Use of cardiac glycoside compound

A compound, cardiac glycoside technology, applied in the field of cardiac glycoside compounds, to achieve high efficiency, significant anti-tumor activity, and good quality of the extract

Active Publication Date: 2015-02-04
TROPICAL CORP STRAIN RESOURCE INST CHINESE ACAD OF TROPICAL AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is still unknown whether the cardiac glycoside compo

Method used

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  • Use of cardiac glycoside compound

Examples

Experimental program
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Effect test

Embodiment 1

[0026] A. After 25.4 kg of calotropis gigantea stems are naturally air-dried and pulverized, by the calotropis gigantea sample: the mass / volume ratio (kg / L) of ethanol aqueous solution is about 1:2, with 50L volume fraction of ethanol aqueous solution of 95% Fully mixed with 25.4kg of horn melon samples, sealed, leached at room temperature for 3 times, each time for 7 days, filtered and combined the extracts, concentrated under reduced pressure until there was no alcohol smell to obtain the ethanol extract;

[0027] B. At room temperature, disperse the ethanol extract in water to make a suspension, according to the volume ratio of ethanol extract: petroleum ether = 1:3, 1:2, 1:1, repeat the ethanol extract with petroleum ether After extracting 3 times, and concentrating under reduced pressure to recover petroleum ether, petroleum ether extract (254.1 g) was obtained;

[0028] C. Filter the water liquid after petroleum ether extraction, separate the filtrate by D-101 macroporou...

Embodiment 2

[0033] After column chromatography, Fr.4-1 (3.2 g) in step E in Example 1 was eluted with an eluent with a volume ratio of chloroform:methanol=25:1, and the same components were collected by TLC thin layer chromatography , to obtain 7 parts Fr.4-1-1~Fr.4-1-7; Fr.4-1-4 (869.5mg) was subjected to silica gel column chromatography, followed by chloroform:methanol=40:1, chloroform : Acetone=6:2 volume ratio of the eluent for elution to finally obtain the cardiac glycoside compound calotropin (109.9mg). The study found that the structural difference between this compound and the target compound of the present invention is that there is no hydroxyl group on the 12-position carbon, while the 12-position carbon of the target compound of the present invention is substituted by a hydroxyl group. In the further in vitro anti-tumor activity test, it was found that the anti-IC50 values ​​of the two compounds were significantly different (see Table 2).

Embodiment 3

[0035] Structural identification of cardiac glycoside compound 12β-hydroxycalotropin:

[0036]The structure of the cardiac glycoside compound 12β-hydroxycalotropin in Example 1 was identified by spectroscopic techniques, including ultraviolet, infrared, nuclear magnetic resonance and high-resolution mass spectrometry. The detection of the cardiac glycoside compound 12β-hydroxycalotropin for the first time in the stem of the horn squash by using 2D-NMR technology 13 C-NMR, 1 The H-NMR data were assigned (see Table 1 below).

[0037] The following are the physical and chemical constants of the cardiac glycoside compound 12β-hydroxycalotropin:

[0038] 12β-hydroxycalotropin: C 29 h 40 o 10 , White amorphous powder (methanol), 10% sulfuric acid ethanol solution is brown. m.p.214-216℃; [α]D+6.4°(c=0.045, MeOH); HR-ESI-MS: m / z[M+Na] + 583.2318 (calcd. For C 29 h 40 o 10 Cl, 583.2310); IRλ max (cm -1 ):3433cm -1 ,2957cm -1 ,2923cm -1 ,2852cm -1 ,1712cm -1 ,1655cm -1...

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Abstract

The invention discloses the use of cardiac glycoside compound 12 beta-hydroxycalotropin in preparing medicines having tumor treating and preventing effects. The cardiac glycoside compound 12 beta-hydroxycalotropin has remarkable anti-tumor activity and is capable of serving as a lead compound for treating tumors; meanwhile, a method for extracting and separating the cardiac glycoside compound 12 beta-hydroxycalotropin provided by the invention is simple, feasible, low in cost, and high in efficiency and yield; the extract is good in quality.

Description

[0001] This application is a divisional application of "a new use of a cardiac glycoside compound". The filing date of the original application is April 11, 2013, and the application number is: 201310124216.4. technical field [0002] The invention relates to a cardiac glycoside compound, in particular to a cardiac glycoside 12β-hydroxycalotropin and its application. Background technique [0003] Tumor is a great threat to human health and life. It and cardiovascular disease have become two major difficulties in medicine, and constitute the first two causes of death in the world. Among the world's 5.2 billion population, about 7 million people are newly diagnosed with cancer every year, and more than 5 million people die of cancer every year, almost every 6 seconds, one cancer patient dies. In my country, an average of 1.5 million people are newly diagnosed with cancer every year, and about 800,000 people die of cancer every year. None of the existing antineoplastic drugs c...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P35/00A61P35/02C07J71/00
CPCA61K31/7048C07J71/0005
Inventor 王茂媛晏小霞王祝年王建荣王清隆王鹏
Owner TROPICAL CORP STRAIN RESOURCE INST CHINESE ACAD OF TROPICAL AGRI SCI
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