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Hai-lin Qin - One of the best experts on this subject based on the ideXlab platform.
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Coptisine Alleviates Pristane-Induced Lupus-Like Disease and Associated Kidney and Cardiovascular Complications in Mice.
Frontiers in Pharmacology, 2020Co-Authors: Yu Yan, Zhi-hui Zhang, Hai-lin Qin, Yucai Chen, Biyu Hou, Kang Liu, Lianhua FangAbstract:Systemic lupus erythaematosus (SLE) is a chronic multi-system autoimmune disease with a high prevalence of kidney and cardiovascular complications. Considering that Rho-associated coiled-coil-containing protein kinases (ROCKs) play important roles in SLE, inflammation, and cardiovascular disease, we hypothesized that Coptisine, which has been found to inhibit ROCKs, may have an effect on SLE. The effect of Coptisine was assessed in female BALB/c mice intraperitoneally injected with 0.5 mL of pristane. Serum autoantibodies were tested every month, blood pressure was measured every 2 months, and serum inflammatory markers, spleen pathologic characteristics, renal injury and vascular function were observed at 6 months. The results showed that Coptisine decreased the levels of serum autoantibodies and serum inflammatory markers in the SLE mice, improved the pathologic characteristics of the spleen, and simultaneously improved renal injury, decreased inflammatory responses in the kidneys, reduced blood pressure, and improved vascular endothelial function. Western blot assays revealed that inhibiting the activation of the NF-κB and Rho/ROCK signalling pathways and downstream signalling molecules might be the potential mechanisms of the effects of Coptisine. Our findings suggest that therapy with Coptisine may be a strategy for preventing SLE and ameliorating associated kidney and cardiovascular complications.
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pharmacokinetics and tissue distribution of Coptisine in rats after oral administration by liquid chromatography mass spectrometry
Biomedical Chromatography, 2017Co-Authors: Yu Yan, Zhi-hui Zhang, Hai-lin Qin, Huifang Zhang, Junke Song, Yucai Chen, Xiaobo Wang, Lianhua FangAbstract:Coptisine, one of the main components isolated from Coptidis rhizoma, has been reported to have many beneficial pharmacological effects including anti-inflammatory, anti-hypercholesterolemia, neuroprotective and cardioprotective properties. However, to date the information related to the in vivo pharmacokinetics (PK) of Coptisine is very limited. The purposes of our study are to establish a fast and sensitive quantification method of Coptisine using liquid chromatography–mass spectrometry (LC–MS) and evaluate the PK profile of Coptisine in rats. The calibration curve for Coptisine was linear from 0.78 to 50 ng/mL. After single-dose oral administration of Coptisine, the mean peak plasma concentration values for groups treated with 30, 75 and 150 mg/kg doses ranged from 44.15 to 66.89 ng/mL, and the mean area under the concentration–time curve values ranged from 63.24 to 87.97 mg/L h. The absolute bioavailability was calculated to range from 1.87 to 0.52%. Coptisine remained in all analyzed samples at low concentrations after oral administration of 30 mg/kg.
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Pharmacokinetics and tissue distribution of Coptisine in rats after oral administration by liquid chromatography–mass spectrometry
Biomedical Chromatography, 2017Co-Authors: Yu Yan, Zhi-hui Zhang, Hai-lin Qin, Huifang Zhang, Junke Song, Yucai Chen, Xiaobo Wang, Lianhua FangAbstract:Coptisine, one of the main components isolated from Coptidis rhizoma, has been reported to have many beneficial pharmacological effects including anti-inflammatory, anti-hypercholesterolemia, neuroprotective and cardioprotective properties. However, to date the information related to the in vivo pharmacokinetics (PK) of Coptisine is very limited. The purposes of our study are to establish a fast and sensitive quantification method of Coptisine using liquid chromatography–mass spectrometry (LC–MS) and evaluate the PK profile of Coptisine in rats. The calibration curve for Coptisine was linear from 0.78 to 50 ng/mL. After single-dose oral administration of Coptisine, the mean peak plasma concentration values for groups treated with 30, 75 and 150 mg/kg doses ranged from 44.15 to 66.89 ng/mL, and the mean area under the concentration–time curve values ranged from 63.24 to 87.97 mg/L h. The absolute bioavailability was calculated to range from 1.87 to 0.52%. Coptisine remained in all analyzed samples at low concentrations after oral administration of 30 mg/kg.
