Evaluation of acacetin inhibition potential against cytochrome P450 in vitro and in vivo

Zhou, Yunfang; Tu, Yanan; Zhou, Quan; Hua, Ailian; Geng, Peiwu; Chen, Feifei; Han, Aixia; Liu, Jin; Dai, Da‐Peng; Wang, Shuanghu; Wang, Junlu; Wen, Charles H.-P.

doi:10.1016/j.cbi.2020.109147

Cited by 14 publications

(9 citation statements)

References 29 publications

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“…According to published article, 14 range of 2-16 μM VEN was dissolved in methanol to meet concentrations at a series of the K m value. Vonoprazan was dissolved in DMSO and diluted at 0-10 μM concentrations with methanol to meet concentrations at about a series multiple of the IC 50 value.…”

Section: Effect Of Vonoprazan On the Metabolism Of Ven In Rat Liver Mmentioning

confidence: 99%

<p>In Vitro and In Vivo Rat Model Assessments of the Effects of Vonoprazan on the Pharmacokinetics of Venlafaxine</p>

Chen¹,

Jiang²,

Xu³

et al. 2020

DDDT

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Purpose The purpose of the present study was to investigate the effects of vonoprazan on the pharmacokinetics of venlafaxine in vitro and in vivo. Methods The mechanism underlying the inhibitory effect of vonoprazan on venlafaxine was investigated using rat liver microsomes. In vitro, the inhibition was evaluated by determining the production of O-desmethylvenlafaxine. Eighteen male Sprague–Dawley rats were randomly divided into three groups: control group, vonoprazan (5 mg/kg) group, and vonoprazan (20 mg/kg) group. A single dose of 20 mg/kg venlafaxine was administrated to rats orally without or with vonoprazan. Plasma was prepared from blood samples collected via the tail vein at different time points and concentrations of venlafaxine and its metabolite, O-desmethylvenlafaxine, were determined by ultra-performance liquid chromatography-tandem mass spectrometry. Results We observed that vonoprazan could significantly decrease the amount of O-desmethylvenlafaxine (IC 50 = 5.544 μM). Vonoprazan inhibited the metabolism of venlafaxine by a mixed inhibition, combining competitive and non-competitive inhibitory mechanisms. Compared with that in the control group (without vonoprazan), the pharmacokinetic parameters of venlafaxine and its metabolite, O-desmethylvenlafaxine, were significantly increased in both 5 and 20 mg/kg vonoprazan groups, with an increase in MR O-desmethylvenlafaxine . Conclusion Vonoprazan significantly alters the pharmacokinetics of venlafaxine in vitro and in vivo. Further investigations should be conducted to check these effects in humans. Therapeutic drug monitoring of venlafaxine in individuals undergoing venlafaxine maintenance therapy is recommended when vonoprazan is used concomitantly.

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Section: Effect Of Vonoprazan On the Metabolism Of Ven In Rat Liver Mmentioning

confidence: 99%

<p>In Vitro and In Vivo Rat Model Assessments of the Effects of Vonoprazan on the Pharmacokinetics of Venlafaxine</p>

Chen¹,

Jiang²,

Xu³

et al. 2020

DDDT

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“…Flavonoids are of low-molecular-weight, comprising polyphenolic compounds, classified into six groups-isoflavonoids, flavanones, flavanols, flavonols, flavones, and anthocyanidins [11]. The primary source of these flavonoids is the regular human diet, including fruits, vegetables, grains, bark, roots, stems, flowers (Table 1 and Figure 1), plant-derived beverages, such as green tea, wine, and cocoa-based products [12][13][14][15][16][17][18][19][20]. Flavonoids have shown various activities, such as inhibiting cell proliferation and angiogenesis, cell cycle arrest, induction in apoptosis, and reversion in multidrug resistance [21,22].…”

