Abstract：
Two new ent-labdane diterpenoids, hypoestesins A-B (1-2) and five new labdane diterpenoids, hypopurolides H-L (3-7), were isolated from the aerial parts of Hypoestes purpurea. All of the structures were fully determined based on extensive analysis of 1H, 13C, 2D NMR, and HRESIMS data. The absolute configurations of 1-3 was established through comparing the experimental and calculated ECD curves and the structure of 5 was confirmed by single crystal X-ray diffraction experiment. Compounds 5-7 were unusual C23 labdane diterpenoids having a γ-acetonyl-α, β-unsaturated γ-lactone unit and each assigned as C-15 epimeric mixture. Furthermore, cytotoxic and anti-inflammatory activities of 3-7 were evaluated. The results showed that 3 had remarkable cytotoxic activity against HL-60, A549, SMMC-7721, MDA-MB-231, and SW480 cancer cell lines with IC50 values ranging from 2.35 to 17.06 μM. Compound 4 showed moderate cytotoxic activity against HL-60 and SMMC-7721 cancer cell lines with IC50 values of 15.12 ± 0.53 and 12.92 ± 0.60 μM, respectively. Furthermore, compound 4 was also found to exhibit inhibitory activity against NO production in RAW 264.7 macrophages with IC50 values of 23.56 ± 0.99 μM, compared to the positive control L-NMMA with an IC50 value of 41.11 ± 1.34 μM.
摘要：
两种新的ent-labdane二萜，hypoestesinsA-B（1-2）和五个新的拉布丹二萜，H-L(3-7),是从紫癜的地上部分中分离出来的。所有的结构都是基于对1H的广泛分析而完全确定的，13C,2DNMR,和HRESIMS数据。通过比较实验和计算的ECD曲线，建立了1-3的绝对构型，并通过单晶X射线衍射实验证实了5的结构。化合物5-7是具有γ-丙酮基-α的不寻常的C23拉丹二萜，β-不饱和γ-内酯单元和每个指定为C-15差向异构混合物。此外，评估了3-7的细胞毒性和抗炎活性。结果表明，3对HL-60，A549，SMMC-7721，MDA-MB-231和SW480癌细胞具有显着的细胞毒活性，IC50值为2.35至17.06μM。化合物4对HL-60和SMMC-7721癌细胞系显示中等细胞毒活性,IC50值为15.12±0.53和12.92±0.60μM,分别。此外，还发现化合物4对RAW264.7巨噬细胞中的NO产生具有抑制活性，IC50值为23.56±0.99μM，与阳性对照L-NMMA相比,IC50值为41.11±1.34μM。