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Synthesis and Structure-Activity Relationships of N-DihydroCoptisine-8-ylidene Aromatic Amines and N-DihydroCoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
Journal of Natural Products, 2016Co-Authors: Meng Xie, Zhi-hui Zhang, Hai-jing Zhang, An-jun Deng, Wen-jie Wang, Hai-lin QinAbstract:In this study, natural quaternary Coptisine was used as a lead compound to design and synthesize structurally stable and actively potent Coptisine analogues. Of the synthesized library, 13 N-dihydroCoptisine-8-ylidene amines/amides were found not only to be noncytotoxic toward intestinal epithelial cells (IECs), but they were also able to activate the transcription of X-box-binding protein 1 (XBP1) targets to varying extents in vitro. Antiulcerative colitis (UC) activity levels were assessed at the in vitro molecular level as well as in vivo in animals using multiple biomarkers as indices. In an in vitro XBP1 transcriptional activity assay, four compounds demonstrated good dose–effect relationships with EC50 values of 0.0708–0.0132 μM. Moreover, two compounds were confirmed to be more potent in vivo than a positive control, demonstrating a curative effect for UC in experimental animals. Thus, the findings of this study suggest that these Coptisine analogues are promising candidates for the development of ...
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Synthesis and Structure–Activity Relationships of N‑DihydroCoptisine-8-ylidene Aromatic Amines and N‑DihydroCoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1
2016Co-Authors: Meng Xie, Zhi-hui Zhang, Hai-jing Zhang, An-jun Deng, Wen-jie Wang, Hai-lin QinAbstract:In this study, natural quaternary Coptisine was used as a lead compound to design and synthesize structurally stable and actively potent Coptisine analogues. Of the synthesized library, 13 N-dihydroCoptisine-8-ylidene amines/amides were found not only to be noncytotoxic toward intestinal epithelial cells (IECs), but they were also able to activate the transcription of X-box-binding protein 1 (XBP1) targets to varying extents in vitro. Antiulcerative colitis (UC) activity levels were assessed at the in vitro molecular level as well as in vivo in animals using multiple biomarkers as indices. In an in vitro XBP1 transcriptional activity assay, four compounds demonstrated good dose–effect relationships with EC50 values of 0.0708–0.0132 μM. Moreover, two compounds were confirmed to be more potent in vivo than a positive control, demonstrating a curative effect for UC in experimental animals. Thus, the findings of this study suggest that these Coptisine analogues are promising candidates for the development of anti-UC drugs
Zongyao Zou - One of the best experts on this subject based on the ideXlab platform.
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the protective effect of Coptisine on experimental atherosclerosis apoe mice is mediated by mapk nf κb dependent pathway
Biomedicine & Pharmacotherapy, 2017Co-Authors: Min Feng, Shu-zhen Kong, Zhen-xu Wang, Zongyao ZouAbstract:Abstract Coptisine is one of main bioactive compounds extracted from the traditional Chinese herbal medicine Rhizoma Coptidis . It is reported that Coptisine can attenuate obesity-related inflammation and oxidant damage in Syrian golden hamsters. Therefore，Coptisine may exhibit beneficial effects for the treatment of atherosclerosis (AS) due to its hypolipidemic and anti-inflammation activities. The present study investigated the anti-atherosclerotic and anti-inflammatory properties of Coptisine using apoE −/− mice as AS model. The atherosclerotic plaque area of aorta, serum lipid profile and the expression of inflammatory cytokines were determined. After Coptisine treatment, the serum level of TC, TG and LDL-C decreased; the serum level of IL-6, IL-1β and TNF-α were decreased; the mRNA levels of NF-κBp65, VCAM-1, ICAM-1, IL-6 and IL-1β in both aorta and liver were down-regulated; the p -p38 and p -JNK1/2 protein expression level were decreased. Coptisine decreased atherosclerotic plaque area significantly through both anti-inflammation and lipid lowering effect. The anti-inflammatory effect of Coptisine is achieved through inhibiting activation of MAPK signaling pathways and NF-κB nuclear translocation. Therefore，the combined anti-inflammation and lipid lowering effect of Coptisine attributed the decreased atherosclerotic plaque area in Coptisine treated apoE −/− mice. The results of this study will afford a novel application for Coptisine in the treatment of atherosclerosis and other chronic inflammatory disease.
