Dear Editor,Activated hepatic stellate cells(HSCs)synthesizing a large amount of extracellular matrix(ECM)are the key events to hepatic fibrosis.1 However,there are no effective drugs for curing liver fibrosis in the ...Dear Editor,Activated hepatic stellate cells(HSCs)synthesizing a large amount of extracellular matrix(ECM)are the key events to hepatic fibrosis.1 However,there are no effective drugs for curing liver fibrosis in the clinic.1 Therefore,clarifying the formation mechanism of liver fibrosis is of great importance for finding anti-liver fibrosis drug targets.Recently,an increasing amount of research has shown that necroptosis regulated by receptor-interacting protein kinase 3(RIP3)plays an important role in inflammatory disease injury and could be used as a drug target.2 We found that RIP3 was highly expressed in liver tissues of wildtype(WT)mice infected with Schistosoma japonicum(S.japonicum),mainly at 6 w(weeks)and 8 w post-infection(Fig.1a)。展开更多
Decoquinate(1), an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a s...Decoquinate(1), an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a series of decoquinate derivatives was designed, synthesized, evaluated as a new class of antischistosomal agents against S. japonicum adult worms in vitro. Among them, compound 15 killed 100% of adult S. japonicum in 72 h at the concentration of 10 mmol/L in vitro, exhibited stronger wormkilling activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents.展开更多
基金supported by grants from the National Key R&D program(2017YFA0506002)the National Natural Science Foundation of China(81802035,81630092)+1 种基金Jiangsu Provincial Department of Science and Technology(BK20192005)the Public Health Research Center at Jiangnan University(JUPH201812).
文摘Dear Editor,Activated hepatic stellate cells(HSCs)synthesizing a large amount of extracellular matrix(ECM)are the key events to hepatic fibrosis.1 However,there are no effective drugs for curing liver fibrosis in the clinic.1 Therefore,clarifying the formation mechanism of liver fibrosis is of great importance for finding anti-liver fibrosis drug targets.Recently,an increasing amount of research has shown that necroptosis regulated by receptor-interacting protein kinase 3(RIP3)plays an important role in inflammatory disease injury and could be used as a drug target.2 We found that RIP3 was highly expressed in liver tissues of wildtype(WT)mice infected with Schistosoma japonicum(S.japonicum),mainly at 6 w(weeks)and 8 w post-infection(Fig.1a)。
基金supported by Laboratory Research Fund funded by Key Laboratory of National Health and Family Planning Commission on Parasitic Disease Control and Prevention,Jiangsu Provincial Key Laboratory on Parasite and Vector Control Technology,Parasitic Disease Prevention and Control Platform(No.WK014-002)fund from the Department of Science and Technology of Jiangsu Province(No.BY2016022-37)+5 种基金fund from the National Natural Science Foundation of China(Nos.21472069,30972581,8120316)fund from the Natural Science Foundation of Jiangsu Province(Nos.BK2012544,BK20151120)fund from the scientific research projects of Jiangsu Provincial Commission of Health and Family Planning(No.H201635)fund from the scientific research projects of Wuxi City Commission of Health and Family Planning(No.Q201656)fund from the Ministry of Education of China(No.JUSRP51516)Jiangsu Science and Technology Department(No.BM2015024)
文摘Decoquinate(1), an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a series of decoquinate derivatives was designed, synthesized, evaluated as a new class of antischistosomal agents against S. japonicum adult worms in vitro. Among them, compound 15 killed 100% of adult S. japonicum in 72 h at the concentration of 10 mmol/L in vitro, exhibited stronger wormkilling activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents.