Gastric ulcer is a very common gastrointestinal disorder affecting a large number of people worldwide.It arises due to an imbalance between aggressive(acid,pepsin and Helicobacter pylori infection)and protective(mucin...Gastric ulcer is a very common gastrointestinal disorder affecting a large number of people worldwide.It arises due to an imbalance between aggressive(acid,pepsin and Helicobacter pylori infection)and protective(mucin secretion,prostaglandin,epidermal growth factors and bicarbonate)factors in the stomach.In this study,the gastroprotective activity has been investigated of the active constituents from Xylocarpus molluccensis.Antiulcer activity of xyloccensins X?Y was investigated and found to be active in various ulcer models in Sprague–Dawley(SD)rats.To understand the mechanism of action of active constituent of natural products,the effects of the compounds on antisecretory and cytoprotective activities were studied.Air dried fruits were extracted with ethanol and fractionated into four fractions.Xyloccensins X?Y were isolated from the active fraction and was tested against different ulcer models.Xyloccensins X?Y were found to possess anti-ulcerogenic activity.The antiulcer activity might be due to its anti-secretory activity and subsequent strengthening of the defensive mechanism.The present study has helped us in identifying a new lead in the form of xyloccensins that could be exploited in the treatment of gastric ulcer disease.展开更多
CDRI compound no. 99/411 is a potent 1,2,4-trioxane antimalarial candidate drug under development at our Institute. An HPLC method for determination of CDRI 99/411 with its starting material and intermediates has been...CDRI compound no. 99/411 is a potent 1,2,4-trioxane antimalarial candidate drug under development at our Institute. An HPLC method for determination of CDRI 99/411 with its starting material and intermediates has been developed and validated for in process quality control and stability studies. The analytical performance parameters such as linearity, precision, accuracy, specificity, limit of detection （LOD） and lower limit of quantification （LLOQ） were determined according to International Conference on Harmonization ICH Q2（R1） guidelines. HPLC separation was achieved on a RP-select B Lichrosphere~ column （250 mm x 4 ram, 5 lam, Merck） using water containing 0.1% glacial acetic acid and acetonitrile as the mobile phase in a gradient elution. The eluents were monitored by a photo diode array detector at 245 and 275 nm. Based on signal to noise ratio of 3 and 10 the LOD of CDRI 99/411 was 0.55 μg/mL, while the LLOQ was 1.05 μg/mL. The calibration curves were linear in the range of 1.05- 68 μg/mL. Precision of the method was determined by inter- and intra-assay variations within the acceptable range.展开更多
文摘Gastric ulcer is a very common gastrointestinal disorder affecting a large number of people worldwide.It arises due to an imbalance between aggressive(acid,pepsin and Helicobacter pylori infection)and protective(mucin secretion,prostaglandin,epidermal growth factors and bicarbonate)factors in the stomach.In this study,the gastroprotective activity has been investigated of the active constituents from Xylocarpus molluccensis.Antiulcer activity of xyloccensins X?Y was investigated and found to be active in various ulcer models in Sprague–Dawley(SD)rats.To understand the mechanism of action of active constituent of natural products,the effects of the compounds on antisecretory and cytoprotective activities were studied.Air dried fruits were extracted with ethanol and fractionated into four fractions.Xyloccensins X?Y were isolated from the active fraction and was tested against different ulcer models.Xyloccensins X?Y were found to possess anti-ulcerogenic activity.The antiulcer activity might be due to its anti-secretory activity and subsequent strengthening of the defensive mechanism.The present study has helped us in identifying a new lead in the form of xyloccensins that could be exploited in the treatment of gastric ulcer disease.
基金Financial support to Shakti Deep Pachauri and Kiran Khandelwal from the Council of Scientifc and Industrial Research (CSIR)New DelhiIndiais gratefully acknowledged
文摘CDRI compound no. 99/411 is a potent 1,2,4-trioxane antimalarial candidate drug under development at our Institute. An HPLC method for determination of CDRI 99/411 with its starting material and intermediates has been developed and validated for in process quality control and stability studies. The analytical performance parameters such as linearity, precision, accuracy, specificity, limit of detection （LOD） and lower limit of quantification （LLOQ） were determined according to International Conference on Harmonization ICH Q2（R1） guidelines. HPLC separation was achieved on a RP-select B Lichrosphere~ column （250 mm x 4 ram, 5 lam, Merck） using water containing 0.1% glacial acetic acid and acetonitrile as the mobile phase in a gradient elution. The eluents were monitored by a photo diode array detector at 245 and 275 nm. Based on signal to noise ratio of 3 and 10 the LOD of CDRI 99/411 was 0.55 μg/mL, while the LLOQ was 1.05 μg/mL. The calibration curves were linear in the range of 1.05- 68 μg/mL. Precision of the method was determined by inter- and intra-assay variations within the acceptable range.
