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Application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines

A technology of alkaloids and derivatives, applied in antibacterial drugs, medical preparations containing active ingredients, pharmaceutical formulations, etc., to achieve the effects of convenient use, significant antibacterial activity, and simple preparation process

Active Publication Date: 2010-09-08
海南泓科生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above patent documents related to the application research of aporphylloid alkaloids are limited to anti-tumor, inhibition of hepatitis virus, treatment of autoimmune diseases, inflammatory reactions, tissue damage or infection caused by autoimmune diseases and related diseases Abnormalities, rejection of transplantation, graft-versus-host disease or allergic disease caused by bone marrow transplantation, or the antifungal effects of such alkaloids, but none of the patent documents refer to aporphi-type alkaloids and their derivatives antibacterial effect

Method used

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  • Application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines
  • Application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines
  • Application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Extraction and separation of monomeric alkaloids 1 to 7 from the root tubers of the small leaflet

[0046] Stephania succifera H.S.Lo et Tsoong (Stephania succifera H.S.Lo et Tsoong) dried root tuber 16.0Kg was pulverized and then leached three times with ethanol with a volume fraction of 95% at room temperature, each time for 7 days. The ethanol was recovered under reduced pressure until there was no alcohol smell, and the ethanol extract was obtained. It is dispersed in water to form a suspension, such as figure 1 As shown, extract 3 times with petroleum ether and ethyl acetate successively, respectively concentrate to obtain petroleum ether extract (168.5g) and ethyl acetate extract (90.3g), after the remaining water part is filtered, pass through D-101 Pore ​​adsorption resin column chromatography, eluting with water and methanol in sequence, collecting the methanol eluate, and concentrating under reduced pressure to obtain methanol extract (133.0 g). Et...

Embodiment 2

[0047] Example 2: Physicochemical and spectral data of monomeric compounds

[0048] Dehydrocbanine (1): Pale yellow needle-like crystals (chloroform), mp 155-156°C, yellow in the presence of sulfuric acid with a volume fraction of 10%, and orange-red in the reaction with potassium bismuth iodide. EI-MS m / z: 337[M] + , combined with 1 H-NMR and 13 C-NMR spectrum data deduces that its molecular formula is C 20 h 19 NO 4 . 1 H-MR (400MHz, CDCl 3 )δ: 8.66 (1H, d, J=9.1Hz, H-11), 7.03 (1H, d, J=9.1Hz, H-10), 6.90 (1H, s, H-3), 6.87 (1H, s, H-7), 6.18 (2H, s, OCH 2 O), 3.99 (3H, s, 8-OCH 3 ), 3.98 (3H, s, 9-OCH 3 ), 3.36 (2H, t, J=6.0Hz, 5-CH 2 ), 3.20 (2H, t, J=6.0Hz, 4-CH 2 ), 3.12 (3H, s, N-CH 3 ); 13 C-NMR (100MHz, CDCl 3 )δ: 143.7(C-1), 117.4(C-1a), 118.7(C-1b), 145.2(C-2), 123.3(C-3), 127.3(C-3a), 30.6(C-4 ), 50.5(C-5), 141.6(C-6a), 94.4(C-7), 129.3(C-7a), 157.5(C-8), 150.2(C-9), 106.8(C-10) , 108.8(C-11), 118.2(C-11a), 100.8(OCH 2 O), 40.5(N-CH 3 ), 60.5 (8...

Embodiment 3

[0055] Embodiment 3: the in vitro antibacterial activity of aporphyllum and oxo-aporphyllin alkaloids

[0056] 3.1 Experimental materials

[0057] 3.1.1 Test drug

[0058] Dehydrogrambanine, grambanine, 7-Oxodehydrocaaverine, 7-oxodehydrocaaverine, 4,5-dioxo-dehydrocarbanine, oxidized grambanine, (-)-Sukhodianine: from small leaves The isolated monomeric compounds were extracted.

[0059] Chloroform: Tianjin Fuyu Fine Chemical Co., Ltd., batch number 20080901

[0060] Dehydrogrambanine, grambanine, 7-Oxodehydrocaaverine, 7-oxodehydrocaaverine, 4,5-dioxodehydrocarbanine, oxidized grambanine, (-)-Sukhodianine were prepared with chloroform respectively At a concentration of 1 mg / ml, the test drug was stored at room temperature 25°C. Before the experiment, the drugs were fully mixed, and the pharmacodynamic tests were carried out separately.

[0061] 3.1.2 Experimental strains

[0062] Staphylococcus aureus (Staphylococcus aureus) ATCC 51650 and methicillin-resistant Staphyl...

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Abstract

The invention discloses application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines. The invention provides a new medical usage and develops a new application field for the known aporphine alkaloid, the oxoaporphine alkaloid, the derivatives thereof and pharmaceutically acceptable salts thereof. The compounds, such as the aporphine alkaloid, the oxoaporphine alkaloid, the derivatives thereof and the pharmaceutically acceptable salts thereof, have remarkable antibacterial activity for staphylococcus aureus and methcillin-resistant staphylococcus aureus, and the invention provides a new compound for seeking for a new antibacterial medicine.

Description

technical field [0001] The present invention relates to the new application of aporphylloid alkaloids, oxo aporphim alkaloids and their derivatives, especially relates to the application of aporphim alkaloids, oxo aporphim alkaloids and their derivatives in Application in the preparation of antibacterial drugs. Background technique [0002] Staphylococcus aureus (Staphylococcus Aureus, SA) is a common pathogen that causes suppurative infection and nosocomial infection, food contamination and bacterial food poisoning clinically, and is also an important zoonotic pathogen. Widely present in the natural environment, it is a common bacterium on the body surface and upper respiratory tract of humans and animals, and it is also one of the most common pathogenic bacteria that cause a variety of suppurative infections. It can cause infections in various tissues and organs of humans, such as local Purulent infection, pneumonia, pseudomembranous enteritis, pericarditis, etc., and eve...

Claims

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Application Information

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IPC IPC(8): A61K31/4741A61K31/473A61P31/04
Inventor 戴好富梅文莉杨德兰王辉
Owner 海南泓科生物科技有限公司
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