Flavonoids from Capsella bursa-pastoris and their hepatoprotective activities in vitro

Two new flavonoids (1 and 2), named 4′,7-dihydroxy-5-hydroxymethyl-8-prenylflavonoid and 4′,7-dihydroxy-5-hydroxymethyl-6,8-diprenylflavonoid, together with seven known flavonoids (3–9) were isolated from the aerial parts of Capsella bursa-pastoris (L.) Medik., Brassicaceae, for the first time. The chemical structures of the purified compounds (1–9) were identified by their spectroscopic data and references. Moreover, compounds (1–9) were evaluated for their hepatoprotective activities against d-galactosamine induced toxicity in WB-F344 cells by using a MTT colorimetric method. As a result, compounds 2, 3, 6, and 9 (10 μM) exhibited moderate hepatoprotective activities. Keywords: 5-Hydroxymethyl flavonoid, NMR, HR-ESI-MS, Spectral data, In vitro, Hepatoprotective activit

Development of novel salicylic acid–donepezil–rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease

AbstractAlzheimer’s disease (AD) is a chronic, progressive brain degenerative disease that is common in the elderly. So far, there is no effective treatment. The multi-target-directed ligands (MTDLs) strategy has been recognised as the most promising approach due to the complexity of the pathogenesis of AD. Herein, novel salicylic acid–donepezil–rivastigmine hybrids were designed and synthesised. The bioactivity results exhibited that 5a was a reversible and selective eqBChE inhibitor (IC50 = 0.53 μM), and the docking provided the possible mechanism. Compound 5a also displayed potential anti-inflammatory effects and significant neuroprotective effect. Moreover, 5a exhibited favourable stabilities in artificial gastrointestinal solution and plasma. Finally, 5a demonstrated potential cognitive improvement in scopolamine-induced cognitive dysfunction. Hence, 5a was a potential multifunctional lead compound against AD

Antiangiogenic phenylpropanoid glycosides from <i>Gynura cusimbua</i>

<p>A new phenylpropanoid glycoside, named <i>α</i>-L-rhamnopyranosyl-(1↔2)-<i>β</i>-D-[4″-(8<i>E</i>)-7-(3,4-dihydroxyphenyl)-8-propenoate, 1″-O-(7<i>S</i>)-7-(3,4-dihydroxyphenyl)-7-methoxy-ethyl]-glucopyranoside (<b>1</b>), together with nine known compounds (<b>2–10</b>) were isolated from the active fraction (<i>n</i><b>-</b>Butanol fraction) of <i>Gynura cusimbua</i> for the first time. The known compounds (<b>2–10</b>) were identified as phenylpropanoid glycosides on the basis of extensive spectral data and references. The antiangiogenic activities of compounds (<b>1–10</b>) were evaluated by MTT assay on HUVECs and wild-type zebrafish <i>in vivo</i> model assay. As a result, compounds <b>1</b>, <b>6</b>, <b>7</b>, <b>8</b> and <b>10</b> exhibited certain antiangiogenic activities.</p

Design, synthesis and evaluation of quinoline-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease

AbstractA series of novel quinoline-O-carbamate derivatives was rationally designed for treating Alzheimer’s disease (AD) by multi-target-directed ligands (MTDLs) strategy. The target compounds were synthesised and evaluated by AChE/BuChE inhibition and anti-inflammatory property. The in vitro activities showed that compound 3f was a reversible dual eeAChE/eqBuChE inhibitor with IC50 values of 1.3 µM and 0.81 µM, respectively. Moreover, compound 3f displayed good anti-inflammatory property by decreasing the production of IL-6, IL-1β and NO. In addition, compound 3f presented significant neuroprotective effect on Aβ25-35-induced PC12 cell injury. Furthermore, compound 3f presented good stabilities in artificial gastrointestinal fluids, liver microsomes in vitro and plasma. Furthermore, compound 3f could improve AlCl3-induced zebrafish AD model by increasing the level of ACh. Therefore, compound 3f was a promising multifunctional agent for the treatment of AD

Cobalt/Copper-Cocatalyzed Synthesis of Imidazo[1,2‑<i>a</i>:3,4‑<i>a</i>′]dipyridiniums from 2<i>H</i>‑[1,2′-Bipyridin]-2-ones and 2‑Bromoacetophenones

A cobalt/copper-cocatalyzed facile synthesis of imidazo­[1,2-<i>a</i>:3,4-<i>a</i>′]­dipyridiniums from 2<i>H</i>-[1,2′-bipyridin]-2-ones and 2-bromoacetophenones is presented. This strategy provides an alternative to the imidazo­[1,2-<i>a</i>:3,4-<i>a</i>′]­dipyridinium synthesis by employing readily available substrates and a simple procedure, which would render this method potentially useful in organic synthesis