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The protective effect of Coptisine on experimental atherosclerosis ApoE-/- mice is mediated by MAPK/NF-κB-dependent pathway.
Biomedicine & Pharmacotherapy, 2017Co-Authors: Min Feng, Shu-zhen Kong, Zhen-xu Wang, Zongyao ZouAbstract:Abstract Coptisine is one of main bioactive compounds extracted from the traditional Chinese herbal medicine Rhizoma Coptidis . It is reported that Coptisine can attenuate obesity-related inflammation and oxidant damage in Syrian golden hamsters. Therefore，Coptisine may exhibit beneficial effects for the treatment of atherosclerosis (AS) due to its hypolipidemic and anti-inflammation activities. The present study investigated the anti-atherosclerotic and anti-inflammatory properties of Coptisine using apoE −/− mice as AS model. The atherosclerotic plaque area of aorta, serum lipid profile and the expression of inflammatory cytokines were determined. After Coptisine treatment, the serum level of TC, TG and LDL-C decreased; the serum level of IL-6, IL-1β and TNF-α were decreased; the mRNA levels of NF-κBp65, VCAM-1, ICAM-1, IL-6 and IL-1β in both aorta and liver were down-regulated; the p -p38 and p -JNK1/2 protein expression level were decreased. Coptisine decreased atherosclerotic plaque area significantly through both anti-inflammation and lipid lowering effect. The anti-inflammatory effect of Coptisine is achieved through inhibiting activation of MAPK signaling pathways and NF-κB nuclear translocation. Therefore，the combined anti-inflammation and lipid lowering effect of Coptisine attributed the decreased atherosclerotic plaque area in Coptisine treated apoE −/− mice. The results of this study will afford a novel application for Coptisine in the treatment of atherosclerosis and other chronic inflammatory disease.
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Coptisine attenuates obesity related inflammation through lps tlr 4 mediated signaling pathway in syrian golden hamsters
Fitoterapia, 2015Co-Authors: Zongyao Zou, Yan-zhi Wang, Shuang Xia, Dong-fang XueAbstract:It is known that obesity resulted from consumption of diets high in fat and calories and associated with a chronic low-grade inflammation. Because the fat, sterol and bile acid metabolism of male Syrian golden hamster are more similar to that of human, in the present study, high fat and high cholesterol (HFHC) induced obese hamsters were used to evaluate the anti-inflammation and hypolipidemic role of Coptisine. The results showed that body weight, plasma lipid levels of total cholesterol (TC), triglyceride (TG), low density lipoprotein-cholesterol (LDL-c), very low density lipoprotein-cholesterol (VLDL-c), ApoB and pro-inflammatory cytokines including TNF-α, IL-6 and lipopolysaccharide (LPS) were significantly altered in hamsters fed with HFHC diet. A strong correlation was observed between the LPS level in serum and the level of LBP and pro-inflammatory cytokines. Coptisine from the concentrations of 60 to 700 mg/L dose-dependently inhibited Enterobacter cloacae growth, which can easily induce obesity and insulin resistance. The results of endotoxin neutralization assay suggest that Coptisine is capable of reducing the LPS content under inflammation status. Real time RT-PCR analyses revealed that Coptisine suppressed TLR-4 in visceral fat of hamsters and decreased CD14 expression in livers of hamsters. These encouraging findings make the development of Coptisine a good candidate for preventing obesity-related diseases through the LPS/TLR-4-mediated signaling pathway.
