AIM: To investigate the effect of gingerol on colonic motility and the action of L-type calcium channel currents in this process.METHODS: The distal colon was cut along the mesenteric border and cleaned with Ca^(2+)-f...AIM: To investigate the effect of gingerol on colonic motility and the action of L-type calcium channel currents in this process.METHODS: The distal colon was cut along the mesenteric border and cleaned with Ca^(2+)-free physiological saline solution. Muscle strips were removed and placed in Ca^(2+)-free physiological saline solution, which was oxygenated continuously. Longitudinal smooth muscle samples were prepared by cutting along the muscle strips and were then placed in a chamber. Mechanical contractile activities of isolated colonic segments in rats were recorded by a 4-channel physiograph. Colon smooth muscle cells were dissociated by enzymatic digestion. L-type calcium currents were recorded using the conventional whole-cell patch-clamp technique.RESULTS: Gingerol inhibited the spontaneous contraction of colonic longitudinal smooth muscle in a dose-dependent manner with inhibition percentages of 13.3% ± 4.1%, 43.4% ± 3.9%, 78.2% ± 3.6% and 80.5% ± 4.5% at 25 μmol/L, 50 μmol/L, 75 μmol/L and 100 μmol/L, respectively(P < 0.01). Nifedipine, an L-type calcium channel blocker, diminished the inhibition of colonic motility by gingerol. Gingerol inhibited L-type calcium channel currents in colonic longitudinal myocytes of rats. At a 75 μmol/L concentration of gingerol, the percentage of gingerolinduced inhibition was diminished by nifedipine from 77.1% ± 4.2% to 42.6% ± 3.6%(P < 0.01). Gingerol suppressed IBa in a dose-dependent manner, and the inhibition rates were 22.7% ± 2.38%, 35.77% ± 3.14%, 49.78% ± 3.48% and 53.78% ± 4.16% of control at 0 m V, respectively, at concentrations of 25 μmol/L, 50 μmol/L, 75 μmol/L and 100 μmol/L(P < 0.01). The steady-state activation curve was shifted to the right by treatment with gingerol. The value of half activation was-14.23 ± 1.12 m V in the control group and-10.56 ± 1.04 m V in the 75 μmol/L group(P < 0.05) with slope factors, Ks, of 7.16 ± 0.84 and 7.02 ± 0.93(P < 0.05) in the control and 75 μmol/L groups, respectively. However, the steady-state inactivation curve was not changed, with a half-inactivation voltage, 0.5 V, of-27.43 ± 1.26 m V in the control group and-26.56 ± 1.53 m V in the 75 μmol/L gingerol group(P > 0.05), and a slope factor, K, of 13.24 ± 1.62 in the control group and 13.45 ± 1.68(P > 0.05) in the 75 μmol/L gingerol group.CONCLUSION: Gingerol inhibits colonic motility by preventing Ca^(2+) influx through L-type calcium channels.展开更多
Leishmaniasis is a vector-borne parasitic neglected tropical disease caused by a group of about 30 different species of the genus Leishmania.It is transmitted by the bite of female phlebotomies sand fly.Three main cli...Leishmaniasis is a vector-borne parasitic neglected tropical disease caused by a group of about 30 different species of the genus Leishmania.It is transmitted by the bite of female phlebotomies sand fly.Three main clinical manifestations of leishmaniasis include cutaneous,visceral,and mucocutaneous leishmaniasis.Visceral leishmaniasis(VL)caused by Leishmania donovani,is an infection of reticuloendothelial system and fatal if untreated.Cholesterol,a sterol that is prominent in the mammalian cell membranes whereas stigmasterol and ergosterol are more prevalent in plants,yeast,and protozoa,respectively.Ergosterols which is absent in human being,is an important constituent of parasite membrane.Sterol C-24 reductase(LdSR)enzyme catalyzes the final step in the ergosterol biosynthesis pathway.The inhibition of biosynthesis of ergosterol may lead to decreased cell viability and growth.Here,we performed the molecular docking-based virtual screening of a library of natural ligands against LdSR to identify a potential inhibitor to fight leishmaniasis.Capsaicin,prenyletin,flavan-3-ol,resveratrol,and gingerol showed the top binding affinity towards LdSR.Based upon ADME properties and bioactivity score,gingerol showed the best lead-likeness and drug-likeness properties.Hence,we further annotated its leishmanicidal properties.We found that gingerol inhibited the growth and proliferation of promastigotes as well as intra-macrophagic amastigotes.Gingerol exerted its antileishmanial action through the induction of reactive oxygen species(ROS)in concentration-dependent manner.Gingerol induced ROS led to apoptosis.Overall,this study described that gingerol would act as possible inhibitor to LdSR.展开更多
