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• W2986049319 endingPage "111839" @default.
• W2986049319 startingPage "111839" @default.
• W2986049319 abstract "The ligustrazine - betulin derivative (TB), TB amino acids derivatives (TB-01 — TB-09) and TB dipeptide derivatives (TB-10 — TB-18) were designed and synthesized. And their in vitro cytotoxic activities were evaluated against four cancer cell lines (Hela, HepG2, BGC-823 and HT-29) and normal cells MDCK by standard methylthiazol tetrazolium (MTT) assay. Most of them demonstrated better antitumor activity than the relevant material betulin. Among them, compound TB-01 showed the best anti-tumor effect on the cancer cells and the lowest toxicity on the normal cells. For example, the cytotoxicity of TB-01 against the cancer cells (mean IC50 = 4.86 ± 1.16 μM) was 3-fold higher than that against the normal cells MDCK (IC50 = 16.11 ± 2.29 μM). Moreover, TB-01 showed better cytotoxic than positive drug cisplatin (DDP) on tumor cells. Besides, the Zebrafish toxicity evaluation test showed that TB-01 demonstrated high biosafety. Subsequently, fluorescent staining, apoptosis detection and cell cycle analysis indicated that TB-01 induced early apoptosis in HepG2 cells and blocked the cell cycle in the G1 phase. In addition, the structure-activity relationships of these derivatives were briefly discussed." @default.
• W2986049319 created "2019-11-22" @default.
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• W2986049319 date "2020-01-01" @default.
• W2986049319 modified "2023-10-16" @default.
• W2986049319 title "Design, synthesis, and biological evaluation of ligustrazine - betulin amino-acid/dipeptide derivatives as anti-tumor agents" @default.
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• W2986049319 doi "https://doi.org/10.1016/j.ejmech.2019.111839" @default.
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