Pub Date : 2019-01-01DOI: 10.21608/APRH.2019.5699.1066
E. Shawky, Nagwan M. Gabr, M. Elgindi, R. Mekky
Objectives: This study aimed to make a broad review of the chemical constituents and biological activities of genus Zygophyllum. Methods: This review covers the peer reviewed articles between 1977 and August, 2018, retrieved from PubMed, Science Direct, Sci-Hub, Springer and Wikipedia Results: In traditional medicine, plants of genus Zygophyllum have been employed and utilized as anti-rheumatic, anti-gout, antidiabetic, anti-hyperlipidemic, antimicrobial, anti-oxidant, antihypertensive, antiseptic, anti-eczema and antidiarrheal. Zygophyllum species have been phytochemically studied leading to the identification of various classes of compounds including triterpenes, flavonoids, saponins, sterols, simple phenolic compounds, and esters. Biological studies on Zygophyllum species have also indicated various bioactive potentials including antioxidant, antidiabetic, antimicrobial antitumor and anti-inflammatory effects. The reported medicinal Zygophyllum species were selected and summarized on basis of their; geographical distribution, traditional uses, chemical constituents and biological activities. Conclusion: It would therefore be important to extensively investigate their phytochemicals and pharmacologically determine their activities for future drug discovery and development.
{"title":"A Comprehensive Review on Genus Zygophyllum","authors":"E. Shawky, Nagwan M. Gabr, M. Elgindi, R. Mekky","doi":"10.21608/APRH.2019.5699.1066","DOIUrl":"https://doi.org/10.21608/APRH.2019.5699.1066","url":null,"abstract":"Objectives: This study aimed to make a broad review of the chemical constituents and biological activities of genus Zygophyllum. Methods: This review covers the peer reviewed articles between 1977 and August, 2018, retrieved from PubMed, Science Direct, Sci-Hub, Springer and Wikipedia Results: In traditional medicine, plants of genus Zygophyllum have been employed and utilized as anti-rheumatic, anti-gout, antidiabetic, anti-hyperlipidemic, antimicrobial, anti-oxidant, antihypertensive, antiseptic, anti-eczema and antidiarrheal. Zygophyllum species have been phytochemically studied leading to the identification of various classes of compounds including triterpenes, flavonoids, saponins, sterols, simple phenolic compounds, and esters. Biological studies on Zygophyllum species have also indicated various bioactive potentials including antioxidant, antidiabetic, antimicrobial antitumor and anti-inflammatory effects. The reported medicinal Zygophyllum species were selected and summarized on basis of their; geographical distribution, traditional uses, chemical constituents and biological activities. Conclusion: It would therefore be important to extensively investigate their phytochemicals and pharmacologically determine their activities for future drug discovery and development.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"53 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73290128","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 : 2019-01-01DOI: 10.21608/APRH.2018.6527.1072
R. Ahmed, E. Elkhrisy, Walaa El-Kashak, M. Raey, M. Nassar, E. Aboutabl
Objectives: This study focused on the identification and characterization of secondary metabolites tentatively from aqueous ethanolic leaf extract of Livistona chinensisby HPLC-PDA-ESI-MS/MS and evaluation of its cytotoxic activity. Methods: The aqueous ethanolic extract was analyzed by high performance liquid chromatography (HPLC) coupled to photodiode array detection of mass spectroscopy (PDA-MS/MS), to detect the secondary metabolites in L. chinensis leaves extract. It was also estimated for its cytotoxicity againsthuman prostate carcinoma (PC3) and hepatocellular liver carcinoma (HepG2) cancer cell lines using SRB (3-(4, 5-dimethyl thiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay. Results: Forty-two secondary metabolites were tentatively identified; the most major compounds were C-glycoside derivatives of apigenin, luteolin and tricin together with phenolic acids. The 70% alcoholic extract of L. chinensis leaves exhibit more antitumor activity against PC3than against HepG2. Conclusion:L. chinensis is a privileged source of C-flavonoids that revealed the efficiency of HPLC-MS metabolomics in natural products drug discovery.
