Research Article Open Access
Srivastava et al., J Proteomics Bioinform 2013, 6:5
http://dx.doi.org/10.4172/jpb.1000269
Research Article Open Access
Proteomics & Bioinformatics
Volume 6(5) 109-124 (2013) - 109
J Proteomics Bioinform
ISSN:0974-276X JPB, an open access journal
Screening and Identification of Salicin Compound from Desmodium
gangeticum and its In vivo Anticancer Activity and Docking Studies with
Cyclooxygenase (COX) Proteins from Mus musculus
Preeti Srivastava
1
*, Vinay K Singh
1
, Brahma Deo Singh
1
, Gaurava Srivastava
2
, Bhuwan B Misra
3
and Vyasji Tripathi
3
1
School of Biotechnology, Faculty of Science, Banaras Hindu University, Varanasi-221005, Uttar Pradesh, India
2
School of Biochemical Engineering, Indian Institute of Technology, Banaras Hindu University, Varanasi-221005, Uttar Pradesh, India
3
Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi-221005, Uttar Pradesh, India
*Corresponding author: Preeti Srivastava, School of Biotechnology, Faculty of
Science, Banaras Hindu University, Varanasi-221005, Uttar Pradesh, India, Tel:
+91-9236060830; Fax: +91- 542-2368693; E-mail: preetibtbhu@gmail.com
Received March 18, 2013; Accepted May 27, 2013; Published May 30, 2013
Citation: Srivastava P, Singh VK, Singh BD, Srivastava G, Misra BB, et al. (2013)
Screening and Identiication of Salicin Compound from Desmodium gangeticum
and its In vivo Anticancer Activity and Docking Studies with Cyclooxygenase (COX)
Proteins from Mus musculus. J Proteomics Bioinform 6: 109-124. doi:10.4172/
jpb.1000269
Copyright: © 2013 Srivastava P, et al. This is an open-access article distributed
under the terms of the Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any medium, provided the
original author and source are credited.
Keywords: Cyclooxygenase; Salicin; Docking; Molecular modeling;
Functional motif; Anti-cancer; Desmodium gangeticum
Abbreviations: COX: Cyclooxygenase; nM: Nanomolar; NSAID:
Nonsteroidal Anti-Inlammatory Drug; DG: Desmodium Gangeticum
Introduction
Plants have been utilized as medicines for thousands of years [1],
initially as crude drugs like tinctures, teas, poultices, powders and
other herbal formulations [1,2]. he identity medicinal plants and
the methods of their use were passed down through oral history, but
eventually this information was recorded in herbals, and subsequently
active compounds were isolated beginning with morphine from opium
in the early 19
th
century [1,3], followed by cocaine, codeine, digitoxin
and quinine [1,4,5]. Isolation and characterization of pharmacologically
active compounds from medicinal plants continue today, and drug
discovery techniques are now being used to standardize herbal
medicines and to elucidate analytical marker compounds. Methods
used to acquire compounds for drug discovery include isolation from
plants and other natural sources, chemical synthesis, combinatorial
chemistry and molecular modeling [6-8]. Drug discovery from
medicinal plants has contributed to cancer treatment, and most new
clinical applications during the last half century relate to cancer [4,5,9].
By 2020, approximately 15 million new cancer cases will be diagnosed,
and 12 million these patients will die [10]. Cancer is caused by both
internal factors such as inherited mutations, hormones, and immune
conditions, and environmental/acquired factors like tobacco, diet,
radiation, and infectious organisms [11]. he attractiveness of natural
compounds as drugs partly stems from their potential ability to
inluence multiple components of the carcinogenesis pathway.
Natural products are typically isolated in quantities insuicient
for lead optimization, lead development, and clinical trials. herefore,
possibilities of their synthesis or semi-synthesis need to be explored
[8,12]. In addition, libraries of natural products and natural-product-
like compounds including their features important for combinatorial
chemistry may be created [13-15].
here are two well established isoforms of the cyclooxigenase (COX)
enzyme that difer in their distribution in the body and in physiological
function. COX-1 is constitutively expressed in normal tissues and it
is involved in maintaining mucosal integrity, platelet aggregation and
gastric cytoprotection [16]. In contrast, COX-2 is not expressed in
normal mucosa, but is expressed very early in response to neoplastic
and inlammatory stimuli, and is extensively overexpressed in diferent
neoplasms, making it an attractive therapeutic target. Besides the
role of COX-2 in the production of inlammatory prostaglandins, its
momentous participation in the initiation/propagation of cancer [17-
21] and in the development of multidrug resistance is well explored
[22,23]. Over-expression of COX-2 probably occurs from the irst
genetically altered cell, through hyperplasia, dysplasia, carcinoma, and
even metastasis of colorectal cancer [24-26]. Number of nonsteroidal
anti-inlammatory drugs (NSAIDs) and selective COX-2 inhibitors
have been investigated for anticancer activities [27-31].
Pharmacological inhibition of COX can provide relief from
inlammation and, as a result, from pain. Non-steroidal anti-
inlammatory drugs, such as aspirin and ibuprofen, exert their efects
through inhibition of COX. Turmeric, ginger, boswellia, hops and some
Abstract
Cancer continues to be a worldwide killer, despite the enormous amount of research and rapid developments
seen during the past decade. It has been suggested that by 2020 more than 15 million new cases of cancer will be
diagnosed. Since it is commonly believed that many are preventable, there is urgent need to identify/develop natural
medicines as effective chemopreventive agents. The purpose of this current study was to assess the effect of isolated
and characterized salicin on cyclooxygenase (COX) proteins by molecular docking studies and by assessments of
the effects of drug-ligand interaction. Salicin isolated from Desmodium gangeticum, a medicinal legume, is a COX
inhibitor. The present study report the extraction, isolation and identiication of salicin and its interaction with COX-1
and COX-2 derivatives, which may be useful for drug-designing for anti-cancer activities. Molecular modeling and
docking studies revealed the binding orientations of salicin into the active sites of COX-1 and COX-2 enzymes.
Extraction, isolation and characterization of the compound 2-(hydroxymethyl) phenyl hexopyranoside, also known as
‘salicin’, from the leaves of D. gangeticum irst time. Anticancer evaluation of salicin in in vivo mice model.