The Experts below are selected from a list of 222 Experts worldwide ranked by ideXlab platform
Yang Liu - One of the best experts on this subject based on the ideXlab platform.
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a novel water soluble Benzothiazole Derivative bd926 triggers ros mediated b lymphoma cell apoptosis via mitochondrial and endoplasmic reticulum signaling pathways
International Journal of Oncology, 2016Co-Authors: Ping Yang, Tai Yang, Kun Zhang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Chongjie ZhangAbstract:Benzothiazole Derivatives are known for various biological activities, and their potency in cancer therapy have received considerable attention in recent years. However, the poor water solubility of most Benzothiazole Derivatives has limited their clinical application. We developed BD926, a novel water-soluble Benzothiazole Derivative and showed here that it could inhibit the proliferation and induce apoptosis of human Ramos B-lymphoma cells. We further showed that BD926 triggered apoptosis through both mitochondria and endoplasmic reticulum pathways. Moreover, BD926 caused cell cycle arrest at G0/G1 stage. Furthermore, accumulation of reactive oxygen species (ROS) were observed after BD926 treatment and ROS inhibitor was able to attenuate BD926-induced apoptosis, which suggested that BD926-induced apoptosis may be due to over-producing ROS. These results demonstrate the anticancer effects of BD926 in cell models and raise the possibility for the application of BD926 in cancer therapy.
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a novel water soluble Benzothiazole Derivative bd926 inhibits human activated t cell proliferation by down regulating the stat5 activation
European Journal of Pharmacology, 2015Co-Authors: Tai Yang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Yantang Wang, Yi Lai, Zhengliang ChenAbstract:Immunosuppressants are widely used for treatment of T cell-mediated autoimmune diseases and allogeneic graft rejection. However, because of the toxicity and tolerance of these drugs, novel immunosuppressants are urgently needed. We synthesized a series of novel water-soluble Benzothiazole Derivatives and found that BD926 [sodium 2-(benzo[d]thiazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-olate] had potent immunosuppressive activity. Treatment with BD926 significantly inhibited anti-CD3/anti-CD28 and alloantigen-induced human T cell proliferation as well as IL2-stimulated activated T cell proliferation in a dose-dependent manner in vitro. BD926 had no obvious cytotoxicity against human resting T cells, IL-4 treated activated T cells and fibroblast-like synoviocytes in our experimental conditions. Furthermore, BD926 induced cell cycle arrest at G0/G1 phase and inhibited the cyclin D3 and CDK 6 expression in activated T cells. BD926 inhibited the STAT5, but not Akt and p70S6K, phosphorylation in a dose-dependent manner in the IL-2-treated activated T cells. Interestingly, BD926 inhibited IFN-γ, IL-6 and IL-17, but not IL-2, IL-4 and IL-10, production in activated T cells. Finally, treatment with BD926 reduced delayed-type hypersensitivity in mice in a dose-dependent manner. Collectively, these data suggest that BD926 may be a lead compound for the design and development of new immunosuppressants for the intervention of allograft rejection and autoimmune diseases.
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bd750 a Benzothiazole Derivative inhibits t cell proliferation by affecting the jak3 stat5 signalling pathway
British Journal of Pharmacology, 2013Co-Authors: Yang Liu, Ping Yang, Tai Yang, Jin Liu, Xingyan Luo, Shuxia Yang, Yantang Wang, J Zheng, Yi Lai, Qiang ZouAbstract:Background and Purpose A series of Benzothiazole Derivatives were screened for immunosuppressive activity; of these compounds BD750 was found to be the most effective immunosuppressant. The purpose of the current study was to determine the immunosuppressive activity of BD750 on T cell proliferation and its potential mode of action.
Qiang Zou - One of the best experts on this subject based on the ideXlab platform.
