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1.辽宁中医药大学第一临床学院(辽宁 沈阳 110847)
2.辽宁中医药大学附属医院肛肠科(辽宁 沈阳 110032)
3.辽宁中医药大学附属医院普外科(辽宁 沈阳 110032)
张文星,男,博士研究生,主要从事中医治疗大肠癌的临床与研究工作
高允海,主任医师,教授,博士研究生导师; E-mail: lnzy123n@126.com
收稿:2025-10-03,
纸质出版:2026-06-10
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张文星,高允海.基于网络药理学和裸鼠体内实验探讨补脾胃泻阴火升阳汤通过HIF⁃1α调节糖酵解途径抗结肠癌的机制[J].上海中医药杂志,2026,60(6):16-26.
ZHANG Wenxing,GAO Yunhai.Explorating mechanism of Bupiwei Xieyinhuo Shengyang Decoction in treating colon cancer via HIF⁃1α⁃mediated regulation of glycolytic pathway based on network pharmacology and nude mouse in vivo experiments[J].Shanghai Journal of Traditional Chinese Medicine,2026,60(6):16-26.
张文星,高允海.基于网络药理学和裸鼠体内实验探讨补脾胃泻阴火升阳汤通过HIF⁃1α调节糖酵解途径抗结肠癌的机制[J].上海中医药杂志,2026,60(6):16-26. DOI: 10.16305/j.1007-1334.2026.z20251003001.
ZHANG Wenxing,GAO Yunhai.Explorating mechanism of Bupiwei Xieyinhuo Shengyang Decoction in treating colon cancer via HIF⁃1α⁃mediated regulation of glycolytic pathway based on network pharmacology and nude mouse in vivo experiments[J].Shanghai Journal of Traditional Chinese Medicine,2026,60(6):16-26. DOI: 10.16305/j.1007-1334.2026.z20251003001.
目的
2
通过网络药理学结合体内实验,探讨补脾胃泻阴火升阳汤治疗结肠癌的作用机制。
方法
2
①利用TCMSP、GeneCards、OMIM、DrugBank数据库搜索补脾胃泻阴火升阳汤活性成分和结肠癌相关靶点,采用STRING平台构建蛋白质-蛋白质相互作用(PPI)网络,并进行基因本体(GO)和京都基因和基因组数据库(KEGG)富集分析。②60只BALB/C裸鼠皮下注射人结肠癌HCT-116细胞建立结肠癌模型,随机分为模型组、中药组(20.93 g·kg
-1
)、西药组(卡培他滨:390 mg·kg
-1
)、中药联合西药组(中药:20.93 g·kg
-1
;卡培他滨:390 mg·kg
-1
)。并对各组裸鼠给予相应药物灌胃,共干预2周。监测裸鼠肿瘤生长情况,测量各组瘤体质量;采用苏木精-伊红(HE)染色法观察裸鼠肿瘤组织病理改变;利用免疫组织化学(免疫组化)技术检测肿瘤组织中缺氧诱导因子-1α(HIF-1α)、葡萄糖转运蛋白1(GLUT1)、己糖激酶2(HK2)以及乳酸脱氢酶A(LDHA)蛋白的表达;借助Western blot和逆转录实时定量聚合酶链反应(RT-qPCR)技术检测肿瘤组织中HIF-1α、GLUT1、HK2、LDHA蛋白及mRNA的表达。
结果
2
①筛选获得补脾胃泻阴火升阳汤与结肠癌的交集基因共141个。其中,肿瘤蛋白p53、蛋白激酶B1(AKT1)、表皮生长因子受体(EGFR)和HIF-1α等可能是补脾胃泻阴火升阳汤治疗结肠癌的关键靶点。其作用机制主要涉及p53、血管内皮生长因子(VEGF)、缺氧诱导因子-1(HIF-1)等信号通路。②与模型组相比,HE染色及免疫组化结果显示,各药物干预组肿瘤组织均出现不同程度的细胞破裂与坏死现象,Western blot检测结果显示,各药物干预组肿瘤组织中HIF-1α
、
GLUT1、HK2以及LDHA蛋白的表达水平均显著降低(
P
<
0.05);RT-qPCR检测结果显示,西药组和中药联合西药组肿瘤组织中
LDHA
的mRNA表达水平,以及各药物组肿瘤组织中
HIF
-
1α
、
GLUT1
和
HK2
的mRNA表达水平均显著降低(
P
<
0.05)。与模型组和中药组相比,中药联合西药组肿瘤组织的破坏程度更显著,肿瘤组织中HIF-1α
、
GLUT1、HK2以及LDHA蛋白的表达水平降低(
P
<
0.05)。
结论
2
补脾胃泻阴火升阳汤应用后可协同抑制糖酵解,从而抑制结肠癌移植瘤的生长,其机制可能与下调HIF-1α表达,抑制糖酵解中的GLUT1、HK2以及LDHA关键酶的表达有关。
Objective
2
To investigate the mechanisms of Bupiwei Xieyinhuo Shengyang Decoction (BpwXyhSyD) in treating colon cancer through network pharmacology combined with
in vivo
experiments.
