scholarly journals Reynoutria Rhizomes as a Natural Source of SARS-CoV-2 Mpro Inhibitors–Molecular Docking and In Vitro Study

2021 ◽  
Vol 14 (8) ◽  
pp. 742
Author(s):  
Izabela Nawrot-Hadzik ◽  
Mikolaj Zmudziński ◽  
Adam Matkowski ◽  
Robert Preissner ◽  
Małgorzata Kęsik-Brodacka ◽  
...  
Keyword(s):  
Epigallocatechin Gallate ◽  
In Vitro Study ◽  
Epicatechin Gallate ◽  
Reynoutria Japonica ◽  
Beneficial Effects ◽  
Main Protease ◽  
Fluorescent Peptide ◽  
The World ◽  
Reynoutria Sachalinensis

More than a year has passed since the world began to fight the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) responsible for the Coronavirus disease 2019 (COVID-19) pandemic, and still it spreads around the world, mutating at the same time. One of the sources of compounds with potential antiviral activity is Traditional Chinese Medicinal (TCM) plants used in China in the supportive treatment of COVID-19. Reynoutria japonica is important part of the Shu Feng Jie Du Granule/Capsule-TCM herbal formula, recommended by China Food and Drug Administration (CFDA) for treatment of patients with H1N1- and H5N9-induced acute lung injury and is also used in China to treat COVID-19, mainly combined with other remedies. In our study, 25 compounds from rhizomes of R. japonica and Reynoutria sachalinensis (related species), were docked into the binding site of SARS-CoV-2 main protease. Next, 11 of them (vanicoside A, vanicoside B, resveratrol, piceid, emodin, epicatechin, epicatechin gallate, epigallocatechin gallate, procyanidin B2, procyanidin C1, procyanidin B2 3,3’-di-O-gallate) as well as extracts and fractions from rhizomes of R. japonica and R. sachalinensis were tested in vitro using a fluorescent peptide substrate. Among the tested phytochemicals the best results were achieved for vanicoside A and vanicoside B with moderate inhibition of SARS-CoV-2 Mpro, IC50 = 23.10 µM and 43.59 µM, respectively. The butanol fractions of plants showed the strongest inhibition of SARS-CoV-2 Mpro (IC50 = 4.031 µg/mL for R. sachalinensis and IC50 = 7.877 µg/mL for R. japonica). As the main constituents of butanol fractions, besides the phenylpropanoid disaccharide esters (e.g., vanicosides), are highly polymerized procyanidins, we suppose that they could be responsible for their strong inhibitory properties. As inhibition of SARS-CoV-2 main protease could prevent the replication of the virus our research provides data that may explain the beneficial effects of R. japonica on COVID-19 and identify the most active compounds worthy of more extensive research.

scholarly journals In vitro evidence for the involvement of H2S pathway in the effect of clodronate during inflammatory response

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Rosangela Montanaro ◽  
Alessio D’Addona ◽  
Andrea Izzo ◽  
Carlo Ruosi ◽  
Vincenzo Brancaleone
Keyword(s):  
Inflammatory Markers ◽  
In Vitro Study ◽  
Inos Expression ◽  
Beneficial Effects ◽  
Tnf Α ◽  
Inflammatory State ◽  
Anti Inflammatory ◽  
Underlying Mechanisms ◽  
Inflammatory Effect

AbstractClodronate is a bisphosphonate agent commonly used as anti-osteoporotic drug. Throughout its use, additional anti-inflammatory and analgesic properties have been reported, although the benefits described in the literature could not solely relate to their inhibition of bone resorption. Thus, the purpose of our in vitro study is to investigate whether there are underlying mechanisms explaining the anti-inflammatory effect of clodronate and possibly involving hydrogen sulphide (H2S). Immortalised fibroblast-like synoviocyte cells (K4IM) were cultured and treated with clodronate in presence of TNF-α. Clodronate significantly modulated iNOS expression elicited by TNF-α. Inflammatory markers induced by TNF-α, including IL-1, IL-6, MCP-1 and RANTES, were also suppressed following administration of clodronate. Furthermore, the reduction in enzymatic biosynthesis of CSE-derived H2S, together with the reduction in CSE expression associated with TNF-α treatment, was reverted by clodronate, thus rescuing endogenous H2S pathway activity. Clodronate displays antinflammatory properties through the modulation of H2S pathway and cytokines levels, thus assuring the control of the inflammatory state. Although further investigation is needed to stress out how clodronate exerts its control on H2S pathway, here we showed for the first the involvement of H2S in the additive beneficial effects observed following clodronate therapy.

