• Vincristine and vinblastin are important alkaloidal phytoconstituents isolated from the plant of Vinca Catharanthus roseus L,

• Family: Apocynaceae

• The Flower may be white, violet or rose in colour.

• The alkaloids isolated from the vinca plant are generally referred to as Vinca alkaloids.

• The Root may contain more amounts of alkaloids (0.15-1.795 %).

• More than 100 alkaloids of the indole group are present in the plant of which 25 are dimeric in nature.

• Vincristine and vinblastine are also dimeric in nature and uses for the treatment of human neoplasm.

Extraction and Semisynthesis of Vinblastin:

1. Dry leaf powder of the Vinca was extracted with 0.1M HCl for half an hour in an ultrasonic bath, centrifuge the mixture for 10 minutes at 2000 rpm.

2. Obtained sediment is re-extracted with more quantity of HCl.

3. Mix both supernatant and filter it.

4. Treat this filtrate with petroleum ether to remove lipophilic compound and chlorophyll.

5. Separate the acidic fraction and treat it with an alkaline solution (pH 10.5) of 10 %in embonic acid add slowly for the precipitate of alkaloid.

6. Increase the pH up to 5.0. separate the precipitate with decantation and this precipitate can be used for the semisynthesis of vinblastin.

7. Mix this precipitate with 0.1M HCl and 0.1 M Citric acid and cool the mixture from 0 to - 5°C using dichloromethane and ice bath.

8. Slowly add 30 % aqueous hydrogen peroxide, 10 % aqueous sodium hypochlorite and 1 % solution of sodium borohydride in methanol for three to five hours.

9. Increase the pH of the mixture up to 9.5, collect the organic layer stepwise and dry it.

Production of Vincristine Sulphate:

1. Dried homogenous ground material treated with dilute tartaric acid was extracted with benzene.

2. Concentrate the benzene extract and perform the steam distillation.

3. The benzene will be separated as distillate and the residue will be left out. Dissolve the residue in methanol and treat it with dilute tartaric acid solution.

4. Perform the distillation.

5. The methanol will separate as distillate and treat the bottom product with dilute solution of ammonia.

6. Extract it and then evaporate the extract to dryness.

7. Dissolve the dry powder and separate the vincristine sulphate by chromatographic method by using alumina column and eluted with benzene, benzene + chloroform, chloroform and chloroform + methanol.

8. Vincristine will be isolated and treat it with sulphuric acid, vincristin sulphate will be obtained.

Estimation:

• Vincristin and vinblastin sulphate are estimated with the help of HPLC.

• The following solution are prepared for the estimation:

• Solution 1: 0.1 percent w/v of the substance being examine.

• Solution 2: Contain 0.2 percent w/v each of vinblastine sulphate RS and vincristine sulphate RS solution.

• Solution 3, 4 and 5: 0.1 percent w/v, 0.002 percent w/v and 0.0001 w/v respectively of vinblastin sulphate (if vinblastin estimated) or vincristin sulphate (if vincristin sulphate estimated).

• Column: Packed with stationary phase LC2.

• Flow rate: 1.0 ml/min. Mobile phase: (For vinblastin)

• Mixture of 70 volume of methanol 30 volume of 1.5 percent w/v of diethylamine (pH adjusted 7.5 with phosphoric acid).

• Detection wavelength: (For vinblastin sulphate) 297 nm.

• Mobile phase: (For vincristin sulphate) Mixture of 50 volume of methanol 38 volume of 1.5 percent w/v of diethylamine (pH adjusted 7.5 with phosphoric acid) 12 volume of acetonitrile.

• Detection wavelength: (For vincristin sulphate) 262 nm.

Utilization:

• Vinblastin sulphate should be store in the refrigerator otherwise it may be unstable.

• It is available in sealed ampoules.

• The vinblastin sulphate is highly used in the treatment of neoplasm, lymphocytic lymphoma, hodgkin’s disease, testicular carcinoma.

• Vinblastin can show its potency in its individual form but generally, it is dispensed in a combination of other drugs to improve its therapeutic efficacy.

• It is dispensed through intravenous route by considering other factors like body surface, patient age, WBC count etc.

• Vincristine sulphate is also available in the ampoule and stored in the refrigerator to improve its stability.

• It is also useful in lymphosarcoma, small cell lung cancer, neuroblastoma, hodgkin’s disease, cervical and breast cancer.

Vincristine and vinblastine have the following utilisations:

• These alkaloids show antimitotic activity which inhibits cell growth.

• They disrupt the microtubules which cause the dissolution of cell mitotic spindle and the growth of cell arrest in metaphase

• Vincristine is included in the CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) chemotherapy regimen for treating non - Hodgkin’s lymphoma.

• It is also a part of MOPP (mustargen, oncovin, procarbazine, and prednisone), COPP (cyclophosphamide, oncovin, procarbazine, and prednisone), and BEACOPP (bleomycin, etoposide, doxorubicin, cyclophosphamide, vincristine, procarbazine, and prednisone ) regimens in Hodgkin’s lymphoma.

• In acute lymphoblastic leukaemia and nephroblastoma, it is part of the less popular Stanford V chemotherapy regimen.

• It is given in combination with prednisone to relief childhood leukaemia.

• It is also an immunosuppressant, hence used in the treatment of Thrombotic Thrombocytopenic Purpura (TTP) or chronic Idiopathic Thrombocytopenic Purpura (ITP).

• Vinblastine is included in the ABVD (Adriamycin, bleomycin, vinblastine, and dacarbazine) chemotherapy regimen for Hodgkin’s lymphoma.

• It is also prescribed in histiocytosis.