Annual mortality of 8.2 million could be attributable to cancer globally, posing a serious health issue; particularly, the high number of nonsmall cell lung cancer (NSCLC) diagnosed cases in recent years highlight the need for development in anticancer agents. In NSCLC, a number of specific inhibitors of phosphatidylinositol-3-kinase (PI3K), Protein kinase B (AKT), and mammalian target of rapamycin are currently under development; however, the early evidence has yielded disappointing results. Ent-kaurane diterpenoid compounds from Cronton tonkinensis have been investigated for several bioactivities such as antibacterial, cytotoxic activity, and so on;; however, lung cancer is not yet studied. In this study, we conducted a molecular docking study of 7 ent-kaurane diterpenoids from C tonkinensis against PI3K targeted anticancer therapies; furthermore, their cytotoxicity effects against A549 lung cancer cells were also evaluated. Obtained results indicated that compounds 7, 6, 2, and 1 exhibited significant inhibitory results in comparison to the reference drug oxaliplatin which suggests further in vitro assay for drug development.

全球每年有 820 万人死于癌症，构成严重的健康问题；特别是，近年来非小细胞肺癌 (NSCLC) 确诊病例的大量增加凸显了开发抗癌药物的必要性。在非小细胞肺癌中，目前正在开发多种磷脂酰肌醇3-激酶（PI3K）、蛋白激酶B（AKT）和哺乳动物雷帕霉素靶点的特异性抑制剂；然而，早期的证据产生了令人失望的结果。已经研究了来自Cronton tonkinensis 的Ent- kaurane 二萜化合物的多种生物活性，例如抗菌、细胞毒活性等；然而，肺癌尚未得到研究。在本研究中，我们对 7 个耳鼻喉科进行了分子对接研究从-kaurane二萜类化合物Ç山豆根针对PI3K靶向抗癌疗法; 此外，还评估了它们对 A549 肺癌细胞的细胞毒性作用。获得的结果表明，化合物7，6，2，和1相比，参考药物奥沙利铂这进一步表明在体外试验中的药物开发表现出显著抑制结果。