1. Academic Validation
  2. Monomeric and dimeric ent-kauranoid-type diterpenoids from rabdosia japonica and their cytotoxicity and anti-HBV activities

Monomeric and dimeric ent-kauranoid-type diterpenoids from rabdosia japonica and their cytotoxicity and anti-HBV activities

  • Fitoterapia. 2017 Apr;118:94-100. doi: 10.1016/j.fitote.2017.03.006.
Hong-Chuan Liu 1 Zhao-Bao Xiang 2 Qiang Wang 3 Bo-Yan Li 4 Yong-Sheng Jin 5 Hai-Sheng Chen 6
Affiliations

Affiliations

  • 1 School of Pharmacy, Second Military Medical University, Shanghai 200433, China; Department of Pharmacy, Beijing Chao-yang Hospital, Capital Medical University, Beijing 100020, China.
  • 2 School of Pharmacy, Second Military Medical University, Shanghai 200433, China; Key Laboratory of Natural Medicine Research of Chongqing Education Commission, Chongqing Technology and Business University, Chongqing 400067, China.
  • 3 Department of Pharmacy, No. 202 Hospital of PLA, Shenyang 110000, China.
  • 4 School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
  • 5 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: ysjin@smmu.edu.cn.
  • 6 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: hschen2012@163.com.
Abstract

Two new ent-kauranoid-type Diterpenoids (1 and 2) and one new rare dimer of ent-kauranoids (3) with a cyclobutane ring by a [2+2] cycloaddition, together with nine known Diterpenoids (4-12) were obtained from the aerial parts of Rabdosia japonica. Their chemical structures were established by 1D and 2D NMR techniques and mass spectrometry and by comparison with spectroscopic data reported. All ent-kauranoids were test for their cytotoxic effects against A549, HCT116, CCRF-CEM and HL-60 tumor cell lines. Compounds 1, 2, 4, 5, 7, 10 and 12 showed potent and selective cytotoxicity. In addition, some selected ent-kauranoids were test for their anti-HBV activities, and the results showed compound 8 had inhibitory effect on HBsAg with a 59% inhibition ratio at the concentration of 20μg/mL.

Keywords

Anti-HBV activity; Cytotoxicity; Labiatae; Rabdosia japonica; ent-kaurane diterpenoid.

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