Polyethers Antibiotics (PEs) Hapten Design and Synthesis
Multidrug-resistant (MDR) pathogens are one of the problems faced by the health care system in recent years, and have raised higher requirements for medical workers to identify new drug candidates. After continuous drug screening, carboxyl polyether, also known as polyether antibiotics (PEs), has received extensive attention. Polyether compounds not only have excellent efficacy against a variety of key infectious disease targets (including protozoa, bacteria and viruses), but also show selectivity and high performance against multiple MDR pathogens. At present, although PEs have been widely used in the potential control of drug-resistant bacteria and parasitic infections, the relevant medical chemistry and pharmacokinetic research data is very limited. Creative Biolabs helps customers produce high-quality antibodies by providing polyether hapten design and synthesis services. Our work can help the detection and research of polyether compounds.
Fig.1 Polyether Polyol Structural Formula.
Structure and Classification of PEs
PEs are a class of powerful antibiotics with ionophore properties, which can bind metal ions and promote their transport across cell membranes. This ability stems from its lipophilic external alkyl backbone and oxygen-rich internal cavity that can bind metal ions, making it a useful tool for studying cation transport mechanisms. Polyether antibiotics have anti-insect activity against the six common Eimeria coccidiosis in chickens and are widely used in the breeding industry. However, the excessive addition of such drugs in the feed will cause a series of problems, such as decreased weight gain of broilers, increased water excretion and animal poisoning. Its residues will eventually threaten human health, so the development of methods and tools for the detection of polyether residues is imperative. Common PEs currently include the following:
- Monensin
- Salinomycin
- Maduramicin
- Lasamycin
Monensin (MON), also known as rumensin, is isolated from the fermentation product of Streptomyces cinnamomi and is a representative drug of polyether ionophore compounds. It is generally used in its sodium salt form. MON is mainly used to control chicken, lamb, calf, rabbit coccidiosis and promote ruminant growth. It can affect the ionic balance of the worm body, cause the worm body to rupture and die, and act on the stage of coccidia development to the first generation of schizonts after infection. Monensin can also increase the rate of feed utilization and weight gain by increasing rumen propionic acid production.
Salinomycin (SAL) is a special antibiotic for monocarboxylic acid polyethers, which has a strong inhibitory and killing effect on most gram-positive bacteria and various coccidiformes. It is not easy to develop drug resistance and cross-resistance, and excretes rapidly with a very low residual amount. SAL helps control diarrhea, growth and survival rates in livestock and control coccidiosis in poultry.
Maduramycin (MAD) is a kind of PEs isolated and extracted from the fermentation product of Actinomyces madurai, and its ammonium salt form is generally used. MAD has stronger anticoccidial activity than other PEs, and can effectively control insect strains that are resistant to other polyether ionophores. However, the safe range of its dosage is narrow, and the concentration exceeding 6mg/kg will inhibit the growth.
Lasamycin (LAS) is isolated from the metabolites of Streptomyces salivarius, which is generally used in the form of its sodium salt, which can kill common chicken coccidiosis. LAS mainly kills spores, coccidia at the early and late stages of asexual reproduction.
Creative Biolabs designed and modified the polyether hapten to couple it with proteins to prepare artificial antigens. Subsequently, polyclonal antibodies can be prepared by immunizing rabbits or monoclonal antibodies can be prepared by immunizing mice, cell fusion, screening and cloning culture. The obtained monoclonal antibody or polyclonal antibody is used for the detection of polyether antibiotic residues in samples of animal-derived food.
If you want to inquire more about the design and synthesis of PEs haptens, please contact us.