scholarly journals Characterization of Anti-Inflammatory and Antioxidant Constituents from Scutellaria baicalensis Using LC-MS Coupled with a Bioassay Method

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3617
Author(s):  
Yoo Kyong Han ◽  
Hyunwoo Kim ◽  
Hyeji Shin ◽  
Jiyeon Song ◽  
Mi Kyeong Lee ◽  
...  
Keyword(s):  
Screening Method ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Scutellaria Baicalensis ◽  
No Production ◽  
Dpph Assay ◽  
Bioactive Constituents ◽  
Total Extract ◽  
Molecular Networking ◽  
Bv2 Cells

An effective and previously demonstrated screening method for active constituents in natural products using LC-MS coupled with a bioassay was reported in our earlier studies. With this, the current investigation attempted to identify bioactive constituents of Scutellaria baicalensis through LC-MS coupled with a bioassay. Peaks at broadly 17–20 and 24–25 min on the MS chromatogram displayed an inhibitory effect on NO production in lipopolysaccharide-induced BV2 microglia cells. Similarly, peaks at roughly 17–19 and 22 min showed antioxidant activity with an 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS)/2,2-diphenyl-1- picrylhydrazyl (DPPH) assay. For confirmation of LC-MS coupled with a bioassay, nine compounds (1–9) were isolated from an MeOH extract of S. baicalensis. As we predicted, compounds 1, 8, and 9 significantly reduced lipopolysaccharide (LPS)-induced NO production in BV2 cells. Likewise, compounds 5, 6, and 8 exhibited free radical-scavenging activities with the ABTS/DPPH assay. In addition, the structural similarity of the main components was confirmed by analyzing the total extract and EtOAc fractions through molecular networking. Overall, the results suggest that the method comprised of LC-MS coupled with a bioassay can effectively predict active compounds without an isolation process, and the results of molecular networking predicted that other components around the active compound node may also be active.

scholarly journals Tirucallane Glycoside from the Leaves of Antidesma bunius and Inhibitory NO Production in BV2 Cells and RAW264.7 Macrophages

2016 ◽  
Vol 11 (7) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Do Thi Trang ◽  
Le Thi Huyen ◽  
Nguyen Xuan Nhiem ◽  
Tran Hong Quang ◽  
Dan Thi Thuy Hang ◽  
...  
Keyword(s):  
Triterpene Glycoside ◽  
Methanol Extract ◽  
Inhibitory Effect ◽  
Published Data ◽  
No Production ◽  
Spectroscopic Methods ◽  
Raw264.7 Macrophages ◽  
Bv2 Cells ◽  
Megastigmane Glycosides ◽  
Strong Inhibitory Effect

One new tirucallane- type triterpene glycoside, antidesoside (1), along with two biflavones, podocarpusflavone A (2) and amentoflavone (3) and two megastigmane glycosides, byzantionoside B (4), and (6 S,9 R)-roseoside (5) were isolated from the methanol extract of Antidesma bunius leaves. Their structures were determined by spectroscopic methods and in comparison with the published data. Compounds 1 - 3 were found to show strong inhibitory effect of NO production in BV2 cells and RAW264.7 macrophages LPS-stimulated, with IC50 values ranging from 8.5 to 26.9 μM.

scholarly journals Acetylcholinesterase inhibitors and antioxidants mining from marine fungi: bioassays, bioactivity coupled LC–MS/MS analyses and molecular networking

2020 ◽  
Vol 2 (4) ◽  
pp. 386-397
Author(s):  
Yingying Nie ◽  
Wencong Yang ◽  
Yayue Liu ◽  
Jingming Yang ◽  
Xiaoling Lei ◽  
...  
Keyword(s):  
Aspergillus Terreus ◽  
Marine Fungi ◽  
Radical Scavenging ◽  
Bioactive Molecules ◽  
Ache Inhibition ◽  
Bioactive Constituents ◽  
Molecular Networking ◽  
Unknown Compound ◽  
Ache Inhibitors ◽  
Larval Toxicity

