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Jagadeesh Nagarajappa Masagalli Melanayakanakatte Kuberappa BasavanaGowda Hee-Sung Chae Won Jun Choi 《Molecules (Basel, Switzerland)》2021,26(5)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key factor in several cardiovascular diseases, as it is responsible for the elevation of circulating low-density lipoprotein cholesterol (LDL-C) levels in blood plasma by direct interaction with the LDL receptor. The development of orally available drugs to inhibit this PCSK9-LDLR interaction is a highly desirable objective. Here, we report the synthesis of naturally occurring moracin compounds and their derivatives with a 2-arylbenzofuran motif to inhibit PCSK9 expression. In addition, we discuss a short approach involving the three-step synthesis of moracin C and a divergent method to obtain various analogs from one starting material. Among the tested derivatives, compound 7 (97.1%) was identified as a more potent inhibitor of PCSK9 expression in HepG2 cells than berberine (60.9%). These results provide a better understanding of the structure–activity relationships of moracin derivatives for the inhibition of PCSK9 expression in human hepatocytes. 相似文献
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Susanna Gorrasi Andrea Franzetti Roberto Ambrosini Francesca Pittino Marcella Pasqualetti Massimiliano Fenice 《Molecules (Basel, Switzerland)》2021,26(5)
The “Saline di Tarquinia” salterns have been scarcely investigated regarding their microbiological aspects. This work studied the structure and composition of their bacterial communities along the salinity gradient (from the nearby sea through different ponds). The communities showed increasing simplification of pond bacterial diversity along the gradient (particularly if compared to those of the sea). Among the 38 assigned phyla, the most represented were Proteobacteria, Actinobacteria and Bacteroidetes. Differently to other marine salterns, where at the highest salinities Bacteroidetes dominated, preponderance of Proteobacteria was observed. At the genus level the most abundant taxa were Pontimonas, Marivita, Spiribacter, Bordetella, GpVII and Lentibacter. The α-diversity analysis showed that the communities were highly uneven, and the Canonical Correspondence Analysis indicated that they were structured by various factors (sampling site, sampling year, salinity, and sampling month). Moreover, the taxa abundance variation in relation to these significant parameters were investigated by Generalized Linear Models. This work represents the first investigation of a marine saltern, carried out by a metabarcoding approach, which permitted a broad vision of the bacterial diversity, covering both a wide temporal span (two years with monthly sampling) and the entire salinity gradient (from the nearby sea up to the crystallisation ponds). 相似文献
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建立了激光致声的产生和测量系统,对蒸馏水、酒精和甘油中的激光致声进行测量分析,分别计算了这3种透明液体在体积模量(0.2~7.0 GPa)、动力粘性系数(0.001~30.000 Pa·s)和所吸收激光脉冲能量(10~400 mJ)变化时对应的激光致声的相关数值。实验和数值计算结果表明:激光致声的主频、峰值声压和声能随着透明液体体积模量的增加而增加;激光致声的峰值声压和声能随着动力粘性系数的增加而减小,随着击穿区所吸收的激光脉冲能量的增加而增加;动力粘性系数和击穿区所吸收的激光脉冲能量对主频的影响不明显。 相似文献