喜马拉雅红豆杉中紫杉烷类化合物的体外和计算机模拟抗癌潜力
In-vitro and in-silico anticancer potential of taxoids from Taxus wallichiana Zucc.
作者信息
Qayum Mughal, Nisar Muhammad, Rauf Abdur, Khan Imran, Kaleem Waqar Ahmad, Raza Muslim, Karim Nasiara, Saleem Munawar Ahmad, Bawazeer Saud, Uysal Sengul, Zengin Gokhan, Jahan Saqib, Ramadan Mohamed Fawzy
机构信息
Department of Pharmacy, Kohat University of Science and Technology, Kohat, 6000, Pakistan.
Department of Pharmacy, University of Swabi, Swabi, 23430, Pakistan.
出版信息
Biol Futur. 2019 Dec;70(4):295-300. doi: 10.1556/019.70.2019.33. Epub 2019 Dec 1.
INTRODUCTION
Natural products derived from medicinal plants provide beneficial cancer chemotherapeutic drugs. Bioactive constituents from plants are explored for their anticancer properties.
METHODS
Three known compounds (deacetylbaccatin III, tasumatrol B, and taxawallin J) were isolated from Taxus wallichiana. Compounds were screened against four cancer cell lines, such as eA498, HepG2, NCI-H226, and MDR 2780AD. Cytotoxic activity was evaluated using MTT assay against cancer cell lines.
RESULTS
Tasumatrol B showed good cytotoxic activity conducted for the improvement of inhibiting potential of these compounds against the cancer drug target protein (EGFR tyrosine kinase enzyme). The docking study showed that all compounds have binding affinities and interaction profile with the receptor tyrosine kinase.
DISCUSSION
The study suggests that these compounds could be used for the discovery of novel inhibitors against the target receptors for the treatment of cancer.
引言
源自药用植物的天然产物可提供有益的癌症化疗药物。人们对植物中的生物活性成分进行了抗癌特性研究。
方法
从喜马拉雅红豆杉中分离出三种已知化合物（去乙酰巴卡亭III、塔苏马酚B和紫杉壁素J）。针对四种癌细胞系，如eA498、HepG2、NCI-H226和MDR 2780AD，对这些化合物进行筛选。使用MTT法评估对癌细胞系的细胞毒性活性。
结果
塔苏马酚B显示出良好的细胞毒性活性，有助于提高这些化合物对癌症药物靶蛋白（表皮生长因子受体酪氨酸激酶）的抑制潜力。对接研究表明，所有化合物与受体酪氨酸激酶都具有结合亲和力和相互作用模式。
讨论
该研究表明，这些化合物可用于发现针对靶受体的新型抑制剂，以治疗癌症。
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