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Coptisine attenuates obesity-related inflammation through LPS/TLR-4-mediated signaling pathway in Syrian golden hamsters
Fitoterapia, 2015Co-Authors: Zongyao Zou, Yan-zhi Wang, Shuang Xia, Dong-fang XueAbstract:It is known that obesity resulted from consumption of diets high in fat and calories and associated with a chronic low-grade inflammation. Because the fat, sterol and bile acid metabolism of male Syrian golden hamster are more similar to that of human, in the present study, high fat and high cholesterol (HFHC) induced obese hamsters were used to evaluate the anti-inflammation and hypolipidemic role of Coptisine. The results showed that body weight, plasma lipid levels of total cholesterol (TC), triglyceride (TG), low density lipoprotein-cholesterol (LDL-c), very low density lipoprotein-cholesterol (VLDL-c), ApoB and pro-inflammatory cytokines including TNF-α, IL-6 and lipopolysaccharide (LPS) were significantly altered in hamsters fed with HFHC diet. A strong correlation was observed between the LPS level in serum and the level of LBP and pro-inflammatory cytokines. Coptisine from the concentrations of 60 to 700 mg/L dose-dependently inhibited Enterobacter cloacae growth, which can easily induce obesity and insulin resistance. The results of endotoxin neutralization assay suggest that Coptisine is capable of reducing the LPS content under inflammation status. Real time RT-PCR analyses revealed that Coptisine suppressed TLR-4 in visceral fat of hamsters and decreased CD14 expression in livers of hamsters. These encouraging findings make the development of Coptisine a good candidate for preventing obesity-related diseases through the LPS/TLR-4-mediated signaling pathway.
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The Safety and Anti-Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters
Lipids, 2014Co-Authors: Yan-zhi Wang, Zongyao Zou, Na Ning, Biao Chen, Xuedong FangAbstract:Current work was conducted to evaluate the cholesterol-lowering effect of Coptisine extracted from Rhizomacoptidis in Syrian golden hamsters. The safety results indicated that Coptisine was a safe and low-toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induced by a high-fat and high-cholesterol diet (HFHC): at a concentration of 70.05 mg/kg, Coptisine significantly led to a decrease in total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-c) levels by 26.70, 15.38, and 22.22 %, respectively, and high-density lipoprotein cholesterol (HDL-c) was increased by 41.74 % in serum of hamsters (p < 0.01). In addition, total bile acid (TBA) levels in feces of hamsters were elevated after Coptisine administration. Further investigation has suggested that the mRNA and protein expression of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMGCR) in the liver of hamsters was down-regulated by high-dosage Coptisine treatment (p < 0.05); mRNA and protein expression of low-density lipoprotein receptor (LDLR) and cholesterol 7α-hydroxylase (CYP7A1) were dramatically up-regulated by Coptisine administration. The apical sodium-dependent bile salt transporter expression was down-regulated in the Coptisine-treated animals, but showed no significant differences from the HFHC groups. Taken together, our results demonstrate that a high dosage of Coptisine could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. These findings suggest a critical role for Coptisine in anti- hypercholesterolemia, and thus it needs to be considered as a potential natural cholesterol lowering agent.
Xianli Meng - One of the best experts on this subject based on the ideXlab platform.
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Coptisine from coptis chinensis exerts diverse beneficial properties a concise review
Journal of Cellular and Molecular Medicine, 2019Co-Authors: Jiasi Wu, Li Xiang, Ping Wang, Donghang Deng, Siyu Su, Sheng Li, Yingfan Hu, Xianli MengAbstract:: Coptisine is a natural small-molecular compound extracted from Coptis chinensis (CC) with a history of using for thousands of years. This work aimed at summarizing Coptisine's activity and providing advice for its clinical use. We analysed the online papers in the database of SciFinder, Web of Science, PubMed, Google scholar and CNKI by setting keywords as 'Coptisine' in combination of 'each pivotal pathway target'. Based on the existing literatures, we find (a) Coptisine exerted potential to be an anti-cancer, anti-inflammatory, CAD ameliorating or anti-bacterial drug through regulating the signalling transduction of pathways such as NF-κB, MAPK, PI3K/Akt, NLRP3 inflammasome, RANKL/RANK and Beclin 1/Sirt1. However, we also (b) observe that the plasma concentration of Coptisine demonstrates obvious non-liner relationship with dosage, and even the highest dosage used in animal study actually cannot reach the minimum concentration level used in cell experiments owing to the poor absorption and low availability of Coptisine. We conclude (a) further investigations can focus on Coptisine's effect on caspase-1-involved inflammasome assembling and pyroptosis activation, as well as autophagy. (b) Under circumstance of promoting Coptisine availability by pursuing nano- or microrods strategies or applying salt-forming process to Coptisine, can it be introduced to clinical trial.
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Pharmacokinetic-Pharmacodynamic Modeling for Coptisine Challenge of Inflammation in LPS-Stimulated Rats.
