2. Academic Validation
  3. 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

  • J Nat Prod. 2015 Mar 27;78(3):500-9. doi: 10.1021/np500988m.
Taizong Wu 1,  Qian Wang 2,  Cheng Jiang 1,  Susan L Morris-Natschke 3,  Hui Cui 1,  Yan Wang 2,  Yuan Yan 2 4,  Jun Xu 1,  Kuo-Hsiung Lee 3 5,  Qiong Gu 1 3
Affiliations

Affiliations

  • 1 †Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.
  • 2 ‡The Institute of Human Virology, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, Guangdong 510080, People's Republic of China.
  • 3 §Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
  • 4 ⊥Department of Microbiology, School of Dental Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
  • 5 ∥Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung, Taiwan.
PMID: 25647077 DOI: 10.1021/np500988m
Abstract

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.

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