In addition to six known flavonoids quercitrin, hyperoside, avicularin, rutin, quercetin and kaemferol, a new flavonol glycoside named 6″_O_acetyl quercetin 3_O_β_ D _alloside (1) was isolated from the aerial par...In addition to six known flavonoids quercitrin, hyperoside, avicularin, rutin, quercetin and kaemferol, a new flavonol glycoside named 6″_O_acetyl quercetin 3_O_β_ D _alloside (1) was isolated from the aerial parts of Hypericum perforatum L. The structures were determined on the basis of spectroscopic methods (UV, IR, FAB_MS, 1H_NMR and 13 C NMR). Antifungal assay of all compounds showed that metabolite 1, quercitrin and quercetin were inhibitory to the growth of phytopathogenic fungus Helminthosporium sativum Pamel King et Bakke with minimum inhibitory concentrations (MICs) of 25, 50 and 50 μg/mL, respectively. Moreover, glycoside 1 and quercitrin were also shown to be able to inhibit the growth of Fusarium graminearum Schw. with MIC of 100 μg/mL. The MICs of ketoconazole used as control against the test fungi were 0.5 μg/mL in our assay.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
Nucleoside phosphorylases (NPases) were found to be induced in Enterobacter aerogenes DGO-04, and cytidine and cytidine 5′-monophosphate (CMP) were the best inducers. Five mmol/L to fifteen mmol/L cytidine or CMP cou...Nucleoside phosphorylases (NPases) were found to be induced in Enterobacter aerogenes DGO-04, and cytidine and cytidine 5′-monophosphate (CMP) were the best inducers. Five mmol/L to fifteen mmol/L cytidine or CMP could distinctly increase the activities of purine nucleoside phosphorylase (PNPase), uridine phosphorylase (UPase) and thymidine phosphorylase (TPase) when they were added into medium from 0 to 8 h. In the process of enzymatic synthesis of adenine arabinoside from adenine and uracil arabinoside with wet cells of Enterobacter aerogenes DGO-04 induced by cytidine or CMP, the reaction time could be shortened from 36 to 6 h. After enzymatic reaction the activity of NPase in the cells induced remained higher than that in the cells uninduced.展开更多
Objective To evaluated the efficiency of low-dose cytosine arabinoside plus aclarubicin with concurrent administration of granulocyte colony-stimulating factor （CAG） regimen for refractory biphenotypic acute leukem...Objective To evaluated the efficiency of low-dose cytosine arabinoside plus aclarubicin with concurrent administration of granulocyte colony-stimulating factor （CAG） regimen for refractory biphenotypic acute leukemia （BAL）. Methods We treated 5 refractory BAL patients by CAG regimen （10 mg.m 2 cytosine arabinoside subcutaneously administrated every 12 hours, day 1-14; 5-7 mg·m^-2 aclarubicin intravenously administrated daily, day 1-8; and concurrently used 200 μg·m^-2·d^-1 granulocyte colony-stimulating factor subcutaneously） from November 2002 to April 2007. The efficacy of the regimen was evaluated by response rate, and the side effects were also measured. Results The complete remission rate was 80%, median duration of absolute neutrophil count〈5.0×10^8/L and platelet count〈2.0×10^10/L was day 13 and day 1, respectively; and the infection rate was low （Ⅲ-Ⅳ infection rate, 20.00%）.展开更多
The crystal structure of the title compound, C26H27O6P, has been determined by single--crystal X-ray diffraction. The crystal is monoclinic with space groupP21, a=16. 193(l), b=5. 804(1), c=12. 512(2) A, β=93. 187(5)...The crystal structure of the title compound, C26H27O6P, has been determined by single--crystal X-ray diffraction. The crystal is monoclinic with space groupP21, a=16. 193(l), b=5. 804(1), c=12. 512(2) A, β=93. 187(5)°, V=1174. 13A3, Dc=1. 319 g/cm3, F(000) =492, μ= 13. 52 cm-1, Z= 2, and final R= 0. 042and Rw= 0. 040 for 2349 reflections (I≥3σ(I)). Structure analysis revealed that thepyranose and 4, 6-O-benzylidene ring of the title compound adopts a distorted chair conformation.展开更多
