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Article ; Online: Production of marine bacterial metalloprotease A69 and evaluation of its potential in preparing soybean peptides with angiotensin‐converting enzyme‐inhibitory activity

Zhang, Xia / Zhao, Wen‐Xiao / Wang, Yan / Cheng, Jun‐Hui / Bao, Kai / He, Jin / Chen, Xiu‐Lan

Journal of the Science of Food and Agriculture. 2023 Nov., v. 103, no. 14, p. 7153-7163

2023 , Page(s) 7153–7163

Abstract: BACKGROUND: Marine bacteria secrete a variety of proteases, which are a good source to explore proteases with application value. However, only a few marine bacterial proteases with a potential in bioactive peptides preparation have been reported. RESULTS: ...

Abstract	BACKGROUND: Marine bacteria secrete a variety of proteases, which are a good source to explore proteases with application value. However, only a few marine bacterial proteases with a potential in bioactive peptides preparation have been reported. RESULTS: The metalloprotease A69 from the marine bacterium Anoxybacillus caldiproteolyticus 1A02591 was successfully expressed in the food safe bacterium Bacillus subtilis as a secreted enzyme. A technique to efficiently produce protease A69 in a 15‐L bioreactor was established, with a production of 8988 U mL⁻¹. Based on optimizing the hydrolysis parameters of A69 on soybean protein, a process for soybean protein peptides (SPs) preparation was set up, in which soybean protein was hydrolyzed by A69 at 4000 U g⁻¹ and 60 °C for 3 h. The prepared SPs had a high content (> 90%) of peptides with a molecular mass less than 3000 Da and contained 18 amino acids. The prepared SPs showed high angiotensin‐converting enzyme (ACE)‐inhibitory activity, with an IC₅₀ value of 0.135 mg mL⁻¹. Moreover, three ACE‐inhibitory peptides, RPSYT, VLIVP and LAIPVNKP, were identified from the SPs using liquid chromatography‐mass spectrometry analysis. CONCLUSION: The marine bacterial metalloprotease A69 has a promising potential for preparing SPs with good nutritional and potential antihypertensive effects, laying a good foundation for its industrial production and application. © 2023 Society of Chemical Industry.
Keywords	Anoxybacillus ; Bacillus subtilis ; agriculture ; aquatic bacteria ; bioreactors ; enzyme inhibitors ; hydrolysis ; liquid chromatography ; mass spectrometry ; metalloproteinases ; molecular weight ; peptides ; peptidyl-dipeptidase A ; soy protein ; soybeans
Language	English
Dates of publication	2023-11
Size	p. 7153-7163
Publishing place	John Wiley & Sons, Ltd.
Document type	Article ; Online
Note	JOURNAL ARTICLE
ZDB-ID	184116-6
ISSN	1097-0010 ; 0022-5142
ISSN (online)	1097-0010
ISSN	0022-5142
DOI	10.1002/jsfa.12797
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Production of marine bacterial metalloprotease A69 and evaluation of its potential in preparing soybean peptides with angiotensin-converting enzyme-inhibitory activity.

Zhang, Xia / Zhao, Wen-Xiao / Wang, Yan / Cheng, Jun-Hui / Bao, Kai / He, Jin / Chen, Xiu-Lan

Journal of the science of food and agriculture

2023 Volume 103, Issue 14, Page(s) 7153–7163

Abstract: Background: Marine bacteria secrete a variety of proteases, which are a good source to explore proteases with application value. However, only a few marine bacterial proteases with a potential in bioactive peptides preparation have been reported.: ... ...

