Metabolite Production
Drug metabolism studies are inextricably linked to many aspects of drug discovery, including the design of candidate compounds and the screening of lead compounds. In vitro metabolism studies can directly observe the selective interaction of candidate compounds with test targets without consuming large amounts of samples and experimental animals, and are fast and easy to perform, suitable for high-throughput screening of candidate compounds with unclear metabolic information. BOC Sciences provides screening, optimization, synthesis and production services for drug candidate metabolites after metabolite identification through metabolic studies. We use recombinant enzymes, liver microsomes or bionic catalysts to scale up the production of metabolites, and then characterized and separated using NMR and chromatography.
Drug Metabolism
Drug metabolism, also known as drug biotransformation, refers to the process of undergoing chemical structural changes in the drug enzyme after the drug is absorbed and distributed in the body. Most drugs undergo metabolic transformation, losing or reducing their activity. However, some drugs have improved activity through metabolic transformation, resulting in more pharmacologically active or more toxic metabolites.
Drug Metabolism Process
- Phase I metabolic reactions
Oxidation, reduction and hydrolysis.
- Phase II metabolic reactions
Conjunction reaction with glucuronic acid, sulfuric acid, and amino acids.
Fig. 1 Drug biotransformation process
In Vitro Methods of Drug Metabolism Studies
Due to the extremely wide distribution of drugs in living organisms and the diversity of organs and enzyme systems for their metabolic transformation, the concentration of drugs and their metabolites in vivo is low, especially for some drugs with high toxic side effects such as anticancer drugs, which are taken in limited doses and have even lower metabolite pairedness, and it is difficult to isolate and detect metabolites directly from plasma, bile and other biological fluids for in vivo metabolic transformation studies. Therefore, the use of in vitro metabolic methods to study metabolic transformation especially in determining the structure of metabolites has received widespread attention.
Nuclear Magnetic Resonance (NMR) Technology
NMR technique can provide direct information on the molecular structure of metabolites, the sample dosage is small, and the determination of one-dimensional spectra takes only 5 min, which is a fast and simple method. The application of 2D-COSY, 2D-NOE spectra provides more information for molecular structure and makes the identification of molecular structure easier. The region of δ0.4~1.7 in the 1H-NMR spectra of human and rat urine is the region with relatively simple signals of endogenous substances, which can be used to observe the CH3, CH2, CH signals of metabolites. In addition, the proton signals in the aromatic hydrogen region at δ6.0~8.5 can also be conveniently used to study the molecular structure of metabolites.
Our Metabolite Production Service
- Production using recombinant enzymes, liver microsomes or bionic catalysts
- Characterization using NMR techniques
- Separation using preparative chromatography
With the help of modern NMR techniques and cryogenically cooled small volume sample units, the amount of purified metabolites in the range of tens to hundreds of micrograms is sufficient for a variety of 1D and 2D NMR experiments.
Our Advantages
- Wide range of bioanalysis
- Compliance with GLP Laboratory Practices
- Standard curves, quality control
Quotation and Ordering
As with all of our live services, we make sure to keep in touch during the study. If you have any special needs or questions about our services, please feel free to contact us to support our experienced experts. We look forward to working with you in the future.