Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV‑1 Activities

Four new oxazole-containing diterpenoids, salvianans A–D (1–4), along with three known diterpenoids (5–7), 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.从丹参（Salvia miltiorrhiza）细胞培养物中分离得到4个新型含恶唑二萜类化合物丹参烷类（salvianans）A-D（1~4），以及3个已知二萜类化合物（5~7）。新型化合物的结构通过波谱学方法与单晶X射线衍射技术得以解析。抗HIV-1活性评价结果显示，化合物2与3分别展现出抑制活性，其半数抑制浓度（IC50）分别为0.03 μM和1.2 μM。加入时间（time of addition, TOA）实验及长末端重复序列（long terminal repeat, LTR）荧光素酶报告基因实验结果表明，化合物2为HIV-1转录抑制剂，有望成为靶向HIV-1转录过程的抗病毒药物先导化合物。