Metabolic profile study of 7, 8-dihydroxyflavone in monkey plasma using high performance liquid chromatography–tandem mass spectrometry

Sun, Taoping; Chen, Sijing; Huang, Hao; Li, Tianqing; Yang, Wei; Liu, Liegang

doi:10.1016/j.jchromb.2017.07.001

Cited by 12 publications

(6 citation statements)

References 33 publications

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“…In vivo pharmacokinetic profiles and metabolism of 7,8-DHF and its metabolites distribute in mouse and monkey brains after oral administration had been well researched [ 25 – 27 ]. It had been identified that the concentration of 7,8-DHF both peaked at 10 min with 70 ng/ml in the plasma and 50 ng/g in the brain after the administration of 7,8-DHF (5 mg/Kg).…”

Section: Discussionmentioning

confidence: 99%

7,8-Dihydroxyflavone Protects Nigrostriatal Dopaminergic Neurons from Rotenone-Induced Neurotoxicity in Rodents

Nie

Sun

et al. 2019

Parkinson's Disease

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7,8-Dihydroxyflavone (7,8-DHF) is thought to be a promising therapeutic agent for various neurodegenerative diseases. The major purpose of this study was to investigate the neuroprotective effects of 7,8-DHF on the rotenone-induced motor deficit of Parkinson’s disease. Nine-month-old rats were treated with rotenone (2 mg/kg/day, i.h.) for 5 weeks to establish the animal model of Parkinson’s disease (PD), and 7,8-DHF (5 mg/kg, i.p.) was administrated daily throughout the whole period of rotenone injection. Five weeks later, an open field test was used to assess the motor ability of the animals. TH immunostaining was performed to evaluate rotenone-induced neurotoxicity on substantia nigra (SN) dopaminergic neurons and the DA terminals in the striatum. Western blot analyses were used to examine the expressions of TH, BDNF/TrkB signaling cascades, phospho-α-synuclein (Ser129), α-synuclein, and phospho-tau (Ser396) in SN. The results revealed that treatment with 7,8-DHF improved PD model’s behavioral performance and reduced dopaminergic neuron loss in the SN and striatum, associated with the activation of TrkB receptors and its signaling cascades, and reduced p-MAPK, p-α-synuclein, and p-tau. Collectively, these results indicated that 7,8-DHF displayed prominent neuroprotective properties, providing a promising therapeutic strategy for PD treatment.

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Section: Discussionmentioning

confidence: 99%

7,8-Dihydroxyflavone Protects Nigrostriatal Dopaminergic Neurons from Rotenone-Induced Neurotoxicity in Rodents

Nie

Sun

et al. 2019

Parkinson's Disease

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“…Despite the fact that DHF has better pharmacokinetic properties (e.g., better oral bioavailability and longer elimination half-life) than orally administered BDNF, it still has a poor oral bioavailability (approximately 4.5% in mice) [14], which can be improved 2.3-fold by 7,8-bis-carbamate ester prodrug formation [14]. During its biotransformation, DHF undergoes conjugation reactions; primarily glucuronide and sulfate metabolites were formed in monkeys after the per os administration of 30 mg/kg DHF [15].…”

Section: Introductionmentioning

confidence: 99%

Interactions of 7,8-Dihydroxyflavone with Serum Albumin as well as with CYP2C9, CYP2C19, CYP3A4, and Xanthine Oxidase Biotransformation Enzymes

et al. 2019

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7,8-dihydroxyflavone (DHF) is a flavone aglycone which has beneficial effects in several central nervous system diseases. Most of the pharmacokinetic properties of DHF have been characterized, while only limited information is available regarding its interactions with serum albumin and biotransformation enzymes. In this study, the interactions of DHF with albumin was examined employing fluorescence spectroscopy and ultrafiltration. Furthermore, the inhibitory effects of DHF on cytochrome P450 (CYP2C9, CYP2C19, and CYP3A4) and xanthine oxidase (XO) enzymes were also tested using in vitro models. Our results demonstrate that DHF forms a stable complex with albumin (K = 4.9 × 105 L/mol) and that it is able to displace both Site I and Site II ligands. Moreover, DHF proved to be a potent inhibitor of each enzyme tested, showing similar or slightly weaker effects than the positive controls used. Considering the above-listed observations, the coadministration of DHF with drugs may interfere with the drug therapy due to the development of pharmacokinetic interactions.

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“…The experimental data of BP neural network model is based on BBD data. In the whole dataset, 80% of the datas are used for training, and 20% of the datas (25)(26)(27)(28)(29) are used for testing (Table 2). The R 2 value of the ANN-BP model (0.99799) indicates that the network performance after training is accurate (Figure 9).…”

Section: Ann-bp Modelingmentioning

confidence: 99%

“…Its advantage is to save time and re duce the consumption of reagents and materials. Artificial intelligence (AI) has good non linear mapping, generalization, self-organization and self-learning capabilities, which have been widely used in robots, language recognition, image recognition, aerospace ap There are many methods for extracting flavonoids at home and abroad, e.g., organic solvent extraction [21], enzymatic hydrolysis [22], resin adsorption [23,24], high performance liquid chromatography [25,26], supercritical extraction [27], microwave extraction [28,29], ultrasonic extraction technology [30,31], and soxhlet extraction [32]. Ultrasonic extraction technology is a new method for extracting active ingredients from plants in recent years and which works by using the strong vibration, cavitation and comminution generated by ultrasonic to extract the active ingredients from plants into solvent.…”

Section: Introductionmentioning

confidence: 99%

Artificial Intelligence Assisted Ultrasonic Extraction of Total Flavonoids from Rosa sterilis

Liu

Ding

et al. 2021

Molecules

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Flavonoids in Rosa sterilis were studied. The flavonoids in Rosa sterilis were extracted by ultrasonic method, and the extraction conditions were modeled and optimized by response the surface methodology and the artificial intelligence method. The results show that the ultrasonic method can effectively extract total flavonoids, and the extraction rate is close to the prediction value of ANN-GA algorithm, which proves the rationality of the model. The order of the effects of the parameters on the experiment was material liquid ratio > extraction power > extraction time > ethanol concentration. In addition, the scavenging effects of flavonoids on DPPH, O2−· and ·OH were also determined, and these indicated that flavonoids have strong antioxidant activities. The kinetics of the extraction process was studied by using the data of the extraction process, and it was found that the extraction process conformed to Fick’s first law.

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Metabolic profile study of 7, 8-dihydroxyflavone in monkey plasma using high performance liquid chromatography–tandem mass spectrometry

Cited by 12 publications

References 33 publications

7,8-Dihydroxyflavone Protects Nigrostriatal Dopaminergic Neurons from Rotenone-Induced Neurotoxicity in Rodents

7,8-Dihydroxyflavone Protects Nigrostriatal Dopaminergic Neurons from Rotenone-Induced Neurotoxicity in Rodents

Interactions of 7,8-Dihydroxyflavone with Serum Albumin as well as with CYP2C9, CYP2C19, CYP3A4, and Xanthine Oxidase Biotransformation Enzymes

Artificial Intelligence Assisted Ultrasonic Extraction of Total Flavonoids from Rosa sterilis

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