HERBAL ANTI CANCER DRUGS

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ANTI CANCER AGENTS FROM NATURAL SOURCES:

ANTI CANCER AGENTS FROM NATURAL SOURCES BY TULASI UDAYAGIRI Y13MPPH140005 PHARMACEUTICAL CHEMISTRY KVSR SCOPS VIJAYAWADA

HERBAL ANTI CANCER DRUGS:

HERBAL ANTI CANCER DRUGS

DEFINITION:

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:

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 )

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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 )

MODE OF ACTION OF NATURAL ANTICANCER DRUGS:

MODE OF ACTION OF NATURAL ANTICANCER DRUGS Purine synthesis Pyrimidine synthesis Ribonucleotides Deoxyribonucleotides DNA RNA Enzymes Proteins Microtubles Camptothecin Etoposide Block topoisomerase functions Paclitaxel Vinca Cholchine Inhibit the function of microtubules

VINCA ALKALOIDS:

VINCA ALKALOIDS B. source: Catharanthus roseus Family: Apocynaceae Part used: Dried whole plant Chemical constituent: Vincristine Vinblastine Ajmalicine Vindesine

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VINBLASTINE VINCRISTINE USES : Hodgkin’s disease Lymphomas Carcinoma Breast Testicular tumors USES: Childhood leukemias Childhood tumors- Wilm’s tumor, Neuroblastoma , Hodgkin’s disease

SAR:

SAR The presence of acetyl group is very essential for vinblastine to exhibit it anti cancer activity. When this is hydrolysed activity gets destroyed. When free hydroxyl groups were acetylated the drug lost its antimalignant activity. The potency of vinblastine reduces drastically when the double bonds were initially hydrogenated and finally converted to carbinol group via reduction.

MODE OF ACTION OF VINCA:

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

ADVERSE REACTIONS OF VINCA ALKALOIDS:

ADVERSE REACTIONS OF VINCA ALKALOIDS vincristine : constipation is a commonly seen toxicity. Others include alopesia, skin rashes, azospermia, amenorrhea. Vinblastine : inflammation of GI tract is seen commonly. Nausea ,vomting,alopesia,secrition of anti diuretic hormone, headache ,depression.

PODOPHYLLUM:

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

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PODOPHYLLOTOXIN TENIPOSIDE

MOA OF PODOPHYLLUM:

MOA OF PODOPHYLLUM Acts by inhibiting topoisomerase II These drugs are most active in late S and early G2 phase uses: These are mainly used in the treatment of hard ken's disease. Adverse reactions : leucopenia, thrombocytopenia .

Taxanes:

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

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PACLITAXEL DOCITAXEL

MOA OF TAXANES:

MOA OF TAXANES These drugs act by interfering with mitotic spindle They prevent micotubule disassembly into tubulin monomers

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Uses of paclitaxol : Treatment of breast cancer, ovarian cancer, AIDS-related kaposi sarcoma, treatment of head, neck, oesophageal, cervical, prostate, and bladder cancer. Adverse reactions : hyper sensitivity reactions, bradycardia,which may progess to heart block, allopesia , mucositis , diarrhea .

DOCETAXAL:

DOCETAXAL Uses : treatment of breast cancer and prostate cancer. Treatment of head, neck, gastric, bladder and refractory ovarian cancer. Adverse reactions : peripheral neuropathy, fatigue , fever may occur. And all the adverse reactions that occur with paclitaxol occurs.

CAMPTOTHECIN:

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

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CAMPTOTHECIN

Semi synthetic derivatives of camtothecin:

Semi synthetic derivatives of camtothecin Topotecan and irinotecan are the semi synthetic derivatives of camtothecin . Structures :

MOA OF CAMPTOTHECIN:

MOA OF CAMPTOTHECIN Camptothecin act by inhibiting topoisomerase -I

USES AND ADVERSE REACTIONS OF CAMPTOTHECIN AND ITS DERIVATIVES:

USES AND ADVERSE REACTIONS OF CAMPTOTHECIN AND ITS DERIVATIVES Used in different types of cancers. Irinotecan : irinotecan can be used in combination with 5-FU and leucovorin as first line treatment of metastatic colon cancer. Topotecan : treatment of ovarian cancer, cervical cancer. Adverse drug reactions : Nausea , vomting,diarrhea,abdominal pain,headache,alopecia,elevation of serum transaminases,alkaline phosphates,emisis,allopesia cancer, lung cancer.

