ANTICANCER ACTIVITY

OF INDOLE-3-CARBINOL
[I3C] DERIVATIVES

SUBHRADIP ROYCHOWDHURY* & SATARUPA

BHATTACHARJEE**
*M.PHARM 1ST YEAR [PHARMACEUTICAL CHEMISTRY] DEPT. OF PHARM. SC.
BIRLA INSTITUTE OF TECHNOLOGY, MESRA-835215
** B.PHARM 4TH YEAR GURU NANAK INSTITUTE OF PHARMACEUTICAL SCIENCE AND
TECHNOLOGY, KOLKATA-114

DEFINITION , TYPES AND CAUSES OF CANCER

Cancer known medically as a malignant neoplasm, is a broad group of diseases involving uncontrolled ,
abnormal cell proliferation

GENESIS OF CANCER

HISTORICAL BACKGROUND OF USE OF I3C

If a cancerous ulcer appears upon the breasts, apply a crushed cabbage

leaf and it will make it well.

- Roman statesman, Cato the Elder [234-149 BC]

Crushing or chewing cabbage leaves causes 72% reduction in risk of breast

cancer and also reduces developing prostate and pancreatic cancer.

SOURCES OF I3C
Primarily found in

cruciferous
vegetables.
Family : Cruciferae.
Genus : Brassica.

DERIVATIVES OF I3C

CHEMICAL PROFILE OF I3C

Oral consumption of Cruciferous vegetables

Glucobrassicin ,a glucosinolate
Myrosinase in plant cell
stomach

Indole-3-glucosinolate
Acid autohydrolysis in

Condensed oligomeric derivatives majorly

DIM,ICZ & LTr1

Modulates the metabolism of carcinogens, such as Benzopyrene, Aflatoxin B 1.
Inhibits activation of various transcription factors.
Anticancer agent for both hormone responsive and triple negative breast tumors.

PROTEIN TARGETS OF
ACTIVITIES
ASSIGNED TO I3C I3C DERIVATIVE DIM

DIM

Di Indolyl Methane

ESTROGEN METABOLISM,
CANCER AND I3C

I3C increases the urinary excretion ratio of 2-hydroxyestrone to 16 alpha

hydroxyestrone.
Inhibits the 4-hydroxylation of estradiol.
Increases 2-hydroxylation keeping away 16 alpha hydroxylation of

estradiol via induction of two isoenzymes CYP4501A1 and CYP4501A2.

DISEASES THAT CAN BE TREATED

WITH I3C
Breast cancer
Lung cancer
Liver cancer
Leukaemia
Cervical cancer
Prostate cancer
Colon cancer
Hepatotoxicity
Systemic lupus erythematosus
In management of HSV
Recurrent respiratory papillomatosis

DOSE AND SAFETY DATA OF

I3C DERIVATIVES
PREGNANCY

AND

LACTATION

Safety has not been

established.
DRUG INTERACTION :
Tamoxifen [Synergistic in Breast Cancer]
Antacids and PPI are contraindicated [As they will prevent acid

condensation to form ICZ]

DOSE : Dosage ranges from 400 mg to 800 mg daily.

CONCLUSION
So from here it can be concluded that
Consumption

of

Indole-3-carbinol,

component

of

cruciferous vegetables, has incredible potential both for

prevention and for treatment of cancer.
While being cytoprotective for the normal cells, it is an

apoptotic agent for the tumor cells.

This potential of Indole-3-carbinol should be further

explored both alone and in combination with various

chemotherapeutic agents for the treatment of cancer.

REFERENCES
Aggarwal et al; Molecular Targets and Anticancer Potential of Indole-3-

Carbinol and Its Derivatives; [Cell Cycle 4:9, 1201-1215; September

2005];2005 Landes Bioscience.
farmacists.blogspot.in/2009/05/indole-3-carbinol-novel-approach-to.html cited

on 26.09.2013
Bardlow H.L. et al; Long-term responses of women to indole-3-carbinol or a

high fibre diet; Cancer Epidemiol Biomarkers Prev 1994;3:591-595.

cancerres.aacrjournals.org/content/67/16/7815.long cited on 26.09.2013
ncbi.nlm.nih.gov/pubmed/22110194 cited on 26.09.2013

THANK YOU