Pub Date : 2019-09-01DOI: 10.21608/ajps.2019.70231
A. Helal
Though clinicians once possessed a robust arsenal of antibiotics, many of these valuable therapeutic agents have fallen prey to the expanded resistance of pathogenic bacteria. Phenylthiazoles were reported previously as a new scaffold that possesses antibacterial activity against an array of clinically-relevant strains of multidrug-resistant staphylococci. Close inspection of the structure-activity-relationships (SAR) of phenylthiazoles revealed important structural features necessary for their antibacterial activity: a nitrogenous head and a lipophilic tail. Incorporating the nitrogenous part within an oxadiazole ring resulted in analogues with a prolonged half-life, while the biphenyl tail revealed the most potent analogue. In the present work, advantageous moieties have been combined together to generate new hybrid scaffolds of phenylpyridine with the objective of promoting new moieties enhancing both antimicrobial resistance activity and drug-like properties. Among the tested oxadiazolylbiphenylpyridines, derivatives 14 and 23 were identified as the most potent analogues with MIC values as low as 8 mg/mL on MRSA-US300 and other studied species.
{"title":"DESIGN AND SYNTHESIS OF NEW HETEROCYCLIC COMPOUNDS TO OVERCOME MICROBIAL RESISTANCE","authors":"A. Helal","doi":"10.21608/ajps.2019.70231","DOIUrl":"https://doi.org/10.21608/ajps.2019.70231","url":null,"abstract":"Though clinicians once possessed a robust arsenal of antibiotics, many of these valuable therapeutic agents have fallen prey to the expanded resistance of pathogenic bacteria. Phenylthiazoles were reported previously as a new scaffold that possesses antibacterial activity against an array of clinically-relevant strains of multidrug-resistant staphylococci. Close inspection of the structure-activity-relationships (SAR) of phenylthiazoles revealed important structural features necessary for their antibacterial activity: a nitrogenous head and a lipophilic tail. Incorporating the nitrogenous part within an oxadiazole ring resulted in analogues with a prolonged half-life, while the biphenyl tail revealed the most potent analogue. In the present work, advantageous moieties have been combined together to generate new hybrid scaffolds of phenylpyridine with the objective of promoting new moieties enhancing both antimicrobial resistance activity and drug-like properties. Among the tested oxadiazolylbiphenylpyridines, derivatives 14 and 23 were identified as the most potent analogues with MIC values as low as 8 mg/mL on MRSA-US300 and other studied species.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82168143","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 : 2019-09-01DOI: 10.21608/ajps.2019.70229
Emanwel A. Aziz
Unexplained infertility remains a frustrating problem for the clinician and a distressing condition for the affected couples. Unexplained infertility has been defined as it is the infertility which no cause can be detected to explain the fertility problem in spite of conventional investigation for both partners. to evaluate the Relation between Vasculer Endothelial Growth Factor (VEGF), sub endometrial wave like movement (JZC) and sub endometrial blood flow detected by 3D as indicator of uterine receptivity in spontnous and stimulated cycles in unexplained infertile women. The sample size was calculated according to Jain et al., (2015) who reported that the level of VEGF in fertile women was 324±20.50 and in infertile women the level was found to be 107.33±24.96. So, by adjusting the confidence interval to 95%, the power of the test to 90%, the ratio between groups was adjusted to 1:2. The sample size was found to be 96 cases divided into 32 controls (fertile women "group C") and 64 cases was divided also into two groups (infertile women with un-stimulated cycle (group A) and 32 cases infertile women with stimulated cycles chlomiphene citrate (group B). This study was performed in the department and out patient clinic of obstetrics and gynecology at Al Zahraa university hospital from September 2016 to September 2019 on ninety six participants. Ninety six participants who qualified the exclusion and inclusion criteria were enrolled in this study: thirty two participants categorized in group (A) diagnosed as unexplained infertility with unstimulated cycle, thirty two participants categorized in group (B) diagnesd as unexplained infertility with stimulated cycle (clomiphene citrate) and thirty two participants normal fertile women categorized in group (C) seeking contraceptive means (control group). All participants on day 21 -22 day of cycle underwent in to 3D transvaginal ultrasound to detect subendometrial blood flow, subendometial wave like movement and on the same day venous blood sample was taken to measure VEGF.