{"title":"Structural Characterization of Polyphenolics in Livistona chinensis Using HPLC-PDA-MS","authors":"R. Ahmed, E. Elkhrisy, Walaa El-Kashak, M. Raey, M. Nassar, E. Aboutabl","doi":"10.21608/APRH.2018.6527.1072","DOIUrl":"https://doi.org/10.21608/APRH.2018.6527.1072","url":null,"abstract":"Objectives: This study focused on the identification and characterization of secondary metabolites tentatively from aqueous ethanolic leaf extract of Livistona chinensisby HPLC-PDA-ESI-MS/MS and evaluation of its cytotoxic activity. Methods: The aqueous ethanolic extract was analyzed by high performance liquid chromatography (HPLC) coupled to photodiode array detection of mass spectroscopy (PDA-MS/MS), to detect the secondary metabolites in L. chinensis leaves extract. It was also estimated for its cytotoxicity againsthuman prostate carcinoma (PC3) and hepatocellular liver carcinoma (HepG2) cancer cell lines using SRB (3-(4, 5-dimethyl thiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay. Results: Forty-two secondary metabolites were tentatively identified; the most major compounds were C-glycoside derivatives of apigenin, luteolin and tricin together with phenolic acids. The 70% alcoholic extract of L. chinensis leaves exhibit more antitumor activity against PC3than against HepG2. Conclusion:L. chinensis is a privileged source of C-flavonoids that revealed the efficiency of HPLC-MS metabolomics in natural products drug discovery.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"61 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83836650","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 : 2018-10-01DOI: 10.21608/APRH.2018.5126.1065
A. Abbas, W. Ibrahim, W. Sakran, A. Badawi
Objective: The aim of this work focused on formulation and evaluation of sildenafil 50 mg orodispersible tablets by sublimation technique. Methods: Active ingredient and excipients mixtures were evaluated for physicochemical changes of the drug utilizing FTIR spectroscopy and DSC thermal analysis. Nineteen proposed formulae N1-N19 were prepared by sublimation technique using menthol as a sublimating agent. Three different types of superdisintegrants (sodium starch glycolate, croscarmellose sodium and plasidone XL) were used in three different ratios (3, 6 and 9 % w/w), percentage of inter-granular and intragranular disintegrant. Hydrophilic filler such as mannitol and hydrophobic filler such as microcrystalline cellulose were used in the ratio (1:1, 2:1 and 4:1 w/w).Elimination of bitterness using sucralose as a potent sweetener. Granulation was achieved by alcoholic solution of PVP K25 as binder at Diosna® high shear mixer. Lubricant (hydrophobic magnesium stearate and hydrophilic sodium stearyl fumarate). Un-lubricated granules were characterized for bulk density, tapped density, true density, particle size distribution, Carr'sindex, Hausner ratio, flow rate and angle of repose. Tablets were firstly compressed on rotary machine then subjected to vacuum oven at 60ᵒC for 6 hours. Post compression characterization for tablets after sublimation including content uniformity, average weight, hardness, thickness, In-vitro disintegration, friability, wetting time, assay and dissolution profile of the proposed formulae against the immediate release marketed tablet Viagra ® 50 mg tablet. Results: The formula (N 16) which granulated using 1% PVP k25 with 9% plasidone XL (60% of it is inter-granular while 30% intra-granular), menthol 1%, Microcrystalline cellulose: Mannitol 1:1 and magnesium stearate was the most effective formulation as it showed wetting time of 30.7 seconds, disintegration time of 25 seconds and cumulative % drug release of 92.8 and 95.8 % after 1 and 3 minute respectively. Conclusion: Sildenafil 50 mg ODT successfully was prepared by sublimation technique with better wetting time, disintegration time, assay dissolution profile, hardness and friability.
{"title":"Evaluation and Characterization of Sildenafil 50 mg Orodispersible Tablets Using Sublimation Technique","authors":"A. Abbas, W. Ibrahim, W. Sakran, A. Badawi","doi":"10.21608/APRH.2018.5126.1065","DOIUrl":"https://doi.org/10.21608/APRH.2018.5126.1065","url":null,"abstract":"Objective: The aim of this work focused on formulation and evaluation of sildenafil 50 mg orodispersible tablets by sublimation technique. Methods: Active ingredient and excipients mixtures were evaluated for physicochemical changes of the drug utilizing FTIR spectroscopy and DSC thermal analysis. Nineteen proposed formulae N1-N19 were prepared by sublimation technique using menthol as a sublimating agent. Three different types of superdisintegrants (sodium starch glycolate, croscarmellose sodium and plasidone XL) were used in three different ratios (3, 6 and 9 % w/w), percentage of inter-granular and intragranular disintegrant. Hydrophilic filler such as mannitol and hydrophobic filler such as microcrystalline cellulose were used in the ratio (1:1, 2:1 and 4:1 w/w).Elimination of bitterness using sucralose as a potent sweetener. Granulation was achieved by alcoholic solution of PVP K25 as binder at Diosna® high shear mixer. Lubricant (hydrophobic magnesium stearate and hydrophilic sodium stearyl fumarate). Un-lubricated granules were characterized for bulk density, tapped density, true density, particle size distribution, Carr'sindex, Hausner ratio, flow rate and angle of repose. Tablets were firstly compressed on rotary machine then subjected to vacuum oven at 60ᵒC for 6 hours. Post compression characterization for tablets after sublimation including content uniformity, average weight, hardness, thickness, In-vitro disintegration, friability, wetting time, assay and dissolution profile of the proposed formulae against the immediate release marketed tablet Viagra ® 50 mg tablet. Results: The formula (N 16) which granulated using 1% PVP k25 with 9% plasidone XL (60% of it is inter-granular while 30% intra-granular), menthol 1%, Microcrystalline cellulose: Mannitol 1:1 and magnesium stearate was the most effective formulation as it showed wetting time of 30.7 seconds, disintegration time of 25 seconds and cumulative % drug release of 92.8 and 95.8 % after 1 and 3 minute respectively. Conclusion: Sildenafil 50 mg ODT successfully was prepared by sublimation technique with better wetting time, disintegration time, assay dissolution profile, hardness and friability.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87897646","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 : 2018-10-01DOI: 10.21608/APRH.2018.18131
