Pub Date : 2000-01-01DOI: 10.1211/146080800128735412
N. A. Adhage, P. Vavia
The study involved the complexation of nimesulide with β-cyclodextrin (β-CyD) by milling. Nimesulide and β-CyD were mixed in the ratios 1:1, 1:2, 1:3 and 1:4 by weight. Each mixture was ground in a ball mill at 50 rev min−1 for 6, 12, 24 and 48 h. The samples were subjected to dissolution studies, differential scanning calorimetry and X-ray diffraction studies and were also evaluated for anti-inflammatory and analgesic activity. The sample containing the 1:4 ratio milled for 6 and 12 h exhibited a lower T90 value compared with nimesulide, ball-milled nimesulide and the freeze-dried complex. Increasing the milling time to 24 or 48 h further increased the T90 (time required for 90% of the drug to dissolve) value. The dissolution rate constant for nimesulide increased with an increase in β-CyD concentration. Milled samples (1:4 ratio milled for 6 and 12 h) also showed significant anti-inflammatory and analgesic activity. The results showed an improved rate of nimesulide absorption and hence better bioavailability by inclusion complex formation of the drug with β-CyD.
{"title":"β‐Cyclodextrin Inclusion Complexation by Milling","authors":"N. A. Adhage, P. Vavia","doi":"10.1211/146080800128735412","DOIUrl":"https://doi.org/10.1211/146080800128735412","url":null,"abstract":"The study involved the complexation of nimesulide with β-cyclodextrin (β-CyD) by milling. Nimesulide and β-CyD were mixed in the ratios 1:1, 1:2, 1:3 and 1:4 by weight. Each mixture was ground in a ball mill at 50 rev min−1 for 6, 12, 24 and 48 h. The samples were subjected to dissolution studies, differential scanning calorimetry and X-ray diffraction studies and were also evaluated for anti-inflammatory and analgesic activity. The sample containing the 1:4 ratio milled for 6 and 12 h exhibited a lower T90 value compared with nimesulide, ball-milled nimesulide and the freeze-dried complex. Increasing the milling time to 24 or 48 h further increased the T90 (time required for 90% of the drug to dissolve) value. The dissolution rate constant for nimesulide increased with an increase in β-CyD concentration. Milled samples (1:4 ratio milled for 6 and 12 h) also showed significant anti-inflammatory and analgesic activity. The results showed an improved rate of nimesulide absorption and hence better bioavailability by inclusion complex formation of the drug with β-CyD.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"57 1","pages":"13-17"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87071999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The effect of an aqueous extract from Rhizoma Smilacis Glabrae (RSG) on liver injury induced by delayed-type hypersensitivity to picryl chloride in mice has been studied. In in-vitro co-culture of non-parenchymal cells (NPC) and hepatocytes isolated from liver-injured mice, pretreatment of NPC, but not parenchymal hepatocytes, with the extract resulted in concentration- and time-dependent inhibition of NPC-induced hepatocyte damage. A significant reduction of in-vitro hepatotoxicity, as measured by inhibition of serum transaminase elevation, was also observed in NPC isolated from mice treated with RSG extract. RSG extract facilitated apoptosis in NPC from liver-injured mice but not in parenchymal hepatocytes. The results suggest that RSG extract protects against liver injury by selective induction of apoptosis in liver-infiltrating cells, mainly activated T lymphocytes. Such characteristics will help provide a novel strategy not only for treatment of liver diseases, but also for regulation of the immune response.
