scholarly journals Scutellaria barbata D. Don Inhibits the Main Proteases (Mpro and TMPRSS2) of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infection

Viruses ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 826
Author(s):  
Sheng-Teng Huang ◽  
Yeh Chen ◽  
Wei-Chao Chang ◽  
Hsiao-Fan Chen ◽  
Hsiang-Chun Lai ◽  
...  
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Major Constituent ◽  
Inhibitory Effects ◽  
Active Components ◽  
Scutellaria Barbata ◽  
Cellular Models ◽  
Experimental Approaches ◽  
Infection Inhibition ◽  
Global Population ◽  
Dependent Mechanism

In late 2019, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pandemic emerged to severely impact the global population, creating an unprecedented need for effective treatments. This study aims to investigate the potential of Scutellaria barbata D. Don (SB) as a treatment for SARS-CoV-2 infection through the inhibition of the proteases playing important functions in the infection by SARS-CoV-2. FRET assay was applied to investigate the inhibitory effects of SB on the two proteases involved in SARS-CoV-2 infection, Mpro and TMPRSS2. Additionally, to measure the potential effectiveness of SB treatment on infection inhibition, cellular models based on the Calu3 and VeroE6 cells and their TMPRSS2- expressing derivatives were assessed by viral pseudoparticles (Vpp) infection assays. The experimental approaches were conjugated with LC/MS analyses of the aqueous extracts of SB to identify the major constituent compounds, followed by a literature review to determine the potential active components of the inhibitory effects on protease activities. Our results showed that SB extracts inhibited the enzyme activities of Mpro and TMPRSS2. Furthermore, SB extracts effectively inhibited SARS-CoV-2 Vpp infection through a TMPRSS2-dependent mechanism. The aqueous extract analysis identified six major constituent compounds present in SB. Some of them have been known associated with inhibitory activities of TMPRSS2 or Mpro. Thus, SB may effectively prevent SARS-CoV-2 infection and replication through inhibiting Mpro and TMPRSS2 protease activities.

452 IN VIVO INHIBITORY EFFECTS OF HEPATITIS B VIRUS X PROTEIN ON LIVER REGENERATION THROUGH A IL-6 DEPENDENT MECHANISM

2012 ◽  
Vol 56 ◽  
pp. S179
Author(s):  
I. Quétier ◽  
N. Brezillon ◽  
H. Massinet ◽  
S. Berissi ◽  
P. Soussan ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Liver Regeneration ◽  
Inhibitory Effects ◽  
X Protein ◽  
B Virus ◽  
Dependent Mechanism

Inhibitory Effects of Active Fraction and Its Main Components of Shaofu Zhuyu Decoction on Uterus Contraction

2010 ◽  
Vol 38 (04) ◽  
pp. 777-787 ◽  
Author(s):  
Shulan Su ◽  
Yongqing Hua ◽  
Jin-Ao Duan ◽  
Wei Zhou ◽  
Erxin Shang ◽  
...  
Keyword(s):  
Ferulic Acid ◽  
Vanillic Acid ◽  
Uterine Contraction ◽  
Active Fraction ◽  
Inhibitory Effects ◽  
Active Components ◽  
Traditional Use ◽  
Pregnant Mice ◽  
Main Components

Shaofu Zhuyu decoction is a famous formula for treating primary dysmenorrhea in China since the Qing dynasty. In this paper, the inhibitory effects of active-guided fraction and its main bioactive components of Shaofu Zhuyu decoction on a model of non-pregnant mice uterine contraction induced by oxytocin in vitro were investigated. Qualitative and quantitative chemical analyses were used to correlate the chemical composition of active fraction with the spasmolytic effects. Seven ingredients in the active fraction were identified and quantified by HPLC-DAD. Three ingredients, ferulic acid, vanillic acid, and typhaneoside, were evaluated for their effects on mice isolated uterine contraction induced by oxytocin in vitro. The ED50 of them were 63.0 μg/ml, 57.6 μg/ml, 109.7 μg/ml, respectively. Furthermore, the inhibitory activity of the combination of these three compounds was prior to the fraction and seven compounds group. The ED50 was 65.5 μg/ml. The data stated that ferulic acid, vanillic acid, and typhaneoside were possibly the main active components in the bioactive fraction of Shaofu Zhuyu decoction. The study also implied that Shaofu Zhuyu decoction may have direct inhibitory effects on the contractility of the mice uterus and justified the traditional use of the prescription for treating the uterine cramping associated dysmenorrhea.

scholarly journals Erratum to “Inhibitory Effects of Litsea cubeba Oil and Its Active Components on Aspergillus flavus”

2021 ◽  
Vol 2021 ◽  
pp. 1-1
Author(s):  
Shiqi Xia ◽  
Hong Lin ◽  
Peilin Zhu ◽  
Peiling Wang ◽  
Shengliang Liao ◽  
...  
Keyword(s):  
Aspergillus Flavus ◽  
Inhibitory Effects ◽  
Active Components ◽  
Litsea Cubeba