Objective:The aim of the research was to study whether microRNA-15a(miR-15a) oligonucleotide could inhibit cell growth and enhance cytarabine(Ara-C)-induced apoptosis in Raji cells.Methods:Transfecting miR-15a oligonu...Objective:The aim of the research was to study whether microRNA-15a(miR-15a) oligonucleotide could inhibit cell growth and enhance cytarabine(Ara-C)-induced apoptosis in Raji cells.Methods:Transfecting miR-15a oligonucleotide into Raji cells with LipofectamineTM 2000,and then combined with Ara-C.IC50 value and cell proliferation were detected by CCK8 assay;the expression levels of Bcl-2 mRNA and protein were evaluated by RT-PCR and indirect immuno-fluorescence.The apoptotic cells were observed by Hoechst Dyeing;AnnexinV/PI double dyeing method was used to detect the cell apoptotic rate by Flow Cytometry(FCM).Results:After Raji cells were transfected with miR-15a oligonucleotide for 48 h,Bcl2 protein expression levels obviously decreased,however,there was no difference in Bcl-2 mRNA levels,as compared with the control group and blank group(P < 0.05).CCK8 assay showed that miR-15a oligonucleotide decreased the cell growth at 24,48 and 72 h,moreover,miR-15a oligonucleotides combined with Ara-C obviously decreased the cell growth than miR-15a group,Ara-C group and scrambled oligonucleotides(SODN) + Ara-C group.Meanwhile,miR-15a oligonucleotides combined with Ara-C significantly decreased IC50 of Ara-C(10.41 μg/mL),which were obviously lower than those of Ara-C group(15.43 μg/mL) and SODN plus Ara-C group(14.92 μg/mL).Plenty of apoptotic cells could be seen with Hoechst dyeing.AnnexinV/PI double dying assays by FCM indicated that the cell apoptotic rates in earlier period and late period of miR-15a + Ara-C group were 20.93% and 25.27%,respectively,which were obviously higher than those of miR-15a group,Ara-C group and SODN plus Ara-C group.Conclusion:miR-15a oligonucleotides can inhibit cell growth and enhance Ara-C-induced apoptosis in Raji cells.展开更多
Objective: To evaluate the therapeutic effect of the fludarabine and cytarabine (FA) regimen on acute myeloid leukemia (AML) at different phases during treatment. Methods: A total of 185 patients with AML were divided...Objective: To evaluate the therapeutic effect of the fludarabine and cytarabine (FA) regimen on acute myeloid leukemia (AML) at different phases during treatment. Methods: A total of 185 patients with AML were divided into 4 groups based on the outcome of previous treatments. Patients in Group 1 had no remission after the first course of induction chemotherapy (n = 55). Patients in Group 2 had no remission after no less than two courses of induction chemotherapy (n = 41). Patients in Group 3 had early relapse (n = 40). Patients in Group 4 had late relapse (n = 49). Patients in groups 2, 3 and 4 had refractory AML or AML with relapse. We assessed the efficacy and toxicity of FA combination chemotherapy in each of these 4 groups. Results: The complete remission (CR) rates of Groups 1, 2, 3 and 4 were 74.5% (41/55), 45.9% (19/41), 17.5% (7/40) and 38.8% (19/49), respectively. The CR rate was higher in Group 1 than in the other 3 groups (34.6%, 45/130) (P = 0.000). A significant correlation was found between CR rate and the number of chemotherapeutic courses (P = 0.023). The main adverse reactions included bone marrow suppression and secondary infection. Conclusion: FA regimen is a good choice for patients with AML, especially those who have failed to achieve CR after the first course of induction chemotherapy.展开更多
The crystal structure of the title compound, C 26 H 27 O 6P, has been determined by single crystal X ray diffraction analysis. The crystal is orthorhombic with space group P2 12 12 1, a=6.154(4), b=17.199(8), c=22.180...The crystal structure of the title compound, C 26 H 27 O 6P, has been determined by single crystal X ray diffraction analysis. The crystal is orthorhombic with space group P2 12 12 1, a=6.154(4), b=17.199(8), c=22.180(3) , V=2347.6 3, D c=1.32 g/cm 3, F(000)=984, μ=1.5 cm -1 , Z =4, and final R =0.075 and R w =0.080 for 1417 reflections (I≥3σ(I)) . The X ray diffraction analysis revealed that the structure of the title compound s similar to that of its parent phosphine and the pyranose and 4, 6 O benzylidene rings remain distorted chair conformations.展开更多