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a novel water soluble Benzothiazole Derivative bd926 triggers ros mediated b lymphoma cell apoptosis via mitochondrial and endoplasmic reticulum signaling pathways
International Journal of Oncology, 2016Co-Authors: Ping Yang, Tai Yang, Kun Zhang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Chongjie ZhangAbstract:Benzothiazole Derivatives are known for various biological activities, and their potency in cancer therapy have received considerable attention in recent years. However, the poor water solubility of most Benzothiazole Derivatives has limited their clinical application. We developed BD926, a novel water-soluble Benzothiazole Derivative and showed here that it could inhibit the proliferation and induce apoptosis of human Ramos B-lymphoma cells. We further showed that BD926 triggered apoptosis through both mitochondria and endoplasmic reticulum pathways. Moreover, BD926 caused cell cycle arrest at G0/G1 stage. Furthermore, accumulation of reactive oxygen species (ROS) were observed after BD926 treatment and ROS inhibitor was able to attenuate BD926-induced apoptosis, which suggested that BD926-induced apoptosis may be due to over-producing ROS. These results demonstrate the anticancer effects of BD926 in cell models and raise the possibility for the application of BD926 in cancer therapy.
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a novel water soluble Benzothiazole Derivative bd926 inhibits human activated t cell proliferation by down regulating the stat5 activation
European Journal of Pharmacology, 2015Co-Authors: Tai Yang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Yantang Wang, Yi Lai, Zhengliang ChenAbstract:Immunosuppressants are widely used for treatment of T cell-mediated autoimmune diseases and allogeneic graft rejection. However, because of the toxicity and tolerance of these drugs, novel immunosuppressants are urgently needed. We synthesized a series of novel water-soluble Benzothiazole Derivatives and found that BD926 [sodium 2-(benzo[d]thiazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-olate] had potent immunosuppressive activity. Treatment with BD926 significantly inhibited anti-CD3/anti-CD28 and alloantigen-induced human T cell proliferation as well as IL2-stimulated activated T cell proliferation in a dose-dependent manner in vitro. BD926 had no obvious cytotoxicity against human resting T cells, IL-4 treated activated T cells and fibroblast-like synoviocytes in our experimental conditions. Furthermore, BD926 induced cell cycle arrest at G0/G1 phase and inhibited the cyclin D3 and CDK 6 expression in activated T cells. BD926 inhibited the STAT5, but not Akt and p70S6K, phosphorylation in a dose-dependent manner in the IL-2-treated activated T cells. Interestingly, BD926 inhibited IFN-γ, IL-6 and IL-17, but not IL-2, IL-4 and IL-10, production in activated T cells. Finally, treatment with BD926 reduced delayed-type hypersensitivity in mice in a dose-dependent manner. Collectively, these data suggest that BD926 may be a lead compound for the design and development of new immunosuppressants for the intervention of allograft rejection and autoimmune diseases.
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bd750 a Benzothiazole Derivative inhibits t cell proliferation by affecting the jak3 stat5 signalling pathway
British Journal of Pharmacology, 2013Co-Authors: Yang Liu, Ping Yang, Tai Yang, Jin Liu, Xingyan Luo, Shuxia Yang, Yantang Wang, J Zheng, Yi Lai, Qiang ZouAbstract:Background and Purpose A series of Benzothiazole Derivatives were screened for immunosuppressive activity; of these compounds BD750 was found to be the most effective immunosuppressant. The purpose of the current study was to determine the immunosuppressive activity of BD750 on T cell proliferation and its potential mode of action.
Yonghong Liu - One of the best experts on this subject based on the ideXlab platform.
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two new altenusin thiazole hybrids and a new Benzothiazole Derivative from the marine sponge derived fungus alternaria sp scsios02f49
Molecules, 2018Co-Authors: Yaping Chen, Ruyan Chen, Yongqi Tian, Yonghong LiuAbstract:Two novel altenusin-thiazole hybrids named altenusinoides A and B (1 and 2), a new Benzothiazole Derivative (3), and three known altenusin Derivatives (4–6) have been obtained from the solid culture of the marine sponge-derived fungal strain, Alternaria sp. SCSIOS02F49. The structures of these new compounds were characterized by NMR, HRESIMS, and X-ray single crystal analysis. Compounds 1 and 2 possess an unusual altenusin-thiazole-fused skeleton core (6/6/5), and compound 3 represents the first Benzothiazole Derivative from fungi. Compounds 4 and 5 showed significant DPPH free-radical-scavenging activities with the prominent IC50 values of 10.7 ± 0.09 μM and 100.6 ± 0.025 μM, respectively. Additionally, compound 5 exhibited COX-2 inhibitory activity with an IC50 value of 9.5 ± 0.08 μM.