T. Khider
Sudan has large area, with multiculture, habits rich biodiversity and medicinal plants, although was divided in 2011 into two countries still rich with valuable medicinal plants. The objective of the present mini review is to indicate and document some medicinal plants from Sudan and reflect their valuable uses in treating some indigenous and tropical diseases. The present minireview gave a look at some of these plants, mentioning their families, distribution, their local names, their habits, the plant part used for treating diseases and mode of treatment. The medicinal and Aromatic Plants Research Institute (MAPRI) of the National Centre for Research (NCR) plays major role in medicinal and aromatic plants investigation, determination, valuation and documentation in Sudan and contributes with local healers in different regions of Sudan, the rediscovering of these plants is highly needed with contribution of overseas pharmaceuticals companies as natural products have less side effects than industrial drugs.
{"title":"A Look at Some Medicinal Plants from Sudan-Mini Review","authors":"T. Khider","doi":"10.21608/APRH.2018.18131","DOIUrl":"https://doi.org/10.21608/APRH.2018.18131","url":null,"abstract":"Sudan has large area, with multiculture, habits rich biodiversity and medicinal plants, although was divided in 2011 into two countries still rich with valuable medicinal plants. The objective of the present mini review is to indicate and document some medicinal plants from Sudan and reflect their valuable uses in treating some indigenous and tropical diseases. The present minireview gave a look at some of these plants, mentioning their families, distribution, their local names, their habits, the plant part used for treating diseases and mode of treatment. The medicinal and Aromatic Plants Research Institute (MAPRI) of the National Centre for Research (NCR) plays major role in medicinal and aromatic plants investigation, determination, valuation and documentation in Sudan and contributes with local healers in different regions of Sudan, the rediscovering of these plants is highly needed with contribution of overseas pharmaceuticals companies as natural products have less side effects than industrial drugs.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91105353","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 : 2018-10-01DOI: 10.21608/APRH.2018.2839.1049
Hossam R Elgiushy, S. Hammad, Ashraf S. Hassan, Nageh Aboutaleb, K. Abouzid
Acrylamide moiety is a pronounced Michael acceptor that has drawn much interest in a wide array of drugs designed for various therapeutic purposes. Herein we outline different synthetic pathways, scientific bases for its chemical reactivity and how it is functionalized for design of new therapeutic entities, in addition to a brief insight into spectrum of reported biological activities of acrylamide containing compounds up to date.
{"title":"Acrylamide moiety, a Valuable Fragment in Medicinal Chemistry: Insight into Synthetic Methodologies, Chemical Reactivity and Spectrum of Biological Activities of Acrylamide Derivatives","authors":"Hossam R Elgiushy, S. Hammad, Ashraf S. Hassan, Nageh Aboutaleb, K. Abouzid","doi":"10.21608/APRH.2018.2839.1049","DOIUrl":"https://doi.org/10.21608/APRH.2018.2839.1049","url":null,"abstract":"Acrylamide moiety is a pronounced Michael acceptor that has drawn much interest in a wide array of drugs designed for various therapeutic purposes. Herein we outline different synthetic pathways, scientific bases for its chemical reactivity and how it is functionalized for design of new therapeutic entities, in addition to a brief insight into spectrum of reported biological activities of acrylamide containing compounds up to date.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72917263","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 : 2018-10-01DOI: 10.21608/APRH.2018.5165.1064
M. Hegazy, Mona S. Elshahed, S. Toubar, Marwa I Helmy
Objectives: The main aim of this study is to apply smart, simple, rapid and accurate methods for simultaneous determination of Paracetamol (PAR), Chlorzoxazone (CXZ) and Diclofenac potassium (DIC), in their bulk powder and tablet dosage form. Methods: Potent processing methods were used which were based on the application of continuous wavelet transform (CWT) and Savitsky–Golay derivatization (SAVGOL) as univariate spectrophotometric methods, partial least squares (PLS) and synergy interval partial least squares (siPLS) as multivariate methods. Results: PAR, CXZ and DIC were determined in the concentration ranges of 2–30, 2–50 and 2–30 μg/mL, respectively. The regressing and validation parameters of the proposed methods revealed the efficiency of the methods. The results obtained for the analysis of those drugs by the proposed methods were statistically compared to those obtained by applying a reported high performance liquid chromatographic method. Statistical comparison was done, and no significant difference was found between the proposed methods and the reported one. Conclusion: Successful determination of ternary mixture containing PAR, CXZ and DIC was achieved with no need for tedious sample separation or pre-treatment derivatization which is considered a great benefit in quality control laboratories.
