CN103446114A - Applications of Sarcaboside A in antibacterial medicament - Google Patents

Applications of Sarcaboside A in antibacterial medicament Download PDF

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Publication number
CN103446114A
CN103446114A CN201310430764XA CN201310430764A CN103446114A CN 103446114 A CN103446114 A CN 103446114A CN 201310430764X A CN201310430764X A CN 201310430764XA CN 201310430764 A CN201310430764 A CN 201310430764A CN 103446114 A CN103446114 A CN 103446114A
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Prior art keywords
sarcaboside
applications
antibacterial
preparing
belongs
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CN201310430764XA
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Chinese (zh)
Inventor
江春平
张广
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Nanjing Guangkangxie Biomedical Technology Co Ltd
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Nanjing Guangkangxie Biomedical Technology Co Ltd
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Priority to CN201310430764XA priority Critical patent/CN103446114A/en
Publication of CN103446114A publication Critical patent/CN103446114A/en
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    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The invention relates to applications of Sarcaboside A in preparing an antibacterial medicament, and belongs to the field of medicines. The Sarcaboside A plays a strong role in inhibiting escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteus and cryptococcus neoformans, thus being capable of serving as an antibacterial compound, and being expected to be applied in preparing related medicaments. The applications of the Sarcaboside A in preparing the antibacterial medicament are disclosed for the first time. As a skeleton type of the Sarcaboside A belongs to a brand-new skeleton type, the Sarcaboside A has unexpectedly strong bacteria inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside A has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the bacteria infection.

Description

The application of Sarcaboside A in anti-bacterial drug
Technical field
The present invention relates to the purposes of Sarcaboside A, relate in particular to the application of Sarcaboside A in preparing anti-bacterial drug.
Background technology
The mankind's health and lives in the enhancing serious threat of the diffusion of pathogenic bacterium and drug resistance thereof, antibacterials are widely used in acquired immune deficiency syndrome (AIDS) as routine administration, organ transplantation and Chronic consumptions are (as cancer, diabetes, uremia etc.) treatment, although the antimicrobial agent of using clinically at present is (as ketoconazole, amikacin, gentamycin, voriconazole, itraconazole, terbinafine, amphotericin, fluconazol etc.) better to the curative effect of skin and superficial place infection, but the cumulative toxicity of these antibacterials is stronger, usually cause lesions of liver and kidney, digestive tract stimulates, dizzy, irritated etc., become one of focus of current medicament research and development so find the novel antibacterial medicine of mechanism of action uniqueness.
The compound S arcaboside A the present invention relates to is one and within 2012, delivers (Li, X.et al., 2012.Two New-Skeleton Compounds from Sarcandra glabra.Helvetica Chimica Acta95 (6), 998-1002.) New skeleton compound, this compound has brand-new framework types, at present not about active report, belong to open first for the purposes of Sarcaboside A in preparing anti-bacterial drug the present invention relates to, because framework types belongs to brand-new framework types, and it is active unexpectedly strong for bacteriostatic, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the control of simultaneously infecting for antibacterial obviously has significant progress.
Summary of the invention
The object of the invention is to:
The application of a kind of Sarcaboside A of the present invention in preparing anti-bacterial drug is provided.
Described compound S arcaboside A structure is as shown in formula I:
Figure BDA0000384446720000021
Sarcaboside A has the effect of very strong inhibition escherichia coli, fluorescent pseudomonas, Staphylococcus aureus, Bacillus proteus, neogenesis cryptococcus, so Sarcaboside A can be used as the compound with antibacterial action, and be expected to be applied in the preparation antibacterials.
It is open first that the purposes of Sarcaboside A in preparing anti-bacterial drug belongs to, because framework types belongs to brand-new framework types, and it is active unexpectedly strong for bacteriostatic, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control of simultaneously infecting for antibacterial obviously has significant progress.
The specific embodiment
The preparation method of compound S arcaboside A involved in the present invention is referring to document (Li, X.et al., 2012.Two New-Skeleton Compounds from Sarcandra glabra.Helvetica Chimica Acta95 (6), 998-1002.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound S arcaboside A tablet involved in the present invention:
Get 20 and digest compound Sarcaboside A, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound S arcaboside A capsule involved in the present invention:
Get 20 and digest compound Sarcaboside A, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: Sarcaboside A antibacterial activity
Antibacterial activity test is the method that adopts concentration dilution, measures triplicate at every turn, and the test pathogen has escherichia coli, fluorescent pseudomonas, Staphylococcus aureus, Bacillus proteus, neogenesis cryptococcus, and bacterial concentration is 10 5individual/mL.The SarcabosideA initial concentration is 50.0 μ g/mL(5% dimethyl sulfoxide DMSO), gradient dilution to 0.098 μ g/mL, the bacterium liquid of equivalent volumes and specimen Mixed culture are in 96 orifice plates, the antibacterial culturing temperature is respectively 37 ℃, after incubation time 24h, observe, if discovery is the sample lowest concentration of antimicrobial while not having bacterium colony to form, i.e. the MIC value.This experiment positive control is amikacin sulfate, and Sarcaboside A the anti-bacterial result is in Table 1.
The table antibiotic MIC value of 1Sarcaboside A (μ g/mL)
Figure BDA0000384446720000031
Conclusion: Sarcaboside A has very strong antibacterial activity, and therefore Sarcaboside A of the present invention is expected to be used to prepare the novel antibacterial medicine.

Claims (1)

1.Sarcaboside the application of A in anti-bacterial drug, described compound S arcaboside A structure as formula Ishown in:
formula I.
CN201310430764XA 2013-09-18 2013-09-18 Applications of Sarcaboside A in antibacterial medicament Pending CN103446114A (en)

Priority Applications (1)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106188212A (en) * 2014-06-25 2016-12-07 虞定生 The application in antibacterials of Cleistanone derivant and pharmaceutically acceptable salt

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106188212A (en) * 2014-06-25 2016-12-07 虞定生 The application in antibacterials of Cleistanone derivant and pharmaceutically acceptable salt

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Application publication date: 20131218