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Preparation of anti-breast cancer type B cardiac glycoside and anti-liver cancer application of anti-breast cancer type B cardiac glycoside

An anti-breast cancer and cardiac glycoside technology, applied in the field of natural medicinal chemistry, can solve the problems of easy metastasis of cancer cells and high postoperative recurrence rate, and achieve the effect of simple and convenient operation, low toxicity and good anti-breast cancer activity

Active Publication Date: 2021-09-28
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are mainly surgical treatment, radiotherapy and other treatment methods, but there are problems such as high recurrence rate after surgery, easy metastasis of cancer cells, etc. Therefore, it is urgent to find new anti-breast cancer drugs that are safe, efficient and low-toxic

Method used

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  • Preparation of anti-breast cancer type B cardiac glycoside and anti-liver cancer application of anti-breast cancer type B cardiac glycoside
  • Preparation of anti-breast cancer type B cardiac glycoside and anti-liver cancer application of anti-breast cancer type B cardiac glycoside
  • Preparation of anti-breast cancer type B cardiac glycoside and anti-liver cancer application of anti-breast cancer type B cardiac glycoside

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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, 15L each time, 7 days each time. 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. N-butanol 50% part (65.8g) crosses MCI reverse-phase column chromatography, with ethanol: water (35%, 50%, 60%,

[0039] 80%) gradient elution to obtain four components Fr.1-Fr.4. Fr.2 was first separated with a normal-phase silica gel column and eluted with dichloromethane:methanol (20:1, 10:1, 8:1, 5:1, 2:1) gradient to obtain six components Fr. 2.1-Fr. 2.6. A large number of crystals were precipitated from Fr.2.2. After the crystals were filtered out, they were washed repeatedly with methanol. The washed sample was subjected to semi-preparative high performance liquid chromatography (65% methanol water, 3 m...

Embodiment 3

[0042] Example 3 Beta-cardiac glycoside compound anti-breast cancer activity

[0043] After adding different concentrations of compounds to MDA-MB-231 cells and culturing them for 48 hours, the supernatant was aspirated, and 100 μL of 10% TCA solution was added gently to fix at 4°C for 1 hour. The fixative was removed, washed 5 times with deionized water, and dried at room temperature. Then add 50 μL SRB solution, shake at room temperature for 5 min, wash 5 times with 1% acetic acid, and dry. Bound SRB was dissolved in 10 mM Tris medium with doxorubicin as a positive control. The absorbance OD value at 540 nm was measured with a Tecan multifunctional microplate reader.

[0044] Anti-breast cancer activity of beta-cardiac glycosides as Figure 4 shown.

[0045] The experimental results showed that the compound showed a concentration-dependent inhibitory effect on MDA-MB-231 cells, and the inhibitory effect was significant, IC 50 2.38×10 - 7 μM.

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Abstract

The invention discloses anti-breast cancer type B cardiac glycoside. The structure of the anti-breast cancer type B cardiac glycoside is shown in the specification. The compound is extracted from Helleborus thibetanus. Dry powder of roots and stems of helleborus thibetanus are soaked with 95% ethanol, and concentrated under reduced pressure to obtain concentrate; the concentrated solution is respectively extracted by using ethyl acetate and n-butyl alcohol which are equal in volume; column chromatography separation is performed on an n-butanol extraction phase through a D101 macroporous resin column, a normal-phase silica gel column, reverse-phase ODS, a gel column and the like in sequence, and purifying is performed through semi-preparative high performance liquid chromatography to obtain a monomeric compound. The type B cardiac glycoside has a good inhibition effect on human breast cancer cells (MDA-MB-231), so that the type B cardiac glycoside can be prepared into a novel anti-breast cancer drug. A material basis is provided for novel anti-breast cancer drugs, and effective scientific data is provided for developing the medicinal value and related clinical application of helleborus thibetanus.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and relates to a compound separated and extracted from iron chopsticks, a preparation method thereof and an application in the preparation of anti-breast cancer drugs. Background technique [0002] Breast cancer is one of the most common malignant tumors in women. According to statistics, the incidence rate accounts for 7-10% of various malignant tumors in the whole body. The etiology of breast cancer is not yet fully understood, and the prevention and treatment of breast cancer has become one of the global research hotspots. At present, there are mainly surgical treatment, radiotherapy and other treatment methods, but there are problems such as high recurrence rate after operation, easy metastasis of cancer cells, etc. Therefore, it is urgent to find new anti-breast cancer drugs that are safe, efficient and low-toxic. Cardiac glycosides are commonly used drugs for the treatment of hea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00
CPCC07J17/005A61K36/71A61P35/00
Inventor 杨凤英解姗段文奇葛迪刘娜孙雅洁
Owner UNIV OF JINAN
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