Compounds with fungus resistance and antineoplastic activity and preparation method and application thereof

A technology of anti-tumor activity and anti-fungal drugs, which is applied in the field of medicine, can solve problems such as treatment failure and human side effects, and achieve the effect of convenient clinical use

Active Publication Date: 2015-11-25
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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  • Compounds with fungus resistance and antineoplastic activity and preparation method and application thereof
  • Compounds with fungus resistance and antineoplastic activity and preparation method and application thereof
  • Compounds with fungus resistance and antineoplastic activity and preparation method and application thereof

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Effect test

Embodiment 1

[0030] The preparation method of the compound with antifungal and antitumor activity provided by the invention, it may further comprise the steps:

[0031] (1) Take dry Selaginella matte, 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;

[0032] (2) Get the ethyl acetate extract (108g) that step (1) prepares, go up silica gel column chromatography, be 95:5~50:50 chloroform:methanol with volume ratio, gradient elution successively, thin-layer chromatography detects 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 chl...

Embodiment 2

[0041] Embodiment 2 antifungal activity experiment

[0042] 1. The present invention conducts in vitro antifungal tests on compound A and compound B, showing that they have obvious fungal inhibitory effects. The cell strains used in the test are the ATCC standard strains provided by the Fungal Center of the Medical Microbial Bacteria (Virus) Species Preservation Management Center of the Ministry of Health, including:

[0043] Candida: Candida albicans (Candida albicans) bacteria number: CMCCC (F) C.1L (ATCC90028)

[0044] Aspergillus: Aspergillus fumigatus No.: CMCCC(F)A1g(ATCC-MYA-3626)

[0045] Trichophyton genus: Trichophyton rubrum (Trichophyton rubrum) bacteria number: CMCCC (F) T.1h (ATCC-MYA-4438)

[0046] Trichophytonmentagrophytes No.: CMCCC(F)T.5e(ATCC-MYA-4439)

[0047] A total of 3 genera, 4 species and 4 strains of common pathogenic fungi were identified.

[0048] 2. Specific experimental methods The experiments were carried out according to the standard metho...

Embodiment 3

[0058] Embodiment 3 anti-tumor experiment

[0059] The present invention has carried out anti-tumor test in vitro on compound B, and the test results show that it has obvious tumor-inhibiting effect. The cell lines used in the test are international tumor cell lines, namely K562 (leukemia cells); SMMC-7721 (liver cancer) A549 (lung adenocarcinoma); BGC-823 (gastric cancer), nasopharyngeal carcinoma maternal line CNE-2Z and cervical cancer HeLa cells.

[0060] The test method is the internationally accepted MTT method: according to the cell growth rate, tumor cells in the logarithmic growth phase are inoculated into 96-well culture plates at 100 μL / well, grown adherently for 24 hours, and then 100 μL / well is administered. Three replicate wells were set up for each concentration. A negative control group, a solvent control group, and a positive control group (paclitaxel injection) were also set up; 2 Cultivate under conditions for 72 hours, then discard the culture medium, ad...

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Abstract

The invention discloses compounds with fungus resistance and antineoplastic activity and a preparation method thereof. The chemical components of selaginella pulvinate are researched systematically and deeply; as shown by spectrum and mass spectrum data analysis, a compound A and a compound B with novel structures are obtained by separating from the selaginella pulvinate. as shown by fungus resistance and antineoplastic activity research in vitro, the compound A and the compound B have obvious inhibiting effects on multiple pathomycetes, comprising candida albicans, smoke-colored aspergillus, red trichophyta, alpha fungus and the like. The compound B has obvious inhibitory activity on leukemia, lung cancer, gastric cancer, nasopharyngeal carcinoma, liver cancer and cervical cancer tumours and the like. The compounds can be conveniently prepared into multiple dosage forms and is convenient to take clinically.

Description

technical field [0001] The present invention relates to a compound with antifungal activity, in particular to a compound with antifungal and antitumor activity extracted from Selaginella genus Selaginella and its application in treating fungal infections and tumor diseases. It belongs to the field of medical technology. Background technique [0002] Malignant tumors are frequently-occurring and common diseases that seriously endanger human health and life. In many countries including China, especially moderately developed countries, the death caused by malignant tumors ranks first or second only to cardiovascular diseases, and the morbidity and mortality are still on the rise worldwide. The successful research of paclitaxel and other drugs shows that it is of great significance to continue to find cytotoxic drugs or lead compounds with new mechanisms of action and unique chemical structures from natural plants, which has become an important field and research hotspot in can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/753C07C45/78C07C45/79C07C45/80A61K31/122A61P35/00
CPCA61P35/02A01N35/06A61P35/00C07C49/753C07C45/78C07C45/79C07C45/80
Inventor 曹园段金廒吴永平
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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