Objective:To correlate the chromatographic and computational method to calculate lipophilicity of selected ginger compounds and to observe the effects of log P on wound healing.Methods:Mixtures of acetonitrile and wat...Objective:To correlate the chromatographic and computational method to calculate lipophilicity of selected ginger compounds and to observe the effects of log P on wound healing.Methods:Mixtures of acetonitrile and water with acetonitrile content between 95%and 50%v/v in 5%increments were kept separately in 10 different chromatographic chambers,saturated with solvent for 2 h.Spots were observed under UV light atλ=254 nm p-anisaldehyde used as a spraying reagent Theoretical calculation was done using the Alogps 2.1 online program at www.vcclab.org/lab/alogps.For percentage wound contraction,five groups of animal(mice)(25-30 g)of either sex were selected.Wound were created on dorsal surface of animals using toothed forceps,scalpel and pointed scissors.The wound areas were calculated using vernier caliper.After making wound mice were orally administered 35 mg/kg 6-shogoal,6-gingerol,8-gingerol and 10-gingerol respectively.Croup E as the control group received tap water.Results:The Iipophilicity values determined in thin layer chromatography were correlated with the theoretically calculated various log P by linear regression analysis.Significant correlations were found between log P values calculated by software program and the experimental reversedphase thin-layer chromatography data.Order of wound healing property of ginger compounds is directly dependent on lipophilieity i.e.more lipophilic compound has highest activity.Conclusions:Experimentally determined lipophilieity(R_(MO))values were correlated with log P determined by software's and found satisfactory.Lipophilieity(R_(MO)is a useful parameter for the determination and prediction of biological activity of ginger compounds.展开更多
Parkinson’s disease(PD)is an age-related neurodegenerative ailment that affects dopamine-producing neurons in a specific area of the brain called the substantia nigra of the ventral midbrain.It is clinically characte...Parkinson’s disease(PD)is an age-related neurodegenerative ailment that affects dopamine-producing neurons in a specific area of the brain called the substantia nigra of the ventral midbrain.It is clinically characterized by movement disorder and marked with unusual synaptic protein alpha-synuclein accumulation in the brain.To date,only a few Food and Drug Administration(FDA)approved drugs are available on the market for the treatment of PD.Nonetheless,these drugs show parasympathomimetic related adverse events and remarkably higher toxicity;hence,it is important to find more efficacious molecules to treat PD.In our study,We chosen 22 natural compounds as inhibitors that potentially block the alpha-synuclein clump-the pathological hallmark of PD-and provide new avenues for its treatment.Most of these molecules exhibited good pharmacokinetic behaviors,making them decisively favorable drug candidates to cure PD.Molecular docking studies were performed to investigate the binding interactions between natural compounds and alpha-synuclein as anti-Parkinson drug targets.Among the examined compounds,curcumin and piperine emerged as promising phytochemicals with the highest binding affinity,key residual stable bindings and showed a good inhibitory features.Thus,the present study indicates that curcumin and piperine hold the potential to be developed as treatment options against PD.Experimental validations are needed for insights into their mechanism of action and potential clinical application.展开更多
Objective:To develop a simple,selective,sensitive and accurate high-performance thin layer chromatography(HPTLC)method to determine the quantity of hesperidin in different varieties of citrus fruits.Methods:The method...Objective:To develop a simple,selective,sensitive and accurate high-performance thin layer chromatography(HPTLC)method to determine the quantity of hesperidin in different varieties of citrus fruits.Methods:The method was carried out in aluminum-backed silica gel 60 F_(254)plates with ethyl acetate-methanol-water 15:3:2(%,v/v)as mobile phase.Results:A compact band was obtained for hesperidin at R_f value of(0.40±0.04).The calibration plot was linear in the range of 100-800 ng/spot of hesperidin and the correlation coefficient of 0.9986was indicative of good linear dependence of peak area on concentration.Limit of detection(8.87ng/spot),limit of quantification(23.21 ng/spot),accuracy(less than 2%)and recovery(ranging from98.55-99.38)were found satisfactory.Conclusions:The method developed can be used for routine analysis of hesperidin in crude drug as well as in herbal and pharmaceutical dosage form containing citrus fruits as an ingredient.展开更多
