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Naphthoquinone compound and use of pharmaceutical composition thereof

A compound and composition technology, applied in the field of naphthoquinone derivatives, can solve the problem of no literature report on the anti-H. pylori activity, achieve good anti-H. pylori effect, inhibit the activity of H. active effect

Inactive Publication Date: 2007-07-04
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature report on the anti-H. pylori activity of the naphthoquinone compounds

Method used

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  • Naphthoquinone compound and use of pharmaceutical composition thereof
  • Naphthoquinone compound and use of pharmaceutical composition thereof
  • Naphthoquinone compound and use of pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039]Take 2Kg of dried rhizomes of sycamore root, crush them, and extract them under reflux with 95% ethanol (5L×3), and recover the ethanol to obtain the extract. The extractant is directly applied to a macroporous resin column, and ethanol-water gradient elution is divided into three fractions of 30%, 50%, and 95%. 95% of the fraction was subjected to 200-300 mesh silica gel column chromatography, petroleum ether-ethyl acetate gradient elution; and then subjected to Shephadex LH-20 (CHCl 3 / CH 3 OH 1:1 elution) column chromatography separation and purification to obtain compounds A1, A2 and A3.

[0040]

[0041] Compound A1: yellow powder, 1 H NMR (300MHz, CDCl3): δ8.58 (1H, d, J=7.2Hz), 8.20 (1H, d, J=7.2Hz), 7.60 (2H, t, J=7.2Hz), 2.10 (2H, m), 1.64 (2H, m), 1.30 (6H, s). Compared with the known compound α-lapachone[1], the above spectral data are completely consistent. Therefore, compound A1 was identified as α-lapachone.

[0042] Compound A2: yellow powder, 1H ...

Embodiment 2

[0044] Embodiment two: the preparation of tablet

[0045] Take 18 grams of compound A1, 120 grams of hydroxypropyl cellulose, 30 grams of micropowdered silica gel, 20 grams of starch, and an appropriate amount of magnesium stearate, mix evenly, use 10% pregelatinized starch as a binder, granulate with wet hair, and dry. Add magnesium stearate for mixing, and compress into 1000 9.7% tablets.

Embodiment 3

[0046] Embodiment three: the preparation of granule

[0047] Take 400 grams of compound A2, 250 grams of sucrose, 120 grams of hydroxypropyl cellulose, 30 grams of micropowdered silica gel, citric acid, and sodium bicarbonate in appropriate amounts, mix evenly, use an appropriate amount of 70% ethanol as a wetting agent, wet granulate, sieve, and dry Dry, pack into 2000 bags of granules.

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Abstract

The invention relates to a naphthaquinones compound which is extracted and separated from plants Chinese parasol tree root and structural formula as general formula (1) (2), specifically relates to the anti-pylorus endless screw spirillum effect of the compounds, and the application in treating and preventing pylorus endless screw spirillum affection disease of the drug combination which contains the compounds.

Description

technical field [0001] The invention relates to a new application of a class of naphthoquinone derivatives, in particular to the anti-helicobacter pylori effect of the compound, and the application of a pharmaceutical composition containing the compound in the treatment and prevention of helicobacter pylori infection. Background technique [0002] Chronic gastritis, gastric ulcer, duodenal ulcer, gastric MALT lymphoma and gastric cancer are diseases that seriously endanger human health and life. Pathological studies have confirmed that all of the above are related to Helicobacter pylori (Hp) infection. It is reported that more than 50% of the population in the world is infected with Helicobacter pylori, the most serious in developing countries, and the infection rate of Helicobacter pylori in adults reaches 60-80%. At present, anti-endocrine drugs and antibiotics combined therapy are mostly used to treat Hp infection clinically, but due to the large side effects, poor tolera...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P31/04A61P1/04
Inventor 胡立宏沈旭蒋华良武大雷白海云
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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