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Aquilarotetrol as well as pharmaceutical composition, preparation method and application thereof

A kind of white wood fragrance and composition technology, which is applied in the field of medicine, can solve the problems of no new compound white woody tetraol, no PES-22 neurodegenerative disease and depression, and achieve significant protective activity and good neuroprotective activity , high yield effect

Pending Publication Date: 2021-12-31
北京中科沉香科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no report on the new compound aquilarotetrol (PES-22) in the prior art, and there is no report on the activity of PES-22 on neurodegenerative diseases and depression

Method used

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  • Aquilarotetrol as well as pharmaceutical composition, preparation method and application thereof
  • Aquilarotetrol as well as pharmaceutical composition, preparation method and application thereof
  • Aquilarotetrol as well as pharmaceutical composition, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation process of compound Pyramidol (PES-22):

[0033] Dried Chinese medicine Aquilaria sinensis, that is, Aquilaria sinensis (Lour.) Spreng. Aquilaria sinensis (Lour.) Spreng. The heartwood (2.9 kg) containing resin was pulverized and ultrasonically extracted with 10 L of 90% ethanol for 5 times, each time for 30 min. The solvent was distilled off from the extract under reduced pressure to obtain an extract (459.3 g). Then suspend the extract in 1L of water, extract with equal volumes of petroleum ether (5×1L), ethyl acetate (5×1L) and n-butanol (5×1L) successively, and recover the solvent to obtain 0.7 g of petroleum ether, ethyl acetate The ester fraction was 374.8 g, the n-butanol fraction was 55.9 g, and the water fraction (raffinate fraction) was 6.9 g.

[0034] Take the n-butanol fraction (55.9g) and mix the sample with 80-100 mesh silica gel, pack it into a column, and carry out gradient elution with ethyl acetate-methanol (100:0→0:1, v / v) as the elue...

Embodiment 2

[0036] Spectral data and structure identification of compound PES-22:

[0037] Aquilarotetrol (PES-22), colorless solid; [α] D 25 -98.1(c 0.13, MeOH); UV(MeOH)λ max (logε)250(3.20)nm; ECD(c 0.0097, MeOH)λ max (Δε)205(-19.88)nm; 1 H NMR and 13 CNMR data in Table 1; ESIMS m / z 331[M+Na] + ;HRESIMS m / z 331.1514[M+Na] + (calcd forC 17 h 24 NaO 5 , 331.1521).

[0038] According to compound PES-22 high resolution mass spectrometry (HRESIMS) and 13 C NMR data (Table 1), it is speculated that its molecular formula is C 17 h 24 o 5 , with 6 degrees of unsaturation. its 1 The H NMR signal (Table 1) indicates that there is a monosubstituted benzene ring [δ7.23(2H,m), 7.19(2H,m), 7.12(1H,m)] and a disubstituted double bond [δ5.96 (1H,m),5.92(1H,m)]. According to the COZY correlation of the compound ( figure 1 ), two fragments can be obtained, namely C-2 to C-6, and C-1' to C-11'; according to H-2 and H-6 and C-1', and H-3, H-5 and H 2 -2' is related to the HMBC of C-1, ...

Embodiment 3

[0042] The neuroprotective activity test method of compound PES-22 is as follows:

[0043] 1. PC12 poorly differentiated cells are cultured in the medium of DMEM+10%FBS+100U / mL double antibody, the temperature of the incubator is 37℃, 5%CO 2 ;

[0044] 2. When PC12 poorly differentiated cells grow to an appropriate number, take PC12 poorly differentiated cells, digest with trypsin, and make cell suspension;

[0045] 3. Pipette the cell suspension into a 15mL centrifuge tube, 800rpm, 5min;

[0046] 4. After the centrifugation is finished, the centrifuge tube is disinfected with alcohol and taken into the ultra-clean bench, and the supernatant is poured into the waste liquid tank;

[0047] 5. Add 5 mL of new complete medium, pipette ten times to blow the cells as much as possible, but not too hard;

[0048] 6. Take 0.02mL of cell suspension, add it to the cell counting plate, and count on the machine;

[0049] 7. Adjust the cell concentration to 1 x 10 5 cells / mL, add to 96...

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PUM

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Abstract

The invention provides aquilarotetrol as well as a pharmaceutical composition, a preparation method and application thereof, and belongs to the technical field of medicines. The invention provides the aquilarotetrol (PES-22)as well as the preparation method thereof, and an application of the aquilarotetrol in preparation of medicines for preventing and treating neurodegenerative diseases and depression. The PES-22 has a remarkable protection effect on corticosterone-induced PC12 cell injury, and can be used for preparing a pharmaceutical composition or a dietary supplement composition for preventing and treating depression.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of crested tetral and the application of crested pyritol in the preparation of medicines and functional foods for preventing and treating neurodegenerative diseases. Background technique: [0002] Depression, also known as depressive disorder, is a mental system disease with complex and diverse pathogenesis. Its typical characteristics are high morbidity, mortality and disability, which seriously threaten the physical and mental health of human beings. In recent years, although people have revealed the potential development mechanism of depression from many aspects, there is still no unified standard. The existing therapeutic drugs have the disadvantage that the curative effect is relatively slow, and some drugs have side effects such as thirst, dry stool, and elevated blood pressure [Gao Guiyuan, Huang Jie, Liu Dan, Zhang Fang, Zhang Chaoqun, Z...

Claims

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Application Information

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IPC IPC(8): C07D307/28A61P25/00A61K31/341A23L33/105
CPCC07D307/28A61P25/00A23L33/105A23V2002/00A23V2200/322A23V2250/21
Inventor 王跃虎张璐罗吉凤杨珺
Owner 北京中科沉香科技股份有限公司
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