CN103393692B - The application of compound in preparation anti-human fungi medicine - Google Patents
The application of compound in preparation anti-human fungi medicine Download PDFInfo
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- CN103393692B CN103393692B CN201310362245.4A CN201310362245A CN103393692B CN 103393692 B CN103393692 B CN 103393692B CN 201310362245 A CN201310362245 A CN 201310362245A CN 103393692 B CN103393692 B CN 103393692B
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Abstract
Do you the present invention relates to Kadcoccitones? the application of A in preparation anti-human fungi medicine, belongs to field of medicaments.Kadcoccitones? does A have very strong suppression red hair moss bacterium, microsporum canis or the disconnected effect sending out moss bacterium, therefore Kadcoccitones? A can be used as the compound with human body fungus, and is expected to be applied preparing in related drugs.
Description
Technical field
The present invention relates to the novelty teabag of compound K adcoccitonesA, particularly relate to the application of KadcoccitonesA in preparation anti-human fungi medicine.
Background technology
The health and lives of the mankind in pathomycete serious threat, antifungal drug is used widely as routine administration, the antimicrobial agent used clinically is at present (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., so the novel antifungal drugs finding mechanism of action uniqueness becomes one of focus of current medicament research and development.
The compound K adcoccitonesA that the present invention relates to is one and delivers (Cheng-QinLiang in 2012, etal., KadcoccitonesAandB, TwoNew6/6/5/5-FusedTetracyclicTriterpenoidsfromKadsuraco ccinea.OrganicLetters, 2012, 14 (24): 6362 – 6365.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to inhibiting HIV (Cheng-QinLiang, etal., KadcoccitonesAandB, TwoNew6/6/5/5-FusedTetracyclicTriterpenoidsfromKadsuraco ccinea.OrganicLetters, 2012, 14 (24): 6362 – 6365.), the purposes of the KadcoccitonesA that the present invention relates in preparation anti-human fungi medicine belongs to first public.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of human body fungi activity according in existing KadcoccitonesA research, provide the application of KadcoccitonesA in preparation anti-human fungi medicine.
Described compound K adcoccitonesA, structure is as shown in formula I:
Formula I
KadcoccitonesA has very strong suppression red hair moss bacterium, microsporum canis or the disconnected effect sending out moss bacterium, so KadcoccitonesA can be used as the compound with the effect of human body fungus, and be expected to be applied in preparation anti-human fungi medicine.
The purposes of the KadcoccitonesA that the present invention relates in preparation treatment anti-human fungi medicine belongs to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for Human Fungi inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously infected for Human Fungi obviously has significant progress.
Detailed description of the invention
The preparation method of compound K adcoccitonesA involved in the present invention is see document (Cheng-QinLiang, etal., KadcoccitonesAandB, TwoNew6/6/5/5-FusedTetracyclicTriterpenoidsfromKadsuraco ccinea.OrganicLetters, 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 by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound K adcoccitonesA tablet involved in the present invention:
Get 5 g of compound KadcoccitonesA, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound K adcoccitonesA capsule involved in the present invention:
Get 5 g of compound KadcoccitonesA, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:KadcoccitonesA human body fungi activity
The experiment of human body fungi activity is the method for employing concentration dilution, and in triplicate, test pathogen has red hair moss bacterium, microsporum canis and a disconnected moss bacterium to each mensuration, and bacterial concentration is 105/mL.KadcoccitonesA 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 test sample Mixed culture are in 96 orifice plates, Human Fungi cultivation temperature is respectively 28 DEG C, observe after incubation time 24h, if find, when not having bacterium colony to be formed be the minimum human body fungi concentration of sample, i.e. MIC value.This experiment positive control is ketoconazole, and KadcoccitonesA human body fungus the results are shown in Table 1.
Table 1KadcoccitonesA human body fungus MIC value (μ g/mL)
Conclusion: KadcoccitonesA has very strong human body fungi activity, and therefore KadcoccitonesA of the present invention is expected to be used to prepare novel anti-human fungi medicine.
Claims (1)
- The application of 1.KadcoccitonesA in preparation anti-human fungi medicine, described compound K adcoccitonesA structure is as shown in formula I:Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310362245.4A CN103393692B (en) | 2013-08-19 | 2013-08-19 | The application of compound in preparation anti-human fungi medicine |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310362245.4A CN103393692B (en) | 2013-08-19 | 2013-08-19 | The application of compound in preparation anti-human fungi medicine |
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| Publication Number | Publication Date |
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| CN103393692A CN103393692A (en) | 2013-11-20 |
| CN103393692B true CN103393692B (en) | 2016-02-10 |
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| CN201310362245.4A Active CN103393692B (en) | 2013-08-19 | 2013-08-19 | The application of compound in preparation anti-human fungi medicine |
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2013
- 2013-08-19 CN CN201310362245.4A patent/CN103393692B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| Kadcoccitones A and B, Two New6/6/5/5-Fused Tetracyclic Triterpenoids;Cheng-Qin Liang,et al;《Organic Letters》;20121211;第14卷(第24期);第6362-6365页 * |
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| CN103393692A (en) | 2013-11-20 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Qiu Xuehui Inventor after: Qiu Junyuan Inventor after: Lin Wenquan Inventor before: Zhang Sufeng |
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| COR | Change of bibliographic data | ||
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Effective date of registration: 20160114 Address after: Longgang Long Street East Community Tongchang road Longgang District Shenzhen 518116 Guangdong province No. 88 Tai Po Industrial Park Comprehensive Building 7 floor (in Longgang Long Street East community love road No. 78 good industrial park 11 Building 5 floor with establishments engaged in production and business activities) Applicant after: Zhang Sufeng Address before: 315016 Hai Guang building, No. 298 West Zhongshan Road, Haishu District, Zhejiang, Ningbo Applicant before: Zhang Sufeng |
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Address after: Pingshan Pingshan street Shenzhen city Guangdong province 518118 six community Jinlong Avenue Baoshan Road No. 16 Sea Branch strategic emerging industrial park A building 01 District five floor six floor Patentee after: Zhang Sufeng Address before: Longgang Long Street East Community Tongchang road Longgang District Shenzhen 518116 Guangdong province No. 88 Tai Po Industrial Park Comprehensive Building 7 floor (in Longgang Long Street East community love road No. 78 good industrial park 11 Building 5 floor with establishments engaged in production and business activities) Patentee before: Zhang Sufeng |