Design and Synthesis of Haptens for Ivermectin

Avermectin (AVM) and ivermectin (IVM) are robust pesticides and acaricides which have been prevalently applied in many fields during the last decades. Ivermectin is a hydrogenated product of AVM B1 and has become one of the best-selling antiparasitic commodities. The hapten is a class of molecules that is too small to be immunogenic in organisms. Sometimes a humoral immune response against haptens is required since antibodies are necessary to be used in the immunodiagnostic system. With rich experience and advanced technologies in antibody development, Creative Biolabs has established a series of powerful, mature platforms to design and synthesize high-quality artificial antigens for challenging projects. Meanwhile, our experts provide custom services and flexible strategies to ivermectin conjugates and are dedicated to assisting clients to stimulate antibody production.

Introduction to Ivermectin

Ivermectin (22,23-dihydroavermectin B1) is a semisynthetic macrocyclic lactone with antiparasitic activity. It is a hydrogenated derivative of AVM (a 16-membered ring macrolide antibiotic) and is produced by soil microorganism Streptomyces avermitilis. The molecule is a new class of broad-spectrum, highly efficient, low-toxicity, and a wide margin of safety antibiotic drugs, with the structure of macrocyclic lactone disaccharide. As neurotoxins, ivermectin acts through the glutamate- or gamma-aminobutyric acid (GABA)-gated chloride channels on nematode neurons and pharyngeal muscle cells, with relatively low toxicity in mammals. The compound has been approved and frequently used at a very low dosage for the control of parasites in many plants and animal species. It has been shown to leave residues in daily foodstuffs, such as vegetables, fruit, milk, and edible animal tissues. Hence, fast, simple, and sensitive analytical methods are needed to reduce and monitor the residues of this antibiotic to ensure public health.

The chemical structure of ivermectin. Fig.1 The chemical structure of ivermectin.

Hapten Design &Synthesis Services at Creative Biolabs

An antigen can be any molecule that binds to the surface receptors of immune system cells and antibodies. An immunogen is a molecule that not only binds to these molecules, but also can stimulate the cell-mediated immune response and the production of antibodies. Preceding studies have demonstrated that if the molecular weight of the small chemical compound is less than 300 Da, an antibody with high quality will be hard or even impossible to generate. Thus, it is necessary to develop haptens for immunization.

Our hapten design workflow. Fig.2 Our hapten design workflow.

There are many target substances, including ivermectin, required to be used in immunotherapy for inducing a humoral immune response. To be able to induce the corresponding immunogenicity in non-immunogenic antigens, Creative Biolabs is dedicated to understanding the mechanism of antibody production and strengthening the research on the hapten preparation for target analytes with super-low molecular weight.

Immunogenic formats of haptens are often prepared by conjugating them with a protein carrier which serves as an immune stimulator. There’re multiple choices of the carrier in our platforms, including but not limited to immunoglobulin fragments, human serum albumin (HSA), bovine serum albumin (BSA), rabbit serum albumin (RSA), keyhole limpet hemocyanin (KLH), etc. In general, the protein carrier is merely regarded as a bulk mass, whose biological activity may be ignored. Ivermectin is a mixture of two homologs (80% B1a and 20% B1b) and both homologs are neurotoxicants and equally potent. This substance is an effective antiparasitic agent introduced to the market as abamectin in animal health. Here, our scientists offer custom development services for hapten design and synthesis by coupling ivermectin to a suitable carrier and linker. Our simplified workflow is displayed in the diagram.

Advantages

  • One-stop hapten preparation services against ivermectin covering from design, synthesis, characterization, and immunizing
  • Sophisticated technicians which have accomplished hundreds of projects for artificial antigen production
  • Cost-effective, time-saving hapten design strategies to ensure the best interests of customers

Because of lacking epitope of haptens, the production of antibodies with high affinity and specificity remains one of the bottlenecks of immunoassays for some small molecules. With extensive expertise in antibody construction, Creative Biolabs has developed efficient, inexpensive platforms to accomplish ivermectin hapten design and synthesis projects. Furthermore, we also provide custom services of specialized anti-hapten antibody development for worldwide customers. If you’re interested in our services, please don’t hesitate to contact us or directly send us an inquiry.

Reference

  1. Krause, K.M.; et al. Aminoglycosides: an overview. Cold Spring Harb Perspect Med. 2016, 6(6): a027029.
All listed services and products are for Research Use Only. Do Not use in any diagnostic or therapeutic applications.

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