Compatibility and stability tests of risperidone with soft-drinks by isothermal titration microcalorimetry

Isothermal titration microcalorimetry has been applied to investigate the compatibility testing of risperidone oral solution with soft-drinks and the interaction with tea tannin such as (–)-epigallocatechin, (–)-epicatechin, theaflavin and their gallates. In aqueous solution, risperidone was exothermically bound to tea tannin with binding affinity (10³–10⁴ M^–1), small enthalpy and entropy changes reflecting van der Waal’s interaction to form an insoluble complex at 1:1 molar ratio. The heat effect of risperidone titrated into soft-drinks containing tannin was exothermic and proportional to the quantity of the complex. While, no significant heat effect was found for risperidone titrated into a pet-bottled water and an infusion of parched barley without tea tannin. These results were agreed with stability testing of risperidone in some soft-drinks by HPLC method.     

Chemical studies of the antioxidant mechanism of theaflavins: radical reaction products of theaflavin 3,3′-digallate with hydrogen peroxide

The objective of the current study is to characterize the reaction products of theaflavin 3,3′-digallate, one of the major characteristic polyphenols of black tea, with hydroxyl radicals generated by hydrogen peroxide, with the aim of gaining insights into specific mechanisms of antioxidant reactions in physiological systems. Two major reaction products were isolated and identified using high-field 1D and 2D NMR spectral analysis. Both of them are A-ring fission products. The observation of these compounds indicates that the A ring rather than the benzotropolone moiety is the initial site for formation of reaction products in the hydrogen peroxide oxidant system.     

Structural identification of mouse fecal metabolites of theaflavin 3,3'-digallate using liquid chromatography tandem mass spectrometry

Black tea consumption has been associated with many health benefits including the prevention of cancer and heart disease. Theaflavins are the major bioactive polyphenols present in black tea. Unfortunately, limited information is available on their biotransformation. In the present study, we investigated the metabolic fate of theaflavin 3,3'-digallate (TFDG), one of the most abundant and bioactive theaflavins, in mouse fecal samples using liquid chromatography/electrospray ionization tandem mass spectrometry by analyzing the MS(n) (n=1-3) spectra. Four metabolites theaflavin, theaflavin 3-gallate, theaflavin 3'-gallate, and gallic acid were identified as the major mouse fecal metabolites of TFDG. Glucuronidated and sulfated, instead of methylated metabolites of theaflavin 3-gallate, theaflavin 3'-gallate, and TFDG were detected and identified as the minor mouse fecal metabolites of TFDG. Our results indicate that TFDG can be degraded in mice. Further studies on the formation of those metabolites in TFDG-treated mice in germ-free conditions are warranted. To our knowledge, this is the first report on the biotransformation of TFDG in mice.     

Significant Inactivation of SARS-CoV-2 In Vitro by a Green Tea Catechin,a Catechin-Derivative,and Black Tea Galloylated Theaflavins

Potential effects of tea and its constituents on SARS-CoV-2 infection were assessed in vitro. Infectivity of SARS-CoV-2 was decreased to 1/100 to undetectable levels after a treatment with black tea, green tea, roasted green tea, or oolong tea for 1 min. An addition of (−) epigallocatechin gallate (EGCG) significantly inactivated SARS-CoV-2, while the same concentration of theasinensin A (TSA) and galloylated theaflavins including theaflavin 3,3′-di-O-gallate (TFDG) had more remarkable anti-viral activities. EGCG, TSA, and TFDG at 1 mM, 40 µM, and 60 µM, respectively, which are comparable to the concentrations of these compounds in tea beverages, significantly reduced infectivity of the virus, viral RNA replication in cells, and secondary virus production from the cells. EGCG, TSA, and TFDG significantly inhibited interaction between recombinant ACE2 and RBD of S protein. These results suggest potential usefulness of tea in prevention of person-to-person transmission of the novel coronavirus.