The biological functions of tripeptides are highly dependent on their stereochemical configurations, making the development of rapid and accurate chiral analysis methods crucial for elucidating their structure-activity relationships and promoting their applications. This study developed a direct chiral analysis method based on ion-mobility-mass spectrometry (IM-MS) coupled with a supramolecular complexation strategy, enabling effective discrimination and quantitative analysis of all eight stereoisomers of the tripeptide Ala-Pro-Glu which contains three chiral centers. In this approach, β-cyclodextrin served as the chiral selector and Mg2+ as the bridging ion, forming stable ternary non-covalent complexes [β-CD+Mg + M-H]+ with the target tripeptides in the gas phase. Analysis using trapped ion mobility spectrometry-time-of-flight mass spectrometry (TIMS-TOF-MS) revealed that tripeptides of different chiral configurations led to complexes with significantly different collision cross-section (CCS, ranging from 327.5 to 349.6 Å2) and mobility (1/K0) values, achieving baseline separation for several isomer pairs (with a maximum resolution Rp-p of 2.056). The study further uncovered that complexes of certain isomers (e.g., L-Ala-D-Pro-D-Glu and L-Ala-L-Pro-D-Glu) existed in two stable conformations, displaying an intriguing mirror-symmetric distribution in terms of CCS values, highlighting the subtle control of chirality over gas-phase ion structures. Quantitative analysis demonstrated a good linear response (R2 > 0.99) for typical isomers (e.g., D-Ala-L-Pro-D-Glu and L-Ala-D-Pro-L-Glu) within the concentration range of 3.0–9.0 μM. The established IM-MS supramolecular chiral analysis strategy, requiring no chiral columns or derivatization steps, and provides a powerful and direct analytical platform for the high-throughput chiral identification and quantification of oligopeptides and other bioactive molecules.
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Tian et al. (2026) studied this question.
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