Strategy for rapid screening of antioxidant and anti‐inflammatory active ingredients in Gynura procumbens (Lour.) Merr. based on UHPLC–Q‐TOF–MS/MS and characteristic ion filtration

2019 ◽  
Author(s):  
Mi Liu ◽  
Mingzhen He ◽  
Hongwei Gao ◽  
Sa Guo ◽  
Jia Jia ◽  
...  
Keyword(s):  
Rapid Screening ◽  
Active Ingredients ◽  
Anti Inflammatory ◽  
Tof Ms

Oxy+ (arthrospira) and its medicinal importance: an appraisal

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Md Anzar Alam ◽  
Mohd Aleemuddin Quamri ◽  
Muzafar Din Ahmad Bhat ◽  
Siddiqui Aafreen ◽  
Ghulamuddin Sofi
Keyword(s):  
Linoleic Acid ◽  
Dietary Supplement ◽  
Autoimmune Disorders ◽  
Natural Source ◽  
Sulfated Polysaccharides ◽  
Active Ingredients ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Obesity Hypertension

AbstractOxy+ is a natural source of arthrospira found in nature, used as a dietary supplement and manufactured in Aruba for lifefactors. Arthrospira contains good quality of proteins, sulfated polysaccharides, γ-linoleic acid, along with an array of carotene and phytopigments, vitamins, and minerals which are reported to be antioxidant, immunomodulator, antihyperglycemic, antidyslipidemic, cardioprotective, hepatoprotective, antiviral, anticancerous, antihypertensive, anti-inflammatory, analgesic, neuroprotective and renoprotective activities. Several studies have shown arthrospira, and active ingredients of it revealed various pharmacological activities. It can be used for the management of various ailments such as diabetes, dyslipidemia, obesity, hypertension, cancer, arthritis, osteoarthritis, autoimmune disorders, etc. This review attempts to explore the hidden benefits of Oxy+ (arthrospira).

scholarly journals An Integrated Strategy for Rapid Discovery and Identification of Quality Markers in Gardenia Fructus Using an Omics Discrimination-Grey Correlation-Biological Verification Method

2021 ◽  
Vol 12 ◽  
Author(s):  
Rong Dong ◽  
Qingping Tian ◽  
Yongping Shi ◽  
Shanjun Chen ◽  
Yougang Zhang ◽  
...  
Keyword(s):  
Liver Injury ◽  
Evaluation System ◽  
Multiple Infection ◽  
Active Components ◽  
Grey Correlation ◽  
Liver Protection ◽  
Quality Markers ◽  
Anti Inflammatory ◽  
Highly Correlated ◽  
Tof Ms

Background: Gardenia Fructus (GF), a traditional Chinese medicine of Gardenia Ellis in Rubiaceae family, has the potential to clear heat and purge fire and has been widely used to treat multiple infection-related diseases. However, the quality markers (Q-Markers) of GF have not been revealed comprehensively.Methods: In this experiment, the transgenic zebrafish lines, Tg (l-fabp:EGFP) and Tg (lyz:EGFP), were used to evaluate two main kinds of traditional efficacies of GF, hepatoprotective and anti-inflammatory effects. All the GF samples from different production areas were tested their anti-liver injury and anti-inflammantory activities. High-performance liquid chromatography-quadrupole time-of-flight mass spectrometry method (HPLC-Q-TOF/MS) was employed for herbal metabonomic analysis of GF samples. Gray correlation analysis (GCA) was utilized to screen out the components closely associated with the activities. Finally, the zebrafish model was applied to verify the bioactivity of the crucial components to determine the Q-Markers of GF.Results: The zebrafish models were established by inducing with hydrogen peroxide or copper sulfate and applied to quickly evaluate the hepatoprotective effect and inflammation of GF samples. 27 potentially active components for liver protection and 21 potentially active components with anti-inflammatory properties were identified by herbal metabolomic analysis based on HPLC-Q-TOF/MS. The GCA result showed that five of the 27 components were highly correlated with liver protection, 15 of the 21 components were highly correlated with anti-inflammatory activity. Among them, geniposide and crocin-1 were confirmed their bioactivities on zebrafish experiment to be responsible for the protective effects of GF against liver injury, and genipin-1-β-D-gentiobioside, quinic acid, gardenoside, d-glucuronic acid, l-malic acid, mannitol, rutin, and chlorogenic acid were confirmed to be responsible for the anti-inflammatory effects. Finally, according to the screening principles of Q-Markers, genipin-1-β-D-gentiobioside, geniposide, and gardenoside were preliminarily identified to be the Q-Markers of GF.Conclusion: This study established an effective research strategy of “Omics Discrimination-Grey Correlation-Biological Verification,” which enabled the rapid identification of key pharmacological components of GF. These markers have provided a scientific basis for constructing a modern quality evaluation system for GF.