OBJECTIVE To prepare gingerol dropping pills and to investigate its protective effect on alcoholic liver injury. METHODS The prescription was selected by orthogonal design method and the effect of the option and ratio...OBJECTIVE To prepare gingerol dropping pills and to investigate its protective effect on alcoholic liver injury. METHODS The prescription was selected by orthogonal design method and the effect of the option and ratio of ground substance,the temperature of drug. The hardness,circular degree,the tail formation and the dissolution time were studied. Totally 40 KM mice were randomly divided into control group,model group,gingerol dropping pill group(400 mg·kg^(-1)·d^(-1)) and positive control group(bifendate,150 mg·kg^(-1)·d^(-1)) of 10 mice each. The mice from the model and two drug groups were administrated with liqueur[0.15 mL/(10 g·d)]daily by gavage for 3 weeks,Two hours later,drug group mice were treated corresponding gingerol dropping pill and bifendate. Meanwhile,the control group were gavaged same amount of normal saline. Finally,when the model of acute alcoholic liver injury was established on the 22 stday,Biochemical indicators of ocular blood in mice were observed.We also observed the change of liver morphology. RESULTS Under optimum conditions,we can obtain dropping pills having circular shape,touching with hardness and short dissolution time. Compared with the control group,the levels of alanine transaminase(ALT),glutamic-oxaloacetic transaminase(AST) and malondialdehyde(MDA) in model group were obviously increased(P<0.01),While the activity of Superoxide dismutase(SOD) were decreased. In addition,In model group,mice liver disorders,hepatic lobule fusion,accompanying a large number of patchy sample liver cell vacuoles,various sizes of fat vacuoles appeared in cytoplasm and inflammatory cell infiltration were visible around the central vein. On the contrary,compared with the model group,drug groups attenuated or even reversed hepatic pathological changes. Form gingerol dropping pill group,an increase in hepatic SOD activity and serum ALT and AST activities were found and a significant decrease in hepatic MDA content were also observed(P<0.01). CONCLUSION The prescription of gingerol dropping pills was reasonable,and the preparation process was simple. Gingerol dropping pills can protect liver from alcoholic liver injury to some extend,and the mechanism may be related to its antioxidant effect.展开更多
OBJECTIVE To investigate the influence of gingerol on the improvement of learning and memory impairment of rat model of Alzheimer disease induced by β-amyloid peptide fragment 25-35(Aβ_(25-35)) and to analysis the p...OBJECTIVE To investigate the influence of gingerol on the improvement of learning and memory impairment of rat model of Alzheimer disease induced by β-amyloid peptide fragment 25-35(Aβ_(25-35)) and to analysis the possible mechanism. METHODS SD rats were randomly divided into 5groups: blank control group,model group,sham-operated group,low dose drug group(gingerol emulsion,10 mg·kg^(-1)·d^(-1)),high dose drug group(gingerol emulsion,50 mg·kg^(-1)·d^(-1)). Model group and two drug groups were injected Aβ_(25-35)(5 μL) in lateral cerebral ventricle. Sham-operated group were injected the same amount of sterile PBS solution. For blank control group without any treatment. When all the rats refresh themselves and had post-operated activities,two drug groups were gavaged with different concentration of gingerol emulsion,Meanwhile,sham-operated group were gavaged with sterile physiological saline,the remaining two groups without any treatment. After three weeks,we make use of Y labyrinth to test the ability of space learning and memory of rats. Finally,rats were sacrificed to collect blood by abdominal aortic method. The content of acetylcholine(ACh),SOD and MDA were detected in serum. RESULTS(1) Compared with blank control group,the ability of learning and memory of model group rats were weakened,the error times increased in Y labyrinth experiment. In addition,the content of ACh and the activity of SOD significantly decreased,the content of MDA increased(P<0.05).(2) On the contrary,the rats gavaged with gingerol emusion have less error times in Y labyrinth experiment compared with model group. the content of Ach and the activity of SOD significantly increased,the content of MDA decreased(P<0.05). However,two different gingerol emusion concentration groups have no significantly difference. CONCLUSION The ability of learning and memory of rats gavaged with gingerol emusion were significantly improved compared with Aβ_(25-35) induced rats without any treatment.Its mechanism may be related to antioxidant and neurotransmitter.展开更多
