AIM:The effects of vitamin D3 have been investigated on various tumors, including colorectal cancer (CRC). 25-hydroxyvitamin-D3-24-hydroxylase (CYP24A1), the enzyme that inactivates the active vitamin D3 metabolite 1,...AIM:The effects of vitamin D3 have been investigated on various tumors, including colorectal cancer (CRC). 25-hydroxyvitamin-D3-24-hydroxylase (CYP24A1), the enzyme that inactivates the active vitamin D3 metabolite 1,25-dihydroxyvitamin D3 (1,25-D3), is considered to be the main enzyme determining the biological halflife of 1,25-D3. During colorectal carcinogenesis, the expression and concentration of CYP24A1 increases significantly, suggesting that this phenomenon could be responsible for the proposed efficacy of 1,25-D3 in the treatment of CRC. The aim of this study was to investigate the anti-tumor effects of vitamin D3 on the human CRC cell line Caco-2 after inhibition of the cytochrome P450 component of CYP24A1 activity. METHODS:We examined the expression of CYP24A1 mRNA and the effects of 1,25-D3 on the cell line Caco-2 after inhibition of CYP24A1. Cell viability and proliferation were determined by means of sulforhodamine-B staining and bromodeoxyuridine incorporation, respectively, while cytotoxicity was estimated via the lactate dehydrogenase content of the cell culture supernatant. CYP24A1 expression was measured by realtime reverse transcription polymerase chain reaction. A number of tetralone compounds were synthesized to investigate their CP24A1 inhibitory activity. RESULTS:In response to 1,25-D3, CYP24A1 mRNA expression was enhanced significantly, in a time- and dose-dependent manner. Caco-2 cell viability and proliferation were not influenced by the administration of 1,25-D3 alone, but were markedly reduced by coadministration of 1,25-D3 and KD-35, a CYP24A1-inhibiting tetralone. Our data suggest that the mechanism of action of co-administered KD-35 and 1,25-D3 does not involve a direct cytotoxic effect, but rather the inhibition of cell proliferation. CONCLUSION:These findings demonstrate that the selective inhibition of CYP24A1 by compounds such as KD-35 may be a new approach for enhancement of the anti-tumor effect of 1,25-D3 on CRC.展开更多
The inhibition effect of tert-butyl alcohol(TBA), identified as the·OH radical inhibitor, on the TiO_2 nano assays(TNA) photoelectrocatalytic oxidation of different organics such as glucose and phthalate was repo...The inhibition effect of tert-butyl alcohol(TBA), identified as the·OH radical inhibitor, on the TiO_2 nano assays(TNA) photoelectrocatalytic oxidation of different organics such as glucose and phthalate was reported. The adsorption performance of these organics on the TNA photoelectrode was investigated by using the instantaneous photocurrent value, and the degradation property was examined by using the exhausted reaction. The results showed that glucose exhibited the poor adsorption and easy degradation performance, phthalate showed the strong adsorption and harddegradation, but TBA showed the weak adsorption and was the most difficult to be degraded. The degradation of both glucose and phthalate could be inhibited evidently by TBA. But the effect on glucose was more obvious. The different inhibition effects of TBA on different organics could be attributed to the differences in the adsorption and the degradation property. For instance, phthalate of the strong adsorption property could avoid from the capture of·OH radicals by TBA in TNA photoelectrocatalytic process.展开更多
AIM: To investigate the effects of lentivirus vector mediated short hairpin RNA interference targeting methionine adenosyltransferase 2β gene (LV-shMAT2B) on hepatocelluar carcinoma (HCC) cells. METHODS: We construct...AIM: To investigate the effects of lentivirus vector mediated short hairpin RNA interference targeting methionine adenosyltransferase 2β gene (LV-shMAT2B) on hepatocelluar carcinoma (HCC) cells. METHODS: We constructed four plasmids of RNA interference targeting the MAT2B gene. After LV-shMAT2B was transfected with L-02 cells and two kinds of HCC cells, cell viability and proliferation were measured with MTT and [3H]thymidine assays respectively. Flow cytometry was used to assess cell apoptosis. The level of S-adenosyl methionine (SAMe) in HepG2 cells was evaluated. The