Preparation method and application of lysimachia capillipes saponin A

A technology of thin-stemmed vanilla saponin, which is applied in the preparation of thin-stemmed vanilla saponin A and the application field in the preparation of anti-tumor drugs, which can solve the problems of low bioavailability and difficulty in the development of new drugs with monomer components, and achieve strong operability , good prospects for the development and application of anti-tumor drugs, and the effect of reducing purification costs

Inactive Publication Date: 2015-11-11
SUZHOU QIUSHI HERBAL HEALTH TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Further studies have shown that saponins B and C have low oral bioavailability and have certain hemolytic properties, so it is difficult to develop new drugs for their monomeric components [ChengZ. .]

Method used

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  • Preparation method and application of lysimachia capillipes saponin A
  • Preparation method and application of lysimachia capillipes saponin A
  • Preparation method and application of lysimachia capillipes saponin A

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: the preparation of fine stem vanilloid A

[0019] Preparation of total vanilla saponins: reference method [Ying Hongmei. Research on the preparation process and quality standard of total vanilla saponins. Master's degree thesis of Zhejiang University, 2011.]. Take 6 kg of fine-stemmed vanilla, extract twice with 70% ethanol under reflux, concentrate the extract, pass it through AB-8 macroporous resin, elute with water, 40% and 70% ethanol in sequence, collect the 70% ethanol eluate, concentrate, and dry , Obtain 240 g of total vanilla saponins (CP-TS). According to HPLC analysis, the contents of saponin B and C are 23% and 21% respectively.

[0020] Alkaline hydrolysis reaction: Weigh 0.5g of CP-TS, add 10mL of 0.07M NaOH, react at 50°C for 48h, neutralize with 1M HCl to pH6-7, load the liquid on a normal-pressure reversed-phase silica gel column, and elute with 60% methanol. Saponin A (170 mg) was obtained; by liquid phase analysis, its purity was 99.2%...

Embodiment 2

[0023] Embodiment 2: the alkaline hydrolysis process investigation of fine stem vanilloid A

[0024] Vanilloid saponins B and C can be efficiently converted into the target product saponin A under controlled mild alkali hydrolysis conditions. Under the influence of relatively intense reaction temperature, alkali concentration, and hydrolysis time, aglycon hemiacetal ring destruction, Side reactions such as glycosyl base hydrolysis. This experiment adopts embodiment 1 alkali hydrolysis raw material and reaction method, through the change of technological parameter, investigates the suitable range of reaction technological parameter.

[0025] (1) Investigation of hydrolysis temperature: Weigh 0.5g of CP-TS, add 10mL of 0.07M NaOH, react at 35, 50, 65 and 80°C for 48h, neutralize with 1M HCl to pH6-7, take samples for HPLC detection. The results are shown in Table 1.

[0026] The influence of table 1 reaction temperature on the content of vanilloid saponin A

[0027]

[002...

Embodiment 3

[0041] Embodiment 3: the preparation of fine stem vanilloid A

[0042] Weigh 10g of CP-TS in Example 1, add 10mL of 0.07M NaOH, react at 50°C for 48h, neutralize with 1M HCl to pH 6-7, load the liquid on the AB-8 macroporous resin column, successively water, 40% and 75% Eluted with ethanol, collected 75% ethanol eluate, concentrated and dried to obtain saponin A (3.5 g); by liquid phase analysis, its purity was 92.4% based on relative peak area.

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Abstract

The invention discloses a preparation method of lysimachia capillipes saponin A. The preparation method mainly comprises the following steps: selecting a lysimachia capillipes plant raw material, extracting the lysimachia capillipes plant raw material by adopting a water or ethanol-water mixed solvent, further purifying by adopting filler such as macroporous resin to obtain a total saponin extract rich in saponin B and C, dissolving the total saponin extract in an appropriate amount of alkaline solution, reacting at 40 to 80 DEG C, neutralizing by utilizing appropriate amount of acid, and further purifying the obtained hydrolysate by adopting filler such as macroporous resin, silica gel, reverse phase silica gel and the like, to obtain a lysimachia capillipes sapoonin A extract with content more than 90 percent. The invention also discloses an application of the lysimachia capillipes saponin A. The compound of the lysimachia capillipes saponin A has a remarkable inhibition effect on 11 human tumor cell lines such as A549 non-small cell lung cancer cells, SMMC-7721 human liver cancer cells, PC3 human prostate cancer cells and the like, has a broad-spectrum anti-cancer effect, and can be used as a drug or a medicine composition to treat malignant tumors.

Description

technical field [0001] The invention relates to a method for preparing vanilloid saponin A, and also relates to the application of vanilloid saponin A in the preparation of antitumor drugs, which belongs to the field of biomedicine. technical background [0002] Malignant tumor is a serious disease that seriously threatens human health. It is an effective method to find effective antitumor drugs and their leads from natural products. Lycimachia Capillipes Hemsl, also known as Manshanxiang, Paicao, Xiangpaicao, etc., is sweet in nature, flat in taste, and the whole herb is used as medicine. Exogenous wind-heat, fever, headache, sore throat, body pain. Literature research shows that total vanilloid saponins have a good anti-tumor effect, wherein vanilloid B and C are the main active ingredients, and the total content of the two in the total saponins is about 60% [Ying Hongmei et al., determined by HPLC-ELSD The content of saponin B and saponin C in saponins C, Chinese Journa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61P35/00A61P35/02
CPCC07J71/0005
Inventor 刘江云田景奎张琳李守信于秀颖
Owner SUZHOU QIUSHI HERBAL HEALTH TECH CO LTD
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