Abstract	Background: Marine bacteria secrete a variety of proteases, which are a good source to explore proteases with application value. However, only a few marine bacterial proteases with a potential in bioactive peptides preparation have been reported. Results: The metalloprotease A69 from the marine bacterium Anoxybacillus caldiproteolyticus 1A02591 was successfully expressed in the food safe bacterium Bacillus subtilis as a secreted enzyme. A technique to efficiently produce protease A69 in a 15-L bioreactor was established, with a production of 8988 U mL Conclusion: The marine bacterial metalloprotease A69 has a promising potential for preparing SPs with good nutritional and potential antihypertensive effects, laying a good foundation for its industrial production and application. © 2023 Society of Chemical Industry.
MeSH term(s)	Glycine max/chemistry ; Angiotensin-Converting Enzyme Inhibitors/chemistry ; Soybean Proteins ; Peptides/chemistry ; Peptide Hydrolases/chemistry ; Endopeptidases/chemistry ; Hydrolysis ; Metalloproteases ; Bacillus subtilis/metabolism ; Angiotensins ; Peptidyl-Dipeptidase A/chemistry
Chemical Substances	Angiotensin-Converting Enzyme Inhibitors ; Soybean Proteins ; Peptides ; Peptide Hydrolases (EC 3.4.-) ; Endopeptidases (EC 3.4.-) ; Metalloproteases (EC 3.4.-) ; Angiotensins ; Peptidyl-Dipeptidase A (EC 3.4.15.1)
Language	English
Publishing date	2023-07-18
Publishing country	England
Document type	Journal Article
ZDB-ID	184116-6
ISSN	1097-0010 ; 0022-5142
ISSN (online)	1097-0010
ISSN	0022-5142
DOI	10.1002/jsfa.12797
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Article ; Online: Xiaoer niuhuang qingxin powder alleviates influenza a virus infection by inhibiting the activation of the TLR4/MyD88/NF-κB signaling pathway.

Ma, Lanying / Wang, Tong / Liu, Meiyi / Ji, Lingyun / Wang, Yanan / Li, Shuting / Zhang, YaNan / Wang, Yuan / Zhao, WenXiao / Wu, ZhiChun / Yu, HuaYun / Zhao, HaiJun

Journal of ethnopharmacology

2024 Volume 328, Page(s) 118000

Abstract: Ethnopharmacological relevance: Xiaoer Niuhuang Qingxin Powder (XNQP) is a classic traditional Chinese medicine formula with significant clinical efficacy for treating febrile convulsions and influenza.: Aim of the study: This study aims to explore ... ...

Abstract	Ethnopharmacological relevance: Xiaoer Niuhuang Qingxin Powder (XNQP) is a classic traditional Chinese medicine formula with significant clinical efficacy for treating febrile convulsions and influenza. Aim of the study: This study aims to explore the potential mechanisms of XNQP in combating combating the influenza A virus, providing a theoretical basis for its clinical application. Materials and methods: The present investigation employed network pharmacology and bioinformatics analysis to determine the TLR4/MyD88/NF-κB signaling pathway as a viable target for XNQP intervention in IAV infection.Subsequently, a mouse model of influenza A virus infection was established, and different doses of XNQP were used for intervention. The protein expression levels of TLR4/MyD88/NF-κB were detected using HE staining, Elisa, immunohistochemistry, immunofluorescence, and western blot. Results: The results showed that treatment with XNQP after IAV infection reduced the mortality and prolonged the survival time of infected mice. It reduced the release of TNF-α and IFN-γ in the serum and alleviated pathological damage in the lung tissue following infection. Additionally, the levels of TLR4, MyD88, NF-κB, and p-NF-κB P65 proteins were significantly reduced in lung tissue by XNQP. The inhibitory effect of XNQP on the expression of MyD88 and NF-κB was antagonized when TLR4 signaling was overexpressed. Consequently, the expression levels of MyD88, NF-κB, and p-NF-κB P65 were increased in lung tissue. Conversely, the expression levels of the proteins MyD88, NF-κB, and p-NF-κB P65 were downregulated when TLR4 signaling was inhibited. Conclusions: XNQP alleviated lung pathological changes, reduced serum levels of inflammatory factors, reduced mortality, and prolonged survival time in mice by inhibiting the overexpression of the TLR4/MyD88/NF-κB signaling pathway in lung tissues after IAV infection.
MeSH term(s)	Mice ; Animals ; Humans ; NF-kappa B/metabolism ; Toll-Like Receptor 4/metabolism ; Myeloid Differentiation Factor 88/metabolism ; Powders ; Influenza, Human ; Signal Transduction ; Influenza A virus ; Drugs, Chinese Herbal
Chemical Substances	NF-kappa B ; niuhuang qingxin ; Toll-Like Receptor 4 ; Myeloid Differentiation Factor 88 ; Powders ; Drugs, Chinese Herbal
Language	English
Publishing date	2024-03-26
Publishing country	Ireland
Document type	Journal Article
ZDB-ID	134511-4
ISSN	1872-7573 ; 0378-8741
ISSN (online)	1872-7573
ISSN	0378-8741
DOI	10.1016/j.jep.2024.118000
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Article ; Online: Research progress on the mechanism of traditional Chinese medicine regulating intestinal microbiota to combat influenza a virus infection.