expressions of cyclin D1, cyclin D2, bcl-xL and bcl-xS were detected with western blot. RESULTS: We constructed LV-shMAT2B successfully. LV-shMAT2B was safe for human normal liver cells. LV-shMAT2B caused dramatic reduction in proliferation compared with controls in HCC cells Bel-7402 (P = 0.054) and HepG2 (P = 0.031). Flow cytometry analysis showed that cell apoptosis caused by LV-shMAT2B was greater in HCC cells Bel-7402 and HepG2 than in control induced by scrambled siRNA (P = 0.047), but apoptosis rates in L-02 induced by LV-shMAT2B and scrambled siRNA respectively had no significant difference. Moreover, LV-shMAT2B significantly suppressed expression of MAT2B leading to growth-inhibition effect on HCC cells by down-regulating cyclin D1. Apoptosis induced by LV-shMAT2B was involved indown-regulating bcl-xL and up-regulating bcl-xS. CONCLUSION: LV-shMAT2B can induce cell apoptosis and growth-inhibition in HCC cells. MAT2B may be a therapy target in HCC in the future.展开更多
Human epidermal growth factor receptor 2(HER2) signaling pathway activation has been identified as a contributor to de novo or acquired resistance to epidermal growth factor receptor(EGFR) inhibitors in a small subset...Human epidermal growth factor receptor 2(HER2) signaling pathway activation has been identified as a contributor to de novo or acquired resistance to epidermal growth factor receptor(EGFR) inhibitors in a small subset of patients with metastatic colorectal cancer(mCRC). Dual anti-HER2-targeted treatment exhibits strong antitumor activity in preclinical models of HER2-positive mCRC, supporting its testing in clinical trials. The HERACLES trial at four Italian academic cancer centers has confirmed the effectiveness of dual blockage of HER2 with trastuzumab plus lapatinib in patients with heavily pretreated HER2-positive mCRC, refractory to the anti-EGFR antibodies cetuximab or panitumumab. Here, we reviewed the preclinical studies exploring the role of HER2 signaling in the development of anti-EGFR therapy resistance and discussed the status of clinical trials assessing the activity of HER2 inhibitors in this setting.展开更多
The effect of steam dilution on the formation of coke and minor products in 2-methylpenatne cracking on ultra stable HY at 673 K has been studied. The results show that steam dilution suppresses the formation of coke ...The effect of steam dilution on the formation of coke and minor products in 2-methylpenatne cracking on ultra stable HY at 673 K has been studied. The results show that steam dilution suppresses the formation of coke and minor aromatic products, but enhances the H/C atomic ratio of coke and the production of di-olefins. This and other evidences suggest that steam dilution enhances the desorption of coke precursors, diolefinic ions and cyclic ions, by inhibiting the further pathological reactions to produce aromatics and polyaromatics. These insights into the chemistry underlying coke formation in hydrocarbon cracking on solid acid catalysts can potentially be applied to the development of additives which inhibit coke formation and control catalyst deactivation.展开更多
New fluorine substituted heterobicyclic nitrogen system as imidozolopyrimidines (2,3), pyrimido- 1,2,4-triazinones (4-7), 1,2,4-triazinyl-1,2,4-triazine (12-16), 1,2,4-triazinyl-1,2,4-triazinones (14-17) and substitut...New fluorine substituted heterobicyclic nitrogen system as imidozolopyrimidines (2,3), pyrimido- 1,2,4-triazinones (4-7), 1,2,4-triazinyl-1,2,4-triazine (12-16), 1,2,4-triazinyl-1,2,4-triazinones (14-17) and substituted thiobarbituric acids (19-20), have been synthesized using the reaction of 3- amino-5,6-di (4'-fluorophenyl)-1,2,4-triazine (1) with α,β–bifunctional compounds. Structures of the title compounds were characterized by UV, IR, 1H/13C-NMR and mass spectrometric method. The studied compounds were tested for CDK2 inhibiting activity in DNA damage, as well as in vitro anti-tumor activity.展开更多
