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Use of protoberberine alkaloid in preparing against bacterial resistance medicament

A technology of original berberine and alkaloids, applied in antibacterial drugs, pharmaceutical formulas, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2010-02-03
成都军区昆明总医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Throughout the reports at home and abroad, except for berberine (berberine), none of the patents specifically refers to the anti-MRSA effect of protoberberine (protoberberine) alkaloids involved in the present invention

Method used

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  • Use of protoberberine alkaloid in preparing against bacterial resistance medicament
  • Use of protoberberine alkaloid in preparing against bacterial resistance medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Extraction and isolation of monomeric alkaloids 1 to 6 from the whole plant of Litectinus chinensis

[0021] Take 1 kg of dried whole herb powder of Corydalis saxicola Bunt., impregnate it with 5 L of 0.5% sulfuric acid at room temperature for 48 hours, and then filter it. Add sodium chloride to the filtrate until the concentration is 10%, and then adjust it to PH10 with saturated sodium hydroxide. Chloroform extraction, recovery of chloroform to obtain total alkali extract. This extract was stirred with acetone, left to stand, filtered, and the acetone was recovered to obtain 14 g of acetone soluble matter and 20 g of insoluble matter. The acetone soluble matter was subjected to low-pressure silica gel column chromatography, and gradient elution with petroleum ether:ethyl acetate=15:1~3:1 gave compounds 3 (0.08g), 4 (0.2g) and 5 (0.4g); Acetone insolubles were subjected to low-pressure silica gel column chromatography, and gradient elution with petroleum et...

Embodiment 2

[0022] Example 2: Physicochemical and spectral data of monomeric compounds 1 to 6

[0023] Coptisine (1)

[0024] yellow prismatic crystals, C 19 h 14 NO 4 + , mp 217-218°C. ESI MS (positive ion mode) m / z: 320. 1 H NMR (DMSO-d 6 , 400MHz): δ H 9.84 (1H, s, H-8), 8.90 (1H, s, H-13), 7.98 (1H, d, J=8.4Hz, H-11), 7.81 (1H, d, J=8.6Hz, H -12), 7.74 (1H, s, H-1), 7.00 (1H, s, H-4), 6.52 (2H, s, OC^O-9, 10), 6.11 (2H, s, OCH 2 0-2, 3), 4.79 (2H, dd, J=6.3, 5.9Hz, H-6), 3.19 (2H, dd, J=6.3, 6.0Hz, H-5); 13 C NMR (DMSO-d 6 , 100MHz): δ C105.1(d, C-1), 147.2(s, C-2), 149.6(s, C-3), 108.0(d, C-4), 130.4(s, C-4a), 26.1(t, C -5), 55.0(t, C-6), 143.9(d, C-8), 120.2(s, C-8a), 143.5(s, C-9), 147.4(s, C-10), 120.7 (d, C-11), 120.8 (d, C-12), 132.4 (s, C-12a), 121.5 (d, C-13), 136.7 (s, C-13a), 111.4 (s, C-13a), 111.4 (s, C- 13b), 101.8(t, OCH 2 O-2,3), 104.2(t, OCH 2 O-9, 10).

[0025] Dehydroapocavidin (2)

[0026] yellow amorphous solid, C 20 h 18 N0 4 + . ESI MS (po...

Embodiment 3

[0035] Embodiment 3: as the screening of the clinical drug-resistant strain MRSA of drug susceptibility test

[0036] 1. Test material

[0037] Antibiotic-sensitive paper sheets (China Institute for the Control of Pharmaceutical and Biological Products), MH agar (Hangzhou Tianhe Microbiological Reagent Co., Ltd.).

[0038] 2. Specimen source

[0039] Four bacterial strains were isolated and screened from clinical specimens in our hospital, numbered MRSA321, MRSA40, MRSA45, and MRSA55, and stored in the refrigerator at -20°C for later use.

[0040] 3. Bacteria identification

[0041] According to the "National Clinical Inspection Operation Regulations" and the bacterial identification method known to those skilled in the art, the above-mentioned sample bacteria are isolated and cultivated, and it is identified as Staphylococcus aureus (SA), and according to the known routine test method for antibiotic susceptibility (K-B Disc method), and the identification of drug-resistant...

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Abstract

The invention discloses an application of protoberberine alkaloid to prepare anti-drug tolerant bacterial drug, in particular to an application of compound coptisine, dehydrokaweidin and dihydroapokaweidin in the anti-drug tolerant bacterial drug, which is characterized by the following: extracting protoberberine from Corydalis saxicola Bunt. of Corydalis of Papaveraceae; displaying obvious inhibition for MRSA in the clinic through pharmacological test; using the compound protoberberine alkaloid as active component to make the drug to treat anti-drug tolerant bacterial drug.

Description

technical field [0001] The invention relates to the use of protoberberine alkaloids in the preparation of anti-drug-resistant bacteria drugs. Background technique [0002] With the widespread use of antibiotics, more and more bacteria are resistant to commonly used antibiotics, and the degree of drug resistance is increasing. At present, Methicillin-resistant Staphylococcus aureus (Methicillin-resistant Staphylococcusaureus, MRSA) infection has been tied with HBV and AIDS as the three most difficult infectious diseases in the world. MRSA is resistant to a variety of antibiotics, has strong pathogenicity and poor treatment effect, and is one of the main pathogenic bacteria causing nosocomial infections. Since the founding of the People's Republic of my country, although China has carried out screening studies on the effects of Chinese herbal medicines against Staphylococcus aureus and other infections, these studies are mostly limited to medicinal material extracts, and the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61P31/04C07D491/147
Inventor 左国营徐贵丽张青刘树玲赵益斌余巍何洪静王根春唐斌
Owner 成都军区昆明总医院
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