• Genomics & Informatics
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• v.13 no.2
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• pp.60-67
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• 2015

The leading cause of cancer mortality globally amongst the women is due to human papillomavirus (HPV) infection. There is need to explore anti-cancerous drugs against this life-threatening infection. Traditionally, different natural compounds such as withaferin A, artemisinin, ursolic acid, ferulic acid, (-)-epigallocatechin-3-gallate, berberin, resveratrol, jaceosidin, curcumin, gingerol, indol-3-carbinol, and silymarin have been used as hopeful source of cancer treatment. These natural inhibitors have been shown to block HPV infection by different researchers. In the present study, we explored these natural compounds against E6 oncoprotein of high risk HPV18, which is known to inactivate tumor suppressor p53 protein. E6, a high throughput protein model of HPV18, was predicted to anticipate the interaction mechanism of E6 oncoprotein with these natural inhibitors using structure-based drug designing approach. Docking analysis showed the interaction of these natural inhibitors with p53 binding site of E6 protein residues 108-117 (CQKPLNPAEK) and help reinstatement of normal p53 functioning. Further, docking analysis besides helping in silico validations of natural compounds also helped elucidating the molecular mechanism of inhibition of HPV oncoproteins.

• Journal of Nutrition and Health
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• v.35 no.1
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• pp.53-59
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• 2002

Green tea has been recognized as a favorite beverage for centuries in Easter and Westers cultures. Recently, anti-tumor effects of green tea constituents have received increasing attention. However, the mechanism of catechin-mediated cytotoxicity against tumor cells remains to be elusive. To elucidate the mechanical insights of anti-tumor effects, (-)epigallocatechin-gallate(EGCG) of catechin was applied to human lung cancer A549 cells. (-)EGCG induced the death of A549 cells, which was revealed as apoptosis in DNA fragmentation assay. (-)EGCG induced the activation of caspase family cysteine proteases including capase-3, -8 and -9 proteases in A549 cells. Furthermore, (-)EGCG increased the phosphotransferase activity of c-Jun N-terminal kinase 1JNK 1), which further induced tole transcriptional activation of activating protein-1(AP-1) in A549 cells. We suggest that (-)EGCG-induced apotosis of A549 cells is mediated by signaling pathway involving caspase family cysteine protease, JNK1 and transcription factor, AP-1.

• Nutritional Sciences
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• v.8 no.3
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• pp.175-180
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• 2005

Green tea, which has high polyphenols amount, is thought to have hypocholesterolemic effects. The present study was performed to further examine the hypocholesterolemic action of green tea, especially (-) epigallocatechin gallate (EGCG) for its effect on diet-induced hypercholesterolemia in rats. Male Sprague-Dawley rats (n=15) were fed a green tea-free diet (control), $1.0\%$ green tea catechin (catechin) or $0.5\%$ green tea catechin EGCG for seven weeks. Hypercholesterolemia was induced by adding $1\%$ cholesterol and $0.5\%$ cholic acid to all diets. There was no difference in food intake and body weight gain among the groups. The green tea EGCG treatment led to a significant improvement in plasma levels of total cholesterol, low density lipoprotein (LDL)-cholesterol and high density lipoprotein (HDL)/LDL ratio (p<0.05). There was no significant effect on the plasma HDL-cholesterol level. The catechin treatment led to a 4.19-fold increase in the LDL-receptor mRNA level compared to the control, but the EGCG treatment did not affect the hepatic LDL-receptor mRNA level. Our results suggest that when blood cholesterol level is down-regulated by green tea EGCG, the LDL receptor gene-independent pathway may dominate the hypocholesterolemic action of EGCG.

• Natural Product Sciences
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• v.19 no.4
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• pp.281-285
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• 2013

This study was designed to investigate the nervous sedative effects of green tea. The sedative effect was evaluated by examination of Monoamine oxidases (MAOs) inhibitory activity in vitro in the brain and liver of rat fed on green tea cultivated and harvested from the different regions and periods. It showed that methanol extracts of green tea inhibited significantly the brain MAO-A activity. Especially late harvested green tea extracts showed potential inhibitory activity. The liver MAO-B activity was also inhibited by all of the green tea extracts with strong intensity. This study confirmed that major compounds of green tea such as catechin, epigallocatechin-3-gallate (EGCG) and L-theanine, which were well known for the main bioactive components in the tea plants, were not associated with the MAO inhibitory activities of green tea. These results suggested that a MAO inhibition activity comes from other minor tea components we have to search in the future.