不明原因的不孕症对临床医生来说仍然是一个令人沮丧的问题，对受影响的夫妇来说也是一个令人痛苦的状况。不明原因不孕症被定义为尽管对伴侣双方进行了常规调查，但仍无法发现原因来解释生育问题的不孕症。目的探讨3D检测血管内皮生长因子(VEGF)、子宫内膜下波样运动(JZC)和子宫内膜下血流与不明原因不孕症女性自发性和受激周期子宫容受性的关系。样本量根据Jain et al.，(2015)报道的可育女性VEGF水平为324±20.50，不可育女性VEGF水平为107.33±24.96计算。因此，通过将置信区间调整为95%，检验的功效调整为90%，组间比例调整为1:2。本研究于2016年9月至2019年9月在Al Zahraa大学附属医院妇产科门诊和门诊部进行，96例患者被分为32例对照组(有生育能力的女性“C组”)，64例患者被分为两组(无刺激周期的不孕女性(A组)和32例有刺激周期的枸橼酸氯米芬不孕女性(B组))。本研究纳入96名符合排除和纳入标准的受试者:32名诊断为不明原因不孕症伴非刺激周期的受试者分为(A)组，32名诊断为不明原因不孕症伴刺激周期的受试者分为(B)组(克罗米芬柠檬酸盐)，32名正常生育的女性分为(C)组，寻求避孕方法(对照组)。所有受试者在月经周期第21 -22天均行3次三维阴道超声检测子宫内膜下血流、子宫内膜下波样运动，并于当日取静脉血检测VEGF。
{"title":"RELATION BETWEEN VASCULER ENDOTHELIAL GROWTH FACTOR AND 3D DOPPLER ULTRASONOGRAPHY WITH SUBENDOMETRAIL WAVE LIKE MOVEMENT IN CASE OF UNEXPLAINED INFERTILITY","authors":"Emanwel A. Aziz","doi":"10.21608/ajps.2019.70229","DOIUrl":"https://doi.org/10.21608/ajps.2019.70229","url":null,"abstract":"Unexplained infertility remains a frustrating problem for the clinician and a distressing condition for the affected couples. Unexplained infertility has been defined as it is the infertility which no cause can be detected to explain the fertility problem in spite of conventional investigation for both partners. to evaluate the Relation between Vasculer Endothelial Growth Factor (VEGF), sub endometrial wave like movement (JZC) and sub endometrial blood flow detected by 3D as indicator of uterine receptivity in spontnous and stimulated cycles in unexplained infertile women. The sample size was calculated according to Jain et al., (2015) who reported that the level of VEGF in fertile women was 324±20.50 and in infertile women the level was found to be 107.33±24.96. So, by adjusting the confidence interval to 95%, the power of the test to 90%, the ratio between groups was adjusted to 1:2. The sample size was found to be 96 cases divided into 32 controls (fertile women \"group C\") and 64 cases was divided also into two groups (infertile women with un-stimulated cycle (group A) and 32 cases infertile women with stimulated cycles chlomiphene citrate (group B). This study was performed in the department and out patient clinic of obstetrics and gynecology at Al Zahraa university hospital from September 2016 to September 2019 on ninety six participants. Ninety six participants who qualified the exclusion and inclusion criteria were enrolled in this study: thirty two participants categorized in group (A) diagnosed as unexplained infertility with unstimulated cycle, thirty two participants categorized in group (B) diagnesd as unexplained infertility with stimulated cycle (clomiphene citrate) and thirty two participants normal fertile women categorized in group (C) seeking contraceptive means (control group). All participants on day 21 -22 day of cycle underwent in to 3D transvaginal ultrasound to detect subendometrial blood flow, subendometial wave like movement and on the same day venous blood sample was taken to measure VEGF.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75403494","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 : 2019-03-01DOI: 10.21608/ajps.2019.64098
M. Bakr
EFFECT OF POLYPHENOLIC COMPOUNDS ISOLATED FROM NANDINA DOMESTICA. THUNB. LEAVES GROWING IN EGYPT AGAINST INDUCED ECZEMA IN MICE.