文摘In addition to six known flavonoids quercitrin, hyperoside, avicularin, rutin, quercetin and kaemferol, a new flavonol glycoside named 6″_O_acetyl quercetin 3_O_β_ D _alloside (1) was isolated from the aerial parts of Hypericum perforatum L. The structures were determined on the basis of spectroscopic methods (UV, IR, FAB_MS, 1H_NMR and 13 C NMR). Antifungal assay of all compounds showed that metabolite 1, quercitrin and quercetin were inhibitory to the growth of phytopathogenic fungus Helminthosporium sativum Pamel King et Bakke with minimum inhibitory concentrations (MICs) of 25, 50 and 50 μg/mL, respectively. Moreover, glycoside 1 and quercitrin were also shown to be able to inhibit the growth of Fusarium graminearum Schw. with MIC of 100 μg/mL. The MICs of ketoconazole used as control against the test fungi were 0.5 μg/mL in our assay.
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Project (No. 07C26213101283) supported by the Innovation Fundfor Technology Based Firms from the Ministry of Science andTechnology of China
文摘Nucleoside phosphorylases (NPases) were found to be induced in Enterobacter aerogenes DGO-04, and cytidine and cytidine 5′-monophosphate (CMP) were the best inducers. Five mmol/L to fifteen mmol/L cytidine or CMP could distinctly increase the activities of purine nucleoside phosphorylase (PNPase), uridine phosphorylase (UPase) and thymidine phosphorylase (TPase) when they were added into medium from 0 to 8 h. In the process of enzymatic synthesis of adenine arabinoside from adenine and uracil arabinoside with wet cells of Enterobacter aerogenes DGO-04 induced by cytidine or CMP, the reaction time could be shortened from 36 to 6 h. After enzymatic reaction the activity of NPase in the cells induced remained higher than that in the cells uninduced.
基金Supported by the Development of Society Foundation of Suzhou (SS0813)the Natural Science Foundation of Jiangsu Province (2004BK424)+2 种基金the 135 Key Department Foundation of Jiangsu Province (135XY0416)the Outstanding Person Fund the Jiangsu Province (LJ200626)the Outstanding Person Fund of the First Affiliated Hospital of Soochow University (2004YQG05)
文摘Objective To evaluated the efficiency of low-dose cytosine arabinoside plus aclarubicin with concurrent administration of granulocyte colony-stimulating factor （CAG） regimen for refractory biphenotypic acute leukemia （BAL）. Methods We treated 5 refractory BAL patients by CAG regimen （10 mg.m 2 cytosine arabinoside subcutaneously administrated every 12 hours, day 1-14; 5-7 mg·m^-2 aclarubicin intravenously administrated daily, day 1-8; and concurrently used 200 μg·m^-2·d^-1 granulocyte colony-stimulating factor subcutaneously） from November 2002 to April 2007. The efficacy of the regimen was evaluated by response rate, and the side effects were also measured. Results The complete remission rate was 80%, median duration of absolute neutrophil count〈5.0×10^8/L and platelet count〈2.0×10^10/L was day 13 and day 1, respectively; and the infection rate was low （Ⅲ-Ⅳ infection rate, 20.00%）.
文摘The crystal structure of the title compound, C26H27O6P, has been determined by single--crystal X-ray diffraction. The crystal is monoclinic with space groupP21, a=16. 193(l), b=5. 804(1), c=12. 512(2) A, β=93. 187(5)°, V=1174. 13A3, Dc=1. 319 g/cm3, F(000) =492, μ= 13. 52 cm-1, Z= 2, and final R= 0. 042and Rw= 0. 040 for 2349 reflections (I≥3σ(I)). Structure analysis revealed that thepyranose and 4, 6-O-benzylidene ring of the title compound adopts a distorted chair conformation.
