Department of Clinical Laboratory Science, College of Applied Sciences-Qurayyat, Jouf University, Qurayyat, Saudi Arabia.
Department of Clinical Laboratory Science, College of Applied Sciences-Sakaka, Jouf University, Sakaka, Saudi Arabia.
J Biomol Struct Dyn. 2024;42(21):11651-11676. doi: 10.1080/07391102.2023.2263889. Epub 2023 Sep 29.
Lung cancer remains a formidable global health challenge, necessitating the exploration of novel therapeutic approaches. This study investigates the potential of Roxb. stem extract as an anticancer agent against human lung cancer, focusing on its antioxidative and ROS-dependent apoptotic effects. Utilizing a combination of network pharmacology and in-vitro experimental validation, we delineate the multifaceted molecular mechanisms underlying the observed effects. The antioxidant potential of stem extract was evaluated by the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azinobis (3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) and ferric reducing/antioxidant power (FRAP), hydroxyl free radical scavenging, reactive nitrogen oxide scavenging and super oxide anion radical scavenging assays. Furthermore, the antiproliferative and proapoptotic effect of stem extract was evaluated against A549 lung adenocarcinoma cell line using the consecrated sulforhodamine B (SBR) and Annexin V-PI assays. Additionally, the mitochondrial membrane potential (MMP) and the total reactive oxygen species (ROS) estimation assays were performed. As a result, network pharmacology analysis revealed a complex interaction network between the bioactive constituents of and key proteins implicated in lung cancer progression. The stem extract showed dose-dependent antioxidant activity against DPPH (IC - 87.38 µg/mL), reactive nitrogen oxide (IC - 318.34 µg/mL), FRAP (IC - 359.96 µg/mL), hydroxy free radicals (IC - 526.12 µg/mL) than ABTS (IC - 698.45 µg/mL) and super oxide anion (IC - 892.71 µg/mL) as well as cytotoxic activity against A549 cells (IC - 436.80 µg/mL). Observations of morphological features in treated cells have revealed hallmark of apoptosis properties. Furthermore, as a result of treatment with stem extract, ROS generation and mitochondrial depolarization were increased in A549 cells, suggesting that this treatment has significant apoptotic properties. . These findings highlight the potential utility of this natural extract as an innovative therapeutic strategy for lung cancer treatment. The integration of network pharmacology and experimental validation enhances our understanding of the underlying mechanisms and provide the way for further translational research.Communicated by Ramaswamy H. Sarma.
肺癌仍然是一个严峻的全球健康挑战,需要探索新的治疗方法。本研究探讨了 Roxb. 茎提取物作为一种抗癌药物治疗人类肺癌的潜力,重点研究其抗氧化和 ROS 依赖性凋亡作用。本研究采用网络药理学和体外实验验证相结合的方法,阐述了观察到的作用的多方面分子机制。通过 2,2-二苯基-1-苦基肼基(DPPH)、2,2-氮杂双(3-乙基-苯并噻唑啉-6-磺酸)(ABTS)和铁还原/抗氧化能力(FRAP)、羟基自由基清除、活性氮氧化物清除和超氧阴离子自由基清除测定评估 Roxb. 茎提取物的抗氧化潜力。此外,采用传统的磺酰罗丹明 B(SBR)和 Annexin V-PI 测定法评估 Roxb. 茎提取物对 A549 肺腺癌细胞系的增殖抑制和促凋亡作用。此外,还进行了线粒体膜电位(MMP)和总活性氧(ROS)估计测定。结果表明,网络药理学分析揭示了 Roxb. 生物活性成分与肺癌进展相关的关键蛋白之间的复杂相互作用网络。Roxb. 茎提取物对 DPPH(IC - 87.38μg/mL)、活性氮氧化物(IC - 318.34μg/mL)、FRAP(IC - 359.96μg/mL)、羟基自由基(IC - 526.12μg/mL)具有剂量依赖性抗氧化活性,优于 ABTS(IC - 698.45μg/mL)和超氧阴离子(IC - 892.71μg/mL),对 A549 细胞也具有细胞毒性作用(IC - 436.80μg/mL)。在处理细胞中观察到形态特征,揭示了凋亡特性的标志性特征。此外,由于 Roxb. 茎提取物的处理,A549 细胞中的 ROS 生成和线粒体去极化增加,表明这种处理具有显著的凋亡特性。这些发现强调了这种天然提取物作为肺癌治疗创新治疗策略的潜力。网络药理学和实验验证的结合增强了我们对潜在机制的理解,并为进一步的转化研究提供了途径。