HyponicosidesA-D(1-4) as well as pharmaceutical composition thereof and application thereof

A technology of dimethylpyroglucinol and its derivatives, which is applied in the field of medicine, and can solve the problems of no dimethylpyroglucinol derivatives, no PC12 cell protection, and no reports of compound 1-4 pharmaceutical compositions, etc.

Active Publication Date: 2019-04-05
KUNMING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no report about these four dimethylpyroglucinol derivatives hyponicosides A-D (1-4) in the prior art, and there is no report on the pharmaceutical composition of compound 1-4 as an active ingredient, nor compound 1-4. 4 The protective effect of the pharmaceutical composition on PC12 cells induced by corticosterone, and its application in the preparation and treatment of mental diseases

Method used

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  • HyponicosidesA-D(1-4) as well as pharmaceutical composition thereof and application thereof
  • HyponicosidesA-D(1-4) as well as pharmaceutical composition thereof and application thereof
  • HyponicosidesA-D(1-4) as well as pharmaceutical composition thereof and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of compounds hyponicosides A-D (1-4):

[0031] Take the dried whole herb of Lymphis chinensis, crush it, soak and extract it with 95% ethanol at room temperature for three times, each time for 48 hours, combine the extracts and recover the ethanol under reduced pressure to obtain an extract, which is dissolved and adsorbed on silica gel with 95% ethanol, and left at room temperature Place and evaporate the solvent, grind and sieve, and then go through silica gel column chromatography, and then use 1:0, 10:1, 5:1, 0:1 chloroform-methanol gradient elution, and the amount of each gradient solvent is 1 / 2 of the column volume. 2 times, the 10:1 chloroform-methanol elution part continued to go through silica gel column chromatography, and was combined into four components by TLC detection. The second component was subjected to silica gel column chromatography and wasocratically eluted with 20:1 chloroform-methanol , combined into 8 subcomponents Fr2.1-Fr2.8 after ...

Embodiment 2

[0033] Structural identification of compound hyponicosidesA-D(1-4):

[0034] Compound 1

[0035] Molecular formula: C 18 h 26 o 9

[0036] Molecular weight: 386

[0037] Appearance: white amorphous powder

[0038] HRESIMS(m / z):409.1466[M+Na] + (Calcd for 409.1469)

[0039] IR(KBr)cm -1 : 3428, 2969, 2928, 2879, 1620, 1460, 1426, 1384, 1148, 1075, 907, 805, 617, 571.

[0040] UV (MeOH) λ max (log ε): 219 (5.24), 287 (4.85) nm.

[0041] 1 H-NMR and 13 See Table 1 for C-NMR data.

[0042] (c 0.003, MeOH)

[0043] Compound 2

[0044] Molecular formula: C 18 h 26 o 9

[0045] Molecular weight: 400

[0046] Appearance: white amorphous powder

[0047] HRESIMS(m / z):423.1629[M+Na] + (Calcd for 423.1630)

[0048] IR(KBr)cm -1 : 3420, 2966, 2931, 2877, 1614, 1459, 1427, 1378, 1286, 1238, 1147, 1074, 907, 818, 796, 775, 657, 631, 567, 519.

[0049] UV (MeOH) λ max (log ε): 219 (4.89), 287 (4.12) nm.

[0050] 1 H-NMR and 13 See Table 1 for C-NMR data.

[0051] ...

Embodiment 3

[0074] Protective effects of compounds hyponicosides A-D(1-4) against corticosterone-induced neurological injury.

[0075] In this example, corticosterone (CORT) was purchased from Sigma, high glucose medium (DMEM), fetal bovine serum (FBS), and PBS were purchased from BI, and PC12 poorly differentiated cells were purchased from the Cell Bank of Kunming Institute of Zoology, Chinese Academy of Sciences, Pancreas Protease was purchased from Gibco, USA; phosphate buffer saline (PBS) was purchased from Wuhan Boster Company; [3-(4,5-dimethylpyridin-2-yl)-5-(3-carboxymethoxyphenyl )-2-(4-sulfophenyl)-2H-tetrazole] (MTS) was purchased from Sigma, USA; desipramine (DIM) was purchased from Beijing Putin Kangli Technology Co., Ltd.

[0076] Experimental design: Each group was designed to do 3 repetitions.

[0077] Blank control group (Blank): no CORT, DIM, only cells and DMSO with a final concentration of 0.1%;

[0078] Model group (NC): DMSO with a final concentration of 120 μM CORT...

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Abstract

The invention discloses hyponicosidesA-D(1-4) separated from Hypericum japonicum, a pharmaceutical composition taking the hyponicosidesA-D(1-4) as an effective component and application of the hyponicosidesA-D(1-4) to preparation of drugs for treating mental diseases. The hyponicosidesA-D(1-4) disclosed by the invention have remarkable protection effects on PC12 cells damaged by induction of corticosterone, so that the hyponicosidesA-D(1-4) have potential for treating mental diseases, preferably treating mental diseases such as depression, senile dementia, anxiety, obsessive-compulsive disorder and schizophrenia of emotional and cognitive impairment.

Description

technical field [0001] The invention belongs to the technical field of medicines, and specifically relates to four dimethylpyroglucinol derivatives hyponicosides A-D (1-4), which are used as active ingredients in a pharmaceutical composition for preparing and treating mental diseases, such as depression, Application in the treatment of Alzheimer's disease, anxiety disorder, obsessive-compulsive disorder and schizophrenia. Background technique: [0002] Mental diseases are mainly a group of nervous system diseases mainly manifested in disorders of behavior and psychological activities. Depression is a common mental illness, mainly manifested as low mood, slow thinking, decreased volitional activity, cognitive impairment, and a series of physical symptoms. In severe cases, even suicidal thoughts and behaviors appear. Features such as high morbidity rate. At present, there are about 350 million depression patients in the world, and the number of people who commit suicide ever...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/08A61K31/7034A61P25/24A61P25/28A61P25/22A61P25/18A61P25/00A23L33/105
CPCA23V2002/00A23L33/105A61P25/00A61P25/18A61P25/22A61P25/24A61P25/28C07H1/08C07H15/203A23V2200/322A23V2250/21
Inventor 王扣王赟王子明李荣生苏婕俪
Owner KUNMING MEDICAL UNIVERSITY
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