家蝇多酚类化合物的分离作用。研究。生长在埃及的叶子对抗小鼠诱发湿疹。
{"title":"EFFECT OF POLYPHENOLIC COMPOUNDS ISOLATED FROM NANDINA DOMESTICA. THUNB. LEAVES GROWING IN EGYPT AGAINST INDUCED ECZEMA IN MICE.","authors":"M. Bakr","doi":"10.21608/ajps.2019.64098","DOIUrl":"https://doi.org/10.21608/ajps.2019.64098","url":null,"abstract":"EFFECT OF POLYPHENOLIC COMPOUNDS ISOLATED FROM NANDINA DOMESTICA. THUNB. LEAVES GROWING IN EGYPT AGAINST INDUCED ECZEMA IN MICE.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81287659","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 : 2019-03-01DOI: 10.21608/ajps.2019.64113
A. Metwaly
In this study, a total of six endophytic fungi have been isolated from Vinca rosea (Apocynaceae) leaves growing in Egypt. The isolated fungi were identified morphologically and microscopically up to species to be; Alternaria phragmospora, Aspergillus awamori, Penicillium duclauxii, Penicillium melinii, Nigrospora sphaerica and Mucor ramosissimus. The extracts of the all identified fungi were screened biologically for antileukemic, cytotoxic, antimalarial, antileishmanial, antimicrobial, antioxidant and anti-inflammatory activities as well as for cannabinoid and opioid receptor binding affinities. Out of the six examined fungal extracts four exhibited promising antimalarial activities, four showed modeate antileukemic activities and two of them exhibited cytotoxic activities, three showed antioxidant activities, three exhibited anti-inflammatory activities, and the only one showed an antifungal activity. Alternaria phragmospora was the most active antimalarial agent inhibiting Plasmodium falciparum D6 and W2 clones with IC50 values of 1.9 and 2.1 μg/mL, respectively. Alternaria phragmospora extractwas subjected to liquid-liquid partition using 90% MeOH, hexane then BuOH and H2O. MeOH and BuOH fractions exhibited strong activities against Plasmodium falciparum D6 clone with IC50 values of 1.3 and 28 μg/mL and W2 clone with IC50 values of 1.4 and 28 μg/mL, respectively. These results may be an excellent opportunity to get a new antimalarial drug derived from endophytic fungi.
{"title":"COMPARATIVE BIOLOGICAL EVALUATION OF SIX ENDOPHYTIC FUNGI ISOLATED FROM VINCA ROSEA LEAVES","authors":"A. Metwaly","doi":"10.21608/ajps.2019.64113","DOIUrl":"https://doi.org/10.21608/ajps.2019.64113","url":null,"abstract":"In this study, a total of six endophytic fungi have been isolated from Vinca rosea (Apocynaceae) leaves growing in Egypt. The isolated fungi were identified morphologically and microscopically up to species to be; Alternaria phragmospora, Aspergillus awamori, Penicillium duclauxii, Penicillium melinii, Nigrospora sphaerica and Mucor ramosissimus. The extracts of the all identified fungi were screened biologically for antileukemic, cytotoxic, antimalarial, antileishmanial, antimicrobial, antioxidant and anti-inflammatory activities as well as for cannabinoid and opioid receptor binding affinities. Out of the six examined fungal extracts four exhibited promising antimalarial activities, four showed modeate antileukemic activities and two of them exhibited cytotoxic activities, three showed antioxidant activities, three exhibited anti-inflammatory activities, and the only one showed an antifungal activity. Alternaria phragmospora was the most active antimalarial agent inhibiting Plasmodium falciparum D6 and W2 clones with IC50 values of 1.9 and 2.1 μg/mL, respectively. Alternaria phragmospora extractwas subjected to liquid-liquid partition using 90% MeOH, hexane then BuOH and H2O. MeOH and BuOH fractions exhibited strong activities against Plasmodium falciparum D6 clone with IC50 values of 1.3 and 28 μg/mL and W2 clone with IC50 values of 1.4 and 28 μg/mL, respectively. These results may be an excellent opportunity to get a new antimalarial drug derived from endophytic fungi.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"38 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82063732","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 : 2019-03-01DOI: 10.21608/ajps.2019.64111
