New 1,3-Diynoic Derivatives of Natural Lembehyne B: Stereoselective Synthesis, Anticancer, and Neuritogenic Activity

Abstract

An original method has been developed for the synthesis of 1,3-dyine derivatives of natural lembehyne B in high yields (50–67%) and with high selectivity (>98%). The key stage of the synthesis is new Ti-catalyzed cross-cyclomagnesiation of oxygenated and aliphatic 1,2-dienes induced by Grignard reagents. For studying the effect of the structure on the antitumor and neuritogenic activities, a series of lembehyne B analogues with different distances between the terminal hydroxy group and the 1,3-diyne moiety was prepared and tested for neuritogenic activity on mouse neuroblastoma Neuro 2A cells and for cytotoxicity, induction of apoptosis, and effects on the cell cycle using Jurkat, U937, K562, HeLa, and Hek293 tumor cell lines.

Free Fatty Acids from Cow Urine DMSO Fraction Induce Cell Death in Breast Cancer Cells without Affecting Normal GMSCs

“…Various forms of long-chain fatty acids obtained from dietary and natural sources have been explored for their anticancer and antibacterial effects by interfering with known molecular targets such as topoisomerase enzymes [ 48 , 49 , 50 , 51 , 52 ]. In the same line, we propose exploration of the effects of COFFAs with a specific inhibitory role against topoisomerase enzymes, including tetracosanedioic acid, 13Z-docosenoicacid (erucic acid), nervonic acid, 3-hydroxy-tetradecanoic acid, and 3-hydroxycapric acid, which are known as potential anticancer drug targets.…”