前列腺癌是男性全球死于癌症的第二大原因。强烈建议开发新型高效治疗策略来治疗前列腺癌。莎草科是一种生态和经济上重要的植物家族，具有多种药理效应。然而，茅莜草（Cyperus exaltatus var. iwasakii，CE）的生物效价尚未知晓。本研究旨在调查CE乙醇提取物对前列腺癌的抗肿瘤作用。利用MTT检测法、细胞计数法、FACS分析、免疫印迹、创伤愈合迁移、侵袭试验、凝胶酶谱分析和EMSA等方法，探究CE在前列腺癌细胞DU145和LNCaP中的体外抗肿瘤效力。对于体内实验，将裸鼠注射LNCaP细胞。随后进行组织学（H＆E和Ki-67）和生化酶试验。急性毒性试验评估了毒性。通过光谱和色谱分析识别CE的植物化学成分。CE对前列腺癌细胞产生了显著的抗增殖效应。在DU145细胞中，CE诱导的抗增殖细胞与G0 / G1期的细胞周期阻滞有关（cyclin D1 / CDK4，cyclin E / CDK2，p21Waf1），而在LNCaP细胞中与G2 / M期的细胞周期阻滞有关（ATR、CHK1、Cdc2、Cdc25c、p21Waf1和p53）。CE刺激了DU145细胞中ERK1 / 2，p38 MAPK和AKT的磷酸化，但仅增加了LNCaP细胞中p38 MAPK的磷酸化。CE处理通过调节转录因子（如AP-1和NF-κB）抑制MMP-9活性抑制了两种类型的前列腺癌细胞的迁移和侵袭。体内实验显示，经口CE治疗后肿瘤重量和大小均减少。组织学检查确认CE抑制了小鼠LNCaP异种移植瘤的生长。CE的管理对小鼠的体重、行为模式、血液生化学和重要器官的组织病理学结果没有不良影响。最后，在CE中鉴定和计量了13种植物化学成分。CE中最丰富的次生代谢产物是阿斯特拉甘林、三吲哚和对香豆酸。我们的研究结果表明，CE对抗前列腺癌具有抗肿瘤效力。这些发现表明，CE可能是前列腺癌预防或治疗的潜在候选物。版权所有©2023 Elsevier GmbH。

Prostate cancer is the second most common cause of cancer death worldwide in men. The development of novel and highly efficient therapeutic strategies is strongly recommended to treat prostate cancer. Cyperaceae are an ecologically and economically important family of plants with several pharmacological effects. However, the biological efficacy of Cyperus exaltatus var. iwasakii (CE) is unknown.This study aimed to investigate the antitumor effect of the ethanol extract of CE against prostate cancer.In vitro antitumor efficacy of CE was explored by the MTT assay, cell counting assay, FACS analysis, immunoblot, wound-healing migration, invasion assay, zymographic assay, and EMSA in prostate cancer cells, DU145 and LNCaP. For in vivo experiments, xenograft mice were injected with LNCaP cells. Histology (H&E and Ki-67) and biochemical enzyme assay were then performed. The toxicity test was evaluated by an acute toxicity assay. The phytochemical constituents of CE were identified by spectrometric and chromatographic analyses.CE exerted a significant antiproliferative effect against prostate cancer cells. CE-induced antiproliferative cells were associated with cell cycle arrest at G0/G1 (cyclin D1/CDK4, cyclin E/CDK2, p21Waf1) in DU145 cells, but G2/M (ATR, CHK1, Cdc2, Cdc25c, p21Waf1, and p53) in LNCaP cells. CE stimulated the phosphorylation of ERK1/2, p38 MAPK, and AKT in DU145 cells, but only p38 MAPK phosphorylation was increased in LNCaP cells. CE treatment suppressed migration and invasion in the two types of prostate cancer cells by inhibiting MMP-9 activity through the regulation of transcription factors, such as AP-1 and NF-κB. In vivo experiments showed a reduction in tumor weight and size following oral CE administration. Histochemistry confirmed that CE inhibited tumor growth in the mouse LNCaP xenograft model. The administration of CE had no adverse effects on body weight, behavioral patterns, blood biochemistry, and histopathology findings of vital organs in mice. Finally, a total of 13 phytochemical constituents were identified and quantified in CE. The most abundant secondary metabolites in CE were astragalin, tricin, and p-coumaric acid.Our results demonstrated the antitumor efficacy of CE against prostate cancer. These findings suggest that CE might be a potential candidate for prostate cancer prevention or treatment.Copyright © 2023 Elsevier GmbH. All rights reserved.