Ma, LanYing / Ji, Lingyun / Wang, Tong / Zhai, Zhe / Su, PeiWei / Zhang, YaNan / Wang, Yuan / Zhao, WenXiao / Wu, ZhiChun / Yu, HuaYun / Zhao, HaiJun

Virology journal

2023 Volume 20, Issue 1, Page(s) 260

Abstract: Influenza A viruses (IAV) are a prevalent respiratory pathogen that can cause seasonal flu and global pandemics, posing a significant global public health threat. Emerging research suggests that IAV infections may disrupt the balance of gut microbiota, ... ...

Abstract	Influenza A viruses (IAV) are a prevalent respiratory pathogen that can cause seasonal flu and global pandemics, posing a significant global public health threat. Emerging research suggests that IAV infections may disrupt the balance of gut microbiota, while gut dysbiosis can affect disease progression in IAV patients. Therefore, restoring gut microbiota balance may represent a promising therapeutic target for IAV infections. Traditional Chinese medicine, with its ability to regulate gut microbiota, offers significant potential in preventing and treating IAV. This article provides a comprehensive review of the relationship between IAV and gut microbiota, highlighting the impact of gut microbiota on IAV infections. It also explores the mechanisms and role of traditional Chinese medicine in regulating gut microbiota for the prevention and treatment of IAV, presenting novel research avenues for traditional Chinese medicine-based IAV treatments.
MeSH term(s)	Humans ; Gastrointestinal Microbiome ; Medicine, Chinese Traditional ; Influenza, Human ; Influenza A virus
Language	English
Publishing date	2023-11-13
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	2160640-7
ISSN	1743-422X ; 1743-422X
ISSN (online)	1743-422X
ISSN	1743-422X
DOI	10.1186/s12985-023-02228-3
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Molecular Mechanism of Polysaccharides Extracted from Chinese Medicine Targeting Gut Microbiota for Promoting Health.

Zhao, Wen-Xiao / Wang, Tong / Zhang, Ya-Nan / Chen, Qian / Wang, Yuan / Xing, Yan-Qing / Zheng, Jun / Duan, Chen-Chen / Chen, Li-Jun / Zhao, Hai-Jun / Wang, Shi-Jun

Chinese journal of integrative medicine

2022 Volume 30, Issue 2, Page(s) 171–180

Abstract: The accumulating evidence revealed that gut microbiota plays an important role in pathological process of disease including obesity, type 2 diabetes mellitus, heart failure, and non-alcoholic fatty liver disease. Polysaccharides extracted from Chinese ... ...

Abstract	The accumulating evidence revealed that gut microbiota plays an important role in pathological process of disease including obesity, type 2 diabetes mellitus, heart failure, and non-alcoholic fatty liver disease. Polysaccharides extracted from Chinese medicine (CM) can not only alleviate pathological status but also promote health by anti-inflammatory, regulating immunity, lowering blood glucose and lipids, anti-cancer, and anti-oxidation. The alterations of gut microbiota composition and metabolism pathways are the potential mechanisms of CM polysaccharides treatment. In addition, they exert functions through gut-organ axis or play an indirect role by synergistic actions with other drugs or components mediated by gut microbiota. This review summarizes the molecular mechanisms of CM polysaccharides interacted with intestinal microbial inhabitants as potential prebiotics for promoting health.
MeSH term(s)	Humans ; Gastrointestinal Microbiome ; Diabetes Mellitus, Type 2/therapy ; Medicine, Chinese Traditional ; Health Promotion ; Prebiotics ; Polysaccharides/pharmacology ; Polysaccharides/therapeutic use
Chemical Substances	Prebiotics ; Polysaccharides
Language	English
Publishing date	2022-05-18
Publishing country	China
Document type	Journal Article ; Review
ZDB-ID	2171254-2
ISSN	1993-0402 ; 1672-0415
ISSN (online)	1993-0402
ISSN	1672-0415
DOI	10.1007/s11655-022-3522-y
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 5823: Show issues

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Article: Effects of Radix Astragali and Its Split Components on Gene Expression Profiles Related to Water Metabolism in Rats with the Dampness Stagnancy due to Spleen Deficiency Syndrome.

