Absorption of angiotensin II antagonists in Ussing chambers, Caco-2, perfused jejunum loop and in vivo:

Boisset, Michel; Botham, Roger P.; Haegele, K. D.; Lenfant, B.; Pachot, Jean I

doi:10.1016/s0928-0987(00)00073-7

Cited by 44 publications

(37 citation statements)

References 20 publications

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“…These results correlate well with the TEER values measured after 120-min exposure to DMSO (10%), which did not result in a decrease of more than 25% of the TEER control value described as the safety limit for transport studies. 18) This indicates that no marked alteration of the Caco2/TC7 cell monolayers occurred with DMSO (10% vol/vol) up to 120-min exposure, which is compatible with permeation assays conducted for new synthesize compounds. However, a recently published study indicated that the use of high concentrations of DMSO (from 4% to 10%) could reduce the transepithelial permeability coefficient of [ 3 H]dexamethasone, underestimating the drug permeability through Caco2 monolayers.…”

Section: Resultssupporting

confidence: 78%

See 1 more Smart Citation

Evaluation of the Cytotoxicity Effect of Dimethyl Sulfoxide (DMSO) on Caco2/TC7 Colon Tumor Cell Cultures.

Violante¹,

Zerrouk²,

Richard³

et al. 2002

Biological & Pharmaceutical Bulletin

204

118

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Section: Resultssupporting

confidence: 78%

“…18) In the present study, we evaluated these to investigate the influence of DMSO on the cell monolayer. A cytotoxic effect of high concentrations of DMSO may induce monolayer disruption and an alteration of cell-to-cell tight junctional complexes.…”

Section: Resultsmentioning

confidence: 99%

Evaluation of the Cytotoxicity Effect of Dimethyl Sulfoxide (DMSO) on Caco2/TC7 Colon Tumor Cell Cultures.

Violante¹,

Zerrouk²,

Richard³

et al. 2002

Biological & Pharmaceutical Bulletin

204

118

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“…The P lumen for glabridin (6.51-11.54 ϫ 10 Ϫ4 cm/s at substrate concentrations of 0.1-2.0 M) was higher than that of verapamil (3.07 ϫ 10 Ϫ5 cm/s) (Johnson et al, 2003), lidocaine (7.5 ϫ 10 Ϫ5 cm/s) (Berggren et al, 2004), and RU60079 (a novel angiotensin II antagonist; 1.4 ϫ 10 Ϫ6 cm/s) (Boisset et al, 2000), but lower than that of warfarin (7.7 ϫ 10 Ϫ3 cm/min) (Okudaira et al, 2000). The much lower P blood (approximately 7-fold) than P lumen of glabridin indicated extensive intestinal efflux and/or gut metabolism.…”

Section: Discussionmentioning

confidence: 88%

Role of P-glycoprotein in the Intestinal Absorption of Glabridin, an Active Flavonoid from the Root ofGlycyrrhiza glabra

Cao¹,

Chen²,

Liang³

et al. 2007

Drug Metab Dispos

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ABSTRACT:Glabridin is a major constituent of the root of Glycyrrhiza glabra, which is commonly used in the treatment of cardiovascular and central nervous system diseases. This study aimed to investigate the role of P-glycoprotein (PgP/MDR1) in the intestinal absorption of glabridin. The systemic bioavailability of glabridin was approximately 7.5% in rats, but increased when combined with verapamil. In single-pass perfused rat ileum with mesenteric vein cannulation, the permeability coefficient of glabridin based on drug disappearance in luminal perfusates (P lumen ) was approximately 7-fold higher than that based on drug appearance in the blood (P blood ). There is an increasing consumption of herbal medicines in recent years in Asian and Western countries. Their incorporation into the medical care system has been encouraged by the World Health Organization despite the lack of evidence for the efficacy of most herbal drugs. Herbal medicines are usually orally administered with longterm regimens. However, the nature of intestinal absorption of the major ingredients of most herbal medicines is unknown, probably because of a lack of sensitive analytical methods, difficulties in the choice of marker components, and difficulties in the establishment and validation of efficient study models. The widely used traditional Chinese medicine, the root of Glycyrrhiza glabra (licorice), is one of the most commonly used herbal medicines in the world because of its exceptional pharmacological properties recognized by traditional Chinese medicine (Zhu, 1998). Licorice has been used as antidotes,We appreciate the financial support provided by the Australian Institute of Chinese Medicine (Grants R-106-00257 and R-106-00282).J.C., X.C., and J.L. contributed equally to this work. Article, publication date, and citation information can be found at http://dmd.aspetjournals.org. doi:10.1124/dmd.106.010801. ABBREVIATIONS:PgP, P-glycoprotein; MDR, multidrug resistance; MRP, multidrug resistance-associated protein; MDCK, Madin-Darby canine kidney; HPLC, high performance liquid chromatography; HBSS, Hanks' balanced salt solution; DMSO, dimethyl sulfoxide; UDPGA, uridine diphosphate glucuronic acid; 711),vinyl]phenyl]-(2-dimethylcarbamoylethylsulfanyl)methylsulfanyl] propionic acid; LC-MS, liquid chromatography-mass spectrometry; MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazonium bromide; PBS, phosphate-buffered saline; IS, internal standard; TEER, transepithelial electric resistance; AP, apical; BL, basolateral; t 1/2␤ , elimination half-life; ABC, ATP-binding cassette; AUC, area under the plasma concentration-time curve; C max , maximum plasma concentration; CL, clearance; V d , volume of distribution; F, systemic bioavailability; P lumen , permeability calculated based on the disappearance of the drug from the intestinal lumen; P blood , permeability calculated based on appearance of the drug in the blood; P app , apparent permeability coefficient; K m , Michaelis-Menten