A redox O2 sensor modulates the SR Ca2+ countercurrent through voltage- and Ca(2+)-dependent Cl- channels

1997 ◽  
Vol 272 (1) ◽  
pp. C324-C332 ◽  
Author(s):  
J. I. Kourie
Keyword(s):  
Inhibitory Action ◽  
Alkylating Agent ◽  
Hill Coefficient ◽  
Channel Activity ◽  
Inhibitory Effects ◽  
Channel Activation ◽  
Cytosolic Side ◽  
Cl Channels ◽  
Conductance State ◽  
Dependent Mechanism

The activity of a relatively small Cl- (SCl) channel in the sarcoplasmic reticulum (SR) vesicles of rabbit skeletal muscle was preserved following their reconstitution into lipid bilayer. Reducing PO2 from approximately 150 to < 1 Torr in the cis-side (cytosolic) reversibly inhibited the channel activity within 2 min. The modulatory effects, deduced from reduction in Cl- current levels and in kinetic parameters of channel activation, in normoxic (PO2 approximately 150 Torr) and hypoxic (low PO2 < 1 Torr) solutions were mimicked by oxidizing and reducing agents, respectively. Cl- current transitions to the main open conductance state were increased by 100 microM of the specific sulfhydryl (SH)-oxidizing agent 4,4'-dithiodipyridine and inhibited by the SH-reducing agent glutathione (GSH) with a Hill coefficient of 8 and inhibition constant of approximately 3.1 mM. The inhibitory effects of 5 mM [GSH]cis were prevented by prior addition of 1 mM iodoacetamide, an alkylating agent, to the cytosolic side of the channel. These findings suggest that an SH-dependent mechanism (redox couple, e.g., reduced/oxidized glutathione) could be involved in the gating of the SCl channel in such a way that SH oxidation (GSSH) favors the open state of the channel, and SH reduction (GSH), which mimics the inhibitory action of low PO2, favors the closed state.

scholarly journals Gallic Acid Attenuates Platelet Activation and Platelet-Leukocyte Aggregation: Involving Pathways of Akt and GSK3β

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Shih-Sheng Chang ◽  
Viola S. Y. Lee ◽  
Yu-Lun Tseng ◽  
Kuan-Cheng Chang ◽  
Kuen-Bao Chen ◽  
...  
Keyword(s):  
Gallic Acid ◽  
Platelet Activation ◽  
Causes Of Death ◽  
Red Wine ◽  
Mechanistic Explanation ◽  
Major Constituent ◽  
Inhibitory Effects ◽  
Leukocyte Aggregation ◽  
Antioxidant Effects

Platelet activation and its interaction with leukocytes play an important role in atherothrombosis. Cardiovascular diseases resulted from atherothrombosis remain the major causes of death worldwide. Gallic acid, a major constituent of red wine and tea, has been believed to have properties of cardiovascular protection, which is likely to be related to its antioxidant effects. Nonetheless, there were few and inconsistent data regarding the effects of gallic acid on platelet function. Therefore, we designed thisin vitrostudy to determine whether gallic acid could inhibit platelet activation and the possible mechanisms. From our results, gallic acid could concentration-dependently inhibit platelet aggregation, P-selectin expression, and platelet-leukocyte aggregation. Gallic acid prevented the elevation of intracellular calcium and attenuated phosphorylation of PKCα/p38 MAPK and Akt/GSK3βon platelets stimulated by the stimulants ADP or U46619. This is the first mechanistic explanation for the inhibitory effects on platelets from gallic acid.

scholarly journals Isolation and Identification of Benzochroman and Acylglycerols from Massa Medicata Fermentata and Their Inhibitory Effects on LPS-Stimulated Cytokine Production in Bone Marrow-Derived Dendritic Cells

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2400 ◽  
Author(s):  
Ya Sun ◽  
Seo Yang ◽  
Young-Sang Koh ◽  
Young Kim ◽  
Wei Li
Keyword(s):  
Bone Marrow ◽  
Dendritic Cells ◽  
Scientific Basis ◽  
Inhibitory Effects ◽  
Active Components ◽  
Isolation And Identification ◽  
Chemical Structures ◽  
Tnf Α ◽  
Ic50 Values ◽  
Reported Data

Massa Medicata Fermentata (MMF), known as Shenqu, is an important traditional Chinese medicine widely used to treat indigestion, vomiting, and diarrhea. In this study, a new benzochroman, 3(S)-3,4-dihydro-5,10-di-β-d-glucopyranoside-2,2-dimethyl-2H-naphtho(2,3-b)pyran-3-ol (1), and five known galactosyl acylglycerols (2–6) were isolated from a methanol extract from MMF. In addition, their chemical structures were determined by chemical and spectroscopic methods, which were compared with the previously reported data. Furthermore, the effects of isolated compounds on lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells were investigated. Compounds 1–3 exhibited significant inhibitory effects on the LPS-induced production of IL-6 and IL-12 p40, with IC50 values ranging from 1.6 to 10.2 μM. Compounds 2 and 3 also exhibited strong inhibitory effects on the LPS-stimulated production of TNF-α with IC50 values of 12.0 and 11.2 μM, respectively. The results might provide a scientific basis for the development of the active components in MMF, as well as for novel anti-inflammatory agents.

