Unlock instant, AI-driven research and patent intelligence for your innovation.

Application of two naphthoquinone compounds in preparing antitumor medicaments

A technology of anti-tumor drugs and pharmaceutical preparations, applied in the field of medicine, can solve the problem that there is not much research on the chemical components of wild walnut.

Inactive Publication Date: 2012-07-11
HUAZHONG UNIV OF SCI & TECH
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There were not many studies on the chemical constituents of wild walnut before, and there were only reports on the antibacterial activity of crude extracts of wild walnut leaves, the determination and analysis of elements in wild walnut shells, and the identification of crude drugs from adulterated products

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of two naphthoquinone compounds in preparing antitumor medicaments
  • Application of two naphthoquinone compounds in preparing antitumor medicaments
  • Application of two naphthoquinone compounds in preparing antitumor medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] 20 kg of dried root bark of wild walnut (Juglans cathayensis Dode) was crushed, extracted by percolation with 95% ethanol, and the extract was concentrated under reduced pressure to obtain 2.5 kg of extract. The extract was evenly dispersed in 40L of water, and extracted with petroleum ether and ethyl acetate in turn. Obtain 400g of ethyl acetate part, mix it with 500g of silica gel, add to the top of the installed silica gel column, elute with petroleum ether: ethyl acetate system gradient, TLC tracking, combine and contain the same components, reduce pressure After concentration and drying, 1.0 g of 2-methoxyjuglone and 0.3 g of 3-methoxyjuglone were obtained from the polar segment of petroleum ether / ethyl acetate 5:1.

[0058] 2-methoxy juglone (2-methoxy juglone) is a brownish-red needle-like crystal, soluble in ethyl acetate, acetone, chloroform, DMSO, etc., and the color of ethanol sulfate is bright yellow spots. EI-MS gives molecular ion peak as 204( figure 1 )...

Embodiment 2

[0061] Active ingredient (by one of two kinds of compounds that embodiment 1 makes 10g

[0062] or composition)

[0063] Lactose 100g

[0064] Cornstarch 25g

[0065] Magnesium Stearate 5g

[0066] Made into 1000 pieces

[0067] Preparation method: uniformly moisten the active ingredient, lactose and starch mixture with water to make a soft material, granulate the wetted mixture, pass through a 20-mesh sieve, dry at 80°C, add magnesium stearate, sieve again, and then The mixture is compressed into tablets, each weighing 140mg, containing 10mg of the active ingredient.

Embodiment 3

[0069] Get 2.5g of the active ingredient (one of the two compounds obtained in Example 1 or the composition), add 200ml of propylene glycol and ethanol, stir to dissolve, add water for injection and dilute to 10000ml, filter through a 0.22 μm microporous membrane, pour Sealed, 20ml / bottle, sterilized by circulating steam for 30 minutes, inspected, packaged, and obtained injection.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
weightaaaaaaaaaa
Login to View More

Abstract

The invention provides application of two naphthoquinone compounds in preparing antitumor medicaments, wherein the two naphthoquinone compounds are 2-methoxyl juglone and 3-methoxyl juglone which are obtained by extraction, separation and purification from wild walnuts or other plants or by chemical synthesis. Experiments indicate that the two naphthoquinone compounds have favorable inhibition activities on various tumor cells of human, such as HepG2, Hela, MCF-7, Caco-2, A549, PANC-1 and the like, also have obvious inhibition effect on transplanted H22 liver cancer tumors of mice and presents a good concentration dependence. Quantitative detection of a flow cytometer indicates that the 2-methoxyl juglone and the 3-methoxyl juglone have an obvious cell apoptosis induction effect on Hela cells. Therefore, 2-methoxyl juglone and 3-methoxyl juglone can be used for preparing the antitumor medicaments.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of two naphthoquinone compounds, 2-methoxyjuglone and 3-methoxyjuglone, in the preparation of antitumor drugs. Background technique [0002] Malignant tumor is one of the diseases that seriously endanger human health. The International Anti-Cancer Alliance declared that the number of deaths from cancer each year far exceeds the sum of the deaths caused by the three diseases of malaria, AIDS and tuberculosis. The alliance pointed out at the World Cancer Research Conference in August 2008 that the global There are 11 million newly diagnosed cancer patients, and about 8 million people die from cancer every year. If the situation does not improve, from now to 2030, the number of newly diagnosed cancer patients will increase to 16 million each year, and the annual cancer death toll is more likely to climb to a staggering number of 11.5 million. Moreover,...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P35/00C07C50/32C07C46/10
Inventor 阮汉利余恒毅
Owner HUAZHONG UNIV OF SCI & TECH