Abstract Marine fungi are potentially important resources for bioactive lead compounds for discovering new drugs for diseases such as Alzheimer’s disease. In this paper, the combined bioassay model of acetylcholinesterase (AChE) inhibition, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, and Artemia larval lethality was used to evaluate the activity and toxicity of 35 marine fungal strains from seas around China. Their bioactive constituents were revealed by thin layer chromatography (TLC) autography, bioactivity coupled LC–MS/MS and Global Natural Products Social Molecular Networking (GNPS). The results show that the extracts of five strains exhibited higher AChE inhibition ratios than the positive control compound, ‘tacrine’, for which the ratio was 89.8% at 200 μg/ml. Six strains displayed both AChE inhibition (inhibition ratios > 20% at 200 μg/ml) and DPPH scavenging activity (scavenging ratios > 30% at 200 μg/ml) together with low Artemia larval toxicity (lethal rates < 12%). TLC autography showed that the fractioned extracts of four strains contained highly diverse and different bioactive constituents, including strains Talaromyces sp. C21-1, Aspergillus terreus C23-3, Trichoderma harzianum DLEN2008005, and Penicillium corylophilum TBG1-17. From the most potent sample F-11-1-b (derived from Aspergillus terreus C23-3), five AChE inhibitors and seven antioxidants were recognized as bioactive molecules by AChE coupled ultrafiltration followed by LC–MS/MS, and LC–MS/MS coupled with DPPH incubation. Furthermore, with the aid of GNPS, the AChE inhibitors were plausibly annotated as territrem analogues including territrems A–C/D, arisugacin A and an unknown compound 4, and the seven antioxidants were assigned as butyrolactone Ι, aspernolide E, a phenolic derivative and possibly unknown compounds 8–10 and 12.

scholarly journals Antioxidant and Anti-Inflammatory Activities of Kigelia africana (Lam.) Benth.

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Alice Nabatanzi ◽  
Sanah M. Nkadimeng ◽  
Namrita Lall ◽  
John D. Kabasa ◽  
Lyndy J. McGaw
Keyword(s):  
Antioxidant Activity ◽  
Cell Viability ◽  
Radical Scavenging ◽  
Indigenous Communities ◽  
Inhibitory Effect ◽  
Inflammatory Activity ◽  
No Production ◽  
Fruit Extract ◽  
Cox 2 ◽  
Anti Inflammatory

Kigelia africana is used to manage inflammation among indigenous communities. We hypothesized that K. africana extracts contain phytoconstituents with good antioxidant and anti-inflammatory activities. The methanolic extract of K. africana fruits and Spathodea campanulata leaves (SPK04), K. africana aqueous fruit extract (KFM02), and K. africana acetone fruit extract (KFM05) were subjected to antioxidant and anti-inflammatory assays. Antioxidant activity was evaluated using the ABTS radical scavenging assay, and the MTT cell viability assay was used for cytotoxicity. The extracts were preincubated with enzymes and assayed for 15-LOX and COX-2 enzyme activity using an ELISA method. Nitric oxide (NO) inhibitory effect of the extracts was evaluated and measurement of proinflammatory cytokines (IL-1β, TNF-α, and IL-6) and the anti-inflammatory cytokine (IL-10) was done using ELISA kits. SPK04 had the highest antioxidant activity with a mean inhibition of 99.37 ± 0.56% and an IC50 of 4.28 µg/mL. SPK04 and KFM05 did not inhibit 15-LOX as their IC50 values were >1000 μg/mL. All extracts were safe on Vero cells at the highest concentration (200 µg/mL) tested. KFM02 was the best inhibitor of NO production and had the highest cell viability at both the lowest (50 µg/mL) and highest concentrations (200 µg/mL). SPK04 was the best COX-2 inhibitor while KFM05 expressed the strongest suppression effect for IL-β and IL-6. KFM02 did not inhibit IL-6 at the highest concentration (200 µg/mL). The order of suppression of TNF-α by the extracts differed across concentrations, KFM05 > SPK04 > KFM02 at 200 µg/mL, KFM02 > SPK04 > KFM05 at 100 µg/mL, and SPK04 > KFM02 > KFM05 at 50 µg/mL. All the tested extracts had no inhibitory effect against IL-10. SPK04, KFM05, and KFM02 had good antioxidant and anti-inflammatory activity and this supports their use as potential anti-inflammatory therapies. This study presents for the first time the antioxidant and anti-inflammatory activity of K. africana and S. campanulata polyherbal extract. It is also among the very few studies that have reported the inhibitory effect of cytokines IL-1β, TNF-α, IL-6, and IL-10 by K. africana.

