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Application of gastrodine derivative

A derivative, gastrodin technology, applied in the application field of gastrodin derivatives, can solve the problems of toxic side effects and low bioavailability, and achieve the effects of strong stability, short synthesis steps and high yield

Active Publication Date: 2016-12-07
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The AChEIs approved by the FDA are tacrine, donepezil, estigmine and galantamine respectively. These drugs are all synthetic products with low bioavailability. It affects the peripheral cholinergic system, leading to different degrees of toxic and side effects (Yang Xiaojun, Liu Ruijun, Li Qifeng, etc. Research status of acetylcholinesterase inhibitors. Journal of Changjiang University, 2005,5,2(5):49-52), among them Crean has been forced to withdraw from the market due to severe liver toxicity

Method used

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  • Application of gastrodine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Inhibition of cholinesterase

[0026] experiment material:

[0027] Test sample: KPC-3000207 (namely the above-mentioned gastrodin derivative), white powder, batch number JT20161014, content >98%;

[0028] Reagents: Acetylcholinesterase (CAS: 9000-81-1), Sigma, batch number SLBK4849V; Acetylcholine iodide (CAS: 2260-50-6) purity ≥ 98%, Sigma, batch number BCBL0098V; DTNB, 5,5-dithiobis( 2-nitrobenzoic acid) (5,5'-Dithiobis (2-nitrobenzoic acid)) (CAS: 69-78-3), Sigma, batch number SHBD2937V; Tris-Base, Purity≥99.9%, Amresco product, Exp: 201512; DMSO, Dimethylsuifoxide, sigma, batch number BCBM7089V; Concentrated hydrochloric acid, Yunnan Shandian Pharmaceutical Co., Ltd., batch number 20090402; NaOH, Shanghai Abby Chemical Reagent Co., Ltd., batch number 20110223; NaHCO3, Beijing Lingyun Building Materials Chemical Co., Ltd., batch number 20090805; Ultrapure water, ready to use, was prepared by a Milli-Q ultrapure water machine (Merch Millipore, Germany). ...

Embodiment 2

[0039] Example 2 In vivo efficacy verification

[0040]Establish rat and mouse cognitive impairment models to verify the pharmacological effects of gastrodin derivatives in vivo.

[0041] experiment material:

[0042] YLS-17B dark shuttle recorder, Shandong Jinan Yiyan Technology Development Co., Ltd.; PowerWaveXS2 full-wavelength microplate reader, BioTek; Q55-200 ultrasonic breaker, Gene Company Limited; AC211S electronic analytical balance, Sartorius Company; LT2000B electronic balance , Changshu Tianliang Instrument Co., Ltd.; DHG-9245A electric constant temperature blast drying oven, Shanghai Yiheng Scientific Instrument Co., Ltd.; Eppendorf series of micro pipettes with various ranges; beaker, measuring cylinder, scissors, ophthalmic curved forceps, hemostat , arterial clips, sutures and other consumables are all made in China.

[0043] Experimental animals:

[0044] SPF-grade male ICR mice (4-5 weeks old, 20-25 g) were provided by the Experimental Animal Laboratory o...

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Abstract

The invention discloses application of a gastrodine derivative, and provides application of the gastrodine derivative in preparation of a cholinesterase inhibitor. The gastrodine derivative has the following structure (please see the structure in the description). The new gastrodine derivative is provided by conducting structure improvement on gastrodine, the derivative can inhibit the activity of cholinesterase, and the new purpose for preparing a drug for preventing and treating a cognitive disorder is not researched or reported yet at present. The compound has the good lipid solubility, is beneficial for penetrating a blood brain barrier, high in stability, short in synthesis step and high in yield and can be applied to industrialized production. The gastrodine derivative has the molecular advantages that glycosyl of gastrodine is directly substituted with ferulic acid, and benzyl hydroxyl on gastrodine aglycone is esterified by nitric acid.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of a gastrodin derivative. Background technique [0002] Cognitive impairment refers to a gradual degeneration of cognitive function caused by disease or brain injury, and the degree of this degeneration is much higher than the normal aging process. It is mainly manifested in cognitive learning in a clear state. Symptoms such as functional decline, memory loss or loss, and social activity skill decline can further develop into dementia (Chen Shengdi. Domestic Research Status of Cognitive Impairment. Chinese Journal of Practical Internal Medicine. 2010,10,30(10):875-878). Cognitive impairment is divided into three categories: chronic neurodegenerative diseases, mainly Alzheimer's disease (AD), vascular cognitive impairment (VCI), and cognitive impairment caused by other diseases. Cognitive impairment mostly occurs in the elderly, and with the rapid d...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P25/28
CPCA61K31/216
Inventor 刘一丹宋立明郝世颖施凯尚建华
Owner KPC PHARM INC
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