{"title":"Efficient processing of Single and Multiple Spectral Variables for Resolution and Quantitation of Paracetamol, Chlorzoxazone and Diclofenac","authors":"M. Hegazy, Mona S. Elshahed, S. Toubar, Marwa I Helmy","doi":"10.21608/APRH.2018.5165.1064","DOIUrl":"https://doi.org/10.21608/APRH.2018.5165.1064","url":null,"abstract":"Objectives: The main aim of this study is to apply smart, simple, rapid and accurate methods for simultaneous determination of Paracetamol (PAR), Chlorzoxazone (CXZ) and Diclofenac potassium (DIC), in their bulk powder and tablet dosage form. Methods: Potent processing methods were used which were based on the application of continuous wavelet transform (CWT) and Savitsky–Golay derivatization (SAVGOL) as univariate spectrophotometric methods, partial least squares (PLS) and synergy interval partial least squares (siPLS) as multivariate methods. Results: PAR, CXZ and DIC were determined in the concentration ranges of 2–30, 2–50 and 2–30 μg/mL, respectively. The regressing and validation parameters of the proposed methods revealed the efficiency of the methods. The results obtained for the analysis of those drugs by the proposed methods were statistically compared to those obtained by applying a reported high performance liquid chromatographic method. Statistical comparison was done, and no significant difference was found between the proposed methods and the reported one. Conclusion: Successful determination of ternary mixture containing PAR, CXZ and DIC was achieved with no need for tedious sample separation or pre-treatment derivatization which is considered a great benefit in quality control laboratories.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"65 3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84271614","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 : 2018-10-01DOI: 10.21608/APRH.2018.5173.1063
H. Ibrahim, F. S. Elshaarawy, E. Haggag
Objectives: This study aimed to isolate the polyphenolic constituents from the methanol extract of Livistona decipiens Becc leaves and evaluate the antioxidant, cytotoxic and antimicrobial activities of the total methanol extract and ethyl acetate fraction Methods: The ethyl acetate and n-butanol fractions of Livistona decipiens leaf methanol extract were subjected separately to different chromatographic separation techniques. Structures of the isolated compounds were established by different spectroscopic techniques (1H / 13C NMR). Antioxidant activitywas evaluated by DPPH assay, while evaluation of cytotoxicity was done according to MTT cell viability assay. Antimicrobial activity was done by agar diffusion method. Results: seven compounds were isolated from the ethyl acetate and n-butanol fractions, they were identified for the first time from the plant as apigenin-8-C-β-D-glucopyranoside (Vitexin) (1), Quercetin-6-C-β-D-glucopyranoside (2),apigenin-6,8-di-C-β-D-glucopyranoside (Vicenin II) (3), 6-O-methyl Kaempferol 3-O-glucopyranoside (4), luteolin-3-C-gentiobiosyl (5),luteolin-6-C-β-D-glucopyranoside (Isoorientin) (6) and luteolin-8-C-β-D-glucopyranoside (Orientin) (7). The ethyl acetate fraction has shown moderate activity against Gram positive and Gram negatvie bacteria, also it showed moderate antioxidant activity with IC50 = 23 ± 0.74 µg/ml when compared to ascorbic acid IC50 = 14.2 ± 0.35 µg/ml. Also ethyl acetate extract has shown cytotoxic activity on MCF-7 cells (human breast cancer cell line), HepG-2 (human hepatocellular carcinoma) and HeLa cells (human cervical cancer cell line), whereas, the methanol extract has shown lower activity. Conclusion: Livistona decipienshave potential medicinal value being rich in polyphenolics and beingantioxidant, cytotoxic and antimicrobial drug.
