Abstract：
:Inspired by the well-documented tumor protecting ability of paullones, recently, we synthesized novel paullone-like scaffolds, indole-fused benzo-oxazepines (IFBOs), and screened them against hepatocellular carcinoma (HCC) specific Hep-G2 cells. Three of the synthesized compounds significantly attenuated the progression of HCC in vitro. By computational studies, we further discovered that IFBOs exhibited a stable binding complex with the IL-6 receptor. In this context, we investigated in vivo study using the nitrosodiethyl amine (NDEA)-induced HCC model, which strengthened our previous findings by showing the blockade of the IL-6 mediated JAK2/STAT3 oncogenic signaling pathway. Treatment with IFBOs showed remarkable attenuation of cellular proliferation, as evidenced through a decrease in the number of nodules, restoration of body weight, oxidative stress parameters, liver marker enzymes and histological architecture. Interestingly, using a metabolomic approach we further discovered that IFBOs can restore the perturbed metabolic profile associated with the HCC condition to normalcy. Particularly, the efficacy of compound 6a for an anti-HCC response was significantly better than the marketed chemotherapeutic drug, 5-fluorouracil. Altogether, these remarkable findings open up possibilities of developing IFBOs as novel future candidate molecules for plausible alternatives for HCC treatment.
journal_name
Sci Repjournal_title
Scientific reportsauthors
Singh AK,Bhadauria AS,Kumar U,Raj V,Rai A,Kumar P,Keshari AK,Kumar D,Maity B,Nath S,Prakash A,Saha Sdoi
10.1038/s41598-018-24288-0subject
Has Abstractpub_date
2018-04-12 00:00:00pages
5932issue
1issn
2045-2322pii
10.1038/s41598-018-24288-0journal_volume
8pub_type
杂志文章abstract：:Intrasynovial tendon injuries are among the most challenging in orthopedics. Despite significant improvements in operative and rehabilitation methods, functional outcomes continue to be limited by adhesions, gap formation, and rupture. Adhesions result from excessive inflammation, whereas tendon gapping and rupture re...
journal_title：Scientific reports
pub_type： 杂志文章
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更新日期：2018-07-23 00:00:00
abstract：:Although attempts have been made to reveal the relationships between bacteria and human health, little is known about the species and function of the microbial community associated with oral diseases. In this study, we report the sequencing of 16 metagenomic samples collected from dental swabs and plaques representing...
journal_title：Scientific reports
pub_type： 杂志文章
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pub_type： 已发布勘误
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pub_type： 杂志文章
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更新日期：2016-07-20 00:00:00
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pub_type： 杂志文章
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更新日期：2017-02-20 00:00:00
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pub_type： 杂志文章,收录出版
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pub_type： 杂志文章,meta分析
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