Design, synthesis and structure–activity relationship of novel semi-synthetic flavonoids as antiproliferative agents
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Flavones
Structure–activity relationship
Objective:To determine the contents of total flavones in the leaves and branches of Lonicera nuwranthoides of different ages in Chongqing. Methods:UV spectrophotometry. Results:Abundant flavone substances were found to exist in the leaves and branches of L. nuwranthoides. The leaves contained more flavones than the branches,and the young leaves contained more flavones than the older leaves. Significant differences were observed between the leaves of different ages and branches of different ages in their flavone contents. The content of total flavones was also significantly different between different plants. Conclusion:The leaves and branches of L. nuwranthoides have great value for development and exploitation.
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Flavanone
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Seven naturally occurring flavones oxygenated at C-2', C-4' and C-5' in ring B were synthesized, together with their isomers, to confirm the proposed structures. The synthesized flavones 1, 2, 3a, 5, 7 and 8 were identical with the corresponding natural flavones, but 4a was not. The spectral properties of these flavones are discussed.
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Pim kinases play a key role in the regulation of signaling pathways including proliferation, migration, and metabolism and are a potential target for cancer therapy. A series of 5-benzylidenethiazolidine-2,4-diones were synthesized as pim kinase inhibitors. The structure–activity relationships (SAR) of the analogues in inhibiting in vitro pim kinase activity as well as the proliferation of leukemia cell lines were examined. SAR studies indicated that a hydroxyl group at the 2-position of the benzene ring of 5-benzylidenethiazolidine-2,4-dione plays an important role in the inhibitory activity against all three pim kinases and replacement with a pyrazinyl group at the 5-position of the benzene ring of 5-benzylidenethiazolidine-2,4-dione improved activity significantly. The compounds exerted anti-proliferative activity against the three leukemia cell lines we tested. The most potent compound, 5i, had an EC50 value of 0.8 µM in the MV4-11 cell line. The result of kinase profiling indicated that compound 5i was highly selective for pim-kinases.
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Thiazolidine
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Flavones are an important class of bioactive constituents in foods, and their structural diversity enables them to interact with different targets. In particular, flavones are known for their anti-inflammatory activity. Herein, we summarized commonly applied in vitro, in vivo, and clinical models in testing anti-inflammatory activity of flavones. The anti-inflammatory structure–activity relationship of flavones was systematically mapped and supported with cross comparisons of that with flavanones, flavanols, and isoflavones. Hydroxyl groups (−OH) are indispensable for the anti-inflammatory function of flavones, and −OH at the C-5 and C-4′ positions enhance while −OH at the C-6, C-7, C-8, and C-3′ positions attenuate their activity. Moreover, the C2–C3 single bond, −OH at the C-3 and B-ring positions undermine flavone aglycones' activity. Most of the flavone aglycones function through NF-κB, MAPK, and JNK-STAT pathways, and their possible cell binding targets are kinase, aryl hydrocarbon receptor (AhR), G-protein coupled receptors, and estrogen receptors. However, the structure and anti-inflammatory activity relationship of flavones were unclear, and further research shall be conducted to close the gap in order to guide development of evidence-based functional foods.
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Structure–activity relationship
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The content of flavones in the extract of Panpax notoginseng was measured and the species of flavones were identified. The results showed that 75% ethanol was an appropriate solvent for extracting flavones from Panpax notoginseng. It was found that there was 0.015mg/mL of flavones in the extract measured on the base of rutin as standard sample. With color reaction, it was identified that the species of flavones in the extract were flavanones.
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As the chief activity component,lotus flavoneshave beenone of the hot points of healthy products research.The research compared the effect of 5 kinds of resins of X-5,HP-20,NKA,AB-8 and HPD-100.The results showed that HP-20 was the best one.Its static absorbtion was 68.90 mg/g resin.The rate of desorption was 87.23%.The research optimized the technique parameters systematically of HP-20 separating lotus flavones.The results showed that the saturated absorption of lotus flavones by HP-20 was 15 BV of lotus flavone of 7 mg/mL concentration.The concentration of lotus flavones could reach 62.06% desorbed by 40% ethanol for one times when the concentration of the added lotus flavones was 200 mg/mL and the speed of desorption was 2 BV/h.The rate of lotus flavones desorbed by 40% ethanol was 81.40% and the total rate of desorbed lotus flavones was 98.17%.The concentration of lotus flavones can reach to 98.87% if they are separated for several times.
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Lotus effect
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The anti-oxidation study for Raspberry flavones had shown that Raspberry flavones could clear up OH-,H2O2 and DPPH in vitro.The strength of order of clearance as follow: the flavones after purifying the flavones after second extraction the flavones after crude extract.The flavones after purifying could obviously hold back oxidation of peanut oil.The anti-oxidation effect of 0.2% flavones in peanut was better than 0.02% BHT.
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Blowing a raspberry
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Flavonols
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