The seeds of Aframomum melegueta K. Schum (grains of paradise, Zingiberaceae) are used as a common spice in African countries and a fine condiment in the European cuisine. In this study, we evaluated the phytochemical...The seeds of Aframomum melegueta K. Schum (grains of paradise, Zingiberaceae) are used as a common spice in African countries and a fine condiment in the European cuisine. In this study, we evaluated the phytochemical profile of various seed extracts of A. melegueta as well as their antimicrobial, antioxidant and enzyme inhibitory effects. In total, 25 diarylheptanoids, five gingerol derivatives and nine phenolic/organic acids were tentatively annotated in A. melegueta by liquid chromatography hyphenated with high resolution tandem mass spectrometry (LC-HRMS/MS). A. melegueta showed a moderate inhibitory activity against different human pathogenic microbial strains, with H. pylori the most sensitive microorganism. A strong antioxidant and enzyme inhibitory potential was shown in various radical scavenging, reducing and chelating assays as well as in cholinesterase, tyrosinase and glucosidase assays. Several specialized metabolites from A. melegueta (diarylheptanoids, gingerols) were shown to be directly linked with the investigated antioxidant and enzyme inhibitory activities, as evaluated through the correlation analysis. In addition, two diarylheptanoids (one heptan-3-ol and one heptan- 3,5-diol) displayed the strongest binding to acetylcholinesterase (AChE) via multiple H-bonds, a couple of π-π interactions and van der Waals interactions all over the catalytic channel of the enzyme, as evidenced by the molecular docking study. Overall, our work brings new contributions to the phyto-complexity and poly-pharmacology of spices from genus Aframomum than can find future applications in pharmaceutical, nutraceutical or cosmeceutical industry.展开更多
Background Gingerol is the generic term for pungent constituents in ginger, which has been reported to be effective for inhibiting vomiting. We attempted to investigate the antiemetic effect of gingerol and its effect...Background Gingerol is the generic term for pungent constituents in ginger, which has been reported to be effective for inhibiting vomiting. We attempted to investigate the antiemetic effect of gingerol and its effective mechanism on substance P and NK1 receptors in minks. Methods The antiemetic effect of gingerol was investigated during a 6-hour observation on a vomiting model in minks induced by cisplatin, (7.5 mg/kg, intraperitoneal). The distribution of substance P and NK1 receptors in the area postrema and ileum were measured by immunohistochemistry, and the expression of NK1 receptor in the area postrema and ileum were measured by Western blotting. Results The frequency of cisplatin induced retching and vomiting was significantly reduced by pretreatment with gingerol in a dose-dependent manner (P 〈0.05). Substance P-immunoreactive was mainly situated in the mucosa and submucosa of the ileum as well as in the neurons of the area postrema. The immunoreactive production of NK1 receptor was mainly situated in the muscular and submucosa of ileum and the neurons of area postrema, gingerol markedly suppressed the increased immunoreactivity of substance P and NK1 receptor induced by cisplatin in a dose-dependent manner (P 〈0.05), and exhibited effective inhibition on the increased expression levels of NK1 receptor in both the ileum and area postrema dose-dependently (P 〈0.05). Conclusions Gingerol has good activity against cisplatin-induced emesis in minks possibly by inhibiting central or peripheral increase of substance P and NK1 receptors.展开更多
TRPA1 channels are non-selective cation channels that could be activated by plant-derived pungent products, including gingerol, a main active constituent of ginger. Ginger could improve the digestive function; however...TRPA1 channels are non-selective cation channels that could be activated by plant-derived pungent products, including gingerol, a main active constituent of ginger. Ginger could improve the digestive function; however whether ginger improves the digestive function through activating TRPA1 receptor in gastrointestinal tract has not been investigated. In the present study, gingerol was used to stimulate cell lines(RIN14B or STC-1) while depletion of extracellular calcium.TRPA1 inhibitor(rethenium red) and TRPA1 gene silencing via TRPA1-specific si RNA were also used for mechanistic studies. The intracellular calcium and secretion of serotonin or cholecystokinin were measured by fura-2/AM and ELISA. Stimulation of those cells with gingerol increased intracellular calcium levels and the serotonin or cholecystokinin secretion. The gingerol-induced intracellular calcium increase and secretion(serotonin or cholecystokinin) release were completely blocked by ruthenium red, EGTA, and TRPA1-specific si RNA. In summary, our results suggested that gingerol derived from ginger might improve the digestive function through secretion releasing from endocrine cells of the gut by inducing TRPA1-mediated calcium influx.展开更多