{"title":"Aqueous Extract from Rhizoma Smilacis Glabrae Alleviates Immunological Liver Damage by Selectively Facilitating the Dysfunction of Liver‐infiltrating Lymphocytes","authors":"Qiang Xu, Jingsong Cao, Feihua Wu, Ting Chen, Jieyun Jiang","doi":"10.1211/146080800128735458","DOIUrl":"https://doi.org/10.1211/146080800128735458","url":null,"abstract":"The effect of an aqueous extract from Rhizoma Smilacis Glabrae (RSG) on liver injury induced by delayed-type hypersensitivity to picryl chloride in mice has been studied. In in-vitro co-culture of non-parenchymal cells (NPC) and hepatocytes isolated from liver-injured mice, pretreatment of NPC, but not parenchymal hepatocytes, with the extract resulted in concentration- and time-dependent inhibition of NPC-induced hepatocyte damage. A significant reduction of in-vitro hepatotoxicity, as measured by inhibition of serum transaminase elevation, was also observed in NPC isolated from mice treated with RSG extract. RSG extract facilitated apoptosis in NPC from liver-injured mice but not in parenchymal hepatocytes. The results suggest that RSG extract protects against liver injury by selective induction of apoptosis in liver-infiltrating cells, mainly activated T lymphocytes. Such characteristics will help provide a novel strategy not only for treatment of liver diseases, but also for regulation of the immune response.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"4 1","pages":"41-47"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83730725","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-01-01DOI: 10.1211/146080800128735421
S. B. Tiwari, V. Udupa, S. Rao, U. Devi
This study was aimed at enhancing the antitumour efficacy of bleomycin by encapsulating it in temperature-sensitive liposomes and using it in combination with localized hyperthermia of tumours for targeted delivery. Large unilammelar vesicles (LUV) made of synthetic lipids (disteroyl phosphatidylcholine and dipalmitoyl phosphatidylcholine) showing gel-to-liquid phase transition at 41°C, were used to encapsulate bleomycin. Comparison of LUV when incubated in saline at various temperatures revealed that maximum drug release (80%) occurred at 42°C compared with less than 5% release at 37°C. Better stability during storage was also observed with thermosensitive bleomycin liposomes. When administered intravenously to C57BL/6J mice bearing melanoma B16F1 tumour at 10 mg kg−1 dose, liposomal bleomycin in combination with hyperthermia (43°C, 30 min or 1 h) exhibited improved anticancer activity as evident by the enhanced volume doubling time and growth delay compared with animals treated with an equivalent dose of free bleomycin with or without hyperthermia. The results suggest that hyperthermia in combination with bleomycin encapsulated in temperature sensitive liposomes may be a useful targeted drug delivery system for more effective management of melanoma B16F1.
本研究旨在通过将博来霉素包封在温度敏感脂质体中，并与肿瘤局部热疗联合使用以靶向给药，从而提高博来霉素的抗肿瘤功效。由合成脂质(二二酰磷脂酰胆碱和双棕榈酰磷脂酰胆碱)制成的大单层囊泡(LUV)在41℃时呈现凝胶-液相转变，用于包封博来霉素。在盐水中不同温度下的LUV比较显示，42°C时药物释放最大(80%)，而37°C时药物释放小于5%。热敏性博莱霉素脂质体在贮存过程中也表现出较好的稳定性。当以10 mg kg - 1剂量静脉注射到携带黑色素瘤B16F1肿瘤的C57BL/6J小鼠时，脂质体博来霉素联合热疗(43°C, 30分钟或1小时)显示出更好的抗癌活性，与使用等量游离博来霉素治疗或不进行热疗的动物相比，体积加倍时间和生长延迟明显增加。结果表明，热疗联合包裹在温度敏感脂质体中的博来霉素可能是一种有用的靶向药物递送系统，可以更有效地治疗黑色素瘤B16F1。
{"title":"Thermochemotherapy: Synergism between hyperthermia and liposomal bleomycin in mice bearing melanoma B16F1","authors":"S. B. Tiwari, V. Udupa, S. Rao, U. Devi","doi":"10.1211/146080800128735421","DOIUrl":"https://doi.org/10.1211/146080800128735421","url":null,"abstract":"This study was aimed at enhancing the antitumour efficacy of bleomycin by encapsulating it in temperature-sensitive liposomes and using it in combination with localized hyperthermia of tumours for targeted delivery. Large unilammelar vesicles (LUV) made of synthetic lipids (disteroyl phosphatidylcholine and dipalmitoyl