Department of Pharmaceutical Analysis, School of Pharmacy, Fujian Medical University, Fuzhou 350122 China.
Department of Pharmaceutical Analysis, School of Pharmacy, Fujian Medical University, Fuzhou 350122 China; Department of Pharmacy, the First Affiliated Hospital of Xiamen University, Xiamen 361003, China.
J Ethnopharmacol. 2018 May 10;217:126-133. doi: 10.1016/j.jep.2018.02.019. Epub 2018 Feb 15.
Bidens pilosa L, belonging to the family of Acanthaceae, has been used as an anticancer medicine in folk in China. In our preliminary experiments, the petroleum ether extract from B. pilosa showed good cytotoxic activity to human lung cancer A549 cell. However, to date, it's lack of the further study on antitumor effect, mechanism and active substances composition of the petroleum ether extract of B. pilosa.
The study aimed to evaluate the anti-lung cancer efficacy of the petroleum ether extract from B. pilosa (PEEBP) in vitro and in vivo, explore the possible anticancer mechanisms, and further disclose the chemical composition of the extract.
B. pilosa was extracted with 75% ethanol (v/v), followed by extracted with petroleum ether to obtain the objective fraction. Antiproliferation effect of the petroleum ether extract in HepG2, A549, CNE and B16 cells was evaluated by MTT assay. The in vivo anticancer effect was examined by A549 cells nude mice xenograft tumor model. The possible effect mechanism was studied by western blot assay. The chemical constituents of the extract was analyzed by GC-MS.
The petroleum ether extract showed favorable antiproliferation activity against the four human cancer cell lines, especially for A549 cells with an IC of 49.11 ± 2.72 μg/mL. The extract inhibited the growth of A549 cell in mice with the inhibitory rates of 24.76%, 35.85% and 53.07% for 90, 180 and 360 mg/kg oral dosages, respectively. The B. pilosa extract could significantly down-regulate the expression of apoptosis-related protein Bcl-2 and up-regulate the protein expression of Bax and Caspase-3. 138 compounds were identified by GC-MS in the extract and the main chemical components were triterpenes, including 4,22-cholestadien-3-one (4.82%), stigmasterol (4.56%), friedelan-3-one (3.28%), etc.
The PEEBP is abundant of triterpenes and has significant anti-tumor activities against human A549 cells in vitro and in vivo, indicating it a potential anticancer agent.
鬼针草（Bidens pilosa L）属于菊科植物，在中国民间被用作抗癌药物。在我们的初步实验中，鬼针草的石油醚提取物对人肺癌 A549 细胞显示出良好的细胞毒性活性。然而，迄今为止，它缺乏对鬼针草石油醚提取物的抗肿瘤作用、机制和活性物质组成的进一步研究。
本研究旨在评估鬼针草石油醚提取物（PEEBP）在体外和体内的抗肺癌功效，探讨可能的抗癌机制，并进一步揭示提取物的化学成分。
用 75%（v/v）乙醇提取鬼针草，然后用石油醚提取目标部位。用 MTT 法评价石油醚提取物对 HepG2、A549、CNE 和 B16 细胞的增殖抑制作用。通过 A549 细胞裸鼠异种移植肿瘤模型检测体内抗癌作用。通过 Western blot 检测研究可能的作用机制。用 GC-MS 分析提取物的化学成分。
石油醚提取物对四种人癌细胞系表现出良好的增殖抑制活性，尤其是对 A549 细胞的 IC 为 49.11±2.72μg/mL。提取物抑制 A549 细胞在小鼠中的生长，90、180 和 360mg/kg 口服剂量的抑制率分别为 24.76%、35.85%和 53.07%。鬼针草提取物能显著下调凋亡相关蛋白 Bcl-2 的表达，上调 Bax 和 Caspase-3 的蛋白表达。通过 GC-MS 在提取物中鉴定出 138 种化合物，主要化学成分为三萜类化合物，包括 4,22-胆甾二烯-3-酮（4.82%）、豆甾醇（4.56%）、friedelan-3-one（3.28%）等。
PEEBP 富含三萜类化合物，对体外和体内人 A549 细胞具有显著的抗肿瘤活性，表明其具有潜在的抗癌作用。
