The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We...The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We also investigated the effect of ARG on complexation efficiency(CE) of βCD towards CFA in an aqueous medium through phase solubility behaviour according to Higuchi and Connors. Although phase solubility studies showed AL(linear) type of solubility curve in presence and absence of ARG, the CE and association constant(Ks) of βCD towards CFA were significantly promoted in presence of ARG,justifying its use as a ternary component. The solid systems of CFA with βCD were obtained by spray drying technique with or without incorporation of ARG and characterized by differential scanning calorimetry(DSC), X-ray powder diffractometry(XRPD), scanning electron microscopy(SEM), and saturation solubility and dissolution studies. The molecular modeling studies provided a better insight into geometry and inclusion mode of CFA inside βCD cavity. The solubility and dissolution rate of CFA were significantly improved upon complexation with βCD as compared to CFA alone. However, ternary system incorporated with ARG performed better than binary system in physicochemical evaluation. In conclusion, ARG could be exploited as a ternary component to improve the physicochemical properties of CFA via βCD complexation.展开更多
Objective:To evaluate the anti-oxidani and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions.Methods:In vitro DPPH radical scavenging activity and lipoxygenase（LOX）...Objective:To evaluate the anti-oxidani and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions.Methods:In vitro DPPH radical scavenging activity and lipoxygenase（LOX） inhibition assays were used to evaluate the anti-oxidant and anti-inflammatory activities respectively.Methanolic extract（MEMI）,successive water extract （SWMI） and ethyl acetate fraction（EMEMI）,n-butanol fraction（BMEMI） and water soluble fraction （WMEMI） of methanolic extract were evaluated along with respective reference standards. Results:In in ritro DPPH radical scavenging activity,the MEMI,EMEMI and BMEMI have offered significant antioxidant activity with IC<sub>50</sub> values of 13.37.3.55 and 14.19μig/mL respectively.Gallic acid,a reference standard showed significant antioxidant activity with IC? value of 1.88 and found to be more potent compared to all the extracts and fractions.In m vitro LOX inhibition assay,the MEMI,EMEMI and BMEMI have showed significant inhibition of LOX enzyme activity with IC<sub>50</sub> values of 96.71.63.21 and 107.44μg/mL respectively.While,reference drug Indometlhacin also offered significant inhibtion against LOX enzyme activity with IC<sub>50</sub> of 57.75.Furthermore,MEMI was found to more potent than SWMI and among the fractions EMEMI was found to possess more potent antioxidant and anti-inflammatory activity.Conclusions:These findings suggest that the MEMI and F.MEMT possess potent anti-oxidani and anti-inflammatory activities in in vitro conditions.展开更多
Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination.Niranthin is a lignan isolated from various Phyllanthus sources.The literature ...Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination.Niranthin is a lignan isolated from various Phyllanthus sources.The literature survey on niranthin highlights wide ranges of the therapeutic potentials.In a present study,based on our previous investigations,we evaluated pure,isolated and characterized niranthin as an anxiolytic agent.The niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole]was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test(EPM)and Light&Dark Exploration test(L&D).GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM task.Molecular docking simulation studies(pdb id:4COF)carried out by Vlife QSAR software showed that niranthin(docking score:−62.1714 kcal/mol)have shown comparatively best docking score compared to the standard drug Diazepam(docking score:−63.1568 kcal/mol).To conclude,Niranthin has probable potential in the management of anxiety disorder.Our in-silico and in-vivo analysis(indirectly)indicated the plausible role of GABA mediation for anxiolytic activity.Although,these studies are preliminary,future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.展开更多
The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition...The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition for predefined particle size of sodium fluoride. The sodium fluoride is mainly used in dental preparation for delivering the fluoride ion to the tooth enamel for that nano-particle size is required. Nowadays the milling process is used to reduce the particle size. But that process has some limitations due to crystalline nature of sodium fluoride;for overcoming those limitations, lyophilization method is used. A 4<sup>3</sup> level full factorial design was used to study the significant influence of process and product variables i.e. 1) Concentration of sodium fluoride, 2) Concentration of PVP, 3) Sample volume, 4) Drying surface, on particle size of sodium fluoride. The experimental design result shows that independent product variables significantly modify the structure and improve particle size reduction of sodium fluoride.展开更多
Herbal plants act as a significant source for discovering new compounds with potential therapeutic activities.Polyalthia longifolia,which is commonly known as an Indian mast tree,has various pharmacological properties...Herbal plants act as a significant source for discovering new compounds with potential therapeutic activities.Polyalthia longifolia,which is commonly known as an Indian mast tree,has various pharmacological properties,such as an anticancer,ulcer protective,hypoglycemic,hypotensive,a corrosion inhibitor,a bio-adsorbent,and few more.Moreover,it is known as false ashoka owing to its close resemblance with Saraca indica(ashoka tree).Various compounds have been reported from the extract of some parts of the plant,such as leaves,bark,root,and seeds.These extracts possess an ability to treat a number of human ailments,such as fever,ulcer,skin diseases,helminthiasis,and cardiac problems.Studies performed on the leave extract shows evidence that some compounds cause cell death in various cancer cell lines.The plant also has some biological applications,such as antibacterial,antiviral,and antimicrobial,which makes it clinically significant and useful.This review is an effort to explore and gather plant information in an organized manner.It reveals detailed information about the propagation,synonyms,vernaculars,varieties of plant,medicinal significance,ecology and distribution,botanical and ethnobotanical description,phytochemical constituents,and pharmacological activity of the plant.展开更多
文摘The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We also investigated the effect of ARG on complexation efficiency(CE) of βCD towards CFA in an aqueous medium through phase solubility behaviour according to Higuchi and Connors. Although phase solubility studies showed AL(linear) type of solubility curve in presence and absence of ARG, the CE and association constant(Ks) of βCD towards CFA were significantly promoted in presence of ARG,justifying its use as a ternary component. The solid systems of CFA with βCD were obtained by spray drying technique with or without incorporation of ARG and characterized by differential scanning calorimetry(DSC), X-ray powder diffractometry(XRPD), scanning electron microscopy(SEM), and saturation solubility and dissolution studies. The molecular modeling studies provided a better insight into geometry and inclusion mode of CFA inside βCD cavity. The solubility and dissolution rate of CFA were significantly improved upon complexation with βCD as compared to CFA alone. However, ternary system incorporated with ARG performed better than binary system in physicochemical evaluation. In conclusion, ARG could be exploited as a ternary component to improve the physicochemical properties of CFA via βCD complexation.
