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<p>We screened for active components with antigastric cancer properties in the sappan L. extract (<i>Caesalpinia sappan</i> L.) and evaluated their antitumor effects <i>in vitro</i> and <i>in vivo</i>. Ten different sappan L. extract samples prepared under varying extraction conditions were analyzed, and their constituents were identified using high-performance liquid chromatography. The inhibitory effect of the extracts on human gastric cancer cells (BGC-823) was assessed using the MTT assay. The active ingredients against gastric cancer were identified by analyzing the correlation between changes in the extract composition and their inhibitory effects on BGC-823 cells. The selected active ingredient against gastric cancer was then characterized using infrared spectroscopy. The sappan L. extract sample containing the highest concentration of the selected active ingredient was designated as the experimental sample. The inhibitory effect of the experimental sample on BGC-823 cells and tumor growth in an ectopic transplanted gastric cancer tumor model of BALB/c nude mice was investigated at different doses, time points, and pH levels. Scratch wound healing assay and Transwell assay were also performed to evaluate the effect of the extract on the migration ability of BGC-823 cells. Brazilin was identified as the active ingredient in the sappan L. extract samples with inhibitory potential against gastric cancer. Brazilin exerted a time-dependent inhibitory effect on BGC-823 cells, with enhanced efficacy under alkaline conditions. It also significantly suppressed the migration ability of BGC-823 cells. When brazilin was intraperitoneally injected into tumor-bearing nude mice, it demonstrated a significant inhibition of subcutaneous tumors, with minimal toxicity. Thus, brazilin is a promising therapeutic agent for gastric cancer treatment owing to its anticancer effects.</p>

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Antitumor Potential of Brazilin from the Traditional Chinese Medicine Caesalpinia sappan L. Against Gastric Cancer: An In Vitro and In Vivo Study

  • 期刊论文

  • 发表日期：

    2025年7月1日

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  • Zhang Yiyin,
  • Zhang Yong,
  • He Junfei,
  • Chen Lixia,
  • Zhao Lili,
  • Yang Yongming,
  • Wang Jing,
  • Yan Lei,
  • Zhang Shengwan,
  • Liu Zhongguo,
  • Zhou Liye,
  • Yang Xihua

摘要

We screened for active components with antigastric cancer properties in the sappan L. extract (Caesalpinia sappan L.) and evaluated their antitumor effects in vitro and in vivo. Ten different sappan L. extract samples prepared under varying extraction conditions were analyzed, and their constituents were identified using high-performance liquid chromatography. The inhibitory effect of the extracts on human gastric cancer cells (BGC-823) was assessed using the MTT assay. The active ingredients against gastric cancer were identified by analyzing the correlation between changes in the extract composition and their inhibitory effects on BGC-823 cells. The selected active ingredient against gastric cancer was then characterized using infrared spectroscopy. The sappan L. extract sample containing the highest concentration of the selected active ingredient was designated as the experimental sample. The inhibitory effect of the experimental sample on BGC-823 cells and tumor growth in an ectopic transplanted gastric cancer tumor model of BALB/c nude mice was investigated at different doses, time points, and pH levels. Scratch wound healing assay and Transwell assay were also performed to evaluate the effect of the extract on the migration ability of BGC-823 cells. Brazilin was identified as the active ingredient in the sappan L. extract samples with inhibitory potential against gastric cancer. Brazilin exerted a time-dependent inhibitory effect on BGC-823 cells, with enhanced efficacy under alkaline conditions. It also significantly suppressed the migration ability of BGC-823 cells. When brazilin was intraperitoneally injected into tumor-bearing nude mice, it demonstrated a significant inhibition of subcutaneous tumors, with minimal toxicity. Thus, brazilin is a promising therapeutic agent for gastric cancer treatment owing to its anticancer effects.