Preparation and anti-liver cancer application of 5alpha-structured type B cardiac glycoside

A cardiac glycoside and type B technology, applied in the field of natural medicinal chemistry, can solve the problems of poor prognosis, multi-drug resistance, and low immunity of the body, and achieve good anti-liver cancer activity, simple and convenient operation, and low cost Effect

Pending Publication Date: 2021-07-09
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As one of the malignant tumors with high morbidity and mortality, there are problems such as high postoperative recurrence rate, easy metastasis of cancer cells, multidrug resistance, low immunity, and poor prognosis after treatment; there is currently no effective treatment Therefore, it is urgent to find new anti-liver cancer drugs that are safe, highly effective and low-toxic

Method used

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  • Preparation and anti-liver cancer application of 5alpha-structured type B cardiac glycoside
  • Preparation and anti-liver cancer application of 5alpha-structured type B cardiac glycoside
  • Preparation and anti-liver cancer application of 5alpha-structured type B cardiac glycoside

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of iron chopstick n-butanol extract

[0036] The collected iron chopsticks is naturally ventilated, weighted 7.5 kg. The crushing to a particle size diameter of less than 3 mm, soaked 4 times with 95% ethanol, 15 L each time, 7 days each time. The solvent was removed by a rotary evaporator to obtain a concentrated liquid 4L; EtOAc EtOAc (EtOAc) EtOAc (EtOAc) N-butanol was added, extracted four times, and the n-butanol phase was obtained, and the water phase was discarded. The n-butan alcohol extract was concentrated under reduced pressure with a rotary evaporator to give a brown red slurry as a bold product (650 g).

Embodiment 2

[0037] Example 2 Preparation of Strong Catosin

[0038] The iron chopsticks were concentrated to 500 mL, showing a deep brown brown-brown-brown viscous liquid, using D101 macroporous resin column chromatography, water, 30%, 50%, 95% ethanol gradient, and finally distilled concentrate Four fractions. The n-butanol 50% (65.8 g) was eluted with EtOAc Ethanol: Water (35%, 50%, 60%, 80%) gradient elution, four components FR.1-fr. 4. FR.1 first elution with n-phase silica gel chromatography eluting with dichloromethane: methanol (15: 1, 8: 1, 5: 1, and 2: 1) gradient, five components FR.1.1-fr. 1.5. FR.1.2 (800 mg) was eluted with methanol-washing release gradient in the reversed chromatography column, and five components were obtained by FR.1.2.1-Fr.1.2.5. FR.1.2.3 is first in the gel column (dichloromethane: methanol = 1: 1), silica gel column (dichloromethane: methanol = 13: 1, 8: 1, 5: 1) further repeatedly purified, and finally The preparative high performance liquid phase (the chr...

Embodiment 3

[0041] Example 3 Strong Chanosine compound anti-liver cancer activity

[0042] Hepatocellular HepG2, rat liver star cells HSC-T6 were added at 37 ° C at 37 ° C in RPMI-1640 medium added 2.05 mm / l glutamine and 10% FBS, at 5% CO 2 Culture in humidification environments. Cells were isolated from the culture flask from the culture flask using trypsin EDTA. Dilute to 5 × 10 with a complete medium 4 After / ml, 100 μl of the cell suspension was added to each of the 96-well cultural sheets. It was then cultured in a 5% carbon dioxide environment at 37 ° C. The test compound of the specified concentration was added to each well and then cultured for 48 h. Dooricin as a positive control. The attached cells were fixed with cold 50% trichloroacetic acid for 30 min and then stained with 0.04% SrB for 30 min. After dissolving the bound SRB in a Tris medium of 10 mM, the absorbance at 450 nm was measured with a TECAN multifunctionramid instrument.

[0043] Anti-liver cancer activity such as ...

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Abstract

The invention discloses a 5alpha-structured type B cardiac glycoside, which has the following structure shown in the specification. The compound is extracted from Helleborus thibetanus (Ranunculaceae) through following steps: soaking dry powder at the rhizome part of Helleborus thibetanus with 95% ethanol, and then, carrying out vacuum concentration to obtain a concentrated solution; respectively extracting the concentrated solution by using ethyl acetate and n-butyl alcohol which are equal in volume; performing column chromatography separation on an n-butanol extract phase by adopting a D101 macroporous resin column, a normal-phase silica gel column, reverse-phase ODS, a gel column and the like, and finally purifying by adopting semi-preparative high performance liquid chromatography. The type B cardiac glycoside has a good inhibition effect on human hepatoma cells (HepG2) and rat hepatic stellate cells (HSC-T6), so that the cardiac glycoside B can be prepared into a novel anti-hepatoma drug. The invention provides a material basis for novel anti-hepatoma drugs, and is beneficial to further development of medicinal value and clinical application of helleborus thibetanus.

Description

Technical field [0001] The present invention relates to the field of natural drug chemistry, and the compounds of the extracted extracted from iron chopsticks and the preparation methods thereof and the application of anti-liver cancer drugs are prepared. Background technique [0002] According to WHO statistics, patients with liver cancer account for 8.2% of global cancer death. In recent years, the incidence and mortality rate of liver cancer have increased year by year, and liver cancer has become one of the major diseases that hinder social development. Therefore, the prevention and treatment of liver cancer has become one of the world's research hotspots. As one of the malignant tumors of high morbidity and high mortality, there is a problem of high postoperative recurrence rate, cancer cell easy transfer, multidrug resistance, body immunity, and poor treatment prognosis; current lack of effective treatment Means, therefore is urgent to find new anti-liver cancer drugs for s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J19/00A61P35/00
CPCC07J19/005A61P35/00
Inventor 杨凤英解姗段文奇葛迪刘娜孙雅洁于颖
Owner UNIV OF JINAN
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