phosphatidylcholine) showing gel-to-liquid phase transition at 41°C, were used to encapsulate bleomycin. Comparison of LUV when incubated in saline at various temperatures revealed that maximum drug release (80%) occurred at 42°C compared with less than 5% release at 37°C. Better stability during storage was also observed with thermosensitive bleomycin liposomes. When administered intravenously to C57BL/6J mice bearing melanoma B16F1 tumour at 10 mg kg−1 dose, liposomal bleomycin in combination with hyperthermia (43°C, 30 min or 1 h) exhibited improved anticancer activity as evident by the enhanced volume doubling time and growth delay compared with animals treated with an equivalent dose of free bleomycin with or without hyperthermia. The results suggest that hyperthermia in combination with bleomycin encapsulated in temperature sensitive liposomes may be a useful targeted drug delivery system for more effective management of melanoma B16F1.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"2016 1","pages":"19-23"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87816406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734415
K. Anis, G. Kuttan,, R. Kuttan
'The cytotoxicity and antitumour activity of the isoquinoline alkaloid berberine was studied in-vitro and in-vivo. Berberine was cytotoxic to L929 cells in culture (IC50 4oPgm~-l), and to mice when given as an acute (LD50 50mgkg-', i.p) or chronic (LD50 15mgkg-' for 10 days, i.p) dosc. At ;I non-toxic concentration berberine dose-dependently inhibited the tumours induced by Dalton's lymphoma ascites tumour cells in mice. Berberine was more active when given inhapritoneally than orally. The simultaneous administration of berberine potentiated the therapeutic effects of radiation, cyclophosphomide and hyperthermia with a decrease in volume of solid tumours in mice. The results indicate the beneficial use of berberine as an adjuvant response modifier in cancer therapy.
{"title":"Role of Berberine as an Adjuvant Response Modifier During Tumour Therapy in Mice","authors":"K. Anis, G. Kuttan,, R. Kuttan","doi":"10.1211/146080899128734415","DOIUrl":"https://doi.org/10.1211/146080899128734415","url":null,"abstract":"'The cytotoxicity and antitumour activity of the isoquinoline alkaloid berberine was studied in-vitro and in-vivo. Berberine was cytotoxic to L929 cells in culture (IC50 4oPgm~-l), and to mice when given as an acute (LD50 50mgkg-', i.p) or chronic (LD50 15mgkg-' for 10 days, i.p) dosc. At ;I non-toxic concentration berberine dose-dependently inhibited the tumours induced by Dalton's lymphoma ascites tumour cells in mice. Berberine was more active when given inhapritoneally than orally. The simultaneous administration of berberine potentiated the therapeutic effects of radiation, cyclophosphomide and hyperthermia with a decrease in volume of solid tumours in mice. The results indicate the beneficial use of berberine as an adjuvant response modifier in cancer therapy.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"15 1","pages":"697-700"},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87834229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734361
V. Gibson, Rosaleen J. Anderson, T. C. Jenkins, D. Cairns
A number of anthraquinone derivatives have been synthesized in good yield and tested for their ability to inhibit the enzymes telomerase and Taq polymerase using a modified telomeric repeat amplification protocol. In addition, all the synthesized compounds were screened against a panel of ovarian carcinoma cell lines (A2780, CH1 and SKOV-3) to determine their cytotoxicity. All compounds tested inhibited telomerase at a concentration of 10 μM, but showed negligible inhibition of Taq polymerase. None of the compounds tested displayed significant general cell toxicity in ovarian cancer cell lines. The synthesized compounds are potential selective inhibitors of human telomerase.
