1.Synthesis and anti-breast cancer activity of novel cyclic mono-carbonyl curcumin analogues
Xianhu FENG ; Yongjie CHEN ; Lin CHEN ; Yi HOU ; Wanjun CAO ; Qiang SU
China Pharmacy 2025;36(5):563-567
		                        		
		                        			
		                        			OBJECTIVE To design and synthesize mono-carbonyl curcumin analogues(MCACs) and investigate the activities of them against breast cancer. METHODS The analogues F1, F2, and F3 were obtained by aldol condensation reaction, and their antitumor activities(including the activities of human breast cancer cell MCF-7 and human lung cancer cell A549) were detected by MTT assay [evaluated with half inhibitory concentration(IC50)]. The results of MTT assay were compared with those of curcumin. Bioinformatics methods were used to collect the core targets of analogues F1, F2 and F3 acting on breast cancer, and then molecular docking verification was carried out. The cell experiments were conducted to investigate the effects of high, medium and low concentrations (16, 8, 4 μmol/L) of F1, F2 and F3 on the expression of the first core target protein as well as the effects of medium concentration of F1, F2 and F3 on the expression of cleaved-caspase-3. RESULTS Compared with curcumin, IC50 of analogues F1, F2 and F3 to A549 and MCF-7 cells(except for IC50 of analogue F2 to A549 cells) were decreased significantly(P< 0.05 or P<0.01); among them, IC50 of analogue F2 to MCF-7 cell was the lowest, being(9.67±1.27) μmol/L. Bioinformatics analysis showed that index of affinity of analogues F1, F2 and F3 with the first core target epidermal growth factor receptor (EGFR), protein kinase B (AKT) and AKT were 5.909 2, 8.402 5 and 6.486 6, respectively; high concentration of F1 could significantly reduce the phosphorylation level of EGFR protein in MCF-7 cells(P<0.01), while low, medium, and high concentrations of F2 and high concentration of F3 could significantly reduce the phosphorylation level of AKT protein in MCF-7 cells(P<0.05 or P<0.01). Medium concentration of F1, F2, and F3 could significantly increase the expression level of cleaved- caspase-3 protein in MCF-7 cells(P<0.01). CONCLUSIONS Designed and synthesized MCACs F1, F2 and F3 all have good anti- breast cancer activity, and F2 has better anti-breast cancer activity.
		                        		
		                        		
		                        		
		                        	
2.Treatment of Anxiety and Depression-related Dry Eyes from Regulating the Liver and the Lung
Wanjun HOU ; Pei LIU ; Jun PENG ; Qinghua PENG
Journal of Traditional Chinese Medicine 2024;65(14):1510-1513
		                        		
		                        			
		                        			This paper proposed to understand the pathogenesis and provide syndrome differentiated treatment for anxiety and depression-related dry eyes from the perspective of the liver and the lung, in order to provide ideas for treatment of this disease with traditional Chinese medicine. It is believed that the occurrence and development of anxiety and depression-related dry eyes is related to the ethereal qi and blood damage and blocked circulation of qi and blood. The liver and the lung are the main located zang-fu (脏腑) organs of the disease, and the qi movement, sweat pores, meridians and collaterals abnormalities of the liver and the lung are the pathological basis. The basic pathogenesis is disharmony of the liver and the lung, loss nourishment of eyes, and loss calm of the mind. In clinical practice, the root treatment is to restore the functions of the liver governing ascent and the lung governing descent, and to open up the sweat pores, meridians and collaterals, while the branch treatment is to promote the production of body fluids, nourish yin and calm the mind. Both the root and the branch causes are treated to restore the physiological functions, and Danzhi Xiaoyao Powder (丹栀逍遥散) combined with Shengmai Powder (生脉散) with modification is often used as the basic prescription. 
		                        		
		                        		
		                        		
		                        	
            
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