Mycobacterium tuberculosis resisting compounds, and applications thereof

A technology of mycobacteria and compounds, applied in the field of medicine, can solve the problems of difficult treatment, unsatisfactory cure rate, increased toxicity of therapeutic drugs, etc., and achieve the effect of enhancing antibacterial activity

Inactive Publication Date: 2011-11-23
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Medical practice shows that the treatment of MDR-TB is very difficult, and its treatment time needs at least 18 to 24 months, so the toxic effect of treatment drugs is significantly increased, and the cure rate is not ideal, only 62% [2]

Method used

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  • Mycobacterium tuberculosis resisting compounds, and applications thereof
  • Mycobacterium tuberculosis resisting compounds, and applications thereof
  • Mycobacterium tuberculosis resisting compounds, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 Mycobacterium tuberculosis is to the in vitro drug susceptibility result determination of PDTC and DETC

[0044] (1) Experimental method:

[0045] (1) Inoculation method of Mycobacterium tuberculosis: Get Mycobacterium tuberculosis H37Rv (ATCC 25618) and H37Ra (ATCC25177) bacterial strains, inoculate in containing 10% ADC, 0.5% glycerol and 0.05% Tween 80 (Sigma-Aldrich, St.Louis , MO) in Middlebrook 7H9 medium, cultured at 37°C.

[0046] (2) Determination of the minimum inhibitory concentration (MIC): Inoculate the H37Rv cultured for 2 weeks into 5 ml Middlebrook 7H9 medium containing 10% ADC and 0.5% glycerol (~6.8pH) at a ratio of 1:100, 37 Cultivate for two weeks. At the same time, add PDTC or DETC diluted by 2 times to form a series of concentration gradients. The minimum inhibitory concentration (MIC) was determined by visually observing the size of the cell particles between the cultures with different dilutions of the drug and the control group w...

Embodiment 2

[0051] Embodiment 2: Determination of serum inhibitory titers after oral administration of corresponding compounds in mice

[0052] (1) Experimental method:

[0053] Mice were given corresponding drugs by intragastric administration, respectively 0.2ml sterile water (control), water containing PDTC (100mg / kg) and DETC (100mg / kg) and water containing INH (25mg / kg). After 1 hour, the blood of mice fed with INH was collected; after 2 hours, the blood of mice fed with PDTC and DETC was collected. Since there were 5-6 mice in each drug group, the sera obtained from mice in each group were pooled together. Serial dilutions of serum (1:2 to 1:64) were then prepared in 7H9 medium containing glycerol and ADC. The two-week-old H37Rv was inoculated into serum at a ratio of 1:100. At 1, 2, and 3 weeks after inoculation, the inhibition of bacterial growth in the test tube was observed with the naked eye. Inhibitory titers were determined by colony forming unit counts in Middlebrook 7H1...

Embodiment 3

[0058] Determination of antibacterial activity to growth phase and stationary phase Mycobacterium tuberculosis under embodiment 3 acidic and neutral conditions

[0059]Apply growth phase bacteria cultured for 21 days and old stationary phase bacteria cultured for 67 days, inoculate in liquid culture containing PDTC (20 μM, equivalent to 3.3 μg / ml) or DETC at pH 5.5 (acidic) or 7.0 (neutral) cultured in medium for 3 days. The results showed that after short-term drug exposure, CFU counts of surviving bacteria showed that PDTC had an effect on both growth and stationary phase bacteria under neutral and acidic culture conditions. PDTC and DETC can kill growth phase bacteria under acidic and neutral culture conditions and stationary phase bacteria under neutral culture conditions. In addition, DETC had stronger antibacterial activity than PDTC for stationary bacteria under acidic culture conditions. At neutral pH, PDTC was more active against growth-phase bacteria. In addition,...

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to mycobacterium tuberculosis resisting compounds, and applications thereof. The compounds comprise pyrrolidine dithiocarbamate (PDTC), diethyl dithiocarbamate (DETC) and disulfiram. The compounds have effective in vitro effects in inhibiting and killing mycobacterium tuberculosis. The compounds can be combined with first-line antituberculosis drugs pyrazinamide and rifampicin, and assist in improving the in vitro antibacterial activities of pyrazinamide, and pyrazinamide plus rifampicin. The compounds provided by the invention can effectively acts upon tuberculosis mycobacterium in growing phases and stationary phases. Mycobacterium tuberculosis resisting activities of the compounds can be presented. The compounds can be used in the treatment of drug-sensitive tuberculosis and multi-drug-resistant tuberculosis, and further can be applied in preparations of novel mycobacterium tuberculosis resisting medicines.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new anti-tuberculosis mycobacterium compound and its application. Background technique [0002] Tuberculosis is a major infectious disease caused by Mycobacterium tuberculosis that seriously endangers human health. According to reports, nearly 32% of the world's population (about 2.1 billion) is infected with Mycobacterium tuberculosis. According to data released by the World Health Organization (WHO) in 2007, the number of newly infected tuberculosis patients in the world is 8.8 million every year, reaching the highest level in recent years. my country is the second largest tuberculosis country in the world. More than 1 / 3 of the population is infected by Mycobacterium tuberculosis. There are 2 million infectious tuberculosis patients and 250,000 deaths due to tuberculosis every year. Statistics from the Ministry of Health show that in 2006, the incidence and mor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/21C07C333/16C07C333/32C07C333/20C07C333/14A61K31/40A61K31/325A61K31/145A61K31/27A61P31/06
Inventor 张颖
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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