Abstract

Context. Polygoni Multiflori Radix (PMR) is originated from the root of Polygonum multiflorum Thunb. and used in oriental countries for centuries. However, little researches pay close attention to the absorption of its major constituents. Objective. Transepithelial transport of TSG, RL, PL, and four anthraquinones is carried out. Materials and Methods. Caco-2 cell monolayer, which represented a well-established model for the study of intestinal transport of nutrients and xenobiotics, was used in this paper. Results. The apparent permeability coefficients (P app) in the Caco-2 cell monolayers were TSG (2.372 × 10−9) < EG (2.391 × 10−9) < EN (2.483 × 10−9) < PL (4.917 × 10−9) < RN (1.707 × 10−8) < RL (1.778 × 10−8) < AE (1.952 × 10−8). Thus, RN, RL, and AE were considered partly absorbed, while other constituents were hardly absorbed. Discussion and Conclusion. Glycosides showed poor permeabilities than aglycones. In the meantime, TSG and EN gave out poor recovery rates in this assay, which indicated that TSG and EN may accumulate or metabolise in the Caco-2 cells. In silico prediction indicated that Gibbs energy (r = 0.751, p < 0.05) and heat of form (r = 0.701, p < 0.05) were strongly positively correlated with P app.

Highlights

  • Polygoni Multiflori Radix ((PMR), heshouwu in Chinese) and Polygoni Multiflori Radix Praeparata ((PMRP), zhiheshouwu in Chinese) are originated from the root of Polygonum multiflorum Thunb. (Polygonaceae) and used in the treatment of nonalcoholic fatty liver disease (NAFLD) and hyperlipidemia in oriental countries for centuries (Figure 1).Preliminary researches [1,2,3,4] indicate that Polygoni Multiflori Radix mainly contains stilbene glycosides (2,3,5,4󸀠tetrahydroxystilbene-2-O-β-D-glucoside (TSG), resveratrol (RL), polydatin (PL), and others) and anthraquinones (emodin (EN), rhein (RN), aloe-emodin (AE), emodin-8O-β-D-glucopyranoside (EG), and others)

  • The integrity of Caco-2 cell monolayer was evaluated by transepithelial electrical resistance (TEER) value between AP side and BL side on alternate days through the 21-day culture period (Figure 3)

  • We could affirm that TSG is the main lipid regulation ingredient of PMR

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Summary

Introduction

Polygoni Multiflori Radix ((PMR), heshouwu in Chinese) and Polygoni Multiflori Radix Praeparata ((PMRP), zhiheshouwu in Chinese) are originated from the root of Polygonum multiflorum Thunb. (Polygonaceae) and used in the treatment of nonalcoholic fatty liver disease (NAFLD) and hyperlipidemia in oriental countries for centuries (Figure 1).Preliminary researches [1,2,3,4] indicate that Polygoni Multiflori Radix mainly contains stilbene glycosides (2,3,5,4󸀠tetrahydroxystilbene-2-O-β-D-glucoside (TSG), resveratrol (RL), polydatin (PL), and others) and anthraquinones (emodin (EN), rhein (RN), aloe-emodin (AE), emodin-8O-β-D-glucopyranoside (EG), and others). Polygoni Multiflori Radix ((PMR), heshouwu in Chinese) and Polygoni Multiflori Radix Praeparata ((PMRP), zhiheshouwu in Chinese) are originated from the root of Polygonum multiflorum Thunb. TSG displayed the most important role in the total cholesterol (TC) lowering effect among all the chemical constituents of Polygonum multiflorum. Little researches pay close attention to the absorption of these major constituents of PMR. Transepithelial transport of TSG, RL, PL, and the four anthraquinones is carried out using human Caco-2 cell monolayer as a model system. Caco-2 cell monolayers represent a well-established model for the study of intestinal transport of nutrients and xenobiotics and are widely used in pharmacology and toxicology researches [6,7,8,9,10]. This research provided important predictive information regarding the oral bioavailability of TSG, RL, PL, EN, RN, AE, and EG

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