Abstract
AbstractExtracts of Cyclocarya paliurus (CP) leaves, a popular sweet tea, inhibit pancreatic β cell apoptosis and have potent hypoglycemic effects, but the identities of the anti-apoptotic bioactive components are still unknown. In the present study, a method using UPLC-Q-TOF/MS based on serum pharmacochemistry combined with target cell extraction was established to rapidly identify direct-acting pancreatic protectants from CP. After orally administering a set amount of CP extract to rats, blood samples were collected to characterize the components that can be absorbed into the blood using UPLC-Q-TOF/MS. Also, target cells (pancreatic β NIT-1 cells) were incubated with CP extract for 24 hours, and cells were collected to identify the components that can bind to the cells using UPLC-Q-TOF/MS. Finally, to evaluate the protective effect of the bioactive components of CP, MTT and TUNEL assays were performed on treated NIT-1 cell induced by streptozotocin (STZ). Three potential direct-acting pancreatic protectants -- kaempferol, quercetin, quadranoside IV -- were identified, and anti-apoptotic effects of kaempferol and quercetin were confirmed in STZ-induced NIT-1 cells. The findings indicate that this combined approach is a feasible, rapid, and expedient tool for capturing potential direct-acting components from natural products such as those from CP leaves.
Highlights
Cyclocarya paliurus (Batal.) Ijinskaja (Juglandaceae) is a type of tall tree distributed in the highlands of the south and southeast of China [1]
We reported that C. paliurus (CP) exhibited a potent hypoglycemic effect in diabetic mice by inhibiting pancreatic β cell apoptosis via regulating MAPK and Akt signaling pathways [2]; we have continued to uncover the association of CP bioactive components with their biological functions in the present study
We aimed to establish an analytical platform using UPLC-quadrupole timeof-flight (Q-TOF)/MS based on serum pharmacochemistry combined with target cell extraction approaches, in order to rapidly identify potential directacting pancreatic protectants from CP against pancreatic β cell apoptosis
Summary
Cyclocarya paliurus (Batal.) Ijinskaja (Juglandaceae) is a type of tall tree distributed in the highlands of the south and southeast of China [1]. C. paliurus (CP) leaves possess natural sweetness, and local people have long. CP leaves are an herbal medicine of Traditional Chinese medicine (TCM). The properties of “clearing heat and removing toxicity” are recorded in the ancient Chinese pharmacopeia Zhong-hua-ben-cao, and extracts have been widely used as an obesity and diabetes treatment [2, 3]. Based on their dual properties as food and drug, CP herbal teas have been approved as a dietary supplement product by the United States Food and Drug Administration (U.S.FDA) since 1991 [2]. Dietary supplements derived from CP are in great demand among Chinese diabetes patients
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