Background The conventional procedure for screening bioactive components from traditional Chinese medicine is time-consuming, expensive and low efficient. Therefore, some alternative strategies are needed urgently. A ...Background The conventional procedure for screening bioactive components from traditional Chinese medicine is time-consuming, expensive and low efficient. Therefore, some alternative strategies are needed urgently. A novel method for screening anti-platelet aggregation components from oleoresins was developed using chicken thrombocyte extract and high performance liquid chromatography. Methods The anti-platelet aggregation components of oleoresins were combined with receptors, channels and enzymes of chicken thrombocytes under physiological environment. Unbound substances were washed away and bound compounds were eluted using specific phosphate buffered solution (PBS). Compounds released from target sites were collected and analyzed by high performance liquid chromatography and LC-MS. The activity of three compounds which were screened from this model was confirmed using platelet aggregation pharmacology in vivo. Results There were four typical compounds that bound to the thrombocytes: 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol, and all had shown anti-platelet aggregation activities. Eight-gingerol displayed the best anti-platelet aggregation effect. Conclusions Chicken thromobcyte extract can be used to isolate chemicals that are ligands of the receptor or other bio-targets on the platelet. This may therefore be a simple and efficient method to screen for anti-platelet aggregation compounds from traditional Chinese medicine.展开更多
Diabetes mellitus is a chronic disease,typified by hyperglycemia resulting from failures in complex multifactorial metabolic functions,that requires life-long medication.Prolonged uncontrolled hyperglycemia leads to m...Diabetes mellitus is a chronic disease,typified by hyperglycemia resulting from failures in complex multifactorial metabolic functions,that requires life-long medication.Prolonged uncontrolled hyperglycemia leads to micro-and macro-vascular complications.Although antidiabetic drugs are prescribed as the first-line treatment,many of them lose efficacy over time or have severe side effects.There is a lack of in-depth study on the patents filed concerning the use of natural compounds to manage diabetes.Thus,this patent analysis provides a comprehensive report on the antidiabetic therapeutic activity of 6 phytocompounds when taken alone or in combinations.Four patent databases were searched,and 17,649 patents filed between 2001 and 2021 were retrieved.0f these,139 patents for antidiabetic therapeutic aids that included berberine,curcumin,gingerol,gymnemic acid,gymnemagenin and mangiferin were analyzed.The results showed that these compounds alone or in combinations,targeting acetylcoenzyme A carboxylase 2,serine/threonine protein kinase,α-amylase,α-glucosidase,lipooxygenase,phosphorylase,peroxisome proliferator-activated receptor-γ(PPAR-γ),protein tyrosine phosphatase 1B,PPARγco-activator-1α,phosphoinositide 3-kinase and protein phosphatase 1 regulatory subunit 3C,could regulate glucose metabolism which are validated by pharmacological rationale.Synergism,or combination therapy,including different phytocompounds and plant extracts,has been studied extensively and found effective,whereas the efficacy of commercial drugs in combination with phytocompounds has not been studied in detail.Curcumin,gymnemic acid and mangiferin were found to be effective against diabetes-related complications.展开更多
Background Cardiorenal syndrome(CRS)is a clinical syndrome with a complex mechanism,and there is currently no specific treatment.Gingerol was confirmed to possess anti-inflammatory,antioxidant and cardiotonic properti...Background Cardiorenal syndrome(CRS)is a clinical syndrome with a complex mechanism,and there is currently no specific treatment.Gingerol was confirmed to possess anti-inflammatory,antioxidant and cardiotonic properties as cardiovascular pharmacological effects.However,in vivo studies have yet to prove that it can improve cardiac function and inhibit fibrosis in rats with cardiorenal syndrome.Methods In this study,34 male Sprague-Dawley(SD)rats were randomly divided into control(n=9),model(n=12)and gingerol groups(n=13).The model and the gingerol groups underwent ligation of the left anterior descending coronary artery and 5/6 subtotal nephrectomy to construct a type 2 cardiorenal syndrome rat model.The rats in gingerol group were injected intraperitoneally with 50 mg/kg gingerol.The same amount of saline was administered to both the control and the model groups.Following 4 weeks of treatment,the rat cardiac function and myocardial fibrosis were evaluated by cardiac ultrasound and blood biochemistry.Results Biochemical results showed that the brain natriuretic peptide(BNP)levels of gingerol group decreased(P<0.05).Cardiac ultrasound revealed that gingerol improved cardiac systolic function and ventricular remodeling(P<0.05).The systolic function of the model group was significantly decreased compared with the control group.Masson staining confirmed that the fibrosis area in the model group was significantly augmented than that in the control group,while the area of fibrosis in the gingerol group was diminished compared to the model group(P<0.01).Moreover,immunofluorescence showed that compared with the control group,the expression of collagen 1,TGF-β1 andα-SMA was significantly increased in the model group,and both collagen deposition and the expression of collagen I,TGF-β1 andα-SMA decreased in gingerol group.Immunohistochemistry revealed that the expression of collagen 1 andα-SMA was significantly increased in the model group compared with the control group,while it was decreased in gingerol group(P<0.05).Conclusions Gingerol can improve the cardiac function and cardiac fibrosis in rats with cardiorenal syndrome.展开更多