Ionosphereic foF2 variations are very sensitive to the seismic effect and results of ionospheric perturbations associated with earthquakes seem to very hopeful for short-term earthquake prediction. On January 18,2011 ...Ionosphereic foF2 variations are very sensitive to the seismic effect and results of ionospheric perturbations associated with earthquakes seem to very hopeful for short-term earthquake prediction. On January 18,2011 at 20: 23 UT a great earthquake( M = 7. 2)occurred in Dalbandin( 28. 73° N,63. 92° E),Pakistan. In this study,we have tried to find out the features of pre-earthquake ionospheric anomalies by using the hourly day time( 08. 00 a. m.- 05. 00 p. m.) data of critical frequency( foF2) obtained by three vertical sounding stations installed in Islamabad( 33. 78°N,73. 06°E),Multan( 32. 26°N,71. 51°E) and Karachi( 24. 89° N,67. 02° E), Pakistan. The results show the significant anomalies of foF2 in the earthquake preparation zone several days prior to the Dalbandin earthquake. It is also observed that the amplitude and frequency of foF2 anomalies are more prominent at the nearest station to the epicenter as compared to those stations near the outer margin of the earthquake preparation zone. The confidence level for ionospheric anomalies regarding the seismic signatures can be enhanced by adding the analysis of some other ionospheic parameters along with critical frequency of the layer F2.展开更多
Objective:To assess in-vitro antioxidant activity of different fraction and perform high performance thin layer chromatography fingerprint analysis of most active fraction of Rumex vesicarius L.(R.vesicarius).Methods:...Objective:To assess in-vitro antioxidant activity of different fraction and perform high performance thin layer chromatography fingerprint analysis of most active fraction of Rumex vesicarius L.(R.vesicarius).Methods:In the present study,acetone,ethyl acetate,n-butanol,and methanol extracts of R.vesicarius were evaluated for radical scavenging activity by studying the inhibition of the level of lipid peroxidation induced by Fe(++)/ascorbate,DNA sugar damage,scavenging of hydrogen peroxide,diphenylphosphine DPPH radical scavenging activity,total phenolic content,total flavonoids content and total proanthocyanidin.High performance thin layer chromatography finger print profiling of R.vesicarius L.was also done.Results:Lipid peroxidation induced by the iron/ascorbate system,hydrogen peroxide,diphenylphosphine and DNA sugar damage were inhibited by the addition of different extract of R.vesicarius.Among them,methanolic extract showed maximum efficacy.The methanolic extract showed the highest total phenolic,total flavonoids and total proanthocyanidin contents.Conclusions:The results suggest that the extracts can be a vital source of phytochemical antioxidants.展开更多
Tuberculosis(TB)disease has become one of the major public health concerns globally,especially in developing countries.Numerous research studies have already been carried out for TB,but we are still struggling for a c...Tuberculosis(TB)disease has become one of the major public health concerns globally,especially in developing countries.Numerous research studies have already been carried out for TB,but we are still struggling for a complete and quick cure for it.The progress of Mycobacterium tuberculosis(MTB)strains resistant to existing drugs makes its cure and control very complicated.Therefore,it is the need of the hour to search for newer and effective drugs that can inhibit an increasing number of putative drug targets.We applied the drug repurposing concept to identify promising FDAapproved drugs against five key-regulatory genes(FurB,IdeR,KstR,MosR,and RegX3)of the MTB.The FDA drugs were virtually screened using a structure-based approach by GOLD versions 5.2,and subjected to rigid docking followed by an induced-fit docking algorithm to enhance the accuracy and prioritize drugs for repurposing.We found 11 candidate drugs(including ZINC03871613,ZINC03871614,ZINC03871615 as top scorer candidate drugs)that were frequently present within the top 20 GoldScore ranks and showed promising results.Furthermore,molecular dynamics simulation was performed to monitor the effect of the top scorer drugs on the structural stability of all the five targets,indicating that inhibitors preferentially bind to the active site of the targets.This work suggests that these known FDA-approved drugs open new application domains in the form of anti-tuberculosis agents.展开更多
