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Article ; Online: Ovatodiolide inhibits SARS-CoV-2 replication and ameliorates pulmonary fibrosis through suppression of the TGF-β/TβRs signaling pathway.

Chiou, Wei-Chung / Huang, Guan-Jhong / Chang, Tein-Yao / Hsia, Tzu-Lan / Yu, Hao-You / Lo, Jir-Mehng / Fu, Pin-Kuei / Huang, Cheng

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

2023 Volume 161, Page(s) 114481

Abstract: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection continues to pose threats to public health. The clinical manifestations of lung pathology in COVID-19 patients include sustained inflammation and pulmonary fibrosis. The macrocyclic ... ...

Abstract	Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection continues to pose threats to public health. The clinical manifestations of lung pathology in COVID-19 patients include sustained inflammation and pulmonary fibrosis. The macrocyclic diterpenoid ovatodiolide (OVA) has been reported to have anti-inflammatory, anti-cancer, anti-allergic, and analgesic activities. Here, we investigated the pharmacological mechanism of OVA in suppressing SARS-CoV-2 infection and pulmonary fibrosis in vitro and in vivo. Our results revealed that OVA was an effective SARS-CoV-2 3CLpro inhibitor and showed remarkable inhibitory activity against SARS-CoV-2 infection. On the other hand, OVA ameliorated pulmonary fibrosis in bleomycin (BLM)-induced mice, reducing inflammatory cell infiltration and collagen deposition in the lung. OVA decreased the levels of pulmonary hydroxyproline and myeloperoxidase, as well as lung and serum TNF-ɑ, IL-1β, IL-6, and TGF-β in BLM-induced pulmonary fibrotic mice. Meanwhile, OVA reduced the migration and fibroblast-to-myofibroblast conversion of TGF-β1-induced fibrotic human lung fibroblasts. Consistently, OVA downregulated TGF-β/TβRs signaling. In computational analysis, OVA resembles the chemical structures of the kinase inhibitors TβRI and TβRII and was shown to interact with the key pharmacophores and putative ATP-binding domains of TβRI and TβRII, showing the potential of OVA as an inhibitor of TβRI and TβRII kinase. In conclusion, the dual function of OVA highlights its potential for not only fighting SARS-CoV-2 infection but also managing injury-induced pulmonary fibrosis.
MeSH term(s)	Humans ; Mice ; Animals ; Pulmonary Fibrosis/chemically induced ; Pulmonary Fibrosis/drug therapy ; Pulmonary Fibrosis/metabolism ; SARS-CoV-2/metabolism ; COVID-19/metabolism ; Lung ; Diterpenes/adverse effects ; Bleomycin/pharmacology ; Transforming Growth Factor beta/metabolism ; Transforming Growth Factor beta1/metabolism ; Fibroblasts ; Signal Transduction
Chemical Substances	ovatodiolide ; Diterpenes ; Bleomycin (11056-06-7) ; Transforming Growth Factor beta ; Transforming Growth Factor beta1
Language	English
Publishing date	2023-03-10
Publishing country	France
Document type	Journal Article
ZDB-ID	392415-4
ISSN	1950-6007 ; 0753-3322 ; 0300-0893
ISSN (online)	1950-6007
ISSN	0753-3322 ; 0300-0893
DOI	10.1016/j.biopha.2023.114481
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Ud II Zs.198: Show issues

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Article ; Online: Ergosterol peroxide blocks HDV infection as a novel entry inhibitor by targeting human NTCP receptor.

Chiou, Wei-Chung / Lyu, Yi-Syuan / Hsia, Tzu-Lan / Chen, Jui-Chieh / Lin, Lie-Chwen / Chang, Ming-Fu / Hsu, Meng-Shiuan / Huang, Cheng

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

2023 Volume 170, Page(s) 116077

Abstract: Hepatitis D virus (HDV), which co-infects or superinfects patients with hepatitis B virus, is estimated to affect 74 million people worldwide. Chronic hepatitis D is the most severe form of viral hepatitis and can result in liver cirrhosis, liver failure, ...