基金Supported by National Basic Research Program of China(973 Program)No.2013CB531703+3 种基金National Natural Science Foundation of ChinaNo.81273919Natural Science Foundation of Liaoning ProvinceNo.2012225020 and No.2013023002
文摘AIM: To investigate the effect of gingerol on colonic motility and the action of L-type calcium channel currents in this process.METHODS: The distal colon was cut along the mesenteric border and cleaned with Ca^(2+)-free physiological saline solution. Muscle strips were removed and placed in Ca^(2+)-free physiological saline solution, which was oxygenated continuously. Longitudinal smooth muscle samples were prepared by cutting along the muscle strips and were then placed in a chamber. Mechanical contractile activities of isolated colonic segments in rats were recorded by a 4-channel physiograph. Colon smooth muscle cells were dissociated by enzymatic digestion. L-type calcium currents were recorded using the conventional whole-cell patch-clamp technique.RESULTS: Gingerol inhibited the spontaneous contraction of colonic longitudinal smooth muscle in a dose-dependent manner with inhibition percentages of 13.3% ± 4.1%, 43.4% ± 3.9%, 78.2% ± 3.6% and 80.5% ± 4.5% at 25 μmol/L, 50 μmol/L, 75 μmol/L and 100 μmol/L, respectively(P < 0.01). Nifedipine, an L-type calcium channel blocker, diminished the inhibition of colonic motility by gingerol. Gingerol inhibited L-type calcium channel currents in colonic longitudinal myocytes of rats. At a 75 μmol/L concentration of gingerol, the percentage of gingerolinduced inhibition was diminished by nifedipine from 77.1% ± 4.2% to 42.6% ± 3.6%(P < 0.01). Gingerol suppressed IBa in a dose-dependent manner, and the inhibition rates were 22.7% ± 2.38%, 35.77% ± 3.14%, 49.78% ± 3.48% and 53.78% ± 4.16% of control at 0 m V, respectively, at concentrations of 25 μmol/L, 50 μmol/L, 75 μmol/L and 100 μmol/L(P < 0.01). The steady-state activation curve was shifted to the right by treatment with gingerol. The value of half activation was-14.23 ± 1.12 m V in the control group and-10.56 ± 1.04 m V in the 75 μmol/L group(P < 0.05) with slope factors, Ks, of 7.16 ± 0.84 and 7.02 ± 0.93(P < 0.05) in the control and 75 μmol/L groups, respectively. However, the steady-state inactivation curve was not changed, with a half-inactivation voltage, 0.5 V, of-27.43 ± 1.26 m V in the control group and-26.56 ± 1.53 m V in the 75 μmol/L gingerol group(P > 0.05), and a slope factor, K, of 13.24 ± 1.62 in the control group and 13.45 ± 1.68(P > 0.05) in the 75 μmol/L gingerol group.CONCLUSION: Gingerol inhibits colonic motility by preventing Ca^(2+) influx through L-type calcium channels.
基金Deanship of Scientific Research at Majmaah University,Al Majmaah,11952,Saudi Arabia for supporting this work under the Group Project No.RGP-2019-31.
文摘Leishmaniasis is a vector-borne parasitic neglected tropical disease caused by a group of about 30 different species of the genus Leishmania.It is transmitted by the bite of female phlebotomies sand fly.Three main clinical manifestations of leishmaniasis include cutaneous,visceral,and mucocutaneous leishmaniasis.Visceral leishmaniasis(VL)caused by Leishmania donovani,is an infection of reticuloendothelial system and fatal if untreated.Cholesterol,a sterol that is prominent in the mammalian cell membranes whereas stigmasterol and ergosterol are more prevalent in plants,yeast,and protozoa,respectively.Ergosterols which is absent in human being,is an important constituent of parasite membrane.Sterol C-24 reductase(LdSR)enzyme catalyzes the final step in the ergosterol biosynthesis pathway.The inhibition of biosynthesis of ergosterol may lead to decreased cell viability and growth.Here,we performed the molecular docking-based virtual screening of a library of natural ligands against LdSR to identify a potential inhibitor to fight leishmaniasis.Capsaicin,prenyletin,flavan-3-ol,resveratrol,and gingerol showed the top binding affinity towards LdSR.Based upon ADME properties and bioactivity score,gingerol showed the best lead-likeness and drug-likeness properties.Hence,we further annotated its leishmanicidal properties.We found that gingerol inhibited the growth and proliferation of promastigotes as well as intra-macrophagic amastigotes.Gingerol exerted its antileishmanial action through the induction of reactive oxygen species(ROS)in concentration-dependent manner.Gingerol induced ROS led to apoptosis.Overall,this study described that gingerol would act as possible inhibitor to LdSR.
