Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities
Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities
复制标题
丹参细胞培养物中含恶唑二萜及其抗 HIV-1 活性
DOI：
10.1021/acs.jnatprod.7b00659
复制
发表时间：
2017
影响因子：
5.1
通讯作者：
Da Jungui
中科院分区：
文献类型：
--
作者：
Zhang Dewu;Guo Jiamei;Zhang Min;Liu Xiao;Ba Mingyu;Tao Xiaoyu;Yu Liyan;Guo Ying;Da Jungui
从丹参细胞培养物中分离得到4个新的含恶唑的二萜类化合物，丹参素A-D(1-4)和3个已知的二萜类化合物(5-7)。用光谱分析和单晶X-射线衍射法确证了新化合物的结构。抗HIV-1活性评价表明，化合物2和3具有抑制活性，其IC50值分别为0.03和1.2μM。添加时间(TOA)实验和长末端重复序列(LTR)荧光素酶报告实验结果表明，化合物2是HIV-1转录抑制物，可能是抗病毒药物作用于HIV-1转录的先导化合物。
Four new oxazole-containing diterpenoids, salvianans A–D (1–4), along with three known diterpenoids (5–7), were isolated fromSalvia miltiorrhizacell 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 that2and3displayed inhibitory activities with IC50values 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 compound2was an HIV-1 transcription inhibitor and might be a lead compound of antiviral agents acting on HIV-1 transcription.