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  1. Article ; Online: Synthesis of 4-thiosubstituted flavan derivatives and their hypoglycemic activities.

    Zhang, Xu / Yun, Ju-Ping / Yang, Ya-Nan / Feng, Zi-Ming / Jiang, Jian-Shuang / Yuan, Xiang / Liu, Wei / Zhang, Pei-Cheng

    Fitoterapia

    2022  Volume 161, Page(s) 105255

    Abstract: A series of 4-thiosubstituted flavan derivatives (1-44) were designed and synthesized. The target compounds were assayed for inhibitory activity against α-glucosidase in vitro, and the results indicated that all compounds displayed significant effects in ...

    Abstract A series of 4-thiosubstituted flavan derivatives (1-44) were designed and synthesized. The target compounds were assayed for inhibitory activity against α-glucosidase in vitro, and the results indicated that all compounds displayed significant effects in the range of IC
    MeSH term(s) Acarbose/pharmacology ; Animals ; Glycoside Hydrolase Inhibitors/pharmacology ; Hypoglycemic Agents/pharmacology ; Mice ; Molecular Docking Simulation ; Molecular Structure ; Structure-Activity Relationship ; alpha-Glucosidases/metabolism
    Chemical Substances Glycoside Hydrolase Inhibitors ; Hypoglycemic Agents ; alpha-Glucosidases (EC 3.2.1.20) ; Acarbose (T58MSI464G)
    Language English
    Publishing date 2022-07-28
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 412385-2
    ISSN 1873-6971 ; 0367-326X
    ISSN (online) 1873-6971
    ISSN 0367-326X
    DOI 10.1016/j.fitote.2022.105255
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: A novel ECG analog 4-(S)-(2,4,6-trimethylthiobenzyl)-epigallocatechin gallate selectively induces apoptosis of B16-F10 melanoma via activation of autophagy and ROS.

    Xie, Jing / Yun, Ju-Ping / Yang, Ya-Nan / Hua, Fang / Zhang, Xiao-Wei / Lin, Heng / Lv, Xiao-Xi / Li, Ke / Zhang, Pei-Cheng / Hu, Zhuo-Wei

    Scientific reports

    2017  Volume 7, Page(s) 42194

    Abstract: Autophagy-induced cancer cell death has become a novel strategy for the development of cancer therapeutic drugs. Numerous studies have indicated that green tea polyphenols induce both autophagy and apoptosis in a variety of cancer cells. Here, we ... ...

    Abstract Autophagy-induced cancer cell death has become a novel strategy for the development of cancer therapeutic drugs. Numerous studies have indicated that green tea polyphenols induce both autophagy and apoptosis in a variety of cancer cells. Here, we synthesized a series of green tea polyphenol analogues, among which JP8 was shown to potently activate autophagy. JP8 treatment had a stronger effect on apoptosis in B16-F10 melanoma cells than that in normal AML-12 hepatocytes. JP8 selectively resulted in reactive oxygen species (ROS) accumulation in B16-F10 cells, and this effect was associated with corresponding increases in key components of the ER stress-mediated apoptosis pathway. Pharmacological inhibition of ROS by N-acetyl-L-cysteine (NAC) attenuated JP8-induced autophagy and apoptosis, indicating an upstream role of ROS in JP8-induced autophagy. An in vivo study showed that JP8 had significant antitumor effects in a B16-F10 xenograft mouse model. Our results indicate that JP8 is a novel anticancer candidate with both autophagy and ROS induction activities.
    MeSH term(s) Animals ; Antineoplastic Agents, Phytogenic/chemical synthesis ; Antineoplastic Agents, Phytogenic/isolation & purification ; Antineoplastic Agents, Phytogenic/pharmacology ; Apoptosis/drug effects ; Autophagy/drug effects ; Catechin/analogs & derivatives ; Catechin/chemical synthesis ; Catechin/isolation & purification ; Catechin/pharmacology ; Cell Line ; Cell Line, Tumor ; Endoplasmic Reticulum Stress/drug effects ; Gene Expression Regulation, Neoplastic ; Hepatocytes/cytology ; Hepatocytes/drug effects ; Hepatocytes/metabolism ; Injections, Subcutaneous ; Male ; Melanoma, Experimental/drug therapy ; Melanoma, Experimental/genetics ; Melanoma, Experimental/metabolism ; Melanoma, Experimental/pathology ; Mice ; Mice, Inbred C57BL ; Neoplasm Proteins/genetics ; Neoplasm Proteins/metabolism ; Plant Extracts/chemistry ; Plant Roots/chemistry ; Reactive Oxygen Species/agonists ; Reactive Oxygen Species/metabolism ; Rhodiola/chemistry ; Signal Transduction ; Tumor Burden/drug effects
    Chemical Substances Antineoplastic Agents, Phytogenic ; Neoplasm Proteins ; Plant Extracts ; Reactive Oxygen Species ; Catechin (8R1V1STN48) ; epigallocatechin gallate (BQM438CTEL)
    Language English
    Publishing date 2017-02-10
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/srep42194
    Database MEDical Literature Analysis and Retrieval System OnLINE

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