The Experts below are selected from a list of 294 Experts worldwide ranked by ideXlab platform
Hong Liu - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives (THPBs) as proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators for the Treatment of Hyperlipidemia.
Acta pharmaceutica Sinica. B, 2019Co-Authors: Xi Cong, Junhua Tong, Zhao Jing, Hualiang Jiang, Jiang Wang, Wang Yiping, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
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design synthesis and biological evaluation of novel tetrahydroprotoberberine derivatives thpbs as proprotein convertase subtilisin kexin type 9 pcsk9 modulators for the Treatment of Hyperlipidemia
Acta Pharmaceutica Sinica B, 2019Co-Authors: Junhua Tong, Hualiang Jiang, Jiang Wang, Jing Zhao, Yiping Wang, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
Junhua Tong - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives (THPBs) as proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators for the Treatment of Hyperlipidemia.
Acta pharmaceutica Sinica. B, 2019Co-Authors: Xi Cong, Junhua Tong, Zhao Jing, Hualiang Jiang, Jiang Wang, Wang Yiping, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
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design synthesis and biological evaluation of novel tetrahydroprotoberberine derivatives thpbs as proprotein convertase subtilisin kexin type 9 pcsk9 modulators for the Treatment of Hyperlipidemia
Acta Pharmaceutica Sinica B, 2019Co-Authors: Junhua Tong, Hualiang Jiang, Jiang Wang, Jing Zhao, Yiping Wang, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
Jiang Wang - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives (THPBs) as proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators for the Treatment of Hyperlipidemia.
Acta pharmaceutica Sinica. B, 2019Co-Authors: Xi Cong, Junhua Tong, Zhao Jing, Hualiang Jiang, Jiang Wang, Wang Yiping, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
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design synthesis and biological evaluation of novel tetrahydroprotoberberine derivatives thpbs as proprotein convertase subtilisin kexin type 9 pcsk9 modulators for the Treatment of Hyperlipidemia
Acta Pharmaceutica Sinica B, 2019Co-Authors: Junhua Tong, Hualiang Jiang, Jiang Wang, Jing Zhao, Yiping Wang, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
Hualiang Jiang - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives (THPBs) as proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators for the Treatment of Hyperlipidemia.
Acta pharmaceutica Sinica. B, 2019Co-Authors: Xi Cong, Junhua Tong, Zhao Jing, Hualiang Jiang, Jiang Wang, Wang Yiping, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
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design synthesis and biological evaluation of novel tetrahydroprotoberberine derivatives thpbs as proprotein convertase subtilisin kexin type 9 pcsk9 modulators for the Treatment of Hyperlipidemia
Acta Pharmaceutica Sinica B, 2019Co-Authors: Junhua Tong, Hualiang Jiang, Jiang Wang, Jing Zhao, Yiping Wang, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
Xi Cong - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives (THPBs) as proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators for the Treatment of Hyperlipidemia.
Acta pharmaceutica Sinica. B, 2019Co-Authors: Xi Cong, Junhua Tong, Zhao Jing, Hualiang Jiang, Jiang Wang, Wang Yiping, Hong LiuAbstract:Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators may attenuate PCSK9-induced low-density lipoprotein receptor (LDLR) degradation in lysosome and promote the clearance of circulating low-density lipoprotein cholesterol (LDL-C). A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized, and evaluated as PCSK9 modulators for the Treatment of Hyperlipidemia. Among them, eight compounds exhibited excellent activities in downregulating hepatic PCSK9 expression better than berberine in HepG2 cells. In addition, five compounds 15 , 18 , 22 , ( R )- 22 , and ( S )- 22 showed better performance in the low-density lipoprotein, labeled with 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate (DiI-LDL) uptake assay, compared with berberine at the same concentration. Compound 22 , selected for in vivo evaluation, demonstrated significant reductions of total cholesterol (TC) and LDL-C in hyperlipidemic hamsters with a good pharmacokinetic profile. Further exploring of lipid-lowering mechanism showed that compound 22 promoted hepatic LDLR expression in a dose-dependent manner in HepG2 cells. Additional results of human ether-a-go-go related gene (hERG) inhibition assay indicated the potential druggability for compound 22 , which is a promising lead compound for the development of PCSK9 modulator for the Treatment of Hyperlipidemia.
