Neo-clerodane diterpenoids from Scutellaria barbata with activity against Epstein-Barr virus lytic replication.
Neo-clerodane diterpenoids from Scutellaria barbata with activity against Epstein-Barr virus lytic replication.
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DOI：
10.1021/np500988m
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发表时间：
2015-02
影响因子：
5.1
通讯作者：
Taizong Wu;Qian Wang;Cheng Jiang;S. Morris-Natschke;H. Cui;Y. Wang;Yuan Yan;Jun Xu;K. Lee;Qiong Gu
中科院分区：
文献类型：
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作者：
Taizong Wu;Qian Wang;Cheng Jiang;S. Morris-Natschke;H. Cui;Y. Wang;Yuan Yan;Jun Xu;K. Lee;Qiong Gu
生物测定引导的分馏进行了EtOAc可溶性提取物的全植物的半枝莲，监测抑制EB病毒（EBV）裂解复制。本文报道了26个新克罗烷二萜类化合物，其中13个为新化合物（1-13，scutolides A-L），13个为已知化合物（14-26）。化合物1-13的结构通过NMR和MS光谱数据进行了鉴定。此外，通过单晶X射线衍射证实了新化合物1和11的构型。评价所有分离的化合物对EBV裂解性复制的抑制作用。11种化合物（3、4、6、11、12、15、16、17、20、22和24）表现出中度至强效抑制作用，EC 50值为3.2 - 23.6 μM，选择性指数（SI）值为2.1 - 109.2。更具体地说，新化合物4显示出最有效的活性，EC 50和SI值分别为3.2 μM和46.1，而化合物24（EC 50 = 16.4 μM）显示出最高的SI值109.2。本研究首次报道了新克罗烷二萜类化合物对EBV裂解性复制表现出显著的抑制作用。
Bioassay-guided fractionation was conducted on an EtOAc-soluble extract of the whole plants of Scutellaria barbata, monitored by inhibition of Epstein-Barr virus (EBV) lytic replication. Twenty-six neo-clerodane diterpenoids were isolated, of which 13 are new (1-13, scutolides A-L) and 13 previously known (14-26). The structures of 1-13 were elucidated by analysis of their NMR and MS spectroscopic data. Furthermore, the configurations of the new compounds 1 and 11 were confirmed by single-crystal X-ray diffraction. All of the isolated compounds were evaluated for inhibitory effects against EBV lytic replication. Eleven compounds (3, 4, 6, 11, 12, 15, 16, 17, 20, 22, and 24) exhibited moderate to potent inhibition, with EC50 values from 3.2 to 23.6 μM and selective index (SI) values from 2.1 to 109.2. More specifically, the new compound 4 showed the most potent activity, with EC50 and SI values of 3.2 μM and 46.1, respectively, while compound 24 (EC50 = 16.4 μM) exhibited the highest SI of 109.2. This study is the first to report that neo-clerodane diterpenoids demonstrate significant inhibition against EBV lytic replication.