Zhao, Wen-Xiao / Cui, Ning / Jiang, Hai-Qiang / Ji, Xu-Ming / Han, Xiao-Chun / Han, Bing-Bing / Wang, Tong / Wang, Shi-Jun

Evidence-based complementary and alternative medicine : eCAM

2017 Volume 2017, Page(s) 4946031

Abstract: Radix Astragali (RA) with slight sweet and warm property is a significant "qi tonifying" herb; it is indicated for the syndrome of dampness stagnancy due to spleen deficiency (DSSD). The purpose of this research was to explore effects of RA and its split ...

Abstract	Radix Astragali (RA) with slight sweet and warm property is a significant "qi tonifying" herb; it is indicated for the syndrome of dampness stagnancy due to spleen deficiency (DSSD). The purpose of this research was to explore effects of RA and its split components on gene expression profiles related to water metabolism in rats with the DSSD syndrome for identifying components representing property and flavor of RA. The results indicated that RA and its split components, especially polysaccharides component, significantly increased the body weight and the urine volume and decreased the water load index of model rats. Our data also indicated differentially expressed genes (DEGs) related to water metabolism involved secretion, ion transport, water homeostasis, regulation of body fluid levels, and water channel activity; the expression of AQP1, AQP3, AQP4, AQP5, AQP6, and AQP8 was improved; calcium, cAMP, MAPK, PPAR, AMPK, and PI3K-Akt signaling pathway may be related to water metabolism. In general, results indicate that RA and its split components could promote water metabolism in rats with the DSSD syndrome via regulating the expression of AQPs, which reflected sweet-warm properties of RA. Effects of the polysaccharides component are better than others.
Language	English
Publishing date	2017-05-21
Publishing country	United States
Document type	Journal Article
ZDB-ID	2171158-6
ISSN	1741-4288 ; 1741-427X
ISSN (online)	1741-4288
ISSN	1741-427X
DOI	10.1155/2017/4946031
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: [Effect of sophocarpine on HERG K+ channels].

Qi, Zhi-Ping / Shi, Shan-Shan / Zhao, Xue-Ling / Zhao, Wen-Xiao / Bai, Yun-Long / Lü, Yan-Jie / Li, Bao-Xin / Yang, Bao-Feng

Yao xue xue bao = Acta pharmaceutica Sinica

2008 Volume 43, Issue 1, Page(s) 44–49

Abstract: Human ether-a-go-go-related gene (HERG) encodes the rapid component of the cardiac delayed rectifier K+ current, which has an important effect on both proarrhythmia and antiarrhythmia. To investigate the effect of sophocarpine (SC) on HERG channel stably ...

Abstract	Human ether-a-go-go-related gene (HERG) encodes the rapid component of the cardiac delayed rectifier K+ current, which has an important effect on both proarrhythmia and antiarrhythmia. To investigate the effect of sophocarpine (SC) on HERG channel stably expressing in human embryonic kidney-293 (HEK293) cells, whole-cell patch-clamp technique was used to record HERG current and kinetic curves. As the result, it was found that SC inhibited HERG current in a concentration-dependent manner (10, 30, 100, and 300 micromol x L(-1)). At 0 mV, 10, 30, 100, and 300 micromol x L(-1) SC respectively inhibited IHERG by Istep ( 10.7 +/- 2.8)% , (11.3 +/- 5.5)% , (47.0 +/- 2.3)% and (53.7 +/- 2.5)% , and Itail (1.1 +/- 3.0)%, (17.1 +/- 3.3)%, (32.7 +/- 1.9)% (P < 0.05, n = 12) and (56.0 +/- 2.4)% (P < 0.05, n = 13). The time constants of inactivation, recovery from inactivation and onset of inactivation were accelerated. SC did not change other channel kinetics (activation and deactivation). It is concluded that SC inhibited the transfected HERG channels by influencing the inactivation state, which is the probable anti-arrhythmic mechanism.
MeSH term(s)	Alkaloids/pharmacology ; Anti-Arrhythmia Agents/pharmacology ; Cell Line ; Dose-Response Relationship, Drug ; Ether-A-Go-Go Potassium Channels/antagonists & inhibitors ; Ether-A-Go-Go Potassium Channels/metabolism ; Ether-A-Go-Go Potassium Channels/physiology ; Humans ; Kidney/cytology ; Kinetics ; Membrane Potentials/drug effects ; Patch-Clamp Techniques ; Plants, Medicinal/chemistry ; Sophora/chemistry
Chemical Substances	Alkaloids ; Anti-Arrhythmia Agents ; Ether-A-Go-Go Potassium Channels ; sophocarpine (6483-15-4)
Language	Chinese
Publishing date	2008-01
Publishing country	China
Document type	English Abstract ; Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	788758-9
ISSN	0513-4870
ISSN	0513-4870
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: [Effect of Daming capsule on expression of connexin43 isoforms in hyperlipemic rat's cardiac muscle].

