Sustainable Bioactive Salts Fully Composed of Natural Products for Enhanced Pharmaceutical Applicability

Abstract

Phenolic acids are attractive plant-derived bioactive substances owing to their wide range of pharmaceutical properties for the prevention of various human diseases as well as their applications in adjuvant therapy. However, phenolic acids exhibit poor water solubility, which limits their bioavailability and applications. In this study, phenolic acids were combined with matrine to form salts. Matrine is an alkaloid from a traditional Chinese herb that also has abundant pharmaceutical features and was employed to enhance the water solubility and pharmaceutical applicability of phenolic acids. Five bioactive salts, i.e., matrinium syringate, matrinium vanillate, matrinium protocatechuate, matrinium caffeinate, and matrinium gallate, were synthesized and characterized. The results show that all the salts have a hydrogenbonding-stabilized orthorhombic crystal structure and exhibit a synergistic effect between the anions and cations. Compared with their raw materials, the salts display reduced melting points, higher water solubility (several to hundreds of times greater), lower cytotoxicity for normal human cells, as well as better anticancer, antibacterial, antioxidant, and anti-inflammatory capabilities, accompanied by relatively high thermal stability (>140 °C). This indicates that formation of salts by combining phenolic acids and matrine is an effective method for enhancing pharmaceutical applicability, which may be further used to develop new nutrients or drugs.

Water as Green Solvent: Methods of Solubilisation and Extraction of Natural Products—Past, Present and Future Solutions

“…Indeed, such removal could imply additional costly and energy-consuming downstream processing steps such as membrane filtrations [20]. In an ideal situation, salts should remain in the final product not only to simplify the process but also to potentially stabilise the extracted NP or even to enhance its properties (compared to those of the free NP solubilised in water) [21].…”

Adsorption ability of Ga5N10 nanomaterial for removing metal ions contamination from drinking water by DFT

“…The chemical characteristics of natural waters are the reflection of the soils and rocks which have been in contact with water. The quality and quantity of the chemical elements in surface waters is affected by geo‐chemical structure of surrounding area, land use, seasonal variations of weather conditions, vegetation and the atmospheric deposit [1, 2].…”

Improvement of the Thermal Stability and Aqueous Solubility of Three Matrine Salts Assembled by the Similar Structure Salt Formers

“…The formation of salt is similar to the formation of cocrystals, which are complexes formed by the transfer of protons from acidic components to alkaline components and the combination of the active pharmaceutical ingredient (API) and cocrystal formers (CCFs) or salt formers (SFs) through hydrogen bonding [ 23 , 24 , 25 ]. Previous studies have demonstrated that MAT can form salts with acids by proton transfer reaction while maintaining its biological activity [ 26 , 27 ]. Mi et al [ 26 ] formed MAT salts with syringic acid (SYR), vanillic acid (VAN), protocatechuic acid (PRO), caffeic acid (CAF), and gallic acid (GAL).…”

“…Previous studies have demonstrated that MAT can form salts with acids by proton transfer reaction while maintaining its biological activity [ 26 , 27 ]. Mi et al [ 26 ] formed MAT salts with syringic acid (SYR), vanillic acid (VAN), protocatechuic acid (PRO), caffeic acid (CAF), and gallic acid (GAL). The obtained salts showed improved anticancer, antioxidant, and anti-inflammatory properties.…”