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Comprehensive evaluation on anti-inflammatory and anti-angiogenic activities in vitro of fourteen flavonoids from Daphne Genkwa based on the combination of efficacy coefficient method and principal component analysis

Authors Zhou, De-Cui; Zheng, Guo; Jia, Li-Ying; He, Xin; Zhang, Chun-Feng; Wang, Chong-Zhi; Yuan, Chun-Su

Journal JOURNAL OF ETHNOPHARMACOLOGY , MAR 25 2021,:268

DOI 10.1016/j.jep.2020.113683 PubMed 33301910

Abstract Ethnopharmacological relevance: Genkwa flos, as a traditional herb, is the dried flower buds of Daphne genkwa Sieb. et Zucc. It is used in traditional medicine for the treatment of cough, sore throats, edema.Aim of the study: The study aimed to explore a new mathematical method for multivariate evaluation, investigate the anti-inflammatory and anti-angiogenic activities of flavonoids in Daphne Genkwa under ex vivo conditions.Materials and methods: The flavonoids monomers in Daphne Genkwa were separated by preparative liquid chromatography and identified by HPLC-ESI-ITMS. An in vitro inflammatory model of macrophage RAW264.7 induced by LPS and an angiogenesis model of human umbilical vein endothelial cells induced by TNF-alpha were established. Flavonoids were extracted and prepared for intervention to detect the amount of secretion after drug intervention to reflect the anti-inflammatory and anti-angiogenic activities of each component. In addition, a new mathematical method, which combined principal component analysis and efficacy coefficient method, was adopted in pharmacodynamic evaluation.Results: Fourteen flavonoids monomers were separated by preparative liquid chromatography and identified by HPLC-ESI-ITMS including H1 (hydroxygenkwanin-5-O-13-D-glucoside), H2 (apigenin-7-O-13-D-glucoside), H3 (kaempferol-3-O-13-D-glucoside), H4 (hydroxygenkwanin-5-O-13-D-primeveroside), H5 (apigenin-5-O-13-D-primeveroside), H6 (apigenin-7-O-13-D-glucuronide), H7 (luteolin-5-O-13-D-glucopyranoside), H8 (genkwain-5-O-13-Dglucoside), H9 (luteolin), H10 (Daphnodorin G), H11 (tiliroside), H12 (apigenin), H13 (3hydroxygenkwain) and H14 (genkwanin). We found that most of flavonoids down-regulated VCAM and MMP-3, while H1, H8, H9, H14 reduced VEGF and ICAM was only decreased by H14.Conclusion: Genkwanin may be the most active anti-rheumatoid arthritis flavonoids in Daphne genkwa. Meanwhile, the new mathematical method used in the study provided a new direction for solving the problem of multi-index pharmacodynamic evaluation.

Species covered 芫花 Daphne genkwa