Intestinal Absorption Profile of Three Polygala Oligosaccharide Esters in Polygalae Radix and the Effects of Other Components in Polygalae Radix on Their Absorption

Abstract

Oligosaccharide esters, which are among the main active components of Polygalae Radix (PR), demonstrate significant pharmacological activities in the human nervous system. In our previous research, some other constituents in PR were able to improve the bioavailability of oligosaccharide esters such as sibiricose A5 (SA5), sibiricose A6 (SA6), and 3,6′-disinapoyl sucrose (DISS), but the related components and their underlying mechanisms remain unknown. The present study aimed to investigate the intestinal absorptive profile of SA5, SA6, and DISS and the absorptive behavior influenced by the coadministration of polygalaxanthone III and total saponins of PR (TS) using an in vitro everted rat gut sac model, along with the possible mechanisms that may influence absorption. The results showed that TS could significantly enhance the absorption of SA5, SA6, and DISS monomers. Verapamil, a P-glycoprotein inhibitor, was able to elevate the absorption of SA5 and SA6, and an absorption experiment using Rho123 led us to conclude that TS influenced the absorption of SA5 and SA6 in a manner similar to that of a P-glycoprotein inhibitor. Sodium caprate, a paracellular absorption enhancer, was found to increase the absorption of SA5, SA6, and DISS. Results showed that the absorption mechanisms of SA5 and SA6 may combine active transport with paracellular passive penetration, while DISS’s absorption was dominated by paracellular passive penetration. However, the relationship between polygala saponins and the absorption of SA5, SA6, and DISS by paracellular passive penetration remain to be examined. This is the direction of our future research.

Characterization and quality evaluation of QiXueShuFu Decoction based on fingerprint and ultra‐performance liquid chromatography‐quadrupole‐orbitrap mass spectrometry

“…The assistant prescription is chosen to enhance the activity of the monarch and the minister, performing a detoxifying activity and the guide prescription helps transport all the active components to the target organs. It was found that the absorption mechanism of 3,6′‐disinapoyl sucrose in the assistant prescription may be a paracellular passive permeation in order to increase the bioavailability of oligosaccharides and enhance the absorption of other components in the body [38]. Isoliquiritigenin in the guide prescription may offset the drug‐induced decrease in cyclooxygenase‐2, contributing to its efficacy as a protector in target organs [39].…”

Comprehensive evaluation of chemical constituents and antioxidant activity between crude and processed Polygalae radix based on UPLC-Q-TOF-MS/MS combined with multivariate statistical analysis

“…Xanthones, a characteristic constituent of the Polygala genus, comprise approximately 30 compounds found in PR and possess pharmacological activities such as antidepressant effects [ 10 ]. Oligosaccharide esters, present in the roots, stems, and leaves of P. tenuifolia , exhibit significant biological activities related to brain protection, anti-dementia, and anti-depression, making them potential candidates for the development of new anti-aging and neuroprotective drugs [ 11 ]. Although numerous chemical and pharmacological studies have been conducted for PR, the difference in chemical compounds and pharmacological activities between the root and root cortex of P. tenuifolia is still unclear.…”

Saponin components in Polygala tenuifolia as potential candidate drugs for treating dementia

“…Traditional plant-based medicinal combinations containing PT, such as Kaixinsan ( Fu et al, 2019 ), Sagacious Confucius’ Pillow Elixir ( Hou et al, 2019 ), and Buyuan Congnao decoction ( Chen et al, 2012a ), have also exhibited pharmacological actions against AD. Regarding its chemical composition, PT contains saponins, sugars and glycosides, polygols, ketones, alkaloids, fatty oils, and resins ( Tian et al, 2015 ; Ba et al, 2019 ; Luo et al, 2024 ), with several of these constituents confirmed to possess anti-dementia properties. Mechanistically, its actions encompass anti-inflammatory ( Zhou et al, 2021 ), antioxidant ( Tang et al, 2022 ), anti-apoptotic ( Choi et al, 2011 ), anti-amyloid beta protein deposition ( Zhao et al, 2015 ), and neurotransmitter regulation ( Lee et al, 2004 ), providing a broad spectrum of interventions.…”