In Silico and In Vitro Studies Evidenced Antcancer Natural Compounds, a
Targetng Chemokine Receptor
Singh Pushpendra and Felix Bast
Centre for Biosciences, Central University of Punjab, Bathinda, Punjab, India
Corresponding author: Singh Pushpendra, Centre for Biosciences, Central University of Punjab, Bathinda, Punjab, India, Tel: 9569330844; E-
mail: pushsingh02@gmail.com
Received: 04 October 2016; Accepted: 15 November 2016; Published: 19 November 2016;
Citaton: Pushpendra S, Bast F. In Silico and in Vitro Studies Evidenced Antcancer Natural Compounds, a Targetng Chemokine Receptor. Ann
Clin Lab Res. 2016, 4: 4.
Abstract
Chemokines are a family of small chemotactc cytokines,
which play a signifcant role in lymphocyte homing to
secondary lymphoid organs in additon to tumor growth
and metastasis. Thus, inhibiton of chemokine receptor
caught atenton for antcancer treatment strategy. We
studied molecular docking of chemokines receptor CXCR2,
CXCR4, and CCR5 against natural and marine compounds.
All selected natural and marine compounds were docked
with the X-ray crystal structure of CXCR2, CXCR4, and
CCR5 retrieved from the PDB by using Maestro 9.6.
Molecular docking was executed by the XP (extra
precision) mode of GLIDE. On the basis of Gscore and
protein-ligand interactons, top-ranking compounds were
outlined. The docking study carried out to summarize the
various Gscore, hydrophobic, electrostatc bond,
hydrogen bond, π-caton and π-π interactons and oversee
the protein-ligand interactons. Moreover, efect of
Epigallocatechin-3-gallate (EGCG) on biological actvity
such as mRNA expression (CXCR2, CCR5, and Bid), cell
proliferaton, ROS, and cell-migraton was reported afer
the 48 hrs treatments in MCF-7 cells. The RT-PCR
densitometric bands analysis showed that compound
EGCG reduced the mRNA expression of CXCR2, CCR5 and
increased the Bid at 40 µM and 80 μM concentraton.
Moreover, EGCG signifcantly reduced cell proliferaton,
ROS generaton and cell-migraton afer 48 hours
treatments.
Keyword: Cancer, Chemokines, Natural and marine
compounds, Maestro 9.6, Molecular docking, In vitro
Introducton
Chemokines are a family of proteins that comprises 44
members in humans, which have a propensity for the
migraton of cells. Chemokines and their receptors,
contributed a signifcant role in physiological functons such as
responses, allowing lymphocyte maturaton, cell survival, cell
proliferaton, and cell-migraton, these movement engaged in
cancer initaton, angiogenesis, tumor growth, and metastasis.
The overexpression of chemokine receptors by blood cancer
and solid tumors augment the possibility of cancer initaton
and progression [1].
CXCR2 predominant chemokine receptor has been
implicated in many cancers including melanoma, breast,
prostate, renal, pancreatc, and esophageal cancer. Targetng
CXCR2 enhances chemotherapeutc response, inhibits the
angiogenesis, and metastasis of breast cancer [2,3]. CXCR4 is
the prime chemokine receptor has been alarmed in many
cancers including melanoma, breast, ovarian, prostate,
pancreatc, colorectal, renal, osteosarcoma, NSCLC, AML, ALL,
multple myeloma [4,5]. Moreover, CXCR2, CXCR4 and CCR5
has a key role in fundamental aspects of cancer, including
proliferaton, migraton, invasion, and angiogenesis [6,7].
Ziconotde, a peptde discovered from marine tropical cone
snail, was approved in the United States in December 2004 for
the treatment of Prialt (Elan Pharmaceutcals). Moreover, in
October 2007, trabectedin (Yondelis; Pharma Mar) became the
frst marine antcancer drug that was approved in the
European Union [8].
Monoclonal antbodies against CXCR2, CXCR4 and CCR5,
have entered into clinical trials for cancer therapy including
MLN1202 and plerixafor [9,10]. Monoclonal antbodies
relatvely have beter optons due to their long half-life in
blood, their ability to establish concrete and high-afnity
interactons with immune cells, together with their
comparatvely low toxicity.
But on the other hand, drugs from monoclonal antbodies
difcult and expensive to develop, in additon to less
convenient to administer than small molecule drugs. Inhibitng
the chemokine ligands/receptors interactons present on the
tumor cells ensued as a new therapeutc approach. MariaVela
2015 reported that CXCR2, CXCR4, and CCR5 chemokine are
most actvated chemokine during the metastases in various
cancer including melanoma, breast cancer, ovarian cancer,
prostate cancer, glioma, neuroblastoma, squamous cell cancer,
head and neck cancer [1]. In this context, receptor-based
molecular docking was performed to identfy multtargeted
inhibitor for chemokine receptor.
Research Article
iMedPub Journals
http://www.imedpub.com/
DOI: 10.21767/2386-5180.1000133
Annals of Clinical and Laboratory Research
ISSN 2386-5180
Vol.4 No.4:133
2016
© Copyright iMedPub | This article is available from: http://www.aclr.com.es/
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