scholarly journals Green tea phytocompounds targets Lansterol 14-α demethylase against ergosterol biosynthesis in Candida glabrata

2021 ◽  
Vol 12 (3) ◽  
pp. 1793-1797
Author(s):  
Priyanka Sirari ◽  
Jigisha Anand ◽  
Devvret ◽  
Ashish Thapliyal ◽  
Nishant Rai
Keyword(s):  
Green Tea ◽  
Candida Glabrata ◽  
Scientific Evidence ◽  
Epigallocatechin Gallate ◽  
Ergosterol Biosynthesis ◽  
Epicatechin Gallate ◽  
P450 Monooxygenase ◽  
Antifungal Potential ◽  
Inhibitory Potential

Green tea is credited as one of the world’s healthiest drinks with enriched antioxidants. It is known for its multi-beneficial health benefits against diabetes, blood pressure, hypertension, gastro-intestinal upset and is bestowed with significant antimicrobial potential. There are previous scientific evidence highlighting the antifungal potential of green tea and has identified it as a potential inhibitor of non-albicans Candida species. Lansterol 14-α demethylase (Erg 11) or CYP51 protein belongs to the cytochrome P450 monooxygenase (CYP) superfamily. Erg 11 is involved in ergosterol biosynthesis and has a significant role in azole drug resistance in Candida glabrata. The present study attempted to identify the inhibitory potential of green tea phytocompounds against inhibition of Erg 11 in Candida glabrata using bioinformatics tool viz., autodock vina software. Out of 15 green tea phytocompounds investigated, the study identified, Rutin (-10.5 kcal) Kaempferitrin (-9.4kcal), Epigallocatechin gallate (-10kcal), Epicatechin gallate (-8.7kcal), and Coumaroylquinic acid (-8.6kcal) acid as the potent phytocompounds which showed significant molecular interaction with Erg 11 in Candida glabrata. In attribution to the constant emergence of azole-resistant isolates, this preliminary analysis therefore, indicated the potential of green tea phytocompounds against inhibition of non-albicans Candida specific candidiasis. However, further, in vitro antimicrobial efficacy of these phytocompounds, the dose regime, drug likeliness, and cytotoxic analysis are required to be investigated and validated.

scholarly journals Bioactive Compounds and Antioxidant Activity of Mango Peel Liqueurs (Mangifera indica L.) Produced by Different Methods of Maceration

Antioxidants ◽  
2019 ◽  
Vol 8 (4) ◽  
pp. 102 ◽  
Author(s):  
Emanuela Monteiro Coelho ◽  
Marcelo Eduardo Alves Olinda de Souza ◽  
Luiz Claudio Corrêa ◽  
Arão Cardoso Viana ◽  
Luciana Cavalcanti de Azevêdo ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Bioactive Compounds ◽  
High Performance ◽  
Mangifera Indica ◽  
Epigallocatechin Gallate ◽  
Reversed Phase ◽  
Epicatechin Gallate ◽  
Bioactive Content ◽  
Mango Peels

The present work had the objective of producing liqueurs from mango peels (varieties “Haden” and “Tommy Atkins”) by processes of alcoholic maceration and maceration with pectinase, as well as to evaluate bioactive compounds by reversed-phase high-performance liquid chromatography coupled to diode array detection and fluorescence-detection (RP-HPLC/DAD/FD) and in vitro antioxidant activity (AOX), for by-product potential reuse. Alcoholic maceration in wine ethanol (65% v/v) produced liqueurs with higher phytochemical and AOX content. Maceration with pectinase resulted in liqueurs with higher quercetin-3-O-glucopyranoside content. In relation to mango varieties, Haden liqueurs presented higher bioactive content than Tommy Atkins liqueurs. The liqueurs presented high antioxidant activity. The main bioactive compounds found were flavanols (epicatechin-gallate, epigallocatechin-gallate), flavonols (quercetin-3-O-glucopyranoside and rutin), and phenolic acids (gallic acid, o-coumaric acid, and syringic acid). The present study showed that the production of liqueur enabled the recovering of an important part of the bioactive content of mango peels, suggesting an alternative for the recovery of antioxidant substances from this by-product.

