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A gynostemma flavonoid compound and its preparation and application in antitumor drugs

A technology of anti-tumor drugs and blue flavonoids, which is applied in the direction of anti-tumor drugs, preparation of sugar derivatives, drug combinations, etc., to achieve good anti-tumor effects

Active Publication Date: 2021-01-19
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on the active ingredients of Gynostemma pentaphyllum mostly focuses on terpenoids, saponins, polysaccharides and other components, and there are few studies on flavonoids. However, Gynostemma pentaphyllum is a natural health product with the same origin as medicine and food. The extraction and purification of flavonoids and the pharmacological The research on the activity and other aspects is of great value, and it needs to be further explored and comprehensively strengthen the bioutilization of Gynostemma pentaphyllum, which is of great significance for the development of new drugs and the guidance of clinical medication.

Method used

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  • A gynostemma flavonoid compound and its preparation and application in antitumor drugs
  • A gynostemma flavonoid compound and its preparation and application in antitumor drugs
  • A gynostemma flavonoid compound and its preparation and application in antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Extraction and separation of flavonoids kaempferol-3-O-[2'-trans-coumaroyl-3'-O-β-D-glucosyl-3'-O-β-D from Gynostemma pentaphyllum - Glucorutin:

[0048] (1) Dry the whole herb of Gynostemma pentaphylla (50°C), pulverize it (10 seconds each time, 3-5 times in a row), pass through a 20-mesh sieve to obtain Gynostemma pentaphylla coarse powder; weigh 5Kg Gynostemma pentaphyllum coarse powder, and extract in batches , 500g each time, heat reflux extraction with 75% ethanol aqueous solution, wherein the solid-to-liquid ratio is 1g:15mL, the reflux extraction temperature is 80°C, the reflux extraction time is 2h, and the reflux extraction times are 3 times; then the extracts are combined , the extract was centrifuged (4000r / min, 10min), and the supernatant was concentrated under reduced pressure at 0.095MPa to a paste (40°C) to obtain an ethanol extract;

[0049] (2) Dissolve the ethanol extract in distilled water, extract with petroleum ether (petroleum ether:dis...

Embodiment 2

[0056] Example 2 Determine the structure of kaempferol-3-O-[2'-trans-coumaroyl-3'-O-β-D-glucosyl-3'-O-β-D-glucorutin

[0057] Weigh 15 mg of Compound 1 (trace amount) prepared in Example 1 and dissolve it in a nuclear magnetic resonance tube with deuterated methanol. Using a Bruker DRX-400 nuclear magnetic resonance instrument, use tetramethylsilane (TMS) as an internal standard to measure its hydrogen Spectrum ( 1 H-NMR)( figure 1 ), fully decoupled carbon spectrum ( 13 C-NMR)( figure 2 ). figure 1 Kaempferol-3-O-[2'-trans-coumaroyl-3'-O-β-D-glucosyl-3'-O-β-D-glucorutin 1 H-NMR spectrum; figure 2 Kaempferol-3-O-[2'-trans-coumaroyl-3'-O-β-D-glucosyl-3'-O-β-D-glucorutin 13 C-NMR spectrum.

[0058] Compound 1 is a yellow pine needle-like crystal, developed by polyamide thin-layer chromatography (methanol: water volume ratio is 1:1), showing a single spot; it has yellow fluorescence under 365nm ultraviolet light; spraying 1% aluminum nitrate color developer, Yellow fluo...

Embodiment 3

[0068]Example 3 MTT method to detect the effect of kaempferol-3-O-[2'-trans-coumaroyl-3'-O-β-D-glucosyl-3'-O-β-D-glucorutin on human Normal hepatocytes (LO 2 ) Metabolic activity

[0069] Human normal hepatocytes (LO 2 ) to 1×10 5 Each / ml concentration was inoculated in 96-well cell culture plate (100 μL / well), and cultured in a 5% carbon dioxide incubator at 37°C. After the cells in the well plate were completely adhered to the wall, 100 μl of the flavonoid compound solutions prepared in Example 1 at different concentrations (25, 50, 100, 200, 400, 800 μg / mL) were added. At the same time, a positive control group was set up. The positive control sample was 5-fluorouracil (5-Fu), and the same 6 concentration gradients were set. A blank cell control group was also set up in the experiment, that is, only 100 μl of complete culture medium was added, and 6 parallels were set for each concentration. . at 37°C, 5% CO 2 Continue culturing in the incubator, take it out after 24 ...

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Abstract

The invention belongs to the field of the traditional Chinese medicine and discloses a gynostemma pentaphylla flavonoid compound, a preparation and an application thereof in an antitumor drug. The method comprises the following steps: (1) extracting the rough gynostemma pentaphylla powder by adopting an alcohol solution for heating and refluxing, centrifuging and concentrating, thereby acquiring gynostemma pentaphylla ethyl alcohol extract; (2) using water for dissolving the extract, filtering, adopting petroleum ether for extracting the filtrate and adopting ethyl acetate for extracting lower-layer water phase; (3) performing vacuum concentration on the ethyl acetate phase, drying and adopting a chloroform-methyl alcohol mixed solvent for isocratic elution in a silica gel column, therebyacquiring multiple fractions; (4) pouring the fractions onto a gel column, eluting with methyl alcohol and collecting the fractions with equal analogous values; (5) pouring the fractions onto a ODS column, using methyl alcohol-water for isocratic elution, collecting the fractions and drying, thereby acquiring the gynostemma pentaphylla flavonoid compound. The gynostemma pentaphylla flavonoid compound prepared according to the invention has the advantages of high anti-tumor activity, low dosage and no toxic or side effect to normal human hepatic cells in same dosage.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicines, and in particular relates to a gynostemma flavonoid compound, a preparation method thereof and an application in antitumor drugs. Background technique [0002] Tumor mortality ranks first or second in the world, which is a great threat to human survival and health. Tumor treatment has always been a difficult problem in the medical field, surgery, chemotherapy and radiotherapy are the usual treatment methods. However, most of the existing treatment methods have serious side effects, such as bleeding, cognitive impairment, multiple, etc., which are mainly related to their non-selective cytotoxicity. For chemotherapy, resistance to emerging drugs is another serious problem. Finding new anticancer drugs with less toxic side effects and selective killing has always been one of the main research goals of scientists all over the world. Natural products, including plants, marine organisms ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/07C07H1/08A61P35/00
CPCC07H1/08C07H17/07
Inventor 姜建国申春燕周思思
Owner SOUTH CHINA UNIV OF TECH
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