scholarly journals New Acetylated Saponins from the Leaves of Trevesia palmata

2018 ◽  
Vol 13 (4) ◽  
pp. 1934578X1801300
Author(s):  
Le Thi Thanh Thao ◽  
Do Quyen ◽  
Duong Binh Vu ◽  
Bui Huu Tai ◽  
Phan Van Kiem
Keyword(s):  
Alkaline Hydrolysis ◽  
Nmr Spectra ◽  
Inhibitory Effect ◽  
No Production ◽  
Esi Ms ◽  
Chemical Structures ◽  
Bv2 Cells ◽  
Weak Activity

Two new acetylated saponins, acetyltrevesiasaponins A (1) and B (2), were isolated from the leaves of Trevesia palmata. Their chemical structures were determined by analysis of HR-ESI-MS and NMR spectra. Compound 2 was also confirmed by alkaline hydrolysis and identification its prosapogenin 2a. Compounds 1, 2, and 2a were evaluated inhibitory effect on NO production in LPS stimulated BV2 cells. Compound 2 showed weak activity (IC50 40.7 μM).

Inhibitory effect of isolated constituents from sclerotia of Poria cocos on LPS-induced NO production

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
SR Lee ◽  
S Lee ◽  
HJ Eom ◽  
HR Kang ◽  
JS Yu ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
No Production ◽  
Poria Cocos

Synthesis, Characterization, Antimicrobial and Antioxidant Potential of Diazenyl Chalcones

2018 ◽  
Vol 18 (10) ◽  
pp. 844-856 ◽  
Author(s):  
Harmeet Kaur ◽  
Balasubramanian Narasimhan
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antioxidant Potential ◽  
Dilution Method ◽  
Dpph Assay ◽  
Antimicrobial Potential ◽  
Structural Conformation ◽  
Uv Visible ◽  
Tube Dilution Method

A series of diazenyl chalcones was prepared by base catalyzed Claisen-Schmidt condensation of synthesized hydroxy substituted acetophenone azo dye with various substituted aromatic/ heteroaromatic aldehydes. The structural conformation of synthesized chalcones was done by a number of physicochemical and spectral means like FTIR, UV-visible, mass, NMR spectroscopy and CHNS/O analysis. These diazenyl chalcones were assessed for their in vitro antimicrobial potential against several Gram-negative, Gram-positive bacterial and fungal strains by serial tube dilution method. The fluconazole and cefadroxil were used as standard drugs. The target compounds were also evaluated for their antioxidant potential by DPPH assay. (2E)-3-(2,4-Dichlorophenyl)-1-(4-((2,6- dihydroxyphenyl)diazenyl)phenyl)prop-2-en-1-one (C-7) had shown very good antimicrobial potential with MIC ranges from 3.79 to 15.76 μg/ml against most of the tested microorganisms. Most of the synthesized diazenyl chalcones were found to be active against B. subtilis. The (2E)-1-(5-((2-Chloro- 4-nitrophenyl)diazenyl)-2-hydroxyphenyl)-3-(2-hydroxynaphthalen-1-yl)prop-2-en-1-one (C-10) had shown high free radical-scavenging activity when compared with the ascorbic acid as the reference antioxidant.