基金The project supported by Col ege Students Of Science and Technology Innovation Project of Tai'an City(2015D064)the National College Students'Innovative and Entrepreneurial Training Project(201510439078)
文摘OBJECTIVE To prepare gingerol dropping pills and to investigate its protective effect on alcoholic liver injury. METHODS The prescription was selected by orthogonal design method and the effect of the option and ratio of ground substance,the temperature of drug. The hardness,circular degree,the tail formation and the dissolution time were studied. Totally 40 KM mice were randomly divided into control group,model group,gingerol dropping pill group(400 mg·kg^(-1)·d^(-1)) and positive control group(bifendate,150 mg·kg^(-1)·d^(-1)) of 10 mice each. The mice from the model and two drug groups were administrated with liqueur[0.15 mL/(10 g·d)]daily by gavage for 3 weeks,Two hours later,drug group mice were treated corresponding gingerol dropping pill and bifendate. Meanwhile,the control group were gavaged same amount of normal saline. Finally,when the model of acute alcoholic liver injury was established on the 22 stday,Biochemical indicators of ocular blood in mice were observed.We also observed the change of liver morphology. RESULTS Under optimum conditions,we can obtain dropping pills having circular shape,touching with hardness and short dissolution time. Compared with the control group,the levels of alanine transaminase(ALT),glutamic-oxaloacetic transaminase(AST) and malondialdehyde(MDA) in model group were obviously increased(P<0.01),While the activity of Superoxide dismutase(SOD) were decreased. In addition,In model group,mice liver disorders,hepatic lobule fusion,accompanying a large number of patchy sample liver cell vacuoles,various sizes of fat vacuoles appeared in cytoplasm and inflammatory cell infiltration were visible around the central vein. On the contrary,compared with the model group,drug groups attenuated or even reversed hepatic pathological changes. Form gingerol dropping pill group,an increase in hepatic SOD activity and serum ALT and AST activities were found and a significant decrease in hepatic MDA content were also observed(P<0.01). CONCLUSION The prescription of gingerol dropping pills was reasonable,and the preparation process was simple. Gingerol dropping pills can protect liver from alcoholic liver injury to some extend,and the mechanism may be related to its antioxidant effect.
基金The project supported by National College Students'Innovative and Entrepreneurial Training Project(201510439078)Science and Technology Development Plan of Tai'an City(201540707)
文摘OBJECTIVE To investigate the influence of gingerol on the improvement of learning and memory impairment of rat model of Alzheimer disease induced by β-amyloid peptide fragment 25-35(Aβ_(25-35)) and to analysis the possible mechanism. METHODS SD rats were randomly divided into 5groups: blank control group,model group,sham-operated group,low dose drug group(gingerol emulsion,10 mg·kg^(-1)·d^(-1)),high dose drug group(gingerol emulsion,50 mg·kg^(-1)·d^(-1)). Model group and two drug groups were injected Aβ_(25-35)(5 μL) in lateral cerebral ventricle. Sham-operated group were injected the same amount of sterile PBS solution. For blank control group without any treatment. When all the rats refresh themselves and had post-operated activities,two drug groups were gavaged with different concentration of gingerol emulsion,Meanwhile,sham-operated group were gavaged with sterile physiological saline,the remaining two groups without any treatment. After three weeks,we make use of Y labyrinth to test the ability of space learning and memory of rats. Finally,rats were sacrificed to collect blood by abdominal aortic method. The content of acetylcholine(ACh),SOD and MDA were detected in serum. RESULTS(1) Compared with blank control group,the ability of learning and memory of model group rats were weakened,the error times increased in Y labyrinth experiment. In addition,the content of ACh and the activity of SOD significantly decreased,the content of MDA increased(P<0.05).(2) On the contrary,the rats gavaged with gingerol emusion have less error times in Y labyrinth experiment compared with model group. the content of Ach and the activity of SOD significantly increased,the content of MDA decreased(P<0.05). However,two different gingerol emusion concentration groups have no significantly difference. CONCLUSION The ability of learning and memory of rats gavaged with gingerol emusion were significantly improved compared with Aβ_(25-35) induced rats without any treatment.Its mechanism may be related to antioxidant and neurotransmitter.
