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Pharmacokinetic comparison of fifteen active compositions in rat plasma after oral administration of raw and honey-processed Aster tataricus extracts
A sensitive ultra-high performance liquid chromatography–tandem mass spectrometry method was developed and validated to clarify pharmacokinetic properties of 15 compounds (quercetin, isorhamnetin, chlorogenic acid, isoquercitrin, caffeic acid, scopoletin, 7-hydroxycoumarin, shionone,ferulic acid, kaempferol-7-O-β-D-glucopyranoside, methyl caffeate, luteolin, kaempferol,epifriedelinol, and protocatechuic acid) in raw and honey-processed Aster tataricus. Separation was carried out on an ACQUITY UPLC® BEH C18 column (2.1 × 100 mm, 1.7 µm) using a gradient elution with mobile phase constituting 0.1% formic acid-water and 0.05% formic acid-methanol.Quantitative analysis was performed using multiple reaction monitoring detection in both positive and negative ionization modes. Calibration curves showed good linearity (r2 > 0.991) over the corresponding concentration range. The intra-day and inter-day precisions were within 10.1%, and accuracy ranged from -11.4% to 12.4%. The extraction recoveries and matrix effects were 78.1%–100.0% and 81.1%–113.7%, respectively. The analytes were stable under four storage conditions with relative standard deviations less than 12.6%. The validated method was successfully applied to compare the pharmacokinetic behaviors of raw and honey-processed Aster tataricus for the first time. The results indicated that the AUCs of shionone, ferulic acid, and protocatechuic acid in honey-processed Aster tataricus group were significantly lower than that of raw Aster tataricus group.
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Standards, including quercetin, isorhamnetin, scopoletin, 7-hydroxycoumarin, shionone, kaempferol-7-O-β-D-glucopyranoside, methyl caffeate, luteolin, kaempferol, protocatechuic acid,
and icariin (internal standard, IS) (purity ≥ 98%) were purchased from Chengdu Desite
Bio-Technology Co., Ltd. (Chengdu, China).
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Simultaneous determination of calycosin, prim-O glucosylcimifugin, and paeoniflorin in rat plasma by HPLC-MS/MS: application in the pharmacokinetic analysis of HQCF
This study aimed to develop and validate a high-performance liquid chromatography– tandem mass spectrometry method to simultaneously determine three bioactive components of the Huangqi Chifeng decoction (HQCF) in rat plasma. Methods: Taxol was used as an internal standard in the developed method. Chromatographic separation was performed on a C18 column using a gradient elution with 0.1% formic acid in acetonitrile (v/v) and 0.1% formic acid in water (v/v) as the mobile phases at a flow rate of 0.4 mLminute1 . All compounds were monitored via selected reaction monitoring with an electrospray ionization source. Results: The lower limits of quantification of paeoniflorin, calycosin, and prim-O-glucosylcimifugin were 15.0, 0.75, and 0.75 ngmL1 , respectively. The calibration curves indicated optimal linearity (r > 0.99) across the concentration ranges. The specificity, precision, accuracy, recovery, matrix effect, and stability of the method were validated. This method was successfully applied in a pharmacokinetics study of the three compounds in rat plasma.
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CA, PG, PA, and Taxol were purchased from Chengdu DeSiTe Biological Technology Co. Ltd. (Chengdu, China).
原文链接：https://doi.org/10.1177/0300060520972902
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Comprehensive evaluation of the antioxidant capacity of Sceptridium ternatum using multiple colorimetric methods and 1,1‐diphenyl‐2‐picrylhydrazyl–high‐performance liquid chromatography analysis
Sceptridium ternatum is a medicinal herb with multiple health benefits. However, its antioxidant activity and active components have not been clarified. In this study, the antioxidant capacity of S. ternatum was comprehensively investigated using multiple colorimetric methods and 1,1‐diphenyl‐2‐picrylhydrazyl–high‐performance liquid chromatography analysis. First, the phenolic content, flavonoid content, and radical scavenging ability of S. ternatum were parallelly determined using colorimetric methods performed in 96‐well microplates. The flavonoid content, rather than the phenolic content, was highly correlated with its antioxidant activity. Sceptridium ternatum was shown to be a rich source of flavonoids, with a highest flavonoid yield of 3.44 ± 0.11 mg/g. Subsequently, 1,1‐diphenyl‐2‐picrylhydrazyl–high‐performance liquid chromatography experiment and quadrupole time‐of‐flight mass spectrometry analyses were carried out for rapid screening of the individual antioxidants. A total of 14 O‐glycosyl flavonoids with quercetin or kaempferol aglycone have been characterized. Particularly, quercetin 3‐O‐rhamnoside‐7‐O‐glucoside exhibited the most potent antioxidant ability. Its half‐maximal effective concentrations for scavenging 1,1‐diphenyl‐2‐picrylhydrazyl and 2,2ʹ‐azino‐bis (3‐ethylbenzthiazoline‐6‐sulfonic acid) radicals were 70.55 ± 2.69 and 106.90 ± 1.76 µg/mL, respectively, which were comparable with those of l‐ascorbic acid. Our results indicated that the combined colorimetric and chromatographic methods provided a practical strategy for the discovery of bioactive compounds from natural products. ...... Quercetin (Que, ≥98% purity) was procured from Chengdu Desite Biotech (Chengdu, China).