scholarly journals EVALUATION OF BENEFICIAL EFFECTS OF LINUM USITATISSIMUM IN CONGESTIVE HEART FAILURE

2017 ◽  
Vol 9 (10) ◽  
pp. 62
Author(s):  
Pravin Tirgar ◽  
Limbasiya Kalpesh
Keyword(s):  
Heart Failure ◽  
Congestive Heart Failure ◽  
Linum Usitatissimum ◽  
Positive Inotropic Effect ◽  
Methanolic Extract ◽  
In Vitro Study ◽  
Control Group ◽  
Force Of Contraction ◽  
Beneficial Effects

Objective: Evaluation of beneficial effects of the seed of Linum usitatissimum in congestive heart failure.Methods: Methanolic extract of seeds of Linumusitatissimum (MELU) was prepared using soxhlet apparatus and oil of seed of Linumusitatissimum (OLU) was isolated using Clevenger apparatus. The positive inotropic action of methanolic extract of seeds of Linum usitatissimum was evaluated using Langendorff’s assembly (in vitro study). Beneficial effects of methanolic extract and oil of seeds of Linum usitatissimum were carried out by doxorubicin (1 mg/kg, i. p. within 3 w) to induce congestive heart failure (in vivo study). Parameters like electrocardiogram (ECG) recording and cytosolic Ca2+level and histopathology of the heart were carried out. In same study diuretic action was evaluated using Lipschitz model.Results: Methanolic extract of seeds of Linum usitatissimum showed significantly increased in positive inotropic effect (force of contraction 48.8±1.53 mm) as compared to control group (force of contraction 17.5±0.76 mm) on Langendorff”s study (in vitro study). In doxorubicin-induced congestive heart failure both MELU and OLU showed significant decreased QT (Note: In cardiology, the QT interval is a measure of the time between the start of the Q wave and the end of the T wave in the heart's electrical cycle. There is no full form for this medical word) interval. The histopathologic study indicated the least damage to the architecture of myocardial membrane. MELU and OLU increased urine output (5.66±0.16 ml and 6.58±0.15 ml respectively) significantly in Lipschitz model as compared to disease control group (4.58±0.15 ml).Conclusion: Present research work emphasizes that the seeds of Linum usitatissimum is beneficial in the management of congestive heart failure because of having positive inotropic effect, diuretic activity and control of rhythmicity of heart.

scholarly journals Site-specific DNA cleavage by mammalian DNA topoisomerase II induced by novel flavone and catechin derivatives

1992 ◽  
Vol 282 (3) ◽  
pp. 883-889 ◽  
Author(s):  
C A Austin ◽  
S Patel ◽  
K Ono ◽  
H Nakane ◽  
L M Fisher
Keyword(s):  
Dna Cleavage ◽  
Topoisomerase Ii ◽  
Complex Analysis ◽  
Antiviral Agents ◽  
Epigallocatechin Gallate ◽  
Tea Plant ◽  
Epicatechin Gallate ◽  
Pyrone Ring ◽  
Cleavable Complex

Four naturally occurring flavones (baicalein, quercetin, quercetagetin and myricetin) and two novel catechins [(-)-epicatechin gallate and (-)-epigallocatechin gallate, from the tea plant Camellia sinensis], which are known inhibitors of reverse transcriptase, were shown to induce mammalian topoisomerase II-dependent DNA-cleavage in vitro. The flavones differed from the catechins in causing unwinding of duplex DNA, but both classes of compound induced enzymic DNA breakage at the same sites on DNA. Moreover, the cleavage specificity was the same as that for the known intercalator 4′-(acridin-9-ylamino)methanesulphon-m-anisidide, suggesting that these agents trap the same cleavable complex. Analysis of some 30 flavonoid compounds allowed elucidation of the structure-function relationships for topoisomerase II-mediated DNA cleavage. For flavonoid inhibitors an unsaturated double bond between positions 2 and 3 of the pyrone ring and hydroxy groups at the 5, 7, 3′ and 4′ positions favoured efficient cleavage. Hydroxy substitutions could be tolerated at the 3, 6 and 5′ positions. Indeed, the absence of substituents at the 3′, 4′ and 5′ positions could be compensated by a hydroxy group at position 6 (baicalein). Similar requirements have been reported for flavonoid inhibitors of protein kinase C that act competitively with ATP, suggesting interaction with a conserved protein feature. Formation of the cleavable complex is a cytotoxic lesion that may contribute to the growth-inhibitory properties of flavones observed for three human tumour cell lines. These results are discussed in regard to the selectivity of antiviral agents.