基金Supported by the deanship at King Saud University with Grant No.RGP-VPP-150
文摘Objective:To correlate the chromatographic and computational method to calculate lipophilicity of selected ginger compounds and to observe the effects of log P on wound healing.Methods:Mixtures of acetonitrile and water with acetonitrile content between 95%and 50%v/v in 5%increments were kept separately in 10 different chromatographic chambers,saturated with solvent for 2 h.Spots were observed under UV light atλ=254 nm p-anisaldehyde used as a spraying reagent Theoretical calculation was done using the Alogps 2.1 online program at www.vcclab.org/lab/alogps.For percentage wound contraction,five groups of animal(mice)(25-30 g)of either sex were selected.Wound were created on dorsal surface of animals using toothed forceps,scalpel and pointed scissors.The wound areas were calculated using vernier caliper.After making wound mice were orally administered 35 mg/kg 6-shogoal,6-gingerol,8-gingerol and 10-gingerol respectively.Croup E as the control group received tap water.Results:The Iipophilicity values determined in thin layer chromatography were correlated with the theoretically calculated various log P by linear regression analysis.Significant correlations were found between log P values calculated by software program and the experimental reversedphase thin-layer chromatography data.Order of wound healing property of ginger compounds is directly dependent on lipophilieity i.e.more lipophilic compound has highest activity.Conclusions:Experimentally determined lipophilieity(R_(MO))values were correlated with log P determined by software's and found satisfactory.Lipophilieity(R_(MO)is a useful parameter for the determination and prediction of biological activity of ginger compounds.
文摘Parkinson’s disease(PD)is an age-related neurodegenerative ailment that affects dopamine-producing neurons in a specific area of the brain called the substantia nigra of the ventral midbrain.It is clinically characterized by movement disorder and marked with unusual synaptic protein alpha-synuclein accumulation in the brain.To date,only a few Food and Drug Administration(FDA)approved drugs are available on the market for the treatment of PD.Nonetheless,these drugs show parasympathomimetic related adverse events and remarkably higher toxicity;hence,it is important to find more efficacious molecules to treat PD.In our study,We chosen 22 natural compounds as inhibitors that potentially block the alpha-synuclein clump-the pathological hallmark of PD-and provide new avenues for its treatment.Most of these molecules exhibited good pharmacokinetic behaviors,making them decisively favorable drug candidates to cure PD.Molecular docking studies were performed to investigate the binding interactions between natural compounds and alpha-synuclein as anti-Parkinson drug targets.Among the examined compounds,curcumin and piperine emerged as promising phytochemicals with the highest binding affinity,key residual stable bindings and showed a good inhibitory features.Thus,the present study indicates that curcumin and piperine hold the potential to be developed as treatment options against PD.Experimental validations are needed for insights into their mechanism of action and potential clinical application.
基金Supported by Deanship of Scientific Research,Salman Bin Abdulaziz University,Al-Kharj,KSA(Grant No.33/S/54)
文摘Objective:To develop a simple,selective,sensitive and accurate high-performance thin layer chromatography(HPTLC)method to determine the quantity of hesperidin in different varieties of citrus fruits.Methods:The method was carried out in aluminum-backed silica gel 60 F_(254)plates with ethyl acetate-methanol-water 15:3:2(%,v/v)as mobile phase.Results:A compact band was obtained for hesperidin at R_f value of(0.40±0.04).The calibration plot was linear in the range of 100-800 ng/spot of hesperidin and the correlation coefficient of 0.9986was indicative of good linear dependence of peak area on concentration.Limit of detection(8.87ng/spot),limit of quantification(23.21 ng/spot),accuracy(less than 2%)and recovery(ranging from98.55-99.38)were found satisfactory.Conclusions:The method developed can be used for routine analysis of hesperidin in crude drug as well as in herbal and pharmaceutical dosage form containing citrus fruits as an ingredient.