Abstract	Hepatitis D virus (HDV), which co-infects or superinfects patients with hepatitis B virus, is estimated to affect 74 million people worldwide. Chronic hepatitis D is the most severe form of viral hepatitis and can result in liver cirrhosis, liver failure, and hepatocellular carcinoma (HCC). Currently, there are no efficient HDV-specific drugs. Therefore, there is an urgent need for novel HDV therapies that can achieve a functional cure or even eliminate the viral infection. In the HDV life cycle, agents targeting the entry step of HDV infection preemptively reduce the intrahepatic viral RNA. Human sodium taurocholate co-transporting polypeptide (hNTCP), a transporter of bile acids on the plasma membrane of hepatocytes, is an essential entry receptor of HDV and is a promising molecular target against HDV infection. Here, we investigated the effect of ergosterol peroxide (EP) on HDV infection in vitro and in vivo. EP inhibited HDV infection of hNTCP-expressing dHuS-E/2 hepatocytes by interrupting the early fusion/endocytosis step of HDV entry. Furthermore, molecular modeling suggested that EP hinders LHBsAg binding to hNTCP by blocking access to S267 and V263. In addition, we generated hNTCP-expressing transgenic (Tg) C57BL/6 mice using the Cre/loxP system for in vivo study. EP reduced the liver HDV RNA level of HDV-challenged hNTCP-Cre Tg mice. Intriguingly, EP downregulated the mRNA level of liver IFN-γ. We demonstrate that EP is a bona fide HDV entry inhibitor that acts on hNTCP and has the potential for use in HDV therapies.
MeSH term(s)	Mice ; Animals ; Humans ; Hepatitis Delta Virus/genetics ; Hepatitis Delta Virus/metabolism ; Carcinoma, Hepatocellular/drug therapy ; Carcinoma, Hepatocellular/metabolism ; Liver Neoplasms/metabolism ; Mice, Inbred C57BL ; Hepatitis D/drug therapy ; Hepatitis D/pathology ; Hepatitis B virus/physiology ; Hepatocytes ; Mice, Transgenic ; Symporters/metabolism
Chemical Substances	ergosterol-5,8-peroxide (UG9TN81TGH) ; Symporters
Language	English
Publishing date	2023-12-28
Publishing country	France
Document type	Journal Article
ZDB-ID	392415-4
ISSN	1950-6007 ; 0753-3322 ; 0300-0893
ISSN (online)	1950-6007
ISSN	0753-3322 ; 0300-0893
DOI	10.1016/j.biopha.2023.116077
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Article ; Online: α-Viniferin and ε-Viniferin Inhibited TGF-β1-Induced Epithelial-Mesenchymal Transition, Migration and Invasion in Lung Cancer Cells through Downregulation of Vimentin Expression.

Chiou, Wei-Chung / Huang, Cheng / Lin, Zi-Jun / Hong, Lian-Sheng / Lai, Yu-Heng / Chen, Jui-Chieh / Huang, Hsiu-Chen

Nutrients

2022 Volume 14, Issue 11

Abstract: Resveratrol has well-known anticancer properties; however, its oligomers, including α-viniferin, ε-viniferin, and kobophenol A, have not yet been well investigated. This is the first study examining the anti-epithelial-mesenchymal transition (EMT) ... ...

Abstract	Resveratrol has well-known anticancer properties; however, its oligomers, including α-viniferin, ε-viniferin, and kobophenol A, have not yet been well investigated. This is the first study examining the anti-epithelial-mesenchymal transition (EMT) effects of α-viniferin and ε-viniferin on A549, NCI-H460, NCI-H520, MCF-7, HOS, and U2OS cells. The results showed that α-viniferin and ε-viniferin significantly inhibited EMT, invasion and migration in TGF-β1- or IL-1β-induced non-small cell lung cancer. α-Viniferin and ε-viniferin also reversed TGF-β1-induced reactive oxygen species (ROS), MMP2, vimentin, Zeb1, Snail,
MeSH term(s)	Animals ; Benzofurans ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Cell Line, Tumor ; Cell Movement ; Down-Regulation ; Epithelial-Mesenchymal Transition ; Humans ; Lung Neoplasms/pathology ; Mice ; Stilbenes ; Transforming Growth Factor beta1/metabolism ; Vimentin/genetics ; Vimentin/metabolism
Chemical Substances	Benzofurans ; Stilbenes ; Transforming Growth Factor beta1 ; Vimentin ; epsilon-viniferin (62218-08-0) ; alpha-viniferin (62218-13-7)
Language	English
Publishing date	2022-05-30
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2518386-2
ISSN	2072-6643 ; 2072-6643
ISSN (online)	2072-6643
ISSN	2072-6643
DOI	10.3390/nu14112294
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Article ; Online: Identification of a novel interaction site between the large hepatitis delta antigen and clathrin that regulates the assembly of genotype III hepatitis delta virus.

