CN102861083B - Application of Houttuynoid B in anti-human fungi medicine - Google Patents

Application of Houttuynoid B in anti-human fungi medicine Download PDF

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CN102861083B
CN102861083B CN 201210418677 CN201210418677A CN102861083B CN 102861083 B CN102861083 B CN 102861083B CN 201210418677 CN201210418677 CN 201210418677 CN 201210418677 A CN201210418677 A CN 201210418677A CN 102861083 B CN102861083 B CN 102861083B
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houttuynoid
medicine
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preparation
fungi
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CN102861083A (en
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张广
王泽正
吴俊华
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Liu Jun
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Abstract

The invention relates to application of Houttuynoid B in preparation of an anti-human fungi medicine, belonging to the technical field of new application of medicine. Houttuynoid B has very strong effect on inhibition of epidrmophyton rubrum, microsporum lanosum or trichophyton tonsurans, so that Houttuynoid B is taken as an anti-human fungi compound and is expected to be applied to the preparation of the relative medicines. The application of Houttuynoid B in preparation of the anti-human fungi medicine provided by the invention is disclosed firstly. The skeleton type belongs to new skeletontype, and the activity of Houttuynoid B on inhibition of human fungi is unexpectedly strong; and the probability that any revelation is provided by other compounds does not exist, Houttuynoid B has the excellent substantive features, and Houttuynoid B obviously has a remarkable progress when being used for preventing and treating human fungi infection.

Description

The application of Houttuynoid B in anti-human body fungi-medicine
Technical field
The present invention relates to the purposes of Houttuynoid B, relate in particular to the application of Houttuynoid B 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 seek the novel antibacterial medicine of mechanism of action uniqueness.
the compound H outtuynoid B that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid B_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid B_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), belong to open first for the purposes of the Houttuynoid B that the present invention relates in the anti-human body fungi-medicine of preparation treatment, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for Human Fungi, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the control that is used for simultaneously the Human Fungi infection obviously has significant progress.
Summary of the invention
The object of the invention is to:
The application of a kind of Houttuynoid B of the present invention in the anti-human body fungi-medicine of preparation is provided.
Described compound H outtuynoid B structure is as shown in formula I:
Figure BDA0000231835931
Houttuynoid B has the effect of the red hair of very strong inhibition moss bacterium, microsporum canis or broken hair moss bacterium, so Houttuynoid B 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 Houttuynoid B that 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 is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously the Human Fungi infection obviously has significant progress.
The specific embodiment
The preparation method of compound H outtuynoid B involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid B_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compound H outtuynoid B tablet involved in the present invention:
Get 20 and digest compound Houttuynoid B, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid B capsule involved in the present invention:
Get 20 and digest compound Houttuynoid B, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: the anti-human body fungi activity of Houttuynoid B
Anti-human body fungi activity experiment is the method that adopts concentration dilution, measures triplicate at every turn, and the test pathogen has red hair moss bacterium, microsporum canis and broken hair moss bacterium, and bacterial concentration is 10 5Individual/mL.Houttuynoid B 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 ℃, observe after incubation time 24h, if be the minimum anti-human body fungi concentration of sample, i.e. MIC value when finding not have bacterium colony to form.This experiment positive control is ketoconazole, and the anti-human body fungus of Houttuynoid B the results are shown in Table 1.
The anti-human body fungus of table 1 Houttuynoid B MIC value (μ g/mL)
Figure BDA0000231835932
Conclusion: Houttuynoid B has very strong anti-human body fungi activity, and therefore Houttuynoid B of the present invention is expected to be used to prepare novel anti-human body fungi-medicine.

Claims (1)

1.Houttuynoid B is in the application of preparation in anti-human body fungi-medicine, its described Human Fungi be red mao of moss bacterium, microsporum canis and trichophyton tonsurans, described compound H outtuynoid B structure as Formula IShown in:
Figure DEST_PATH_IMAGE001
Formula I.
CN 201210418677 2012-10-27 2012-10-27 Application of Houttuynoid B in anti-human fungi medicine Active CN102861083B (en)

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