Study On Polyamine-?cyclodextrin/Mangiferin Inclusion Complex And Cucurbit Uril[n] As Blockers For Uric Acid-Mediated Inflammatory Pathway

Cyclodextrin and its derivatives have been widely used as pharmaceutical carriers in pharmaceutical excipients and carriers.Cyclodextrin utilizes its hydrophobicity in the cavity and the hydrophilicity outside to specifically select some drugs whose size can match to the host and guest.Some drugs that are difficult to dissolve in water and have high bioavailability can greatly enhance the biological activity of these drugs by self-assembly with cyclodextrin.Because?-cyclodextrin has only a little water solubilization,it cannot improve the water solubilization of the drug when it is used as drug carrier and the application range is limited.Therefore,the hydroxypropyl-?cyclodextrin is gradually derived.Various forms of derivatives such as sulfobutylether-?cyclodextrin,and polyamine-?cyclodextrin enhance the water solubilization of the drug.In this paper,four kinds of polyamine-?cyclodextrin were prepared and mixed with the poorly water-soluble mangiferin by saturated aqueous solution method,through ~1H and 2D NMR spectra,powder X-ray diffraction,differential scanning calorimetry and scanning electron microscopy to prove that the inclusion complexes were successfully prepared.The inclusion complexes were characterized to determine the inclusion ratio,inclusion mode,water solubility,and the in vitro assay verified that mangiferin encapsulated with polyamine-?cyclodextrin effectively improved the anticancer application by MTT.Another macrocyclic cavity carrier compound is cucurbit[n]uril which also a good carrier of drugs.The urea of cucurbit[n]uril and its derivatization are also hotspots in the research of supramolecular chemistry.It is widely used in the recognition and self-assembly of host and guest.It differs from the cyclodextrin series of compounds in that cucurbit[n]uril contains have more C=O functional groups and can have better molecular recognition with five-or six-membered rings.Here,we used acyclic cucurbit[n]uril to molecularly recognize uric acid molecules.Uric acid is the main cause of hyperuricemia.The accumulation of uric acid in the human body cannot be metabolized in time,which can cause hyperuricemia and hyperuricemia.It can lead to the formation of gout.Once the tophi was formed,it is generally only possible to remove the stones by surgery in order to eliminate the symptoms of gout attacks.Since uric acid is a nitrogen-containing compound,it can be self-assembled with acyclic cucurbit[n]uril to form a inclusion complex.Therefore,we prepare three acyclic cucurbit[n]urils(ACB)and investigate the inclusion complexation behaviors of ACB with uric acid(UA)via fluorescence spectroscopy,nuclear magnetic resonance.The effect of UA with binding of ACB on the expression of inflammatory biomarkers in human hepatoma HepG2 cells has been examined and the C-reactive protein(CRP)has been characterized by western blot.The results showed that the recognition and tight binding of UA molecules by ACB successfully blocked the inflammatory stimulation of uric acid on HepG2 cells and inhibited the expression of the major inflammatory factor CRP.This could herald a cure for some forms of hyperuricemia.