基金partly supported by the Natural Science Foundation of China,Contract No. 41274061
文摘Ionosphereic foF2 variations are very sensitive to the seismic effect and results of ionospheric perturbations associated with earthquakes seem to very hopeful for short-term earthquake prediction. On January 18,2011 at 20: 23 UT a great earthquake( M = 7. 2)occurred in Dalbandin( 28. 73° N,63. 92° E),Pakistan. In this study,we have tried to find out the features of pre-earthquake ionospheric anomalies by using the hourly day time( 08. 00 a. m.- 05. 00 p. m.) data of critical frequency( foF2) obtained by three vertical sounding stations installed in Islamabad( 33. 78°N,73. 06°E),Multan( 32. 26°N,71. 51°E) and Karachi( 24. 89° N,67. 02° E), Pakistan. The results show the significant anomalies of foF2 in the earthquake preparation zone several days prior to the Dalbandin earthquake. It is also observed that the amplitude and frequency of foF2 anomalies are more prominent at the nearest station to the epicenter as compared to those stations near the outer margin of the earthquake preparation zone. The confidence level for ionospheric anomalies regarding the seismic signatures can be enhanced by adding the analysis of some other ionospheic parameters along with critical frequency of the layer F2.
基金Supported by Deanship of Scientific Research,Salman binAbdulaziz University,Al-Kharj Saudi Arabia(Grant No.4/1432)
文摘Objective:To assess in-vitro antioxidant activity of different fraction and perform high performance thin layer chromatography fingerprint analysis of most active fraction of Rumex vesicarius L.(R.vesicarius).Methods:In the present study,acetone,ethyl acetate,n-butanol,and methanol extracts of R.vesicarius were evaluated for radical scavenging activity by studying the inhibition of the level of lipid peroxidation induced by Fe(++)/ascorbate,DNA sugar damage,scavenging of hydrogen peroxide,diphenylphosphine DPPH radical scavenging activity,total phenolic content,total flavonoids content and total proanthocyanidin.High performance thin layer chromatography finger print profiling of R.vesicarius L.was also done.Results:Lipid peroxidation induced by the iron/ascorbate system,hydrogen peroxide,diphenylphosphine and DNA sugar damage were inhibited by the addition of different extract of R.vesicarius.Among them,methanolic extract showed maximum efficacy.The methanolic extract showed the highest total phenolic,total flavonoids and total proanthocyanidin contents.Conclusions:The results suggest that the extracts can be a vital source of phytochemical antioxidants.
文摘Tuberculosis(TB)disease has become one of the major public health concerns globally,especially in developing countries.Numerous research studies have already been carried out for TB,but we are still struggling for a complete and quick cure for it.The progress of Mycobacterium tuberculosis(MTB)strains resistant to existing drugs makes its cure and control very complicated.Therefore,it is the need of the hour to search for newer and effective drugs that can inhibit an increasing number of putative drug targets.We applied the drug repurposing concept to identify promising FDAapproved drugs against five key-regulatory genes(FurB,IdeR,KstR,MosR,and RegX3)of the MTB.The FDA drugs were virtually screened using a structure-based approach by GOLD versions 5.2,and subjected to rigid docking followed by an induced-fit docking algorithm to enhance the accuracy and prioritize drugs for repurposing.We found 11 candidate drugs(including ZINC03871613,ZINC03871614,ZINC03871615 as top scorer candidate drugs)that were frequently present within the top 20 GoldScore ranks and showed promising results.Furthermore,molecular dynamics simulation was performed to monitor the effect of the top scorer drugs on the structural stability of all the five targets,indicating that inhibitors preferentially bind to the active site of the targets.This work suggests that these known FDA-approved drugs open new application domains in the form of anti-tuberculosis agents.
