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Identification of Potent Caspase-8 Inhibitors from a Library of Fluorescent Natural Products Screened by an AIEgen-based Light-up Probe
摘要： Fluorescent natural products are a rich source of drugs and chemical probes. But their inborn fluorescence may interfere with the fluorescence-based screening assays. Caspase-8 is a key player in apoptosis. Inhibition of caspase-8 found to be beneficial for inflammatory and neurodegenerative diseases. But its small molecular inhibitors remain sparsely reported. In this study, we firstly developed a caspase-8 targeting light-up probe based on an AIEgen. This fluorescent dye has a Stokes shift of 200 nm which could avoid the inborn fluorescence signal of natural products. When screening a library of 86 fluorescent natural products, we found for the first time Gossypol showed potent inhibition towards caspase-8 in vitro and in situ. This unique kind of light-up probe coupled with colored natural products could be an efficient way in the hit discovery for druggable targets.
关键词： natural product,aggregation-induced emission,inhibitor screening,caspase-8,fluorescence
更新于2025-09-23 15:22:29
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Structural characterization of Argania spinosa Moroccan wooden artifacts during natural degradation progress using infrared spectroscopy (ATR-FTIR) and X-Ray diffraction (XRD)
摘要： The present work is focused on spectroscopic study of four samples of Argan wooden artifact pertaining to the 17th, 18th, 20th and 21st centuries. The objective is to characterize their unknown structures by the study of their non degraded parts and to investigate changes occurred in their degraded parts due to the natural degradation process. Attenuated total re?ectance Fourier transform infrared spectroscopy gauges the presence of many functional groups related to cellulose I and/or II (OH, C–O–C and –CH2), hemicelluloses (particularly C?O (cid:2)1), and lignin (OH phenolic, Car-O and C?Car) and provides qualitative information on the state of wood alteration by informing on the evolution of new former C?O bands. The degree of conversion to carbonyl group, especially quinone or p-quinone at 1650 cm (cid:2)1, is correlated to lignin degradation, while the absence of the C?O acetoxy absorption is ascribable to occurred deterioration in hemicelluloses, and (cid:2)1. X-ray diffraction determines the presence of two forms of cellulose; amorphous cellulose at 18.5(cid:3) 2θ and predominant crystalline cellulose Iβ at 2θ ? 22.6(cid:3) which characterized by an intense peak. The decrease of crystallinity index values con?rms the deterioration level and obvious changes in crystallinity level. However, the microcrystalline structure appears unaltered because no signi?cant changes were observed for calculated cristallite seize. The obtained results depend on the prolonged time of ageing, natural deterioration phenomena, and wood part (internal or external) that is exposed to degradation. The combination of these two methods is useful for an accurate estimation of the degradation level of argan wood.
关键词： Chemistry,Argan wood artifact,XRD,Analytical chemistry,Natural product chemistry,Materials Chemistry,Natural degradation,Archaeology,ATR-FTIR spectroscopy,Crystallinity,Lignocelluloses,Structural characterization,Materials Science,Organic chemistry
更新于2025-09-12 10:27:22
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Rapid syntheses of (?)-FR901483 and (+)-TAN1251C enabled by complexity-generating photocatalytic olefin hydroaminoalkylation
摘要： We report a common strategy to facilitate the syntheses of the polycyclic alkaloids (?)-FR901483 (1) and (+)-TAN1251C (2). A divergent synthetic strategy provides access both natural products through a pivotal spirolactam intermediate (3), which can be accessed on a gram-scale. A photocatalytic olefin hydroaminoalkylation brings together three readily available building blocks and forges the majority of the carbon framework present in 1 and 2 in a single operation, leading to concise total syntheses. The complexity-generating photocatalytic process also provides direct access to novel non-racemic spirolactam scaffolds that are likely to be of interest to early-stage drug discovery programs.
关键词： medicinal chemistry,natural product synthesis,amine synthesis,photoredox chemistry,radical chemistry
更新于2025-09-12 10:27:22