&lt;i&gt;In vitro&lt;/i&gt; evidence of baicalein’s inhibition of the metabolism of zidovudine (AZT)

Wang, Yu-Cun; Yang, Haiyan; Kong, Lingting; Yu, Fenglei

doi:10.4314/ahs.v14i1.26

Cited by 2 publications

(1 citation statement)

References 10 publications

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“…It also detoxifies drugs because glucuronidated metabolites possess less activity or toxicity than their parent forms [ 8 ]. Many cases of UGT inhibition-mediated drug interactions have been reported [ 5 , 7 ] including UGT1A1 inhibition by psoralidin that causes irinotecan’ toxicity [ 9 ], UGT1A3 inhibition by gemfibrozil that enhances susceptibility of statins [ 10 ], UGT1A6 inhibition by silybin that attenuates fenofibrate-induced UGT1A6 [ 11 ], UGT1A6 inhibition by phenobarbital and phenytoin that causes hepatotoxicity of acetamoniphen [ 12 , 13 ], UGT1A9 inhibition by mefenamic acid that changes exposure of dapagliflozin’s metabolite [ 14 ], and UGT2B7 inhibition by valproic acid that changes efficacy and toxicity of zidovudine [ 15 ]. Regulatory agencies have recognized the importance of UGT-mediated drug interactions in drug discovery research and patients’ safety [ 2 , 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity

2018

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Herb–drug interaction (HDI) limits clinical application of herbs and drugs, and inhibition of herbs towards uridine diphosphate (UDP)-glucuronosyltransferases (UGTs) has gained attention as one of the important reasons to cause HDIs. Sauchinone, an active lignan isolated from aerial parts of Saururus chinensis (Saururacease), possesses anti-oxidant, anti-inflammatory, and anti-viral activities. In pharmacokinetics of sauchinone, sauchinone is highly distributed to the liver, forming extensive metabolites of sauchinone via UGTs in the liver. Thus, we investigated whether sauchinone inhibited UGTs to explore potential of sauchinone–drug interactions. In human liver microsomes (HLMs), sauchinone inhibited activities of UGT1A1, 1A3, 1A6, and 2B7 with IC50 values of 8.83, 43.9, 0.758, and 0.279 μM, respectively. Sauchinone also noncompetitively inhibited UGT1A6 and 2B7 with Ki values of 1.08 and 0.524 μM, respectively. In in vivo interaction study using mice, sauchinone inhibited UGT2B7-mediated zidovudine metabolism, resulting in increased systemic exposure of zidovudine when sauchinone and zidovudine were co-administered together. Our results indicated that there is potential HDI between sauchinone and drugs undergoing UGT2B7-mediated metabolism, possibly contributing to the safe use of sauchinone and drug combinations.

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Section: Introductionmentioning

confidence: 99%

Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity

2018

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Non communicable diseases and infections refuse to go away despite current knowledge and scientific advances.

Tumwine¹

2014

Afr H. Sci.

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It is a pleasure to welcome you to this first issue of African Health Sciences for 2014. We bring you papers on non-communicable diseases, infections, herbal medicine, reproductive health and medical education. The paper by Adisa and Fakeye 1 , introduces us to an interesting component of patient management in type 2 diabetes, that is, adherence to the medication. More than 75% of the patients were not aware of the indication for the prescribed medicine. Possible barriers to nonadherence included lack of knowledge, poor attitude, high cost, confusing doze of medicine, and premature discontinuation due to side effects. Saudi authors have studied the 'impact of mild versus moderate intensity aerobic walking exercise training on markers of bone metabolism and hand grip strength in moderate hemophilia patients'.2 On the other hand, Ugandan authors 3 describe histopathological types of cancer of the esophagus , while Chinese authors 4 report on the anti-human gastric cancer effect of astragalosides.

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<i>In vitro</i> evidence of baicalein’s inhibition of the metabolism of zidovudine (AZT)

Cited by 2 publications

References 10 publications

Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity

Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity

Non communicable diseases and infections refuse to go away despite current knowledge and scientific advances.

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