Flavonoid-based Sialylation Inhibitor Development at CD BioGlyco

Flavonoid-based sialylation inhibitor is expected to be an effective target for the treatment of a variety of diseases. At CD BioGlyco, we provide a flavonoid-based sialylation inhibitor development service and also provide assays for the inhibitory activity of the inhibitors.

• Exploration of the mechanism of inhibition of sialylation by flavonoids
  Sialyltransferase is a type II membrane protein with a cytoplasmic tail at the N-terminus, followed by a transmembrane region and a long catalytic domain at the C-terminus. Among other things, the sialic acid motif L facilitates binding to the donor substrate cytidine 5'-monophosphate-N-acetylneuraminic acid (CMP-NeuAc). We utilize kinetic experimental structures to explore the interaction of flavonoids with either the sialic acid motif L or the S region. From there, we test the inhibitory effect of such compounds on sialylation.
• Assay of inhibitory effect of flavonoids
  We use kinetic experiments to determine the inhibitory concentration (IC) values of flavonoids. The core structure of flavonoids contains an a-ring, b-ring, and c-ring, etc. We test the inhibitory activity of flavonoids containing different rings to screen the core structure with an inhibitory effect.
• Evaluation of the inhibitory effect of flavonoid-based sialylation inhibitor
  We use kinetic assays combined with high-performance liquid chromatography (HPLC) to detect the expression activity of sialyltransferase. By comparing the activity of the enzyme with and without the addition of flavonoids, we determine whether these flavonoids are inhibitory.
  We also provide cell models or in vitro assays to further evaluate inhibitor activity.

Fig.1 Flavonoid-based sialylation inhibitor development. (CD BioGlyco)

Publication

Technology: Kinetic testing of the inhibitory effect of flavonoids on sialic acid transferase

Journal: Biochemical and Biophysical Research Communications

IF: 3.1

Published: 2009

Results: Three characteristics of flavonoids with inhibitory activity were identified through structure-inhibitory activity relationships. First, the activity required a double bond between the C2-C3 bonds. Second, increasing the hydrophilicity on the b-ring significantly enhanced the inhibitory activity. Third, the introduction of a hydrophobic functional group on the hydroxyl group of the ring enhanced the inhibitory activity. Then the kinetic analysis carried out by the authors using galactose-I showed that the flavonoids have a mixed inhibitory mechanism. Finally, it was concluded that flavonoids with the above characteristics can be used to control the expression of sialic acid.

Fig.2 Core a represents the main structure of flavone or flavonol derivatives. (Hidari, et al., 2009)

Applications

• Flavonoid-based sialylation inhibitors can be used as lead compounds in the development of targeted drugs.
• Flavonoid-based sialylation inhibitors can be used in studies to control pathological manifestations, such as inflammation and microbial infections.
• Flavonoid-based sialylation inhibitors can be used to develop lead compounds for modifying sialylation in vitro and in vivo.

Advantages

• Our professional R&D team will customize the glycosylation inhibitor development program according to the client's requirements.
• Our responsive and proactive service team anticipates our client's needs and exceeds their expectations to ensure a positive experience and satisfaction.
• We have integrated the world's leading inhibitor research and development technology and developed products with good stability and high quality.

CD BioGlyco provides first-class Glycosylation Inhibitor Development services to our clients and also provides custom development solutions to our clients, each step of the solution has passed the quality test. If you are interested in our services, please feel free to contact us.