Objective To observe the clinical effect of benzene sulfonic amlodipine combined with traditional Chinese medicine (TCM) Yangxueqingnao granules for treatment of patients with hypertensive urgencies (HU) with acute headache, and its effect on serum brain derived neurotrophic factor (BDNF) level.Methods A prospective study was conducted, 186 HU patients with acute headache admitted to the Department of Cardiology in the Affiliated Hospital of Southwest University from January 2014 to December 2016 were enrolled, and they were divided into a control group (90 cases) and an observation group (96 cases) by random number table method. The patients in control group received benzene sulfonic amlodipine (10 mg, once a day) and the patients in observation group were additionally given Yangxueqingnao granules (4 g, 3 times a day for consecutive 7 days) on the basis of treatment in control group. The mean arterial pressure (MAP), the nature and location of headache and the levels of serum BNDF were examined before and after treatment and compared between them in the two groups, the degree of headache was evaluated by visual analogue scale (VAS), and the clinical therapeutic effects in the two groups were observed.Results There were no statistical significant differences in MAP (mmHg, 1 mmHg = 0.133 kPa) between the two groups before treatment and at 2 hours, on 1, 3, 7 days after treatment (control group: 99.7±9.5, 94.2±9.1, 88.6±7.6, 81.8±9.3, 75.6±5.3 respectively, the observation group: 95.4±13.5, 91.2±8.1. 88.9±8.7, 83.2±8.6, 77.2±4.8 respectively, allP > 0.05). Compared with the control group, after treatment for 1, 3, 7 days, the nature of acute headache (dull pain, distending pain) was relieved more significantly, the number of patients with whole head headache was decreased more obviously in observation group [dull pain (cases): 16, 8, 3 vs. 28, 24, 18, distending pain (cases): 11, 6, 2 vs. 22, 16, 10, whole head pain (cases): 12, 5, 3 vs. 26, 20, 16, allP < 0.05]. With the prolongation of treatment, the VAS scores in the two groups were gradually decreased, on 7 days after treatment they reached to the lowest levels, and the degree of descent in the observation group was more significant than that in the control group (0.5±0.4 vs. 1.4±0.9,P < 0.05); thelevels of serum BNDF in the two groups were gradually increased after the 1st day of treatment, reached to the highest level on 7 days after treatment,and the degree of increase in observation group was more obvious than that in the control group (ng/L: 24.8±2.3 vs. 17.8±2.2). The therapeutic effective rate of the observation group was significantly higher than that of the control group [70.8% (68/96) vs. 53.3% (48/90),P < 0.05].Conclusion The combination of benzene sulfonic amlodipine and Yangxueqingnao granules can effectively relieve the acute headache in HU patients, and its mechanism is related to the increase in expression of BDNF.

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.

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.