• Journal of Life Science
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• v.12 no.2
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• pp.75-79
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• 2002

Tea catechins, the most important compounds in tea polyphenols, can efficiently scavenge superoxide anion free-radical ($O_2$.), hydroxyl radical. (.OH) The mechanism of scavenging active oxygen free radicals was investigated by ESR spin trapping technique and Chemiluminescence. Results showed that various tea catechins constitute an antioxidant cycle in accordance with the decreasing order of the first reductive potential, and produce the effect of cooperative strength each other. Esterificated catechins could scavenge active oxygen free radicals more effectively than the non-esterificated ones. When.OH and $O_2$.- were scavenged by (-)-epigallocatechin gallate [(-)- EGCG], the stoichiometric factors were 6, and the rate constants of scavenging reaction reached $7.71{\times}10^6$ and $3.52{\times}10^{11}$ L $mmol^{-1}s^{-1}$, respectively. In the mean time, tea catechins could scavenge superoxide anion fiee radical ($O_2$-.) and hydroxyl radical (.OH) in a dose dependent manner. But at higher concentration or pH value, tea catechins can induce the prooxidant.

• Genomics & Informatics
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• v.12 no.2
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• pp.64-70
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• 2014

Human papillomavirus (HPV) infection is the leading cause of cancer mortality among women worldwide. The life-threatening infection caused by HPV demands the need for designing anticancerous drugs. In the recent years, different compounds from natural origins, such as carrageenan, curcumin, epigallocatechin gallate, indole-3-carbinol, jaceosidin, and withaferin, have been used as a hopeful source of anticancer therapy. These compounds have been shown to suppress HPV infection by different researchers. In the present study, we explored these natural inhibitors against E6 oncoprotein of high-risk HPV-16, which is known to inactivate the p53 tumor suppressor protein. A robust homology model of HPV-16 E6 was built to anticipate the interaction mechanism of E6 oncoprotein with natural inhibitory molecules using a structure-based drug designing approach. Docking analysis showed the interaction of these natural compounds with the p53-binding site of E6 protein residues 113-122 (CQKPLCPEEK) and helped the restoration of p53 functioning. Docking analysis, besides helping in silico validation of natural compounds, also helps understand molecular mechanisms of protein-ligand interactions.

• International Journal of Oral Biology
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• v.30 no.3
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• pp.77-84
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• 2005

EGCG[(-)-epigallocatechin gallate], is a major component of green tea has been considered as a major antioxidant constituent. It has been considered as potential chemopreventive and chemotherapeutic agents. However, very little is known about the cellular actions by which EGCG mediates its therapeutic effects. Various aspects of antioxidant activity of EGCG were evaluated in this study. EGCG itself did not show significant cytotoxicity. Significant 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity was observed in all ranges of concentration ($0.8-100{\mu}g/ml$) used in this study. Protective effect of EGCG against hydrogen peroxide induced cell death was observed. Relatively high lipid peroxidation inhibitory activity were detected ($IC_{50}$ was about $20{\mu}g/ml$). EGCG also dose-dependently enhanced the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) in V79-4 cells. In concentrations of $100{\mu}g/ml$ of EGCG, activities of SOD, CAT and GPX were measured as 36.9 U/mg of protein, 22.9 U/mg of protein and 17.8 U/mg of protein, respectively. When these values were compared with those of the control groups (24.9 U/mg of protein, 14.9 U/mg of protein and 11.7 U/mg of protein), the relative increases were calculated as 48, 54 and 52%, respectively. Taken together, our findings suggest that EGCG can act as an antioxidant by scavenging radicals and enhancing antioxidant enzyme activities.

