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Compounds with antifungal activity and their preparation methods and applications

An antifungal drug and antifungal technology, applied in the field of medicine, can solve problems such as human side effects and treatment failure, and achieve the effect of convenient preparation and clinical administration

Active Publication Date: 2015-08-05
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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  • Compounds with antifungal activity and their preparation methods and applications
  • Compounds with antifungal activity and their preparation methods and applications
  • Compounds with antifungal activity and their preparation methods and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation method of compound I with antifungal activity provided by the invention comprises the following 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, merge the fractions of the same spot; then go to silica gel column chromatography respectively, use the volume ratio of 95:5~80:20 chlorofo...

Embodiment 2

[0032] Embodiment 2 antifungal activity experiment

[0033] 1. The present invention conducts an in vitro antifungal test on compound I, 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 No.: CMCCC(F)A1g(ATCC-MYA-3626)

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

[0037] Trichophytonmentagrophytes 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 standard methods of yeast M-27A3 and filame...

Embodiment 3 Embodiment 1

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

[0049] Calculate the half lethal dose LD of mice according to Bliss method 50 value, LD 50 The value is 1.38 mg / kg, and the experimental results show that the compound I provided by the present invention has low acute toxicity.

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Abstract

The invention discloses a new compound I with the antifungal activity. The new compound I is obtained by systematic in-depth study on the chemical components of selaginella pulvinata maxim and separation from the selaginella pulvinata maxim through analysis on wave spectrum and mass spectrum data. Shown by in-vitro antifungal activity, the new compound I provided by the invention has obvious inhibiting effect on candida albicans, aspergillus fumigates, trichophyton rubrum and alpha fungus and the like, is low in toxicity and can be developed into a new antifungal medicine.

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 endoscopic techniques, and the wide application of high-efficiency broad-spectrum antibiotics, immunosuppressants and corticosteroids, the rate of fungal infection 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;...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D217/16A61K31/472A61P31/10
CPCC07D217/16
Inventor 曹园段金廒吴永平姚毅
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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