A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1H-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR) HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin). This research provides useful clues for further design and discovery of anti-diabetic agents.
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Self-emulsifying drug delivery system (SEDDS) is a kind of solid or liquid formulation composed of drugs, oil,
surfactant and cosurfactant. It could form a fine emulsion (micro/nano) in the gastrointestinal tract after oral
administration. Later on, the formed emulsion is absorbed through the lymphatic pathway. The oral bioavailability of
drugs in SEDDS would be improved for bypassing the first-pass effect of the liver. Therefore, SEDDS has become a vital
strategy to increase the oral bioavailability of poor water-soluble drugs. In addition, there is no aqueous phase in SEDDS,
thus SEDDS is a homogeneous system, consequently being suitable for large-scale production and more stable than
conventional emulsion. However, the role of formulation aspects in the biological property of SEDDS is not fully clear. In
order to prepare the satisfying SEDDS to improve oral drug bioavailability, we need to fully understand the various
factors that affect the in vivo behavior of SEDDS. In this review, we would explore the role of ingredient (drugs, oils,
surfactant and cosurfactant) of SEDDS in increasing oral drug bioavailability. We would also discuss the effect of
physicochemical property (particle size and Zeta potential) of SEDDS on the oral drug bioavailability enhancement. This
review would provide an approach to develop a rational SEDDS to improving oral drug bioavailability.
The strategy of stereodivergent reactions on racemic mixtures (stereodivergent RRM) was employed for the first time in intramolecular benzoin reactions and led to the rapid access of chromanones/flavanones with two consecutive stereocenters. The easily separable stereoisomers of the products were obtained with moderate to excellent enantioselectivities in a single step. Catechol type additives proved crucial in achieving the desired diastereo- and enantioselectivities.
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