FS-7 inhibits MGC-803 cells growth in vitro and in vivo via down-regulating glycolysis

Deng, Xin; Li, Zhongli; Xiong, Runde; Liu, Juan; Liu, Renbo; Peng, Junmei; Chen, Yanming; Lei, Xiaoyong; Cao, Xuan; Zheng, Xiaohui; Xie, Zhizhong; Tang, Guotao

doi:10.1016/j.biopha.2018.11.001

Cited by 6 publications

(5 citation statements)

References 59 publications

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“…In our previous study, the synthesized flavonoid derivatives containing a trimethoxy group showed the expected target inhibition and anti-tumor activity in vivo and in vitro. [22][23][24][25]30 Here, we further introduced bioactive indole and salicylic acid and synthesized two trimethoxy-flavone derivatives with salicylic acid-modified indole substituents. In the screening of several cell lines, compound 8f showed significant antiproliferative activity against human hepatoma cell lines HepG-2 and SMMC-7721, with IC 50 values of 4.63 ± 1.13 μM and 3.11 ± 0.35 μM, respectively, while it showed low cytotoxicity against human normal hepatocyte LO2.…”

Section: Discussionmentioning

confidence: 99%

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Synthesis and anti-hepatocellular carcinoma evaluation of salicylic acid-modified indole trimethoxy flavonoid derivatives

et al. 2023

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Section: Discussionmentioning

confidence: 99%

“…2A). [22][23][24][25] To further expand the exploration of this strategy, the anti-tumor activity of the classic NSAID acetylsalicylic acid (aspirin) was noted. Among them, salicylic acid and acetate salicylic acid have also been reported to reduce the level of glycolysis in tumor cells by inhibiting PFK in glycolysis.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and anti-hepatocellular carcinoma evaluation of salicylic acid-modified indole trimethoxy flavonoid derivatives

et al. 2023

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“…There are many small molecule drugs that inhibit the progression of gastric cancer by targeting HIF [ 74 , 126 , 127 , 128 , 129 , 130 , 131 , 132 , 133 , 134 , 135 , 136 , 137 ]. Unfortunately, although so many small molecule drugs have been found to inhibit the progression of gastric cancer through HIF, none of them can be used clinically, so more basic and clinical researches are needed.…”

Section: Small Molecule Drugs Targeting Hif To Inhibit Gastric Cancermentioning

confidence: 99%

“…Yun-Ning Huang et al exhibited that dextran sulfate (DS) could inhibit EMT in gastric cancer cells by inhibiting the expression of HIF [125]. There are many small molecule drugs that inhibit the progression of gastric cancer by targeting HIF [74,[126][127][128][129][130][131][132][133][134][135][136][137]. Unfortunately, although so many small molecule drugs have been found to inhibit the progression of gastric cancer through HIF, none of them can be used clinically, so more basic and clinical researches are needed.…”

Section: Small Molecule Drugs Targeting Hif To Inhibit Gastric Cancermentioning

confidence: 99%

HIF in Gastric Cancer: Regulation and Therapeutic Target

Guan

Yang

et al. 2022

Molecules

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HIF means hypoxia-inducible factor gene family, and it could regulate various biological processes, including tumor development. In 2021, the FDA approved the new drug Welireg for targeting HIF-2a, and it is mainly used to treat von Hippel-Lindau syndrome, which demonstrated its good prospects in tumor therapy. As the fourth deadliest cancer worldwide, gastric cancer endangers the health of people all across the world. Currently, there are various treatment methods for patients with gastric cancer, but the five-year survival rate of patients with advanced gastric cancer is still not high. Therefore, here we reviewed the regulatory role and target role of HIF in gastric cancer, and provided some references for the treatment of gastric cancer.

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“…In addition, the chemical structures of the above VADs all have trimethoxy‐substituted benzene rings, which caught our attention (Figure 1). Based on the combination principles, we previously designed flavonoid derivatives with trimethoxy groups, FB‐15 and FS‐7 (Figure 2a) (Deng et al, 2017, 2019, 2020; Z. Wang et al, 2018), which downregulated β3‐tubulin, HIF‐1α, and glycolysis‐related HKII or PFKP kinases, respectively. And they exhibited significant antitumor activity in vitro and in vivo.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and antitumor evaluation of trimethoxyflavonoid with arylurea structure against hepatocellular carcinoma

Sun

Yin

Zhao

et al. 2023

Drug Development Research

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Simultaneous targeting of tumor vasculature and inhibitors of tumor cell glycolysis may be a promising antitumor strategy. Here, we reported the total synthesis and biological evaluation of A-ring arylurea flavonoid derivatives with B-ring trimethoxy group, which exhibited potent antitumor activity against a variety of tumor cells in vitro. Most of the derivatives showed in vitro antitumor activity on HepG-2, HGC-27, MDA-MB-231, and A549 cells. Among them, compounds 8e, 8f, 8g, 8h, 8j, and 8l also exhibited significant anti-proliferation effects on liver tumor cell subtypes BEL-7402 and SMMC-7721. Compound 8l had the lowest IC 50 value (5.61 ± 0.39 μM) on HepG-2 cells, and showed the effects of inhibiting colony formation, arresting the cell cycle in G 0 /G 1 phase, and inducing apoptosis in a concentration-dependent manner. In addition, the toxicity of compound 8l on human normal cells LO2 and GES-1 was lower than that of sorafenib. The inhibitory effects of compound 8l on the expression of glycolytic rate-limiting enzymes HKII, PFK-1, PKM2 and vascular endothelial growth factor were further evaluated.Corresponding reduction in intracellular lactate was also detected after compound 8 treatment. Our results support an antitumor strategy targeting tumor vasculature and glycolysis to discover and develop a new generation of antitumor drugs.

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FS-7 inhibits MGC-803 cells growth in vitro and in vivo via down-regulating glycolysis

Cited by 6 publications

References 59 publications

Synthesis and anti-hepatocellular carcinoma evaluation of salicylic acid-modified indole trimethoxy flavonoid derivatives

Synthesis and anti-hepatocellular carcinoma evaluation of salicylic acid-modified indole trimethoxy flavonoid derivatives

HIF in Gastric Cancer: Regulation and Therapeutic Target

Design, synthesis, and antitumor evaluation of trimethoxyflavonoid with arylurea structure against hepatocellular carcinoma

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