Four novel 5-substituted pyridine-2(1H)-one derivatives were designed and synthesized by using addition-elimination reactions.The structures of these novelly synthesized compounds were verified by ~1H NMR,ESI-MS and s...Four novel 5-substituted pyridine-2(1H)-one derivatives were designed and synthesized by using addition-elimination reactions.The structures of these novelly synthesized compounds were verified by ~1H NMR,ESI-MS and single crystal X-ray diffraction.Furthermore,all four compounds(most notably compound 7a) were found to be highly efficient against hepatitis B virus (HBV) in cultured HepG2 2.2.15 cell,making them promising drug candidates for potential bioactive molecule against hepatitis B.展开更多
Hepatitis B virus(HBV)infection causing acute and chronic hepatitis is a serious problem worldwide,whereas the current treatment methods are unsatisfactory.Traditional Chinese herbs that have long been used for medici...Hepatitis B virus(HBV)infection causing acute and chronic hepatitis is a serious problem worldwide,whereas the current treatment methods are unsatisfactory.Traditional Chinese herbs that have long been used for medicinal purposes are fascinating sources for novel anti-HBV candidates.This paper summarizes the progress of anti-HBV constituents from diverse medicinal plants in China to provide information for searching new anti-HBV drugs from natural sources.展开更多
Human ISG20 gene was cloned and the effect of its anti-HBV was primarily studied. The ISG20 gene was amplified from HeLa cells by RT-PCR and recombinant vector expressing ISG20 was constructed by genetic engineering. ...Human ISG20 gene was cloned and the effect of its anti-HBV was primarily studied. The ISG20 gene was amplified from HeLa cells by RT-PCR and recombinant vector expressing ISG20 was constructed by genetic engineering. The overexpression of ISG20 in HepG2 cells was detected by Western blot and the levels of secretion of HBs antigen and HBe antigen tested by ELISA. The results showed that: (1) Sequence of ISG20 cloned was consistent to that published in Genebank; (2) Recombinant vector expressing ISG20 could be expressed in HepG2 cells by transfection; (3) The overexpression of ISG20 protein could reduce the levels of the secretion of HBs antigen and HBe antigen in transfected HepG2 cells. It was suggested that the overexpression of recombinant ISG20 in culture cells could reduce the synthesis of HBV proteins.展开更多
A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity an...A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 μmol/L and 2530 μmol/L, respectively.展开更多
A series of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the des...A series of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.展开更多
Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with...Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with the IC50 values of sub μmol/L level. The ICso of anti-HBsAg activities of 5c and 5j reached 0.01 μmol/L respectively which were 16 fold more potent than that of 3TC. Compounds 3, 5e, 5g, 5h and 5i showed admirable inhibitory activity to both HBsAg and HBeAg. The bioassay results indicated the S-substituted 7-mercapto-4-methylcoumarin analogs merit attention as novel anti-HBV agents.展开更多
Fourteen new geranyl phenyl ethers(1–14)along with three known compounds(15–17)were isolated from Illicium micranthum,and their structures were elucidated by comprehensive spectroscopic methods.Illimicranins A–H(1...Fourteen new geranyl phenyl ethers(1–14)along with three known compounds(15–17)were isolated from Illicium micranthum,and their structures were elucidated by comprehensive spectroscopic methods.Illimicranins A–H(1–8)were characterized as geranyl vanillin ethers,while 9 and 10 were dimethyl acetal derivatives.Illimicranins I and J(11 and 12)were rare geranyl isoeugenol ethers.Illimicranins K and L(13 and 14)represented the first example of geranyl guaiacylacetone ether and geranyl zingerone ether,respectively.Compounds 1,2 and 15 exhibited anti-HBV(hepatitis B virus)activity against HBsAg(hepatitis B surface antigen)and HBeAg(hepatitis B e antigen)secretion,and HBV DNA replication.展开更多
A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug (NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a "one pot synthesis" method and their in ...A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug (NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a "one pot synthesis" method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index (SI) values of 0.48μmol/L and 763.72, respectively.展开更多
文摘Four novel 5-substituted pyridine-2(1H)-one derivatives were designed and synthesized by using addition-elimination reactions.The structures of these novelly synthesized compounds were verified by ~1H NMR,ESI-MS and single crystal X-ray diffraction.Furthermore,all four compounds(most notably compound 7a) were found to be highly efficient against hepatitis B virus (HBV) in cultured HepG2 2.2.15 cell,making them promising drug candidates for potential bioactive molecule against hepatitis B.