Methods
2
①Using TCMSP, GeneCards, OMIM, and DrugBank databases to search for active ingredients and colon cancer-related targets of BpwXyhSyD, a protein-protein interaction (PPI) network was constructed using the STRING platform, while Gene Ontology(GO)and Kyoto Gene and Genome Database (KEGG) enrichment analysis were performed. ②Sixty BALB/C nude mice were subcutaneously injected with human colon concer HCT-116 cells to establish a colon cancer model and randomly divided into four groups: model group, traditional Chinese medicine (TCM) group (20.93 g·kg
-1
), Western medicine group (capecitabine: 390 mg·kg
-1
), and combined TCM-Western medicine group (TCM: 20.93 g·kg
-1
; capecitabine: 390 mg·kg
-1
). Mice in each group received corresponding drug interventions for a total of 2 weeks. Tumor growth was monitored by measuring tumor weights in each group. Histopathological changes in tumor tissues were observed using hematoxylin and eosin (HE) staining. Immunohistochemical techniques were employed to detect the expression of HIF-1α, GLUT1, HK2, and LDHA in tumor tissues. Western blot and RT-qPCR analyses were conducted to assess the protein and mRNA expression levels of HIF-1α, GLUT1, HK2, and LDHA in tumor tissues.
Results
2
①A total of 141 intersection genes between the BpwXyhSyD and colon cancer were successfully identified. Among these, p53, AKT1, EGFR, and HIF-1α may represent key therapeutic targets for the BpwXyhSyD in colon cancer treatment. The underlying mechanisms primarily involve signaling pathways such as p53
, VEGF and HIF-1. ②Compared with the model group, HE staining and immunohistochemistry revealed varying degrees of cellular disruption and necrosis in tumor tissues across all drug intervention groups. Western blot analysis demonstrated significantly reduced relative expression levels of HIF-1α, GLUT1, HK2, and LDHA proteins in tumor tissues treated with each intervention. RT-qPCR results demonstrated significantly reduced mRNA expression levels of
LDHA
in both the Western medicine group and the TCM-Western medicine group(
P
<
0.05), along with significantly reduced mRNA expression of
HIF⁃1α
,
GLUT1
, and
HK2
in all drug intervention groups (
P
<
0.05). Furthermore, compared with the model group and the TCM group, the tumor tissue in the TCM-Western medicine group exhibited more pronounced destruction, along with lower expression levels of HIF-1α, GLUT1, HK2, and LDHA proteins(
P
<
0.05).
Conclusion
2
The use of BpwXyhSyD synergistically inhibits glycolysis, thereby suppressing the growth of colon cancer xenografts. The mechanism may involve downregulating HIF-1α expression and inhibiting the expression of key enzymes in glycolysis, including GLUT1, HK2, and LDHA.
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