Chiou, Wei-Chung / Lu, Hsu-Feng / Chen, Jui-Chieh / Lai, Yu-Heng / Chang, Ming-Fu / Huang, Yuan-Li / Tien, Ni / Huang, Cheng

Virology journal

2022 Volume 19, Issue 1, Page(s) 163

Abstract: Background: Hepatitis delta virus (HDV), a satellite virus of hepatitis B virus (HBV), is a small, defective RNA virus strongly associated with the most severe form of hepatitis and progressive chronic liver disease and cirrhosis. Chronic hepatitis D, ... ...

Abstract	Background: Hepatitis delta virus (HDV), a satellite virus of hepatitis B virus (HBV), is a small, defective RNA virus strongly associated with the most severe form of hepatitis and progressive chronic liver disease and cirrhosis. Chronic hepatitis D, resulting from HBV/HDV coinfection, is considered to be the most severe form of viral hepatitis and affects 12-20 million people worldwide. Involved in the endocytosis and exocytosis of cellular and viral proteins, clathrin contributes to the pathogenesis and morphogenesis of HDV. Previously, we demonstrated that HDV-I and -II large hepatitis delta antigens (HDAg-L) possess a putative clathrin box that interacts with clathrin heavy chain (CHC) and supports HDV assembly. Methods: Virus assembly and vesicular trafficking of HDV virus-like particles (VLPs) were evaluated in Huh7 cells expressing HDV-I, -II and -III HDAg-L and hepatitis B surface antigen (HBsAg). To elucidate the interaction motif between HDAg-L and CHC, site-directed mutagenesis was performed to introduce mutations into HDAg-L and CHC and analyzed using coimmunoprecipitation or pull-down assays. Results: Comparable to HDV-I virus-like particles (VLPs), HDV-III VLPs were produced at a similar level and secreted into the medium via clathrin-mediated post-Golgi vesicular trafficking. Mutation at F27 or E33 of CHC abolished the binding of CHC to the C-terminus of HDV-III HDAg-L. Mutation at W207 of HDV-III HDAg-L inhibited its association with CHC and interfered with HDV-III VLP formation. We elucidated mechanism of the binding of HDV-III HDAg-L to CHC and confirmed the pivotal role of clathrin binding in the assembly of genotype III HDV. Conclusions: A novel W box which was identified at the C terminus of HDV-III HDAg-L is known to differ from the conventional clathrin box but also interacts with CHC. The novel W box of HDAg-L constitutes a new molecular target for anti-HDV-III therapeutics.
MeSH term(s)	Clathrin/metabolism ; Clathrin Heavy Chains/genetics ; Clathrin Heavy Chains/metabolism ; Genotype ; Hepatitis B Surface Antigens/metabolism ; Hepatitis B virus/genetics ; Hepatitis Delta Virus/genetics ; Hepatitis delta Antigens/chemistry ; Hepatitis delta Antigens/genetics ; Hepatitis delta Antigens/metabolism ; Humans ; RNA, Viral/metabolism ; Viral Proteins/genetics ; Virus Replication
Chemical Substances	Clathrin ; Hepatitis B Surface Antigens ; Hepatitis delta Antigens ; RNA, Viral ; Viral Proteins ; hepatitis delta virus large antigen ; Clathrin Heavy Chains (114899-12-6)
Language	English
Publishing date	2022-10-17
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2160640-7
ISSN	1743-422X ; 1743-422X
ISSN (online)	1743-422X
ISSN	1743-422X
DOI	10.1186/s12985-022-01866-3
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Article: Gut microbiota-directed intervention with high-amylose maize ameliorates metabolic dysfunction in diet-induced obese mice

Chiou, Wei-Chung / Lai, Wei-Han / Cai, Yu-Lin / Du, Meng-Lun / Lai, Hsi-Mei / Chen, Jui-Chieh / Huang, Hsiu-Chen / Liu, Hui-Kang / Huang, Cheng

Food & function. 2022 Sept. 22, v. 13, no. 18

2022

Abstract: Obesity is a chronic disease that may lead to the development of metabolic diseases, cardiovascular diseases, and cancers and has been predicted to affect one billion adults by 2030. Owing to the pivotal role of the gut microbiota in health, including ... ...

