期刊
FITOTERAPIA
卷 161, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.fitote.2022.105258
关键词
Gerbera piloselloides (L.) Cass.; Phenone-monoterpenes; Chromone-monoterpenes; Coumarin-monoterpenes; Bioactivity; Biosynthetic pathway
资金
- CAMS Innovation Fund for Medical Sciences (CIFMS) [2021-I2M-1-028]
- Chinese Na- tional S & T Special Project on Major New Drug Innovation [2019ZX09735002]
This study identified several previously undescribed compounds from the extract of Gerbera piloselloides, including some that showed inhibitory effects on nitric oxide production and cancer cell proliferation.
A phytochemical investigation of the 95% ethanol extract from Gerbera piloselloides obtained fourteen com-pounds, including three undescribed phenone-monoterpenes (1a/1b and 2), seven undescribed chromone-monoterpenes (3a/3b-5a/5b and 6), and one undescribed coumarin-monoterpene (8). Among them, four pairs of enantiomers (1a/1b and 3a/3b-5a/5b) were successfully isolated by the chiral-phase HPLC resolution. The structures and absolute configurations were unambiguously determined based on comprehensive spectroscopic data, electronic circular dichroism (ECD) data, and X-ray diffraction analysis. Structurally, compound 1 is the first 5-methylphenone monoterpene formed through a circular 6-membered carbocycle. And their anti-inflammatory and antiproliferative activities were evaluated via LPS stimulated RAW 264.7 cells and five human cancer lines (HepG2, MDA-MB-231, SCG-7901, A549 and MCF-7), respectively. Compounds 4b, 5a and 5b showed moderate inhibitory effect against nitric oxide (NO) production with IC(50 )values ranging from 12.52 to 15.75 mu M. Compound 8 significantly inhibited the proliferation of MDA-MB-231 human cancer line in a dose -dependent manner. Furthermore, the connection between phenone-monoterpenes, chromone-monoterpenes, and coumarin-monoterpenes in biosynthesis were also discussed.
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