Sapogenin derivatives, their synthesis and use and method based upon the use

A saponin and compound technology, applied in the field of sapogenin and its derivatives, can solve the problem of poor saponin effect

Inactive Publication Date: 2005-10-05
菲特法姆股份有限公司
View PDF4 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Saponins tend to dissolve in water, while saponins are fat-soluble, so saponins are less effective at penetrating the cerebrovascular barrier

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Sapogenin derivatives, their synthesis and use and method based upon the use
  • Sapogenin derivatives, their synthesis and use and method based upon the use
  • Sapogenin derivatives, their synthesis and use and method based upon the use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0168] Cell-based analysis

[0169] For episarsaporin formate ethyl acid, sarsasapogenin formate ethyl acid, episarsasogenin formate ethyl acid, episarsasogenin succinic acid, episarsasogenin acetic acid And the effect of sarsasapogenin on the expression of m receptor in CHO cells transfected by m receptor was observed. The number of receptors is used [ 3 H] NMS binding and subtracting non-specific binding analysis. The compound is dissolved in dimethyl sulfoxide (DMSO), and the control group is DMSO.

[0170] method:

[0171] On the day before the experiment, Chinese hamster ovary (CHO) cells with high muscarinic receptor expression (approximately 2.2 pmol per mg protein) were cultured in 24-well culture dishes. The culture medium was replaced with a culture medium containing a carrier (DMSO) or test compound. After 2 / 3 days, the culture medium was replaced once, and the cells were allowed to stand for another 2 / 3 days. The cell line was placed in a saturated concentration of N-m...

Embodiment 2

[0178] Alzheimer's disease pattern

[0179] In a living Alzheimer's disease model, amyloid beta and ibotenic acid are injected into the brain of rats, causing loss of receptors in the brain and cognitive impairment. Previous studies have shown that local injection of starch-like β into the nucleus vasalis of the rat brain leads to hypocholinergic function and behavioral impairment for up to 2 months after surgery (Giovannelli et al., 1995: Neuroscience, 66, 781-792). In addition, at the same time, amyloid β and a small amount of ibotenic acid were transferred to the hippocampus of rats in a benign and synergistic manner to produce nerve loss, accompanied by the penetration of ganglion cells to the surrounding and distant parts of the injection site (Morimoto et al., 1998 : Neuroscience, 84, 479-487).

[0180] method:

[0181] Our study used Morimoto's method (Morimoto et al., 1998: Neuroscience, 84, 479-487), with some modifications (instead of bilateral injection with unilateral ...

Embodiment 3

[0204] Learning and memory test

[0205] The old Sprague-Dawley rats were randomly divided into 4 groups, a control group, which seemed to receive sarsasapogenin, episarasapogenin ethyl carbonate, or smilaxin (18 mg per day). / kg, n=10) 3 groups up to 3 months. A control group (n=14) composed of young rats that did not receive any treatment is also included in this example. The daily dose of the drug is mixed with a minimum amount of food and given to individual rats every morning.

[0206] Y-maze is used for learning and memory test. There is an array of copper rods on the floor of each branch of the Y-maze, which can be supplied with currents of different voltages when needed. Each branch is 45cm long and has a 15W bulb at the end, which can be lit when needed. After using the drug for 3 months, each rat received the following training for 7 consecutive days. During each training period, the rat was placed in a branch of the Y-maze. After resting for 2 minutes, an electric curre...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

Disclosed are compounds of formula II, wherein: R is selected from alkylcarbonyl, or alkoxycarbonyl, wherein any alkyl is optionally substituted with aryl, amino, alkoxycarbonylamino, mono-alkyl-amino, di-alkyl-amino, N-alkyl, N-alkoxycarbonyl-amino, or a carboxylic acid residue (-COOH), or any combination thereof. The compounds are used in foodstuffs, food supplements, beverages or medicaments for use in the treatment of cognitive dysfunction, non-cognitive neurodegeneration, non-cognitive neuromuscular degeneration, and receptor loss.

Description

Invention field [0001] The present invention relates to a sapogenin and its derivatives, its synthesis and use, and a method based on its use. [0002] The use of sapogenin and its derivatives is to treat cognitive dysfunction, non-cognitive neurological decline, non-cognitive neuromuscular decline and receptor loss. Furthermore, the present invention relates to compositions for these treatments. Background of the invention [0003] Cognitive dysfunction is a characteristic of the state and symptoms of dementia, such as Alzheimer's disease (AD), Alzheimer's type dementia (SDAT), Lewi body dementia and vascular dementia. Lower degree of cognitive impairment is also characteristic of certain non-dementia states and symptoms, such as moderate cognitive impairment (MCI), age-related memory impairment (AAMI) and autism. [0004] Non-cognitive neurological decline (ie, neurological decline without cognitive dysfunction) and non-cognitive neuromuscular decline (ie, neuromuscular decline...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A23L1/30A61KA61K31/58A61K31/585A61K36/18A61P3/02A61P9/02A61P9/04A61P11/06A61P21/00A61P21/04A61P25/00A61P25/02A61P25/08A61P25/14A61P25/16A61P25/28A61P27/00A61P27/02C07J41/00C07J71/00C07J75/00
CPCA61K31/585C07J71/00A61P11/06A61P21/00A61P21/04A61P25/00A61P25/02A61P25/08A61P25/14A61P25/16A61P25/28A61P27/00A61P27/02A61P3/02A61P9/02A61P9/04A61K31/58
Inventor P·巴勒克拉夫J·哈森P·冈宁D·里斯夏宗勤胡雅儿
Owner 菲特法姆股份有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap