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
Objective:To develop and validate a simple,accurate HPTLC method for the analysis of 8-gingerol and to determine the quantity of 8-gingerol inZingiber officinaleextract and gingercontaining dietary supplements,teas an...Objective:To develop and validate a simple,accurate HPTLC method for the analysis of 8-gingerol and to determine the quantity of 8-gingerol inZingiber officinaleextract and gingercontaining dietary supplements,teas and commercial creams.Methods:The analysis was performed on 10×20 cm aluminium-backed plates coated with 0.2 mm layers of silica gel 60 F254(E-Merck,Germany)with n-hexane:ethyl acetate 60:40(v/v)as mobile phase.Camag TLC Scanner III was used for the UV densitometric scanning at 569.Results:This system was found to give a compact spot of 8-gingerol at retention factor(Rf) value of(0.39依0.04)and linearity was found in the ranges 50-500 ng/spot(r2=0.9987).Limit of detection(12.76 ng/spot),limit of quantification(26.32 ng/spot),accuracy(less than 2%)and recovery(ranging from 98.22-99.20)were found satisfactory.Conclusions:The HPTLC method developed for quantification of 8-gingerol was found to be simple,accurate,reproducible,sensitive and is applicable to the analysis of 8-gingerol in Zingiber officinaleextract and ginger-containing dietary supplements,teas and commercial creams.展开更多
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
Objective: To study in vitro anti-hydatic and immunomodulatory effects of ginger and [6]-gingerol as an alternative therapy for Cystic echinococcosis. Methods: Effect of a commonly used herbal product and ginger(Zingi...Objective: To study in vitro anti-hydatic and immunomodulatory effects of ginger and [6]-gingerol as an alternative therapy for Cystic echinococcosis. Methods: Effect of a commonly used herbal product and ginger(Zingiber officinale) towards protoscoleces(PSC) and cyst wall in vitro was studied. The effect of [6]-gingerol, and the pungent constituent of ginger, was also evaluated on PSC culture. Furthermore, the activity of both extracts in association with interferon-gamma(IFN-γ) on PSC co-cultured with mononuclear cells of hydatic patients was evaluated. The nitric oxide(NO) production was measured in each co-culture. Results: Ginger exhibited a concentration- and time-dependent cytotoxic effect against PSC and cyst wall. Interestingly, ginger was more effective than the [6]-gingerol. Moreover, additional parasitic effect between extracts and IFN-γ are also observed in co-cultures. Furthermore, both extracts attenuated the NO production elicited by this infection or by the IFN-γ. Conclusions: Ginger has an important anti-hydatic effect in vitro. This effect is amplified in the presence of IFN-γ. Moreover, this herbal product may protect against host's cell death by reducing the high levels of NO. Ginger may act, at least, through the [6]-gingerol. All our data suggest the promising use of ginger in the treatment of Echinococcus granulosus infection.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
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
The active ingredients of ginger(Zingiber officinale)are 6-gingerol,8-gingerol,and 10-gingerol.Ginger is reported to be an antioxidant,anticancer,and anti-inflammatory agent because of its bioactive metabolites.The 3 ...The active ingredients of ginger(Zingiber officinale)are 6-gingerol,8-gingerol,and 10-gingerol.Ginger is reported to be an antioxidant,anticancer,and anti-inflammatory agent because of its bioactive metabolites.The 3 gingerols share a standard ring structure with different side chains.The maintenance of telomeric length by telomerase is a major issue in almost all cancers.Targeting TERRA G4 could provide a method to inhibit telomerase activity.Molecular docking,molecular dynamics simulations,molecular mechanics Poisson-Boltzmann surface area,principal component analysis,and free energy landscape analysis were performed to evaluate gingerol-TERRA G4 interactions,the extent and stability of these interactions,and the binding free energy and stability of the complexes of the 3 gingerols with TERRA G4.The results revealed that 10-gingerol has superior binding and stabilizing potential for TERRA G4 structures.These findings suggest that TERRA G4 could be a promising therapeutic target for cancer and that 10-gingerol may serve as a potential anticancer lead compound.Further in vitro and in vivo studies to determine the effective dose and toxicity are necessary to evaluate its safety and efficacy.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
