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1

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

2

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

3

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

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

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

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Henan Province Hospital of TCM, Zhengzhou 450002, China





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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,*

Fuente: http://mdpi.com/



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