ISSN: 0975 -8542
Journal of Global Pharma Technology
Available Online at: www.jgpt.co.in
RESEARCH ARTICLE
©2009-2019, JGPT. All Rights Reserved 1
Synthesis, Characterization and Preliminary Cytotoxic Study of
Sinapic Acid and its Analogues
Yasser Fakri Mustafa
Department of Pharmaceutical Chemistry, College of Pharmacy/University of Mosul-41002, Mosul, Iraq.
Abstract
The use of natural products to treat human diseases especially cancer is an interesting trend in
pharmaceutical research. Sinapic acid, being a member of hydroxycinnamic acid family and having well-
established pharmacological properties, could have a potential antitumor activity that has not been
investigated sufficiently. This work aimed to test the preliminary cytotoxic effect of sinapic acid and nine
of its synthesized analogues utilizing MTT assay on four cancer cell lines; which are: HeLa, AMN3, SKG,
and MCF-7. The chemical structures of the intermediates and of the synthesized products were
approving by analyzing their IR,
1
H-NMR,
13
C-NMR, and MS-ESI spectra. Results of the cytotoxicity
study indicated that sinapic acid analogues 3a, 3c, 3d, 3e and 3h have lower IC50 values than that of
positive control on the tested cancer cell lines, while sinapic acid itself and the other synthesized
analogues did not have such cytotoxic effect.
Keywords: Sinapic acid, Analogues, Gastrodigenin, MTT, Cytotoxicity.
Introduction
Cancer is a foxy disease that can start and
progress without any warning. This,
combined with the difficulty of its treatment,
makes cancer a serious global health problem
that can strike anyone at any time [1].
Cancer is a condition in which the cellular
monitoring of apoptosis is lost leading to
uncontrolled proliferation of cells. This
results in the formation of neoplastic tumor
that starts benign until its progression to the
malignancy as it metastasizes to other
tissues or organs [2].Utilization of natural
products for management of various human
disorders including cancer became an
interesting area of research in the last
decades [3]. Phytochemicals with antitumor
activity can exert their effect through
different mechanisms such as induction of
apoptosis, inhibition of topoisomerase I or II,
and modification of cellular metabolism
[4].Phenolic compounds are a group of key
secondary metabolites found mainly in the
plant kingdom and they have a wide
spectrum of physiological activities [5]. One
of the most interesting classes of such
compounds is a hydroxycinnamic acids
family, to which sinapic, p-coumaric, ferulic,
vanillic and caffeic acids belong [6]. Sinapic
acid (Figure 1) is frequently found in human
diet because of its high prevalence in many
vegetables (e.g. white onion), fruits (e.g.
lemon), cereal grains (e.g. rice) and herbs
(e.g. borage). Like other members of its
family, sinapic acid is naturally found in the
free form or as a glycoside [7].
HO
OCH
3
H
3
CO COOH
3,5-dimethoxy-4-hydroxycinnamic acid
Fig. 1: Chemical structure of sinapic acid