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Preparation of beta cardiac glycoside and anti-angiogenesis application thereof

An anti-angiogenesis and cardiac glycoside technology, applied in the field of natural medicinal chemistry, can solve the problems of hypoxia and acidosis, and achieve the effects of low toxicity, low cost, and simple and convenient operation.

Active Publication Date: 2021-08-17
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are adverse reactions such as local severe hypoxia and acidosis

Method used

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  • Preparation of beta cardiac glycoside and anti-angiogenesis application thereof
  • Preparation of beta cardiac glycoside and anti-angiogenesis application thereof
  • Preparation of beta cardiac glycoside and anti-angiogenesis application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of embodiment 1 iron chopsticks n-butanol extract

[0036] The rhizome part of the iron chopsticks collected was air-dried naturally and weighed to obtain 7.5kg. Crush until particle size diameter is less than 3mm, soak 4 times with 95% ethanol, each time 15L, each time 7 days. All soaking liquids are removed solvent with rotary evaporator, obtain concentrated solution 4L; Add 12L ethyl acetate to extract in concentrated solution, extract 4 times, collect the organic phase (ethyl acetate phase) after extraction; Add n-butanol to the mixture, extract four times, obtain the n-butanol phase similarly, and discard the water phase. The n-butanol extract was concentrated under reduced pressure with a rotary evaporator to constant weight to obtain a brownish-red slurry as a crude extract (650 g).

Embodiment 2

[0037] The preparation of embodiment 2 beta cardiac glycosides

[0038] The n-butanol phase of the iron chopsticks is concentrated to 500mL, presenting a dark brown-red viscous liquid, which is chromatographed on a D101 macroporous resin column, eluted with gradients of water, 30%, 50%, and 95% ethanol, and finally distilled and concentrated to obtain Four fractions. 30% of n-butanol was partially concentrated under reduced pressure to obtain a brown-black viscous substance (212g), which was loaded by wet method and packed into a column (200-300 mesh silica gel column) by wet method, using a gradient of dichloromethane-methanol-water eluent Five fractions (Fr.1-Fr.5) were eluted. Fr.4 was firstly subjected to normal-phase silica gel column chromatography and gradient elution with dichloromethane:methanol (15:1, 8:1, 5:1, 2:1) to obtain five components Fr.4.1-Fr. 4.5. Continue to separate Fr.4.4 on a reverse-phase chromatographic column by gradient elution of methanol-water ...

Embodiment 3

[0041] Example 3 Beta-cardiac glycoside compound anti-angiogenic activity

[0042] Firstly, human umbilical vein endothelial cells were treated with drugs for 24 hours, then the supernatant was sucked off, and 100 uL of 10% TCA was slowly added to fix the cells, left to stand for 5 minutes, and then placed in a refrigerator at 4°C for 1 hour; Rinse with deionized water 5 times and dry in the air; add 50uL SRB buffer solution into a 96-well plate and place on a shaker for 10min to mix well. Measure its absorbance at 540nm with a microplate reader, and calculate the OD value.

[0043] Experimental results show that the compound has no obvious effect on human normal human umbilical vein endothelial cells (HUVEC), but has obvious inhibitory effect on human umbilical vein endothelial cells induced by VEGF.

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Abstract

The invention discloses a beta cardiac glycoside and a preparation method and application thereof. The structure of the beta cardiac glycoside is as follows: the compound is extracted from Helleborus thibetanus (Ranunculaceae): dry powder at the rhizome part of the Helleborus thibetanus is soaked with 95% ethanol, and then is concentrated under reduced pressure to obtain a concentrated solution; the concentrated solution is respectively extracted by using ethyl acetate and n-butyl alcohol which are equal in volume; column chromatography separation is peformed on an n-butanol extraction phase by adopting a D101 macroporous resin column, a normal-phase silica gel column, a reverse-phase ODS (Octadecylsilyl), a gel column and the like, and finally purifying is performed by adopting semi-preparative high performance liquid chromatography. The beta cardiac glycoside has a good inhibition effect on angiogenesis of human umbilical vein endothelial cells (HUVEC) so that the beta cardiac glycoside can be prepared into a novel anti-angiogenesis medicine. The invention provides a material basis for novel anti-vascular drugs, and is beneficial to further development of medicinal value and clinical application of helleborus thibetanus.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and relates to a preparation method of a compound isolated from iron chopsticks and its application in the preparation of anti-angiogenesis drugs. Background technique [0002] According to statistics: Malignant tumors rank No. 1 among the causes of death of urban residents in my country. Studies have found that both tumor growth and metastasis are dependent on blood vessels, and proposed that anti-angiogenic therapy has become a new field. At present, anti-angiogenic drug therapy has become one of the important methods for the treatment of brain metastases from lung cancer. On the basis of traditional therapeutic intervention, actively exploring the combined application of anti-angiogenic drug therapy has become one of the important research directions. Current anti-angiogenic drugs for the treatment of cancer include monoclonal antibodies, endogenous angiogenesis inhibitors, and vasc...

Claims

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Application Information

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IPC IPC(8): C07J17/00A61K36/71A61P35/00
CPCC07J17/00A61K36/71A61P35/00Y02A50/30
Inventor 杨凤英解姗段文奇孟宁孙雅洁于颖
Owner UNIV OF JINAN
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