Uses of butylidenephthalide and method for preparing pharmaceutical composition from butylidenephthalide

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

Inactive Publication Date: 2016-02-10
EVERFRONT BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 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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  • Uses of butylidenephthalide and method for preparing pharmaceutical composition from butylidenephthalide
  • Uses of butylidenephthalide and method for preparing pharmaceutical composition from butylidenephthalide
  • Uses of butylidenephthalide and method for preparing pharmaceutical composition from butylidenephthalide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Synthesis of aqueous phase butenylphthalide

[0040] Butenyl phthalide (n-butylidenephthalide, Bdph, W333301) and F127 polymer substance (Pluronic F127, P2443) were obtained from Sigma-Aldrich, USA. After mixing 10 mg of butenylphthalide and F127 macromolecular substance at a weight ratio of 1:1 or 1:2, dissolve it in 2 ml of tetrahydrofuran (tetrahydrofuran), add it to 10 ml of water, and then heat rapidly The tetrahydrofuran was removed and freeze-dried. Afterwards, it is dissolved in water again, and the butenylphthalide particles emulsified in the solution have a size of about 30-200 nm and a polydispersity index of 0.2-0.5.

Embodiment 2

[0041] Example 2: Cell Culture

[0042] Human pluripotent stem cells were cultured in serum-free medium Essential8 TM (LifeTechnology company, USA), and with matrigel TM Matrigel (Becton-Dickinson Company, USA) was used for attachment culture. Aspirate the culture medium, wash the cells twice with phosphate buffer, then add the enzyme Accutase TM (MerckMillipore Company, USA) After reacting for 2 to 5 minutes, neutralize with culture medium, wash down the cells and break up into small clumps, centrifuge at 1000rpm for 2 minutes, then absorb the supernatant, and put them into a new culture dish Culture in medium for about 3 to 5 days, then subculture, and the culture medium must be changed every day during the culture period.

Embodiment 3

[0043] Example 3: Neural cell differentiation

[0044] Culture the human pluripotent stem cells to 8-9 minutes full, wash the cells with phosphate buffered saline twice, and use the enzyme Accutase TM After acting for 2 to 5 minutes, add culture medium to dilute the enzyme, then wash the cells down, break up to an appropriate size, and centrifuge at 800rpm for about 2 minutes, and then place the cells in a place containing 20% ​​serum replacement (knockoutserum replacement, KSR for short). , LifeTechnology Company, U.S.A.) DMEM-F12 medium, carried out suspension culture with uncovered petri dish for 2 days, and obtained embryoid body (Embryonicbody) suspension.

[0045] Put the suspended embryoid body in a centrifuge tube, after natural sedimentation, remove the supernatant, and carry out suspension culture for 2 days with the neural induction medium containing BiSF small molecule drug, and then, the suspended embryoid body will appear ring-shaped epithelial cells Structure, ...

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Abstract

The present invention discloses uses of butylidenephthalide, an analog thereof or a combination of the butylidenephthalide and the analog thereof in preparation of pharmaceutical compositions for treatment or prevention of neurodegenerative diseases, and a method for preparing the pharmaceutical composition from the butylidenephthalide. According to the present invention, the disclosed butylidenephthalide can reduce the intracellular amyloid beta-protein concentration so as to achieve the effect of treatment or prevention of neurodegenerative diseases; and according to the preparation method of the disclosed pharmaceutical composition, the polymer substance is adopted as the drug carrier to coat the butylidenephthalide adopted as the active component into the polymer substance so as to slow down or reduce the cytotoxicity of the butylidenephthalide, improve the safety of the pharmaceutical composition, and treat or prevent neurodegenerative diseases.

Description

technical field [0001] The present invention relates to the use of compounds, in particular to the use of butenylphthalide and a method for preparing it as a pharmaceutical composition. Background technique [0002] Alzheimer's disease is the neurodegenerative disease with the highest incidence rate in the world, and its main pathological feature is excessive deposition of β-amyloid protein (Aβ) in the brain, forming Aβ plaques (Glenner and Wong1984 ; Masters, C.L.etal., 1985) and intracellular tangles of nerve fibers (neurofibrillarytangles, NFT) (Grundke-Iqbal, I.etal., 1986; Goedert, M.etal., 1988). The Aβ plaque is composed of amyloid protein precursor (APP), BACE enzyme (β-siteamyloidprecursorprotein cleavingenzyme) (Hussain, I.etal., 1999; Vassar, R.etal., 1999) and γ-secretase (γ-secretase). ) produced after cleavage (Wolfe, M.S.etal., 1999; Yu, G.etal., 2000), mainly including two forms of Aβ40 and Aβ42 (Jarrett, J.T.etal., 1993). When amyloid beta accumulates in l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K47/34A61P25/28
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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