原文链接;https://doi.org/10.1002/jssc.202000550
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Fangchinoline suppresses conjunctival melanoma by directly binding FUBP2 and inhibiting the homologous recombination pathway
Abstract
Conjunctival melanoma (CM) is a rare and fatal ocular tumour with poor prognosis. There is an urgent need of effective therapeutic drugs against CM. Here, we reported the discovery of a novel potential therapeutic target for CM.
Through phenotypic screening of our in-house library, fangchinoline was discovered to signifificantly inhibit the growthof CM cells including CM-AS16, CRMM1, CRMM2 and CM2005.1. Further mechanistic experiments indicated that
fangchinoline suppressed the homologous recombination (HR)-directed DNA repair by binding with far upstream element binding protein 2 (FUBP2) and downregulating the expression of HR factors BRCA1 and RAD51. In vitro and
in vivo antitumour experiments revealed that fangchinoline increased the effificacy of cisplatin by blocking HR factors and reduced the drug dose and toxicity. In conclusion, our work provides a promising therapeutic strategy for the
treatment of CM that is worthy of extensive preclinical investigation.
Fangchinoline (98%) was from Chengdu DeSiTe Biological Technology Co., Ltd ( Chengdu, China).
原文链接：https://doi.org/10.1038/s41419-021-03653-4
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采用旋涡辅助固相分散法同时提取防风藤中5种有效成分
Abstract:
Saposhnikoviae Radix (SR), one of top-grade herbs, is widely used to treat cold, headache, fevers, cough, rheumatism and cardiovascular diseases in prescriptions. A vortex-assisted matrix solid phase dispersion (VA-MSPD) extraction method applying a reusable dispersant was developed to extract four chromones and one coumarin from Saposhnikoviae Radix (SR), which followed by high performance liquid chromatography analysis (HPLC). The novel dispersant, acetonitrile modified carbon-coated magnetite nanoparticles (Fe3O4@C@ ACN MNP), could be reused for 10 times and it still possesses excellent extraction performance. Various optimal experimental condition of VA-MSPD was considered and obtained reliable matrix linearity (r2 > 0.999) and good recovery (94.8%–105%). In order to recovery the dispersant from sample-dispersant powder after elution, methanol/water (50:50, v/v) was applied as washing solution to separate the dispersant and samples, so that the percent recovery of modified materials was obtained as 88.6% (RSD = 0.74%). The results indicated that Fe3O4@C@ACN MNP could be considered as sustainable dispersant and it exhibited tremendous potential for efficacious extraction of chromones and coumarins.
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2. Materials and methods
2.1. Chemicals and reagents
Reference components of 4′-O-β-D-glucosyl-5-O-methylvisamminol, prim-O-D-glucosylcimifugin, cimifugin, psoralen and sec-O-glucosylha-maudol (purity >99%) were supplied by Chengdu Desite Biotech Co., Ltd. (Chengdu, China).
原文链接：https://doi.org/10.1016/j.scp.2021.100524
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6-Gingerol Alleviates Neonatal Hypoxic-Ischemic Cerebral ...
Hypoxic-ischemic encephalopathy (HIE) is one main cause of neonatal death and disability,causing substantial injury to white and gray matter, which can lead to severe neurobehavioral dysfunction, including intellectual disability and dyskinesia.Inflammation, nerve cell death, and white matter injury are important factors in the pathological process of HIE. 6-Gingerol is a ginger extract, which reduces inflammatory response and cell death. However, the role of 6-Gingerol in neonatal hypoxic-ischemic brain injury (HIBI) remains unknown. In this study, we constructed a mouse HIBI model and analyzed the protective effect of 6-Gingerol on HIBI by using behavioral tests, histological staining, qPCR and western blot. Here, we found that 6-Gingerol treatment could alleviate HIBI and improve short-term reflex performance, which is closely related to cell death and neuroinflammation. Additionally, 6-Gingerol reduced neuronal apoptosis, pro-inflammatory factor release, as well as microglial activation. Furthermore, 6-Gingerol significantly improved motor disability, which is associated with white matter damage. Thus, our results showed that 6-Gingerol could reduce the loss of myelin sheaths, alleviate cell death of oligodendrocytes, and stimulate the maturation of oligodendrocytes. In terms of mechanism, we found that 6-Gingerol decreased histone H3K27me3 levels, activated AKT pathway and inhibited the activation of ERK and NF-κB pathway at 3 days post-HIBI. Taken together, our data clearly indicate that 6-Gingerol plays a neuroprotective role against HIBI by epigenetic modification and regulation of AKT, ERK, and NF-κB pathways, inhibiting inflammatory responses and reducing cell death.
MATERIALS AND METHODS
HIBI Model and Drugs Administration
6-Gingerol (DESITE, Chengdu, China) ...
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