Schisandrin B: A dual inhibitor of P-glycoprotein and multidrug resistance-associated protein 1

Sun, Meng; Xu, Xiaoli; Lu, Qinghua; Pan, Qiangrong; Hu, Xun

doi:10.1016/j.canlet.2006.03.009

Cited by 68 publications

(50 citation statements)

References 33 publications

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“…This communication, combined with our previous reports [13,16,17,18,22,23], provides evidence that Sch B can protect Dox-induced acute and chronic cardiotoxicity and enhancing its anticancer activity.…”

Section: Discussionsupporting

confidence: 78%

“…This could substantially limit the drug penetration and ultimately significantly reduce Dox and Sch B concentration in 4T1 tumor. Considering the dose-dependent characteristics (the least effective concentrations of both Dox and Sch B) [17,18,22,23], the enhancing effect by Sch B could be abolished. Nevertheless, Sch B combined with Dox significantly reduced spontaneous metastatic foci in lung.…”

Section: Discussionmentioning

confidence: 99%

“…S180 or 4T1 cells were seeded at a density of 5610 3 cells/well in 96-well plates and incubated with Dox of indicated concentration in the presence or absence of 50 mM Sch B as described by us previously [16,17,18,22,23]. At 72 hours after plating, MTT assays were performed according to the manufacturer's instructions.…”

Section: Cell Proliferation Assaymentioning

confidence: 99%

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235 Schisandrin B prevents doxorubicin-induced chronic cardiotoxicity and enhances its anticancer activity in vivo

Hu¹,

Xu²,

Sun³

et al. 2010

European Journal of Cancer Supplements

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Section: Discussionsupporting

confidence: 78%

Section: Discussionmentioning

confidence: 99%

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235 Schisandrin B prevents doxorubicin-induced chronic cardiotoxicity and enhances its anticancer activity in vivo

Hu¹,

Xu²,

Sun³

et al. 2010

European Journal of Cancer Supplements

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“…It has shown that several constituents isolated from S. sphenanthera can interact with CYP3A and/or P-glycoprotein (P-gp) [1][2][3][4]. Tacrolimus (FK506) is a widely used immunosuppressive drug in various solid-organ transplantations and is co-medicated with multiple drugs under clinical conditions [5,6].…”

Section: Introductionmentioning

confidence: 99%

Effects of Schisandra sphenanthera extract on the pharmacokinetics of midazolam in healthy volunteers

Xin

et al. 2009

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Schisandra sphenanthera extract (SchE) and tacrolimus are often co-administered in treating renal and liver transplant recipients in China.• Our previous study has demonstrated that SchE can increase the oral bioavailability of tacrolimus. WHAT THIS STUDY ADDS• The results of this study show that SchE can markedly increase the blood concentration and oral bioavailability of midazolam in healthy volunteers.• This finding suggests that SchE may be an inhibitor of CYP3A and is likely to alter the disposition of drugs that are metabolized by CYP3A. AIMSTo assess the effect of Schisandra sphenanthera extract (SchE) on the pharmacokinetics of midazolam, a probe drug of CYP3A, and its metabolite 1′-hydroxy midazolam in healthy volunteers. METHODSTwelve healthy male volunteers were orally treated with SchE, three capsules twice daily for 7 days. Pharmacokinetic investigations of oral midazolam administration at 15 mg were performed both before and at the end of the SchE treatment period. The plasma midazolam and 1′-hydroxy midazolam concentrations were determined by high-performance liquid chromatography-tandem mass spectrometry. Estimated pharmacokinetic parameters before and with SchE were calculated with noncompartmental techniques. RESULTSFollowing administration of SchE, the average increases (%) of individual increases in AUC, AUMC and Cmax of midazolam were 119.4% [95% confidence interval (CI) 83.9, 155.0], 183.4% (95% CI 120.5, 246.2) and 85.6% (95% CI 14.4, 156.9), respectively (P < 0.01 or 0.05). On average, there was a 133.3% (95% CI 8.9, 257.7) increase in midazolam tmax (P < 0.01). The average decrease (%) in CL/F was 52.1% (95% CI 44.9, 59.4) (P < 0.01). No significant changes were seen in midazolam half-life. After co-administration of SchE, the average increase (%) in tmax of 1′-hydroxy midazolam was 150.0% (95% CI 22.2, 277.8) (P < 0.05). No significant differences were observed in the other pharmacokinetic parameters of 1′-hydroxy midazolam. CONCLUSIONSSchE can markedly increase the oral bioavailability of midazolam in healthy volunteers. SchE is an inhibitor of CYP3A and has a high susceptibility to alter the disposition of drugs metabolized by CYP3A.

