Zheng Dong-Shu, Chen Liang-Shu
Department of Otolaryngology Head and Neck Surgery, The First Affiliated Hospital of Xiamen University, Xiamen, Fujian 361003, P.R. China.
Ward of Cadre Care, The First Affiliated Hospital of Xiamen University, Xiamen, Fujian 361003, P.R. China.
Exp Ther Med. 2017 Oct;14(4):3273-3278. doi: 10.3892/etm.2017.4883. Epub 2017 Aug 3.
Nasopharyngeal carcinoma (NPC) is a malignant disease that threatens the health of humans. To find effective agents for the inhibition of Epstein-Barr virus (EBV) infection, which is associated with NPC, a phytochemical investigation of was carried out in the present study. Five triterpenoids were identified, including ganoderic acid A (compound 1), ganoderic acid B (compound 2), ganoderol B (compound 3), ganodermanontriol (compound 4), and ganodermanondiol (compound 5), on the basis of spectroscopic analysis. An inhibition of EBV antigens activation assay was implemented to elucidate the triterpenoids from and potentially prevent NPC. All the triterpenoids showed significant inhibitory effects on both EBV EA and CA activation at 16 nmol. At 3.2 nmol, all the compounds moderately inhibited the activation of the two antigens. The activity of telomerase was inhibited by these triterpenoids at 10 µM. Molecular docking demonstrated that compound 1 was able to inhibit telomerase as a ligand. In addition, the physicochemical properties of these compounds were calculated to elucidate their drug-like properties. These results provided evidence for the application of these triterpenoids and whole in the treatment of NPC.
鼻咽癌(NPC)是一种威胁人类健康的恶性疾病。为了寻找抑制与鼻咽癌相关的爱泼斯坦-巴尔病毒(EBV)感染的有效药物,本研究对[具体物质]进行了植物化学研究。通过光谱分析鉴定出了五种三萜类化合物,包括灵芝酸A(化合物1)、灵芝酸B(化合物2)、灵芝醇B(化合物3)、灵芝萜三醇(化合物4)和灵芝萜二醇(化合物5)。实施了EBV抗原激活抑制试验,以阐明[具体物质]中的三萜类化合物并潜在预防鼻咽癌。所有三萜类化合物在16 nmol时对EBV EA和CA激活均表现出显著抑制作用。在3.2 nmol时,所有化合物均适度抑制这两种抗原的激活。这些三萜类化合物在10 µM时可抑制端粒酶活性。分子对接表明化合物1能够作为配体抑制端粒酶。此外,计算了这些化合物的物理化学性质以阐明其类药性质。这些结果为这些三萜类化合物及整个[具体物质]在鼻咽癌治疗中的应用提供了证据。