Progress on the relationship of aldehyde dehydrogenase 2 with human diseases and its small-molecule activators / 药学实践杂志

Aldehyde dehydrogenase 2 (ALDH2) is one of important factors against from the damage under oxidative stress in human body. A high proportion of East Asians carry ALDH2 inactive mutation gene. There are many diseases closely related to ALDH2, such as cardiovascular diseases, neurodegenerative diseases and liver diseases. Recent studies also have found that ALDH2 is associated with ferroptosis. Therefore, ALDH2 has becoming a potential target for the treatment of the above related diseases. Several types of small molecule activators with potential value of clinical application have been reported. The research progress on the structure and function of ALDH2 , the relationship with human diseases and its activators were summarized in this paper.

Progress on physiological activities and synthetic methods of ebselen / 药学实践杂志

Organoselenium compounds are bioactive substances with extensive physiological activities .As a representa-tive compound ,ebselen could be used as mimics of glutathione peroxidase ,and in the treatment of many diseases ,such as car-diovascular and cerebrovascular diseases ,inflammation and noise-induced hearing loss .the research progress in physiological activities and synthetic methods of ebselen were reviewed in this paper .

Research progress in the catalytic rearrangement reaction of benzyl phenyl ethers / 药学实践杂志

The rearrangement reaction of benzyl phenyl ethers (BPE) plays an important role in the organic chemistry and drug synthesis .This paper briefly reviewed the rearrangement reaction and its possible mechanism in various catalytic sys-tems ,such as trifluoroacetic acid ,phosphotungstic acid ,cyclodextrin ,molten tin and aluminium bromide .

Synthesis, XRD analysis and anti-tumor activity of novel compounds containing tetrahydronaphthalen-2-ol / 药学实践杂志

Objective To synthesize the enantiomers of ( E)-6-methoxy-1-(3,4,5-trimethoxybenzylidene )-1,2,3,4-tetra-hydronaphthalen-2-ol,determine their structures by XRD and evaluate their anti-tumor activity in vitro.Methods The target compounds were prepared from 2,6-Dimethoxybenzoyl chloride.The key intermediate,(E)-6-methoxy-1-(3,4,5-trimethoxybenzylidene)-1,2,3,4-tetrahydronaphthalen-2-one,was obtained through Cornforth reduction and Knoevenael reaction ,and the final R,S compounds were got by CBS asymmetric reduction .The structure of the target compounds were determined by XRD .The target compounds were rested by anti-tu-bulin and anti-tumor assay.Results The structure of the target compounds were determined by 1 H NMR,13 C NMR,MS,and XRD analy-sis.The yield of asymmetric reduction reaction was 90.3%,e.e.%was 99.04%,in vitro anti-tumor assay showed all of the S isomer had stronger anticancer activity than the R isomer ,especially on CCRF-CEM cell(IC50 =1 nmol/L),HCT-116 cell(IC50 =0.14μmol/L) and inhibition of tubulin polymerization ( IC50 =0.41μmol/L) .Conclusion The CBS asymmetric reduction was a good way to get high-yield and high optical purity compound .The S isomer with outstanding anticancer activity was worth further research .