基金This work was financially supported by the Program of Yunling Scholarship,the Youth Innovation Promotion Association,CAS,the Applied Basic Research Programs of Yunnan Province(2017FB137)the CAS Hundred Talents Program,and the CAS"Light of West China"Program(Western Youth Scholars"A").
文摘Hepatitis B virus(HBV)infection causing acute and chronic hepatitis is a serious problem worldwide,whereas the current treatment methods are unsatisfactory.Traditional Chinese herbs that have long been used for medicinal purposes are fascinating sources for novel anti-HBV candidates.This paper summarizes the progress of anti-HBV constituents from diverse medicinal plants in China to provide information for searching new anti-HBV drugs from natural sources.
基金a grant from the National KeyBasic Research Program of China (No. 20014CB510 008)
文摘Human ISG20 gene was cloned and the effect of its anti-HBV was primarily studied. The ISG20 gene was amplified from HeLa cells by RT-PCR and recombinant vector expressing ISG20 was constructed by genetic engineering. The overexpression of ISG20 in HepG2 cells was detected by Western blot and the levels of secretion of HBs antigen and HBe antigen tested by ELISA. The results showed that: (1) Sequence of ISG20 cloned was consistent to that published in Genebank; (2) Recombinant vector expressing ISG20 could be expressed in HepG2 cells by transfection; (3) The overexpression of ISG20 protein could reduce the levels of the secretion of HBs antigen and HBe antigen in transfected HepG2 cells. It was suggested that the overexpression of recombinant ISG20 in culture cells could reduce the synthesis of HBV proteins.
文摘A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 μmol/L and 2530 μmol/L, respectively.
文摘A series of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.
基金a grant from National Science Foundation of China(No.20272010 and 30200348)awarded to P.Xia and Y.Chert,respectively.
文摘Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with the IC50 values of sub μmol/L level. The ICso of anti-HBsAg activities of 5c and 5j reached 0.01 μmol/L respectively which were 16 fold more potent than that of 3TC. Compounds 3, 5e, 5g, 5h and 5i showed admirable inhibitory activity to both HBsAg and HBeAg. The bioassay results indicated the S-substituted 7-mercapto-4-methylcoumarin analogs merit attention as novel anti-HBV agents.
基金supported by Chongqing Research and Frontier Technology(cstc2020jcyj-msxmX0537)the State Key Laboratory of Drug Research(SIMM1903KF-14)Fundamental Research Funds for the Central Universities(No.2020CDJ-LHZZ-006)。
文摘Fourteen new geranyl phenyl ethers(1–14)along with three known compounds(15–17)were isolated from Illicium micranthum,and their structures were elucidated by comprehensive spectroscopic methods.Illimicranins A–H(1–8)were characterized as geranyl vanillin ethers,while 9 and 10 were dimethyl acetal derivatives.Illimicranins I and J(11 and 12)were rare geranyl isoeugenol ethers.Illimicranins K and L(13 and 14)represented the first example of geranyl guaiacylacetone ether and geranyl zingerone ether,respectively.Compounds 1,2 and 15 exhibited anti-HBV(hepatitis B virus)activity against HBsAg(hepatitis B surface antigen)and HBeAg(hepatitis B e antigen)secretion,and HBV DNA replication.
基金supported by the National Natural Science Foundation of China(Nos.20962004,81260473)Projects of Guizhou Science and Technology Department(Nos.2013-3031,2012-3013)Excellent Youth Scientific Talents Foundation of Guizhou(No.2013-45)
文摘A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug (NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a "one pot synthesis" method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index (SI) values of 0.48μmol/L and 763.72, respectively.