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β‐Cyclodextrin Inclusion Complexation by Milling β -环糊精包合物的铣削络合
Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735412
N. A. Adhage, P. Vavia
{"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":null,"pages":null},"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}
引用次数: 22
Aqueous Extract from Rhizoma Smilacis Glabrae Alleviates Immunological Liver Damage by Selectively Facilitating the Dysfunction of Liver‐infiltrating Lymphocytes 菝葜水提物通过选择性促进肝浸润淋巴细胞功能障碍减轻免疫性肝损伤
Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735458
Qiang Xu, Jingsong Cao, Feihua Wu, Ting Chen, Jieyun Jiang
{"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":null,"pages":null},"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}
引用次数: 2
Thermochemotherapy: Synergism between hyperthermia and liposomal bleomycin in mice bearing melanoma B16F1 热化疗:热疗和博来霉素脂质体对黑色素瘤B16F1小鼠的协同作用
Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735421
S. B. Tiwari, V. Udupa, S. Rao, U. Devi
{"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":null,"pages":null},"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}
引用次数: 5
Role of Berberine as an Adjuvant Response Modifier During Tumour Therapy in Mice 小檗碱在小鼠肿瘤治疗中的辅助反应调节剂作用
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734415
K. Anis, G. Kuttan,, R. Kuttan
{"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":null,"pages":null},"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}
引用次数: 36
Synthesis of Mono- and Bis-substituted Anthraquinones as Inhibitors of Human Telomerase 单和双取代蒽醌类人端粒酶抑制剂的合成
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734361
V. Gibson, Rosaleen J. Anderson, T. C. Jenkins, D. Cairns
{"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":null,"pages":null},"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}
引用次数: 3
Effects of Guanfu Base G on the Kinetics of Use‐dependent Block in Maximum Upstroke Velocity in Guinea‐pig Isolated Papillary Muscles 冠复碱G对豚鼠离体乳头肌最大上冲速度使用依赖性阻滞动力学的影响
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734398
Zhang Luyong, Jiao Huifang, Wang Qiu-juan, Liu Jinhan
{"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":null,"pages":null},"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}
引用次数: 0
Is Precipitation with Sulphosalicylic Acid Valid for Obtaining Free Valproic Acid and Phenytoin 磺胺水杨酸沉淀法可以得到游离丙戊酸和苯妥英吗
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734343
A. Sánchez, R. García, J. A. Duran, J. A. Abadín
{"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":null,"pages":null},"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}
引用次数: 0
Hypolipidaemic and antioxidant activity of diallyl disulphide in rats 二硫二烯丙基对大鼠的降血脂和抗氧化活性
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734406
J. Dhuley, S. Naik, S. Rele, A. Banerji
{"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":null,"pages":null},"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}
引用次数: 22
Role of Potassium Channels in the GABA Inhibitory Action on the Cholinergic Response to Electrical Field Stimulation in Guinea-pig Ileum 钾通道在GABA抑制豚鼠回肠电场刺激胆碱能反应中的作用
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734389
B. Baragatti, V. Calderone, M. Breschi, E. Martinotti
{"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":null,"pages":null},"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}
引用次数: 1
Effects of Icariside II from Epimedium koreanum on Tumour Cell Lines In‐vitro 韩国淫羊藿Icariside II对肿瘤细胞的体外作用
Pharmacy and Pharmacology Communications Pub Date : 1999-12-01 DOI: 10.1211/146080899128734424
Xin Lin, Wen‐kui Li, P. Xiao
{"title":"Effects of Icariside II from Epimedium koreanum on Tumour Cell Lines In‐vitro","authors":"Xin Lin, Wen‐kui Li, P. Xiao","doi":"10.1211/146080899128734424","DOIUrl":"https://doi.org/10.1211/146080899128734424","url":null,"abstract":"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. \u0000 \u0000 \u0000 \u0000Icariside II was cytotoxic to all cell lines tested. The inhibition (53–88%) observed was at 10−5M. \u0000 \u0000 \u0000 \u0000The results suggest that icariside II may be a potentially useful antitumour agent.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1999-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87418127","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}
引用次数: 6
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