Unlock instant, AI-driven research and patent intelligence for your innovation.

Use of diazocine analogue in preparation of antineoplastic and antifungal medicine

An anti-tumor drug, anti-fungal drug technology, applied in the direction of anti-tumor drugs, anti-fungal agents, drug combinations, etc., can solve problems such as few researches

Inactive Publication Date: 2004-12-29
SHANDONG UNIV
View PDF0 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The diazocine compound 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]-diazaocine involved in the present invention is used in biological There are few studies in vivo, and there are no reports on the preparation of this type of compound by myxobacteria fermentation, and the application of this type of compound in the preparation of antitumor and antifungal drugs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Use of diazocine analogue in preparation of antineoplastic and antifungal medicine
  • Use of diazocine analogue in preparation of antineoplastic and antifungal medicine
  • Use of diazocine analogue in preparation of antineoplastic and antifungal medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] How to prove that 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]-diazapine inhibits fungi below by Example 1 Function (take Mucor as an example).

[0057] 1. Bacteria to be tested: Mucor biemalis 3.40

[0058] 2. TF medium (g / L) peptone 1%; glucose 1%; agar 1.6%; pH7.0

[0059] 3.2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]-diazocine concentration gradient acquisition: according to the distribution of the culture plate, Perform a ten-fold serial dilution of the stock solution, and the minimum dilution should reach 10 -6 , so that the determined MIC falls within the determined range

[0060] 4. Add 150 μl culture medium and 10 μl 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5] to each well of the 96-well plate -Diazocine solution and 50 μl mucormyces spore suspension, each drug concentration was repeated more than three times.

[0061] 5. Incubate at 30°C for 18 hours, subject to the growth visible to the naked eye in the control group...

Embodiment 2

[0065] How to prove that 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]-diazocine is effective for tumor cells by Example 2 below Inhibitory effect (taking liver cancer cell Bel-7402 as an example).

[0066] 1. Cell line: Bel-7402 (adherent cells)

[0067] 2. Preparation of 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]-diazocine solution: preparation concentration from 0.12mg / ml to 0.03 The mg / ml gradient decreases.

[0068] 3. PBS preparation: KCl 0.2g / l; KH 2 PO 4 0.2g / l; NaCl 8.0g / l; NaCl 2 HPO 4 .7H 2 O 1.56 g / l. D-Hanks solution: KCl 0.4g / l; KH 2 PO 4 0.06g / l; NaCl 8.0g / l; NaCl 2 HPO 4 .7H 2 O0.06g / l; NaHCO 3 0.35g / l; phenol red 0.02g / l.

[0069] MTT preparation: the concentration of the preservation solution is 5mg / ml, and the final concentration of the addition is 0.4mg / ml. Sterilize by filtration and store at -70°C. When in use, add MEM medium, make a 1:10 dilution, and filter to sterilize.

[0070] 4. Insert the cells into the ...

Embodiment 3

[0074]How to prove that 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]diazocine can induce tumor cell growth by Example 3 Apoptosis occurs (taking cervical cancer cell Hela as an example).

[0075] 1. Add 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis-(4-phenol)-[1,5]-diazoocine to the culture medium of Hela, the concentration 35ng / ml, incubated for 72 hours.

[0076] 2. In a 1.5ml microcentrifuge tube, centrifuge to pellet 1×10 6 -2×10 6 For Hela cells, wash the cells to be tested twice with PBS, remove the supernatant; add 400 μl cell lysate and 2 μl proteinase K, mix well, incubate in a 37°C water bath for 1 hour, add 2 μl RNase, and incubate for another 1 hour.

[0077] 3. In a desktop centrifuge, centrifuge at 14,000rpm at room temperature for 10 minutes, transfer the supernatant to another clean microcentrifuge tube; use phenol: chloroform = 1: 1, phenol: chloroform: isoamyl alcohol = 25: 24 : 1 solution and chloroform aliquots were extracted once for one hour eac...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention discloses 2, 6-di-(6-mercapto-3-pyridyl)-4, 8-di-(4-phenol)-[1, 5]-diazocine as one new type of diazocine compound and its application in preparing antitumor and anti-fungus medicine. The compound of the present invention has important significance and application foreground in preparing medicine for treating liver cancer, cervical carcinoma, kidney cancer and leukaemia, and the medicine for treating mycotic infection of human, animal and plant.

Description

(1) Technical field [0001] The present invention relates to the application of antitumor and antifungal drugs in biomedical technology, in particular to a novel diazocine compound 2,6-bis-(6-mercapto-3-pyridine)-4,8-bis- (4-phenol)-[1,5]-diazocine, application in the preparation of antitumor and antifungal drugs. (2) Background technology [0002] Myxobacteria are the highest prokaryotic group with complex multicellular behavior and morphogenesis, and play an important role in the study of cell differentiation, development and biological evolution. In recent years, myxobacteria, as a group of microorganisms that can produce abundant secondary metabolites, have received increasing attention. Among prokaryotes, Myxobacteria ranks only behind Actinomycetes and Bacillus in terms of the number of biologically active substances that have been found. At present, more than 600 biologically active substances have been found from myxobacteria, accounting for about 3.5% of the total ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/551A61P31/10A61P35/00
Inventor 李越中胡玮
Owner SHANDONG UNIV