Compound with antifungal activity and preparation method and application thereof

An antifungal drug and antifungal technology, applied in the directions of antifungal agents, separation/purification of carbonyl compounds, organic chemistry, etc., can solve the problems of human toxicity and side effects, treatment failure, etc., and achieve the effect of convenient preparation and convenient clinical use

Active Publication Date: 2015-02-25
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, chemically synthesized antifungal drugs are facing a severe situation: first, the existing antifungal drugs have different degrees of toxic and side effects on the human body; second, large-scale clinical drug resistance is becoming more and more serious, almost all antifungal drugs Drug-resistant strains have been found in all fungal drugs, and drug resistance has become the main reason for the failure of clinical antifungal therapy

Method used

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  • Compound with antifungal activity and preparation method and application thereof
  • Compound with antifungal activity and preparation method and application thereof
  • Compound with antifungal activity and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation method of compound II with antifungal activity provided by the invention, it may further comprise the steps:

[0026] (1) Take the dried Selaginella matta, crush it, add 10 times the concentration of 95% ethanol to reflux and extract 3 times, each time for 2 hours, combine the extracts, concentrate under reduced pressure until there is no alcohol smell, dilute with water, then use petroleum ether, Extraction with ethyl acetate and water-saturated n-butanol, take the ethyl acetate extract and recover the solvent under reduced pressure to obtain the total ethyl acetate extract;

[0027] (2) Take the ethyl acetate extract (108g) prepared in step (1), put it on silica gel column chromatography, use chloroform:methanol whose volume ratio is 95:5~50:50, gradient elution successively, thin-layer chromatography detection Identify, combine the fractions of the same spot; get six fractions (Fr.1~Fr.6), put Fr.2 on silica gel column chromatography, use the volume r...

Embodiment 2

[0032] Embodiment 2 antifungal activity experiment

[0033] 1. The present invention conducts in vitro antifungal tests on compound II, which shows that it has a more obvious effect of inhibiting fungi. The cell strains used in the test are ATCC standard strains provided by the Fungal Center of the Medical Microbial Bacteria (Virus) Species Preservation Management Center of the Ministry of Health, including:

[0034] Candida genus: Candida albicans (Candida albicans) bacteria number: CMCCC(F)C .1L (ATCC90028)

[0035] Aspergillus: Aspergillus fumigatus (Aspergillus fumigatus) No.: CMCCC(F)A 1g (ATCC-MYA-3626)

[0036] Trichophyton genus: Trichophyton rubrum No.: CMCCC(F)T .1h (ATCC-MYA-4438)

[0037] Trichophyton mentagrophytes bacteria number: CMCCC(F)T .5e (ATCC-MYA-4439)

[0038] A total of 3 genera, 4 species and 4 strains of common pathogenic fungi were identified.

[0039] 2. Specific experimental methods The experiments were conducted with reference to the standar...

Embodiment 3 Embodiment 1

[0048] Example 3 Acute Toxicity Test of Compound II Gained in Example 1

[0049] Calculate the half lethal dose LD of mice according to Bliss method 50 value, LD 50 The value is 1.42 mg / kg, and the experimental results show that the compound II provided by the present invention has low acute toxicity.

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Abstract

The invention discloses a novel compound II with antifungal activity. The chemical components of Selaginella pulvinata Maxim are subjected to systematic intensive study, and the spectrum and mass spectrometric data analysis proves that the novel compound II is separated from the Selaginella pulvinata Maxim. The in-vitro antifungal activity research proves that the compound II disclosed by the invention has the effects of obviously inhibiting multiple pathogenic fungi such as Candida albicans, aspergillus fumigatus, trichophyton rubrum and alpha fungus, is low in toxicity and safe in clinical administration, and is expected to be developed into a novel antifungal medicament.

Description

technical field [0001] The present invention relates to a compound with antifungal activity, in particular to a new compound with antifungal activity extracted from the whole herb of Selaginella genus Selaginella and its application in treating fungal infections. It belongs to the field of medical technology. Background technique [0002] In recent years, with the increasing number of cancer and AIDS patients, the widespread development of organ transplantation, catheter intubation and endoscopy, and the wide application of high-efficiency spectrum antibiotics, immunosuppressants and corticosteroids, the fungal infection rate has continued to increase. Azole (including imidazoles, triazoles) and polyene antifungal drugs are clinically commonly used antifungal drugs that can effectively treat deep and superficial fungal infections, such as ketoconazole, clotrimazole, Miconazole, econazole, etc.; fluconazole, itraconazole, voriconazole, etc. in triazoles; amphotericin B in po...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/835C07C45/78A61P31/10
CPCC07C45/78C07C49/835
Inventor 曹园段金廒吴永平姚毅
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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