• Journal of the Korean Society of Food Science and Nutrition
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• v.24 no.2
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• pp.299-304
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• 1995

Antioxidative effect of tea extracts from green tea(steamed, roasted), oolong tea and black tea was investigated. Antioxidative activities of the crude catechin fraction were the most effective in oolong tea which contained the highest level of (-)-epigallocatechin gallate(EGCg). The water-soluble fraction obtained from oolong tea exhibited binding with more ferrous than copper ions. It showed a synergistic effect when used with an antioxidant such as BHT(0.5mg) and $\alpha$-tocopherol(2mg). Especially, this synergistic effect was exhibited more with BHT than with $\alpha$-tocopherol. Also steamed green tea, roasted green tea and oolong tea showed remarkable free radical scavenging action. The SC50(the concentration of a water-soluble fraction which is required to scavenge 50% of 100$\mu$M 1, 1-diphenyl-2-picryl hydrazyl radicals) of steamed and roasted green tea, oolong tea and black tea extracts were 11.3$\mu\textrm{g}$/ml, 11.4$\mu\textrm{g}$/ml, 12.7 $\mu\textrm{g}$/ml and 14.9$\mu\textrm{g}$/ml, respectively. It is assumed that the antioxidative activity of tea extracts is due to inhibition of peroxidation free radical scavenging and binding action of ferrous ions by mainly tea polyphenol compounds.

• Korean Journal of Pharmacognosy
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• v.50 no.1
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• pp.1-10
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• 2019

Recently, companion animal culture has grown rapidly and mature, raising interest in preventing and treating animal diseases. In particular, viral infection was a serious threat to companion animal health because there was no proper antiviral drugs. Synthetic antiviral drugs have limitations such as low efficiency, toxicity, and occurrence of resistant viruses. Therefore, attempts to find new anti-viral drugs from natural sources have continued. This review focused on the natural products and active substances that exhibit antiviral activity against three viruses: canine distemper virus (CDV), canine parvovirus (CPV), and feline calicivirus (FCV) that cause fatal diseases in dogs and cats. Natural plant extracts, flavonoids, polysaccharides, alkaloids and saponins showed antiviral activity with various mechanisms and differences in activity depending on the structure. Especially, quercetin and epigallocatechin-3-gallate (EGCG) showed antiviral activity through a multi-mechanism that interferes with the attachment and penetration stages of the virus and inhibits the viral polymerase within the cell. Some natural plant extracts showed a virucidal activity and showed the potential effect as a preventative agent to prevent the viral infection. This review is expected to provide research trend on the development of antiviral natural products for companion animals.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.561-571
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• 2002

The action mechanisms of several chemopreventive agents derived from herbal medicine and edible plants have become attractive issues in cancer research. Tea is the most widely consumed beverage worldwide. Recently, the cancer chemopreventive actions of tea have been intensively investigated. It have been demonstrated that the active principles of tea were attributed to their tea polyphenols. Recently, tremendous progress has been made in elucidating the molecular mechanisms of cancer chemoprevention by tea and tea polyphenols. The suppression of various tumor biomarkers including growth factor receptor tyrosine kinases, cytokine receptor kinases, P13K, phosphatases, ras, raf, MAPK cascades, NㆍFB, IㆍB kinase, PKA, PKB, PKC, c-jun, c-fos, c-myc, cdks, cyclins, and related transducing proteins by tea polyphenols has been studied in our laboratory and others. The IㆍB kinase (IKK) activity in LPS-activated murine macrophages (RAW 264.7 cells) was found to be inhibited by various tea polyphenols including (-) epigallocatechin-3-gallate (EGCG), theaflavin (TF-1), theaflavin-3-gal-late (TF-2) and theaflavin-3,3'-digallate (TF-3). TF-3 inhibited IKK activity in activated macrophages more strongly than did the other tea polyphenols. TF-3 inhibited both IKK1 and IKK2 activity and prevented the degradation of IㆍBㆍand IㆍBㆍin activated macrophage cells. The results suggested that the inhibition of IKK activity by TF-3 and other tea polyphenols could occur by a direct effect on IKKs or on upstream events in the signal transduction pathway. TF-3 and other tea polyphenols blocked phosphorylation of IB from the cytosolic fraction, inhibited NFB activity and inhibited increases in inducible nitric oxide synthase levels in activated macrophage. TF-3 and other tea polyphenols also inhibited strongly the activities of xanthine oxidase, cyclooxygenase, EGF-receptor tyrosine kinase and protein kinase C. These results suggest that TF-3 and other tea polyphenols may exert their cancer chemoprevention through suppressing tumor promotion and inflammation by blocking signal transduction. The mechanisms of this inhibition may be due to the blockade of the mitogenic and differentiating signals through modulating EGFR function, MAPK cascades, NFkB activation as wll as c-myc, c-jun and c-fos expression.