基金Supported by the grants from the Natural Science Program Foundation of the Guangdong Province (No.04010446)the Overseas Chinese Affairs Office of the State Council Key Discipline Construction Fund (No.51205002)
文摘Objective:The aim of the research was to study whether microRNA-15a(miR-15a) oligonucleotide could inhibit cell growth and enhance cytarabine(Ara-C)-induced apoptosis in Raji cells.Methods:Transfecting miR-15a oligonucleotide into Raji cells with LipofectamineTM 2000,and then combined with Ara-C.IC50 value and cell proliferation were detected by CCK8 assay;the expression levels of Bcl-2 mRNA and protein were evaluated by RT-PCR and indirect immuno-fluorescence.The apoptotic cells were observed by Hoechst Dyeing;AnnexinV/PI double dyeing method was used to detect the cell apoptotic rate by Flow Cytometry(FCM).Results:After Raji cells were transfected with miR-15a oligonucleotide for 48 h,Bcl2 protein expression levels obviously decreased,however,there was no difference in Bcl-2 mRNA levels,as compared with the control group and blank group(P < 0.05).CCK8 assay showed that miR-15a oligonucleotide decreased the cell growth at 24,48 and 72 h,moreover,miR-15a oligonucleotides combined with Ara-C obviously decreased the cell growth than miR-15a group,Ara-C group and scrambled oligonucleotides(SODN) + Ara-C group.Meanwhile,miR-15a oligonucleotides combined with Ara-C significantly decreased IC50 of Ara-C(10.41 μg/mL),which were obviously lower than those of Ara-C group(15.43 μg/mL) and SODN plus Ara-C group(14.92 μg/mL).Plenty of apoptotic cells could be seen with Hoechst dyeing.AnnexinV/PI double dying assays by FCM indicated that the cell apoptotic rates in earlier period and late period of miR-15a + Ara-C group were 20.93% and 25.27%,respectively,which were obviously higher than those of miR-15a group,Ara-C group and SODN plus Ara-C group.Conclusion:miR-15a oligonucleotides can inhibit cell growth and enhance Ara-C-induced apoptosis in Raji cells.
基金Supported by a grant from the Planned Science and Technology Project of Guangzhou (No. 2006Z3-E0401)
文摘Objective: To evaluate the therapeutic effect of the fludarabine and cytarabine (FA) regimen on acute myeloid leukemia (AML) at different phases during treatment. Methods: A total of 185 patients with AML were divided into 4 groups based on the outcome of previous treatments. Patients in Group 1 had no remission after the first course of induction chemotherapy (n = 55). Patients in Group 2 had no remission after no less than two courses of induction chemotherapy (n = 41). Patients in Group 3 had early relapse (n = 40). Patients in Group 4 had late relapse (n = 49). Patients in groups 2, 3 and 4 had refractory AML or AML with relapse. We assessed the efficacy and toxicity of FA combination chemotherapy in each of these 4 groups. Results: The complete remission (CR) rates of Groups 1, 2, 3 and 4 were 74.5% (41/55), 45.9% (19/41), 17.5% (7/40) and 38.8% (19/49), respectively. The CR rate was higher in Group 1 than in the other 3 groups (34.6%, 45/130) (P = 0.000). A significant correlation was found between CR rate and the number of chemotherapeutic courses (P = 0.023). The main adverse reactions included bone marrow suppression and secondary infection. Conclusion: FA regimen is a good choice for patients with AML, especially those who have failed to achieve CR after the first course of induction chemotherapy.
文摘The crystal structure of the title compound, C 26 H 27 O 6P, has been determined by single crystal X ray diffraction analysis. The crystal is orthorhombic with space group P2 12 12 1, a=6.154(4), b=17.199(8), c=22.180(3) , V=2347.6 3, D c=1.32 g/cm 3, F(000)=984, μ=1.5 cm -1 , Z =4, and final R =0.075 and R w =0.080 for 1417 reflections (I≥3σ(I)) . The X ray diffraction analysis revealed that the structure of the title compound s similar to that of its parent phosphine and the pyranose and 4, 6 O benzylidene rings remain distorted chair conformations.