Scientific Reports, 2019Co-Authors: Li Wang, Li Xiang, Wenge Huang, Xianli Meng, Ping WangAbstract:Pro-inflammatory factors are important indicators for assessing inflammation severity and drug efficacy. Coptisine has been reported to inhibit LPS-induced TNF-α and NO production. In this study, we aim to build a pharmacokinetic-pharmacodynamic model to quantify the Coptisine time course and potency of its anti-inflammatory effect in LPS-stimulated rats. The plasma and lung Coptisine concentrations, plasma and lung TNF-α concentrations, plasma NO concentration, and lung iNOS expression were measured in LPS-stimulated rats after intravenous injection of three Coptisine doses. The Coptisine disposition kinetics were described by a two-compartment model. The Coptisine distribution process from the plasma to the lung was described by first-order dynamics. The dynamics of plasma TNF-α generation and elimination followed zero-order kinetics and the Michaelis-Menten equation. A first-order kinetic model described the TNF-α diffusion process from the plasma to the lung. A precursor-pool indirect response model was used to describe the iNOS and NO generation induced by TNF-α. The inhibition rates of TNF-α production by Coptisine (54.73%, 26.49%, and 13.25%) calculated from the simulation model were close to the decline rates of the plasma TNF-α AUC (57.27%, 40.33%, and 24.98%, respectively). Coptisine suppressed plasma TNF-α generation in a linear manner, resulting in a cascading reduction of iNOS and NO. The early term TNF-α response to stimulation is a key factor in the subsequent inflammatory cascade. In conclusion, this comprehensive PK-PD model provided a rational explanation for the interlocking relationship among TNF-α, iNOS and NO production triggered by LPS and a quantitative evaluation method for inhibition of TNF-α production by Coptisine.
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Coptisine from coptis chinensis inhibits production of inflammatory mediators in lipopolysaccharide stimulated raw 264 7 murine macrophage cells
European Journal of Pharmacology, 2016Co-Authors: Jiasi Wu, Ping Wang, Hai Zhang, Boyang Hu, Lijuan Yang, Fei Wang, Xianli MengAbstract:Coptis chinensis has been used for the treatment of inflammatory diseases in China and other Asian countries for centuries. However, the chemical constituents and mechanism underlying the anti-inflammatory activity of this medicinal plant are poorly understood. Here, Coptisine, the main constituent of C. chinensis, was shown to potently inhibit the production of nitric oxide (NO) by suppressing the protein and mRNA expressions of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Coptisine also inhibited the production of the pro-inflammatory cytokines interleukin-1β (IL-1β) and interleukin-6 (IL-6) by suppressing expression of cytokine mRNA. Coptisine suppressed the degradation of inhibitor of nuclear factor κBα (IκBα) and phosphorylation of extracellular signal-regulated kinase (ERK), c-Jun NH2-terminal kinase (JNK), p38 mitogen-activated protein kinase (MAPK), and phosphoinositide 3-kinase/Akt (PI3K/Akt). Coptisine had no effect on the expression of toll-like receptor 4 (TLR-4) and myeloid differentiation factor 88 (MyD88) as well as LPS binding to TLR-4. Coptisine also inhibited carrageenan-elicited rat paw edema and reduced the release of TNF-α and NO in rat inflamed tissue. These results suggest that Coptisine inhibits LPS-stimulated inflammation by blocking nuclear factor-kappa B, MAPK, and PI3K/Akt activation in macrophages, and can be used as an agent for the prevention and treatment of inflammatory diseases.
Saketh D Sriram - One of the best experts on this subject based on the ideXlab platform.