文摘The seeds of Aframomum melegueta K. Schum (grains of paradise, Zingiberaceae) are used as a common spice in African countries and a fine condiment in the European cuisine. In this study, we evaluated the phytochemical profile of various seed extracts of A. melegueta as well as their antimicrobial, antioxidant and enzyme inhibitory effects. In total, 25 diarylheptanoids, five gingerol derivatives and nine phenolic/organic acids were tentatively annotated in A. melegueta by liquid chromatography hyphenated with high resolution tandem mass spectrometry (LC-HRMS/MS). A. melegueta showed a moderate inhibitory activity against different human pathogenic microbial strains, with H. pylori the most sensitive microorganism. A strong antioxidant and enzyme inhibitory potential was shown in various radical scavenging, reducing and chelating assays as well as in cholinesterase, tyrosinase and glucosidase assays. Several specialized metabolites from A. melegueta (diarylheptanoids, gingerols) were shown to be directly linked with the investigated antioxidant and enzyme inhibitory activities, as evaluated through the correlation analysis. In addition, two diarylheptanoids (one heptan-3-ol and one heptan- 3,5-diol) displayed the strongest binding to acetylcholinesterase (AChE) via multiple H-bonds, a couple of π-π interactions and van der Waals interactions all over the catalytic channel of the enzyme, as evidenced by the molecular docking study. Overall, our work brings new contributions to the phyto-complexity and poly-pharmacology of spices from genus Aframomum than can find future applications in pharmaceutical, nutraceutical or cosmeceutical industry.
基金This work was supported by National Natural Science Foundation of China (No. 30873108) and Natural Science Foundation of Shandong Province (No. Y2007C097).Acknowledgements: The first author of this article wants to express his special thanks to Professor WANG Kai of Department of Hepatology in Qilu Hospital of Shandong University for the suggestion and comments on experiments and manuscript. The author also thanks Qingdao University Guide for the Care and Use of Laboratory Animals for providing the animals.
文摘Background Gingerol is the generic term for pungent constituents in ginger, which has been reported to be effective for inhibiting vomiting. We attempted to investigate the antiemetic effect of gingerol and its effective mechanism on substance P and NK1 receptors in minks. Methods The antiemetic effect of gingerol was investigated during a 6-hour observation on a vomiting model in minks induced by cisplatin, (7.5 mg/kg, intraperitoneal). The distribution of substance P and NK1 receptors in the area postrema and ileum were measured by immunohistochemistry, and the expression of NK1 receptor in the area postrema and ileum were measured by Western blotting. Results The frequency of cisplatin induced retching and vomiting was significantly reduced by pretreatment with gingerol in a dose-dependent manner (P 〈0.05). Substance P-immunoreactive was mainly situated in the mucosa and submucosa of the ileum as well as in the neurons of the area postrema. The immunoreactive production of NK1 receptor was mainly situated in the muscular and submucosa of ileum and the neurons of area postrema, gingerol markedly suppressed the increased immunoreactivity of substance P and NK1 receptor induced by cisplatin in a dose-dependent manner (P 〈0.05), and exhibited effective inhibition on the increased expression levels of NK1 receptor in both the ileum and area postrema dose-dependently (P 〈0.05). Conclusions Gingerol has good activity against cisplatin-induced emesis in minks possibly by inhibiting central or peripheral increase of substance P and NK1 receptors.
基金supported by the National Natural Science Foundation of China(Nos.30973003&30901993)Administration of TCM of Jiangsu province(No.LZ11093)
文摘TRPA1 channels are non-selective cation channels that could be activated by plant-derived pungent products, including gingerol, a main active constituent of ginger. Ginger could improve the digestive function; however whether ginger improves the digestive function through activating TRPA1 receptor in gastrointestinal tract has not been investigated. In the present study, gingerol was used to stimulate cell lines(RIN14B or STC-1) while depletion of extracellular calcium.TRPA1 inhibitor(rethenium red) and TRPA1 gene silencing via TRPA1-specific si RNA were also used for mechanistic studies. The intracellular calcium and secretion of serotonin or cholecystokinin were measured by fura-2/AM and ELISA. Stimulation of those cells with gingerol increased intracellular calcium levels and the serotonin or cholecystokinin secretion. The gingerol-induced intracellular calcium increase and secretion(serotonin or cholecystokinin) release were completely blocked by ruthenium red, EGTA, and TRPA1-specific si RNA. In summary, our results suggested that gingerol derived from ginger might improve the digestive function through secretion releasing from endocrine cells of the gut by inducing TRPA1-mediated calcium influx.
基金This work was supported by the grants from the National Natural Science Foundation of China (No. 30400596), Jinan University Natural Science Foundation (No. 51204017) and the Chinese Traditional Medicine Foundation of Guangdong Province (No. 104005).