目的:从枇杷叶甲醇提取物中分离出多酚类成分，并对总甲醇提取物和乙酸乙酯部位的抗氧化、细胞毒和抗菌活性进行评价。方法:采用不同的色谱分离技术分别对枇杷叶甲醇提取物的乙酸乙酯部位和正丁醇部位进行分离。通过不同的波谱技术(1H / 13C NMR)确定了分离化合物的结构。DPPH法测定抗氧化活性，MTT法测定细胞毒性。用琼脂扩散法测定其抑菌活性。结果:从乙酸乙酯和正丁醇组分中分离得到7个化合物，首次从该植物中鉴定为芹菜素-8- c -β- d -葡萄糖吡喃苷(Vitexin)(1)、槲皮素-6- c -β- d -葡萄糖吡喃苷(2)、芹菜素-6,8-di- c -β- d -葡萄糖吡喃苷(Vicenin II)(3)、6- o -甲基山奈酚3- o -葡萄糖吡喃苷(4)、木犀草素-3- c -gentiobiosyl(5)、木犀草素-6- c -β-D-glucopyranoside (Isoorientin)(6)和木犀草素-8- c -β-D-glucopyranoside (Orientin)(7).乙酸乙酯部位对革兰氏阳性菌和革兰氏阴性菌均表现出中等的抗氧化活性，IC50 = 23±0.74µg/ml，而抗坏血酸IC50 = 14.2±0.35µg/ml。乙酸乙酯提取物对MCF-7细胞(人乳腺癌细胞系)、HepG-2细胞(人肝细胞癌)和HeLa细胞(人宫颈癌细胞系)也显示出细胞毒性活性，而甲醇提取物的活性较低。结论:菟丝子富含多酚类物质，具有抗氧化、细胞毒性和抗菌作用，具有潜在的药用价值。
{"title":"Investigation of Livistona decipiens Leaf Methanol Extract and Evaluation of Antioxidant, Antimicrobial and Cytotoxic Activities","authors":"H. Ibrahim, F. S. Elshaarawy, E. Haggag","doi":"10.21608/APRH.2018.5173.1063","DOIUrl":"https://doi.org/10.21608/APRH.2018.5173.1063","url":null,"abstract":"Objectives: This study aimed to isolate the polyphenolic constituents from the methanol extract of Livistona decipiens Becc leaves and evaluate the antioxidant, cytotoxic and antimicrobial activities of the total methanol extract and ethyl acetate fraction Methods: The ethyl acetate and n-butanol fractions of Livistona decipiens leaf methanol extract were subjected separately to different chromatographic separation techniques. Structures of the isolated compounds were established by different spectroscopic techniques (1H / 13C NMR). Antioxidant activitywas evaluated by DPPH assay, while evaluation of cytotoxicity was done according to MTT cell viability assay. Antimicrobial activity was done by agar diffusion method. Results: seven compounds were isolated from the ethyl acetate and n-butanol fractions, they were identified for the first time from the plant as apigenin-8-C-β-D-glucopyranoside (Vitexin) (1), Quercetin-6-C-β-D-glucopyranoside (2),apigenin-6,8-di-C-β-D-glucopyranoside (Vicenin II) (3), 6-O-methyl Kaempferol 3-O-glucopyranoside (4), luteolin-3-C-gentiobiosyl (5),luteolin-6-C-β-D-glucopyranoside (Isoorientin) (6) and luteolin-8-C-β-D-glucopyranoside (Orientin) (7). The ethyl acetate fraction has shown moderate activity against Gram positive and Gram negatvie bacteria, also it showed moderate antioxidant activity with IC50 = 23 ± 0.74 µg/ml when compared to ascorbic acid IC50 = 14.2 ± 0.35 µg/ml. Also ethyl acetate extract has shown cytotoxic activity on MCF-7 cells (human breast cancer cell line), HepG-2 (human hepatocellular carcinoma) and HeLa cells (human cervical cancer cell line), whereas, the methanol extract has shown lower activity. Conclusion: Livistona decipienshave potential medicinal value being rich in polyphenolics and beingantioxidant, cytotoxic and antimicrobial drug.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"80 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75302917","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 : 2018-10-01DOI: 10.21608/APRH.2018.4312.1060
Tahany Ghareeb, S. El-toumy, Hussieny Elgendy, E. Haggag
Objectives: This study aimed to explore the secondary metabolites from the methanolic extract of Euphorbia retusa forssk, as it is known for its use in folk medicine and for being rich in bioactive molecules. Methods: The methanolic extractwas fractionated by different chromatographic techniques and the structures of the isolated compounds were elucidated by UV, 1H and 13C NMR spectroscopy. Hepatoprotective activity of E. retusa extract was evaluated on CCl4-induced liver damage in rats through biochemical assessment of serum ALT as well as MDA, GSH and NO. It was also evaluated through histopathological study of liver autopsy samples. Results: From the aqueous methanolic extract of Euphorbia retusa forssk. aerial parts seven known phenolic compounds; kamferol-3-O-β-D- glucopyranoside (1), quercetin -3-O-β-D- glucopyranoside (2), 3,3`dimethoxy ellagic acid (3), ellagic acid (4), gallic acid (5), kamferol (6) and quercetin (7) were isolated and identified by chromatographic and spectroscopic analysis. Administration of the extract (100 and 200 mg/kg body weight) significantly decreased the AST and ALT levels, inhibited the CCl4 -induced elevated levels of NO and MDA and increased the level of hepatic GSH. A comparative histopathological study of liver exhibited almost nearly normal architecture as compared to toxicant group. Conclusion: Euphorbia retusaextract has shown to have hepatoprotective activityon CCl4-induced liver damage in rats which might be attributed to its phenolic contents.