scholarly journals Inhibitory Effects of Daiokanzoto (Da-Huang-Gan-Cao-Tang) on P-Glycoprotein

2012 ◽  
Vol 2012 ◽  
pp. 1-7
Author(s):  
Yuka Watanabe ◽  
Nobutomo Ikarashi ◽  
Toshiyuki Satoh ◽  
Kiyomi Ito ◽  
Wataru Ochiai ◽  
...  
Keyword(s):  
Epigallocatechin Gallate ◽  
Licorice Root ◽  
Drug Transporter ◽  
Inhibitory Effects ◽  
Epicatechin Gallate ◽  
Glycoprotein P ◽  
Atpase Assay ◽  
P Glycoprotein ◽  
Herbal Ingredient

We have studied the effects of various Kampo medicines on P-glycoprotein (P-gp), a drug transporter,in vitro. The present study focused on Daiokanzoto (Da-Huang-Gan-Cao-Tang), which shows the most potent inhibitory effects on P-gp among the 50 Kampo medicines studied, and investigated the P-gp inhibitory effects of Daiokanzoto herbal ingredients (rhubarb and licorice root) and their components by an ATPase assay using human P-gp membrane. Both rhubarb and licorice root significantly inhibited ATPase activity, and the effects of rhubarb were more potent than those of licorice root. The content of rhubarb in Daiokanzoto is double that in licorice root, and the inhibition patterns of Daiokanzoto and rhubarb involve both competitive and noncompetitive inhibition, suggesting that the inhibitory effects of Daiokanzoto are mainly due to rhubarb. Concerning the components of rhubarb, concentration-dependent inhibitory effects were observed for (−)-catechin gallate, (−)-epicatechin gallate, and (−)-epigallocatechin gallate. In conclusion, rhubarb may cause changes in the drug dispositions of P-gp substrates through the inhibition of P-gp. It appears that attention should be given to the interactions between these drugs and Kampo medicines containing rhubarb as an herbal ingredient.

scholarly journals Biomechanical-Based Protocol for in vitro Study of Cartilage Response to Cyclic Loading: A Proof-of-Concept in Knee Osteoarthritis

2021 ◽  
Vol 9 ◽  
Author(s):  
Paolo Caravaggi ◽  
Elisa Assirelli ◽  
Andrea Ensini ◽  
Maurizio Ortolani ◽  
Erminia Mariani ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Study ◽  
Cartilage Explants ◽  
Joint Loading ◽  
Design And Optimization ◽  
Cartilage Metabolism ◽  
Beneficial Effects ◽  
Physiological Loading

Osteoarthritis (OA) is an evolving disease and a major cause of pain and impaired mobility. A deeper understanding of cartilage metabolism in response to loading is critical to achieve greater insight into OA mechanisms. While physiological joint loading helps maintain cartilage integrity, reduced or excessive loading have catabolic effects. The main scope of this study is to present an original methodology potentially capable to elucidate the effect of cyclic joint loading on cartilage metabolism, to identify mechanisms involved in preventing or slowing down OA progression, and to provide preliminary data on its application. In the proposed protocol, the combination of biomechanical data and medical imaging are integrated with molecular information about chondrocyte mechanotransduction and tissue homeostasis. The protocol appears to be flexible and suitable to analyze human OA knee cartilage explants, with different degrees of degeneration, undergoing ex vivo realistic cyclic joint loading estimated via gait analysis in patients simulating mild activities of daily living. The modulation of molecules involved in cartilage homeostasis, mechanotransduction, inflammation, pain and wound healing can be analyzed in chondrocytes and culture supernatants. A thorough analysis performed with the proposed methodology, combining in vivo functional biomechanical evaluations with ex vivo molecular assessments is expected to provide new insights on the beneficial effects of physiological loading and contribute to the design and optimization of non-pharmacological treatments limiting OA progression.

scholarly journals Cytotoxic Effect of Addition of Different Concentrations of Nanohydroxyapatite to Resin Modified and Conventional Glass Ionomer Cements on L929 Murine Fibroblasts

2021 ◽  
Author(s):  
Parisa Golkar ◽  
Ladan Ranjbar Omrani ◽  
Shide Zohourinia ◽  
Elham Ahmadi ◽  
Faeze Asadian
Keyword(s):  
Cytotoxic Effect ◽  
In Vitro Study ◽  
Biological Properties ◽  
The Other ◽  
Glass Ionomer Cements ◽  
Glass Ionomer ◽  
Beneficial Effects ◽  
Significant Difference ◽  
Murine Fibroblasts

