Luteinizing hormone-releasing hormone (LHRH) is the key regulator of the hypothalamic-pituitary-gonadal (HPG) axis, which is responsible for the development and functioning of the reproductive system. Delivery of a co...Luteinizing hormone-releasing hormone (LHRH) is the key regulator of the hypothalamic-pituitary-gonadal (HPG) axis, which is responsible for the development and functioning of the reproductive system. Delivery of a continuous supply of LHRH agonists causes down-regulation of the LHRH receptors, resulting in a marked decrease in androgens in males and estrogens in females. LHRH analogues are widely used in the treatment of various diseases, including prostate and breast cancer, and reproductive disorders, such as infertility and precocious puberty. However, they require parenteral administration, and no oral formulations are currently available. We synthesized two types of LHRH mini-dendrimers using thioether ligation, aiming to enhance the stability and bioavailability of the peptide drug while maintaining its biologically active conformation. These two compounds include a poly-lysine core conjugated to either the C-terminus of LHRH or a D-amino acid in position 6 of the LHRH sequence. The synthesized dendrimers were analysed using dynamic light scattering, and showed particle sizes of 155 and 115 nm, respectively. The nanometer size, well-defined structure and water solubility of these dendritic analogues make them excellent candidates for further exploration in oral peptide drug delivery.展开更多
A series of novel ester-capped carbosilane dendrimers（G0-COOCH3–G2-COOCH3） were designed and successfully synthesized via a hybrid divergent–convergent method through a facile hydrosilylation reaction. The structu...A series of novel ester-capped carbosilane dendrimers（G0-COOCH3–G2-COOCH3） were designed and successfully synthesized via a hybrid divergent–convergent method through a facile hydrosilylation reaction. The structures of these dendrimers were confirmed by FTIR,1H NMR, and HRMS analyses.展开更多
Long chain branched dendrimers 1, 2 and 3 were easily prepared according to the convergent strategy based on the A2B type monomer from 5-hydroxyisophthalic acid. These dendrimers have a nucleophilic phenol focal group...Long chain branched dendrimers 1, 2 and 3 were easily prepared according to the convergent strategy based on the A2B type monomer from 5-hydroxyisophthalic acid. These dendrimers have a nucleophilic phenol focal group, which is useful to further chemistry.展开更多
Unsymmetrical dendrons 1,2 and 3 were easily prepared according to a novel convergent strategy from 3,4-methylenedioxybenzaldehyde as starting material.
文摘Luteinizing hormone-releasing hormone (LHRH) is the key regulator of the hypothalamic-pituitary-gonadal (HPG) axis, which is responsible for the development and functioning of the reproductive system. Delivery of a continuous supply of LHRH agonists causes down-regulation of the LHRH receptors, resulting in a marked decrease in androgens in males and estrogens in females. LHRH analogues are widely used in the treatment of various diseases, including prostate and breast cancer, and reproductive disorders, such as infertility and precocious puberty. However, they require parenteral administration, and no oral formulations are currently available. We synthesized two types of LHRH mini-dendrimers using thioether ligation, aiming to enhance the stability and bioavailability of the peptide drug while maintaining its biologically active conformation. These two compounds include a poly-lysine core conjugated to either the C-terminus of LHRH or a D-amino acid in position 6 of the LHRH sequence. The synthesized dendrimers were analysed using dynamic light scattering, and showed particle sizes of 155 and 115 nm, respectively. The nanometer size, well-defined structure and water solubility of these dendritic analogues make them excellent candidates for further exploration in oral peptide drug delivery.
基金support by the National Natural Science Foundation of China(No.21307053)China Postdoctoral Science Foundation Funded Project(No.2013M541911)+1 种基金Promotive Research Fund for Excellent Young and Middle-Aged Scientists of Shandong Province(No.BS2013CL044)Natural Science Foundation of Ludong University(No.LY2011004)
文摘A series of novel ester-capped carbosilane dendrimers（G0-COOCH3–G2-COOCH3） were designed and successfully synthesized via a hybrid divergent–convergent method through a facile hydrosilylation reaction. The structures of these dendrimers were confirmed by FTIR,1H NMR, and HRMS analyses.
基金Project supported by the National Natural Science Foundation of China （No. 20472025 and QT No. 20021001）.
文摘Long chain branched dendrimers 1, 2 and 3 were easily prepared according to the convergent strategy based on the A2B type monomer from 5-hydroxyisophthalic acid. These dendrimers have a nucleophilic phenol focal group, which is useful to further chemistry.
文摘Unsymmetrical dendrons 1,2 and 3 were easily prepared according to a novel convergent strategy from 3,4-methylenedioxybenzaldehyde as starting material.
