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New application of cardiac glycoside compound

A compound and cardiac glycoside technology, which is applied in the field of cardiac glycoside compounds to achieve the effects of good extract quality, simple and easy separation method and high yield

Active Publication Date: 2013-07-10
TROPICAL CORP STRAIN RESOURCE INST CHINESE ACAD OF TROPICAL AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is still unknown whether the cardiac glycoside compound 12β-hydroxycalotropin in croissanthus has anti-tumor effects

Method used

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  • New application of cardiac glycoside compound
  • New application of cardiac glycoside compound
  • New application of cardiac glycoside compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A, the horn melon ( Calotropis gigantea ) stem 25.4 kg natural air-dried and pulverized, according to the mass / volume ratio (kg / L) of croissant melon sample: ethanol aqueous solution of about 1:2, 50 L of ethanol aqueous solution with a volume fraction of 95% and 25.4 kg crocus melon sample Fully mix, seal, and extract at room temperature for 3 times, each time for 7 days, filter and combine the extracts, and concentrate under reduced pressure until there is no alcohol smell to obtain the ethanol extract;

[0026] 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, concentrating under reduced pressure and recovering petroleum ether, petroleum ether extract (254.1 g) was obtained;

[0027] C. Filter the water liquid after petroleum ether extraction, separate the filtrate by D-101 macr...

Embodiment 2

[0032] After column chromatography, Fr.4-1 (3.2 g) in step E in Example 1 was eluted with chloroform:methanol=25:1 volume ratio eluent, 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 (869.5 mg) was subjected to silica gel column chromatography, followed by chloroform:methanol=40:1, chloroform : The eluent of acetone=6:2 volume ratio is eluted, finally obtains cardiac glycoside compound calotropin (109.9 mg). 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 further in vitro antitumor activity tests, the anti-IC 50 The values ​​are significantly different (see Table 2).

Embodiment 3

[0034] Structural identification of cardiac glycoside compound 12β-hydroxycalotropin:

[0035]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).

[0036] The following are cardiac glycoside compounds 12β-hydroxycalotropin The physical and chemical constants:

[0037] 12β-hydroxycalotropin: C 29 h 40 o 10 , white amorphous powder (methanol), 10% sulfuric acid ethanol solution is brown. m.p. 214-216 °C; [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 ): 3433 cm -1 , 2957 cm -1 , 2923 cm -1 , 2852 cm -1...

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Abstract

The invention discloses an application of a cardiac glycoside compound 12 beta-hydroxycalotropin in preparing medicines for treating and preventing tumors. The cardiac glycoside compound 12 beta-hydroxycalotropin has obvious antitumor activity and can be served as a lead compound for treating the tumors. Moreover, an extraction and separation method of the cardiac glycoside compound 12 beta-hydroxycalotropin provided by the invention is simple and practicable and low in cost, and has high efficiency and yield and good extract quality.

Description

technical field [0001] The present invention relates to a cardiac glycoside compound, in particular to a cardiac glycoside compound 12β-hydroxycalotropin and its application. Background technique [0002] 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 can completely and effectively cure the disease. At the same time, due to the continuous discovery of new tumors, people are forced to find new anti-tumor drugs. For a long time, finding anti-tu...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P35/00A61P35/02C07J71/00
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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