Vinca Alkaloids

1. VINCA

2. CONTENTS:
 SYNONYMS
 BIOLOGICAL SOURCE
 GEOGRAPHICAL SOURCE
 CHEMICAL CONSTITUENTS
 MECHANISM OF ACTION
 ISOLATION AND ESTIMATION OF VINCA
 CHEMICAL TEST
 USES
 MARKETED PRODUCTS

3. Synonyms: Vinca rosea , Catharanthus , Periwinkle, Madagascar
periwinkle
Biological source: Vinca consists of the dried leaves and aerial
parts of Catharanthus roseus belongs to the family Apocyanaceae.
Geographical source: Vinca is indigenous to Madagascar.
Cultivated in India, South Africa , U.S.A. , Europe ,Australia.

4. CHEMICAL CONSTITUENTS:
.Majority of them are Indole and Dihydroindole derivatives.
.Other alkaloids present in vinca are Ajmalicine , Serpentine ,Lochnerine and
Tetrahydroalstonine.

5. CHEMISTRY:

6. MOA:

7. ISOLATION:
Vinca leaves & herb mixed & extracted with aq:alcoholic
acetic acid solution
Aq:extract concentrated & residue further extracted with 2%
HCl
pH adjusted to 4 with NaOH & extracted with benzene
pH raised to 7 & again extracted with benzene (to seperate
alkaloids)
The benzene extract with pH 7 are mixed ,concentrated,dried
Dissolved in benzene –methylene chloride (65:35)

8. Further subjected to chromatographic fractionation on neutral
alumina column with benzene –methylene chloride as eluent(using
glidient elution technique)
Vinblastine rich fraction are evaporated to dryness to yield
vinblastine sulphate which crystallise from alcohol.
Further elution of column give vincristine which is dried and
crystallised from alcohol.

9. IDENTIFICATION:
TLC METHOD-1
•Stationary phase - Silica gel
•Mobile phase - Acetonitrile:Benzene (30:70)
•Detecting agent - 1% solution of Cerric ammonium sulphate in
85% phosphoric acid
•Rf value - 0.39
REFERENCE:
Textbook of pharmacognosy & phytochemistry by Biren shah &
A.K.Seth

10. ESTIMATION OF VINCA:
•A simple reversed-phase liquid chromatographic method .
•Developed for the simultaneous quantitation of the anticancerous drugs
vincristine, vinblastine, and their precursors catharanthine and vindoline .
•By using a Merck Chromolith Performance reversed-phase high-performance
liquid chromatography column.
• A better resolution is obtained in comparison with available particulate-type
C18 columns.
•Chromatography is carried isocratically with a mobile phase of acetonitrile-
0.1M phosphate buffer containing 0.5% glacial acetic acid (21:79, v/v; pH 3.5)
•A flow rate of 1.2 mL/min and UV detection at 254 nm.
REFERENCE:
https://www.ncbi.nlm.nih.gov › pubmed

11. CHEMICAL TEST:
USES:
>Vincristine sulphate is used for acute lymphoid leukemia,small cell lung cancer,cervical & breast
cancer
>Vinblastine sulphate used in the treatment of carcinoma like Testicular carcinoma in combination
with cis platin.
>Treatment of Hodgkin’s & non-Hodgkin’s lymphoma.
>Vinca exhibits hypotensive & antidiabetic actions.
>Administered with Bleomycin & Cis platin for the treatment of metastatic testicular carcinoma.
>Treatment of acute leukemia in children.

12. There are four major vinca alkaloids in clinical use:
Vinblastine (VBL), vinorelbine (VRL), vincristine
(VCR) and vindesine (VDS). VCR, VBL and VRL have
been approved for use in the United States.
 Vinflunine (A novel drug, which is a fluorinated
derivative of vinorelbine) , also a new synthetic
vinca alkaloid, which has been approved in Europe
for the treatment of second-line transitional cell
carcinoma of the urothelium is being developed for
other malignancies.
Vinca alkaloids are the second-most-used class of
cancer drugs and will stay among the original cancer

13. MARKETED PRODUCTS:
DRUG TREATMENT DOSAGE
1. Vinca rosea herbal
tincture
Childhood
leukemia,Hodgkin’s
disease
1-2 ml/ 3 times daily
2.Vincristine liposomal
Brand:MARQIBO
Acute lymphoblastic
leukemia
0.16mg/ml (i.v.)
3.Vinorelbine
Brand:NAVELBINE
Non-small cell lung
cancer
.10mg/ml
.50mg/ml (i.v.)
4.Vinblastine
Brand:VELBAN
Testicular
cancer,Hodgkin’s
disease
.1mg/ml(i.v.)
.10mg(powder inj.)
5.Oncovin
Brand: VINCRISTINE
SULPHATE
Blood disorders,Acute
leukemia
i.v. or infusion