Differential systemic exposure to galangin after oral and intravenous administration to rats

Chen, Feng; Tan, Yin Feng; Li, Hai Long; Qin, Zhen; Cai, Hong; Lai, Wei Yong; Zhang, Xiao Po; Li, Yong Hui; Guan, Wei; Li, You Bin; Zhang, Jun Qing

doi:10.1186/s13065-015-0092-5

Cited by 27 publications

(12 citation statements)

References 31 publications

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“…The bioavailability of kaempferol after oral administration (100 mg/kg) in Spargue-Dawley rats was 2% [51]. After a single oral dose of galangin (10 mg/kg) only 220 ng/mL of the unmetabolized compound were detected in rat plasma [52].…”

Section: Discussionmentioning

confidence: 95%

Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids

et al. 2019

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We investigated the effect of 21 flavonoids in a three-dimensional in vitro system for their ability to inhibit gap formation by MCF-7 breast cancer spheroids in monolayers of lymphendothelial cells. Different representatives of the classes of flavones, flavonols, and flavanones were tested in the circular chemorepellent-induced defects (CCID)-assay. Bay11-7082, a known inhibitor of CCID formation served as the positive control. This study provides the first comparison of the potential of flavonoids to suppress features influencing the intravasation of MCF-7 breast cancer cells aggregates through the lymph endothelial barrier. The most significant effects were seen after incubation with the flavones luteolin, chrysin, and apigenin. Additional hydroxylation or methoxylation in positions 6 or 8, as expected, resulted in decreased activity. The tested flavanones remained without or low efficacy.

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Section: Discussionmentioning

confidence: 95%

Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids

et al. 2019

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“…First, the pharmacokinetic parameters of galangin remained to be unambiguously elucidated. Previous studies showed that the oral bioavailability of galangin was very low because it changed to glucuronidated forms after hepatic metabolism (24,25). The intravenous administration or molecular chemical modification may improve its efficiency in vivo.…”

Section: Discussionmentioning

confidence: 99%

Galangin suppresses human osteosarcoma cells: An exploration of its underlying mechanism

Yang

Han

et al. 2016

Oncology Reports

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Osteosarcoma is the most common malignant bone tumor that frequently affects adolescents. Osteosarcoma cells tend to proliferate and invade other tissues such as those of the lungs. Currently, neoadjuvant chemotherapy is the primary strategy to prevent tumor progression. However, its adverse effects result in poor long-term outcomes. Previous research has shown that galangin exhibits antitumor properties on several types of cancer cells; however its effect on osteosarcoma cells is yet unknown. The aims of this study were to evaluate the effects of galangin on the proliferation, apoptosis, migration, and invasion of osteosarcoma cells and to explore the underlying mechanisms. We found that the proliferation of MG63 and U20S osteosarcoma cells decreased significantly, while the apoptosis of MG63 cells accelerated significantly after exposure to galangin. In addition, the migration and invasion of MG63 cells were significantly inhibited by galangin. Moreover, phosphoinositide 3-kinase (PI3K) and Aktp-Thr308 expression levels were found to be significantly lower in galangin-treated MG63 cells than in the control cells, and the protein expression levels of their downstream regulators cyclin D1 and matrix metalloproteinase 2/9 were also downregulated in galangin-treated groups, while those of p27Kip1, caspase-3, and caspase-8 were upregulated. These findings suggest that galangin suppresses osteosarcoma cells by inhibiting their proliferation and invasion and accelerating their apoptosis, and the mechanism may be associated with the inhibition of PI3K and its downstream signaling pathway.

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“…The rhizomes of A. officinarum are used as a medicine for treatment of emesis, stomach ache and abdominal pain in China (Chen et al, 2015). The rhizomes of A. officinarum are used as a medicine for treatment of emesis, stomach ache and abdominal pain in China (Chen et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Development and validation of an LC–MS/MS method for the determination of DPHB in rat plasma and its application in pharmacokinetic studies

Chen

et al. 2018

Biomedical Chromatography

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The aim of the present study was to develop a rapid, specific and sensitive LC-MS/MS method for the determination of DPHB [7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-4-hepten-3-one] in rat plasma using yakuchinone A as an internal standard (IS). n-Hexane was used for the extraction of DPHB from rat plasma. Chromatographic separation of DPHB was achieved using a Kinetex XB-C column (2.10 × 50 mm, 2.6 μm) at 40°C. The mobile phase consisted of water (containing 0.1‰ formic acid, A) and acetonitrile (containing 0.1‰ formic acid, B) under a gradient elution at a flow rate of 0.3 mL min . Positive electrospray ionization and multiple reaction monitoring mode were used for detection. The selected precursor ion to product ion pairs, m/z 311.3 → 137.0 for DPHB and m/z 313.1 → 137.0 for yakuchinone A, were monitored. Good linearity was observed over the concentration range from 2 to 2000 ng mL (r = 0.9969). The recovery efficiency of DPHB from rat plasma was 54.8-69.7%, while the matrix effect ranged from 99.7 to 113%. Intra- and inter-day precision and accuracy values were within ±15% at three different quality control concentration levels. This validated method was successfully applied to pharmacokinetic studies in rats after a single p.o. or i.v. dose of DPHB solution. The route of administration significantly influenced systemic exposure to DPHB, and low bioavailability of DPHB was observed. The method developed here will be further improved and used in future pharmacokinetic studies.

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Differential systemic exposure to galangin after oral and intravenous administration to rats

Cited by 27 publications

References 31 publications

Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids

Structural Insight into the In Vitro Anti-Intravasative Properties of Flavonoids

Galangin suppresses human osteosarcoma cells: An exploration of its underlying mechanism

Development and validation of an LC–MS/MS method for the determination of DPHB in rat plasma and its application in pharmacokinetic studies

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