Objective:To study the effects of TSH inhibition after total thyroidectomy on Tg, VEGF, TSGF, CD44V6, sIL-2R and T lymphocyte subsets in patients with differentiated thyroid carcinoma (DTC).Methods: A total of 100 pat...Objective:To study the effects of TSH inhibition after total thyroidectomy on Tg, VEGF, TSGF, CD44V6, sIL-2R and T lymphocyte subsets in patients with differentiated thyroid carcinoma (DTC).Methods: A total of 100 patients with DTC in our hospital from January 2014 to January 2017 were enrolled in this study. The subjects were divided into the control group (n=50) and the treatment group (n=50) randomly. The control group was treated with thyroid hormone replacement therapy, the treatment group was treated with levothyroxine sodium oral therapy, the two groups were treated for 1 week. The serum Tg, VEGF, TSGF, CD44V6, sIL-2R and peripheral blood CD3+, CD4+, CD8+ of the two groups before and after treatment were compared.Results:There were no significant differences of the serum Tg, VEGF, TSGF, CD44V6, sIL-2R of the two groups before treatment. The serum Tg, VEGF, TSGF, CD44V6, sIL-2R of the two groups after treatment were significantly lower than before treatment, and that of the treatment group after treatment were significantly lower than the control group. There were no significantly differences of the peripheral blood CD3+, CD4+, CD8+ of the two groups before treatment. The peripheral blood CD3+, CD4+ of the two groups after treatment were significantly higher than before treatment, the peripheral blood CD8+ of the two groups after treatment were significantly lower than before treatment, and that of the treatment group after treatment were significantly better than the control group.Conclusion:TSH inhibition after total thyroidectomy for patients with DTC can reduce the serum Tg, VEGF, TSGF, CD44V6, sIL-2R levels, improve the cellular immunity function, and it was worthy clinical application.展开更多
It is highly desirable to enhance the long-term stability of perovskite solar cells(PSCs)so that this class of photovoltaic cells can be effectively used for the commercialization purposes.In this contribution,attempt...It is highly desirable to enhance the long-term stability of perovskite solar cells(PSCs)so that this class of photovoltaic cells can be effectively used for the commercialization purposes.In this contribution,attempts have been made to use the two-step sequential method to dope EuBr_(2)into FAMAPbI_(3)perovskite to promote the stability.It is shown that the device durability at 85℃in air with RH of 20%-40%is improved substantially,and simultaneously the champion device efficiency of 23.04%is achieved.The enhancement in stability is attributed to two points:(ⅰ)EuBr_(2)doping effectively inhibits the decomposition andα-δphase transition of perovskite under ambient environment,and(ⅱ)EuBr_(2)aggregates in the oxidized format of Eu(BrO_(3))_(3)at perovskite grain boundaries and surface,hampering humidity erosion and mitigates degradation through coordination with H_(2)O.展开更多
Objective:To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum.Methods:The effects of oral treatment with hydro-ethanolic extract(125,250 and 500 mg/kg)of the stem bark of Chrysophyl...Objective:To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum.Methods:The effects of oral treatment with hydro-ethanolic extract(125,250 and 500 mg/kg)of the stem bark of Chrysophyllum albidum and glibenclamide for 21 d on glucose level,serum enzyme markers for liver function,lipid profile,total protein,serum urea,serum creatinine,and body weight were evaluated in experimental diabetic rats administered with 45 mg/kg of streptozotocin.In vitro assays including glucose uptake in C2 C12 cells and 3 T3-L1 adipose tissues,α-glucosidase andα-amylase inhibition were employed to evaluate the possible mechanism of hypoglycemic action of the extract.DPPH and nitric oxide radical antioxidant activity of the extract was also measured.Results:The increased levels of blood glucose,triglycerides,lowdensity lipoprotein,total cholesterol,serum aspartate,and alanine transaminases,creatinine,and urea in the diabetic animals were reduced significantly(P<0.01)after treatment with Chrysophyllum albidum extract.The decreased total protein and high-density lipoprotein concentrations were normalized after treatment.In addition,the extract significantly(P<0.01)increased the transport of glucose in 3 T3-L1 cells and C2 C12 myotubes and exhibited considerable potential to inhibitα-amylase andα-glucosidase.It also demonstrated potent antioxidant action by scavenging considerably DPPH and nitric oxide radicals.Conclusions:Chrysophyllum albidum stem bark extract exhibits considerable antidiabetic effect by stimulating glucose uptake and utilization in C2 C12 myotubes and 3 T3-L1 adipocytes as well as inhibiting the activities ofα-amylase andα-glucosidase.展开更多
