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School of pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China


Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China


Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & Chinese Medicine Development of Henan Province, Zhengzhou 450046, China


National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicine, Beijing 100700, China


Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100500, China


Henan Province Hospital of TCM, Zhengzhou 450002, China


Author to whom correspondence should be addressed.

Academic Editor: Thomas J. Schmidt

Abstract Three types of ent-kaurane diterpenoids were isolated from the aerial parts of Isodon excisoides, including three new diterpenoids, 1α,7α,14β-trihydroxy-20-acetoxy-ent-kaur-15-one 1; 1α,7α,14β,18-tetrahydroxy-20-acetoxy-ent-kaur-15-one 2; and 1α-acetoxy-14β-hydroxy-7α,20-epoxy-ent-kaur-16-en-15-one 3; together with six known diterpenes henryin 4; kamebanin 5; reniformin C 6; kamebacetal A 7; kamebacetal B 8; and oridonin 9. The structures of the isolated compounds were elucidated by means of nuclear magnetic resonance spectroscopy and high-resolution mass spectrometry in conjunction with published data for their analogs, as well as their fragmentation patterns. Compounds 5 and 9 were isolated from Isodon excisoides for the first time. To explore the structure-activity relationships of the isolated compounds, they were tested for their cytotoxic effects against five human cancer cell lines: HCT-116, HepG2, A2780, NCI-H1650, and BGC-823. Most of the isolated compounds showed certain cytotoxic activity against the five cancer cell lines with IC50 values ranging from 1.09–8.53 µM. Among the tested compounds, compound 4 exhibited the strongest cytotoxic activity in the tested cell lines, with IC50 values ranging from 1.31–2.07 µM. Compounds 1, 6, and 7 exhibited selective cytotoxic activity. View Full-Text

Keywords: Isodon excisoides; ent-kaurane diterpene; cytotoxic activity; structure-activity relationship Isodon excisoides; ent-kaurane diterpene; cytotoxic activity; structure-activity relationship

Autor: Li-Ping Dai 1,2,3, Chun Li 2,4, Han-Ze Yang 5, Yan-Qing Lu 1,2, Hong-Yan Yu 6, Hui-Min Gao 2,5 and Zhi-Min Wang 2,5,*



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