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“…Analysis of the chemical composition of Schisandra chinensis demonstrated that the biologically active compounds are dibenzocyclooctadiene lignans, which have revealed a wide variety of active effects including antihepatotoxic (Chiu et al, 2003;Ip et al, 2000;Hikino et al, 1984), antioxidant and detoxificant (Ip et al, 1995;Ip & Ko, 1996;Mak et al, 1997;Chiu et al, 2005), anticancer (Wu et al, 2004), and anti-amnestic activities (Kim et al, , 2006. Recently, dibenzocyclooctadiene lignans were reported to reverse cancer drug resistance by targeting P-glycoprotein (P-gp) (Pan et al, 2005(Pan et al, , 2006Wan et al 2006), multidrug resistance-associated protein 1 (MRP1) (Li et al, 2007;Sun et al, 2007), and enhancing apoptosis (Li et al, 2006). Schisandrin C, as one of the important active dibenzocyclooctadiene lignans of Schisandra chinensis (Figure 1), has been used as a liver protective drug (Kiso et al, 1985).…”

Section: Introductionmentioning

confidence: 99%

Activity of Schisandrin C Isolated fromSchisandra chinensisagainst Human Cancer Cell Lines

Lü

Liang

Wei

et al. 2008

Pharmaceutical Biology

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Schisandrin C, a dibenzocyclooctadiene lignan isolated from the fruits of Schisandra chinensis (Turcz.) Baill. (Schisandraceae), was investigated for cytotoxicity and influence on three human cancer cell lines. Among human hepatocelluar carcinoma cells (Bel-7402), human breast cancer cells (Bcap37) and human nasopharyngeal carcinoma cells (KB-3-1), Bel-7402 cells were most sensitive with IC 50 equal to 81.58 ± 1.06 µM after treatment with schisandrin C for 48 h. Cytotoxicity of schisandrin C on tumor cells depends on cellular accumulation of the drug. The intracellular schisandrin C concentration was assayed by high-performance liquid chromatography (HPLC) and showed that schisandrin C could permeate the cell membrane. Staining with Hoechst 33258 showed fragmentation and condensation of chromatin in the cell treated with 75 µM schisandrin C for 24 h. Flow cytometric analysis was performed to determine hypodiploid cells. The results of flow cytometry indicated that the percentage of hypodiploid Bel-7402 cells was 40.61 ± 1.43% after 24 h treatment with 100 µM schisandrin C. The treatment resulted in the appearance of a hypodiploid peak (sub-G 0 /G 1 region), probably due to the presence of apoptosing cells and apoptotic bodies with DNA content less than 2n. To our knowledge, this is the first report against human hepatocelluar carcinoma cells (Bel-7402) of schisandrin C.

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Schisandrin B: A dual inhibitor of P-glycoprotein and multidrug resistance-associated protein 1

Cited by 68 publications

References 33 publications

235 Schisandrin B prevents doxorubicin-induced chronic cardiotoxicity and enhances its anticancer activity in vivo

235 Schisandrin B prevents doxorubicin-induced chronic cardiotoxicity and enhances its anticancer activity in vivo

Effects of Schisandra sphenanthera extract on the pharmacokinetics of midazolam in healthy volunteers

Activity of Schisandrin C Isolated fromSchisandra chinensisagainst Human Cancer Cell Lines

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