Abstract	Obesity is a chronic disease that may lead to the development of metabolic diseases, cardiovascular diseases, and cancers and has been predicted to affect one billion adults by 2030. Owing to the pivotal role of the gut microbiota in health, including metabolism and energy homeostasis, dietary fiber, the primary energy resource for the gut microbiota, not only helps reduce appetite and short-term food intake but also modulates the structure of the gut microbiota. In this study, we investigated whether high-amylose maize (HAM), with a particular amount of dietary fiber, improves dysmetabolism and gut microbiota dysbiosis in diet-induced obese mice. Promisingly, the HAM dietary intervention not only reduced body weight gain, adipocyte hypertrophy, and dyslipidemia but also mitigated non-alcoholic fatty liver disease, insulin resistance, impaired glucose tolerance, and inflammation in the liver and epididymal white adipose tissues in high-fat diet (HFD)-fed obese mice. In addition, the HAM dietary intervention ameliorated gut microbiota dysbiosis in HFD-fed mice. Changes in families, genera, and species of gut biota that have a relative abundance of 0.01% in at least one group were scrutinized. At the species level, HAM dietary intervention increased Bifidobacterium pseudolongum, Bifidobacterium animalis, Bifidobacterium bifidum, and Lactobacillus paraplantarum and decreased Streptococcus agalactiae, Mucispirillum schaedleri, and Alistipes indistinctus. This change in the gut microbiota driven by the HAM diet was strongly associated with obesity-related indices, highlighting the nutraceutical potential of HAM for improving overall metabolic health. Taken together, this study demonstrates the potential of the HAM diet for mediating metabolic syndrome and gut microbiota dysbiosis.
Keywords	Bifidobacterium animalis ; Bifidobacterium bifidum ; Bifidobacterium pseudolongum ; Lactobacillus paraplantarum ; Mucispirillum ; Streptococcus agalactiae ; adipocytes ; appetite ; body weight changes ; chronic diseases ; corn ; dietary fiber ; dietary supplements ; dysbiosis ; epididymis ; fatty liver ; food intake ; glucose tolerance ; high fat diet ; homeostasis ; hyperlipidemia ; hypertrophy ; inflammation ; insulin resistance ; intestinal microorganisms ; liver ; metabolic syndrome ; nutritional intervention ; obesity ; primary energy
Language	English
Dates of publication	2022-0922
Size	p. 9481-9495.
Publishing place	The Royal Society of Chemistry
Document type	Article
ZDB-ID	2612033-1
ISSN	2042-650X ; 2042-6496
ISSN (online)	2042-650X
ISSN	2042-6496
DOI	10.1039/d2fo01211a
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Identification of a novel interaction site between the large hepatitis delta antigen and clathrin that regulates the assembly of genotype III hepatitis delta virus

Chiou, Wei-Chung / Lu, Hsu-Feng / Chen, Jui-Chieh / Lai, Yu-Heng / Zhang, Mingfu / Huang, Yuan-Li / Tien, Ni / Huang, Cheng

Virol J. 2022 Dec., v. 19, no. 1 p.163-163

2022

Abstract: BACKGROUND: Hepatitis delta virus (HDV), a satellite virus of hepatitis B virus (HBV), is a small, defective RNA virus strongly associated with the most severe form of hepatitis and progressive chronic liver disease and cirrhosis. Chronic hepatitis D, ... ...

