Obesity and related metabolic diseases are becoming worldwide epidemics that lead to increased death rates and heavy health care costs. Effective treatment options have not been found yet. Here, based on the observation that baicalin, a flavonoid from the herbal medicine , has unique antisteatosis activity, we performed quantitative chemoproteomic profiling and identified carnitine palmitoyltransferase 1 (CPT1), the controlling enzyme for fatty acid oxidation, as the key target of baicalin. The flavonoid directly activated hepatic CPT1 with isoform selectivity to accelerate the lipid influx into mitochondria for oxidation. Chronic treatment of baicalin ameliorated diet-induced obesity (DIO) and hepatic steatosis and led to systemic improvement of other metabolic disorders. Disruption of the predicted binding site of baicalin on CPT1 completely abolished the beneficial effect of the flavonoid. Our discovery of baicalin as an allosteric CPT1 activator opens new opportunities for pharmacological treatment of DIO and associated sequelae.

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Fluorescent microspheres are widely used as biological tracers. In this study, uniformly sized chitosan microspheres crosslinked with glutaraldehyde (CG microspheres) and formaldehyde (CF microspheres) are successfully prepared by the Shirasu Porous Glass (SPG) membrane emulsification technique. Selectively reduced CG microspheres (SRCG microspheres) are obtained by NaBH4 reduction. These chitosan microspheres are found to exhibit fluorescent properties without conjugation to any fluorescent agent. The fluorescence color varies with different crosslinkers and can be modulated by further chemical reduction, whereas the fluorescence intensity can be controlled by tuning the particle size and degree of crosslinking. The autofluorescence of the microspheres is applied to study the phagocytosis of HepG2 cells using the microspheres as novel tracers. Quantitative and qualitative evaluations show that these chitosan microspheres serve as bright, inert, durable, and extremely photostable tracers.