OBJECTIVE Prepulse inhibition(PPI)of the acoustic startle response provides a measure of sensorimotor gating system mecha⁃nisms,which is known to be impaired in schizo⁃phrenia patients.We assessed the effects of the 5...OBJECTIVE Prepulse inhibition(PPI)of the acoustic startle response provides a measure of sensorimotor gating system mecha⁃nisms,which is known to be impaired in schizo⁃phrenia patients.We assessed the effects of the 5-HT2A/2C receptor agonist(±)2,5-dimethoxy-4-methylamphetamine(DOM),the NMDA receptor antagonist ketamine,the dopamine receptor ago⁃nist methamphetamine(Meth)on PPI and the startle magnitude in SD rats.METHODS AND RESULTS Systemic administration of the three compounds all dose-dependently reduced PPI.However,as far as startle magnitude,only DOM at the doses of 3 mg·kg-1 reduced that,while both ketamine and Meth did not change the startle magnitudes.Furthermore,to determine whether 5-HT2A receptor mediate this effect,the non-spe⁃cific 5-HT2 receptor antagonist cyproheptadine,specific 5-HT2A receptor antagonist ketanserin and specific 5-HT2C receptor antagonist SB242084 were tested.Cyproheptadine,ketan⁃serin and SB242084 did not alter startle ampli⁃tude by themselves in SD rats and only ketanserin slightly increased PPI at higher dose(3 mg·kg-1).PPI impairment induced by DOM was restored by pretreatment of cyproheptadine(1 mg·kg-1)and ketanserin(1 mg·kg-1),while not by pretreat⁃ment of SB242084(1 mg·kg-1).Damage of PPI induced by ketamine and Meth was not reversed by cyproheptadine(1 and 5 mg·kg-1).CONCLU⁃SION The receptor mechanisms underlying the disruption of PPI caused by DOM,ketamine and Meth were different from each other,at least 5-HT2A receptor was not the junction receptor for which the three chemicals acted.展开更多
基金Supported by Research Grants ETT022/2006 and ETT151/2009 from the Ministry of Health,HungaryTáMOP-4.2.1/B-09/1/KONV-2010-0005 from Creating the Center of Excellence at the University of Szegedsupported by the European Union and cofinanced by the European Regional Fund
文摘AIM:The effects of vitamin D3 have been investigated on various tumors, including colorectal cancer (CRC). 25-hydroxyvitamin-D3-24-hydroxylase (CYP24A1), the enzyme that inactivates the active vitamin D3 metabolite 1,25-dihydroxyvitamin D3 (1,25-D3), is considered to be the main enzyme determining the biological halflife of 1,25-D3. During colorectal carcinogenesis, the expression and concentration of CYP24A1 increases significantly, suggesting that this phenomenon could be responsible for the proposed efficacy of 1,25-D3 in the treatment of CRC. The aim of this study was to investigate the anti-tumor effects of vitamin D3 on the human CRC cell line Caco-2 after inhibition of the cytochrome P450 component of CYP24A1 activity. METHODS:We examined the expression of CYP24A1 mRNA and the effects of 1,25-D3 on the cell line Caco-2 after inhibition of CYP24A1. Cell viability and proliferation were determined by means of sulforhodamine-B staining and bromodeoxyuridine incorporation, respectively, while cytotoxicity was estimated via the lactate dehydrogenase content of the cell culture supernatant. CYP24A1 expression was measured by realtime reverse transcription polymerase chain reaction. A number of tetralone compounds were synthesized to investigate their CP24A1 inhibitory activity. RESULTS:In response to 1,25-D3, CYP24A1 mRNA expression was enhanced significantly, in a time- and dose-dependent manner. Caco-2 cell viability and proliferation were not influenced by the administration of 1,25-D3 alone, but were markedly reduced by coadministration of 1,25-D3 and KD-35, a CYP24A1-inhibiting tetralone. Our data suggest that the mechanism of action of co-administered KD-35 and 1,25-D3 does not involve a direct cytotoxic effect, but rather the inhibition of cell proliferation. CONCLUSION:These findings demonstrate that the selective inhibition of CYP24A1 by compounds such as KD-35 may be a new approach for enhancement of the anti-tumor effect of 1,25-D3 on CRC.
