Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2026
HPLC-FLD guided multimodal chromatographic isolation of pancreatic lipase modulators from Saxifraga tangutica.
СтатьяНазвание и аннотация: Перевод пока не подготовлен
Обработка статьи · этапы, ошибки и управление
Загрузка состояния…
Ошибки и ограничения
История · было → стало
Состояние обновляется каждые 5 секунд, пока блок открыт. Процент показывается только там, где известен объём работы. Пауза останавливает продолжение этапа; текущий запрос к источнику может завершиться.
Liu Chuang, Ma Jianbin, Zhao Qin, Du Yurong, Dang Jun
Аннотация
BACKGROUND: Translating biological recognition into chromatographic information that can continuously guide targeted isolation remains challenging in natural products.
METHODS: HPLC coupled with fluorescence detection (HPLC-FLD) was combined with multimodal preparative chromatography to recognize, track, and isolate candidate pancreatic lipase (PL)-affinity ligands from Saxifraga tangutica. Their effects on PL were evaluated by activity and kinetic assays, with DFT calculations and molecular docking as complementary analyses.
RESULTS: Three flavonoid glycosides with chromatographic purities above 95% were isolated: Q3XG (160.8 mg), Q3AG (167.9 mg), and Q3GG (623.1 mg). Q3XG activated PL with an EC₅₀ of 4.78 ± 0.95 μg/mL, whereas Q3AG and Q3GG inhibited PL with IC₅₀ values of 38.33 ± 1.97 and 43.86 ± 2.87 μg/mL, respectively. Kinetic analysis showed that Q3XG decreased the apparent Km and slightly increased the apparent Vmax, whereas Q3AG and Q3GG showed the opposite changes, consistent with mixed-type inhibition. DFT and docking analyses indicated differences in electronic properties and predicted PL-ligand interaction patterns.
CONCLUSION: Integration of HPLC-FLD with multimodal chromatography preserved the link between affinity signals and target peaks throughout chromatographic tracking, selectivity optimization, and preparative isolation, providing a practical route to functionally validated ligands from complex natural products.
METHODS: HPLC coupled with fluorescence detection (HPLC-FLD) was combined with multimodal preparative chromatography to recognize, track, and isolate candidate pancreatic lipase (PL)-affinity ligands from Saxifraga tangutica. Their effects on PL were evaluated by activity and kinetic assays, with DFT calculations and molecular docking as complementary analyses.
RESULTS: Three flavonoid glycosides with chromatographic purities above 95% were isolated: Q3XG (160.8 mg), Q3AG (167.9 mg), and Q3GG (623.1 mg). Q3XG activated PL with an EC₅₀ of 4.78 ± 0.95 μg/mL, whereas Q3AG and Q3GG inhibited PL with IC₅₀ values of 38.33 ± 1.97 and 43.86 ± 2.87 μg/mL, respectively. Kinetic analysis showed that Q3XG decreased the apparent Km and slightly increased the apparent Vmax, whereas Q3AG and Q3GG showed the opposite changes, consistent with mixed-type inhibition. DFT and docking analyses indicated differences in electronic properties and predicted PL-ligand interaction patterns.
CONCLUSION: Integration of HPLC-FLD with multimodal chromatography preserved the link between affinity signals and target peaks throughout chromatographic tracking, selectivity optimization, and preparative isolation, providing a practical route to functionally validated ligands from complex natural products.