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Coptisine induced cell cycle arrest at g2 m phase and reactive oxygen species dependent mitochondria mediated apoptosis in non small cell lung cancer a549 cells
Tumor Biology, 2017Co-Authors: Poorna Chandra Rao, Sajeli Begum, Mahendra Sahai, Saketh D SriramAbstract:This study aimed to explore the effect of Coptisine on non-small-cell lung cancer and its mechanism through various in vitro cellular models (A549). Results claimed significant inhibition of proliferation by Coptisine against A549, H460, and H2170 cells with IC50 values of 18.09, 29.50, and 21.60 µM, respectively. Also, Coptisine exhibited upregulation of pH2AX, cell cycle arrest at G2/M phase, and downregulation of the expression of cyclin B1, cdc2, and cdc25C and upregulation of p21 dose dependently. Furthermore, induction of apoptosis in A549 cells by Coptisine was characterized by the activation of caspase 9, caspase 8, and caspase 3, and cleavage of poly adenosine diphosphate ribose polymerase. In addition, Coptisine was found to increase reactive oxygen species generation, upregulate Bax/Bcl-2 ratio, disrupt mitochondrial membrane potential, and cause cytochrome c release into the cytosol. Besides, treatment with a reactive oxygen species inhibitor (N-acetyl cysteine) abrogated Coptisine-induced growth inhibition, apoptosis, reactive oxygen species generation, and mitochondrial dysfunction. Thus, the mediation of reactive oxygen species in the apoptosis-induced effect of Coptisine in A549 cells was corroborated. These findings have offered new insights into the effect and mechanisms of action of Coptisine against non-small-cell lung cancer.
Dong-fang Xue - One of the best experts on this subject based on the ideXlab platform.
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Coptisine attenuates obesity related inflammation through lps tlr 4 mediated signaling pathway in syrian golden hamsters
Fitoterapia, 2015Co-Authors: Zongyao Zou, Yan-zhi Wang, Shuang Xia, Dong-fang XueAbstract:It is known that obesity resulted from consumption of diets high in fat and calories and associated with a chronic low-grade inflammation. Because the fat, sterol and bile acid metabolism of male Syrian golden hamster are more similar to that of human, in the present study, high fat and high cholesterol (HFHC) induced obese hamsters were used to evaluate the anti-inflammation and hypolipidemic role of Coptisine. The results showed that body weight, plasma lipid levels of total cholesterol (TC), triglyceride (TG), low density lipoprotein-cholesterol (LDL-c), very low density lipoprotein-cholesterol (VLDL-c), ApoB and pro-inflammatory cytokines including TNF-α, IL-6 and lipopolysaccharide (LPS) were significantly altered in hamsters fed with HFHC diet. A strong correlation was observed between the LPS level in serum and the level of LBP and pro-inflammatory cytokines. Coptisine from the concentrations of 60 to 700 mg/L dose-dependently inhibited Enterobacter cloacae growth, which can easily induce obesity and insulin resistance. The results of endotoxin neutralization assay suggest that Coptisine is capable of reducing the LPS content under inflammation status. Real time RT-PCR analyses revealed that Coptisine suppressed TLR-4 in visceral fat of hamsters and decreased CD14 expression in livers of hamsters. These encouraging findings make the development of Coptisine a good candidate for preventing obesity-related diseases through the LPS/TLR-4-mediated signaling pathway.
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Coptisine attenuates obesity-related inflammation through LPS/TLR-4-mediated signaling pathway in Syrian golden hamsters
Fitoterapia, 2015Co-Authors: Zongyao Zou, Yan-zhi Wang, Shuang Xia, Dong-fang XueAbstract:It is known that obesity resulted from consumption of diets high in fat and calories and associated with a chronic low-grade inflammation. Because the fat, sterol and bile acid metabolism of male Syrian golden hamster are more similar to that of human, in the present study, high fat and high cholesterol (HFHC) induced obese hamsters were used to evaluate the anti-inflammation and hypolipidemic role of Coptisine. The results showed that body weight, plasma lipid levels of total cholesterol (TC), triglyceride (TG), low density lipoprotein-cholesterol (LDL-c), very low density lipoprotein-cholesterol (VLDL-c), ApoB and pro-inflammatory cytokines including TNF-α, IL-6 and lipopolysaccharide (LPS) were significantly altered in hamsters fed with HFHC diet. A strong correlation was observed between the LPS level in serum and the level of LBP and pro-inflammatory cytokines. Coptisine from the concentrations of 60 to 700 mg/L dose-dependently inhibited Enterobacter cloacae growth, which can easily induce obesity and insulin resistance. The results of endotoxin neutralization assay suggest that Coptisine is capable of reducing the LPS content under inflammation status. Real time RT-PCR analyses revealed that Coptisine suppressed TLR-4 in visceral fat of hamsters and decreased CD14 expression in livers of hamsters. These encouraging findings make the development of Coptisine a good candidate for preventing obesity-related diseases through the LPS/TLR-4-mediated signaling pathway.