Xing, Yan / Yue, Peng / Sun, Li-hua / Zhao, Wen-xiao / Wang, Ying / Zhang, Yong / Liu, Xin / Lu, Yan-jie / Yang, Bao-feng

Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica

2007 Volume 32, Issue 14, Page(s) 1440–1445

Abstract: Objective: To find the molecular mechanism of decreasing blood fat effect of Darning capsule on hyperlipemic rat, we study the expression of connexin43 in the myocardium before and after using the capsule.: Method: Forty Wistar rats were randomly ... ...

Abstract	Objective: To find the molecular mechanism of decreasing blood fat effect of Darning capsule on hyperlipemic rat, we study the expression of connexin43 in the myocardium before and after using the capsule. Method: Forty Wistar rats were randomly divided into 5 group: control group, hyperlipemia model group, Daming capsule group of high dose, middle dose and low dose (200, 100, 50 mg kg(-1) d(-1)). Each group had 8 rats. Hyperlipemic rat model was made firstly, the blood was obtained via vena caudalis and the indexes of TC, TG, LDL, HDL and NEFA in the serum were measured. The myocardial total RNA was extracted by Trizol method. To compare the expression of connexin43 in the following groups: hyperlipemia, normal and drug, we used the technique of RT-PCR, immunostaining and microconfoul. Result: The concentrations of TC, TG, LDL and NEFA in hyperlipemic serum were increased (P <0. 05), while that of HDL was decreased (P <0. 05). After treating with Daming capsule, the concentration of the preceding four indexes were decreased and the concentrations of HDL was increased up to nearly normal level. No significant difference was found in the ECG of the three groups. As compared with the normal group, the mRNA expressions of connexin43 in hyperlipemia group was weakened (P <0.05), while that of the drug group was enhanced(P <0.05). The same result in immunostaining was observed. Conclusion: Hyperlipemic rat model was successfully established and Daming capsule has the effect of lowering blood lipid. Furthermore, the molecular mechanism of Darning capsule is related with the change of Cx43 closely.
MeSH term(s)	Animals ; Capsules ; Cholesterol/blood ; Connexin 43/biosynthesis ; Connexin 43/genetics ; Drugs, Chinese Herbal/isolation & purification ; Drugs, Chinese Herbal/pharmacology ; Fatty Acids, Nonesterified/blood ; Hyperlipidemias/blood ; Hyperlipidemias/metabolism ; Hypolipidemic Agents/administration & dosage ; Hypolipidemic Agents/pharmacology ; Male ; Myocardium/metabolism ; Plants, Medicinal/chemistry ; Protein Isoforms/biosynthesis ; Protein Isoforms/genetics ; RNA, Messenger/biosynthesis ; Random Allocation ; Rats ; Rats, Wistar ; Triglycerides/blood
Chemical Substances	Capsules ; Connexin 43 ; Drugs, Chinese Herbal ; Fatty Acids, Nonesterified ; Hypolipidemic Agents ; Protein Isoforms ; RNA, Messenger ; Triglycerides ; Cholesterol (97C5T2UQ7J)
Language	Chinese
Publishing date	2007-07
Publishing country	China
Document type	English Abstract ; Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1004649-5
ISSN	1001-5302 ; 0254-0029
ISSN	1001-5302 ; 0254-0029
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 3056: Show issues

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Article ; Online: The novel mechanism of oxymatrine affecting HERG currents at different temperatures.

Hu, Mei-Qin / Dong, Zeng-Xiang / Zhao, Wen-Xiao / Sun, Jing / Zhao, Xin / Gu, Dong-Fang / Zhang, Yan / Li, Bao-Xin / Yang, Bao-Feng

Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology

2010 Volume 26, Issue 4-5, Page(s) 513–522

Abstract: Background/aims: Human ether-à-go-go-related gene (hERG) has an important role in the repolarization of the cardiac action potential. Our studies were to investigate the effects of oxymatrine (one of the natural constituents extracted from Chinese herb ... ...

