Recombinant Escherichia coli pUDP,which overexpressed uridine phosphorylase（UPase）,was constructed.0.5 mmol·L 1lactose had a similar induction effect as the commonly used inducer IPTG during 2.5-5.5 h of cell g...Recombinant Escherichia coli pUDP,which overexpressed uridine phosphorylase（UPase）,was constructed.0.5 mmol·L 1lactose had a similar induction effect as the commonly used inducer IPTG during 2.5-5.5 h of cell growth.The lactose-induced UPase was stable at 50°C.Wet cells of pUDP was used as catalyst to biosynthesize 5-fluorouridine from 30 mmol·L 1uridine and 5-fluorouracil in phosphate buffer（pH 7.0）catalyzed at 50°C for 1.5 h and the yield of 5-fluorouridine was higher than 68%.Under the optimum reaction conditions for production of 5-fluorouridine,5-methyluridine and azauridine were synthesized from uridine by pUDP,the yield was 61.7%and 47.2%respectively.Deoxynucleosides were also synthesized by pUDP,but the yield was only about 20%.展开更多
New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were ev...New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were evaluated.It was demonstrated that most of compounds had stronger antiviral acitivity than acyclovir,while their toxicities were similar or lower to acyclovir.展开更多
An environmentally benign and highly efficient one-pot preparation of α-aminophosphonates under solvent-free conditions was developed. By employing this method, 5-aminophosphonate substituted pyrimidine nucleosides w...An environmentally benign and highly efficient one-pot preparation of α-aminophosphonates under solvent-free conditions was developed. By employing this method, 5-aminophosphonate substituted pyrimidine nucleosides were synthesized in good to excellent yields starting from 5-forrnyl-2＇-deoxyuridine, aniline and dimethylphosphite.展开更多
Pyrimidine nucleosides(PN)are abundant in mammalian milk and mainly involved in glycogen deposition and lipid metabolism.To investigate the effects of maternal supplementation with pyrimidine nucleoside on glucose,fat...Pyrimidine nucleosides(PN)are abundant in mammalian milk and mainly involved in glycogen deposition and lipid metabolism.To investigate the effects of maternal supplementation with pyrimidine nucleoside on glucose,fatty acids(FAs),and amino acids(AAs)metabolism in neonatal piglets.Forty pregnant sows were randomly assigned into the control(CON)group(fed a basal diet,n=20)or the PN group(fed a basal diet supplemented with PN at 150 g/t,n=20).Litter size,born alive and birth litter weight were recorded.The serum and placenta of sows,and jejunum and liver of neonatal piglets were sampled.The results indicated that supplementing sow diets with PN decreased birth mortality and increased the birth weight of piglets(P<0.05).In addition,neonates from sows supplemented with PN had higher glucose levels in serum and liver compared with the CON group(P<0.05).Moreover,maternal PN supplementation regulated the ratio of saturated FAs and polyunsaturated FAs,and AAs content in serum and liver of piglets(P<0.05).Furthermore,an up-regulation of m RNA expression of genes related to glucose and AA transport were observed in the neonatal jejunum from the PN group(P<0.05).Additionally,hepatic protein expressions of phosphorylated hormone-sensitive lipase(P-HSL),HSL,sterol regulatory element-binding transcription factor 1c(SREBP-1c),and phosphorylated protein kinase B(P-AKT)was higher in the piglets from the PN group than the CON group(P<0.05).Together,maternal PN supplementation may regulate nutrient metabolism of neonatal piglets by modulating the gene expression of glucose and AA transporters in placenta and jejunum,and the gene and protein expression of key enzymes related to lipid metabolism in liver of neonatal piglets,which may improve the reproductive performance of sows.展开更多
A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compound...A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compounds were stronger than those of acyclovir, while their toxicities were similar to those of acyclovir.展开更多
