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

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.

Antibiotics ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 1550
Author(s):  
Karin Sasagawa ◽  
Hisanori Domon ◽  
Rina Sakagami ◽  
Satoru Hirayama ◽  
Tomoki Maekawa ◽  
...  

Streptococcus pneumoniae is a causative pathogen of several human infectious diseases including community-acquired pneumonia. Pneumolysin (PLY), a pore-forming toxin, plays an important role in the pathogenesis of pneumococcal pneumonia. In recent years, the use of traditional natural substances for prevention has drawn attention because of the increasing antibacterial drug resistance of S. pneumoniae. According to some studies, green tea exhibits antibacterial and antitoxin activities. The polyphenols, namely the catechins epigallocatechin gallate (EGCG), epigallocatechin (EGC), epicatechin gallate (ECG), and epicatechin (EC) are largely responsible for these activities. Although matcha green tea provides more polyphenols than green tea infusions, its relationship with pneumococcal pneumonia remains unclear. In this study, we found that treatment with 20 mg/mL matcha supernatant exhibited significant antibacterial activity against S. pneumoniae regardless of antimicrobial resistance. In addition, the matcha supernatant suppressed PLY-mediated hemolysis and cytolysis by inhibiting PLY oligomerization. Moreover, the matcha supernatant and catechins inhibited PLY-mediated neutrophil death and the release of neutrophil elastase. These findings suggest that matcha green tea reduces the virulence of S. pneumoniae in vitro and may be a promising agent for the treatment of pneumococcal infections.


2020 ◽  
Vol 21 (4) ◽  
pp. 1404 ◽  
Author(s):  
Yuchen Gu ◽  
Gautier Moroy ◽  
Jean-Louis Paul ◽  
Anne-Sophie Rebillat ◽  
Mara Dierssen ◽  
...  

Epigallocatechin gallate (EGCG) is an inhibitor of DYRK1A, a serine/threonine kinase considered to be a major contributor of cognitive dysfunctions in Down syndrome (DS). Two clinical trials in adult patients with DS have shown the safety and efficacy to improve cognitive phenotypes using commercial green tea extract containing EGCG (45% content). In the present study, we performed a preclinical study using FontUp®, a new nutritional supplement with a chocolate taste specifically formulated for the nutritional needs of patients with DS and enriched with a standardized amount of EGCG in young mice overexpressing Dyrk1A (TgBACDyrk1A). This preparation is differential with previous one used, because its green tea extract has been purified to up 94% EGCG of total catechins. We analyzed the in vitro effect of green tea catechins not only for EGCG, but for others residually contained in FontUp®, on DYRK1A kinase activity. Like EGCG, epicatechin gallate was a noncompetitive inhibitor against ATP, molecular docking computations confirming these results. Oral FontUp® normalized brain and plasma biomarkers deregulated in TgBACDyrk1A, without negative effect on liver and cardiac functions. We compared the bioavailability of EGCG in plasma and brain of mice and have demonstrated that EGCG had well crossed the blood-brain barrier.


2019 ◽  
Vol 15 (1) ◽  
pp. 3-10 ◽  
Author(s):  
Satheesh Babu Natarajan ◽  
Suriyakala Perumal Chandran ◽  
Sahar Husain Khan ◽  
Packiyaraj Natarajan ◽  
Karthiyaraj Rengarajan

Background: Tea (Camellia sinensis, Theaceae) is the second most consumed beverage in the world. Green tea is the least processed and thus contain rich antioxidant level, and believed to have most of the health benefits. </p><p> Methods: We commenced to search bibliographic collection of peer reviewed research articles and review articles to meet the objective of this study. </p><p> Results: From this study, we found that the tea beverage contains catechins are believed to have a wide range of health benefits which includes neuroprotective, anti-inflammatory, antiulcer, antiviral, antibacterial, and anti-parasitic effects. The four major catechin compounds of green tea are epigallocatechin (EGC), epicatechin (EC), epigallocatechin gallate (EGCG), and epicatechin gallate (ECG), of which EGCG is the major constituent and representing 50-80% of the total catechin content. And also contain xanthine derivatives such as caffeine, theophylline, and theobromine, and the glutamide derivative theanine. It also contains many nutritional components, such as vitamin E, vitamin C, fluoride, and potassium. We sum up the various green tea phytoconstituents, extraction methods, and its medicinal applications. </p><p> Conclusion: In this review article, we have summarized the pharmacological importance of green tea catechin which includes antioxidant potential, anti-inflammatory, antimicrobial, anticancer, antidiabetic and cosmetic application.


2008 ◽  
Vol 78 (3) ◽  
pp. 242-249 ◽  
Author(s):  
Jun Xu ◽  
Jue Wang ◽  
Fei Deng ◽  
Zhihong Hu ◽  
Hualin Wang

2021 ◽  
Author(s):  
Li Wang ◽  
Xin Huang ◽  
Huijuan Jing ◽  
Xin Ye ◽  
Chao Jiang ◽  
...  

Epigallocatechin gallate (EGCG) and epicatechin gallate (ECG) are the most abundant ester catechins of green tea polyphenols (GTPs) with numerous potential bioactivities, which have a wide application prospect in the...


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 ◽  
...  

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.


