In the present study,daunomydn （DIM） was chosen to conjugate cowdently with amonoclonal antitibody,MGb<sub>2</sub>,against human gastric cancer cells via a cis-aconitic anhydride linker（directly） or a ...In the present study,daunomydn （DIM） was chosen to conjugate cowdently with amonoclonal antitibody,MGb<sub>2</sub>,against human gastric cancer cells via a cis-aconitic anhydride linker（directly） or a dextmn bridge （indirectly,） The mo-lar ratio of MGb<sub>2</sub> to DM in the conjugates was1:6 （direct method） and 1:54 （indirect method）,respectively.The ELISA results revealed theantibody after conjugation retained antigen-binding capacity.The conjugates showed a highly se-lective cytotoxicity to the target cells.In lh cytotoxidty test,cytotoxidty of the conjugates wasgreater than that of free DM or irrevalent conjugates to human gastric cancer cell lines,SGC-7901and very low as far as non-target cells （HeLa） were concerned.It is sugared that theselective cytotoxidty on target cells of the conjugates is mediated by the monoclonal antibody.展开更多
Three spin labeled daunomycin derivatives 2-4 were synthesized and their biological activities were tested against mouse leukemia L1210 and human liver cancer BEL-7402 cells in vitro.
Objective： To explore the relationship between survivin and drug resistance, and the changes of the survivin expression in HL-60 cells treated with three kinds of chemotherapeutic drugs. Methods： HL- 60 cells were t...Objective： To explore the relationship between survivin and drug resistance, and the changes of the survivin expression in HL-60 cells treated with three kinds of chemotherapeutic drugs. Methods： HL- 60 cells were treated with appropriate concentration of daunomycin （DNR）, mitoxantrone （MIT） or arsenic trioxide （As2O3）. The expression of survivin mRNA and protein on the first or third day was detected by RT-PCR and Western blot respectively. Results： The expression of survivin mRNA was decreased on the first day by 10% in DNR-treated group, 40% in MIT-treated group （P〈0.01） and 25% in As2O3-treated group （P〈0.01） respectively. On the third day, the expression of survivin mRNA in DNR- and MIT-treated group was up-regulated to 120% （P〈0.05） and 165% （P〈0.01） respectively as compared with that on the first day, but down-regulated to 68% in As2O3-treated group （P〈0.01）. As compared with control group, the expression of survivin protein in DNR- or MIT-treated group was increased by 14% or 11% on the third day respectively, but it was decreased by 18% in As2O3-treated group. Conclusion： In DNR- and MIT-treated group, the expression of surivin was decreased at first and then increased obviously, which may be one of the causes for resistance to chemotherapy against leukemia. Different from other two drugs, As2O3 may play an important role in restoring chemotherapy sensitivity.展开更多
文摘In the present study,daunomydn （DIM） was chosen to conjugate cowdently with amonoclonal antitibody,MGb<sub>2</sub>,against human gastric cancer cells via a cis-aconitic anhydride linker（directly） or a dextmn bridge （indirectly,） The mo-lar ratio of MGb<sub>2</sub> to DM in the conjugates was1:6 （direct method） and 1:54 （indirect method）,respectively.The ELISA results revealed theantibody after conjugation retained antigen-binding capacity.The conjugates showed a highly se-lective cytotoxicity to the target cells.In lh cytotoxidty test,cytotoxidty of the conjugates wasgreater than that of free DM or irrevalent conjugates to human gastric cancer cell lines,SGC-7901and very low as far as non-target cells （HeLa） were concerned.It is sugared that theselective cytotoxidty on target cells of the conjugates is mediated by the monoclonal antibody.
文摘Three spin labeled daunomycin derivatives 2-4 were synthesized and their biological activities were tested against mouse leukemia L1210 and human liver cancer BEL-7402 cells in vitro.
基金This project was supported by a grant from the National Natural Sciences Foundation of China (No. 30370595).
文摘Objective： To explore the relationship between survivin and drug resistance, and the changes of the survivin expression in HL-60 cells treated with three kinds of chemotherapeutic drugs. Methods： HL- 60 cells were treated with appropriate concentration of daunomycin （DNR）, mitoxantrone （MIT） or arsenic trioxide （As2O3）. The expression of survivin mRNA and protein on the first or third day was detected by RT-PCR and Western blot respectively. Results： The expression of survivin mRNA was decreased on the first day by 10% in DNR-treated group, 40% in MIT-treated group （P〈0.01） and 25% in As2O3-treated group （P〈0.01） respectively. On the third day, the expression of survivin mRNA in DNR- and MIT-treated group was up-regulated to 120% （P〈0.05） and 165% （P〈0.01） respectively as compared with that on the first day, but down-regulated to 68% in As2O3-treated group （P〈0.01）. As compared with control group, the expression of survivin protein in DNR- or MIT-treated group was increased by 14% or 11% on the third day respectively, but it was decreased by 18% in As2O3-treated group. Conclusion： In DNR- and MIT-treated group, the expression of surivin was decreased at first and then increased obviously, which may be one of the causes for resistance to chemotherapy against leukemia. Different from other two drugs, As2O3 may play an important role in restoring chemotherapy sensitivity.
