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Article

Potential Anticancer Lipoxygenase Inhibitors from the Red Sea-Derived Brown Algae Sargassum cinereum: An In-Silico-Supported In-Vitro Study

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Department of Pharmacology, College of Pharmacy, Jouf University, Sakaka 72341, Aljouf, Saudi Arabia
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Department of Pharmacognosy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62511, Egypt
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Department of Botany and Microbiology, Faculty of Science, South Valley University, Qena 83523, Egypt
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Department of Pharmacognosy, College of Pharmacy, Jouf University, Sakaka 72341, Saudi Arabia
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Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Cairo 11371, Egypt
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Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72341, Saudi Arabia
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Clinical Pharmacology Department, Faculty of Medicine, Beni-Suef University, Beni-Suef 62511, Egypt
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Department of Pharmacognosy, Faculty of Pharmacy, Modern University for Technology and Information, Cairo 11371, Egypt
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Department of Clinical Pharmacy, College of Pharmacy, Jouf University, Sakaka 72341, Aljouf, Saudi Arabia
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Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
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Department of Pharmacognosy, Faculty of Pharmacy, Nahda University, Beni-Suef 62513, Egypt
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Department of Pharmacognosy, Faculty of Pharmacy, Minia University, Minia 61519, Egypt
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Department of Pharmacognosy, Faculty of Pharmacy, Deraya University, 7 Universities Zone, New Minia 61111, Egypt
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Health Sciences Research Unit, Jouf university, Sakaka 72341, Aljouf, Saudi Arabia
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Mohamed-Elamir F. Hegazy, Paul W. Pare and Ahmed Atef El-Beih
Antibiotics 2021, 10(4), 416; https://doi.org/10.3390/antibiotics10040416
Received: 27 March 2021 / Revised: 6 April 2021 / Accepted: 7 April 2021 / Published: 10 April 2021
LC-MS-assisted metabolomic profiling of the Red Sea-derived brown algae Sargassum cinereum “Sargassaceae” dereplicated eleven compounds 111. Further phytochemical investigation afforded two new aryl cresol 1213, along with eight known compounds 1421. Both new metabolites, along with 19, showed moderate in vitro antiproliferative activity against HepG2, MCF-7, and Caco-2. Pharmacophore-based virtual screening suggested both 5-LOX and 15-LOX as the most probable target linked to their observed antiproliferative activity. The in vitro enzyme assays revealed 12 and 13 were able to inhibit 5-LOX more preferentially than 15-LOX, while 19 showed a convergent inhibitory activity toward both enzymes. Further in-depth in silico investigation revealed the molecular interactions inside both enzymes’ active sites and explained the varying inhibitory activity for 12 and 13 toward 5-LOX and 15-LOX. View Full-Text
Keywords: Sargassum cinereum; metabolic profiling; aryl cresols; docking; 5-LOX; 15-LOX; virtual screening; in silico Sargassum cinereum; metabolic profiling; aryl cresols; docking; 5-LOX; 15-LOX; virtual screening; in silico
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MDPI and ACS Style

Alzarea, S.I.; Elmaidomy, A.H.; Saber, H.; Musa, A.; Al-Sanea, M.M.; Mostafa, E.M.; Hendawy, O.M.; Youssif, K.A.; Alanazi, A.S.; Alharbi, M.; Sayed, A.M.; Abdelmohsen, U.R. Potential Anticancer Lipoxygenase Inhibitors from the Red Sea-Derived Brown Algae Sargassum cinereum: An In-Silico-Supported In-Vitro Study. Antibiotics 2021, 10, 416. https://doi.org/10.3390/antibiotics10040416

AMA Style

Alzarea SI, Elmaidomy AH, Saber H, Musa A, Al-Sanea MM, Mostafa EM, Hendawy OM, Youssif KA, Alanazi AS, Alharbi M, Sayed AM, Abdelmohsen UR. Potential Anticancer Lipoxygenase Inhibitors from the Red Sea-Derived Brown Algae Sargassum cinereum: An In-Silico-Supported In-Vitro Study. Antibiotics. 2021; 10(4):416. https://doi.org/10.3390/antibiotics10040416

Chicago/Turabian Style

Alzarea, Sami I., Abeer H. Elmaidomy, Hani Saber, Arafa Musa, Mohammad M. Al-Sanea, Ehab M. Mostafa, Omnia Magdy Hendawy, Khayrya A. Youssif, Abdullah S. Alanazi, Metab Alharbi, Ahmed M. Sayed, and Usama Ramadan Abdelmohsen. 2021. "Potential Anticancer Lipoxygenase Inhibitors from the Red Sea-Derived Brown Algae Sargassum cinereum: An In-Silico-Supported In-Vitro Study" Antibiotics 10, no. 4: 416. https://doi.org/10.3390/antibiotics10040416

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