scholarly journals Alleviating the Intestinal Absorption of Rhein in Rhubarb through Herb Compatibility in Tiaowei Chengqi Tang in Caco-2 Cells

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Ying Peng ◽  
Min Fan ◽  
Chongsheng Peng ◽  
Mengyue Wang ◽  
Xiaobo Li
Keyword(s):  
Intestinal Absorption ◽  
Breast Cancer Resistance Protein ◽  
Critical Role ◽  
Cell Monolayer ◽  
Intracellular Uptake ◽  
Clinical Use ◽  
Cancer Resistance ◽  
Detoxification Mechanism ◽  
Resistance Protein ◽  
Insight Into

Tiaowei Chengqi Tang (TWCQT) is composed of rhubarb, processed liquorice, and Natrii Sulfas, which is used as a purgative in traditional Chinese medicine (TCM). This study focused on the intestinal absorption of rhein in disassembly of the TWCQT extracts through the Caco-2 cell monolayer model to explicate the possible detoxification mechanism of herb-herb compatibility in TWCQT. The results showed that the intestinal absorption of rhein occurred through active diffusion, and rhein might be composed of breast cancer resistance protein (BCRP) substrates. The extract of processed liquorice increased the exclusion rate and reduced intracellular uptake of rhein. The consistent results observed in TWCQT further implied that processed liquorice in TWCQT could suppress the absorption of rhein across the Caco-2 cell monolayer. It has therefore been concluded that the active ingredients of processed liquorice may play a critical role in reducing the intestinal absorption of rhein to alleviate the toxicity of rhubarb in TWCQT. Because of BCRP’s involvement in rhein transport, we conjectured that some components in processed liquorice could inhibit the transport of rhein, possibly by mediating BCRP. These results would provide new insight into this ancient drug combination in toxicity reduction and clinical use.

scholarly journals Characterization of the Intestinal Absorption of Morroniside from Cornus officinalis Sieb. et Zucc via a Caco-2 Cell Monolayer Model

2020 ◽  
Author(s):  
Renjie Xu ◽  
Hongdan Zhu ◽  
Lingmin Hu ◽  
Beimeng Yu ◽  
Xiaohua Zhan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Intestinal Absorption ◽  
Breast Cancer Resistance Protein ◽  
Cell Monolayer ◽  
Biologically Active ◽  
Reverse Direction ◽  
Cancer Resistance ◽  
Cornus Officinalis ◽  
Resistance Protein

AbstractMorroniside is biologically active polyphenols found in Cornus officinalis Sieb. et Zucc (CO) which exhibits a broad spectrum of pharmacological activities, such as protecting nerves, preventing diabetic liver damage and renal damage. However, little data is available regarding its mechanism of intestinal absorption. Here, a human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study on the absorption and transport of morroniside, the effects of time, donor concentration, pH, temperature and inhibitors, the absorption and transport of morroniside were investigated. The bidirectional permeability of morroniside from the apical (AP) to the basolateral (BL) side and in the revese direction was studied. When administrated was set at three tested concentrations (5, 25 and 100μM), the Papp value in AP-to-BL direction was ranged from 1.59 to 2.66×10−6cm/s. In the reverse direction, BL-to-AP, the value was ranged from 2.67 to 4.10 ×10−6cm/s. The data indicated that morroniside transport was both pH- and temperature-dependent. The morroniside’s permeability process affected by treatment with various inhibitors, such as the multidrug resistance protein inhibitors MK571 and benzbromarone, the breast cancer resistance protein inhibitor apigenin. It can be found that the mechanisms of intestinal absorption of morroniside may involve multiple transport pathways like passive diffusion as well as efflux protein-mediated active transport especially the multidrug resistance protein2 and breast cancer resistance protein. After CO was added, PappAB increased significantly by about 125.26%, it can therefore be assumed that some ingredients in the crude material promote morroniside’s absorption in the small intestine.

scholarly journals The role of breast cancer resistance protein (Bcrp/Abcg2) in triptolide-induced testis toxicity

2015 ◽  
Vol 4 (5) ◽  
pp. 1260-1268 ◽  
Author(s):  
Chunzhu Li ◽  
Guozhen Xing ◽  
Kazuya Maeda ◽  
Chunyong Wu ◽  
Likun Gong ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Resistance Protein ◽  
Clinical Use ◽  
Cancer Resistance ◽  
Cumulative Toxicity ◽  
Resistance Protein

Triptolide possesses unique immunosuppressive and anti-tumor activities. However, its clinical use is limited by the cumulative toxicity in the testis and the mechanisms are poorly understood.

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