Abstract: The present disclosure provides methods of enhancing immunity, comprising administering TGR5 agonist such as a bile acid (BA) to a subject in need thereof. Provided also herein are methods of inhibiting immunity, comprising administering TGR5 antagonist to a subject in need thereof. The present disclosure further provides methods of identifying immunomodulatory agent, comprising contacting TGR5 with a candidate agent.
Abstract: Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y?C1-4 straight carbon chain, M1 and/or M2=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
Type:
Grant
Filed:
October 13, 2010
Date of Patent:
January 26, 2016
Assignees:
West China Hospital, Sichuan University, Yichang Humanwell Pharmaceutical Co., Ltd.
Abstract: Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y=C1-4 straight carbon chain, M1 and/or M2=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
Type:
Application
Filed:
October 13, 2010
Publication date:
April 4, 2013
Applicants:
Yichang Humanwell Pharmaceutical Co., Ltd., West China Hospital, Sichuan University