Yanqi Han1, Mengge Zhou1, Liqiang Wang2, Xuhui Ying1, Jiamin Peng1, Min Jiang3, Gang Bai1, Guoan Luo4. 1. State Key Laboratory of Medicinal Chemical Biology, Tianjin Key Laboratory of Molecular Drug Research, College of Pharmacy, Nankai University, Tianjin 300071, People's Republic of China. 2. Tianjin Entry-Exit Inspection and Quarantine Bureau, Tianjin 300461, People's Republic of China. 3. State Key Laboratory of Medicinal Chemical Biology, Tianjin Key Laboratory of Molecular Drug Research, College of Pharmacy, Nankai University, Tianjin 300071, People's Republic of China. Electronic address: minjiang@nankai.edu.cn. 4. State Key Laboratory of Medicinal Chemical Biology, Tianjin Key Laboratory of Molecular Drug Research, College of Pharmacy, Nankai University, Tianjin 300071, People's Republic of China; Department of Chemistry, Tsinghua University, Beijing 100084, People's Republic of China.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Flos Chrysanthemi (FC), a commonly used traditional Chinese medicine, has five major cultivars ("Boju", "Chuju", "Gongju", "Hangbaiju" and "Huaiju") from different sources. However, the active constituents of these cultivars have not been studied or characterized with respect to their bioactivity, which is a serious problem when considering quality and safety. AIM OF THE STUDY: To evaluate the differences among the five cultivars of FC, and to establish a method for the standardization and quality control of FC related to its bioactivity. MATERIALS AND METHODS: In this study, the different ingredients in five cultivars of FC were identified by UPLC-Q/TOF and PCA, and the anti-inflammatory ingredients of FC were predicted and screened by artificial neural network (ANN) and an NF-κB luciferase reporter gene assay system. Using this comprehensive method, we successfully screened the anti-inflammatory markers of different cultivars of FC. RESULTS: Nineteen marker ingredients were confirmed to contribute strongly to the cluster, and eleven compounds in the five cultivars of FC were found to exert potential anti-inflammatory effects. Among these compounds, the NF-κB inhibitor activity of apigenin-7-O-6″-malonyl-glucoside, luteolin-7-O-rutinoside, quercetin-7-O-galactoside, quercetin-3-O-glucoside, apigenin-7-O-rutinoside and apigenin-7-O-glucoside were first reported here. Chlorogenic acid, luteolin-7-O-glucoside, 3,5-dicaffeoylquinic acid and luteolin were confirmed to be the most important anti-inflammatory marker ingredients useful for the quality control of FC. CONCLUSIONS: The proposed efficient and systematic method is helpful for the standardization and quality control of FC. Moreover, this comprehensive strategy may prove to be a powerful technique for the rapid establishment of quality control procedures related to bioactivity for other herbal samples and foods.
ETHNOPHARMACOLOGICAL RELEVANCE: Flos Chrysanthemi (FC), a commonly used traditional Chinese medicine, has five major cultivars ("Boju", "Chuju", "Gongju", "Hangbaiju" and "Huaiju") from different sources. However, the active constituents of these cultivars have not been studied or characterized with respect to their bioactivity, which is a serious problem when considering quality and safety. AIM OF THE STUDY: To evaluate the differences among the five cultivars of FC, and to establish a method for the standardization and quality control of FC related to its bioactivity. MATERIALS AND METHODS: In this study, the different ingredients in five cultivars of FC were identified by UPLC-Q/TOF and PCA, and the anti-inflammatory ingredients of FC were predicted and screened by artificial neural network (ANN) and an NF-κB luciferase reporter gene assay system. Using this comprehensive method, we successfully screened the anti-inflammatory markers of different cultivars of FC. RESULTS: Nineteen marker ingredients were confirmed to contribute strongly to the cluster, and eleven compounds in the five cultivars of FC were found to exert potential anti-inflammatory effects. Among these compounds, the NF-κB inhibitor activity of apigenin-7-O-6″-malonyl-glucoside, luteolin-7-O-rutinoside, quercetin-7-O-galactoside, quercetin-3-O-glucoside, apigenin-7-O-rutinoside and apigenin-7-O-glucoside were first reported here. Chlorogenic acid, luteolin-7-O-glucoside, 3,5-dicaffeoylquinic acid and luteolin were confirmed to be the most important anti-inflammatory marker ingredients useful for the quality control of FC. CONCLUSIONS: The proposed efficient and systematic method is helpful for the standardization and quality control of FC. Moreover, this comprehensive strategy may prove to be a powerful technique for the rapid establishment of quality control procedures related to bioactivity for other herbal samples and foods.
Authors: Monika Anna Olszewska; Aleksandra Owczarek; Anna Magiera; Sebastian Granica; Piotr Michel Journal: Int J Mol Sci Date: 2021-10-26 Impact factor: 5.923