Section: Introductionmentioning

confidence: 99%

Targeting PI3K/Akt/mTOR Pathway by Different Flavonoids: A Cancer Chemopreventive Approach

Zughaibi

Suhail

Tarique

et al. 2021

IJMS

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Cancer is, globally, one of the main causes of death. Even though various therapies are available, they are still painful because of their adverse side effects. Available treatments frequently fail due to unpromising responses, resistance to classical anticancer drugs, radiation therapy, chemotherapy, and low accessibility to tumor tissues. Developing novel strategies to minimize adverse side effects, improve chemotherapy sensitivity, and control cancer progression is needed. Many studies have suggested small dietary molecules as complementary treatments for cancer patients. Different components of herbal/edible plants, known as flavonoids, have recently garnered attention due to their broad biological properties (e.g., antioxidant, antiviral, antimicrobial, anti-inflammatory, anti-mutagenic, anticancer, hepatoprotective, and cardioprotective). These flavonoids have shown anticancer activity by affecting different signaling cascades. This article summarizes the key progress made in this area and discusses the role of flavonoids by specifically inhibiting the PI3K/Akt/mTOR pathway in various cancers.

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“…According to European Medicine Agency (EMA) and the FDA guidelines for bioanalytical method validation [7,8], rigorous tests of linearity, LLOQ, selectivity, accuracy, precision, matrix effect and stability were evaluated. Each validation run, consisting of one set of calibration standards and three replicates of QC plasma samples, were performed within three consecutive days according to previous work [9][10][11][12][13][14].…”

Section: Methods Validationsmentioning

confidence: 99%

Validated UPLC-MS/MS method for the determination of ivosidenib in rat plasma: Application to a pharmacokinetic study

Chen¹,

Chen

et al. 2023

AChrom

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Ivosidenib (AG-120) is an unlisted, but estimated to be valid, oral inhibitor for isocitrate dehydrogenase 1 (IDH1) in the phase Ⅰ study of IDH1-mutated acute myeloid leukemia (AML) patients. This paper presents the investigation and validation of a rapid, effective, qualitative and quantitative determination method of ivosidenib in rat plasma by ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). The samples were treated using acetonitrile precipitation to remove protein influence. Then, the supernatant was extracted to analyze plasma concentration traits. In the UPLC system, acetonitrile and water containing 0.1% formic acid were selected as a cosolvent mobile phase, applying a gradient elution to isolate compounds in a C18 column. Mass detections were performed on a triple quadruple mass spectrometer in positive ion mode. Electroshock characteristic fragment ionization was used for m/z 583.95→214.53 for ivosidenib for quantitative determination, m/z 583.95→186.6 for qualitative determination, and m/z 492.06→354.55 for IS. The selectivity, linearity, stability, accuracy and precision were verified by reaching the guideline criteria from European Medicine Agency (EMA) and the Food and Drug Administration (FDA). The calibration curve was linear over the concentration range of 2–2,000 ng mL−1 for ivosidenib in rat plasma with a lower limit of quantification (LLOQ) of at least 2 ng mL−1. Additionally, there was no distinct matrix effect or carry-over phenomenon. The method was successfully established and applied to separate ivosidenib from plasma, with the entire analytical process being performed within 3 min for each sample, which shows high-efficiency and convenience for further studies of ivosidenib.

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Evaluation of acacetin inhibition potential against cytochrome P450 in vitro and in vivo

Cited by 14 publications

References 29 publications

<p>In Vitro and In Vivo Rat Model Assessments of the Effects of Vonoprazan on the Pharmacokinetics of Venlafaxine</p>

<p>In Vitro and In Vivo Rat Model Assessments of the Effects of Vonoprazan on the Pharmacokinetics of Venlafaxine</p>

Targeting PI3K/Akt/mTOR Pathway by Different Flavonoids: A Cancer Chemopreventive Approach

Validated UPLC-MS/MS method for the determination of ivosidenib in rat plasma: Application to a pharmacokinetic study

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