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基于网络药理学探究桑黄多酚的体外抗肿瘤作用及其机制

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[目的]分离、筛选瓦尼桑黄(Sanghuangporus vaninii)子实体中具有良好抗肿瘤活性的多酚组分,并对其抗肿瘤活性和潜在作用机制进行解析.[方法]采用超声辅助提取法提取乙酸乙酯部位的组分,通过对肝癌细胞HepG-2 的抑制活性筛选出具有良好抗肿瘤作用的多酚组分,基于超高效液相色谱-四极杆飞行时间质谱(UPLC-Q-TOF-MS)技术鉴定其主要成分,利用网络药理学策略阐释其潜在抗肿瘤作用机制.[结果]分离制备获得了 5 种(SVa-SVe)多酚组分,其中SVe多酚组分表现出独特的抗肿瘤活性,100 μg/mL浓度下对HepG-2 细胞抑制率为 76.54%.SVe可以显著地促进HepG-2 细胞凋亡和诱导其细胞周期阻滞,并呈现剂量依赖性.成分分析显示,SVe主要由 31 种化合物组成,基于网络药理学分析表明,SVe中的osmundacetone、hispolon、phellibaumin A、davallialactone等关键化合物通过与多个靶点蛋白作用(STAT3、mTOR、VEGFA、SRC、ERBB2 和HSP90AA),发挥抗肿瘤活性.[结论]来源于桑黄的多酚提取物SVe通过诱导细胞凋亡和细胞周期阻滞对HepG-2 细胞具有独特的抑制活性,其中的多酚化合物通过多靶点发挥作用.
In Vitro Anti-tumor Effect and Its Mechanism of Polyphenols from Sanghuangporus vaninii Based on Network Pharmacology
[Objective]The polyphenolic components with excellent anti-cancer activity from the fruiting body of Sanghuangporus vaninii were isolated and screened,and their anti-cancer activity and potential mechanisms of action were analyzed.[Method]Ultrasound-assisted extraction was used to extract components from the ethyl acetate fraction.Polyphenolic components with excellent anti-cancer effects were screened for their inhibitory activity on liver cancer cell HepG-2.The main components were identified using ultra-high performance liquid chromatography quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS)technology,and the potential mechanism of anti-cancer was elucidated using network pharmacology strategies.[Result]Five polyphenolic components(SVa-SVe)were isolated and prepared,among which SVe polyphenolic component demonstrated unique anti-cancer activity,with an inhibition rate of 76.54%on HepG-2 cells at a concentration of 100 μg/mL.SVe significantly promoted apoptosis and induced cell cycle arrest in HepG-2 cells,showing a dose-dependent effect.Ingredient analysis showed that SVe was mainly composed of 31 compounds.Based on network pharmacology analysis,key compounds such as osmundacetone,hispolo,phellibaumin A,davallialactone in SVe exerted anti-cancer activity by interacting with multiple target proteins(STAT3,mTOR,VEGFA,SRC,ERBB2,and HSP90AA).[Conclusion]The extract SVe derived from S.vaninii possessed unique inhibitory activity on HepG-2 cells by inducing apoptosis and cell cycle arrest,which was related to the presence of polyphenolic substances.

Sanghuangporus vaniniipolyphenolsliver cancernetwork pharmacology

王雨阳、刘朋、张忠、陈万超、吴迪、李文、杨焱

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上海市农业科学院食用菌研究所 农业农村部南方食用菌资源利用重点实验室 国家食用菌工程技术研究中心 国家食用菌加工技术研发中心,上海 201403

瓦尼桑黄 多酚 肝癌 网络药理学

2024

生物技术通报
中国农业科学院农业信息研究所

生物技术通报

CSTPCD北大核心
影响因子:0.505
ISSN:1002-5464
年,卷(期):2024.40(11)