Ultrafiltration coupled with high-performance liquid chromatography and quadrupole-time-of-flight mass spectrometry for screening lipase binders from different extracts of Dendrobium officinale

Abstract

Pancreatic lipase plays essential roles in the digestion, transport, and processing of dietary lipids in humans. Inhibition of pancreatic lipase leading to the decrease of lipid absorption may be used for treating obesity. In the present study, a new approach of ultrafiltration coupled with high-performance liquid chromatography and quadrupole-time-of-flight mass spectrometry was established for rapidly detecting lipase binders from different extracts of medicinal plants. Rutin, a model inhibitor of lipase, was selected to optimize the screening conditions, including ion strength, temperature, pH, and incubation time. Meanwhile, the specificity of the approach was investigated by using denatured lipase and inactive compound emodin. The optimal screening conditions were as follows: ion strength 75 mM, temperature 37 °C, pH 7.4, and incubation time 10 min. Furthermore, linearity, accuracy, precision, and matrix effect of the approach were well validated. Finally, lipase binders were screened from different extracts of Dendrobium officinale by applying the established approach and were subsequently subjected to traditional lipase inhibitory assay. Eleven lipase inhibitors were identified, eight of which, namely naringenine, vicenin II, schaftoside, isoschaftoside, isoquercetrin, kaempferol 3-O-β-D-glucopyranoside, vitexin 2″-O-glucoside, and vitexin 2″-O-rhamnoside, were reported for the first time. In addition, docking experiments were performed to determine the preferred binding sites of these new lipase inhibitors.

Chemical fingerprint and bioactivity evaluation of Globularia orientalis L. and Globularia trichosantha Fisch. & C. A. Mey. using non‐targeted HPLC‐ESI‐QTOF‐MS approach

“…On its behalf, peak 50 ( m / z 445) was tentatively characterised for the first time in G. trichosantha as phenylethyl‐ O ‐β‐ d ‐glucopyranosyl‐β‐ d ‐glucopyranoside which yielded a fragment with m / z 121 corresponding to the phenethyl alcohol. Furthermore, peak 57 was previously described in other plants but not in the studied samples. It has been tentatively characterised as coelovirin A which has a fragmentation pattern depicted in Figure (C).…”

Putative Genes Identified in Alkaloids Biosynthesis in Dendrobium officinale by Correlating the Contents of Main Bioactive Metabolites with Genes Expression between Protocorm-like Bodies and Leaves

“…Furthermore, D. o cinale plays an important role in treating atrophic gastritis, diabetes, cancer, cardiovascular, disease-cataract and delaying aging [3]. Its bioactive components include major D. o cinale polysaccharides (DOPs) [4] and alkaloids [5], and minimal avonoids [6]. DOPs have many pharmacological activities such as curving hypoglycemia [7], antioxidation [8], immunomodulation [9] and anti-tumor.…”

Rapid Screening for α-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration–HPLC-MS

“…Therefore, the ultrafiltration coupled with HPLC-MS (UF-HPLC-MS) method could not only identify numerous interesting and/or novel compounds without tedious prior isolations, but also illustrate the potential biological mechanisms by providing pivotal insights into bio-molecular structures and ligands binding properties with high specificity and sensitivity, which is very powerful for the rapidly screening and identification of potential ligands in natural products at the early drug discovery stage (Katoch et al, 2012; Qin et al, 2015; Chen et al, 2016). A number of researches have referred to this method to screen and identify ligands from complex natural mixtures (Zhu et al, 2013; Li et al, 2015; Qin et al, 2015; Tao et al, 2015; Chen et al, 2016). However, to our best knowledge, UF-HPLC-MS method has not been applied to screen and identify α-glucosidase inhibitors from G. sylvestre , not to say its metabolites.…”