Curcumin-based antioxidant and glycohydrolase inhibitor compounds: Synthesis and in vitro appraisal of the dual activity against diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Enzyme Inhibitor ◽  
Radical Scavenging Activity ◽  
Curcuma Longa ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Inhibitory Effect ◽  
Curcumin Derivatives ◽  
Reducing Power Assay

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.

scholarly journals Optimized Supercritical CO2 Extraction Enhances the Recovery of Valuable Lipophilic Antioxidants and Other Constituents from Dual-Purpose Hop (Humulus lupulus L.) Variety Ella

Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 918
Author(s):  
Nóra Emilia Nagybákay ◽  
Michail Syrpas ◽  
Vaiva Vilimaitė ◽  
Laura Tamkutė ◽  
Audrius Pukalskas ◽  
...  
Keyword(s):  
Supercritical Co2 ◽  
Antioxidant Properties ◽  
Extraction Yield ◽  
Biologically Active ◽  
High Yield ◽  
Acid Extraction ◽  
Supercritical Co2 Extraction ◽  
Bioactive Constituents ◽  
Total Extract

The article presents the optimization of supercritical CO2 extraction (SFE-CO2) parameters using response surface methodology (RSM) with central composite design (CCD) in order to produce single variety hop (cv. Ella) extracts with high yield and strong in vitro antioxidant properties. Optimized SFE-CO2 (37 MPa, 43 °C, 80 min) yielded 26.3 g/100 g pellets of lipophilic fraction. This extract was rich in biologically active α- and β-bitter acids (522.8 and 345.0 mg/g extract, respectively), and exerted 1481 mg TE/g extract in vitro oxygen radical absorbance capacity (ORAC). Up to ~3-fold higher extraction yield, antioxidant recovery (389.8 mg TE/g pellets) and exhaustive bitter acid extraction (228.4 mg/g pellets) were achieved under the significantly shorter time compared to the commercially used one-stage SFE-CO2 at 10–15 MPa and 40 °C. Total carotenoid and chlorophyll content was negligible, amounting to <0.04% of the total extract mass. Fruity, herbal, spicy and woody odor of extracts could be attributed to the major identified volatiles, namely β-pinene, β-myrcene, β-humulene, α-humulene, α-selinene and methyl-4-decenoate. Rich in valuable bioactive constituents and flavor compounds, cv. Ella hop SFE-CO2 extracts could find multipurpose applications in food, pharmaceutical, nutraceutical and cosmetics industries.

Ultraviolet blocking and antioxidant polyvinyl alcohol films incorporated with baicalin extraction from Scutellaria baicalensis Georgi

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Jinshu Liu ◽  
Xiaoyan Ma ◽  
Wenzhao Shi ◽  
Jianwei Xing ◽  
Chaoqun Ma ◽  
...  
Keyword(s):  
Water Vapor ◽  
Polyvinyl Alcohol ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Water Vapor Permeability ◽  
Scutellaria Baicalensis ◽  
Vapor Permeability ◽  
Protective Film ◽  
Uv Blocking

Abstract Baicalin, an active flavonoid ingredient of Scutellaria baicalensis Georgi, was extracted by heat reflux extraction and showed the same significance UV absorption property with standard baicalin. Active films were prepared from polyvinyl alcohol (PVA) containing baicalin extract by casting method. The effect of baicalin extracts on the UV-blocking, optical, antioxidant property, water vapor permeability, swelling and mechanical properties of the films were studied. UV–vis transmittance spectra showed that PVA films incorporated with baicalin extract blocked ultraviolet light range from 280–400 nm even with low concentration of baicalin (0.5 wt%) and maintain the high transparency in visible spectrum. The outstanding UV-blocking properties of PVA films incorporated with baicalin extract were also confirmed by Rhodamine B degradation. Baicalin conferred antioxidant properties to PVA films as determined by DPPH radical scavenging activity. Due to the interaction between hydroxy groups of baicalin and PVA molecule, water vapor permeability, swelling and elongation at break of the films were decreased accompanied with the increasing in tensile strength and Young’s modulus. FTIR reveal that the interaction between PVA molecules was significant changed by the introduction of baicalin. These results suggest that PVA film incorporated with baicalin extract can be used for the development of functional protective film.

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