Objectives: In this study we assessed the cytotoxic effect of nanohydroxyapatite (NHA) incorporated into resin modified and conventional glass ionomer cements (RMGICs and CGICs) on L929 murine fibroblasts. Materials and Methods: In this in vitro study, 0wt%, 1wt%, 2wt%, 5wt%, 7wt% and 10wt% concentrations of NHA were added to Fuji II LC RMGIC and Fuji IX CGIC powders. Eighteen samples (5×3mm) were fabricated from each type of glass ionomer, in six experimental groups (n=3): CG0, CG1, CG2, CG5, CG7, CG10, RMG0, RMG1, RMG2, RMG5, RMG7, and RMG10. Samples were incubated for 72h. The overlaying solution was removed and added to L929 fibroblasts. The methyl thiazolyl tetrazolium bromide (MTT) assay was performed at 24, 48 and 72h. The wavelength was read by a spectrophotometer. Data were analyzed by ANOVA and Tukey’s test. Results: There was no significant difference in cytotoxicity of the two types of glass ionomers, with and without NHA, except for CG0 and RMG0 groups after 72h. RMG0 group was significantly more cytotoxic than the CG0 group (P<0.05). In CG groups during the first 24h, the cytotoxicity of CG5 and CG7 groups was significantly higher than that of CG1; while, there was no significant difference between the RMG groups. Cytotoxicity significantly decreased in all groups after 24h (P<0.05). Conclusion: Incorporation of NHA into Fuji II LC RMGIC and Fuji IX CGIC did not affect their biocompatibility and therefore its addition to these materials can provide favorable biological properties, especially considering its beneficial effects on the other properties of GICs.

scholarly journals Cytoprotective roles of epigallocatechin gallate and resveratrol on staurosporine-treated mesenchymal stem cells in in vitro culture

2021 ◽  
Vol 67 (3) ◽  
pp. 45-52
Author(s):  
Arkadiusz Burczak ◽  
Magdalena Kosiedowska ◽  
Paulina Borkowska ◽  
Jan Kowalski
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Negative Impact ◽  
Colorimetric Assay ◽  
Antioxidant Properties ◽  
Circulatory System ◽  
Epigallocatechin Gallate ◽  
Regenerative Capacity ◽  
Beneficial Effects

Summary Introduction: There are many scientific reports on the beneficial effects of epigallocatechin gallate and resveratrol on the human body, e.g. antioxidant properties, a protective effect on the circulatory system and reduction of inflammation. Objective: The aim of the study was to evaluate the effect of these substances on the survival of mesenchymal stem cells (MSC) in the presence of the pro-apoptotic factor staurosporine. Methods: Cell viability WST-1 colorimetric assay. Results: It was confirmed that both 25 µM/ml and 50 µM/ml of epigallocatechin and 50 µM/ml of resveratrol statistically significantly increased the MSC survival rate. Conclusion: An excess supply of epigallocatechin gallate (50 µM/ml and higher) has a cytotoxic effect on MSC, which may have a negative impact on the body’s auto-regenerative capacity. Under toxic and stressful conditions, resveratrol and epigallocatechin gallate perform cytoprotective functions, thereby reducing the negative impact of toxic environmental conditions on the mesenchymal stem cells.

scholarly journals Ivermectin the Promising Drug to Stave off the COVID-19 Crisis: A Review

2021 ◽  
Vol 7 (2) ◽  
pp. 95-98
Author(s):  
Zakia Jahan ◽  
Masudul Hassan
Keyword(s):  
Infectious Diseases ◽  
Specific Treatment ◽  
In Vitro Study ◽  
Antiviral Effect ◽  
Viral Particles ◽  
The World ◽  
Infected Cells ◽  
Almost All ◽  
First Time

The Coronavirus disease 2019 (COVID-19) outbreak, forcing us to face unprecedented moments in the world. The huge devastating impact of the world due to the covid-19 attack causes the brink of no return. However, there is no proven and specific treatment for Covid -19. Very few medications have received Emergency Use of Authorization. A recent in vitro study was the first time to find out and to assess the antiviral effect of Ivermectin on COVID-19. The study showed that Ivermectin was active against COVID- 19-infected cells, was able to kill effectively almost all viral particles within 48 h. In these moments of crisis, FDA-approved ivermectin is a ray of hope. Bangladesh Journal of Infectious Diseases 2020;7(2):95-98

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