The plant Peristrophe bicalyculata (Retz) Nees is used for the treatment of cancer. While its leaf extracts have been shown to inhibit the growth of some cancer cells, there is little information supporting the constituents’ anti-tumour potential. This study, therefore, investigated the effects of the plant’s leaf extracts on cancer cells and the associated cellular/molecular mechanisms. Extracts were prepared using hexane (PBH), chloroform (PBC), ethyl acetate (PBE) and methanol (PBM) and constituents were identified by Liquid Chromatography-Mass Spectrometry (LC-MS). Their cytotoxic effects on human cervical (HeLa) and lung cancer (MRC5-SV2) cells were assessed using the MTT and LDH release assays. Reactive oxygen species (ROS) production was assessed using 2′,7′-dichlorofluorescein diacetate (DCFDA) and mitochondrial membrane potential by staining with JC-1 (5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethylbenzimidazolyl-carbocyanine iodide). Caspase activation was determined using a Caspase-Glo-3/7 assay, and DNA damage by the Comet assay. Changes to mRNA expression were assessed using Quantitative Real-Time PCR. PBC, PBE and PBM reduced cell viability and induced LDH release, with IC₅₀ values (48 h, MTT, in μg/ml), respectively, of 6.21 ± 0.70, 23.39 ± 3.92, and 22.43 ± 3.58 (HeLa); and 1.98 ± 0.33, 8.57 ± 1.91 and 28.24 ± 5.57 (MRC5-SV2). PBC induced ROS, while PBC, PBE and PBM impaired mitochondrial membrane potential and induced caspase 3/7 activation. PBC and PBE induced DNA damage, and PBE induced caspase-3 mRNA expression. Constituents of the extracts included derivatives of gallic acid, dipeptides, diterpenoids and flavones. We conclude that P. bicalyculata contains cytotoxic principles that could be potential leads for developing novel anti-cancer agents.

植物Peristrophe biclyculata(Retz) Nees 用于治疗癌症。虽然它的叶子提取物已被证明可以抑制某些癌细胞的生长，但几乎没有信息支持这些成分的抗肿瘤潜力。因此，本研究调查了植物叶提取物对癌细胞的影响以及相关的细胞/分子机制。使用己烷 (PBH)、氯仿 (PBC)、乙酸乙酯 (PBE) 和甲醇 (PBM) 制备提取物，并通过液相色谱-质谱 (LC-MS) 鉴定成分。使用 MTT 和 LDH 释放试验评估了它们对人宫颈 (HeLa) 和肺癌 (MRC5-SV2) 细胞的细胞毒性作用。使用 2',7'-二氯荧光素二乙酸酯 (DCFDA) 和 JC-1 (5,5',6, 6'-四氯-1,1',3,3'-四乙基苯并咪唑基-碘化羰花青）。使用 Caspase-Glo-3/7 测定法测定 Caspase 活化，并通过 Comet 测定法测定 DNA 损伤。使用定量实时 PCR 评估 mRNA 表达的变化。PBC、PBE 和 PBM 降低细胞活力并诱导 LDH 释放，IC_{50 个}值（48 小时，MTT，以 μg/ml 为单位），分别为 6.21 ± 0.70、23.39 ± 3.92 和 22.43 ± 3.58 (HeLa)；和 1.98 ± 0.33、8.57 ± 1.91 和 28.24 ± 5.57 (MRC5-SV2)。PBC 诱导 ROS，而 PBC、PBE 和 PBM 损害线粒体膜电位并诱导 caspase 3/7 活化。PBC和PBE诱导DNA损伤，PBE诱导caspase-3 mRNA表达。提取物的成分包括没食子酸、二肽、二萜和黄酮的衍生物。我们得出结论，P. bicalyculata含有细胞毒性原理，可能是开发新型抗癌剂的潜在线索。