Lemna minor (L. minor), the common duckweed, contains a high protein substance and is considered as a good source of potential bioactive peptides. The objective of this study is to investigate the effect of enzymatic hydrolysis times (60–180 min) and enzyme concentrations (0.5–3.5%v/w) with Alcalase and Flavourzyme on the recovery, hydrolysis degree (DH), and antioxidant properties of peptides derived from defatted L. minor. The protein recovery, hydrolysis degree (DH), and antioxidant activities obtained by enzymatic were compared with the alkaline treatment method. The results showed that the protein recovery, DH values, and antioxidant activities were enhanced by increasing the enzyme concentration and hydrolysis time. Specifically, the recovery of protein and DH values reached the highest level after the enzymatic hydrolysis by Flavourzyme or Alcalase at 1.5 v/w enzyme for 120 min. At the same enzymatic hydrolysis condition, the samples hydrolyzed by Flavourzyme had a higher inhibitory effect on the ABTS•+ and DPPH•+ radical scavenging than those hydrolyzed by Alcalase and the alkaline treatment. Further study also showed that the DH values, amino acid contents, and antioxidant activities of the protein extracts were positively correlated. Thus, the extractions with Flavourzyme and Alcalse were a good method to produce a significant amount of amino acids and smaller peptides.
A multistep synthesis was developed to prepare new 1,2,3-triazole-amino acid conjugates (6 and 7). These compounds contain the diaryl ether moiety and were synthesized via SNAr reaction under mild condition and in good yield. Their structures were confirmed by spectroscopic analyses (HR-MS, NMR, IR). These compounds showed significant antiproliferative activity (>30%) toward the breast MCF7 and liver HepG2 cancer cells lines at <10 µM concentration.
Treatment of the Fmoc‐protected amino alcohol (II), a “so‐called” N,O‐acetal, with TmsCl results in formation of a chloromethylcarbamate intermediate, which reacts with enamines to give β‐amino ketenes and aldehydes.
Trimethylsilyl halide activation of Fmoc-protected N,O-acetals yields reactive intermediates capable of efficiently adding to a variety of enamines. NMR studies have provided evidence that a stable halomethyl carbamate intermediate forms in solution. Good yields are obtained over a broad range of enamine nucleophiles encompassing both cyclic and acyclic ketone-derived and aldehyde-derived enamines. Preliminary studies suggest that the enamine additions occur through a concerted, S(N)2-type mechanism.
Diarylether (DE) is a privileged structure found in both natural products and synthetic compounds including small molecule drugs. We present the synthesis of a series of 13 new DE‐amino acid conjugates which were screened for cancer cells antiproliferation activity. Structure‐activity relationship suggests ester and phenyl groups in DE‐Phe‐OEt 4 c are important for the activity. Compound 4 c inhibited strongly MCF‐7 3D tumor sphere formation and have favourable calculated physical chemical properties according to Lipinski's rule of 5. Docking study suggests estrogen receptor and/ or 3a‐HSD type 3 protein could be the target(s) for anticancer activity of this class of compounds.
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