Structural Modifications of Active Ingredients in Herbal Medicines

Inquiry

The chemical composition of herbal medicines is diverse and complex and also has a certain degree of structural novelty, but often poor pharmacokinetic properties affect its drugability, so it can be used as a good lead compound for further chemical modification to improve drugability and enhance the application value of herbal chemical components. To improve the physicochemical properties, enhance the biological activity or reduce the toxicity of the active ingredients of herbal medicines, and obtain new active ingredients with high biological activity, high bioavailability, and low adverse effects, Lifeasible can structurally modify the active ingredients extracted and isolated from herbal medicines to help you carry out one of the essential elements of drug research and development.

Structural modifications of mangiferin

The pharmacological activity of mangiferin is extensive, but its pharmacological action is limited mainly by its low transmembrane permeability. To improve its transmembrane permeability, we can chemically modify the structure of mangiferin to obtain new highly lipid-soluble derivatives.

Structural modification of costunolide and dehydrocostus lactone

Radix aucklandiae is a traditional herb, but because its active ingredient is not very potent, it cannot yet be used directly as a medicine. We can modify the structure of costunolide to increase its biological activity significantly.

Structural modification of berberine

Berberine belongs to the group of alkaloids and has a wide range of physiological functions. We can modify it by linking the nitrogen atom to ether and ester groups, which can increase its activity.

Structural modifications of gastrodin and gastrodigenin

The physiological and biochemical properties of gastrodin and gastrodigenin are numerous but not very active. We can structurally modify the phenolic hydroxyl groups by introducing different groups.

Structural modification of ginsenoside

Several structural modifications of ginsenoside with enhanced anticancer biological activity can be obtained by esterification, alkylation, sulphation, oxidation, and catalytic hydrogenation.

Structural modifications of paclitaxel

Paclitaxel plays a vital role in the field of anti-tumor drugs, and the development of well-soluble paclitaxel precursors with enhanced biological activity is our primary goal for structural modification.

Structural modification of vinblastine (VBL) and vincristine (VCR)

VBL and VCR are drugs with anti-tumor activity, and we have been able to significantly enhance their anti-tumor biological activity by appropriately modifying the catharanthine ring.

Structural modification of artemisinin

Artemisinin has good efficacy in treating malaria and has low adverse effects, but its poor hydrophilicity and lipophilicity make it difficult to formulate into suitable dosage forms, which can be overcome by structural modification.

Chemical methods have been the first choice for structural modification of active ingredients in herbal medicines because they are relatively simple and the process is relatively mature. In recent years, biotransformation methods have also been increasingly used. In addition to this, Lifeasible allows structural modification and structural optimization of different herbal chemical components based on different activities, which can improve their targeting and efficacy to improve the physicochemical properties of the herb, increase its biological activity or reduce its adverse effects while we care whether the method is environmentally friendly. Please feel free to contact us to submit your request for structural modification of your target.

For Research Use Only. Not For Clinical Use.