Abstract	BACKGROUND: Hepatitis delta virus (HDV), a satellite virus of hepatitis B virus (HBV), is a small, defective RNA virus strongly associated with the most severe form of hepatitis and progressive chronic liver disease and cirrhosis. Chronic hepatitis D, resulting from HBV/HDV coinfection, is considered to be the most severe form of viral hepatitis and affects 12–20 million people worldwide. Involved in the endocytosis and exocytosis of cellular and viral proteins, clathrin contributes to the pathogenesis and morphogenesis of HDV. Previously, we demonstrated that HDV-I and -II large hepatitis delta antigens (HDAg-L) possess a putative clathrin box that interacts with clathrin heavy chain (CHC) and supports HDV assembly. METHODS: Virus assembly and vesicular trafficking of HDV virus-like particles (VLPs) were evaluated in Huh7 cells expressing HDV-I, -II and -III HDAg-L and hepatitis B surface antigen (HBsAg). To elucidate the interaction motif between HDAg-L and CHC, site-directed mutagenesis was performed to introduce mutations into HDAg-L and CHC and analyzed using coimmunoprecipitation or pull-down assays. RESULTS: Comparable to HDV-I virus-like particles (VLPs), HDV-III VLPs were produced at a similar level and secreted into the medium via clathrin-mediated post-Golgi vesicular trafficking. Mutation at F27 or E33 of CHC abolished the binding of CHC to the C-terminus of HDV-III HDAg-L. Mutation at W207 of HDV-III HDAg-L inhibited its association with CHC and interfered with HDV-III VLP formation. We elucidated mechanism of the binding of HDV-III HDAg-L to CHC and confirmed the pivotal role of clathrin binding in the assembly of genotype III HDV. CONCLUSIONS: A novel W box which was identified at the C terminus of HDV-III HDAg-L is known to differ from the conventional clathrin box but also interacts with CHC. The novel W box of HDAg-L constitutes a new molecular target for anti-HDV-III therapeutics.
Keywords	Hepatitis B virus ; Hepatitis delta virus ; chronic hepatitis ; clathrin ; endocytosis ; exocytosis ; genotype ; hepatitis B antigens ; mixed infection ; morphogenesis ; pathogenesis ; people ; precipitin tests ; satellite viruses ; site-directed mutagenesis ; therapeutics ; viral hepatitis ; virus assembly
Language	English
Dates of publication	2022-12
Size	p. 163.
Publishing place	BioMed Central
Document type	Article ; Online
ZDB-ID	2160640-7
ISSN	1743-422X
ISSN	1743-422X
DOI	10.1186/s12985-022-01866-3
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Article ; Online: Repurposing existing drugs: identification of SARS-CoV-2 3C-like protease inhibitors.

Chiou, Wei-Chung / Hsu, Meng-Shiuan / Chen, Yun-Ti / Yang, Jinn-Moon / Tsay, Yeou-Guang / Huang, Hsiu-Chen / Huang, Cheng

Journal of enzyme inhibition and medicinal chemistry

2021 Volume 36, Issue 1, Page(s) 147–153

Abstract: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for coronavirus disease 2019 (COVID-19). Since its emergence, the COVID-19 pandemic has not only distressed medical services but also caused economic upheavals, marking urgent ... ...

Abstract	Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for coronavirus disease 2019 (COVID-19). Since its emergence, the COVID-19 pandemic has not only distressed medical services but also caused economic upheavals, marking urgent the need for effective therapeutics. The experience of combating SARS-CoV and MERS-CoV has shown that inhibiting the 3-chymotrypsin-like protease (3CLpro) blocks the replication of the virus. Given the well-studied properties of FDA-approved drugs, identification of SARS-CoV-2 3CLpro inhibitors in an FDA-approved drug library would be of great therapeutic value. Here, we screened a library consisting of 774 FDA-approved drugs for potent SARS-CoV-2 3CLpro inhibitors, using an intramolecularly quenched fluorescence (IQF) peptide substrate. Ethacrynic acid, naproxen, allopurinol, butenafine hydrochloride, raloxifene hydrochloride, tranylcypromine hydrochloride, and saquinavir mesylate have been found to block the proteolytic activity of SARS-CoV-2 3CLpro. The inhibitory activity of these repurposing drugs against SARS-CoV-2 3CLpro highlights their therapeutic potential for treating COVID-19 and other Betacoronavirus infections.
MeSH term(s)	Antiviral Agents/pharmacology ; COVID-19/virology ; Catalytic Domain ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus 3C Proteases/chemistry ; Cysteine Proteinase Inhibitors/pharmacology ; Drug Evaluation, Preclinical ; Drug Repositioning ; Fluorescent Dyes ; Humans ; Molecular Docking Simulation ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; Substrate Specificity ; COVID-19 Drug Treatment
Chemical Substances	Antiviral Agents ; Cysteine Proteinase Inhibitors ; Fluorescent Dyes ; 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Coronavirus 3C Proteases (EC 3.4.22.28)
Language	English
Publishing date	2021-01-07
Publishing country	England
Document type	Journal Article
ZDB-ID	2082578-X
ISSN	1475-6374 ; 1475-6366
ISSN (online)	1475-6374
ISSN	1475-6366
DOI	10.1080/14756366.2020.1850710
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Zs.A 3004: Show issues

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Article ; Online: Ergosterol peroxide inhibits HBV infection by inhibiting the binding of the pre-S1 domain of LHBsAg to NTCP.

