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Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-11-29 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00659
Dewu Zhang 1 , Jiamei Guo 1 , Min Zhang 1 , Xiao Liu 1 , Mingyu Ba 1 , Xiaoyu Tao 1 , Liyan Yu 1 , Ying Guo 1 , Jungui Dai 1
Affiliation  

Four new oxazole-containing diterpenoids, salvianans A–D (14), along with three known diterpenoids (57), were isolated from Salvia miltiorrhiza cell cultures. The structures of the new compounds were elucidated using spectroscopic methods and single-crystal X-ray diffraction. The evaluation for their anti-HIV-1 activities revealed that 2 and 3 displayed inhibitory activities with IC50 values of 0.03 and 1.2 μM, respectively. The time of addition (TOA) assay and long terminal repeat (LTR) luciferase reporter assay results indicated that compound 2 was an HIV-1 transcription inhibitor and might be a lead compound of antiviral agents acting on HIV-1 transcription.

中文翻译:

丹参细胞培养物中含恶唑的二萜及其抗HIV-1活性

四个新的含恶唑二萜类化合物,salvianans A-d(1 - 4)中,用三个已知二萜类化合物(沿5 - 7)中,从分离丹参细胞培养物。使用光谱方法和单晶X射线衍射阐明了新化合物的结构。对它们的抗HIV-1活性的评估表明,23表现出抑制活性,IC 50值分别为0.03和1.2μM。添加时间(TOA)分析和长末端重复(LTR)荧光素酶报告基因分析结果表明化合物2 是HIV-1转录抑制剂,可能是抗病毒剂对HIV-1转录起作用的先导化合物。
更新日期:2017-11-29
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