Citric acid was reacted with α,β-diamines, β-amino thiols and β-amino alcohols to produce fluorescent derivatives of 2-pyridone (QY up to ∼79%). The chemical structures of these compounds were confirmed by analyses of 1D, 2D NMR and ESI-MS data.

A series of new derivatives of N-(2-methoxyphenyl)piperazine have been synthesized for their affinity toward serotonergic receptors and for their potential antidepressant-like activity. They have been evaluated toward receptors 5-HT1A , 5-HT6 , and 5-HT7 , as well as in vivo in the tail suspension, locomotor activity, and motor co-ordination tests. All the tested compounds proved very good affinities toward 5-HT1A and 5-HT7 receptors. The most promising compound was 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride, exhibiting affinity toward receptors Ki <1 nm (5-HT1A ) and Ki = 34 nm (5-HT7 ). Antidepressant-like activity (tail suspension test) was observed at 2.5 mg/kg b.w. (mice, i.p.), and the effect was stronger than that observed for imipramine (5 mg/kg b.w.). Sedative activity was observed at ED50 (locomotor test, mice, i.p.) = 17.5 mg/kg b.w. and neurotoxicity was observed at TD50 (rotarod, mice, i.p.) = 53.2 mg/kg b.w.

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The study compares lyophilized broccoli sprouts and florets in terms of their chemical composition, cytotoxic and proapoptotic potential against hepatocellular carcinoma HepG2, colorectal cancer SW480, and skin fibroblast BJ cells. Sinapic and isochlorogenic acids were predominant phenolics in the sprouts and florets, respectively. The amount of sulforaphane in the sprouts was significantly higher vs. florets. Oleic and linoleic acids dominated in the sprouts, while caproic, stearic and oleic acids in the florets. Broccoli sprouts were selectively cytotoxic on HepG2 and SW480 cells, with proapoptotic effect for the latter, while the florets were less selective, but more active, with profound proapoptotic effect for HepG2 cells (77.4%). Thus, lyophilized broccoli sprouts may be effectively used in dietary chemoprevention.Electronic supplementary materialThe online version of this article (10.1007/s11130-018-0665-2) contains supplementary material, which is available to authorized users.

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