272 © 2017 Journal of Advanced Pharmacy Education & Research | Published by SPER Publications
Introduction
Lung cancer is the major cause of cancer mortality worldwide
accounting for 1.5 million deaths in 2012.
[1]
It constitutes 13% of the
newly diagnosed cancer cases in 2015.
[2]
Among the major two types
of lung cancer, the non-small cell lung cancer (NSCLC) contributes to
80% of lung cancer deaths, which urges the need for novel therapies
in the effective treatment and management of NSCLC.
[3]
ABSTRACT
Non-small cell lung cancer (NSCLC) contributes to 80% of lung cancer death. The poor survival rate is contributed by the uncontrolled
proliferation, evasion of apoptosis, ubiquitous expression of cell survival genes, and resistance to anticancer therapies.This prompts the search
for novel and potent drugs for the effective treatment and management of NSCLC. Marine seaweeds are rich in novel bioactives widely
employed in pharma, medical, cosmetic, and food industries. For the current study, the ethyl acetate extract of Sargassum wightii is utilized
to test antiproliferative efficacy against the NSCLC cell line A549. From ethyl acetate extract, two compounds, namely, n-hexadecanoic acid
and l-(+)-ascorbic acid 2,6 dihexadecanoate were identified by mass spectrometry analysis.These compounds interacted with the cell survival
protein PI3K which is upregulated in most of human cancers. The in silico results demonstrated that the algal compounds interacted with the
target PI3K with a C score of 5. The in vitro antiproliferative activity of the ethyl acetate extract was analyzed by MTT assay. The apoptotic
hallmarks including fragmentation of nuclei and DNA were observed in treated cells.The real-time polymerase chain reaction analysis of gene
encoding PI3K showed the downregulation of the gene. The current results suggest that the compounds of S. wightii have antiproliferative
activity and can control lung cancer through induction of apoptosis.
Keywords: Non-small cell lung cancer, Sargassum wightii, antiproliferative property, n-hexadecanoic acid, l–(+)-ascorbic acid 2, 6
dihexadecanoate
Novel anticancerous compounds from Sargassum
wightii: In silico and in vitro approaches to test the
antiproliferative effcacy
S. M. Fazeela Mahaboob Begum
1
, S. Priya
1,2
, Raji Sundararajan
3
, S. Hemalatha
1
1
School of Life Sciences, B.S. Abdur Rahman University, Chennai, Tamil Nadu, India,
2
Xinovem, Golden Jubilee Biotech Park, Chennai, India,
3
School of Engineering
Technology, Purdue University, West Lafayette, IN 47907, USA
Correspondence: S. Hemalatha, School of Life Sciences, B.S. Abdur Rahman University, Chennai, Tamil Nadu, India. E-mail: hemalatha.sls@bsauniv.ac.in
Apoptosis or programed cell death maintains the balance between
cell proliferation and cell death. Uncontrolled proliferation results
in oncogenesis. In NSCLC cell lines, the deletion or inactivation of
the tumor suppressor genes directly contributes to the uncontrolled
proliferation and prolonged survival of cancer cells.
[4]
Hence, drugs
that can inhibit uncontrolled proliferation and induce apoptosis may
be effective in the management and treatment of cancer.
A number of FDA-approved anticancer drugs are derived from the
sea, including cytarabine, eribulin mesylate, and trabectedin. This
has triggered the pharmaceutical industries to focus on marine
natural products, and many marine bioactives have entered into the
pre-clinical and clinical trials.
[5]
Marine seaweeds are a rich source
in novel bioactives, which are widely employed in pharma, medical,
cosmetic, and food industries. The marine brown algae of genus
Sargassum is reported to possess antithrombotic, antiplatelet, antiviral,
and anticancer properties.
[6-8]
In the current study, the marine brown
algae Sargassum wightii was extracted, and the phytoconstituents were
analyzed for the antiproliferative efficacy against the NSCLC cell line
How to cite this article: Begum SMFM, Priya S, Sundararajan R, Hemalatha S. Novel
anticancerous compounds from Sargassum wightii: In silico and in vitro approaches to test the
antiproliferative efficacy. J Adv Pharm Edu Res 2017;7(3):272-277.
Source of Support: Nil, Conflict of Interest: None declared.
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Original Article