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Extraction method and application of anticancer active monomer in curcuma

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: 2017-12-19
TIANJIN YAOYU BIOLOGICAL TECH
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  • Summary
  • 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
  • Extraction method and application of anticancer active monomer in curcuma
  • Extraction method and application of anticancer active monomer in curcuma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0044] One-dimensional liquid chromatography using Silica 150 × 250mm, 10μm, The mobile phase adopts the mixing of organic phases, wherein the organic phase A is n-hexane, the B phase is ethanol, and the gradient elution mode: the B phase concentration is 0-50% gradient elution for 30 minutes. The absorption wavelength was selected at 210 nm by an ultraviolet detector, the preparation temperature was room temperature, the injection volume was 100 mL / needle, the mobile phase fl...

Embodiment 2

[0048] The purpose component obtained in Example 1 is tested for purity using an analytical chromatographic column, such as image 3 As shown, the purity reached 99.0%, and it was a monomer compound. The chromatographic column is a normal phase silica gel column Silica 4.6×250mm, 10μm,

[0049] The target components were analyzed by nuclear magnetic resonance (Bruker A.G AVIII600PLUS, Hanmeng Biotechnology (Tianjin) Co., Ltd.), and the nuclear magnetic spectrum was as follows Figure 4 , 5 As shown, the NMR data of the monomer compound obtained from 1H NMR and 13C NMR spectra are shown in Table 1.

[0050] Table 1: 1H NMR (600MHz) and 13C NMR (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

8

106.75

...

Embodiment 3

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

[0057] One-dimensional liquid chromatography using Silica 150 × 250mm, 10μm, The mobile phase adopts the mixing of organic phases, wherein the organic phase A is n-hexane, the B phase is ethanol, and the gradient elution mode is: the B phase concentration is 0-50% gradient elution for 30 minutes. The absorption wavelength was selected at 210 nm by an ultraviolet detector, the preparation temperature was room temperature, the sample injection volume was 150 mL / needle, and the ...

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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 the tuber of the traditional Chinese medicine Curcuma radix, and the application of the extracted anticancer active monomers in the preparation of anti-liver cancer and anti-lung cancer drugs. Background technique [0002] Curcuma curcuma, a traditional Chinese medicine, is the rhizome of the ginger family, turmeric. Modern pharmacological studies have shown that the volatile oil of Curcuma curcuma has anti-tumor and antibacterial effects; Curcuma has anti-tumor effects and anti-early pregnancy effects. In addition, Curcuma curcuma has a significant effect on cardiovascular, gastrointestinal smooth muscle, acute renal failure, and also has a liver-protecting effect. [0003] At present, the application of traditional Chinese medicine Curcuma radix is ​​mainly used for its volatile oil injection and compound ...

Claims

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Application Information

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Patent Type & Authority Patents(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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