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Supported by Deanship of Scientific Research,Salman B in Abdulaziz University,Al-kharj,KSA(Grant No.33/S/54)
文摘Objective:To develop and validate a simple,accurate HPTLC method for the analysis of 8-gingerol and to determine the quantity of 8-gingerol inZingiber officinaleextract and gingercontaining dietary supplements,teas and commercial creams.Methods:The analysis was performed on 10×20 cm aluminium-backed plates coated with 0.2 mm layers of silica gel 60 F254(E-Merck,Germany)with n-hexane:ethyl acetate 60:40(v/v)as mobile phase.Camag TLC Scanner III was used for the UV densitometric scanning at 569.Results:This system was found to give a compact spot of 8-gingerol at retention factor(Rf) value of(0.39依0.04)and linearity was found in the ranges 50-500 ng/spot(r2=0.9987).Limit of detection(12.76 ng/spot),limit of quantification(26.32 ng/spot),accuracy(less than 2%)and recovery(ranging from 98.22-99.20)were found satisfactory.Conclusions:The HPTLC method developed for quantification of 8-gingerol was found to be simple,accurate,reproducible,sensitive and is applicable to the analysis of 8-gingerol in Zingiber officinaleextract and ginger-containing dietary supplements,teas and commercial creams.
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supported by National Project in Health(PNRSanté-2011-2014)
文摘Objective: To study in vitro anti-hydatic and immunomodulatory effects of ginger and [6]-gingerol as an alternative therapy for Cystic echinococcosis. Methods: Effect of a commonly used herbal product and ginger(Zingiber officinale) towards protoscoleces(PSC) and cyst wall in vitro was studied. The effect of [6]-gingerol, and the pungent constituent of ginger, was also evaluated on PSC culture. Furthermore, the activity of both extracts in association with interferon-gamma(IFN-γ) on PSC co-cultured with mononuclear cells of hydatic patients was evaluated. The nitric oxide(NO) production was measured in each co-culture. Results: Ginger exhibited a concentration- and time-dependent cytotoxic effect against PSC and cyst wall. Interestingly, ginger was more effective than the [6]-gingerol. Moreover, additional parasitic effect between extracts and IFN-γ are also observed in co-cultures. Furthermore, both extracts attenuated the NO production elicited by this infection or by the IFN-γ. Conclusions: Ginger has an important anti-hydatic effect in vitro. This effect is amplified in the presence of IFN-γ. Moreover, this herbal product may protect against host's cell death by reducing the high levels of NO. Ginger may act, at least, through the [6]-gingerol. All our data suggest the promising use of ginger in the treatment of Echinococcus granulosus infection.
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.
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.
文摘The active ingredients of ginger(Zingiber officinale)are 6-gingerol,8-gingerol,and 10-gingerol.Ginger is reported to be an antioxidant,anticancer,and anti-inflammatory agent because of its bioactive metabolites.The 3 gingerols share a standard ring structure with different side chains.The maintenance of telomeric length by telomerase is a major issue in almost all cancers.Targeting TERRA G4 could provide a method to inhibit telomerase activity.Molecular docking,molecular dynamics simulations,molecular mechanics Poisson-Boltzmann surface area,principal component analysis,and free energy landscape analysis were performed to evaluate gingerol-TERRA G4 interactions,the extent and stability of these interactions,and the binding free energy and stability of the complexes of the 3 gingerols with TERRA G4.The results revealed that 10-gingerol has superior binding and stabilizing potential for TERRA G4 structures.These findings suggest that TERRA G4 could be a promising therapeutic target for cancer and that 10-gingerol may serve as a potential anticancer lead compound.Further in vitro and in vivo studies to determine the effective dose and toxicity are necessary to evaluate its safety and efficacy.
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.