Pathogens ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 763
Author(s):  
Ameliya Dickson ◽  
Elise Cooper ◽  
Lenu B. Fakae ◽  
Bo Wang ◽  
Ka Lung Andrew Chan ◽  
...  

We examined the inhibitory effect of matcha green tea (Camellia sinensis) and epigallocatechin gallate (EGCg; the most abundant catechin in tea) on the vegetative growth and encystation of Acanthamoeba castellanii T4 genotype. The sulforhodamine B (SRB) stain-based colorimetric assay and hemocytometer counting were used to determine the reduction in A. castellanii trophozoite proliferation and encystation, in response to treatment with C. sinensis or EGCg. Fourier transform infrared (FTIR) microscopy was used to analyze chemical changes in the trophozoites and cysts due to C. sinensis treatment. Hot brewed and cold brewed matcha inhibited the growth of trophozoites by >40% at a 100 % concentration. EGCg at concentrations of 50 to 500 µM significantly inhibited the trophozoite growth compared to control. Hot brewed matcha (100% concentration) also showed an 87% reduction in the rate of encystation compared to untreated control. Although 500 µM of EGCg increased the rate of encystation by 36.3%, 1000 µM reduced it by 27.7%. Both percentages were not significant compared to control. C. sinensis induced more cytotoxicity to Madin Darby canine kidney cells compared to EGCg. FTIR chemical fingerprinting analysis showed that treatment with brewed matcha significantly increased the levels of glycogen and carbohydrate in trophozoites and cysts.


2019 ◽  
Vol 6 (7) ◽  
pp. 190179 ◽  
Author(s):  
Christine Xue ◽  
Joyce Tran ◽  
Hongsu Wang ◽  
Giovanna Park ◽  
Frederick Hsu ◽  
...  

Amyloid-β (Aβ) oligomers play a central role in the pathogenesis of Alzheimer's disease. Oligomers of different sizes, morphology and structures have been reported in both in vivo and in vitro studies, but there is a general lack of understanding about where to place these oligomers in the overall process of Aβ aggregation and fibrillization. Here, we show that Aβ42 spontaneously forms oligomers with a wide range of sizes in the same sample. These Aβ42 samples contain predominantly oligomers, and they quickly form fibrils upon incubation at 37°C. When fractionated using ultrafiltration filters, the samples enriched with smaller oligomers form fibrils at a faster rate than the samples enriched with larger oligomers, with both a shorter lag time and faster fibril growth rate. This observation is independent of Aβ42 batches and hexafluoroisopropanol treatment. Furthermore, the fibrils formed by the samples enriched with larger oligomers are more readily solubilized by epigallocatechin gallate, a main catechin component of green tea. These results suggest that the fibrils formed by larger oligomers may adopt a different structure from fibrils formed by smaller oligomers, pointing to a link between oligomer heterogeneity and fibril polymorphism.


1992 ◽  
Vol 282 (3) ◽  
pp. 883-889 ◽  
Author(s):  
C A Austin ◽  
S Patel ◽  
K Ono ◽  
H Nakane ◽  
L M Fisher

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.


2007 ◽  
Vol 25 (18_suppl) ◽  
pp. 8114-8114
Author(s):  
R. Burger ◽  
H. Czekalla ◽  
K. Richter ◽  
T. Ahrens ◽  
A. Guenther ◽  
...  

8114 Background: Epigallocatechin gallate (EGCG) is the predominant polyphenolic constituent of green tea leaves that possesses antitumor, antiinflammatory, and antioxidant activity. EGCG exerts its effects through potentially multiple mechanisms including inhibition of growth factor receptor signalling. The compound is currently under investigation in a phase I/II clinical trial for treatment of patients with early stage chronic lymphocytic leukemia at Mayo Clinic. The goal of our study was to examine the in vitro effects of EGCG in multiple myeloma (MM). Methods: A panel of human myeloma cell lines (n=6) including the IL-6 dependent INA-6 cell line was used to evaluate the sensitivity to EGCG. Cells were cultured for three days in the absence or presence of EGCG at concentrations between 6.25 μM and 100 μM. Cell viability was determined in a colorimetric tetrazolium (MTS) based assay and by trypanblue exclusion. For signalling experiments, INA-6 cells were IL-6 and serum starved and then treated with EGCG for two hours before IL-6 was added. Whole cell lysates were prepared and subjected to SDS-PAGE and Western blot analysis. Results: EGCG inhibited the in vitro growth of human myeloma cell lines by inducing cell death in a time and dose-dependent manner. IC50 concentrations were between 12,5 μM and 50 μM. IL-6 mediated growth of INA-6 cells was inhibited at similar doses. The addition of excess amounts of IL-6 could not protect from EGCG induced cytotoxicity. Pretreatment of INA-6 cells with EGCG resulted in a dose-dependent inhibition of IL-6 induced STAT3 tyrosine phosphorylation. In these cells, stimulation with IL-6 leads to upregulation of Mcl-1 expression. In contrast, phosphorylation of p44/p42 MAPK, which is constitutively activated in INA-6 cells, was not affected. Conclusion: EGCG has growth inhibitory activity on myeloma cells. Specific inhibition of signalling pathways that regulate expression of anti-apoptotic proteins could be one mechanism how EGCG exerts its activity. Our work provides the rationale for further studies to evaluate the effect of EGCG not only in B-CLL, but also in plasma cell tumors. No significant financial relationships to disclose.


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