目的:研究大戟甲醇提取物的次生代谢产物，大戟甲醇提取物具有丰富的生物活性分子，在民间医学中具有广泛的应用价值。方法:采用不同的色谱技术对甲醇提取物进行分馏，并用紫外、1H和13C NMR对分离得到的化合物进行结构鉴定。通过血清ALT、丙二醛(MDA)、谷胱甘肽(GSH)和一氧化氮(NO)的生化测定，评价蛇麻提取物对ccl4所致大鼠肝损伤的保护作用。通过肝脏解剖样本的组织病理学研究也对其进行了评估。结果:从大戟乙醇水提物中提取。航空部分七种已知酚类化合物;分离得到kamferol-3- o -β- d - glucopyranoside(1)、槲皮素-3- o -β- d - glucopyranoside(2)、3,3 '二甲氧基鞣花酸(3)、鞣花酸(4)、没食子酸(5)、kamferol(6)和槲皮素(7)。100和200 mg/kg体重组显著降低AST和ALT水平，抑制CCl4诱导的NO和MDA水平升高，提高肝脏GSH水平。肝脏的比较组织病理学研究显示，与中毒组相比，肝脏的结构几乎正常。结论:大戟提取物对ccl4所致大鼠肝损伤具有保护作用，其机制可能与其酚类物质有关。
{"title":"Secondary Metabolites and Hepatoprotective Activity of Euphorbia retusa","authors":"Tahany Ghareeb, S. El-toumy, Hussieny Elgendy, E. Haggag","doi":"10.21608/APRH.2018.4312.1060","DOIUrl":"https://doi.org/10.21608/APRH.2018.4312.1060","url":null,"abstract":"Objectives: This study aimed to explore the secondary metabolites from the methanolic extract of Euphorbia retusa forssk, as it is known for its use in folk medicine and for being rich in bioactive molecules. Methods: The methanolic extractwas fractionated by different chromatographic techniques and the structures of the isolated compounds were elucidated by UV, 1H and 13C NMR spectroscopy. Hepatoprotective activity of E. retusa extract was evaluated on CCl4-induced liver damage in rats through biochemical assessment of serum ALT as well as MDA, GSH and NO. It was also evaluated through histopathological study of liver autopsy samples. Results: From the aqueous methanolic extract of Euphorbia retusa forssk. aerial parts seven known phenolic compounds; kamferol-3-O-β-D- glucopyranoside (1), quercetin -3-O-β-D- glucopyranoside (2), 3,3`dimethoxy ellagic acid (3), ellagic acid (4), gallic acid (5), kamferol (6) and quercetin (7) were isolated and identified by chromatographic and spectroscopic analysis. Administration of the extract (100 and 200 mg/kg body weight) significantly decreased the AST and ALT levels, inhibited the CCl4 -induced elevated levels of NO and MDA and increased the level of hepatic GSH. A comparative histopathological study of liver exhibited almost nearly normal architecture as compared to toxicant group. Conclusion: Euphorbia retusaextract has shown to have hepatoprotective activityon CCl4-induced liver damage in rats which might be attributed to its phenolic contents.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88156678","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 : 2018-09-30DOI: 10.21608/APRH.2018.3926.1059
M. Aboelmagd, A. Said, S. Ross, E. Haggag
Objective: This study aimed at phytochemical investigation of the 70% alcoholic extract of Erythrina corallodendron L. flowers and biological evaluation of the isolated compounds for their activity as antiprotozoal drugs also evaluation the binding affinity to opioid and cannabinoid receptors as well as the inhibition activity against monoamine oxidase (MAO) enzymes. Method: The 70% alcoholic extract was subjected to successive column chromatographic (CC) separations using silica gel normal phase, reversed phase RP-18, Diaion HP-20, and Sephadex LH-20. The structural elucidation of the isolated compounds was achieved using HR-ESI-MS, UV, 1D and 2D NMR spectroscopic analysis. The isolated compounds were screened in vitro for the binding affinity to opioid and cannabinoid receptors using receptor binding assay as well as the inhibition activity against MAO enzymes using kynuramine deamination assay, while their antiprotozoal activity was evaluatedusing parasitelactate dehydrogenase serum assay (pLDH). Results: The phytochemical evaluation of the alcoholic extract of E.corallodendron flowers, afforded the isolation of an indole alkaloid Hypaphorine 1, a new flavonoid glucoside; Kaempferol-3-O-α-sophoroside 2 and three known flavonoid C-glycosides vis;, Neoschaftoside 3, Isoschaftoside 4 and Vicenin-II 5. Compounds 3 and 4 are reported for the first time from genus Erythrina. Compounds 4 and 5 showed significant antimalarial activity both with IC50 value 1.7µg/mL against (D6) strain and with IC50 1.4 and 1.1 µg/mL against (W2) strain, respectively. Compound 3 showed selective inhibition to MAO-B with IC50 value of 32.08 µM and selective index (SI) > 3.12. Conclusion: The significant antiplasmodial activity of compounds 4 and 5 correlated the known antimalarial activity of different Erythrina species to flavonoid C-glycosides, Also compounds 3 and 4 are position isomers but exhibited different response against MAO-B which gives indication about the selectivity pattern of the flavonoid C-glycosides with MAO-B receptor subtype.
