Bouchouka Racha Lydia, Kabouche Zahia, Defondaumière Marie, Debiossat Marlène, Ghezzi Catherine, Riou Laurent, Taha Tarek H, Boufahja Fehmi, Bendif Hamdi, Garzoli Stefania
Laboratoire d'Obtention de Substances Thérapeutiques, Université de Constantine 1, Frères Mentouri, Campus Chaabet Ersas, Constantine 25000, Algeria.
INSERM, LRB, Université de Grenoble Alpes, 38000 Grenoble, France.
Molecules. 2025 Aug 31;30(17):3570. doi: 10.3390/molecules30173570.
(Lamiaceae) remains unexplored despite its pharmacological potential. In this study, for the first time, the antiproliferative, pro-apoptotic, cell cycle arrest, and vasorelaxant effects of the -butanolic extract (BESD) and a VLC fraction (BF1SD) of were investigated. Antiproliferative activity was evaluated on PC3 and MDA-MB-231 cell lines via MTT assay (72 h). Apoptosis (Annexin V-FITC/PI) and cell cycle arrest (PI/RNase) were assessed by flow cytometry (24 h, 250-1000 µg/mL). Vasorelaxant effects were studied ex vivo on rat aortic rings. LC-HRMS/MS was used for phytochemical analysis. BESD showed higher antiproliferative activity (IC: 196 ± 6 µg/mL for PC3, 182 ± 8 µg/mL for MDA-MB-231) than BF1SD (IC: 281 ± 6 µg/mL and 273 ± 3 µg/mL, respectively). Apoptosis was dose-dependent, with BF1SD displaying a stronger effect at 1000 µg/mL (67.3 ± 0.5% vs. 49.9 ± 0.7% for BESD). BESD induced G2/M arrest, while BF1SD caused G0/G1 and G2/M arrest. Vasorelaxation was endothelium-dependent, likely mediated by NO. Identified compounds (hyperoside, luteolin-7-glucoside, and rutin) may contribute to these effects. BESD and BF1SD exhibit anticancer and vasorelaxant properties, indicating potential therapeutic use against cancer and cardiovascular diseases. Further studies are needed to isolate active compounds and confirm their effects in vivo.
唇形科植物尽管具有药理潜力,但仍未得到充分研究。在本研究中,首次对[植物名称]的正丁醇提取物(BESD)和一个超液相色谱馏分(BF1SD)的抗增殖、促凋亡、细胞周期阻滞和血管舒张作用进行了研究。通过MTT法(72小时)评估对PC3和MDA-MB-231细胞系的抗增殖活性。通过流式细胞术(24小时,250 - 1000μg/mL)评估凋亡(Annexin V-FITC/PI)和细胞周期阻滞(PI/RNase)。在大鼠主动脉环上进行离体研究血管舒张作用。使用液相色谱 - 高分辨质谱联用(LC-HRMS/MS)进行植物化学分析。BESD显示出比BF1SD更高的抗增殖活性(PC3细胞系的IC50为196±6μg/mL,MDA-MB-231细胞系的IC50为182±8μg/mL;BF1SD的IC50分别为281±6μg/mL和273±3μg/mL)。凋亡呈剂量依赖性,BF1SD在1000μg/mL时显示出更强的作用(67.3±0.5%,而BESD为49.9±0.7%)。BESD诱导G2/M期阻滞,而BF1SD导致G0/G1期和G2/M期阻滞。血管舒张是内皮依赖性的,可能由一氧化氮介导。鉴定出的化合物(金丝桃苷、木犀草素 - 7 - 葡萄糖苷和芦丁)可能促成了这些作用。BESD和BF1SD具有抗癌和血管舒张特性,表明对癌症和心血管疾病具有潜在的治疗用途。需要进一步研究分离活性化合物并在体内证实其作用。