Anoor Pawan Kumar, Yadav A Nichita, Rajkumar Karthik, Kande Ramesh, Tripura Chaturvedula, Naik K Srinivas, Burgula Sandeepta
Department of Microbiology, University College of Science, Osmania University, Hyderabad, Telangana 500007, India.
CSIR-Centre for Cellular and Molecular Biology Annexe-II, Medical Biotechnology Campus, Annexe-II, Hyderabad, Telangana 500007, India.
Mol Clin Oncol. 2022 Sep 13;17(5):151. doi: 10.3892/mco.2022.2584. eCollection 2022 Nov.
(Ap) has been a part of traditional medicine for its anti-inflammatory effects, treatment of snake bites and liver abnormalities. Several investigations have revealed its bioactive components to be andrographolides. The methanolic extracts of leaves from Ap were characterized, the non-andrographolides were identified and screened for anti-proliferative activity. The extracts showed significant toxicity against numerous cancer cells including HeLa, MCF7, BT549, 293 and A549 cells. Anti-proliferative activity and effect on cancer cell invasion (metastatic potential) and cell migration were examined. The extracts revealed significant inhibition of the ability of HeLa cells in repairing the gap created by a vertical wound made on a confluent cell monolayer. Similarly, a 40% reduction in cell migration was observed in presence of the extracts. Significant anti-angiogenic activity in terms of reduced blood capillary formation was observed on the Chorioallantoic membranes of embryonated hen eggs co-inoculated with HeLa cells and the extracts. Analysis of HeLa cells treated with the extracts using flow cytometry indicated the arrest of cell cycle progression at the G2/M phase. Variation in the Bax/Bcl-2 ratio and elevated caspase-3 levels by immunoblotting confirmed cell death induction via the apoptotic pathway. Investigation of the extracts by gas chromatography-mass spectrometry displayed the predominant components to be 2(5H)-Furanone (14.73%), Quinic acid (17.32%), and Phytol (11.43%). These components have been previously known to have anticancer activity, while being studied individually in other plants. This is the first study, to the best of our knowledge, on the anti-proliferative and anti-angiogenic activity of the non-andrographolide components from Ap.
穿心莲因其抗炎作用、治疗蛇咬伤和肝脏异常而一直是传统医学的一部分。多项研究表明其生物活性成分是穿心莲内酯。对穿心莲叶片的甲醇提取物进行了表征，鉴定并筛选了非穿心莲内酯的抗增殖活性。提取物对包括HeLa、MCF7、BT549、293和A549细胞在内的多种癌细胞显示出显著毒性。研究了提取物的抗增殖活性及其对癌细胞侵袭（转移潜能）和细胞迁移的影响。提取物显示出对HeLa细胞修复汇合细胞单层上垂直伤口所形成间隙能力的显著抑制。同样，在提取物存在的情况下，观察到细胞迁移减少了40%。在与HeLa细胞和提取物共同接种的鸡胚绒毛尿囊膜上，观察到毛细血管形成减少，具有显著的抗血管生成活性。使用流式细胞术分析用提取物处理的HeLa细胞表明细胞周期进程停滞在G2/M期。通过免疫印迹法检测Bax/Bcl-2比值的变化和caspase-3水平的升高，证实通过凋亡途径诱导细胞死亡。通过气相色谱-质谱联用对提取物进行研究，结果显示主要成分是2(5H)-呋喃酮（14.73%）、奎尼酸（17.32%）和叶绿醇（11.43%）。这些成分此前已知具有抗癌活性，并且在其他植物中已分别进行过研究。据我们所知，这是第一项关于穿心莲非穿心莲内酯成分的抗增殖和抗血管生成活性的研究。