Abstract	Background/aims: Human ether-à-go-go-related gene (hERG) has an important role in the repolarization of the cardiac action potential. Our studies were to investigate the effects of oxymatrine (one of the natural constituents extracted from Chinese herb Sophora flavescens Ait) on hERG-encoded K(+) channels at different temperatures and its underlying mechanism. Methods: The effects of oxymatrine were examined on hERG channels stably expressed in HEK293 cells using a whole-cell patch clamp technique. Results: At the temperature 30°C, oxymatrine inhibited hERG current in a concentration-dependent manner and the IC(50) was ∼665 μM. However at the temperature of 20°C, low concentration oxymatrine C≤100 μM increased hERG current density. However, high concentration oxymatrine C>100 μM inhibited the hERG current density significantly. Oxymatrine only affected the activation kinetic of hERG channels at all temperatures and had a high binding affinity for open state of hERG channels except the 300 μM-20°C group which had a high binding affinity for inactive state of hERG channels. Conclusion: Oxymatrine is a low potency blocker of hERG K+ channels at 30°C, low concentration oxymatrine affect the hERG activation gating with accelerating hERG tail current at 20°C, oxymatrine is a potential hERG activator at low temperatures.
MeSH term(s)	Alkaloids/pharmacology ; Electrophysiological Phenomena ; Ether-A-Go-Go Potassium Channels/antagonists & inhibitors ; Ether-A-Go-Go Potassium Channels/metabolism ; Ether-A-Go-Go Potassium Channels/physiology ; HEK293 Cells ; Humans ; Kinetics ; Patch-Clamp Techniques ; Protein Binding ; Quinolizines/pharmacology ; Temperature
Chemical Substances	Alkaloids ; Ether-A-Go-Go Potassium Channels ; Quinolizines ; oxymatrine (85U4C366QS)
Language	English
Publishing date	2010-10-29
Publishing country	Germany
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1067572-3
ISSN	1421-9778 ; 1015-8987
ISSN (online)	1421-9778
ISSN	1015-8987
DOI	10.1159/000322319
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: The Novel Mechanism of Oxymatrine Affecting hERG Currents at Different Temperatures

Hu, Mei-Qin / Dong, Zeng-Xiang / Zhao, Wen-Xiao / Sun, Jing / Zhao, Xin / Gu, Dong-Fang / Zhang, Yan / Li, Bao-Xin / Yang, Bao-Feng

Cellular Physiology and Biochemistry

2010 Volume 26, Issue 4-5, Page(s) 513–522

Abstract: Background/Aims: Human ether-à-go-go-related gene (hERG) has an important role in the repolarization of the cardiac action potential. Our studies were to investigate the effects of oxymatrine (one of the natural constituents extracted from Chinese herb ... ...

Institution	Department of Pharmacology, Harbin Medical University, Harbin State-Province Key Laboratory of Biopharmaceutical Engineering, Harbin Mei-Qin Hu and Zeng-Xiang Dong made equal contributions to this study
Abstract	Background/Aims: Human ether-à-go-go-related gene (hERG) has an important role in the repolarization of the cardiac action potential. Our studies were to investigate the effects of oxymatrine (one of the natural constituents extracted from Chinese herb Sophora flavescens Ait) on hERG-encoded K channels at different temperatures and its underlying mechanism. Methods: The effects of oxymatrine were examined on hERG channels stably expressed in HEK293 cells using a whole-cell patch clamp technique. Results: At the temperature 30°C, oxymatrine inhibited hERG current in a concentration-dependent manner and the IC50 was ∼665 µM. However at the temperature of 20°C, low concentration oxymatrine C≤100 µM increased hERG current density. However, high concentration oxymatrine C>100 µM inhibited the hERG current density significantly. Oxymatrine only affected the activation kinetic of hERG channels at all temperatures and had a high binding affinity for open state of hERG channels except the 300 µM-20°C group which had a high binding affinity for inactive state of hERG channels. Conclusion: Oxymatrine is a low potency blocker of hERG K+ channels at 30°C, low concentration oxymatrine affect the hERG activation gating with accelerating hERG tail current at 20°C, oxymatrine is a potential hERG activator at low temperatures.
Keywords	HEK293 cell ; hERG channel ; Patch clamp ; Oxymatrine ; Temperature
Language	English
Publishing date	2010-10-29
Publisher	S. Karger AG
Publishing place	Basel, Switzerland
Document type	Article
Note	Original Paper
ZDB-ID	1067572-3
ISSN	1421-9778 ; 1015-8987
ISSN (online)	1421-9778
ISSN	1015-8987
DOI	10.1159/000322319
Database	Karger publisher's database

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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