Huang, Hsing / Huang, Hsiu-Chen / Chiou, Wei-Chung / Lin, Lie-Chwen / Chen, Jui-Chieh / Liu, Hui-Kang / Lai, Yu-Heng / Huang, Cheng

Antiviral research

2021 Volume 195, Page(s) 105184

Abstract: Hepatitis B virus (HBV) infection leads to severe liver diseases, including cirrhosis and hepatocellular carcinoma (HCC). More than 257 million individuals are chronically infected, particularly in the Western Pacific region and Africa. Although ... ...

Abstract	Hepatitis B virus (HBV) infection leads to severe liver diseases, including cirrhosis and hepatocellular carcinoma (HCC). More than 257 million individuals are chronically infected, particularly in the Western Pacific region and Africa. Although nucleotide and nucleoside analogues (NUCs) and interferons (IFNs) are the standard therapeutics for HBV infection, none eradicates HBV covalently closed circular DNA (cccDNA) from the infected hepatocytes. In addition, long-term treatment with NUCs increases the risk of developing drug resistance and IFNs may cause severe side effects in patients. Thus, a novel HBV therapy that can achieve a functional cure, or even complete elimination of the virus, is highly desirable. Regarding the HBV life cycle, agents targeting the entry step of HBV infection reduce the intrahepatic cccDNA pool preemptively. The initial entry step in HBV infection involves interaction between the pre-S1 domain of the large hepatitis B surface protein (LHBsAg) and the sodium taurocholate cotransporting polypeptide (NTCP), which is a receptor for HBV. In this study, ergosterol peroxide (EP) was identified as a new inhibitor of HBV entry. EP inhibits an early step of HBV entry into DMSO-differentiated immortalized primary human hepatocytes HuS-E/2 cells, which were overexpressed NTCP. Also, EP interfered directly with the NTCP-LHBsAg interaction by acting on the NTCP. In addition, EP had no effect on HBV genome replication, virion integrity or virion secretion. Finally, the activity of EP against infection with HBV genotypes A-D highlights the therapeutic potential of EP for fighting HBV infection.
MeSH term(s)	DNA, Circular/metabolism ; Ergosterol/analogs & derivatives ; Ergosterol/pharmacology ; Hep G2 Cells ; Hepatitis B/pathology ; Hepatitis B/virology ; Hepatitis B virus/drug effects ; Hepatitis B virus/genetics ; Hepatitis B virus/physiology ; Humans ; Organic Anion Transporters, Sodium-Dependent/genetics ; Organic Anion Transporters, Sodium-Dependent/metabolism ; Symporters/genetics ; Symporters/metabolism ; Virus Internalization/drug effects ; Virus Replication
Chemical Substances	DNA, Circular ; Organic Anion Transporters, Sodium-Dependent ; Symporters ; sodium-bile acid cotransporter (145420-23-1) ; ergosterol-5,8-peroxide (UG9TN81TGH) ; Ergosterol (Z30RAY509F)
Language	English
Publishing date	2021-10-07
Publishing country	Netherlands
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	306628-9
ISSN	1872-9096 ; 0166-3542
ISSN (online)	1872-9096
ISSN	0166-3542
DOI	10.1016/j.antiviral.2021.105184
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Article ; Online: The inhibitory effects of PGG and EGCG against the SARS-CoV-2 3C-like protease.

Chiou, Wei-Chung / Chen, Jui-Chieh / Chen, Yun-Ti / Yang, Jinn-Moon / Hwang, Lih-Hwa / Lyu, Yi-Shuan / Yang, Hsin-Yi / Huang, Cheng

Biochemical and biophysical research communications

2021 Volume 591, Page(s) 130–136

Abstract: The coronavirus disease (COVID-19) pandemic, resulting from human-to-human transmission of a novel severe acute respiratory syndrome coronavirus (SARS-CoV-2), has led to a global health crisis. Given that the 3 chymotrypsin-like protease (3CLpro) of SARS- ...

