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Application and preparation method of triterpenoid saponin compound

A technology for triterpenoid saponins and compounds is applied in the field of application and preparation of triterpenoid saponins, and can solve problems such as being difficult to completely remove biofilms and the like

Inactive Publication Date: 2018-03-20
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Animal experiments have also shown that free Candida species diffused from biofilms are more virulent than non-biofilm free Candida species, resulting in worse outcomes for their infections
Biofilm-associated infection is difficult to control because of its stronger drug resistance, and it is difficult to completely clear the biofilm with common antifungal drug treatment
At present, there is no ideal countermeasure against Candida biofilm clinically. How to prevent and overcome the problem of biofilm drug resistance has become a very challenging topic in clinical practice.

Method used

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  • Application and preparation method of triterpenoid saponin compound
  • Application and preparation method of triterpenoid saponin compound
  • Application and preparation method of triterpenoid saponin compound

Examples

Experimental program
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Effect test

Embodiment 1

[0172] Weigh 1 kg of Sapindus chinensis medicinal material, pulverize it and put it in a container, add 10 L of water, extract by ultrasonic for 1 hour, filter, and concentrate the filtrate to obtain the extract extract;

[0173] Take 2kg D101 type macroporous resin, load the sample after pretreatment, and then elute with water, 25% ethanol solution, 50% ethanol solution, 75% ethanol solution, 95% ethanol solution, each gradient elution is 10 column volumes , collect 75%-95% ethanol eluate, concentrate under reduced pressure to obtain total saponins;

[0174] Dissolve the total saponins in methanol, mix the sample with silica gel, conduct silica gel column chromatography, use ethyl acetate-methanol for gradient elution, and further separate the eluted part of ethyl acetate-methanol 10:1 by preparative high-performance liquid chromatography , wherein the high performance liquid chromatography condition is: ODS chromatographic column, mobile phase is 75% methanol elution, flow r...

Embodiment 2

[0176] Weigh 1kg of Sapindus sapinsinum medicinal material, crush it and put it in a container, add 10L of 10% ethanol solution, decoct for 1 hour, filter, and concentrate the filtrate to obtain the extract extract;

[0177] Take 2.5kg D392 type macroporous resin, load the sample after pretreatment, successively elute with water, 25% ethanol solution, 50% ethanol solution, 75% ethanol solution, 95% ethanol solution, collect 75% ethanol eluate, Concentrate under reduced pressure to obtain total saponins;

[0178] Dissolve the total saponins in methanol, mix the sample with silica gel, conduct silica gel column chromatography, and use a dichloromethane-methanol system for gradient elution, and further separate the dichloromethane-methanol 8:1 part by preparative high-performance liquid chromatography, Wherein the high performance liquid chromatography conditions are: ODS chromatographic column, the mobile phase is 80% methanol elution, the flow rate is 10ml / min, the detection wa...

Embodiment 3

[0180] Weigh 1 kg of Sapindus sapindus medicinal material, crush it and put it in a container, add 10 L of 50% methanol water, heat and reflux for extraction for 1 hour, filter, and concentrate the filtrate to obtain the extract extract;

[0181] Take 1.5kg of HPD-100 type macroporous resin, pre-treat and load the sample, sequentially elute with water, 25% ethanol solution, 50% ethanol solution, 75% ethanol solution, 95% ethanol solution, and collect 50%-75% ethanol The eluate was concentrated under reduced pressure to obtain total saponins;

[0182] Dissolve the total saponins in methanol, mix the sample with silica gel, conduct silica gel column chromatography, and use a dichloromethane-methanol system for gradient elution, and further separate the dichloromethane-methanol 8:1 part by preparative high-performance liquid chromatography, Wherein the high performance liquid chromatography conditions are: ODS chromatographic column, the mobile phase is 85% methanol elution, the ...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to application and a preparation method of a triterpenoid saponin compound. The compound is used for preparing a drugfor treating fungal infection and has the following chemical structure as shown in the description. The invention also provides the preparation method. Soapberries are systematically separated to screen two triterpenoid saponins. The compound is clear in anti-fungus mechanism and the anti-fungus action is obviously superior to that of other soapberry total saponins, soapberry saponin A, soapberrysaponin B and Clemontanoside C. The anti-fungus action of the compound is equivalent to that of market main current drugs at present and the action on capsular candida is obviously superior to that of market main current drugs. The compound has the advantages of clear mechanism, exact curative effect and easiness in industrial production, and is particularly suitable for drug resistance of the market main current drugs at present and infection induced by capsular candida.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application and preparation method of a triterpene saponin compound. Background technique [0002] Due to the wide application of various antibiotics and the development of organ transplantation and other technologies, the prevalence and mortality of fungal infections are on the rise worldwide. According to the different parts of the human body, fungal infectious diseases can be divided into superficial fungal infections, skin fungal infections, subcutaneous tissue fungal infections and systemic fungal infections. Among them, superficial fungal infection and skin fungal infection are collectively referred to as superficial fungal infection, and subcutaneous tissue fungal infection and systemic fungal infection are collectively referred to as invasive fungal infection. [0003] Superficial fungal infection is an infection caused by pathogenic fungi invading the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61P31/10A61P15/02A61P17/00C07J63/00
CPCA61K31/704C07J63/008
Inventor 苗得足胡清文焦启扬曹桂东于志波
Owner REYOUNG PHARMA
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