scholarly journals Human iPSC-derived brain endothelial microvessels in a multi-well format enable permeability screens of anti-inflammatory drugs

2021 ◽  
Author(s):  
Sven Fengler ◽  
Birgit Kurkowsky ◽  
Sanjeev Kumar Kaushalya ◽  
Wera Roth ◽  
Philip Denner ◽  
...  
Keyword(s):  
Stem Cell ◽  
Neurodegenerative Diseases ◽  
Induced Pluripotent Stem Cell ◽  
Barrier Properties ◽  
Brain Diseases ◽  
Rapid Screening ◽  
Sodium Fluorescein ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Optimizing drug candidates for blood-brain barrier (BBB) penetration in humans remains one of the key challenges and many devastating brain diseases including neurodegenerative diseases still do not have adequate treatments. So far, it has been difficult to establish state-of-the-art human stem cell derived in vitro models that mimic physiological barrier properties including a 3D microvasculature in a format that is scalable enough to screen drugs for BBB penetration in early drug development phases. To address this challenge, we established human induced pluripotent stem cell (iPSC)-derived brain endothelial microvessels in a standardized and scalable multi-well plate format. iPSC-derived brain microvascular endothelial cells (BMECs) were supplemented with primary cell conditioned media and grew to intact microvessels in 10 days of culturing. Produced microvessels show a typical BBB phenotype including endothelial protein expression, tight-junctions and polarized localization of efflux transporter. Microvessels exhibited physiological relevant trans-endothelial electrical resistance (TEER), were leak tight for 10 kDa dextran-Alexa 647 and strongly limited the permeability of sodium fluorescein (NaF). Permeability tests with reference compounds confirmed the suitability of our model as platform to identify potential BBB penetrating anti-inflammatory drugs. In summary, the here presented brain microvessel platform recapitulates physiological properties and allows rapid screening of BBB permeable anti-inflammatory compounds that has been suggested as promising substances to cure so far untreatable neurodegenerative diseases.

The effect of Wogonoside on the expression of pulmonary fibrosis factor in Mycoplasma pneumoniae pneumonia

2020 ◽  
Author(s):  
Huihui Wang ◽  
Xiaoxi Wang ◽  
Zhimin Yang ◽  
Huixing Xu ◽  
Xin Wang ◽  
...  
Keyword(s):  
Mycoplasma Pneumoniae ◽  
Active Ingredient ◽  
A549 Cells ◽  
Scutellaria Baicalensis ◽  
Chinese Herbs ◽  
Affinity Constant ◽  
Active Ingredients ◽  
Pulmonary Interstitial Fibrosis ◽  
Mycoplasma Pneumoniae Pneumonia ◽  
Tof Ms