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Two New Altenusin/Thiazole Hybrids and a New Benzothiazole Derivative from the Marine Sponge-Derived Fungus Alternaria sp. SCSIOS02F49
MDPI AG, 2018Co-Authors: Yaping Chen, Ruyan Chen, Yongqi Tian, Yonghong LiuAbstract:Two novel altenusin-thiazole hybrids named altenusinoides A and B (1 and 2), a new Benzothiazole Derivative (3), and three known altenusin Derivatives (4⁻6) have been obtained from the solid culture of the marine sponge-derived fungal strain, Alternaria sp. SCSIOS02F49. The structures of these new compounds were characterized by NMR, HRESIMS, and X-ray single crystal analysis. Compounds 1 and 2 possess an unusual altenusin-thiazole-fused skeleton core (6/6/5), and compound 3 represents the first Benzothiazole Derivative from fungi. Compounds 4 and 5 showed significant DPPH free-radical-scavenging activities with the prominent IC50 values of 10.7 ± 0.09 μM and 100.6 ± 0.025 μM, respectively. Additionally, compound 5 exhibited COX-2 inhibitory activity with an IC50 value of 9.5 ± 0.08 μM
Tai Yang - One of the best experts on this subject based on the ideXlab platform.
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a novel water soluble Benzothiazole Derivative bd926 triggers ros mediated b lymphoma cell apoptosis via mitochondrial and endoplasmic reticulum signaling pathways
International Journal of Oncology, 2016Co-Authors: Ping Yang, Tai Yang, Kun Zhang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Chongjie ZhangAbstract:Benzothiazole Derivatives are known for various biological activities, and their potency in cancer therapy have received considerable attention in recent years. However, the poor water solubility of most Benzothiazole Derivatives has limited their clinical application. We developed BD926, a novel water-soluble Benzothiazole Derivative and showed here that it could inhibit the proliferation and induce apoptosis of human Ramos B-lymphoma cells. We further showed that BD926 triggered apoptosis through both mitochondria and endoplasmic reticulum pathways. Moreover, BD926 caused cell cycle arrest at G0/G1 stage. Furthermore, accumulation of reactive oxygen species (ROS) were observed after BD926 treatment and ROS inhibitor was able to attenuate BD926-induced apoptosis, which suggested that BD926-induced apoptosis may be due to over-producing ROS. These results demonstrate the anticancer effects of BD926 in cell models and raise the possibility for the application of BD926 in cancer therapy.
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a novel water soluble Benzothiazole Derivative bd926 inhibits human activated t cell proliferation by down regulating the stat5 activation
European Journal of Pharmacology, 2015Co-Authors: Tai Yang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Yantang Wang, Yi Lai, Zhengliang ChenAbstract:Immunosuppressants are widely used for treatment of T cell-mediated autoimmune diseases and allogeneic graft rejection. However, because of the toxicity and tolerance of these drugs, novel immunosuppressants are urgently needed. We synthesized a series of novel water-soluble Benzothiazole Derivatives and found that BD926 [sodium 2-(benzo[d]thiazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-olate] had potent immunosuppressive activity. Treatment with BD926 significantly inhibited anti-CD3/anti-CD28 and alloantigen-induced human T cell proliferation as well as IL2-stimulated activated T cell proliferation in a dose-dependent manner in vitro. BD926 had no obvious cytotoxicity against human resting T cells, IL-4 treated activated T cells and fibroblast-like synoviocytes in our experimental conditions. Furthermore, BD926 induced cell cycle arrest at G0/G1 phase and inhibited the cyclin D3 and CDK 6 expression in activated T cells. BD926 inhibited the STAT5, but not Akt and p70S6K, phosphorylation in a dose-dependent manner in the IL-2-treated activated T cells. Interestingly, BD926 inhibited IFN-γ, IL-6 and IL-17, but not IL-2, IL-4 and IL-10, production in activated T cells. Finally, treatment with BD926 reduced delayed-type hypersensitivity in mice in a dose-dependent manner. Collectively, these data suggest that BD926 may be a lead compound for the design and development of new immunosuppressants for the intervention of allograft rejection and autoimmune diseases.