文摘Objective:To evaluate the anti-oxidani and anti-inflammatory activity of leaf extracts and fractions of Mangifera indica in in vitro conditions.Methods:In vitro DPPH radical scavenging activity and lipoxygenase（LOX） inhibition assays were used to evaluate the anti-oxidant and anti-inflammatory activities respectively.Methanolic extract（MEMI）,successive water extract （SWMI） and ethyl acetate fraction（EMEMI）,n-butanol fraction（BMEMI） and water soluble fraction （WMEMI） of methanolic extract were evaluated along with respective reference standards. Results:In in ritro DPPH radical scavenging activity,the MEMI,EMEMI and BMEMI have offered significant antioxidant activity with IC<sub>50</sub> values of 13.37.3.55 and 14.19μig/mL respectively.Gallic acid,a reference standard showed significant antioxidant activity with IC? value of 1.88 and found to be more potent compared to all the extracts and fractions.In m vitro LOX inhibition assay,the MEMI,EMEMI and BMEMI have showed significant inhibition of LOX enzyme activity with IC<sub>50</sub> values of 96.71.63.21 and 107.44μg/mL respectively.While,reference drug Indometlhacin also offered significant inhibtion against LOX enzyme activity with IC<sub>50</sub> of 57.75.Furthermore,MEMI was found to more potent than SWMI and among the fractions EMEMI was found to possess more potent antioxidant and anti-inflammatory activity.Conclusions:These findings suggest that the MEMI and F.MEMT possess potent anti-oxidani and anti-inflammatory activities in in vitro conditions.
基金support provided by Rajarambapu College of Pharmacy,Kasegaon,Sangli-415404Maharashtra,India and Krishna institute of medical sciences,Karad,Maharashtra,India for carrying out this research.
文摘Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination.Niranthin is a lignan isolated from various Phyllanthus sources.The literature survey on niranthin highlights wide ranges of the therapeutic potentials.In a present study,based on our previous investigations,we evaluated pure,isolated and characterized niranthin as an anxiolytic agent.The niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole]was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test(EPM)and Light&Dark Exploration test(L&D).GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM task.Molecular docking simulation studies(pdb id:4COF)carried out by Vlife QSAR software showed that niranthin(docking score:−62.1714 kcal/mol)have shown comparatively best docking score compared to the standard drug Diazepam(docking score:−63.1568 kcal/mol).To conclude,Niranthin has probable potential in the management of anxiety disorder.Our in-silico and in-vivo analysis(indirectly)indicated the plausible role of GABA mediation for anxiolytic activity.Although,these studies are preliminary,future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.
文摘The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition for predefined particle size of sodium fluoride. The sodium fluoride is mainly used in dental preparation for delivering the fluoride ion to the tooth enamel for that nano-particle size is required. Nowadays the milling process is used to reduce the particle size. But that process has some limitations due to crystalline nature of sodium fluoride;for overcoming those limitations, lyophilization method is used. A 4<sup>3</sup> level full factorial design was used to study the significant influence of process and product variables i.e. 1) Concentration of sodium fluoride, 2) Concentration of PVP, 3) Sample volume, 4) Drying surface, on particle size of sodium fluoride. The experimental design result shows that independent product variables significantly modify the structure and improve particle size reduction of sodium fluoride.
基金funding support from the National Natural Science Foundation of China(No.82074251)the Hunan Natural Science Foundation of China(No.2018JJ2413)the Hunan Provincial Health and Health Commission Project(No.c2018032)。
文摘Herbal plants act as a significant source for discovering new compounds with potential therapeutic activities.Polyalthia longifolia,which is commonly known as an Indian mast tree,has various pharmacological properties,such as an anticancer,ulcer protective,hypoglycemic,hypotensive,a corrosion inhibitor,a bio-adsorbent,and few more.Moreover,it is known as false ashoka owing to its close resemblance with Saraca indica(ashoka tree).Various compounds have been reported from the extract of some parts of the plant,such as leaves,bark,root,and seeds.These extracts possess an ability to treat a number of human ailments,such as fever,ulcer,skin diseases,helminthiasis,and cardiac problems.Studies performed on the leave extract shows evidence that some compounds cause cell death in various cancer cell lines.The plant also has some biological applications,such as antibacterial,antiviral,and antimicrobial,which makes it clinically significant and useful.This review is an effort to explore and gather plant information in an organized manner.It reveals detailed information about the propagation,synonyms,vernaculars,varieties of plant,medicinal significance,ecology and distribution,botanical and ethnobotanical description,phytochemical constituents,and pharmacological activity of the plant.