Abstract BACKGROUND Mycoplasma pneumoniae pneumonia (MPP) is an acute respiratory infectious pneumonia with pulmonary interstitial fibrosis. TGF-β1 is well accepted as the central mediator for fibrosis which promotes the formation of tissue fibrosis factor. Qinbaiqingfei pellet (Qinbai) has already been approved as the first effective new traditional Chinese medicine which can delay activities of Mycoplasma pneumoniae (M.pneumoniae) and protect lung epithelial cells in clinical trials. However, the mechanism of Qinbai inhibiting the expression of TGF-β1 is still unclear. METHODS The Chinese herbs in Qinbai were screened by surface plasmon resonance (SPR) and it was deteimined that Scutellaria baicalensis extracts in Qinbai showed the best binding with TGF-β1. Then the active ingredient whicn can be bound with TGF-β1 protein in the solution of Qinbai and Scutellaria baicalensis was isolated and analyzed by UPLC-Q-TOF-MS, which proved the active ingredient was Wogonoside. The affinity constant of Wogonoside and TGF-β1 protein was measured by SPR affinity analysis. A549 cells infected with M.pneumoniae were intervened by Wogonoside, and then the expression of TGF-β1 and Smad3 in A549 cells were analyzed by PCR and western blotting. RESULTS The results showed the bound effect of Scutellaria baicalensis and TGF-β1 was effective. The active ingredients which can be bound with TGF-β1 in the solution of Scutellaria baicalensis and Qinbai were obtained and analyzed to investigate the mechanism of Qinbai inhibiting the expression of TGF-β1. UPLC-Q-TOF-MS results showed that the active ingredients was Wogonoside. SPR affinity analysis showed that the affinity constant was 21.71 µM. Pharmacological experiments revealed that Wogonoside strongly inhibited the expression of TGF-β1 and Smad3 in A549 cells infected by M.pneumoniae. CONCLUSION Wogonoside in Qinbai can be bound with TGF-β1 and down-regulate the expression of lung fibrosis factors TGF-β1 and Smad3. The finding may improve our understanding the molecular mechanism of Qinbai mediating MPP and provide new sights into the future pharmacological investigation of Qinbai.

scholarly journals Coelonin, an Anti-Inflammation Active Component of Bletilla striata and Its Potential Mechanism

2019 ◽  
Vol 20 (18) ◽  
pp. 4422 ◽  
Author(s):  
Fusheng Jiang ◽  
Meiya Li ◽  
Hongye Wang ◽  
Bin Ding ◽  
Chunchun Zhang ◽  
...  
Keyword(s):  
Molecular Mechanism ◽  
Kinase Inhibitor ◽  
Negative Regulator ◽  
Antibody Array ◽  
Dependent Manner ◽  
Active Ingredients ◽  
Bletilla Striata ◽  
Tnf Α ◽  
Anti Inflammatory

Ethanol extract of Bletilla striata has remarkable anti-inflammatory and anti-pulmonary fibrosis activities in the rat silicosis model. However, its active substances and molecular mechanism are still unclear. To uncover the active ingredients and potential molecular mechanism of the Bletilla striata extract, the lipopolysaccharide (LPS)-induced macrophage inflammation model and phospho antibody array were used. Coelonin, a dihydrophenanthrene compound was isolated and identified. It significantly inhibited LPS-induced interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) expression at 2.5 μg/mL. The microarray data indicate that the phosphorylation levels of 32 proteins in the coelonin pre-treated group were significantly down-regulated. In particular, the phosphorylation levels of the key inflammatory regulators factor nuclear factor-kappa B (NF-κB) were significantly reduced, and the negative regulator phosphatase and tensin homologue on chromosome ten (PTEN) was reduced. Moreover, the phosphorylation level of cyclin dependent kinase inhibitor 1B (p27Kip1), another downstream molecule regulated by PTEN was also reduced significantly. Western blot and confocal microscopy results confirmed that coelonin inhibited LPS-induced PTEN phosphorylation in a dose-dependent manner, then inhibited NF-κB activation and p27Kip1 degradation by regulating the phosphatidylinositol-3-kinases/ v-akt murine thymoma viral oncogene homolog (PI3K/AKT) pathway negatively. However, PTEN inhibitor co-treatment analysis indicated that the inhibition of IL-1β, IL-6 and TNF-α expression by coelonin was independent of PTEN, whereas the inhibition of p27Kip1 degradation resulted in cell-cycle arrest in the G1 phase, which was dependent on PTEN. The anti-inflammatory activity of coelonin in vivo, which is one of the main active ingredients of Bletilla striata, deserves further study.

