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A potent betulinic acid analogue ascertains an antagonistic mechanism between autophagy and proteasomal degradation pathway in HT-29 cells
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  • 作者:Debasmita Dutta ; Biswajit Chakraborty ; Ankita Sarkar ; Chinmay Chowdhury…
  • 关键词:Apoptosis ; Autophagy ; Betulinic acid analogue ; Proteasomal pathway
  • 刊名:BMC Cancer
  • 出版年:2016
  • 出版时间:December 2016
  • 年:2016
  • 卷:16
  • 期:1
  • 全文大小:2,236 KB
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  • 作者单位:Debasmita Dutta (1)
    Biswajit Chakraborty (2)
    Ankita Sarkar (1)
    Chinmay Chowdhury (2)
    Padma Das (1)

    1. Cancer Biology and Inflammatory Disorder Division, CSIR-Indian Institute of Chemical Biology, 4 Raja S. C. Mullick Road, Kolkata, 700032, India
    2. Organic and Medicinal Chemistry Division, CSIR-Indian Institute of Chemical Biology, 4 Raja S. C. Mullick Road, Kolkata, 700032, India
  • 刊物主题:Cancer Research; Oncology; Stem Cells; Animal Models; Internal Medicine;
  • 出版者:BioMed Central
  • ISSN:1471-2407
文摘
Background Betulinic acid (BA), a member of pentacyclic triterpenes has shown important biological activities like anti-bacterial, anti-malarial, anti-inflammatory and most interestingly anticancer property. To overcome its poor aqueous solubility and low bioavailability, structural modifications of its functional groups are made to generate novel lead(s) having better efficacy and less toxicity than the parent compound. BA analogue, 2c was found most potent inhibitor of colon cancer cell line, HT-29 cells with IC50 value 14.9 μM which is significantly lower than standard drug 5-fluorouracil as well as parent compound, Betulinic acid. We have studied another mode of PCD, autophagy which is one of the important constituent of cellular catabolic system as well as we also studied proteasomal degradation pathway to investigate whole catabolic pathway after exploration of 2c on HT-29 cells.

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