基金the National High Technology Research and Development Program of China (Grant No.2009AA063003)the National Nature Science Foundation of China (No.20677039) for financial support
文摘The inhibition effect of tert-butyl alcohol(TBA), identified as the·OH radical inhibitor, on the TiO_2 nano assays(TNA) photoelectrocatalytic oxidation of different organics such as glucose and phthalate was reported. The adsorption performance of these organics on the TNA photoelectrode was investigated by using the instantaneous photocurrent value, and the degradation property was examined by using the exhausted reaction. The results showed that glucose exhibited the poor adsorption and easy degradation performance, phthalate showed the strong adsorption and harddegradation, but TBA showed the weak adsorption and was the most difficult to be degraded. The degradation of both glucose and phthalate could be inhibited evidently by TBA. But the effect on glucose was more obvious. The different inhibition effects of TBA on different organics could be attributed to the differences in the adsorption and the degradation property. For instance, phthalate of the strong adsorption property could avoid from the capture of·OH radicals by TBA in TNA photoelectrocatalytic process.
文摘AIM: To investigate the effects of lentivirus vector mediated short hairpin RNA interference targeting methionine adenosyltransferase 2β gene (LV-shMAT2B) on hepatocelluar carcinoma (HCC) cells. METHODS: We constructed four plasmids of RNA interference targeting the MAT2B gene. After LV-shMAT2B was transfected with L-02 cells and two kinds of HCC cells, cell viability and proliferation were measured with MTT and [3H]thymidine assays respectively. Flow cytometry was used to assess cell apoptosis. The level of S-adenosyl methionine (SAMe) in HepG2 cells was evaluated. The expressions of cyclin D1, cyclin D2, bcl-xL and bcl-xS were detected with western blot. RESULTS: We constructed LV-shMAT2B successfully. LV-shMAT2B was safe for human normal liver cells. LV-shMAT2B caused dramatic reduction in proliferation compared with controls in HCC cells Bel-7402 (P = 0.054) and HepG2 (P = 0.031). Flow cytometry analysis showed that cell apoptosis caused by LV-shMAT2B was greater in HCC cells Bel-7402 and HepG2 than in control induced by scrambled siRNA (P = 0.047), but apoptosis rates in L-02 induced by LV-shMAT2B and scrambled siRNA respectively had no significant difference. Moreover, LV-shMAT2B significantly suppressed expression of MAT2B leading to growth-inhibition effect on HCC cells by down-regulating cyclin D1. Apoptosis induced by LV-shMAT2B was involved indown-regulating bcl-xL and up-regulating bcl-xS. CONCLUSION: LV-shMAT2B can induce cell apoptosis and growth-inhibition in HCC cells. MAT2B may be a therapy target in HCC in the future.
