Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming ...Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming mice (dosage, 0.1 g·kg^(-1)·d^(-1)) intragastrically for 7 successive days. The contents of selenium in heart, liver, spleen, kidneys, lungs, stomach, brain, muscle, and bone were determined by fluorometric method on the eighth day. MTT assay was used to study tumor growth inhibition of Eb in vitro, and lymphocyte transformation, hemolysin formation and phagocytosis assay were used to study its immunocompetence. Results After 7 days′ administration of Eb, the tissue contents of sele-(nium) in liver, spleen, lungs, kidneys, and bone of mice increased, especially those in liver and spleen increased significan-tly, compared with controls; but no significant changes of such contents were found in muscle, heart, brain, and stomach. Eb demonstrated inhibitory effects on human Bel-7402, BGC-823, and Calu-3 cancer cell lines in vitro. Eb also showed ability to enhance lymphocyte transformation and serum hemolysin formation in vitro and increase the phagocytosis of macrophages. Conclusion The validated antitumor and immunostimulatory activities of Eb suggest a hypothesis that Eb may behave as a biological response modifier when used as an antitumor agent. Eb is worthy of further study in developing a new antineoplastic and immunity enhancing agent in the light of its antitumor activity, immunocompetence and specific distribution in liver, lungs, kidneys, bone, and spleen.展开更多
Ethaselen, an organoselenium compound designed and synthesized in the School of Pharmaceutical Sciences, Peking University, has been entitled to independent intellectual property rights both at home and abroad. As one...Ethaselen, an organoselenium compound designed and synthesized in the School of Pharmaceutical Sciences, Peking University, has been entitled to independent intellectual property rights both at home and abroad. As one of the novel antitumor drugs, ethaselen has been extensively studied in Phase I clinical trial, and its biological target is thioredoxin reductase. In this review, we focus on the ethaselen＇s efficacy and pharmacological actions, including antitumor effects both in vitro and in vivo, and immunologic functions. These research findings not only provide the theoretical basis for the anticancer study of ethaselen, but also guide the clinical trial of ethaselen.展开更多
Key intermediate bis[2-amino-4,5-(15-crown-5)phenyl]diselenide was obtained by the convenient redox method. Crown-ether type host molecule containing Se-Se bond 2,11-dioxo-4,5:8,9-di(benzo[4',5']-15-crown-5)-6...Key intermediate bis[2-amino-4,5-(15-crown-5)phenyl]diselenide was obtained by the convenient redox method. Crown-ether type host molecule containing Se-Se bond 2,11-dioxo-4,5:8,9-di(benzo[4',5']-15-crown-5)-6,7-diselena-3,10,16-triazabicyclo[10,3,1]hexadeca-1(16), 4, 8, 12, 14-pentaene was synthesized with high dillution technique.展开更多
The organoselenium-induced ring-closure reaction of O-allyl oximes gave cyclic iminium salts, which reacted with Grignard reagents to produce N-alkyl-4-phenylselenoisoxazolidines. 2,5-Dihydroisoxazoles could be obtain...The organoselenium-induced ring-closure reaction of O-allyl oximes gave cyclic iminium salts, which reacted with Grignard reagents to produce N-alkyl-4-phenylselenoisoxazolidines. 2,5-Dihydroisoxazoles could be obtained in good yields by subsequent selenoxide syn-elimination.展开更多
Selenium-enriched probiotics were supplemented into feedstuff of Landrace stock boars at a concentration of 0.3 mg/kg （concentration of selenium）, and the semen quality of the stock boars were observed. The results ...Selenium-enriched probiotics were supplemented into feedstuff of Landrace stock boars at a concentration of 0.3 mg/kg （concentration of selenium）, and the semen quality of the stock boars were observed. The results showed that the semen motility, rate of intact acrosome, and activity of glutathione peroxidase were higher in the experimental boars than in the control, but rate of sperm deformity was lower in the experimental boars than in the control. Therefore, the selenium-enriched probiotics greatly improve semen quality of stock boars.展开更多
文摘Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming mice (dosage, 0.1 g·kg^(-1)·d^(-1)) intragastrically for 7 successive days. The contents of selenium in heart, liver, spleen, kidneys, lungs, stomach, brain, muscle, and bone were determined by fluorometric method on the eighth day. MTT assay was used to study tumor growth inhibition of Eb in vitro, and lymphocyte transformation, hemolysin formation and phagocytosis assay were used to study its immunocompetence. Results After 7 days′ administration of Eb, the tissue contents of sele-(nium) in liver, spleen, lungs, kidneys, and bone of mice increased, especially those in liver and spleen increased significan-tly, compared with controls; but no significant changes of such contents were found in muscle, heart, brain, and stomach. Eb demonstrated inhibitory effects on human Bel-7402, BGC-823, and Calu-3 cancer cell lines in vitro. Eb also showed ability to enhance lymphocyte transformation and serum hemolysin formation in vitro and increase the phagocytosis of macrophages. Conclusion The validated antitumor and immunostimulatory activities of Eb suggest a hypothesis that Eb may behave as a biological response modifier when used as an antitumor agent. Eb is worthy of further study in developing a new antineoplastic and immunity enhancing agent in the light of its antitumor activity, immunocompetence and specific distribution in liver, lungs, kidneys, bone, and spleen.
基金National Natural Science Foundation of China(Grant No.30472036)
文摘Ethaselen, an organoselenium compound designed and synthesized in the School of Pharmaceutical Sciences, Peking University, has been entitled to independent intellectual property rights both at home and abroad. As one of the novel antitumor drugs, ethaselen has been extensively studied in Phase I clinical trial, and its biological target is thioredoxin reductase. In this review, we focus on the ethaselen＇s efficacy and pharmacological actions, including antitumor effects both in vitro and in vivo, and immunologic functions. These research findings not only provide the theoretical basis for the anticancer study of ethaselen, but also guide the clinical trial of ethaselen.
文摘Key intermediate bis[2-amino-4,5-(15-crown-5)phenyl]diselenide was obtained by the convenient redox method. Crown-ether type host molecule containing Se-Se bond 2,11-dioxo-4,5:8,9-di(benzo[4',5']-15-crown-5)-6,7-diselena-3,10,16-triazabicyclo[10,3,1]hexadeca-1(16), 4, 8, 12, 14-pentaene was synthesized with high dillution technique.
基金Project supported by the National Natural Science Foundation of China (Nos. 20332060,20272050).
文摘The organoselenium-induced ring-closure reaction of O-allyl oximes gave cyclic iminium salts, which reacted with Grignard reagents to produce N-alkyl-4-phenylselenoisoxazolidines. 2,5-Dihydroisoxazoles could be obtained in good yields by subsequent selenoxide syn-elimination.
基金funded by Production,Teaching & Research Project of the Ministry of Education of Guangdong Province(2006D90204008)
文摘Selenium-enriched probiotics were supplemented into feedstuff of Landrace stock boars at a concentration of 0.3 mg/kg （concentration of selenium）, and the semen quality of the stock boars were observed. The results showed that the semen motility, rate of intact acrosome, and activity of glutathione peroxidase were higher in the experimental boars than in the control, but rate of sperm deformity was lower in the experimental boars than in the control. Therefore, the selenium-enriched probiotics greatly improve semen quality of stock boars.
