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Naphthalenedione compounds

A compound, C1-C6 technology, applied in the direction of active ingredients of hydroxyl compounds, active ingredients of heavy metal compounds, drug combinations, etc., can solve problems such as poor results, side effects, and unsatisfactory

Inactive Publication Date: 2009-07-15
SUNTEN PHYTOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But many of these treatments are unsatisfactory due to poor efficacy or side effects

Method used

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  • Naphthalenedione compounds
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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Some compounds were isolated from Amebia euchroma (Royle) Johnst. Specifically, 1.65 kg of medicinal materials were soaked in 32 L of acetone for 3 days, and then filtered through a 200 mesh filter. The filtrate was concentrated under vacuum to obtain herbal extracts. 100 mg of the extract was dissolved in 50 ml of 100% methanol. The solution was sonicated for 30 minutes and filtered through a 0.45 micron filter membrane. It was processed by HPLC and eluted with 75% methanol. Six compounds were detected and separated by HPLC. The chromatographic conditions of analytical HPLC are: mobile phase: (A)H 2 O: CH 3 CN: AcOH = 800 ml: 200 ml: 10 ml, (B) H 2 O: CH 3 CN: MeOH: AcOH = 100 ml: 450 ml: 450 ml: 1 ml; flow rate, 0.8 ml / min; detection wavelength, 515 nm: column temperature, 40°C; gradient, linear from 10% B to 100% B; run Time, 60 minutes.

[0066]Collect fractions containing each compound. Under vacuum, the solvent in the collected fraction was removed to obtain a residue...

Embodiment 2

[0070] Using Carter's equivalent in 1991 in J. Pharmacol. Exp. Ther., 256(3): 929-937 and Safayhi's equivalent in 2000 in Planta Medica, 66: 110-113 and the modified method to study the above compounds (1 or 10μM) and the effect of extracts prepared from Xinjiang Lithospermum on 5-lipoxygenase activity. They were found to inhibit 5-lipoxygenase activity. Use nordihydroguaiaretic acid (NDGA), epigallocatechin-3 gallate (EGCG) and ciclpirox olamine as positive controls. The results are summarized below Table 2A and 2B.

[0071] Table 2A Inhibition of 5-lipoxygenase I

[0072]

[0073] Table 2B 5-Lipoxygenase II Inhibition

[0074]

[0075] It is known that 5-lipoxygenase is a key enzyme in the biosynthesis of leukotrienes and an important mediator in the process of inflammation and allergy. This result suggests that these compounds have dual anti-inflammatory and anti-allergic activities. The experiment was repeated with different concentrations of compounds, and similar results...

Embodiment 3

[0077] The activity of the above-mentioned compounds and extracts on Acne bacillus (a bacterial agent that causes pimples (acne)) was studied. Specifically, using Modugno equal to 1994 in Antimicrobial Agents and Chemotherapy, 38:2362-2368 and Missiek equal to 1973 in Antimicrobial Agents Chemtherapy, 3:40-48, the modified method was used to examine the compound or extract against bacteria (ATCC6919) Inhibition of growth. The results are summarized in Table 3.

[0078] Table 3 Anti-acne bacillus activity

[0079]

[0080] The results indicate that the above compounds and extracts can be used to treat acne infections.

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Abstract

This invention relates to compositions containing a compound of formula (I). Each variable is defined in the specification. Also disclosed are methods of using these compositions to treat acne, psoriasis, and infective skin ulcer.

Description

[0001] Related application [0002] This application claims the priority of U.S. Provisional Application No. 60 / 790259 filed on April 7, 2006, the content of which is incorporated herein by reference. Technical field [0003] The present invention generally relates to methods and compositions for treating inflammation-related disorders or microbial infections. Background technique [0004] Inflammation is the body's defense response to injury, infection, or antigenic stimulation. In some cases, the inflammation continues safely after the causative agent is removed. For example, it often coexists with signs of dermatitis, asthma, and angiogenesis. Some therapies have been developed to suppress undesired inflammatory reactions. However, many of these therapies are not satisfactory due to poor results or side effects. Therefore, there is still a need for a new treatment to treat undesired inflammation. [0005] Microbial infection is a major cause of inflammation. For example, infe...

Claims

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Application Information

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IPC IPC(8): A61K31/32
CPCY10S514/866A61K31/12A61K31/137Y10S514/887A61K31/222Y10S514/928A61K31/122A61K31/255A61P17/00A61P17/02A61P17/04A61P17/06A61P17/10A61P31/00A61P37/08A61P43/00C07C50/06A61K31/05
Inventor 简督宪朱伊文庄武璋李明宗
Owner SUNTEN PHYTOTECH