Applications of piceatannol 3-O'-glucoside or piceatannol 3-O'-glucoside derivatives

A technology of tristilbene and its derivatives, which is applied in the field of biopharmaceuticals and can solve problems such as no reports on the use of drugs for the treatment and prevention of ALS

Inactive Publication Date: 2019-02-01
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The prior art shows that tristilbene and its derivatives have activity in the treatment of ischemic cardiovascular and cerebrovascular diseases, but there is no report on the use of drugs in the treatment and prevention of ALS

Method used

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  • Applications of piceatannol 3-O'-glucoside or piceatannol 3-O'-glucoside derivatives
  • Applications of piceatannol 3-O'-glucoside or piceatannol 3-O'-glucoside derivatives
  • Applications of piceatannol 3-O'-glucoside or piceatannol 3-O'-glucoside derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Effect of Example 1 on Amyotrophic Lateral Sclerosis Cell Model

[0035] 1 test article

[0036] Tristilbene, molecular weight 406, white crystal or crystalline powder, purity 99.6%, batch number 20120402;

[0037] Picetanol, molecular weight 244, reddish-brown powder, purity 99.8%, batch number 906099a;

[0038] Resveratrol, molecular weight 228, white powder, purity 99.8%, batch number CY120325.

[0039] 2 Experimental cells and plasmids

[0040] NSC34 mouse neuron cells were purchased from Guangzhou Geneo Biotechnology Co., Ltd. Cells were cultured in DMEM medium containing 10% FBS at 37°C, 5% CO 2 cultivated in an incubator. Plasmids pF141pAcGFPl SOD1WT and pF145pAcGFPl SOD1G93A were constructed and sequenced by Protin Biotechnology (Beijing) Co., Ltd.

[0041] 3 Reagents and instruments

[0042] DMEM medium, polylysine, DMSO (Gibco, USA); Lipofectamine2000 (Invtrogen, USA); fetal bovine serum (FBS, Hycolne, USA); penicillin-streptomycin (Sigma); ammonium per...

Embodiment 2

[0061] Example 2 In vitro antioxidant effect

[0062] 1 test article

[0063] Tristilbene, molecular weight 406, white crystal or crystalline powder, purity 99.6%, batch number 20120402;

[0064] Picetanol, molecular weight 244, reddish-brown powder, purity 99.8%, batch number 906099a;

[0065] Resveratrol, molecular weight 228, white powder, purity 99.8%, batch number CY120325.

[0066] The above samples were all provided by the Pharmaceutical Research Institute of Kunming Pharmaceutical Group, sealed at room temperature and kept away from light. During the test, it was weighed with a 1 / 100,000 electronic analytical balance, dissolved, prepared and diluted with DMSO, and the concentration of DMSO in each detection system was controlled at 1%.

[0067] 2 reference substance

[0068] Vitamin C, purity 99.5%, CSPC Weisheng Pharmaceutical (Shijiazhuang) Co., Ltd., batch number 1130172056;

[0069] Edaravone injection, 30mg / 20mL, Kunming Jida Pharmaceutical Co., Ltd., batch n...

Embodiment 3

[0107] Example 3 Effects on Glutamic Acid-Induced Neuroexcitotoxicity

[0108] 1 Experimental materials

[0109] 1.1 Test sample

[0110] Tristilbene, molecular weight 406, white crystal or crystalline powder, purity 99.6%, batch number 20120402;

[0111] Picetanol, molecular weight 244, reddish-brown powder, purity 99.8%, batch number 906099a;

[0112] Resveratrol, molecular weight 228, white powder, purity 99.8%, batch number CY120325.

[0113] Preparation method: The test substance is first prepared into 10mM stock solution with DMSO, and then diluted with normal saline to the required concentration.

[0114] 1.2 Negative control substance

[0115] Sodium chloride injection (0.9% normal saline), Qingzhou Yaowang Pharmaceutical Co., Ltd., batch number: 2215110901, specification: 500ml / bottle.

[0116] 1.3 Positive control substance

[0117] Edaravone injection, Nanjing Xiansheng Dongyuan Pharmaceutical Co., Ltd., batch number: 80-170102, specification: 5ml: 10mg.

[0...

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PUM

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Abstract

The invention belongs to the technical field of biological pharmacy, and especially relates to applications of piceatannol 3-O'-glucoside or piceatannol 3-O'-glucoside derivatives. It is shown by research that piceatannol 3-O'-glucoside or the piceatannol 3-O'-glucoside derivatives are capable of inhibiting excitatory amino acid toxicity, preventing nerve cell apoptosis, increasing nerve cell activity, reducing MDA level in nerve cells, and promoting nerve cell proliferation, and posses obvious protection effects on ALS cell models.

Description

technical field [0001] The invention relates to the technical field of biopharmaceuticals, in particular to the use of tristilbeside or its derivatives. Background technique [0002] Motor neuron disease (MND) is a group of chronic progressive neurodegenerative diseases of unknown etiology that selectively invade spinal cord anterior horn cells, brainstem motor neurons, cortical pyramidal cells and pyramidal tracts. According to different clinical manifestations, motor neuron disease can generally be divided into the following four types: amyotrophic lateral sclerosis (ALS); progressive muscular atrophy (PMA); progressive bulbar palsy (PBP); primary lateral Hardened (PLS). Its harmfulness lies in the selective retrograde damage to motor neurons, which manifests as dysfunction and atrophy of the muscles controlled by neurons. If the throat and respiratory muscles are involved, life will end. In addition, motor neuron involvement leads to inability or incoordination of the c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61K31/05A61P25/00A61P39/06A61P21/00
CPCA61K31/05A61K31/7034A61P21/00A61P25/00A61P39/06
Inventor 杨兆祥刘一丹陈云建龚云麒杨旭娟施凯刘国光尚建华
Owner KPC PHARM INC
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