CN103463099A - Application of Kadcoccitones A in preparing antibacterial medicines - Google Patents
Application of Kadcoccitones A in preparing antibacterial medicines Download PDFInfo
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- CN103463099A CN103463099A CN2013104770631A CN201310477063A CN103463099A CN 103463099 A CN103463099 A CN 103463099A CN 2013104770631 A CN2013104770631 A CN 2013104770631A CN 201310477063 A CN201310477063 A CN 201310477063A CN 103463099 A CN103463099 A CN 103463099A
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- Prior art keywords
- kadcoccitones
- application
- compound
- preparing antibacterial
- antibacterial medicines
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- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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Abstract
The invention relates to application of Kadcoccitones A in preparing antibacterial medicines. Kadcoccitones A has a strong effect in inhibiting escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteusbacillus vulgaris and cryptococcus neoformans, can be used as an antibacterial compound, is disclosed for the first time, has a strong activity for inhibiting bacteria, has a highlighted substantial characteristic, and is remarkably progressed when being used for preventing and treating bacterial infection.
Description
Technical field
The present invention relates to the new purposes of compound K adcoccitones A, relate in particular to the application of Kadcoccitones A in preparing anti-bacterial drug.
Background technology
Antibacterials have been widely used in the treatment of acquired immune deficiency syndrome (AIDS), organ transplantation and Chronic consumptions (as cancer, diabetes, uremia etc.) as routine administration, although the antimicrobial agent of using clinically at present is 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 stimulate, dizzy, irritated etc., so the novel antibacterial medicine of searching mechanism of action uniqueness becomes one of focus of current medicament research and development.
The compound K adcoccitones A the present invention relates to is one and within 2012, delivers (Cheng-Qin Liang, et al., Kadcoccitones A and B, Two New6/6/5/5-Fused Tetracyclic Triterpenoids from Kadsura coccinea.Organic Letters, 2012, 14 (24): 6362 – 6365.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to inhibiting HIV, invalid to kinds of tumors, (Cheng-Qin Liang, et al., Kadcoccitones A and B, Two New6/6/5/5-Fused Tetracyclic Triterpenoids from Kadsura coccinea.Organic Letters, 2012, 14 (24): 6362 – 6365.), it is open first that the purposes of Kadcoccitones A in preparing anti-bacterial drug the present invention relates to belongs to.
Summary of the invention
The object of the invention is to, according in existing Kadcoccitones A research, not finding that it has the present situation of the report of antibacterial activity, provides the application of Kadcoccitones A in preparing anti-bacterial drug.
Described compound K adcoccitones A structure is as shown in formula I:
Formula I
Experimentation shows that Kadcoccitones A has the effect that suppresses escherichia coli, fluorescent pseudomonas, Staphylococcus aureus, Bacillus proteus, neogenesis cryptococcus, so Kadcoccitones A can be used as the compound with antibacterial action, and be expected to be applied in the preparation antibacterials, belong to open first, and it is active strong for bacteriostatic, possess outstanding substantive distinguishing features, the control of simultaneously infecting for antibacterial obviously has significant progress.
The specific embodiment
The preparation method of compound K adcoccitones A involved in the present invention is referring to document (Cheng-Qin Liang, et al., Kadcoccitones A and B, Two New6/6/5/5-Fused Tetracyclic Triterpenoids from Kadsura coccinea.Organic Letters, 2012,14 (24): 6362 – 6365.)
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 K adcoccitones A tablet involved in the present invention:
Get 5 and digest compound Kadcoccitones A, add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound K adcoccitones A capsule involved in the present invention:
Get 5 and digest compound Kadcoccitones A, add starch 195 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The experimentation of experimental example 1:Kadcoccitones 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.Kadcoccitones A 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 Kadcoccitones A the anti-bacterial result is in Table 1.
The table antibiotic MIC value of 1Kadcoccitones A (μ g/mL)
Conclusion: Kadcoccitones A has very strong antibacterial activity, and therefore Kadcoccitones A of the present invention is expected to be used to prepare the novel antibacterial medicine.
Claims (1)
1.Kadcoccitones the application of A in preparing anti-bacterial drug, described compound K adcoccitones A structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013104770631A CN103463099A (en) | 2013-10-14 | 2013-10-14 | Application of Kadcoccitones A in preparing antibacterial medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013104770631A CN103463099A (en) | 2013-10-14 | 2013-10-14 | Application of Kadcoccitones A in preparing antibacterial medicines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103463099A true CN103463099A (en) | 2013-12-25 |
Family
ID=49788292
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013104770631A Withdrawn CN103463099A (en) | 2013-10-14 | 2013-10-14 | Application of Kadcoccitones A in preparing antibacterial medicines |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103463099A (en) |
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2013
- 2013-10-14 CN CN2013104770631A patent/CN103463099A/en not_active Withdrawn
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20131225 |