Effects of psoralen on the pharmacokinetics of anastrozole in rats

Zhang, Yuzhu; Wu, Jingjing; Zhou, Yue; Yin, Yulian; Chen, Hongfeng

doi:10.1080/13880209.2018.1501584

Cited by 12 publications

(5 citation statements)

References 20 publications

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“…The Kinetex‐C 18 110A chromatographic column is shorter than the chromatographic column in the existing analysis methods for ATZ (Regenthal et al, 2018; Zhang et al, 2018), which can shorten the chromatographic analysis time. Moreover, the inner diameter of the chromatographic column is relatively small and it is easy to obtain high ionization efficiency.…”

Section: Resultsmentioning

confidence: 99%

A novel anastrozole intravaginal ring for endometriosis: Pharmacokinetic characteristics and mucosal irritation

Yang

Dong

et al. 2023

Biomedical Chromatography

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In order to achieve the long-term management of endometriosis, a more economical and environmentally friendly material, ethylene vinyl acetate (EVA), was used to prepare a intravaginal ring with anastrozole (ATZ). This paper has compared the pharmacokinetic parameters with oral tablets (Aida ® ) in mini pigs and evaluated the uterine targeted effect and mucosal irritation of the ring. A bioassay method was developed and validated for the determination of ATZ in mini pigs. The determination of ATZ was achieved by LC-MS/MS using terfenadine as the internal standard. Separation was achieved on a Kinetex-C 18 110A chromatographic column (3 Â 30 mm, 2.6 μm; Phenomenex) with a gradient mobile phase consisting of methanol (0.1% formic acid) and water (0.1% formic acid). The method has been proved to be scientific and sensitive through methodological validation and can be easily and quickly applied to the determination of the content of anastrozole in mini pigs. The pharmacokinetic test results show that there was no significant difference in pharmacokinetic parameters between the two formulations. The intravaginal ring has a passive targeting effect on the uterus, and its mucosal irritation is acceptable. The intravaginal ring provides a new method for long-term management of endometriosis.

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Section: Resultsmentioning

confidence: 99%

A novel anastrozole intravaginal ring for endometriosis: Pharmacokinetic characteristics and mucosal irritation

Yang

Dong

et al. 2023

Biomedical Chromatography

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“…Like the IMP, another furocoumarin, psoralen, is a mechanism-based inactivator of CYP2B6 (Ji et al, 2015). In addition, psoralen has been demonstrated to significantly increase exposure of anastrozole, a P450 substrate, in rat vivo, and significantly decrease intrinsic clearance rates by psoralen pre-treatment in rat liver microsome (Zhang et al, 2018), indicating that furocoumarins result in DDI.…”

Section: Discussionmentioning

confidence: 99%

Inhibitory Effect of Imperatorin on the Pharmacokinetics of Diazepam In Vitro and In Vivo

et al. 2020

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Background: Diazepam is a benzodiazepine drug used to treat anxiety, insomnia, and muscle spasms. Imperatorin is a phytochemical isolated from medicinal plants and is widely used in herbal medicine. The aim of this study was to investigate the interactions between imperatorin and diazepam in vitro and in vivo and to provide evidence-based guidance for the safe clinical use of the drug. Methods: In vitro inhibition of imperatorin was assessed by incubating rat liver microsomes with diazepam to determine IC 50 values and the type of inhibition. For in vivo assessment, six rats were pretreated with 50 mg/kg imperatorin for two weeks, six were administered saline, and a single dose of 10 mg/kg diazepam was administered orally to both groups 30 min after the administration of imperatorin. Results: Imperatorin inhibited the in vitro metabolism of diazepam via the competitive mechanism of CYP450. The IC 50 values of imperatorin to nordazepam and temazepam were 1.54 mM and 1.80 mM, respectively. The inhibitory constant values for temazepam and nordazepam were 1.24 mM and 1.29 mM, respectively. Long-term administration of imperatorin significantly increased the AUC (0-12h) , AUC (0-∞) , and Cmax of diazepam, while Vz/F and CLz/F were decreased significantly (P < 0.05). In turn, the AUC (0-12h) , AUC (0-∞) , and Cmax of nordazepam and temazepam decreased significantly, and Vz/F and CLz/F increased significantly (P < 0.05). Conclusions: This study demonstrates that imperatorin inhibits the metabolism of diazepam both in vitro and in vivo. These results indicated that more attention should be paid when taking diazepam together with food or herbs containing IMP, although further investigation is still needed.

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“…It has been used to treat a number of diseases including leukoderma, psoriasis, osteoporosis and asthma [ 12 ]. Psoralen is the major active ingredient of PCL [ 13 , 14 ], which exhibits multiple biological properties including anti-inflammatory, anti-tumor, anti-vitiligo, anti-urticaria, and immunomodulatory activities [ 15 , 16 ]. However, the beneficial effect of psoralen on DN is rarely studied.…”

Section: Introductionmentioning

confidence: 99%

Psoralen alleviates high glucose-induced HK-2 cell injury by inhibition of Smad 2 signaling via upregulation of microRNA 874

Lin

Zhong

et al. 2020

BMC Pharmacol Toxicol

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Background: Diabetic nephropathy (DN) causes the vast proportion of excess mortality for patients with diabetes. Novel therapeutic approaches slowing down its incidence is still lacking. Psoralen is the major active ingredient of Psoralea corylifolia Linn. (PCL), which was used to treat a number of diseases. In this study, we aimed to investigate whether psoralen could alleviate DN using in vitro model. Methods: Cell viability assay and immunofluorescence were used to evaluate the effect of psoralen on high glucose (HG)-stimulated human kidney HK-2 cells (48 h). RT-qPCR was used to detect the expressions of miRNA in cells. Cell transfection, apoptosis assay, inflammatory cytokines detection and Western blot were further performed to explore the underlying molecular mechanisms. Results: HG-induced toxicity of HK-2 cells was alleviated by psoralen. Meanwhile, the secretion of inflammatory cytokines and extracellular matrix (ECM) accumulation induced by HG in HK-2 cells were also decreased by psoralen. In addition, the expression of miR-874 in HK-2 cells was significantly upregulated by psoralen. Western blot assays indicated that psoralen could reverse HG-induced increase of TLR-4/NF-κB and Smad2 via upregulation of miR-874. Conclusion: This study demonstrated that psoralen could significantly alleviate HG-induced HK-2 cell injury via upregulation of miR-874. In addition, HG-induced increase of TLR-4/NF-κB and Smad2 was revered by psoralen. Therefore, psoralen might serve as an agent for the treatment of DN.

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Effects of psoralen on the pharmacokinetics of anastrozole in rats

Cited by 12 publications

References 20 publications

A novel anastrozole intravaginal ring for endometriosis: Pharmacokinetic characteristics and mucosal irritation

A novel anastrozole intravaginal ring for endometriosis: Pharmacokinetic characteristics and mucosal irritation

Inhibitory Effect of Imperatorin on the Pharmacokinetics of Diazepam In Vitro and In Vivo

Psoralen alleviates high glucose-induced HK-2 cell injury by inhibition of Smad 2 signaling via upregulation of microRNA 874

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