Diabetic cardiomyopathy (DCM) is one of the chief diabetes mellitus complications. Inflammation factors may be one reason for the damage from DM. The purpose of this research is to study the potential protective effects of puerarin on DM and the possible mechanisms of action related to NF-κB signal pathway. Following administration of puerarin to the disease model rat, several changes were observed including the changes of serum biochemical index, improved diastolic dysfunction, and enhanced endogenous antioxidant enzymes activities, further NF-κB signaling activation. Puerarin showed cardio-protective effects on DCM by inhibiting inflammation, and it might be a potential candidate for the treatment of DCM.
Forty-five gypsogenin and gypsogenic acid derivatives were synthesized and screened for their cytotoxic activities. Their structures were established using IR, 1H NMR, 13C NMR, and LC-MS spectroscopic data, and they were subjected to extensive biological testing. In the MTT assays, nearly all the compounds displayed good cytotoxicity in the low μM range for several human tumor cell lines (A549, MC3-8, TE-1, HepG-2 and MCF-7). The preliminary bioassay test suggested that most of these gypsogenin and gypsogenic acid derivatives showed different degrees of antitumor activities. In particular, some compounds displayed moderate antitumor activity. They were shown to destroy cell membranes and increase their permeability, which led to the outflow of intracellular nucleic acid.
11 August 2022 in Journal of Enzyme Inhibition and Medicinal Chemistry
Vascular calcification is a process similar to bone formation, which is highly adjustable and active. Currently, there are no specific drugs to delay or reverse vascular calcification. Through the screening of 44 coumarin compounds synthesised by our group, compound 14 was obtained to dose-dependently inhibit the calcification of vascular smooth muscle cells without affecting the normal proliferation of cells, decreasing the intracellular calcium concentration, inhibiting the activity of ALP enzyme. In conclusion, the calcium lowering effect of compound 14 is a potential candidate for drugs for the treatment of vascular calcification.