Novel pyrimidine nucleoside-3,5-dicyanopyridine hybrids （4） or pyridine attached acylureas （5） were selectively and efficiently prepared from the reaction of 2′-deoxyuddin-5-yl-methylene malononitrile （1）, malo...Novel pyrimidine nucleoside-3,5-dicyanopyridine hybrids （4） or pyridine attached acylureas （5） were selectively and efficiently prepared from the reaction of 2′-deoxyuddin-5-yl-methylene malononitrile （1）, malononitrile （2） and thiophenol （3） or from an unexpected uracil ring-opening and pyddine ring-forming sequence via the reaction of 1 and 3. It is the first time such a sequence has ever been reported.展开更多
The chemical synthesis of Guanine arabinoside （ara-G） is extremely complex, time-consuming, and seriously polluted. A two-step enzymatic synthesis process was developed to acquire ara-G easily. 2,6-Diaminopurine ara...The chemical synthesis of Guanine arabinoside （ara-G） is extremely complex, time-consuming, and seriously polluted. A two-step enzymatic synthesis process was developed to acquire ara-G easily. 2,6-Diaminopurine arabinoside （ara-DA） was first synthesized with purine nucleoside phosphorylase and pyrimidine nucleoside phosphorylase produced by Enterobacter aerogenes DGW-07. The conversion yield of ara-DA could reach above 90% when the reaction liquid contained 30 mmol·L^-1 uracil arabinoside as arabinose donor, 10 mmol·L^- 1 2,6-diaminopurine as arabinose acceptor in pH 7.0 20 mmol·L^-1 phosphate buffer, and reacted at 60℃ for 48h. Then, ara-DA was effectively transformed into ara-G with adenylate deaminase produced by Aspergillus oryzae DAW-01. The total process had no complex separation and purification.展开更多
Promoted and mediated by an ionic liquid-[bmim][BF4], fused pyrans or arylbis（4-hydroxy-6-methyl-2-oxo-2H-pyran-3- yl）methanes were efficiently and selectively prepared from the reaction of aldehyde and 4-hydroxy-6-...Promoted and mediated by an ionic liquid-[bmim][BF4], fused pyrans or arylbis（4-hydroxy-6-methyl-2-oxo-2H-pyran-3- yl）methanes were efficiently and selectively prepared from the reaction of aldehyde and 4-hydroxy-6-methyl-2-oxo-pyran with or without acetic anhydride. By using these novel procedures, pyrimidine nucleoside-fused pyran and arylbis（pyranon-3-yl）methane hybrids with potential biological activities were constructed.展开更多
基金Supported by"Production,Education&Research"item of Shanghai Baoshan(08-H-4)
文摘Recombinant Escherichia coli pUDP,which overexpressed uridine phosphorylase（UPase）,was constructed.0.5 mmol·L 1lactose had a similar induction effect as the commonly used inducer IPTG during 2.5-5.5 h of cell growth.The lactose-induced UPase was stable at 50°C.Wet cells of pUDP was used as catalyst to biosynthesize 5-fluorouridine from 30 mmol·L 1uridine and 5-fluorouracil in phosphate buffer（pH 7.0）catalyzed at 50°C for 1.5 h and the yield of 5-fluorouridine was higher than 68%.Under the optimum reaction conditions for production of 5-fluorouridine,5-methyluridine and azauridine were synthesized from uridine by pUDP,the yield was 61.7%and 47.2%respectively.Deoxynucleosides were also synthesized by pUDP,but the yield was only about 20%.
基金the National Natural Science Foundation of China(No.30572240)
文摘New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were evaluated.It was demonstrated that most of compounds had stronger antiviral acitivity than acyclovir,while their toxicities were similar or lower to acyclovir.
基金National Natural Science Foundation of China(Nos.20772025 and 20972042)the Program for Science & Technology Innovation Talents in Universities of Henan Province(No.2008HASTIT006)+1 种基金Innovation Scientists and Technicians Troop Construction Projects of Henan Province(No.104100510019)the Natural Science Foundation of Henan Province(Nos.092300410192 and 094300510054)
文摘An environmentally benign and highly efficient one-pot preparation of α-aminophosphonates under solvent-free conditions was developed. By employing this method, 5-aminophosphonate substituted pyrimidine nucleosides were synthesized in good to excellent yields starting from 5-forrnyl-2＇-deoxyuridine, aniline and dimethylphosphite.
