【摘 要】
：
Main observation and conclusionrnUncaria rhynchophylla has been widely used to treat central nervous system diseases for a long history.After investigation of U.rhynchophylla,eleven monoterpene indole alkaloids,including four new compounds uncarialins J-M
【机 构】
：
Dalian Key Laboratory of Metabolic Target Characterization and Traditional Chinese Medicine Interven
论文部分内容阅读
Main observation and conclusionrnUncaria rhynchophylla has been widely used to treat central nervous system diseases for a long history.After investigation of U.rhynchophylla,eleven monoterpene indole alkaloids,including four new compounds uncarialins J-M (1-4) and seven known ana-logues (5-11),were isolated and identified.Their structural characterization was conducted using HRESIMS,1D and 2D NMR,elec-tronic circular dichroism (ECD) spectra,and quantum chemical computations.Compounds 1,2,7,and 9-11 displayed significant ag-onistic effects towards 5-HT1A receptor,and their EC50 values were 7.86,7.32,2.24,1.18,1.52,and 3.75 μmol/L,respectively.Fur-thermore,in vivo experimental results fully revealed that hirsuteine (7) displayed a significant antidepression effect in unpredictable chronic mild stress (UCMS)-induced depression mice mainly via regulating 5-HT1A signaling pathway.Molecular docking and site-directed amino acid mutation verified that amino acid residues Asp116 and Asn386 were the binding sites of hirsuteine (7) with 5-HT1A receptor.In addition,pre-treatment of mice with WAY 100635 also blocked the anti-depression effect of hirsuteine (7),which further demonstrated that 5-HT1A receptor was a potential target of hirsuteine (7) to effectively treat depression.These findings indi-cated the therapeutic material basis of U.rhynchophylla and the anti-depression underlying mechanism of hirsuteine (7),and further provided the useful guidance for the development of hirsuteine (7) as a potential antidepressant candidate.
其他文献
The recent Ir/Pd co-catalyzed photo carboxylation of aromatic halides with CO2 has shown high efficiency and excellent functional group tolerance for preparing aromatic carboxylic acids and esters. With the aid of density functional theory (DFT) calculati
Fluorescent sensing for specific detection of berberine is an important issue in view of its potential jeopardization to food safety and human health, but remains less investigated. To the best of our knowledge, there is no fluorescence turn-on and ratiom
The asymmetric transfer hydrogenation (ATH) of a wide range of ketones catalyzed by manganese complex as well as chiral PxNy-type ligand under mild conditions was investigated. Using 2-propanol as hydrogen source, various ketones could be enantioselective
Fluorescent supramolecular nucleoside-based organogels or hydrogels have attracted increasing attention owing to their tunable stability, drug delivery, tissue engineering, and inherent biocompatibili-ty for applications in designing sensors. As the tempe
Disclosed herein is an efficient Ag-catalyzed [4+1] heteroannulation reaction of enamides with α-carbonyl sulfoxonium ylides. The diastereoselective transformation provides a practical access to a diverse range of multi-functionalized oxazoline derivative
We report a 2-iodoxybenzoic acid (IBX)-mediated intarmolecular oxidative spiro-fused tandem cyclization reaction of tryptophan analogs bearing an N-arylamides side-chain to rapidly afford polycyclic spiroindolines featuring multiple stereocenters includin
Diseases caused by microbial bacteria such as Haemophilus influenzae type b (Hib), Streptococcus pneumoniae and Neisseria meningitidis are still very serious disease, which has brought a lot of burden to many countries. Development of vaccine has brought
Aphamines A–C (1–3), three pairs of acyclic diterpene dimer enantiomers with an unprecedent ploymerization pattern, were discovered from Aphanamixis polystachya by NMR-guided isolation and chiral resolution. The elucidation of their novel carbon skeletons
An efficient Pd-catalyzed double annulation reaction of 1-(2,6-dibromophenyl)-1H-pyrroles with arynes is developed to synthesize π-extended dibenzo[d,k]ullazines in good to excellent yields. For the first time, the parent dibenzo[d,k]ullazine core is obta
A Ru(Ⅱ)-catalyzed para-difluoroalkylation of aromatic aldehydes and ketones with a transient directing group has been developed. It utilizes less expensive ruthenium catalysts and allows facile access to challenging difluoroalkylated aldehydes. The mechan