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Novel anticancerous compounds from Sargassum wightii: In silico and in vitro approaches to test the antiproliferative efficacy

S. M. Fazeela Mahaboob Begum , S. Priya , Raji Sundararajan , S. Hemalatha


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.

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