The electrochemical behavior of trifluoperazine at decanethiol self-assembledmonolayer (SAM) modified gold electrodes (i. e. C_(10) H_(21) SH/Au) has been studied,Trifluoperazine can effectively accumulate on C_(10) H...The electrochemical behavior of trifluoperazine at decanethiol self-assembledmonolayer (SAM) modified gold electrodes (i. e. C_(10) H_(21) SH/Au) has been studied,Trifluoperazine can effectively accumulate on C_(10) H_(21) SH/Au electrodes and generate asensitive anodic peak at about 0.63 V (vs. SCE) in 0.05 mol/L pH 9.4 Na_2 B_4 O_7 buffer solution.Under the selected conditions, the anodic peak current was linear to trifluoperazine concentrationin the range of 5.0 X 10^(-7)-3.O X 10^(-3) mol/Lwith correlation coefficient of 0.997, thedetection limit was 3.0 X 10^(-5) mol/L. This method was applied to the determination oftrifluoperazine in drug samples and the recovery was 97.3%-104.0% It was found that sodium dodecylsulfate (SDS) could make the anodic peak current increase. In the presence of SDS, the peak at about0.63 V turned into two peaks, resulting from the change of the electrochemical mechanism.展开更多
INTRODUCTIONCalmodulin(CaM),widely distributed in almost alleukaryotic cells,is a major intracellular calcium receptorresponsible for mediating the Ca<sup>2+</sup> signal to a multitude ofdifferent enzym...INTRODUCTIONCalmodulin(CaM),widely distributed in almost alleukaryotic cells,is a major intracellular calcium receptorresponsible for mediating the Ca<sup>2+</sup> signal to a multitude ofdifferent enzyme systems and is thought to play a vital rolein the regulation of cell proliferative cycle.Recently,展开更多
Severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2)continues to evolve,generating new variants that pose a threat to global health;therefore,it is imperative to obtain safe and broad‐spectrum antivirals aga...Severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2)continues to evolve,generating new variants that pose a threat to global health;therefore,it is imperative to obtain safe and broad‐spectrum antivirals against SARS‐CoV‐2 and its variants.To this end,we screened compounds for their ability to inhibit viral entry,which is a critical step in virus infection.Twenty compounds that have been previously reported to inhibit SARS‐CoV‐2 replication were tested by using pseudoviruses containing the spike protein from the original strain(SARS‐CoV‐2‐WH01).The cytotoxicity of these compounds was determined.Furthermore,we identified six compounds with strong antagonistic activity against the WH01 pseudovirus,and low cytotoxicity was identified.These compounds were then evaluated for their efficacy against pseudoviruses expressing the spike protein from B.1.617.2(Delta)and B.1.1.529(Omicron),the two most prevalent circulating strains.These assays demonstrated that two phenothiazine compounds,trifluoperazine 2HCl and thioridazine HCl,inhibit the infection of Delta and Omicron pseudoviruses.Finally,we discovered that these two compounds were highly effective against authentic SARS‐CoV‐2 viruses,including the WH01,Delta,and Omicron strains.Our study identified potential broad‐spectrum SARS‐CoV‐2 inhibitors and provided insights into the development of novel therapeutics.展开更多
基金Supported by the National Natural Science Foundation of China (20173040)
文摘The electrochemical behavior of trifluoperazine at decanethiol self-assembledmonolayer (SAM) modified gold electrodes (i. e. C_(10) H_(21) SH/Au) has been studied,Trifluoperazine can effectively accumulate on C_(10) H_(21) SH/Au electrodes and generate asensitive anodic peak at about 0.63 V (vs. SCE) in 0.05 mol/L pH 9.4 Na_2 B_4 O_7 buffer solution.Under the selected conditions, the anodic peak current was linear to trifluoperazine concentrationin the range of 5.0 X 10^(-7)-3.O X 10^(-3) mol/Lwith correlation coefficient of 0.997, thedetection limit was 3.0 X 10^(-5) mol/L. This method was applied to the determination oftrifluoperazine in drug samples and the recovery was 97.3%-104.0% It was found that sodium dodecylsulfate (SDS) could make the anodic peak current increase. In the presence of SDS, the peak at about0.63 V turned into two peaks, resulting from the change of the electrochemical mechanism.
基金the Natural Science Fundation of Jiangsu Province,№BK95141307
文摘INTRODUCTIONCalmodulin(CaM),widely distributed in almost alleukaryotic cells,is a major intracellular calcium receptorresponsible for mediating the Ca<sup>2+</sup> signal to a multitude ofdifferent enzyme systems and is thought to play a vital rolein the regulation of cell proliferative cycle.Recently,
基金supported by grants from National Key R&D Program of China(2020YFA0707600 to Z.Z.and X.L.)the National Natural Science Foundation of China(81930063 and 81971948 to J.W.and X.L.)hinese Academy of Medical Science(CAMS)Innovation Fund for Medical Sciences(2021-I2M-1-038 to J.W.)。
文摘Severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2)continues to evolve,generating new variants that pose a threat to global health;therefore,it is imperative to obtain safe and broad‐spectrum antivirals against SARS‐CoV‐2 and its variants.To this end,we screened compounds for their ability to inhibit viral entry,which is a critical step in virus infection.Twenty compounds that have been previously reported to inhibit SARS‐CoV‐2 replication were tested by using pseudoviruses containing the spike protein from the original strain(SARS‐CoV‐2‐WH01).The cytotoxicity of these compounds was determined.Furthermore,we identified six compounds with strong antagonistic activity against the WH01 pseudovirus,and low cytotoxicity was identified.These compounds were then evaluated for their efficacy against pseudoviruses expressing the spike protein from B.1.617.2(Delta)and B.1.1.529(Omicron),the two most prevalent circulating strains.These assays demonstrated that two phenothiazine compounds,trifluoperazine 2HCl and thioridazine HCl,inhibit the infection of Delta and Omicron pseudoviruses.Finally,we discovered that these two compounds were highly effective against authentic SARS‐CoV‐2 viruses,including the WH01,Delta,and Omicron strains.Our study identified potential broad‐spectrum SARS‐CoV‐2 inhibitors and provided insights into the development of novel therapeutics.