Latest ArticlesPraeruptorin C (PC), D (PD) and E (PE) are important compounds extracted from Peucedanum praeruptorum DUNN and have been reported to exert multiple pharmacological activities. The present study is purposed to determine the inhibition of PC, PD and PE on the activity of important phase I metabolic enzymes-carboxylesterases (CES). In vitro human liver microsomes (HLM) incubation system was used to determine the inhibition potential of PC, PD and PE on the activity of CES1 and CES2. Inhibition behaviour was determined, and in vitro-in vivo extrapolation was performed by using the combination of in vitro inhibition kinetic parameter (Ki) and in vivo exposure level of PD. PD exhibited the strongest inhibition on the activity of CES1, with 81.7% activity inhibited by 100 μmol·L-1 of PD. PD noncompetitively inhibited the activity of CES1 with the Ki to be 122.2 μmol·L-1, indicating inhibition potential of PD towards CES1 in vivo. Therefore, closely monitoring the endogenous metabolic disorders caused by PD and interaction between PD and drugs mainly undergoing CES1-catalyzed metabolism is very necessary.
Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-combination strategy. The structures of target compounds were elucidated by IR, 1H NMR, 13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate (ADP) and (AA) arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.
Traditional anti-depressant therapy based on the regulation of monoamine neurotransmitters has shown certain limitations. Recently, accumulating clinical and preclinical studies have reported the tantalizing link between immune dysregulation, inflammatory process and the initiation and exacerbation of major depressive disorder (MDD). With a deepening understanding of neural-immune-metabolic interactions, an immunometabolism driven disease network has attracted huge interests in understanding neuronal inflammation and dysfunction underlying MDD pathogenesis and intervention. This review describes recent data uncovering immunometabolic dysregulation as a key factor in MDD network, with a focus on the recent appreciation of immune-metabolic actions of several anti-depressant compounds. The implications for the discovery of novel antidepressant drugs and clinical management of MDD are discussed.
This study was designed to screen the targets of bioactive ingredients of Baihe Dihuang Tang, and investigate the "multi-components, multi-targets and multi-pathways" intervention mechanism of Baihe Dihuang Tang on psychological sub-health. The ADME/T calculation method was used to screen the active ingredient of Baihe Dihuang Tang, and then using ADME/T calculation method to filtrate the active components of Baihe Dihuang Tang, then Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), PharmMapper database and Medical Subject Headings (MeSH) were combined to forecast and filtrate the targets of the main active ingredients. In addition, the predicted targets were verified by the Surflex-dock in Sybyl. The Cytoscape software was used to construct the Baihe Dihuang Tang ingredients-targets-disease network, while ClueGO software was used to analyze the molecular function and biological process of the targets. There are total 11 active ingredients and 21 targets in Baihe Dihuang Tang. A good interaction between them was supported by the score. The 21 targets were mainly involved in gamma-aminobutyric acid signaling pathway, cAMP metabolic process and monoamine transport relevant biological processes. Thus, Baihe Dihuang Tang may play a role in the intervention of psychological sub-health by regulating the activity of G-protein coupled amine receptor and the expression of monoamine neurotransmitter, which reflects the features of traditional Chinese medicine multi-components, multi-targets and multi-pathways. This research provides evidences on the pharmacological mechanism of Baihe Dihuang Tang effect on psychological sub-health.
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