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Extraction method and application of anticancer active monomer in Curcuma zedoaria

A technology of anti-cancer activity and extraction method, which is applied in the direction of organic active ingredients, medical preparations containing active ingredients, anti-tumor drugs, etc., and can solve the difficulties in ensuring the effectiveness of clinical medication, safety and sustainability, and lack of effective substances Basic and pharmacodynamic research, complex volatile oil components of zedoary, etc., to achieve good separation, high batch-to-batch consistency, and good biological activity

Active Publication Date: 2016-05-25
TIANJIN YAOYU BIOLOGICAL TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the application of traditional Chinese medicine Curcuma is mainly based on its volatile oil injection and compound Curcuma oil for anti-cancer effect, which is relatively limited.
In addition, the components of zedoary volatile oil are complex, and the anticancer effects of different components are also very different. The lack of necessary material basis and efficacy research, and the lack of reasonable quality control standards make it difficult to ensure the effectiveness, safety and reliability of clinical medication. Persistent

Method used

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  • Extraction method and application of anticancer active monomer in Curcuma zedoaria
  • Extraction method and application of anticancer active monomer in Curcuma zedoaria
  • Extraction method and application of anticancer active monomer in Curcuma zedoaria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]Use curcuma as raw material, grind it into powder, weigh 4kg, dissolve it in 25L of 98% ethanol solution, and carry out reflux extraction, and finally obtain the filtrate by rotary evaporation to dryness, and then dissolve it in n-hexane-ethanol with a volume fraction of n-hexane of 70%. In a binary mixed solvent, prepare an extract with a concentration of 100 mg / mL, pass through a 0.45 μm microporous membrane, and prepare by one-dimensional liquid chromatography.

[0044] One-dimensional liquid chromatography adopts Silica150×250mm, 10μm, The mobile phase adopts the mixture of organic phases, wherein the organic phase A phase is n-hexane, B phase is ethanol, gradient elution mode: B phase concentration 0-50% gradient elution for 30 minutes. Adopt the ultraviolet detector 210nm to select the absorption wavelength, the preparation temperature is room temperature, the injection volume is 100mL / needle, the mobile phase flow rate is 600mL / min, collect the component of 15.5-...

Embodiment 2

[0048] The purpose component that embodiment 1 obtains utilizes analytical chromatographic column to carry out purity test, as image 3 As shown, the purity reaches 99.0%, and it is a monomeric compound. The chromatographic column selects the normal phase silica gel chromatographic column Silica4.6×250mm, 10μm,

[0049] The target components were subjected to NMR analysis (BrukerA.GAVIII600PLUS, Hanmeng Biotechnology (Tianjin) Co., Ltd.), and the NMR spectra were as follows: Figure 4 , 5 As shown, the NMR data of the monomer compound obtained according to 1HNMR and 13CNMR spectrograms are shown in Table 1.

[0050] Table 1: 1HNMR (600MHz) and 13CNMR (600MHz) (CDCl 3 ,TMS,ppm)

[0051] Carbon number

δC

δH(JinHz)

1

134.05

4.90(d,10.4)

2

27.30

1.95(m)2.26(m)

3

36.13

1.71(m)2.05(m)

4

47.91

2,47(m)

5

209.27

6

40.26

3.30(d,15.2),3.58(d15.2)

7

154.45

...

Embodiment 3

[0056] Use curcuma as raw material, grind it into powder, weigh 4kg, dissolve it in 25L of 98% ethanol solution, and carry out reflux extraction, and finally obtain the filtrate by rotary evaporation to dryness, and then dissolve it in n-hexane-ethanol with a volume fraction of n-hexane of 70%. In a binary mixed solvent, prepare an extract with a concentration of 100 mg / mL, pass through a 0.45 μm microporous membrane, and prepare by one-dimensional liquid chromatography.

[0057] One-dimensional liquid chromatography adopts Silica150×250mm, 10μm, The mobile phase is a mixture of organic phases, wherein the organic phase A is n-hexane, B is ethanol, and the gradient elution method: B phase concentration 0-50% gradient elution for 30 minutes. The absorption wavelength was selected by an ultraviolet detector at 210nm, the preparation temperature was room temperature, the injection volume was 150mL / needle, the flow rate of the mobile phase was 660mL / min, the components were colle...

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Abstract

The invention provides an extraction method of an anticancer active monomer in Curcuma zedoaria. The method includes: taking Curcuma zedoaria tuber as the raw material, grinding the Curcuma zedoaria tuber into powder, then conducting ethanol extraction, concentrating the filtrate, then dissolving the product in a n-hexane-ethanol mixed solvent; conducting one-dimensional liquid chromatography separation: employing a normal phase silica gel chromatographic column, adopting a binary mobile phase with n-hexane as the phase A and ethanol as the phase B, carrying out elution with the phase B at a concentration of 0-50%, and collecting the 15.5-17min eluent; performing dissolving with the n-hexane-ethanol mixed solvent; conducting two-dimensional liquid chromatography separation: employing an Acchrom X-Amide chromatographic column, adopting a binary mobile phase with n-hexane as the phase A and ethanol as the phase B, carrying out elution with the phase B at a concentration of 0-30%, and collecting the 17-18min eluent so as to obtain a target product. The invention provides a new compound never reported before, the process has the characteristics of simplicity, low cost, large preparation capacity and good repeatability, and the obtained monomer compound has high purity, good biological activity and anticancer drug development potential.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical products, in particular to a method for extracting anticancer active monomers from curcuma tuber, a traditional Chinese medicine, and the application of the extracted anticancer active monomers in the preparation of anti-liver cancer and anti-lung cancer drugs. Background technique [0002] The traditional Chinese medicine Zedoary is the rhizome of the turmeric plant in the ginger family. Zedoary has the effects of promoting qi, breaking blood, eliminating stagnation and relieving pain. Modern pharmacological studies have shown that zedoary volatile oil has anti-tumor and antibacterial effects; curcumol has anti-tumor effects and anti-early pregnancy effects. In addition, curcuma has significant effects on cardiovascular, gastrointestinal smooth muscle, and acute renal failure, and also has hepatoprotective effect. [0003] At present, the application of traditional Chinese medicine Curcum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/93A61K31/365A61P35/00
CPCC07D307/93
Inventor 张耀洲韩朝陆洪李上文庞莉王欢欢马红杨珊珊盖其静杜思邈
Owner TIANJIN YAOYU BIOLOGICAL TECH
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