{"title":"Synthesis of Mono- and Bis-substituted Anthraquinones as Inhibitors of Human Telomerase","authors":"V. Gibson, Rosaleen J. Anderson, T. C. Jenkins, D. Cairns","doi":"10.1211/146080899128734361","DOIUrl":"https://doi.org/10.1211/146080899128734361","url":null,"abstract":"A number of anthraquinone derivatives have been synthesized in good yield and tested for their ability to inhibit the enzymes telomerase and Taq polymerase using a modified telomeric repeat amplification protocol. In addition, all the synthesized compounds were screened against a panel of ovarian carcinoma cell lines (A2780, CH1 and SKOV-3) to determine their cytotoxicity. \u0000 \u0000 \u0000 \u0000All compounds tested inhibited telomerase at a concentration of 10 μM, but showed negligible inhibition of Taq polymerase. None of the compounds tested displayed significant general cell toxicity in ovarian cancer cell lines. \u0000 \u0000 \u0000 \u0000The synthesized compounds are potential selective inhibitors of human telomerase.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"90 1","pages":"669-671"},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81525734","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734398
Zhang Luyong, Jiao Huifang, Wang Qiu-juan, Liu Jinhan
The use-dependent block in the maximum upstroke velocity (Vmax) caused by Guanfu base G, a new diterpene alkaloid, was investigated in isolated papillary muscles of guinea-pigs. Guanfu base G (1–8 μM) produced a concentration-dependent decrease in Vmax and action potential amplitude, but had no effect on the resting potential and duration of the action potential. In the presence of Guanfu base G (4 and 8 μM), trains of stimuli at interstimulus intervals ranging from 4800 to 300 ms, led to an exponential decline in Vmax. This use-dependent block was enhanced at higher stimulation frequencies. The onset rate constants of use-dependent Vmax blocked by Guanfu base G (at interstimulus intervals of 300 ms) were 0.0748 ± 0.0046 AP−1 and 0.0767 ± 0.0041 AP−1 at 4 and 8 μM, respectively. The time constants for the recovery of Vmax from use-dependent block were 66.3 ± 6.5 and 68.5 ± 4.8 s, respectively. These findings suggest that Guanfu base G is a sodium channel-blocking drug with slow kinetics. The characteristic of a marked use-dependent Vmax block by Guanfu base G might be of benefit in the prevention and treatment of arrhythmias.
{"title":"Effects of Guanfu Base G on the Kinetics of Use‐dependent Block in Maximum Upstroke Velocity in Guinea‐pig Isolated Papillary Muscles","authors":"Zhang Luyong, Jiao Huifang, Wang Qiu-juan, Liu Jinhan","doi":"10.1211/146080899128734398","DOIUrl":"https://doi.org/10.1211/146080899128734398","url":null,"abstract":"The use-dependent block in the maximum upstroke velocity (Vmax) caused by Guanfu base G, a new diterpene alkaloid, was investigated in isolated papillary muscles of guinea-pigs. \u0000 \u0000 \u0000 \u0000Guanfu base G (1–8 μM) produced a concentration-dependent decrease in Vmax and action potential amplitude, but had no effect on the resting potential and duration of the action potential. In the presence of Guanfu base G (4 and 8 μM), trains of stimuli at interstimulus intervals ranging from 4800 to 300 ms, led to an exponential decline in Vmax. This use-dependent block was enhanced at higher stimulation frequencies. The onset rate constants of use-dependent Vmax blocked by Guanfu base G (at interstimulus intervals of 300 ms) were 0.0748 ± 0.0046 AP−1 and 0.0767 ± 0.0041 AP−1 at 4 and 8 μM, respectively. The time constants for the recovery of Vmax from use-dependent block were 66.3 ± 6.5 and 68.5 ± 4.8 s, respectively. \u0000 \u0000 \u0000 \u0000These findings suggest that Guanfu base G is a sodium channel-blocking drug with slow kinetics. The characteristic of a marked use-dependent Vmax block by Guanfu base G might be of benefit in the prevention and treatment of arrhythmias.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"49 1","pages":"683-688"},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77189787","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734343
A. Sánchez, R. García, J. A. Duran, J. A. Abadín
The aim of this study was to compare ultrafiltration with protein precipitation with sulphosalicylic acid in the separation of free and protein-bound serum phenytoin and valproic acid. Blood samples from 49 epileptic patients chronically treated with phenytoin (27) and valproic acid (22) were assayed. Free phenytoin or valproic acid were determined by fluorescent polarization immunoanalysis. The results showed that the free serum concentrations obtained by protein precipitation (24.9 ± 8.3 and 2.55 ± 1.61 mg L−1 for valproic acid and diphenylhydantoin, respectively) were almost three-fold those from ultrafiltration (7.5 ± 6.2 and 0.86 ± 0.6 mg L−1, respectively). Protein separation using sulphosalicylic acid is not a valid technique for obtaining the free serum concentration of phenytoin or valproic acid.
