Glycosylation Modified Natural Products
BOC Sciences offers chemical modification methods for natural products including acetyl methyl peroxide, acetylation and glycosylation. Structural modification of natural products not only increases structural diversity, but also improves activity and bioavailability. Among them, the use of carbohydrate as the sugar base donor for structural modification has a significant effect on improving solubility and antitumor activity. Glycosylation of natural products and drugs can often effectively change the physical and chemical activities of the parent molecules, so the use of carbohydrate groups to glycosylation of natural products is an important means of new drug development. We are good at helping customers to develop natural products from various fields, and help customers to better and faster use products in medicine, daily chemicals and other industries.
Background
Due to their unique chemical structures, natural products have a variety of unique pharmacological activities. Many natural products have been proven to have many activities such as anti-inflammatory and anti-bacterial, anti-viral, antioxidant, anti-malignant, anti-laser radiation and modulation of human immune function, and have been successfully developed for clinical applications. However, only a small percentage of natural products are directly used for the treatment of diseases without modification. This is due to the deficiencies in the physicochemical properties of most natural products, such as solubility and bioavailability, which lead to insufficient druggability; in addition, low pharmacological activity or excessive adverse effects are another major reason why natural products cannot be directly applied to clinical treatment. Through structural modification, we can improve the physicochemical properties, biological activity and reduce the adverse effects of natural products.
Our Services
BOC Sciences' chemistry and biology experts modify the structure of glycosyl side chains, thereby affecting the biological activity, substrate suitability and pharmacological properties of the parent compound. Using chemical and enzymatic methods, our researchers have developed a variety of natural product glycosylation modifications to help our clients better develop the medicinal properties of their natural products.
Glycosylation modification services
- Activation of monosaccharides
Monosaccharides must undergo nucleoside monophosphorylation (NMP) or nucleoside diphosphorylation (NDP) before they can be utilized.
- Structure and action mechanism of glycosyltransferases (GTs)
Glycosyltransferases are key enzymes in the glycosylation process, catalyzing the reaction of NDP sugars and glycosidic ligands to attach glycosyl groups to the N (N-linked glycosylation), O (O-linked glycosylation) or C (C-linked glycosylation), and S (S-linked glycosylation) of the acceptor to complete glycosylation.
Glycosylation side chain modification services
The modification methods are combinatorial biology, GTs modification, in vitro glycan randomization, novel glycan randomization, and glycosyl side chain modification using the reversibility of GTs.
Role of Glycosylation Modified Natural Products
- Increase the water solubility of compounds, hydrophilic sugar derivatives bound to glycosidic ligands can increase the end product.
- The binding of hydrophilic sugar derivatives to the glycoside ligand increases the hydrophilicity of the end product and facilitates the activity.
- Glycosylation is a self-protective mechanism for the producing bacteria, and many macrolide producing bacteria are able to protect themselves by inactivating the products through glycosylation of desosaminyl-2'-OH.
- It affects the reactivity and recognition specificity of natural products, and some glycosylation groups are directly involved in the reaction.
If you have a requirement about our services, please contact us by phone or email, our colleagues will reply to you within three working days.
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