilitate the rational design of small molecule therapeutics. 19
  • 20. 7. CONCLUSION Anticancer drug screening is necessary to prioritize compounds for further development. In the era of target oriented molecular cancer therapeutics, screening procedures are tailored towards the specific area. They however require, careful design and validation. So, knowledge on this screening methods can lay a path for screening of the novel anticancer drugs with more selectivity and specificity. 20
  • 21. 8. REFERENCES •  Kumar V, Abbas AK, Aster JC. Robbins Basic Pathology. 9th ed. Philadelphia, PA: Saunders. 2013. , Neoplasm; pp. 161–214. • Talmadge JE, Singh RK, Fidler IJ, Raz A. Murine models to evaluate novel and conventional therapeutic strategies for cancer. Am J Pathol., 2007;170:793–804. • Farber S. Some observations on the effect of folic acid antagonists on acute leukemia and other forms of incurable cancer. Blood.,1949;4:160–7. • Elion GB, Singer S, Hitchings GH. Antagonists of nucleic acid derivatives. VIII. Synergism in combinations of biochemically related antimetabolites. J Biol Chem., 1954;208:477–88. 21
  • 22. . 22