neo-Clerodane Diterpenoids from Scutellaria barbata and Their Inhibitory Effects on LPS-Induced Nitric Oxide Production

2015 ◽  
Vol 78 (9) ◽  
pp. 2292-2296 ◽  
Author(s):  
Eung Tae Yeon ◽  
Jin Woo Lee ◽  
Chul Lee ◽  
Qinghao Jin ◽  
Hari Jang ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Production ◽  
Inhibitory Effects ◽  
Scutellaria Barbata ◽  
Oxide Production ◽  
Clerodane Diterpenoids

scholarly journals Rapid Characterization of Chemical Components in Edible Mushroom Sparassis crispa by UPLC-Orbitrap MS Analysis and Potential Inhibitory Effects on Allergic Rhinitis

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 3014 ◽  
Author(s):  
Zhixin Wang ◽  
Jingyu Liu ◽  
Xiangjian Zhong ◽  
Jinjie Li ◽  
Xin Wang ◽  
...  
Keyword(s):  
Allergic Rhinitis ◽  
High Performance ◽  
Edible Mushroom ◽  
Inflammatory Activity ◽  
Chemical Components ◽  
Inhibitory Effects ◽  
Active Components ◽  
Proinflammatory Mediators ◽  
Sparassis Crispa ◽  
Anti Inflammatory

Sparassis crispa is a kind of edible fungus widely grows in the north temperate zone, which shows various medicinal properties. Due to the complexity of chemical constitutes of this species, few investigations have acquired a comprehensive configuration for the chemical profile of it. In this study, a strategy based on ultra-high performance liquid chromatography (UPLC) combined with Orbitrap mass spectrometer (MS) was established for rapidly characterizing various chemical components in S. crispa. Through the summarized MS/MS fragmentation patterns of reference compounds and systematic identification strategy, a total of 110 components attributed to six categories were identified for the first time. Moreover, allergic rhinitis (AR) is a worldwide inflammatory disease seriously affecting human health, and the development of drugs to treat AR has been a topic of interest. It has been reported that the extracts of S. crispa showed obvious inhibitory effects on degranulation of mast cell- and allergen-induced IgE and proinflammatory mediators, but the active components and specific mechanism were still not clear. Src family kinases (SFKs) participate in the initial stage of allergy occurrence, which are considered the targets of AR treatment. Herein, on the basis of that self-built chemical database, virtual screening was applied to predict the potential SFKs inhibitors in S. crispa, using known crystal structures of Hck, Lyn, Fyn, and Syk as receptors, followed by the anti-inflammatory activity evaluation for screened hits by intracellular calcium mobilization assay. As results, sparoside A was directly confirmed to have strong anti-inflammatory activity with an IC50 value of 5.06 ± 0.60 μM. This study provides a useful elucidation for the chemical composition of S. crispa, and demonstrated its potential inhibitory effects on AR, which could promote the research and development of effective agents from natural resources.

scholarly journals Arylalkanones from Horsfieldia macrobotrys are Effective Antidiabetic Agents Achieved by α-Glucosidase Inhibition and Radical Scavenging

2015 ◽  
Vol 10 (2) ◽  
pp. 1934578X1501000
Author(s):  
Rico Ramadhan ◽  
Preecha Phuwapraisirisan
Keyword(s):  
Ascorbic Acid ◽  
Mixed Type ◽  
Competitive Inhibition ◽  
Critical Role ◽  
Radical Scavenging ◽  
Inhibitory Effects ◽  
Active Components ◽  
Diabetes Therapy ◽  
Antidiabetic Agents ◽  
East Kalimantan

Horsfielda macrobotrys Merr has long been used by Dayak people in East Kalimantan of Indonesia, for diabetes therapy. Inspired by ethnopharmacological use and promising α-glucosidase and radical scavenging activities, an attempt to identify the active components was carried out. Bioassay-guided isolation yielded two related arylalkanones named 1-(2,4,6-trihydroxyphenyl)-9-phenylnonan-1-one (1) and malabaricone A (2). Arylalkanone 1 showed potent radical scavenging comparable with that of the standard antioxidant, ascorbic acid, and promising inhibition against α-glucosidases. Noticeably, arylalkanone 1 was 3-30 times more potent than malabaricone A (2) in all bioassays examined, thus suggesting the critical role in exerting bioactivities of the hydroxy group on the aryl moiety. This hypothesis was also supported by reduction in inhibitory effects of the methyl ether analogues 1a and 2a. Arylalkanone 1 inhibited yeast α-glucosidase in a mixed-type manner in which the noncompetitive pathway was dominant over competitive inhibition. This study is the first report of α-glucosidase inhibition of arylalkenone-type compounds and the first phytochemicals from H. macrobotrys.

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