Abstract	The coronavirus disease (COVID-19) pandemic, resulting from human-to-human transmission of a novel severe acute respiratory syndrome coronavirus (SARS-CoV-2), has led to a global health crisis. Given that the 3 chymotrypsin-like protease (3CLpro) of SARS-CoV-2 plays an indispensable role in viral polyprotein processing, its successful inhibition halts viral replication and thus constrains virus spread. Therefore, developing an effective SARS-CoV-2 3CLpro inhibitor to treat COVID-19 is imperative. A fluorescence resonance energy transfer (FRET)-based method was used to assess the proteolytic activity of SARS-CoV-2 3CLpro using intramolecularly quenched fluorogenic peptide substrates corresponding to the cleavage sequence of SARS-CoV-2 3CLpro. Molecular modeling with GEMDOCK was used to simulate the molecular interactions between drugs and the binding pocket of SARS-CoV-2 3CLpro. This study revealed that the V
MeSH term(s)	Binding Sites ; COVID-19/epidemiology ; COVID-19/prevention & control ; COVID-19/virology ; Catechin/analogs & derivatives ; Catechin/chemistry ; Catechin/metabolism ; Catechin/pharmacology ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus 3C Proteases/chemistry ; Coronavirus 3C Proteases/metabolism ; Drug Evaluation, Preclinical/methods ; Humans ; Hydrolyzable Tannins/chemistry ; Hydrolyzable Tannins/metabolism ; Hydrolyzable Tannins/pharmacology ; Kinetics ; Models, Molecular ; Molecular Docking Simulation ; Molecular Structure ; Pandemics ; Protease Inhibitors/chemistry ; Protease Inhibitors/metabolism ; Protease Inhibitors/pharmacology ; Protein Binding ; Protein Domains ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; SARS-CoV-2/physiology ; Virus Replication/drug effects
Chemical Substances	Hydrolyzable Tannins ; Protease Inhibitors ; pentagalloylglucose (3UI3K8W93I) ; Catechin (8R1V1STN48) ; epigallocatechin gallate (BQM438CTEL) ; 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Coronavirus 3C Proteases (EC 3.4.22.28)
Language	English
Publishing date	2021-01-06
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	205723-2
ISSN	1090-2104 ; 0006-291X ; 0006-291X
ISSN (online)	1090-2104 ; 0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2020.12.106
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Article ; Online: Gut microbiota-directed intervention with high-amylose maize ameliorates metabolic dysfunction in diet-induced obese mice.

Chiou, Wei-Chung / Lai, Wei-Han / Cai, Yu-Lin / Du, Meng-Lun / Lai, Hsi-Mei / Chen, Jui-Chieh / Huang, Hsiu-Chen / Liu, Hui-Kang / Huang, Cheng

Food & function

2022 Volume 13, Issue 18, Page(s) 9481–9495

Abstract	Obesity is a chronic disease that may lead to the development of metabolic diseases, cardiovascular diseases, and cancers and has been predicted to affect one billion adults by 2030. Owing to the pivotal role of the gut microbiota in health, including metabolism and energy homeostasis, dietary fiber, the primary energy resource for the gut microbiota, not only helps reduce appetite and short-term food intake but also modulates the structure of the gut microbiota. In this study, we investigated whether high-amylose maize (HAM), with a particular amount of dietary fiber, improves dysmetabolism and gut microbiota dysbiosis in diet-induced obese mice. Promisingly, the HAM dietary intervention not only reduced body weight gain, adipocyte hypertrophy, and dyslipidemia but also mitigated non-alcoholic fatty liver disease, insulin resistance, impaired glucose tolerance, and inflammation in the liver and epididymal white adipose tissues in high-fat diet (HFD)-fed obese mice. In addition, the HAM dietary intervention ameliorated gut microbiota dysbiosis in HFD-fed mice. Changes in families, genera, and species of gut biota that have a relative abundance of 0.01% in at least one group were scrutinized. At the species level, HAM dietary intervention increased
MeSH term(s)	Amylose ; Animals ; Diet, High-Fat/adverse effects ; Dietary Fiber ; Dysbiosis/microbiology ; Gastrointestinal Microbiome ; Mice ; Mice, Inbred C57BL ; Mice, Obese ; Obesity/metabolism ; Zea mays
Chemical Substances	Dietary Fiber ; Amylose (9005-82-7)
Language	English
Publishing date	2022-09-22
Publishing country	England
Document type	Journal Article
ZDB-ID	2612033-1
ISSN	2042-650X ; 2042-6496
ISSN (online)	2042-650X
ISSN	2042-6496
DOI	10.1039/d2fo01211a
Database	MEDical Literature Analysis and Retrieval System OnLINE

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