{"title":"Is Precipitation with Sulphosalicylic Acid Valid for Obtaining Free Valproic Acid and Phenytoin","authors":"A. Sánchez, R. García, J. A. Duran, J. A. Abadín","doi":"10.1211/146080899128734343","DOIUrl":"https://doi.org/10.1211/146080899128734343","url":null,"abstract":"The aim of this study was to compare ultrafiltration with protein precipitation with sulphosalicylic acid in the separation of free and protein-bound serum phenytoin and valproic acid. \u0000 \u0000 \u0000 \u0000Blood samples from 49 epileptic patients chronically treated with phenytoin (27) and valproic acid (22) were assayed. Free phenytoin or valproic acid were determined by fluorescent polarization immunoanalysis. The results showed that the free serum concentrations obtained by protein precipitation (24.9 ± 8.3 and 2.55 ± 1.61 mg L−1 for valproic acid and diphenylhydantoin, respectively) were almost three-fold those from ultrafiltration (7.5 ± 6.2 and 0.86 ± 0.6 mg L−1, respectively). \u0000 \u0000 \u0000 \u0000Protein separation using sulphosalicylic acid is not a valid technique for obtaining the free serum concentration of phenytoin or valproic acid.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"5 1","pages":"667-668"},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84662961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734406
J. Dhuley, S. Naik, S. Rele, A. Banerji
The efficacy of diallyl disulphide (DADS), a constituent of garlic oil, as a hypolipidaemic and antioxidant agent was evaluated in rats. In normolipidaemic rats DADS, at doses ranging from 10 to 50 mg kg−1, decreased plasma triglyceride without affecting cholesterolaemia and fast-or noradrenaline-induced lipolysis. DADS proved effective in reducing fructose-induced hypertriglyceridaemia and dietary hypercholesterolaemia in rats, in the latter model DADS significantly raised both the HDL cholesterol and the HDL/VLDL + LDL cholesterol ratio. DADS proved ineffective on triton induced hyperlipidaemia. To gain insight into the antioxidant effect of DADS, hepatic and cardiac antioxidant enzyme activity and glutathione content were studied in rats fed on a high diet and DADS. The antioxidant enzyme activity was significantly enhanced whereas glutathione content was markedly restored in rats fed on a high fat diet simultaneously with DADS. Thus, it appears that DADS exert antioxidant protection by activating the associated antioxidant enzymes.
研究了大蒜油成分二烯丙基二硫醚(DADS)在大鼠体内的降血脂和抗氧化作用。在正常脂血症大鼠中，剂量范围为10至50 mg kg - 1的DADS可降低血浆甘油三酯，而不影响胆固醇血症和快速或去甲肾上腺素诱导的脂肪分解。在大鼠模型中，DADS可有效降低果糖诱导的高甘油三酯血症和膳食性高胆固醇血症，在后者模型中，DADS可显著提高高密度脂蛋白胆固醇和HDL/VLDL + LDL胆固醇比值。DADS对triton诱导的高脂血症无效。为了深入了解DADS的抗氧化作用，研究了高饲粮和DADS喂养的大鼠肝脏和心脏抗氧化酶活性和谷胱甘肽含量。同时饲喂高脂饲料的大鼠抗氧化酶活性显著增强，谷胱甘肽含量显著恢复。因此，DADS似乎通过激活相关的抗氧化酶来发挥抗氧化保护作用。
{"title":"Hypolipidaemic and antioxidant activity of diallyl disulphide in rats","authors":"J. Dhuley, S. Naik, S. Rele, A. Banerji","doi":"10.1211/146080899128734406","DOIUrl":"https://doi.org/10.1211/146080899128734406","url":null,"abstract":"The efficacy of diallyl disulphide (DADS), a constituent of garlic oil, as a hypolipidaemic and antioxidant agent was evaluated in rats. \u0000 \u0000 \u0000 \u0000In normolipidaemic rats DADS, at doses ranging from 10 to 50 mg kg−1, decreased plasma triglyceride without affecting cholesterolaemia and fast-or noradrenaline-induced lipolysis. DADS proved effective in reducing fructose-induced hypertriglyceridaemia and dietary hypercholesterolaemia in rats, in the latter model DADS significantly raised both the HDL cholesterol and the HDL/VLDL + LDL cholesterol ratio. DADS proved ineffective on triton induced hyperlipidaemia. \u0000 \u0000 \u0000 \u0000To gain insight into the antioxidant effect of DADS, hepatic and cardiac antioxidant enzyme activity and glutathione content were studied in rats fed on a high diet and DADS. The antioxidant enzyme activity was significantly enhanced whereas glutathione content was markedly restored in rats fed on a high fat diet simultaneously with DADS. \u0000 \u0000 \u0000 \u0000Thus, it appears that DADS exert antioxidant protection by activating the associated antioxidant enzymes.