Chalcones are polyphenolic flavonoid substances with various pharmacological effects and low toxicity.In this study, 15 novel trifluoromethyl chalcone derivatives (3a-3o) were designed and synthesized using the chalcone nucleus of natural licorice chalcone as the lead compound skeleton in order to find the candidate drugs with high efficiency and low toxicity against cervical cancer.The structures of the target compounds were confirmed by 1H NMR, 13C NMR and HRMS. The inhibitory activities of compounds 3a-3o, licorice chalcone, cisplatin and Nutlin3a on SiHa, HeLa and C-33A human cervical cancer cells and H8 and HaCaT normal cells were determined by MTT assay, and the structure-activity relationship was analyzed.Transwell and flow cytometry methods were used to assess the target compounds'' ability to inhibit cell migration and invasion, promote apoptosis, and arrest the cell cycle.Molecular docking technology was used to further study the binding characteristics of the target compound with MDM2 protein.The results showed that the compounds had different degrees of inhibitory activity against the three types of cervical cancer cells.Compound 3n showed the strongest activity against HeLa cells (IC50 = 11.69 μmol/L), which was superior to the lead compound, and had lower toxicity against the two normal cells.Compound 3n was found to significantly inhibit the migration and invasion of HeLa cells, induce apoptosis and arrest the cell cycle at G2/M phase.The results of molecular docking showed that the effective binding of compound 3n to MDM2 protein may be one of its anti-tumor mechanisms.This study provides an experimental basis for the screening of new anti-cervical cancer candidate drug from chalcone derivatives.

There are about 100 species in the genus Coreopsis which distributed in the America, south of Africa and Hawaiian Islands, and 7 species are distributed in China. The inflorescences of Coreopsis tinctoria Nutt. is the Uigur herb 'Snow chrysanthemum' which is named 'Shemuju' with the effects of heat-cleaning, detoxicating, dampness-dissipating and dysentery-curing in the Xinhua Herbal Scheme. The chemical constituents from Coreopsis plants mainly contain flavonoids, phenylpropanoids, sesquiterpenes, and sterols, which show anti-inflammatory activities in modern pharmaceutical research. This article presents an overview of the chemical constituents and pharmaceutical activities, prospects of development and exploitation of Coreopsis plants, hopefully to provide a basis for further research and development of Coreopsis plants.
Animals ; Coreopsis ; chemistry ; Drug Discovery ; methods ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Plants, Medicinal ; chemistry

Objective To conduct a pharamacognosical study on snow chrysanthemum (coreopsis tinctoria nutt.),and lay a theoretical foundation for its origin identification. Methods The properties, structure,and micro-characters of snow chrysanthemum powder were observed and described; the main components were analyzed, and finger-print was built with HPLC, aiming at analyzing snow chrysanthemum from property,microscopic,and physicochemical aspects. Results The macro-character and micro-characters of snow chrysanthemum are described as follows: the capitula of snow chrysanthemum is consistent with that of asteraceae species with two colors of the ray floret,yellow on the upper part,and purple brown in the middle of basal part. Powder under the microscope presents yellow spine spheroidal pollen grains, light yellow to brown red secretary canal scrap, papilla with simple cellular hair,basal part cell,and inner wall cells of pollen sac. The HPLC fingerprint was determined. Conclusion Snow chrysanthemum shares the common features with asteraceae species, and is different from Coreopsis lanceolate L,and Coreopsis grandiflora Hogg in the same genus. This study supplemented the gap in the pharacognosical study of snow chrysanthemum for origin identification.

OBJECTIVE To design and synthesize of a series of novel azachalcone derivatives and study of their anti-cervical cancer activity and mechanism of action. METHODS A series of novel chalcone derivatives were designed and synthesized by using glycyrrhiza chalcone as the lead compound and VEGFR-2 and P-gp as the target sites using the active substructure splicing principle, and the structures were characterized by 1H-NMR, 13C-NMR and HR-MS. MTT, ELISA, co-dosing with cisplatin, Western blotting and molecular docking assays were used to preliminarily evaluate the proliferation inhibitory activity and mechanism of action of the target compounds on cervical cancer and cisplatin-resistant cervical cancer cells. RESULTS Compound 7h showed some antitumor activity and reversal of cisplatin resistance, and had some inhibitory effects on phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, with no significant differences on P-gp protein expression compared with the blank group in the concentration range of 0.5, 1.0, 1.5 μmol·L−1. CONCLUSION The anti-cervical cancer activity and reversal of cisplatin resistance of compound 7h may be related to its inhibition of VEGFR-2 and P-gp targets.