CN103446115A - Applications of Sarcaboside A in medicament against human fungus - Google Patents

Applications of Sarcaboside A in medicament against human fungus Download PDF

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Publication number
CN103446115A
CN103446115A CN 201310430897 CN201310430897A CN103446115A CN 103446115 A CN103446115 A CN 103446115A CN 201310430897 CN201310430897 CN 201310430897 CN 201310430897 A CN201310430897 A CN 201310430897A CN 103446115 A CN103446115 A CN 103446115A
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China
Prior art keywords
sarcaboside
fungus
applications
human fungus
against human
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CN 201310430897
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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 CN 201310430897 priority Critical patent/CN103446115A/en
Publication of CN103446115A publication Critical patent/CN103446115A/en
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Abstract

The invention relates to applications of Sarcaboside A in preparing a medicament against human fungus, and belongs to the field of medicines. The Sarcaboside A plays a strong role in inhibiting trichophyton rubrum, microsporum lanosum or trichophyton tonsurans, therefore, the Sarcaboside A can serve as a compound with an anti-human fungus function, and is expected to be applied in preparing related medicaments. The applications of the Sarcaboside A in preparing the medicament against human fungus 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 an unexpectedly strong human fungus 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 human fungus infection.

Description

The application of Sarcaboside A in anti-human body fungi-medicine
Technical field
The present invention relates to the purposes of Sarcaboside A, relate in particular to the application of Sarcaboside A in the anti-human body fungi-medicine of preparation.
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 Acta 95 (6), 998-1002.) New skeleton compound, this compound has brand-new framework types, at present not about active report, purposes for the Sarcaboside A the present invention relates in the anti-human body fungi-medicine of preparation treatment belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for Human Fungi, 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 Human Fungi 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 the anti-human body fungi-medicine of preparation is provided.
Described compound S arcaboside A structure is as shown in formula I:
Figure BDA0000384157501
Sarcaboside A has the effect of very strong inhibition trichophyton, microsporum canis or trichophyton tonsurans, so Sarcaboside A can be used as the compound with the effect of anti-human body fungus, and is expected to be applied in the anti-human body fungi-medicine of preparation.
The purposes of the Sarcaboside A the present invention relates in the anti-human body fungi-medicine of preparation treatment belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for Human Fungi, 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 Human Fungi 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 Acta 95 (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: the anti-human body fungi activity of Sarcaboside A
Anti-human body fungi activity experiment is the method that adopts concentration dilution, measures triplicate at every turn, and the test pathogen has trichophyton, microsporum canis and trichophyton tonsurans, and bacterial concentration is 10 5individual/mL.Sarcaboside 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 Human Fungi cultivation temperature is respectively 28 ℃, after incubation time 24h, observe, while if find, not having bacterium colony to form, be the minimum anti-human body fungi concentration of sample, i.e. MIC value.This experiment positive control is ketoconazole, and the anti-human body fungus of Sarcaboside A the results are shown in Table 1.
The anti-human body fungus of table 1 Sarcaboside A MIC value (μ g/mL)
Figure BDA0000384157502
Conclusion: Sarcaboside A has very strong anti-human body fungi activity, and therefore Sarcaboside A of the present invention is expected to be used to prepare novel anti-human body fungi-medicine.

Claims (1)

1.Sarcaboside the application of A in anti-human body fungi-medicine, described compound S arcaboside A structure as formula Ishown in:
Figure 2013104308977100001DEST_PATH_IMAGE001
formula I.
CN 201310430897 2013-09-18 2013-09-18 Applications of Sarcaboside A in medicament against human fungus Pending CN103446115A (en)

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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