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bd750 a Benzothiazole Derivative inhibits t cell proliferation by affecting the jak3 stat5 signalling pathway
British Journal of Pharmacology, 2013Co-Authors: Yang Liu, Ping Yang, Tai Yang, Jin Liu, Xingyan Luo, Shuxia Yang, Yantang Wang, J Zheng, Yi Lai, Qiang ZouAbstract:Background and Purpose A series of Benzothiazole Derivatives were screened for immunosuppressive activity; of these compounds BD750 was found to be the most effective immunosuppressant. The purpose of the current study was to determine the immunosuppressive activity of BD750 on T cell proliferation and its potential mode of action.
Jin Liu - One of the best experts on this subject based on the ideXlab platform.
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a novel water soluble Benzothiazole Derivative bd926 triggers ros mediated b lymphoma cell apoptosis via mitochondrial and endoplasmic reticulum signaling pathways
International Journal of Oncology, 2016Co-Authors: Ping Yang, Tai Yang, Kun Zhang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Chongjie ZhangAbstract:Benzothiazole Derivatives are known for various biological activities, and their potency in cancer therapy have received considerable attention in recent years. However, the poor water solubility of most Benzothiazole Derivatives has limited their clinical application. We developed BD926, a novel water-soluble Benzothiazole Derivative and showed here that it could inhibit the proliferation and induce apoptosis of human Ramos B-lymphoma cells. We further showed that BD926 triggered apoptosis through both mitochondria and endoplasmic reticulum pathways. Moreover, BD926 caused cell cycle arrest at G0/G1 stage. Furthermore, accumulation of reactive oxygen species (ROS) were observed after BD926 treatment and ROS inhibitor was able to attenuate BD926-induced apoptosis, which suggested that BD926-induced apoptosis may be due to over-producing ROS. These results demonstrate the anticancer effects of BD926 in cell models and raise the possibility for the application of BD926 in cancer therapy.
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a novel water soluble Benzothiazole Derivative bd926 inhibits human activated t cell proliferation by down regulating the stat5 activation
European Journal of Pharmacology, 2015Co-Authors: Tai Yang, Yang Liu, Jin Liu, Xingyan Luo, Shuxia Yang, Qiang Zou, Yantang Wang, Yi Lai, Zhengliang ChenAbstract:Immunosuppressants are widely used for treatment of T cell-mediated autoimmune diseases and allogeneic graft rejection. However, because of the toxicity and tolerance of these drugs, novel immunosuppressants are urgently needed. We synthesized a series of novel water-soluble Benzothiazole Derivatives and found that BD926 [sodium 2-(benzo[d]thiazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-olate] had potent immunosuppressive activity. Treatment with BD926 significantly inhibited anti-CD3/anti-CD28 and alloantigen-induced human T cell proliferation as well as IL2-stimulated activated T cell proliferation in a dose-dependent manner in vitro. BD926 had no obvious cytotoxicity against human resting T cells, IL-4 treated activated T cells and fibroblast-like synoviocytes in our experimental conditions. Furthermore, BD926 induced cell cycle arrest at G0/G1 phase and inhibited the cyclin D3 and CDK 6 expression in activated T cells. BD926 inhibited the STAT5, but not Akt and p70S6K, phosphorylation in a dose-dependent manner in the IL-2-treated activated T cells. Interestingly, BD926 inhibited IFN-γ, IL-6 and IL-17, but not IL-2, IL-4 and IL-10, production in activated T cells. Finally, treatment with BD926 reduced delayed-type hypersensitivity in mice in a dose-dependent manner. Collectively, these data suggest that BD926 may be a lead compound for the design and development of new immunosuppressants for the intervention of allograft rejection and autoimmune diseases.
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bd750 a Benzothiazole Derivative inhibits t cell proliferation by affecting the jak3 stat5 signalling pathway
British Journal of Pharmacology, 2013Co-Authors: Yang Liu, Ping Yang, Tai Yang, Jin Liu, Xingyan Luo, Shuxia Yang, Yantang Wang, J Zheng, Yi Lai, Qiang ZouAbstract:Background and Purpose A series of Benzothiazole Derivatives were screened for immunosuppressive activity; of these compounds BD750 was found to be the most effective immunosuppressant. The purpose of the current study was to determine the immunosuppressive activity of BD750 on T cell proliferation and its potential mode of action.