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New triterpenoid saponin compounds as well as preparation method and application thereof

A technology for triterpenoid saponins and compounds, applied in the field of new triterpenoid saponins and their preparation, can solve the problem of being difficult to completely remove biofilms and the like

Inactive Publication Date: 2018-05-11
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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  • New triterpenoid saponin compounds as well as preparation method and application thereof
  • New triterpenoid saponin compounds as well as preparation method and application thereof
  • New triterpenoid saponin compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0198] 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;

[0199] 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;

[0200] 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 HPLC conditions are: ODS chromatographic column, the mobile phase is 75% methanol elution, the flow rate is 10ml / min, the det...

Embodiment 2

[0202] 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;

[0203]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;

[0204] 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 condition is: ODS chromatographic column, mobile phase is 80% methanol elution, flow rate 10ml / min, detection wavelength is 205nm,...

Embodiment 3

[0206] 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;

[0207] Take 1.5kg of HPD-100 type macroporous resin, carry out pretreatment and load the sample, and then carry out elution with water, 50% ethanol solution, 75% ethanol solution, 95% ethanol solution, collect 50%~75% ethanol eluate, reduce Press and concentrate to obtain total saponins;

[0208] 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 condition is: ODS chromatographic column, mobile phase is 85% methanol elution, flow rate 10ml / min, detection...

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Abstract

The invention belongs to the technical field of drugs, and particularly relates to new triterpenoid saponin compounds as well as a preparation method and an application thereof. The compounds are soapnut saponin W, soapnut saponin S, soapnut saponin T, soapnut saponin U and soapnut saponin V, and chemical structures of the compounds are shown in the description. The preparation method of the compounds are further provided for systematic separation of sapindus, the five triterpenoid saponins are screened out, the antifungal effect is remarkably better than that of total soapnut saponin, soapnutsaponin A and soapnut saponin B, and the compounds are comparable to mainstream drugs in the current market, have better effect on coated candida than the mainstream drugs in the current market, havethe advantages of being clear in mechanism and exact in curative effect and facilitating industrial production, and are particularly suitable for treating drug resistance to the mainstream drugs in the current market and infection caused by coated candida.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a new triterpene saponin compound and its preparation method and application. 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...

Claims

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Application Information

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IPC IPC(8): C07J63/00C07H15/256C07H1/08A61K31/704A61P31/10
CPCC07H1/08C07H15/256C07J63/008
Inventor 苗得足胡清文焦启扬于志波
Owner REYOUNG PHARMA
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