方法:采用硅胶正相、反相RP-18、diaip -20、Sephadex LH-20进行连续柱层析(CC)分离。利用HR-ESI-MS、UV、1D和2D NMR对分离化合物进行了结构解析。结果:对花冠花醇提物进行了植物化学鉴定，分离出一种新的类黄酮苷-吲哚类生物碱Hypaphorine 1;山奈酚-3- o -α-槐苷2和三种已知的类黄酮c -糖苷vis;新谷草苷3、异谷草苷4和长春素- ii 5。化合物3和4为首次从赤藓属植物中分离得到。化合物4和5对(D6)和(W2)菌株的IC50分别为1.7µg/mL和1.4和1.1µg/mL，具有显著的抗疟活性。
{"title":"A Novel Compound and Biological Evaluation of Phytoconstituents Isolated from Erythrina corallodendron L. Flowers","authors":"M. Aboelmagd, A. Said, S. Ross, E. Haggag","doi":"10.21608/APRH.2018.3926.1059","DOIUrl":"https://doi.org/10.21608/APRH.2018.3926.1059","url":null,"abstract":"Objective: This study aimed at phytochemical investigation of the 70% alcoholic extract of Erythrina corallodendron L. flowers and biological evaluation of the isolated compounds for their activity as antiprotozoal drugs also evaluation the binding affinity to opioid and cannabinoid receptors as well as the inhibition activity against monoamine oxidase (MAO) enzymes. Method: The 70% alcoholic extract was subjected to successive column chromatographic (CC) separations using silica gel normal phase, reversed phase RP-18, Diaion HP-20, and Sephadex LH-20. The structural elucidation of the isolated compounds was achieved using HR-ESI-MS, UV, 1D and 2D NMR spectroscopic analysis. The isolated compounds were screened in vitro for the binding affinity to opioid and cannabinoid receptors using receptor binding assay as well as the inhibition activity against MAO enzymes using kynuramine deamination assay, while their antiprotozoal activity was evaluatedusing parasitelactate dehydrogenase serum assay (pLDH). Results: The phytochemical evaluation of the alcoholic extract of E.corallodendron flowers, afforded the isolation of an indole alkaloid Hypaphorine 1, a new flavonoid glucoside; Kaempferol-3-O-α-sophoroside 2 and three known flavonoid C-glycosides vis;, Neoschaftoside 3, Isoschaftoside 4 and Vicenin-II 5. Compounds 3 and 4 are reported for the first time from genus Erythrina. Compounds 4 and 5 showed significant antimalarial activity both with IC50 value 1.7µg/mL against (D6) strain and with IC50 1.4 and 1.1 µg/mL against (W2) strain, respectively. Compound 3 showed selective inhibition to MAO-B with IC50 value of 32.08 µM and selective index (SI) > 3.12. Conclusion: The significant antiplasmodial activity of compounds 4 and 5 correlated the known antimalarial activity of different Erythrina species to flavonoid C-glycosides, Also compounds 3 and 4 are position isomers but exhibited different response against MAO-B which gives indication about the selectivity pattern of the flavonoid C-glycosides with MAO-B receptor subtype.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"277 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88238881","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}
F. S. Elshaarawy, S. Mina, Nagwan M. Gabr, S. M. Abdel-Khalik, Rehab Kamel, H. Ibrahim, E. Haggag
Objectives: This study aimed to compare two Livistona species; Livistona decipiens Becc and Livistona australis Mart for their phenolic and carbohydrate contents and for their protective activity against ulcerative colitis. Methods: A high performance liquid chromatographic (HPLC) technique with inline connected to photo diode array detector (DAD) and electro array (EA) used for detection of the polyphenolic contents. Also HPLC with refractive index detection (HPLC-RI) was used to determine and to quantify carbohydrate contents before and after partial acid hydrolysis, using 0.2 N H2SO4, for 3 h at 100°C, for each of the defatted methanol extract concentrate. Protective activity against ulcerative colitis was evaluated by acetic acid inducing-ulcers method for both methanol extracts of both species. Results: Both investigated Livistona species are rich in polyphenolic constituents, showing a great similarity. The major flavonoid compound in both species was luteolin-6-C-arabinoside-8-C-glucoside and the major aglycone was acacetin, while the major phenolic acid in both species was ellagic acid. However there was a difference in the carbohydrate content between the two species, the main sugars, before hydrolysis, in L. decipiens were arabinose, mannose and sucrose, while the main sugars in L. australis were glucose, fructose and maltose. However, stachyose was the major polysaccharide obtained after partial acid hydrolysis. L. australis showed protective activity against ulcerative colitis in lower dose 500 mg/kg when compared to L. decipiens that only showed effectiveness at a doubled dose 1000 mg/kg. Conclusion: Both Livistona species have potential medicinal value being rich in polyphenolic and polysaccharide contents and having protective activity against ulcerative colitis.
