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Spirostanol glycoside-type compound, and application and preparation method thereof

A spirosteroid saponin and compound technology, applied in the field of medicine, can solve problems such as oxidation and oxygenation deficiency, immune system disorders, and DNA repair, and achieve anti-hypoxic and significant effects

Active Publication Date: 2013-01-09
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In addition, hypoxia is the main cause of immune system diseases, which can cause immune system disorders; hypoxia is a significant factor in immune and degenerative diseases, hypoxia can lead to the occurrence of various degenerative diseases; hypoxia causes chronic pain, all chronic Pain and illness are all caused by the lack of oxygen in the physiological amount of normal cells; oxygen is an antidote for important cells, and hypoxia will result in insufficient oxidation and oxygenation, leaving cells in a toxic environment and causing detoxification obstacles; hypoxia affects DNA. repair

Method used

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  • Spirostanol glycoside-type compound, and application and preparation method thereof
  • Spirostanol glycoside-type compound, and application and preparation method thereof
  • Spirostanol glycoside-type compound, and application and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] (1) Grind 6.5 kg of dried whole herb of Selaginella uncinata (Desv.) Spring, heat and reflux extract three times with 15 times the amount of 60% ethanol, the extraction temperature is 10-150°C, 2 hours each time, to obtain primary extract;

[0038] (2) Remove insoluble matter by filtration, and dry the filtrate under reduced pressure to obtain ethanol extract.

[0039] (3) The ethanol extract was extracted three times with equal volumes of petroleum ether, chloroform, ethyl acetate and n-butanol;

[0040] (4) Take the n-butanol extract and dry it under reduced pressure in vacuum to obtain the n-butanol extract. The n-butanol extract was dried under reduced pressure in vacuo to obtain n-butanol extract.

[0041](5) The n-butanol extract was subjected to open silica gel column chromatography, and chloroform:methanol were 99:1, 98:2, 97:3, 95:5, 9:1, 8:2, 7:3 , 6:4 solvent gradient elution. Comprehensively using gel SephadexLH-20 column chromatography, ODS column chrom...

Embodiment 2

[0062] Compounds 1-6 prepared in Example 1 were formulated into liquids with a concentration of 180 μmol / L, 90 μmol / L, and 45 μmol / L as the drug group, and 10% DMSO (dimethyl sulfoxide) as the control group. Baicalin was used as a positive control, and the cell hypoxia protection test was performed on PC12 cells, and the survival percentage of PC12 cells was calculated. The experimental results are calculated by Student’s t test (t-distribution test), expressed as: (mean ± standard deviation). The results are shown in Table 4.

[0063] Table 4. Protective effect of compounds 1-6 on hypoxic nerve cell PC12

[0064]

[0065] Note: Compared with the control group, *P<0.05, **P<0.01

[0066] (P: Statistically significant; P<0.05: Indicates that the difference is statistically significant; P<0.01: Indicates that there is a significant difference.)

[0067] Conclusion: It can be seen from Table 4 that compared with the blank solvent group, compounds 1-6 have stronger prote...

Embodiment 3

[0069] The compounds 1-6 prepared in Example 1 were formulated into a drug solution with a concentration of 40 mg / mL as the drug group, and 20% DMSO was used as the control group to carry out the airtight hypoxia tolerance test in mice, and observe the mice in airtight conditions. The following survival time. The experimental results are calculated by Student’s t test (t-distribution test), expressed as: (mean ± standard deviation). n is the number of mice. The results are shown in Table 5.

[0070] The impact of table 5 compounds on the survival time of mice under hypoxic conditions ( n=10)

[0071]

[0072] Note: Compared with the control group, *P<0.05, **P<0.01

[0073] (P: Statistically significant; P<0.05: Indicates that the difference is statistically significant; P<0.01: Indicates that there is a significant difference.)

[0074] Conclusion: It can be seen from Table 5 that compared with the control group, compound 1-6 can significantly improve the surviva...

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Abstract

The invention discloses a spirostanol glycoside-type compound, and application and a preparation method thereof. The invention provides the application of the spirostanol glycoside-type compound to the preparation of anti-hypoxic medicines or food. The spirostanol glycoside-type compound has the following general structural formula. The method for preparing the spirostanol glycoside-type compound comprises the following steps of: crushing dried selaginella uncinata spring, and performing reflux extraction on the crushed selaginella uncinata spring by adding a solvent or water; removing insoluble substances by filtration or centrifugation, and drying under reduced pressure to obtain initial extract; dispersing the initial extract into isometric water, and performing extraction by adding petroleum ether, chloroform, ethyl acetate and normal butyl alcohol in sequence; and drying the liquid extract of normal butyl alcohol under reduced pressure to obtain extract of normal butyl alcohol; and separating and purifying the extract of normal butyl alcohol by the chromatography to obtain the spirostanol glycoside-type compound.

Description

technical field [0001] The invention relates to a spirosteroid saponin compound and its application and preparation method, belonging to the field of medicine. Background technique [0002] Selaginella uncinata (Desv.) Spring is the whole herb of Selaginella uncinata (Desv.) Spring, which grows in damp mountains and rocks, and is mainly distributed in Guangxi, Guangdong, Fujian, Zhejiang, Anhui and Southwest China. According to the Chinese Medicine Dictionary, it uses the whole herb as medicine and is called Cuiyucao. It is mainly used to treat edema, jaundice, gonorrhea, red and white dysentery, hematemesis, damp phlegm cough, joint rheumatic pain, accumulated injury in the chest and hypochondriac, hemorrhoids, leg cramps and other diseases. [0003] Steroidal saponins (Steroidal saponins) is a class of important biologically active substances in plants, and the study of steroidal saponins has always occupied an important position in natural product chemistry. The aglycon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P39/00A23L1/30
Inventor 郑俊霞郑扬张焜赵肃清高昊范明吴丽颖
Owner GUANGDONG UNIV OF TECH
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