ANTICANCER ANTIBIOTICS :

ANTICANCER ANTIBIOTICS Dactinomycin: Source : streptomyces parvulus Structure :

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STRUCTURE OF DAUXORUBICEN

DAUNORUBICIN:

DAUNORUBICIN Structure : Uses : treatment of acuteleukameia, broad spectrum of antibiotic .

IDARUBICIN:

IDARUBICIN Structure : Uses : It is a synthetic drug,granulocytic,lymphocytic,treatment of breast cancer,thyorid cancer, lung cancer. Adverse reaction : cardiac toxicity

STRUCTURAL ACTIVITY RELATIONSHIP:

STRUCTURAL ACTIVITY RELATIONSHIP Intercalation into DNA changes its physical properties. Changes into the substitutions on the actinomycin influence their binding to DNA and make it less effective. Opening of the lactone ring or changing the stereochemistry of an amino acid abolishes the activity. The replacement of the 4 aand 6 methyl groups by the other substituent's reduces its activity. Replacement of the 2 nd amino group by other substituent's decreases the activity .

MECHANISM OF ACTION:

MECHANISM OF ACTION Dactinomycin intercalates into double helical DNA . In the intercalation process the helix unweanse partially to permit the flat phenoxazone chromophore to feed between the successive base pair. In simple it inhibitis the synthesis of DNA dependent ribosomal RNA and DNA synthesis .

USES AND ADVERSE REACTIONS:

USES AND ADVERSE REACTIONS It is used in the treatment of wilhs tumour in children and testicular cancer. Toxic effect: Bone marrow depression. DOXORUBICIN : Source : streptomyces peucitis

OTHER SEMI SYNTHETIC DERIVATIVES:

OTHER SEMI SYNTHETIC DERIVATIVES Structures: Daunomycinol and adriamycinol

:

Many analogs of doxorubicin are prepared by changing the sugar moiety. They are 4-deoxy rubicin,4-epidoxorubicin,4-ortho tetrahydropyranyl doxorubicin which are called as esorubicin, epirubicin, pyrarubicin respectively.

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esorubicin epirubicin pyrarubicin

AUROLIC ACID GROUP OF ANTIBIOTICS:

AUROLIC ACID GROUP OF ANTIBIOTICS These antibiotics contain aurolic acid. They are lipramycin, flicamycin, auluomycin,chromomycin and the related compound. They contain a complex structure consisting of aglycol and 2 carbohydrate rings. The aglycones are tetrahydroanthracene derivatives with phenol hydroxyl group and a vinyl group side chain which is oxygenated. The carbohydrate chains contain either 2,3 or 2,6 dideoxy sugars of novel structure .

Mitomycin :

Mitomycin Structure : It contains urethane,aziridine and quinone nucleus. It acts as alkylating agent due to presence of aziridine nucleus.

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MITHRAMYCIN STREPTOZOCIN

USES AND ADVERSE REACTIONS :

USES AND ADVERSE REACTIONS Uses : Treatment of testicular cancer. Adverse effects: anorexia, thrombocytopenia. STREPTOZOCIN : It belongs to nitrosourea group of anticancer agent. t act mainly by inhibiting DNA. MITHRAMYCIN : It is an aurolicacid derivative. It forms complex with magnesium and calcium metals. It mainly acts by inhibition of RNA synthesis by acting on RNA polymerase enzyme mainly by inhibiting DNA synthesis.

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Bryostatins are a group of macrolide lactones first isolated in the 1960s by George Pettit from extracts of a species of bryozoan , Bugula neritina . The structure of bryostatin 1 was determined in 1982. To date 20 different bryostatins have been isolated. Bryostatins are a potent modulators of protein kinase C . They are currently under investigation as anti- cancer agents and as a memory enhancing agent. ANTI CANCER AGENTS FROM MARINE ORGANISMS

STRUCTURES :

STRUCTURES Bryostatin, dolastatin : Bryostatin

CONCLUSION:

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 devlopment 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

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REFERENCE Internet Williom’s foye

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