Application of butenyl phthalide and method for preparing butenyl phthalide into pharmaceutical composition

A technology of butenylphthalide and butenylbenzene, which is applied to the application of butenylphthalide and its preparation as a pharmaceutical composition, can solve problems such as threats to human health, and achieve the treatment or prevention of neurodegenerative diseases , the effect of improving safety

Pending Publication Date: 2021-03-09
EVERFRONT BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] It can be seen that neurodegenerative diseases such as Alzheimer's disease do pose a great threat to human health, and based on the fact that there is still no clinically effective drug, therefore, the development of medicines for the treatment or prevention of neurodegenerative diseases Composition is an important subject for scientists

Method used

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  • Application of butenyl phthalide and method for preparing butenyl phthalide into pharmaceutical composition
  • Application of butenyl phthalide and method for preparing butenyl phthalide into pharmaceutical composition
  • Application of butenyl phthalide and method for preparing butenyl phthalide into pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Synthetic Hydrazine Butylphthalide

[0041] Butenyldenephthalide, BDPH, W333301) and F127 polymer substance were obtained from Sigma-Aldrich, US Sigma-Aldrich (PLURONIC F127, P2443). After mixing 10 mg-butardylphenylphthalide and F127 polymer substances in a ratio of 1: 1 or 1: 2, it was dissolved in Tetrahydrofuran, and then added to 10 ml of water, and then heated quickly Tetrahydrofuran was removed to perform freeze drying. Thereafter, the dissolved in water is rehydrated, and the olymiacphphiphenylene particles after the emulsion in the solution are about 30 to 200 nm, and the polydispersity index is 0.2-0.5.

Embodiment 2

[0042] Example 2: Cell culture

[0043] Culture human universal stem cells in serum-free medium Essential 8 TM (Life Technology, United States), and Matrigel TM Bastropin (Becton-Dickinson, USA) is attached. Unexplified the culture fluid, washed with phosphate buffer 2 times, add an enzyme ACCUTASE TM (Merck Millipore, the United States) reacted 2 to 5 minutes later in culture liquid, and the cells were scattered into a small group, and centrifuged 1000 rpm, 2 minutes, and then absorbed the supernatant, and put it in new culture. The culture was cultured for about 3 to 5 days, and the culture fluid was replaced daily during culture during culture.

Embodiment 3

[0044] Example 3: Neuronal differentiation

[0045] Human universal stem cells were cultured to 8-9, and the cells were rinsed with phosphate buffer 2 times, with an enzyme ACCUTASE TM After 2 ~ 5 minutes, the culture solution was added to the enzyme, then rinsed up the cells, scattered until it was appropriate for about 2 minutes, and then placed in the cells in a 20% replacement serum (Knock Out SerumReplacement). DMEM-F12 medium referred to as KSR, Life Technology, USA), was suspended for 2 days, and the Embryonic body suspension was obtained.

[0046] The suspension type embryoid is for the centrifuge tube. After natural settlement, the supernatant is removed, and the neurological inducing medium containing BISF small molecular drug is submitted for 2 days, then the suspended type embryo has a cyclic epithelial cell. Structure, where small molecule drugs contain 0.5 μm BiO (Sigma-Aldrich, USA), 10 ng / ml of fibroblast growth factor-2 (FGF-2, Peprotech, USA) and 10μm SB431542 ...

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PUM

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Abstract

The invention discloses application of butenyl phthalide, analogues thereof or a combination of the butenyl phthalide and the analogues to preparation of a pharmaceutical composition for treating or preventing neurodegenerative diseases, and a method for preparing the pharmaceutical composition from the butenyl phthalide and the analogues thereof. The disclosed butenyl phthalide has the capabilityof reducing the concentration of beta amyloid protein in cells, so that the effect of treating or preventing neurodegenerative diseases can be achieved. Therefore, according to the preparation methodof the pharmaceutical composition disclosed by the invention, the macromolecular substance is used as a drug carrier, and the butenyl phthalide serving as an active ingredient is coated in the macromolecular substance, so that the cytotoxicity of the butenyl phthalide is alleviated or reduced; and the effects of improving the safety of the pharmaceutical composition and treating or preventing neurodegenerative diseases are achieved.

Description

[0001] The present application is a score application for the presentation of invention patent applications, "butenylphenylphthaleine), 2014, 2014, 2014,4103,626,2632. Technical field [0002] The present invention relates to the use of a compound, and more particularly to the use of butenylphenylphthalide and a method of preparing it as a pharmaceutical composition. Background technique [0003] Azheimeria is the highest incidence of neurodegeneity in the world. The main pathological characteristics are deposited in the brain to form a A [beta] plaque (PLAQUE) in the brain. Glennerand Wong 1984; MASTERS, Clet Al., 1985) and Neurofibrillary Tangles, NFT (Grundke-iqbal, Id Al., 1986; Goidert, M. Eti) . Aβ plaque is driven by amyloid protein Precursor, App), which is subjected to Bace Enzyme (β-Site Amyloid Precursor Protein Cleaving Enzyme) (HUSSAIN, I.ET Al., 1999; Vassar, R. Et Al., 1999) ) And gamma secrease (γ-secretase) was cut (Wolfe, Mset Al., 1999; Yu, G.ET Al., 2000), main...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K47/34A61K36/23A61K36/28A61P25/28
Inventor 苏鸿麟张嘉佑黄效民卢怀恩韩鸿志林欣荣赖秉杉
Owner EVERFRONT BIOTECH
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