scholarly journals Quadrupole Time-of-Flight Mass Spectrometry: A Paradigm Shift in Toxicology Screening Applications

2019 ◽  
Vol 40 (3) ◽  
pp. 135-146 ◽  
Author(s):  
Darren Allen ◽  
Brett McWhinney
Keyword(s):  
Mass Spectrometry ◽  
Sensitivity And Specificity ◽  
Biological Samples ◽  
Time Of Flight ◽  
New Drugs ◽  
Rapid Screening ◽  
New Psychoactive Substances ◽  
Flight Mass Spectrometry ◽  
Analytical Approaches ◽  
Tof Ms

The screening of biological samples for the presence of illicit or legal substances is an important frontline tool in both clinical and forensic toxicology. In the clinical setting, drug screening is a useful tool for the clinician in improving patient care and guiding treatment. Analytical approaches for the screening of drugs in biological samples are extensive and well documented, though many rapid screening techniques often lack appropriate sensitivity and specificity, requiring careful clinical interpretation. The continuous emergence of new psychoactive substances presents a considerable analytical challenge in maintaining up-to-date methods for the detection of relevant drugs. Adapting and validating methods for the detection of new substances can be a complicated and costly undertaking. There is also a considerable lag time between the emergence of new drugs and the release of commercial assays for detection. Quadrupole time-of-flight mass spectrometry (Q-TOF-MS) has gained considerable attention over the last decade as an analytical technique that is capable of meeting the challenges of a rapidly changing drug landscape. Exhibiting both high sensitivity and specificity in drug detection, Q-TOF-MS also allows methods to be rapidly updated for newly emerging psychoactive agents. The coupling of Q-TOF-MS with techniques such as liquid or gas chromatography can provide both rapid and comprehensive screening solutions that are gaining popularity in the clinical laboratory setting.

scholarly journals Rapid Screening and Structural Characterization of Antioxidants from the Extract ofSelaginella doederleiniiHieron with DPPH-UPLC-Q-TOF/MS Method

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Gang Wang ◽  
Shun Yao ◽  
Xiu-Xiu Zhang ◽  
Hang Song
Keyword(s):  
Mass Spectrometry ◽  
High Performance ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Rapid Screening ◽  
Flight Mass Spectrometry ◽  
First Time ◽  
Strong Capacity ◽  
Tof Ms

2,2-Diphenyl-1-picrylhydrazyl-ultra-high performance liquid chromatography-Q-time-of-flight mass spectrometry (DPPH-UPLC-Q-TOF/MS), as a rapid and efficient means, now was used for the first time to screen antioxidants fromSelaginella doederleinii. The nine biflavone compounds were screened as potential antioxidants. The biflavones were structurally identified and divided into the three types, that is, amentoflavone-type, robustaflavone-type, and hinokiflavone-type biflavonoids. Among the compounds bilobetin (3) and putraflavone (8) were found fromSelaginella doederleiniifor the first time and others including amentoflavone (1), robustaflavone (2), 4′-methoxy robustaflavone (4), podocarpusflavone A (5), hinokiflavone (6), ginkgetin (7), and heveaflavone (9) were identified previously in the plant. Moreover, nine biflavones possessed a good antioxidant activity via their DPPH free radical scavenging. It demonstrates that DPPH-UPLC-Q-TOF/MS exhibits strong capacity in separation and identification for small molecule. The method is suitable for rapid screening of antioxidants without the need for complicated systems and additional instruments.

Comprehensive characterization by UHPLC-ESI-Q-TOF-MS from an Eryngium bourgatii extract and their antioxidant and anti-inflammatory activities

2013 ◽  
Vol 50 (1) ◽  
pp. 197-204 ◽  
Author(s):  
María de la Luz Cádiz-Gurrea ◽  
Salvador Fernández-Arroyo ◽  
Jorge Joven ◽  
Antonio Segura-Carretero
Keyword(s):  
Anti Inflammatory ◽  
Comprehensive Characterization ◽  
Tof Ms
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