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“…cm/s at 2.0 g/ml) were higher than those for verapamil (3.07 ϫ 10 Ϫ5 cm/s) (Johnson et al, 2003), lidocaine (7.5 ϫ 10 Ϫ5 cm/s) (Berggren et al, 2004), and RU60079 (a novel angiotensin II antagonist, 1.4 ϫ 10 Ϫ6 cm/s) (Boisset et al, 2000), but lower than that for warfarin (7.7 ϫ 10 Ϫ3 cm/min), a drug absorbed in unchanged form (Okudaira et al, 2000). These data may suggest that CTS is highly and well absorbed.…”

Section: ϫ4mentioning

confidence: 80%

A Mechanistic Study of the Intestinal Absorption of Cryptotanshinone, the Major Active Constituent ofSalvia miltiorrhiza

Zhang¹,

Huang²,

Guan³

et al. 2006

J Pharmacol Exp Ther

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The nature of intestinal absorption of most herbal medicine is unknown. Cryptotanshinone (CTS) is the principal active constituent of the widely used cardiovascular herb Salvia miltiorrhiza (Danshen). We investigated the oral bioavailability of CTS in rats and the mechanism for its intestinal absorption using several in vitro and in vivo models: 1) Caco-2 cell monolayers; 2) monolayers of MDCKII cells overexpressing P-glycoprotein (PgP); and 3) single-pass rat intestinal perfusion with mesenteric vein cannulation. The systemic bioavailabilities of CTS after oral and intraperitoneal administration at 100 mg/kg were 2.05 and 10.60%, respectively. In the perfused rat intestinal model, permeability coefficients based on CTS disappearance from the luminal perfusate (P lumen ) were 6.7-to 10.3-fold higher than permeability coefficients based on drug appearance in venous blood (P blood ). P blood significantly increased in the presence of the P-gP inhibitor, verapamil. CTS transport across Caco-2 monolayers was pH-, temperature-and ATP-dependent. The transport from the apical (AP) to the basolateral (BL) side was 3-to 9-fold lower than that from the BL to the AP side. Inclusion of verapamil (50 M) in both AP and BL sides abolished the polarized CTS transport across Caco-2 cells. Moreover, CTS was significantly more permeable in the BL to AP than in the AP to BL direction in MDCKII and MDR1-MDCKII cells. The permeability coefficients in the BL to AP direction were significantly higher in MDCKII cells overexpressing PgP. These findings indicate that CTS is a substrate for PgP that can pump CTS into the luminal side.

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Absorption of angiotensin II antagonists in Ussing chambers, Caco-2, perfused jejunum loop and in vivo:

Cited by 44 publications

References 20 publications

Evaluation of the Cytotoxicity Effect of Dimethyl Sulfoxide (DMSO) on Caco2/TC7 Colon Tumor Cell Cultures.

Evaluation of the Cytotoxicity Effect of Dimethyl Sulfoxide (DMSO) on Caco2/TC7 Colon Tumor Cell Cultures.

Role of P-glycoprotein in the Intestinal Absorption of Glabridin, an Active Flavonoid from the Root ofGlycyrrhiza glabra

A Mechanistic Study of the Intestinal Absorption of Cryptotanshinone, the Major Active Constituent ofSalvia miltiorrhiza

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