The dialysis method has been traditionally used for the conversion of native human plasminogen(Glu-Hpg) to lys-plasminogen(Lys-Hpg). Here is described a solid-phase synthesis method for the preparation of an acyl-plas...The dialysis method has been traditionally used for the conversion of native human plasminogen(Glu-Hpg) to lys-plasminogen(Lys-Hpg). Here is described a solid-phase synthesis method for the preparation of an acyl-plasminogen-streptokinase activator complex(APSAC) from Lys-Hpg, streptokinase(SK) and chemical modification (agent(4-amidinophenyl-4′-aminobenzoate hydrochloride)) with the L-lysine-Sepharose 4B Column as the carrier. The new method significantly increases the product yield and purity over the liquid-phase methods. The APSAC prepared with the new method exhibits a significant thrombolytic effect with a long half-life of about 8.8 h in rabbits.展开更多
The chemical modification of human plasminogen(HPg) was studied with 1-ethyl-3-(3- dimethyl aminopropyl) carbodiimide(EDC), N -acetylimidazole(NAI), 1,2-cyclohexanedione(CHD), chloramine T(Ch-T) and N -bro...The chemical modification of human plasminogen(HPg) was studied with 1-ethyl-3-(3- dimethyl aminopropyl) carbodiimide(EDC), N -acetylimidazole(NAI), 1,2-cyclohexanedione(CHD), chloramine T(Ch-T) and N -bromosuccinimide(NBS) as modifying reagents at its carboxyl group, tyrosine, arginine, methionine and tryptophan residues, respectively. The results indicate that tyrosine and arginine residues are not essential for HPg activity, while carboxyl groups, methionine and tryptophan residues are important for the activity of HPg. The Keech and Farrant′s kinetic analysis reveals that one tryptophan residue, one methionine residue and two carboxyl groups are essential for HPg activity.展开更多
AIM: To evaluate the efficacy of rituximab combined with cyclophosphamide, vincristine, doxorubicin, and prednisone (CHOP) in treating the initially diagnosed diffuse large B cell lymphoma (DLBL). METHODS: From Apr.20...AIM: To evaluate the efficacy of rituximab combined with cyclophosphamide, vincristine, doxorubicin, and prednisone (CHOP) in treating the initially diagnosed diffuse large B cell lymphoma (DLBL). METHODS: From Apr.2002 to Feb. 2003, 52 patients were enrolled in this study. Chemotherapy was conducted with cyclophosphamide 600 mg·m^-2, vincristine 1.4 mg·m^-2,doorubicin 25mg·m^-2 on d 1 and prednisone 60 mg·d^-l for successive 5 d (standard CHOP). There were 6 courses, 3 wk each. Rituximab 375 mg·m^-2 was infused once a week, 2 d before the first course of chemotherapy (successive infusion) for 4 times on standard dose or for 6 times on extended dose. Or rituximab was infused once every 3 wk, 2 d before each CHOP (separated infusion) for 4 times on the schedule of standard dose or for 6 times on the extended dose. RESULTS: The complete response (CR) rate (60%) and total effective (100%) were achieved in 50 patients who were evaluated for efficacy, respectively. And among 34 patients in Ann Arbor stage Ⅲ and Ⅳ, 15 patients were completely relieved. The complete effective rate was 44%. Fifty patients were followed-up for (8±s 5) wk, 2-30wk and estimated progress free survival (PFS) rate of 16 wk was 87 %. Standard and extend regimen were not different in effect, as well as the separated or concentrated infusion of rituximab (P>0.05). The regimen could be well tolerated, and the major adverse reactions were infusion-related response (32 % ) and hematological toxicities (20 %). CONCLUSION:Rituximab in combined with CHOP can be successfully applied to the therapy of initially diagnosed diffuse large B cell lymphoma, with high CR rate and mild adverse reactions.展开更多
基金Supported by the Natural Science Foundation of Jilin Province(No. 2 0 0 3- 0 5 - 5 0 - 2 ) and the Creative Foundation of JilinU niversit
文摘The dialysis method has been traditionally used for the conversion of native human plasminogen(Glu-Hpg) to lys-plasminogen(Lys-Hpg). Here is described a solid-phase synthesis method for the preparation of an acyl-plasminogen-streptokinase activator complex(APSAC) from Lys-Hpg, streptokinase(SK) and chemical modification (agent(4-amidinophenyl-4′-aminobenzoate hydrochloride)) with the L-lysine-Sepharose 4B Column as the carrier. The new method significantly increases the product yield and purity over the liquid-phase methods. The APSAC prepared with the new method exhibits a significant thrombolytic effect with a long half-life of about 8.8 h in rabbits.
基金Supported by the Natural Science Foundation of Jilin Province( No.0 30 912 )
文摘The chemical modification of human plasminogen(HPg) was studied with 1-ethyl-3-(3- dimethyl aminopropyl) carbodiimide(EDC), N -acetylimidazole(NAI), 1,2-cyclohexanedione(CHD), chloramine T(Ch-T) and N -bromosuccinimide(NBS) as modifying reagents at its carboxyl group, tyrosine, arginine, methionine and tryptophan residues, respectively. The results indicate that tyrosine and arginine residues are not essential for HPg activity, while carboxyl groups, methionine and tryptophan residues are important for the activity of HPg. The Keech and Farrant′s kinetic analysis reveals that one tryptophan residue, one methionine residue and two carboxyl groups are essential for HPg activity.
文摘AIM: To evaluate the efficacy of rituximab combined with cyclophosphamide, vincristine, doxorubicin, and prednisone (CHOP) in treating the initially diagnosed diffuse large B cell lymphoma (DLBL). METHODS: From Apr.2002 to Feb. 2003, 52 patients were enrolled in this study. Chemotherapy was conducted with cyclophosphamide 600 mg·m^-2, vincristine 1.4 mg·m^-2,doorubicin 25mg·m^-2 on d 1 and prednisone 60 mg·d^-l for successive 5 d (standard CHOP). There were 6 courses, 3 wk each. Rituximab 375 mg·m^-2 was infused once a week, 2 d before the first course of chemotherapy (successive infusion) for 4 times on standard dose or for 6 times on extended dose. Or rituximab was infused once every 3 wk, 2 d before each CHOP (separated infusion) for 4 times on the schedule of standard dose or for 6 times on the extended dose. RESULTS: The complete response (CR) rate (60%) and total effective (100%) were achieved in 50 patients who were evaluated for efficacy, respectively. And among 34 patients in Ann Arbor stage Ⅲ and Ⅳ, 15 patients were completely relieved. The complete effective rate was 44%. Fifty patients were followed-up for (8±s 5) wk, 2-30wk and estimated progress free survival (PFS) rate of 16 wk was 87 %. Standard and extend regimen were not different in effect, as well as the separated or concentrated infusion of rituximab (P>0.05). The regimen could be well tolerated, and the major adverse reactions were infusion-related response (32 % ) and hematological toxicities (20 %). CONCLUSION:Rituximab in combined with CHOP can be successfully applied to the therapy of initially diagnosed diffuse large B cell lymphoma, with high CR rate and mild adverse reactions.