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"1 1","pages":"689-696"},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87817244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734389
B. Baragatti, V. Calderone, M. Breschi, E. Martinotti
γ-Aminobutyric acid B (GABAB) receptor activation inhibits the cholinergic response to electrical field stimulation (EFS) in guinea-pig ileum. The involvement of potassium channels in this GABA inhibitory action was investigated. The modulatory effect of GABA was not modified after pre-incubation of the organ with 1 mM tetraethylammonium chloride, a non-selective potassium channel antagonist. Nevertheless, the non-selective K+ channels antagonists, 4-aminopyridine (3 mM) and quinine (200 μM), and the selective KATP channel antagonist glibenclamide (1 μM), significantly reduced the inhibitory effects of GABA. The results suggest a coupling between GABAB receptors and KATP channels in the guinea-pig ileum.
{"title":"Role of Potassium Channels in the GABA Inhibitory Action on the Cholinergic Response to Electrical Field Stimulation in Guinea-pig Ileum","authors":"B. Baragatti, V. Calderone, M. Breschi, E. Martinotti","doi":"10.1211/146080899128734389","DOIUrl":"https://doi.org/10.1211/146080899128734389","url":null,"abstract":"γ-Aminobutyric acid B (GABAB) receptor activation inhibits the cholinergic response to electrical field stimulation (EFS) in guinea-pig ileum. The involvement of potassium channels in this GABA inhibitory action was investigated. \u0000 \u0000 \u0000 \u0000The modulatory effect of GABA was not modified after pre-incubation of the organ with 1 mM tetraethylammonium chloride, a non-selective potassium channel antagonist. Nevertheless, the non-selective K+ channels antagonists, 4-aminopyridine (3 mM) and quinine (200 μM), and the selective KATP channel antagonist glibenclamide (1 μM), significantly reduced the inhibitory effects of GABA. \u0000 \u0000 \u0000 \u0000The results suggest a coupling between GABAB receptors and KATP channels in the guinea-pig ileum.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"18 1","pages":"679-681"},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75925717","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 1999-12-01DOI: 10.1211/146080899128734424
Xin Lin, Wen‐kui Li, P. Xiao
Epimedium koreanum is one of the most popular medicinal plants in China, its major constituents being 8-prenyl flavonoids. We studied the effects of one of these flavonoids, icariside II (3, 5, 7-trihydroxy-4′-methoxyflavone-3-O-α-L-rhamnopyranoside) on the invitro growth of five human tumour cell lines, human promyelocytic leukaemia HL-60, human erythroleukaemia K562, human nasopharyngeal carcinoma cell KB, macrophage of human pulmonary carcinoma cell PG and human gastric carcinoma cell BGC, using the MTT assay. Icariside II was cytotoxic to all cell lines tested. The inhibition (53–88%) observed was at 10−5M. The results suggest that icariside II may be a potentially useful antitumour agent.
韩国淫羊藿(Epimedium koreanum)是中国最受欢迎的药用植物之一，其主要成分为8-戊烯基黄酮类化合物。采用MTT法研究了其中一种黄酮类化合物红糖苷II(3,5,7 -三羟基-4′-甲氧基黄酮-3- o -α- l -鼠李糖苷)对人早幼粒细胞白血病HL-60、人红细胞白血病K562、人鼻咽癌细胞KB、人肺癌细胞PG巨噬细胞和人胃癌细胞BGC五种肿瘤细胞系体外生长的影响。Icariside II对所有细胞系均有细胞毒性。10−5M时，抑制率为53 ~ 88%。结果表明，icariside II可能是一种潜在的有用的抗肿瘤药物。
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