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Transport properties of puerarin and effect of Radix Angelicae Dahuricae extract on the transport of puerarin in Caco-2 cell model.
J Ethnopharmacol. 2012 Dec 18; 144(3):677-82.JE

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Angelicae Dahurica (Hoffm.)Benth.& Hook.f.ex Franch.&Sav combined with Pueraria labota (Willd.)Ohwi has been widely used as herb-pairs in traditional Chinese medicine (TCM) for utilization of antipyretic analgesic and anti-inflammatory drugs, and modern pharmacological studies have shown that application compatibility of the two drugs has the effects of cardiovascular disease treatment. The previous study has proved that Radix Angelicae Dahuricae extract could enhance the intestinal absorption of puerarin in Pueraria. But the underlying compatibility mechanism of the two herbs remains unknown. In this study we tried to further evaluate the improvement of Radix Angelicae Dahuricae extract on the puerarin using the Caco-2 cell model and explore the transport properties of puerarin through the above research to discuss the possible effect mechanism of Radix Angelicae Dahuricae extract on the transport of puerarin and the underlying compatibility mechanism of the two herbs.

AIM OF STUDY

The aim of this work was to study the transport properties of puerarin in Radix Pueraria across Caco-2 cell membrane and to explore how the Radix Angelicae Dahuricae extract affected the transport of puerarin using the well-characterized, human-based intestinal Caco-2 cell model as a platform.

MATERIALS AND METHODS

The bidirectional transport, and the effects of time, drug concentration, pH, P-gp inhibitors (Verapamil, Cyclosporin A), MRP inhibitor (MK-571) and EDTA-Na(2) (tight junction modulator) on the absorption of puerarin were observed. Then the influence of extract of Radix Angelicae Dahuricae on the transport of puerarin was studied. Drug concentration was measured by HPLC and the apparent permeability coefficients (Papp) and apparent permeability ratio (PDR) were calculated.

RESULTS AND CONCLUSIONS

The results showed that the transport (Papp) of puerarin in Caco-2 cell monolayer model had time and concentration dependence, and the transport showed saturation characteristics with the time and concentration of puerarin to a certain degree. The Papp of puerarin transported on Caco-2 cell monolayer model was significantly changed when the specified inhibitors of P-gp were added to the model and the PDR decreased from 1.74 to 0.43. The absorption of puerarin was improved when combined with Radix Angelicae Dahuricae. The intestinal absorption of puerarin is by passive diffusion as the dominating process and active transportation was mediated by P-gp and MRP transporter in Caco-2 cell monolayer model, and Radix Angelicae Dahuricae could enhance the intestinal absorption of puerarin.

Authors+Show Affiliations

Key Laboratory of Modern Preparation of TCM, Jiangxi University of Traditional Chinese Medicine, Ministry of Education, Nanchang, 330004, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23085309

Citation

Liang, Xin-Li, et al. "Transport Properties of Puerarin and Effect of Radix Angelicae Dahuricae Extract On the Transport of Puerarin in Caco-2 Cell Model." Journal of Ethnopharmacology, vol. 144, no. 3, 2012, pp. 677-82.
Liang XL, Zhao LJ, Liao ZG, et al. Transport properties of puerarin and effect of Radix Angelicae Dahuricae extract on the transport of puerarin in Caco-2 cell model. J Ethnopharmacol. 2012;144(3):677-82.
Liang, X. L., Zhao, L. J., Liao, Z. G., Zhao, G. W., Zhang, J., Chao, Y. C., Yang, M., & Yin, R. L. (2012). Transport properties of puerarin and effect of Radix Angelicae Dahuricae extract on the transport of puerarin in Caco-2 cell model. Journal of Ethnopharmacology, 144(3), 677-82. https://doi.org/10.1016/j.jep.2012.10.011
Liang XL, et al. Transport Properties of Puerarin and Effect of Radix Angelicae Dahuricae Extract On the Transport of Puerarin in Caco-2 Cell Model. J Ethnopharmacol. 2012 Dec 18;144(3):677-82. PubMed PMID: 23085309.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transport properties of puerarin and effect of Radix Angelicae Dahuricae extract on the transport of puerarin in Caco-2 cell model. AU - Liang,Xin-Li, AU - Zhao,Li-Jun, AU - Liao,Zheng-Gen, AU - Zhao,Guo-Wei, AU - Zhang,Jing, AU - Chao,Yun-Chao, AU - Yang,Ming, AU - Yin,Rong-Li, Y1 - 2012/10/23/ PY - 2012/04/05/received PY - 2012/10/03/revised PY - 2012/10/07/accepted PY - 2012/10/23/entrez PY - 2012/10/23/pubmed PY - 2013/5/10/medline SP - 677 EP - 82 JF - Journal of ethnopharmacology JO - J Ethnopharmacol VL - 144 IS - 3 N2 - ETHNOPHARMACOLOGICAL RELEVANCE: Angelicae Dahurica (Hoffm.)Benth.& Hook.f.ex Franch.&Sav combined with Pueraria labota (Willd.)Ohwi has been widely used as herb-pairs in traditional Chinese medicine (TCM) for utilization of antipyretic analgesic and anti-inflammatory drugs, and modern pharmacological studies have shown that application compatibility of the two drugs has the effects of cardiovascular disease treatment. The previous study has proved that Radix Angelicae Dahuricae extract could enhance the intestinal absorption of puerarin in Pueraria. But the underlying compatibility mechanism of the two herbs remains unknown. In this study we tried to further evaluate the improvement of Radix Angelicae Dahuricae extract on the puerarin using the Caco-2 cell model and explore the transport properties of puerarin through the above research to discuss the possible effect mechanism of Radix Angelicae Dahuricae extract on the transport of puerarin and the underlying compatibility mechanism of the two herbs. AIM OF STUDY: The aim of this work was to study the transport properties of puerarin in Radix Pueraria across Caco-2 cell membrane and to explore how the Radix Angelicae Dahuricae extract affected the transport of puerarin using the well-characterized, human-based intestinal Caco-2 cell model as a platform. MATERIALS AND METHODS: The bidirectional transport, and the effects of time, drug concentration, pH, P-gp inhibitors (Verapamil, Cyclosporin A), MRP inhibitor (MK-571) and EDTA-Na(2) (tight junction modulator) on the absorption of puerarin were observed. Then the influence of extract of Radix Angelicae Dahuricae on the transport of puerarin was studied. Drug concentration was measured by HPLC and the apparent permeability coefficients (Papp) and apparent permeability ratio (PDR) were calculated. RESULTS AND CONCLUSIONS: The results showed that the transport (Papp) of puerarin in Caco-2 cell monolayer model had time and concentration dependence, and the transport showed saturation characteristics with the time and concentration of puerarin to a certain degree. The Papp of puerarin transported on Caco-2 cell monolayer model was significantly changed when the specified inhibitors of P-gp were added to the model and the PDR decreased from 1.74 to 0.43. The absorption of puerarin was improved when combined with Radix Angelicae Dahuricae. The intestinal absorption of puerarin is by passive diffusion as the dominating process and active transportation was mediated by P-gp and MRP transporter in Caco-2 cell monolayer model, and Radix Angelicae Dahuricae could enhance the intestinal absorption of puerarin. SN - 1872-7573 UR - https://www.unboundmedicine.com/medline/citation/23085309/Transport_properties_of_puerarin_and_effect_of_Radix_Angelicae_Dahuricae_extract_on_the_transport_of_puerarin_in_Caco_2_cell_model_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-8741(12)00683-6 DB - PRIME DP - Unbound Medicine ER -