基金supported by grants from National key R&D program of China(2021YFD1301002)the Tianjin Synthetic Biotechnology Innovation Capacity Improvement Project(TSBICIP-CXRC-031)。
文摘Pyrimidine nucleosides(PN)are abundant in mammalian milk and mainly involved in glycogen deposition and lipid metabolism.To investigate the effects of maternal supplementation with pyrimidine nucleoside on glucose,fatty acids(FAs),and amino acids(AAs)metabolism in neonatal piglets.Forty pregnant sows were randomly assigned into the control(CON)group(fed a basal diet,n=20)or the PN group(fed a basal diet supplemented with PN at 150 g/t,n=20).Litter size,born alive and birth litter weight were recorded.The serum and placenta of sows,and jejunum and liver of neonatal piglets were sampled.The results indicated that supplementing sow diets with PN decreased birth mortality and increased the birth weight of piglets(P<0.05).In addition,neonates from sows supplemented with PN had higher glucose levels in serum and liver compared with the CON group(P<0.05).Moreover,maternal PN supplementation regulated the ratio of saturated FAs and polyunsaturated FAs,and AAs content in serum and liver of piglets(P<0.05).Furthermore,an up-regulation of m RNA expression of genes related to glucose and AA transport were observed in the neonatal jejunum from the PN group(P<0.05).Additionally,hepatic protein expressions of phosphorylated hormone-sensitive lipase(P-HSL),HSL,sterol regulatory element-binding transcription factor 1c(SREBP-1c),and phosphorylated protein kinase B(P-AKT)was higher in the piglets from the PN group than the CON group(P<0.05).Together,maternal PN supplementation may regulate nutrient metabolism of neonatal piglets by modulating the gene expression of glucose and AA transporters in placenta and jejunum,and the gene and protein expression of key enzymes related to lipid metabolism in liver of neonatal piglets,which may improve the reproductive performance of sows.
基金the National Natural Science Foundation of China(No.30572240).
文摘A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compounds were stronger than those of acyclovir, while their toxicities were similar to those of acyclovir.
基金the National Natural Science Foundation of China(No.20772025)the Program for Science & Technology Innovation Talents in Universities of Henan Province(No.2008HASTIT006)the Natural Science Foundation of Department of Education of Henan Province(No.2008A150013)
文摘Novel pyrimidine nucleoside-3,5-dicyanopyridine hybrids （4） or pyridine attached acylureas （5） were selectively and efficiently prepared from the reaction of 2′-deoxyuddin-5-yl-methylene malononitrile （1）, malononitrile （2） and thiophenol （3） or from an unexpected uracil ring-opening and pyddine ring-forming sequence via the reaction of 1 and 3. It is the first time such a sequence has ever been reported.
基金Supported by the Innovation Fund for Technology Based Firms from Ministry of Science and Technology of China(07C26213101283)
文摘The chemical synthesis of Guanine arabinoside （ara-G） is extremely complex, time-consuming, and seriously polluted. A two-step enzymatic synthesis process was developed to acquire ara-G easily. 2,6-Diaminopurine arabinoside （ara-DA） was first synthesized with purine nucleoside phosphorylase and pyrimidine nucleoside phosphorylase produced by Enterobacter aerogenes DGW-07. The conversion yield of ara-DA could reach above 90% when the reaction liquid contained 30 mmol·L^-1 uracil arabinoside as arabinose donor, 10 mmol·L^- 1 2,6-diaminopurine as arabinose acceptor in pH 7.0 20 mmol·L^-1 phosphate buffer, and reacted at 60℃ for 48h. Then, ara-DA was effectively transformed into ara-G with adenylate deaminase produced by Aspergillus oryzae DAW-01. The total process had no complex separation and purification.
基金the National Natural Science Foundation of China(No.20772025)the Program for Science & Technology Innovation Talents in Universities of Henan Province(No.2008HASTIT006)the Natural Science Foundation of Department of Education of Henan Province(No.2008A150013).
文摘Promoted and mediated by an ionic liquid-[bmim][BF4], fused pyrans or arylbis（4-hydroxy-6-methyl-2-oxo-2H-pyran-3- yl）methanes were efficiently and selectively prepared from the reaction of aldehyde and 4-hydroxy-6-methyl-2-oxo-pyran with or without acetic anhydride. By using these novel procedures, pyrimidine nucleoside-fused pyran and arylbis（pyranon-3-yl）methane hybrids with potential biological activities were constructed.
