植物化学物质一直是癌症治疗的有希望的研究对象，对各种癌症起始和进展阶段都有影响。Kaempferide是一种单甲氧基黄酮，在体内体外对多种癌症表现出强效的抗癌作用。我们使用MTT ((3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四唑溴化物)测定法评估了Kaempferide对HCC的抗癌活性。 HepG2，Huh7和N1S1用于初步的体外研究，随后通过caspase-3和9进行细胞凋亡分析。在N1S1正交注射SD（Sprague Dawley）大鼠模型中研究了该化合物的体内效应，其中动物分别给予kaempferide（每周3次25mg/kg）和载体（Cremophor：乙醇）iv。对比了控制组和治疗癌症样本中caspase-9和关键的肿瘤标记转化生长因子β1（TGF-β 1）的表达情况。Kaempferide引起了3种HCC细胞株（HepG2：IC50=27.94±2.199µM；Huh7：IC50=25.65±0.956µM；N1S1：IC50=15.18±3.68µM）的剂量依赖性细胞毒性，此外还在体外证实了caspase依赖性凋亡。Kaempferide在体内显示出显著的减小肿瘤大小和肿瘤体积的作用。通过苏木精和伊红（H&E）染色的组织病理学评价证实，与载体处理组相比，在kaempferide处理动物中，明显的细胞变化导致了肿瘤的减小。治疗组中caspase-9水平也增加了。TGF-β 1，是肝癌侵袭和转移中的关键指标，也在治疗组中下调了（对照组=207.8±22.9pg/mL，kaempferide治疗=157.3±13.8pg/mL）。我们首次报道了Kaempferide作为HCC的一个有希望的替代品的潜力，这进一步需要进行临床验证。©2023年。作者独家许可Springer-Verlag GmbH Germany，Springer Nature的一部分。

Phytochemicals have been promising candidates for cancer therapy, affecting various cancer initiation and progression stages. Kaempferide is a mono methoxy flavone that shows potent anticancer effects on multiple cancers both in vitro and in vivo.We evaluated the anticancer activity of kaempferide against HCC using an MTT ((3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay. HepG2, Huh7, and N1S1 were used for preliminary in vitro studies. This is followed by an apoptosis analysis assessed by caspase-3 and 9. The in vivo effects of the compound were studied in the N1S1 orthotopically injected SD (Sprague Dawley) rat model, where the animal was given kaempferide (25 mg/kg thrice a week) and vehicle (Cremophor:ethanol) iv. The expression of caspase-9 and a critical tumor marker, transforming growth factor beta 1 (TGF-β 1), were assessed in both control and treatment tumor samples.Kaempferide-induced dose-dependent cytotoxicity in three HCC cell lines (HepG2: IC50 = 27.94 ± 2.199 µM; Huh7: IC50 = 25.65 ± 0.956 µM; and N1S1: IC50 = 15.18 ± 3.68 µM). Furthermore, caspase-dependent apoptosis was confirmed in vitro. Kaempferide showed a significant reduction in tumor size and tumor volume in vivo. Histopathological evaluation by hematoxylin and eosin (H&E) staining confirmed that altered cells were significantly demolished in the kaempferide-treated animals, which correlates with tumor reduction compared to the vehicle-treated group. Caspase-9 levels were also found to be increased in the treatment group. TGF-β 1, a crucial marker in invasion and metastasis of liver cancer, was also downregulated in the treatment group (control = 207.8 ± 22.9 pg/mL and kaempferide-treated = 157.3 ± 13.8 pg/mL).We report for the first time the potential of kaempferide as a promising alternative against HCC, which further warrants its clinical validation.© 2023. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.