目的:本研究旨在比较两个Livistona种;牛肉藤和牛肉藤的酚类和碳水化合物含量以及对溃疡性结肠炎的保护作用。方法:采用光电二极管阵列检测器(DAD)和电子阵列检测器(EA)相结合的高效液相色谱法(HPLC)检测多酚含量。采用高效液相色谱(HPLC)和折射率检测(HPLC- ri)测定了各脱脂甲醇提取物浓缩液在100°C下，用0.2 N H2SO4部分酸水解3 h后的碳水化合物含量。采用醋酸诱导溃疡法评价两种植物甲醇提取物对溃疡性结肠炎的保护作用。结果:两种植物均含有丰富的多酚类成分，具有很大的相似性。两种植物的主要类黄酮化合物为木犀草素-6- c -阿拉伯糖苷-8- c -葡萄糖苷，主要苷元为荆芥苷，主要酚酸为鞣花酸。但两种植物的碳水化合物含量存在差异，水解前的主要糖类为阿拉伯糖、甘露糖和蔗糖，而水解前的主要糖类为葡萄糖、果糖和麦芽糖。而水苏糖是经部分酸水解得到的主要多糖。与乳杆菌相比，南乳杆菌在低剂量500mg /kg时显示出对溃疡性结肠炎的保护作用，而乳杆菌只有在双倍剂量1000mg /kg时才显示出效果。结论:两种植物均含有丰富的多酚和多糖，对溃疡性结肠炎具有保护作用，具有潜在的药用价值。
{"title":"HPLC investigation of carbohydrates and phenolic constituents of Livistona decipiens and Livistona australis leaves and assessment of their ulceroprotective activity","authors":"F. S. Elshaarawy, S. Mina, Nagwan M. Gabr, S. M. Abdel-Khalik, Rehab Kamel, H. Ibrahim, E. Haggag","doi":"10.21608/APRH.2018.8068","DOIUrl":"https://doi.org/10.21608/APRH.2018.8068","url":null,"abstract":"Objectives: This study aimed to compare two Livistona species; Livistona decipiens Becc and Livistona australis Mart for their phenolic and carbohydrate contents and for their protective activity against ulcerative colitis. Methods: A high performance liquid chromatographic (HPLC) technique with inline connected to photo diode array detector (DAD) and electro array (EA) used for detection of the polyphenolic contents. Also HPLC with refractive index detection (HPLC-RI) was used to determine and to quantify carbohydrate contents before and after partial acid hydrolysis, using 0.2 N H2SO4, for 3 h at 100°C, for each of the defatted methanol extract concentrate. Protective activity against ulcerative colitis was evaluated by acetic acid inducing-ulcers method for both methanol extracts of both species. Results: Both investigated Livistona species are rich in polyphenolic constituents, showing a great similarity. The major flavonoid compound in both species was luteolin-6-C-arabinoside-8-C-glucoside and the major aglycone was acacetin, while the major phenolic acid in both species was ellagic acid. However there was a difference in the carbohydrate content between the two species, the main sugars, before hydrolysis, in L. decipiens were arabinose, mannose and sucrose, while the main sugars in L. australis were glucose, fructose and maltose. However, stachyose was the major polysaccharide obtained after partial acid hydrolysis. L. australis showed protective activity against ulcerative colitis in lower dose 500 mg/kg when compared to L. decipiens that only showed effectiveness at a doubled dose 1000 mg/kg. Conclusion: Both Livistona species have potential medicinal value being rich in polyphenolic and polysaccharide contents and having protective activity against ulcerative colitis.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"112 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79586400","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}
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