Journal Articles - Natural Science - 2020

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Browsing Journal Articles - Natural Science - 2020 by Author "Duc-Dung Pham"
  • Publication
    Design and synthesis of new lupeol derivatives and their α-glucosidase inhibitory and cytotoxic activities
    ( 2020)
    Hoang-Vinh-Truong Phan
    ;
    Thuc-Huy Duong
    ;
    Duc-Dung Pham
    ;
    Hoang-Anh Pham
    ;
    Van-Kieu Nguyen
    ;
    Thi-Phuong Nguyen
    ;
    Huu-Hung Nguyen
    ;
    Ngoc-Hong Nguyen
    ;
    Pornpat Sam-ang
    ;
    Kiettipum Phontree
    ;
    Jirapast Sichaem
    were designed, synthesised and evaluated for their a-glucosidase inhibitory and cytotoxic activities. Among synthetic derivatives, lupeol analogues 2b and 2e containing a benzylidene chain exhibited the best activity against a-glucosidase and superior to the positive agent with the IC50 values of 29.4 ± 1.33 and 20.1 ± 0.91 lM, respectively. Lupeol analogues 2d and 3a showed weak cytotoxicity against K562 cell line with the IC50 values of 76.6 ± 2.40 and 94.4 ± 1.51 lM, respectively.
  • Publication
    Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents
    ( 2020)
    Ngoc-Hong Nguyen
    ;
    Van-Giau Vo
    ;
    Hoang-Vinh-Truong Phan
    ;
    Thanh-The Ngo
    ;
    Jirapast Sichaem
    ;
    Thi-Phuong Nguyen
    ;
    Huu-Hung Nguyen
    ;
    Duc-Dung Pham
    ;
    Tien-Cong Nguyen
    ;
    Van-Kieu Nguyen
    ;
    Thuc-Huy Duong
    Twelve benzylidene derivatives, one Baeyer-Villiger oxidative, six imine derivatives were successfully designed and synthesized from phyllanthone. In the search for potential new anti-diabetic agents, phyllanthone along with its benzylidene and oxidation analogues were evaluated for enzyme inhibition against α-glucosidase. In the benzylidene series, most analogues displayed stronger activity than the mother compound. 1c revealed the strongest activity, outperforming the acarbose positive control with an IC50 value of 19.59 μM. Phyllanthone and its derivatives were then tested for cytotoxic activity against the K562 cell line. The imine analogues displayed the most powerful cytotoxic activity with 3c, 3d having IC50 values of 57.55 and 68.02 μM, respectively.