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Application of 12,15-dioxo-α-ostendene in pharmaceuticals

A kind of ostene, action technology, applied in the field of medicine

Active Publication Date: 2022-06-21
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are no reports in the prior art that the sesquiterpenoid PFC-37 has activity on neurodegenerative diseases and Parkinson's disease

Method used

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  • Application of 12,15-dioxo-α-ostendene in pharmaceuticals
  • Application of 12,15-dioxo-α-ostendene in pharmaceuticals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Preparation process of compound PFC-37:

[0018] The dried agarwood (heartwood of Aquilaria sinensis (Lour.) Spreng.; 2.9kg) was pulverized, 90% ethanol was ultrasonically extracted at 60°C for 30min, and finally a concentrated crude extract (459.3g) was obtained. Then the extract was suspended in water, extracted with equal volumes of petroleum ether, ethyl acetate and n-butanol in turn, and the solvent was recovered to obtain 0.7 g of petroleum ether extract, 374.8 g of ethyl acetate extract, and 52.5 g of n-butanol extract .

[0019] The ethyl acetate extraction part (374.8g) was mixed with an equal amount of 80-100 mesh silica gel, and was segmented by normal phase silica gel column chromatography, the eluent was petroleum ether-ethyl acetate system (50:1, 30:1 , 20:1, 10:1, 5:1, 3:1, 2:1, 1:1, 0:1, v / v) gradient elution, followed by ethyl acetate-methanol system ( 5:1, 3:1, 2:1, 1:1, 0:1, v / v), the same components were combined by TLC to obtain 5 parts (Fr.Y-1~Fr...

Embodiment 2

[0025] The neuroprotective activity test method of compound PFC-37 is as follows:

[0026] 1. PC12 poorly differentiated cells were cultured in DMEM high glucose + 10% FBS + 100U / mL double antibody medium, incubator temperature 37°C, 5% CO 2 ;

[0027] 2. When PC12 poorly differentiated cells grow to an appropriate number, trypsin digestion to prepare a cell suspension;

[0028] 3. Aspirate the cell suspension into a 15mL centrifuge tube, 800rpm, 5min;

[0029] 4. After centrifugation, the centrifuge tube is sterilized with alcohol and taken into the ultra-clean bench, and the supernatant is poured into the waste liquid tank;

[0030]5. Add 5 mL of new complete medium, pipette ten times, and blow away the cells as much as possible, but not too hard;

[0031] 6. Take 0.02mL of cell suspension, add it to the cell counting plate, and count;

[0032] 7. Adjust the cell concentration to 1 × 10 5 cells / mL, added to 96-well plate, 0.1 mL per well, and cultured in a cell incubato...

Embodiment 3

[0041] Effect of neuroprotective activity of compound PFC-37:

[0042] The neuroprotective activity data of the compound PFC-37 are shown in Table 1. At the compound concentration of 1 μM and 2 μM, MPP + The induced PC12 cell injury had significant protective activity (P<0.001).

[0043] Table 1. Compound PFC-37 vs MPP + Protective effect of induced PC12 cell injury

[0044]

[0045] Notes to Table 1: Compared with the model group, **P<0.01, ***P<0.001.

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Abstract

The invention provides the application of 12,15-dioxo-α-osthole (PFC-37) in the preparation of drugs for preventing and treating neurodegenerative diseases and Parkinson's disease. PFC‑37 to MPP + The induced PC12 injury has a significant protective effect, and can be used to prepare a pharmaceutical composition or a dietary supplement composition for preventing and treating Parkinson's disease.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, in particular to the application of 12,15-dioxo-α-ostene in the preparation of medicines for preventing and treating neurodegenerative diseases. Background technique: [0002] Parkinson's disease is a common neurological disease in middle-aged and elderly people. At present, levodopa replacement therapy is mainly used to treat Parkinson's disease, but it cannot prevent the progress of Parkinson's disease. The efficacy begins to decline after 3 to 5 years, and there are not only early adverse reactions (anorexia, nausea, dizziness, mental disorders and dyskinesia). Symptoms, etc.), long-term use will also lead to "switching phenomenon", end-of-dose phenomenon and dystonia, etc. [Sun Jing, Xiong Hang, Yao Yuxi. Progress in the treatment of Parkinson's disease. Medical Review, 2020, 26(2): 1157-1160, 1165.]. Therefore, finding new therapeutic drugs and methods is a hot and difficult point of res...

Claims

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Application Information

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IPC IPC(8): A61K31/11A61P25/28A61P25/16A23L33/10
CPCA61K31/11A61P25/28A61P25/16A23L33/10
Inventor 王跃虎罗吉凤何倩张璐魏舒娅夏梦媛
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI