Teicoplanin Glycopeptide Antimicrobial Antibiotics

English name：Teicoplanin

CAS number：61036-62-2

English synonym:Tagocid;TEIC;Teicoplaninsterile;lyophilisedteicoplanin;TazobactuMSodiuM+PiperacillinSodiuM;TeichoMycin,TeChemicalbookcoplanin,Targocid,TeicoMid,8327A,DL507IT,L12507,MDL507,MW1900;TeicoplanincoMplex;TEICOPLANIN[A(2-1)shown]

Molecular formula：C78H77Cl2N8O32R

Molecular weight：1709.39

EINECS No:1308068-626-2

Teicoplanin properties

Melting point: 310 °C (decomp)

RTECS number :WY1559000

Storage conditions :2-8°C

Solubility: H2O: soluble, 10mg/mL

Morphological:powder

Color :White to light yellow

Water soluble: Slightly soluble in water

CAS database: 61036-62-2

Structural formula:

Summarize

Teicoplanin is a glycopeptide antibiotic produced by the fermentation of actinomycetes. It is a new generation of glycopeptide antibiotics developed after vancomycin. Teicoplanin is currently one of the most promising anti-drug resistant antibiotics in domestic clinic, with stronger fat solubility and longer half-life than vancomycin. It has good body fluid distribution, light adverse drug reactions, can be administered intravenously or muscularly, and is more convenient for application.

Preparation

The invention relates to a preparation method of Teicoplanin. The preparation method is: using Teicoplanin producing bacteria to prepare Teicoplanin, and continuously removing the produced Teicoplanin from the fermentation system during the fermentation process, so that the content of Teicoplanin in the fermentation system is less than 15 mg/L.

Pharmacology and toxicology

Teicoranin is a glycopeptide bactericidal antibiotic produced by actinomycetes fermentation. The mechanism of action is to inhibit the synthesis of cell wall and interfere with the synthesis of new parts in peptidoglycan. The drug binds to the aminoacyl-D-alanylon-D-alanine at the end of the mucopeptide in the cell wall of the bacteria in the dividing and breeding stage, thereby preventing the synthesis of the bacterial cell wall membrane and achieving the inhibition and killing of bacteria. This product is effective against gram-positive aerobic and anaerobic bacteria, including Staphylococcus aureus and coagulase negative staphylococcus (including methicillin-resistant strains), Streptococcus pyogenes, Streptococcus pneumoniae, corynebacterium, Clostridium difficile, digestive streptococcus, etc. This product is not effective against gram-negative bacteria.

Indication

Clinical mainly used penicillin, cephalosporin resistant gram-positive bacteria infection, such as endocarditis, osteomyelitis, sepsis and respiratory tract, urinary tract, skin infection.

Biological activity

Teicoplanin (Teichomycin) is a prophylactic antibiotic.

In vitro study

Teicoplanin is associated with a small increase in gastrointestinal colonizing Candida albicans. The inhibitory effect of Teicoplanin on proteoglycan polymerization but not on nucleic acid and protein synthesis suggests that the effect of the wall is due to the accumulation at this level of soluble precursors of proteoglycan continuously produced by the cell. Teicoplanin, at a concentration of 1mg/ mL, enables rapid dissolution of exponential phase cells of Streptococcus faecalis. Teicoplanin inhibits peptidoglycan synthesis in intact and cell-free systems. The induced cleavage of Teicoplanin is dependent on the addition of antibiotics to the growth phase of B. pumilus. Teicoplanin induced cleavage of Strep. jhecalis CCM 1875 after a long lag stage, which was not very extensive.

In vivo study

In neutropenia mice, Teicoplanin increased survival, while G-CSF treatment did not. Teicoplanin combined with G-CSF improved survival when compared with groups II, III, and IV.

Chemical property

Be soluble in organic solvents such as methanol, ethanol and DMSO.

Security information

WGK Germany:3

Customs code: 294,19,000,000

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