Tags

Type your tag names separated by a space and hit enter

Inhibitory Effects of Benzaldehyde, Vanillin, Muscone and Borneol on P-Glycoprotein in Caco-2 Cells and Everted Gut Sac.
Pharmacology. 2018; 101(5-6):269-277.P

Abstract

AIMS

In clinical practice, herbal medicines have played an important role in the modulation of drug transporters through the combination of conventional prescription drugs, which necessitates the elucidation of herb-drug interactions. The present study was designed to investigate the inhibitory effects and mechanisms of benzaldehyde, vanillin, muscone, and borneol on P-glycoprotein (P-gp).

METHODS

The effects of the 4 compounds on the intracellular accumulation of rhodamine-123 (Rho-123) in vinblastine-treated Caco-2 (VB-Caco-2) cells were studied by monitoring fluorescence intensity through a flow cytometry assay, and the effects of these compounds on Rho-123 transport through VB-Caco-2 monolayers and Rho-123 intestinal absorption in the rat everted gut sac were investigated by high-performance liquid chromatography. Moreover, P-gp expression in VB-Caco-2 cells was assessed using flow cytometry and Western blot analysis, and the relative ABCB1 mRNA level was determined by Real-time RT-PCR.

KEY FINDINGS

The results showed that benzaldehyde, vanillin, muscone, and borneol significantly increased Rho-123 uptake in VB-Caco-2 cells, increased the absorption rate and apparent permeability coefficient of Rho-123 in rat jejunum and ileum, and decreased the efflux ratio of Rho-123 from 6.52 to less than 2 during transport across VB-Caco-2 cell monolayers. In addition, these compounds reduced the protein and ABCB1 mRNA levels of P-gp in VB-Caco-2 cells.

CONCLUSIONS

These data indicate that benzaldehyde, vanillin, muscone and borneol could effectively reverse multidrug resistance via inhibiting the P-gp function and expression pathway. The data provide fodder for further investigation into the interaction between the 4 compounds and other drugs transported by P-gp.

Authors+Show Affiliations

Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education/College of Life Science, Northwest University, Xi'an, China.Hospital of Xi'an City, Xi'an, China.Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education/College of Life Science, Northwest University, Xi'an, China.Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education/College of Life Science, Northwest University, Xi'an, China.Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education/College of Life Science, Northwest University, Xi'an, China.Shenzhen Longhua District Central Hospital, Shenzhen, China.Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education/College of Life Science, Northwest University, Xi'an, China.Shenzhen Longhua District Central Hospital, Shenzhen, China.Hospital of Xi'an City, Xi'an, China.Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education/College of Life Science, Northwest University, Xi'an, China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29502118

Citation

Wang, Shixiang, et al. "Inhibitory Effects of Benzaldehyde, Vanillin, Muscone and Borneol On P-Glycoprotein in Caco-2 Cells and Everted Gut Sac." Pharmacology, vol. 101, no. 5-6, 2018, pp. 269-277.
Wang S, Tan N, Ma C, et al. Inhibitory Effects of Benzaldehyde, Vanillin, Muscone and Borneol on P-Glycoprotein in Caco-2 Cells and Everted Gut Sac. Pharmacology. 2018;101(5-6):269-277.
Wang, S., Tan, N., Ma, C., Wang, J., Jia, P., Liu, J., Yang, Y., Xie, Z., Zhao, K., & Zheng, X. (2018). Inhibitory Effects of Benzaldehyde, Vanillin, Muscone and Borneol on P-Glycoprotein in Caco-2 Cells and Everted Gut Sac. Pharmacology, 101(5-6), 269-277. https://doi.org/10.1159/000487144
Wang S, et al. Inhibitory Effects of Benzaldehyde, Vanillin, Muscone and Borneol On P-Glycoprotein in Caco-2 Cells and Everted Gut Sac. Pharmacology. 2018;101(5-6):269-277. PubMed PMID: 29502118.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibitory Effects of Benzaldehyde, Vanillin, Muscone and Borneol on P-Glycoprotein in Caco-2 Cells and Everted Gut Sac. AU - Wang,Shixiang, AU - Tan,Nan, AU - Ma,Cuicui, AU - Wang,Jie, AU - Jia,Pu, AU - Liu,Jianghong, AU - Yang,Yang, AU - Xie,Zhanxiong, AU - Zhao,Kun, AU - Zheng,Xiaohui, Y1 - 2018/03/02/ PY - 2017/08/04/received PY - 2018/01/25/accepted PY - 2018/3/5/pubmed PY - 2018/9/14/medline PY - 2018/3/5/entrez KW - Multidrug resistance KW - Benzaldehyde KW - Borneol KW - Muscone KW - P-glycoprotein KW - Vanillin SP - 269 EP - 277 JF - Pharmacology JO - Pharmacology VL - 101 IS - 5-6 N2 - AIMS: In clinical practice, herbal medicines have played an important role in the modulation of drug transporters through the combination of conventional prescription drugs, which necessitates the elucidation of herb-drug interactions. The present study was designed to investigate the inhibitory effects and mechanisms of benzaldehyde, vanillin, muscone, and borneol on P-glycoprotein (P-gp). METHODS: The effects of the 4 compounds on the intracellular accumulation of rhodamine-123 (Rho-123) in vinblastine-treated Caco-2 (VB-Caco-2) cells were studied by monitoring fluorescence intensity through a flow cytometry assay, and the effects of these compounds on Rho-123 transport through VB-Caco-2 monolayers and Rho-123 intestinal absorption in the rat everted gut sac were investigated by high-performance liquid chromatography. Moreover, P-gp expression in VB-Caco-2 cells was assessed using flow cytometry and Western blot analysis, and the relative ABCB1 mRNA level was determined by Real-time RT-PCR. KEY FINDINGS: The results showed that benzaldehyde, vanillin, muscone, and borneol significantly increased Rho-123 uptake in VB-Caco-2 cells, increased the absorption rate and apparent permeability coefficient of Rho-123 in rat jejunum and ileum, and decreased the efflux ratio of Rho-123 from 6.52 to less than 2 during transport across VB-Caco-2 cell monolayers. In addition, these compounds reduced the protein and ABCB1 mRNA levels of P-gp in VB-Caco-2 cells. CONCLUSIONS: These data indicate that benzaldehyde, vanillin, muscone and borneol could effectively reverse multidrug resistance via inhibiting the P-gp function and expression pathway. The data provide fodder for further investigation into the interaction between the 4 compounds and other drugs transported by P-gp. SN - 1423-0313 UR - https://www.unboundmedicine.com/medline/citation/29502118/Inhibitory_Effects_of_Benzaldehyde_Vanillin_Muscone_and_Borneol_on_P_Glycoprotein_in_Caco_2_Cells_and_Everted_Gut_Sac_ L2 - https://www.karger.com?DOI=10.1159/000487144 DB - PRIME DP - Unbound Medicine ER -