文摘Human epidermal growth factor receptor 2(HER2) signaling pathway activation has been identified as a contributor to de novo or acquired resistance to epidermal growth factor receptor(EGFR) inhibitors in a small subset of patients with metastatic colorectal cancer(mCRC). Dual anti-HER2-targeted treatment exhibits strong antitumor activity in preclinical models of HER2-positive mCRC, supporting its testing in clinical trials. The HERACLES trial at four Italian academic cancer centers has confirmed the effectiveness of dual blockage of HER2 with trastuzumab plus lapatinib in patients with heavily pretreated HER2-positive mCRC, refractory to the anti-EGFR antibodies cetuximab or panitumumab. Here, we reviewed the preclinical studies exploring the role of HER2 signaling in the development of anti-EGFR therapy resistance and discussed the status of clinical trials assessing the activity of HER2 inhibitors in this setting.
基金Supported by the National Natural Science Foundation of China （20673099） and Scientific Research Fund of Ningbo Cit （2006A610065）.
文摘The effect of steam dilution on the formation of coke and minor products in 2-methylpenatne cracking on ultra stable HY at 673 K has been studied. The results show that steam dilution suppresses the formation of coke and minor aromatic products, but enhances the H/C atomic ratio of coke and the production of di-olefins. This and other evidences suggest that steam dilution enhances the desorption of coke precursors, diolefinic ions and cyclic ions, by inhibiting the further pathological reactions to produce aromatics and polyaromatics. These insights into the chemistry underlying coke formation in hydrocarbon cracking on solid acid catalysts can potentially be applied to the development of additives which inhibit coke formation and control catalyst deactivation.
文摘New fluorine substituted heterobicyclic nitrogen system as imidozolopyrimidines (2,3), pyrimido- 1,2,4-triazinones (4-7), 1,2,4-triazinyl-1,2,4-triazine (12-16), 1,2,4-triazinyl-1,2,4-triazinones (14-17) and substituted thiobarbituric acids (19-20), have been synthesized using the reaction of 3- amino-5,6-di (4'-fluorophenyl)-1,2,4-triazine (1) with α,β–bifunctional compounds. Structures of the title compounds were characterized by UV, IR, 1H/13C-NMR and mass spectrometric method. The studied compounds were tested for CDK2 inhibiting activity in DNA damage, as well as in vitro anti-tumor activity.
文摘Objective:To study the effects of TSH inhibition after total thyroidectomy on Tg, VEGF, TSGF, CD44V6, sIL-2R and T lymphocyte subsets in patients with differentiated thyroid carcinoma (DTC).Methods: A total of 100 patients with DTC in our hospital from January 2014 to January 2017 were enrolled in this study. The subjects were divided into the control group (n=50) and the treatment group (n=50) randomly. The control group was treated with thyroid hormone replacement therapy, the treatment group was treated with levothyroxine sodium oral therapy, the two groups were treated for 1 week. The serum Tg, VEGF, TSGF, CD44V6, sIL-2R and peripheral blood CD3+, CD4+, CD8+ of the two groups before and after treatment were compared.Results:There were no significant differences of the serum Tg, VEGF, TSGF, CD44V6, sIL-2R of the two groups before treatment. The serum Tg, VEGF, TSGF, CD44V6, sIL-2R of the two groups after treatment were significantly lower than before treatment, and that of the treatment group after treatment were significantly lower than the control group. There were no significantly differences of the peripheral blood CD3+, CD4+, CD8+ of the two groups before treatment. The peripheral blood CD3+, CD4+ of the two groups after treatment were significantly higher than before treatment, the peripheral blood CD8+ of the two groups after treatment were significantly lower than before treatment, and that of the treatment group after treatment were significantly better than the control group.Conclusion:TSH inhibition after total thyroidectomy for patients with DTC can reduce the serum Tg, VEGF, TSGF, CD44V6, sIL-2R levels, improve the cellular immunity function, and it was worthy clinical application.
