Thermosensitive transient receptor potential vanilloid 2 (thermoTRPV2) is a nonselective Ca ²⁺ ‐permeable cation channel broadly expressed, and is implicated in the pathology of diseases such as diabetes and pancreatitis. However, the physiological and pharmacological functions of TRPV2 channels have not been extensively investigated because of the absence of specific modulators. In this study, we report a pair of natural coumarin derivative enantiomers (−)‐murraxocin (B304‐1) and (+)‐murraxocin (B304‐2) from Murraya exotica for their selective inhibition of TRPV2 channels expressed in HEK293 cells and native TRPV2 currents in differentiated brown adipocytes. Whole‐cell patch clamp recordings confirmed the enantiomers B304‐1 and B304‐2 could selectively inhibit the agonist mediated activation of TRPV2 current with IC ₅₀ values of 22.2 ± 7.8 μM and 3.7 ± 0.7 μM, respectively. Molecular docking and site‐directed mutagenesis revealed a key residue I600 of TRPV2 critical for the binding of the enantiomers. Furthermore, B304‐1 and B304‐2 significantly reversed TRPV2 agonist‐induced inhibition of mouse brown adipocyte differentiation. Taken together, our identification of two natural coumarin enantiomers provides valuable tools and chemical leads for further elucidation of TRPV2 channel function, and pharmacological modulation of thermoTRPV2 in brown adipocytes may represent a new therapeutic strategy for treatment of energy imbalance or metabolic disorders.

CARA can monitor lipase activity through hydrolyzing the ester bond to interrupt the FRET process.

Hydrogen sulfide has been shown to play important regulatory roles in more and more physiological and pathological processes. Therefore, it is necessary to develop highly sensitive, selective and reliable probes for detecting hydrogen sulfide to reveal its specific role in the progression of certain diseases. Here, a novel ratiometric fluorescent probe for imaging hydrogen sulfide was designed by connecting the azide group with the N-methylquinoline quaternary ammonium salt through a styrene group. This probe has high selectivity and good sensitivity, and can image the changes of endogenous hydrogen sulfide in living cells.

A fluorescent probe that was designed based on the 6-amino chromone fluorophore for detecting H₂S can distinguish H₂S from Cys/GSH under acidic conditions.