Toxicology Reports · 2015 · 44 citations · 19 references
MedicineOncologyPharmacologyCancer PharmacologyChemotherapyMolecular OncologyOncology PharmacologyOral Anticancer AgentsAlternative MedicineAnticancer ActivityAnticancer Natural ProductsChemical Structure-activity RelationshipsComplementary Medicine
Flaxseed as well as its oil component possess antitumor activities against different types of cancer and have been used by some patients as complementary and/or alternative medicine. Linoorbitides (LOBs) are one family of flaxseed compounds that has implications for anticancer and antioxidant activity . The cytotoxicity of [1-9-NαC]-linusorb-B3 (LOB3), [1-9-NαC]-linusorb-B2 (LOB2), [1-9-NαC],[1-R s ,S s -MetO]-linusorb-B2 ([MetO]-LOB2) and [1-8-NαC],[1-R s ,S s -MetO]-linusorb-B1 ([MetO]-LOB1) was measured against human breast cancer Sk-Br-3 and MCF7 cell lines and melanoma A375 cell line. Overall cytotoxicity is cell-type specific. It scales as the hydrophobicity and concentration of the LOBs with the most abundant LOB3 being the most cytotoxic. Oral administration of LOB3 as a potential therapeutic agent might not be applicable as a much too high and/or frequent dose would be required to achieve a serum concentration of 400–500 μg/mL due to bioavailability and pharmacokinetic factors. However, LOB3 may be suitable for topical treatment formulations or as a lead compound in developing anticancer LOB derivatives.
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Jianmin Chen, P. Mark Stavro, Lilian U. Thompson · Nutrition and Cancer · 2002 · 200 citations
High-affinity Cyclic Peptide Matriptase Inhibitors
Pedro Quimbar, Uru Malik, Christian P. Sommerhoff et al. · Journal of Biological Chemistry · 2013 · 140 citations · Full text