基金Project supported by the Fundamental Research Program of Shanxi Province,China (Grant No.20210302124228)the National Key Research and Development Program of China (Grant No.2022YFB4200203)+1 种基金the Key Project of Natural Science Foundation of Tianjin (Grant No.22JCZDJC00120)the 111 Project (Grant No.B16027)。
文摘It is highly desirable to enhance the long-term stability of perovskite solar cells(PSCs)so that this class of photovoltaic cells can be effectively used for the commercialization purposes.In this contribution,attempts have been made to use the two-step sequential method to dope EuBr_(2)into FAMAPbI_(3)perovskite to promote the stability.It is shown that the device durability at 85℃in air with RH of 20%-40%is improved substantially,and simultaneously the champion device efficiency of 23.04%is achieved.The enhancement in stability is attributed to two points:(ⅰ)EuBr_(2)doping effectively inhibits the decomposition andα-δphase transition of perovskite under ambient environment,and(ⅱ)EuBr_(2)aggregates in the oxidized format of Eu(BrO_(3))_(3)at perovskite grain boundaries and surface,hampering humidity erosion and mitigates degradation through coordination with H_(2)O.
基金supported by some funds from KNUST Research Fund(KReF)
文摘Objective:To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum.Methods:The effects of oral treatment with hydro-ethanolic extract(125,250 and 500 mg/kg)of the stem bark of Chrysophyllum albidum and glibenclamide for 21 d on glucose level,serum enzyme markers for liver function,lipid profile,total protein,serum urea,serum creatinine,and body weight were evaluated in experimental diabetic rats administered with 45 mg/kg of streptozotocin.In vitro assays including glucose uptake in C2 C12 cells and 3 T3-L1 adipose tissues,α-glucosidase andα-amylase inhibition were employed to evaluate the possible mechanism of hypoglycemic action of the extract.DPPH and nitric oxide radical antioxidant activity of the extract was also measured.Results:The increased levels of blood glucose,triglycerides,lowdensity lipoprotein,total cholesterol,serum aspartate,and alanine transaminases,creatinine,and urea in the diabetic animals were reduced significantly(P<0.01)after treatment with Chrysophyllum albidum extract.The decreased total protein and high-density lipoprotein concentrations were normalized after treatment.In addition,the extract significantly(P<0.01)increased the transport of glucose in 3 T3-L1 cells and C2 C12 myotubes and exhibited considerable potential to inhibitα-amylase andα-glucosidase.It also demonstrated potent antioxidant action by scavenging considerably DPPH and nitric oxide radicals.Conclusions:Chrysophyllum albidum stem bark extract exhibits considerable antidiabetic effect by stimulating glucose uptake and utilization in C2 C12 myotubes and 3 T3-L1 adipocytes as well as inhibiting the activities ofα-amylase andα-glucosidase.
文摘OBJECTIVE Prepulse inhibition(PPI)of the acoustic startle response provides a measure of sensorimotor gating system mecha⁃nisms,which is known to be impaired in schizo⁃phrenia patients.We assessed the effects of the 5-HT2A/2C receptor agonist(±)2,5-dimethoxy-4-methylamphetamine(DOM),the NMDA receptor antagonist ketamine,the dopamine receptor ago⁃nist methamphetamine(Meth)on PPI and the startle magnitude in SD rats.METHODS AND RESULTS Systemic administration of the three compounds all dose-dependently reduced PPI.However,as far as startle magnitude,only DOM at the doses of 3 mg·kg-1 reduced that,while both ketamine and Meth did not change the startle magnitudes.Furthermore,to determine whether 5-HT2A receptor mediate this effect,the non-spe⁃cific 5-HT2 receptor antagonist cyproheptadine,specific 5-HT2A receptor antagonist ketanserin and specific 5-HT2C receptor antagonist SB242084 were tested.Cyproheptadine,ketan⁃serin and SB242084 did not alter startle ampli⁃tude by themselves in SD rats and only ketanserin slightly increased PPI at higher dose(3 mg·kg-1).PPI impairment induced by DOM was restored by pretreatment of cyproheptadine(1 mg·kg-1)and ketanserin(1 mg·kg-1),while not by pretreat⁃ment of SB242084(1 mg·kg-1).Damage of PPI induced by ketamine and Meth was not reversed by cyproheptadine(1 and 5 mg·kg-1).CONCLU⁃SION The receptor mechanisms underlying the disruption of PPI caused by DOM,ketamine and Meth were different from each other,at least 5-HT2A receptor was not the junction receptor for which the three chemicals acted.