文摘Background The conventional procedure for screening bioactive components from traditional Chinese medicine is time-consuming, expensive and low efficient. Therefore, some alternative strategies are needed urgently. A novel method for screening anti-platelet aggregation components from oleoresins was developed using chicken thrombocyte extract and high performance liquid chromatography. Methods The anti-platelet aggregation components of oleoresins were combined with receptors, channels and enzymes of chicken thrombocytes under physiological environment. Unbound substances were washed away and bound compounds were eluted using specific phosphate buffered solution (PBS). Compounds released from target sites were collected and analyzed by high performance liquid chromatography and LC-MS. The activity of three compounds which were screened from this model was confirmed using platelet aggregation pharmacology in vivo. Results There were four typical compounds that bound to the thrombocytes: 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol, and all had shown anti-platelet aggregation activities. Eight-gingerol displayed the best anti-platelet aggregation effect. Conclusions Chicken thromobcyte extract can be used to isolate chemicals that are ligands of the receptor or other bio-targets on the platelet. This may therefore be a simple and efficient method to screen for anti-platelet aggregation compounds from traditional Chinese medicine.
文摘Diabetes mellitus is a chronic disease,typified by hyperglycemia resulting from failures in complex multifactorial metabolic functions,that requires life-long medication.Prolonged uncontrolled hyperglycemia leads to micro-and macro-vascular complications.Although antidiabetic drugs are prescribed as the first-line treatment,many of them lose efficacy over time or have severe side effects.There is a lack of in-depth study on the patents filed concerning the use of natural compounds to manage diabetes.Thus,this patent analysis provides a comprehensive report on the antidiabetic therapeutic activity of 6 phytocompounds when taken alone or in combinations.Four patent databases were searched,and 17,649 patents filed between 2001 and 2021 were retrieved.0f these,139 patents for antidiabetic therapeutic aids that included berberine,curcumin,gingerol,gymnemic acid,gymnemagenin and mangiferin were analyzed.The results showed that these compounds alone or in combinations,targeting acetylcoenzyme A carboxylase 2,serine/threonine protein kinase,α-amylase,α-glucosidase,lipooxygenase,phosphorylase,peroxisome proliferator-activated receptor-γ(PPAR-γ),protein tyrosine phosphatase 1B,PPARγco-activator-1α,phosphoinositide 3-kinase and protein phosphatase 1 regulatory subunit 3C,could regulate glucose metabolism which are validated by pharmacological rationale.Synergism,or combination therapy,including different phytocompounds and plant extracts,has been studied extensively and found effective,whereas the efficacy of commercial drugs in combination with phytocompounds has not been studied in detail.Curcumin,gymnemic acid and mangiferin were found to be effective against diabetes-related complications.
文摘Background Cardiorenal syndrome(CRS)is a clinical syndrome with a complex mechanism,and there is currently no specific treatment.Gingerol was confirmed to possess anti-inflammatory,antioxidant and cardiotonic properties as cardiovascular pharmacological effects.However,in vivo studies have yet to prove that it can improve cardiac function and inhibit fibrosis in rats with cardiorenal syndrome.Methods In this study,34 male Sprague-Dawley(SD)rats were randomly divided into control(n=9),model(n=12)and gingerol groups(n=13).The model and the gingerol groups underwent ligation of the left anterior descending coronary artery and 5/6 subtotal nephrectomy to construct a type 2 cardiorenal syndrome rat model.The rats in gingerol group were injected intraperitoneally with 50 mg/kg gingerol.The same amount of saline was administered to both the control and the model groups.Following 4 weeks of treatment,the rat cardiac function and myocardial fibrosis were evaluated by cardiac ultrasound and blood biochemistry.Results Biochemical results showed that the brain natriuretic peptide(BNP)levels of gingerol group decreased(P<0.05).Cardiac ultrasound revealed that gingerol improved cardiac systolic function and ventricular remodeling(P<0.05).The systolic function of the model group was significantly decreased compared with the control group.Masson staining confirmed that the fibrosis area in the model group was significantly augmented than that in the control group,while the area of fibrosis in the gingerol group was diminished compared to the model group(P<0.01).Moreover,immunofluorescence showed that compared with the control group,the expression of collagen 1,TGF-β1 andα-SMA was significantly increased in the model group,and both collagen deposition and the expression of collagen I,TGF-β1 andα-SMA decreased in gingerol group.Immunohistochemistry revealed that the expression of collagen 1 andα-SMA was significantly increased in the model group compared with the control group,while it was decreased in gingerol group(P<0.05).Conclusions Gingerol can improve the cardiac function and cardiac fibrosis in rats with cardiorenal syndrome.