A. Metwaly
In this study, a total of four endophytic fungi have been isolated from Nigella sativa (Ranunculaceae) seeds growing in Egypt. The isolated fungi were identified morphologically and microscopically up to species to be; Alternaria pluriseptata, Aspergillus tubingensis, Aspergillus parasiticus and Eurotium pseudoglaucus. The extracts of the all identified fungi were screened biologically for antileukemic, cytotoxic, antimalarial, antileishmanial, antimicrobial, antioxidant and anti-inflammatory activities as well as for cannabinoid and opioid receptor binding affinities. All the examined fungal extracts showed good antileukemic activities with Ic50 values ranging from 0.025 to 0.8 µg/ml, while two of them showed cytotoxic activities against Pig kidney epithelial (LLC-PK1) cells. Two fungal extracts exhibited antimalarial activities, three showed antioxidant activities and two exhibited anti-inflammatory activities
{"title":"COMPARATIVE BIOLOGICAL EVALUATION OF FOUR ENDOPHYTIC FUNGI ISOLATED FROM NIGELLA SATIVA SEEDS","authors":"A. Metwaly","doi":"10.21608/ajps.2019.64111","DOIUrl":"https://doi.org/10.21608/ajps.2019.64111","url":null,"abstract":"In this study, a total of four endophytic fungi have been isolated from Nigella sativa (Ranunculaceae) seeds growing in Egypt. The isolated fungi were identified morphologically and microscopically up to species to be; Alternaria pluriseptata, Aspergillus tubingensis, Aspergillus parasiticus and Eurotium pseudoglaucus. The extracts of the all identified fungi were screened biologically for antileukemic, cytotoxic, antimalarial, antileishmanial, antimicrobial, antioxidant and anti-inflammatory activities as well as for cannabinoid and opioid receptor binding affinities. All the examined fungal extracts showed good antileukemic activities with Ic50 values ranging from 0.025 to 0.8 µg/ml, while two of them showed cytotoxic activities against Pig kidney epithelial (LLC-PK1) cells. Two fungal extracts exhibited antimalarial activities, three showed antioxidant activities and two exhibited anti-inflammatory activities","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73080316","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 : 2019-03-01DOI: 10.21608/ajps.2019.64102
S. Sallam
This study was conducted duringtwo successive seasons of 2014-2015 and 2015-2016 at Biotechnology Department, Phytochemistry Department and Farm of Applied Research Center of Medicinal Plants (ARCMP) affiliated to the National Organization for Drug Control And Research (NODCAR). The present work aimed to investigate the effect of inoculation Apium graveolens L. seeds with arbuscular mycorrhizal fungi (my) and/or microbein (mi) biofertilizer and foliar spray plants with Thidiazuron (TDZ) combined with chemical fertilizer at half or full dose of NPK on number of spores Am fungi (kg soil-1), AM fungi colonization , enzymatic activities (dehydrogenase activity [µg TPF/g dry soil/day] & Nitrogenase activity [nmol C2H4/g rhizosphere/ hour]), growth parameters (fresh weight of shoots per plant (g), fresh weight of roots per plant (g), dry weight of shoots per plant (g), dry weight of roots per plant (g), Plant height (cm), number of umbel per plant [at full flowering stage] & dry weight of fruits per plant [at harvest stage]) and chemical composition (plant pigments [chlorophyll a, chlorophyll b and carotenoides], macro elements content (%), total carbohydrates, and crude protein). The results in both seasons showed that, the highest values of number of AM fungi spores (kg soil-1) in celery (Apium graveolens L.) roots, AM fungi colonization %, enzymatic activities, growth parametersand chemical composition obtained at inoculating seeds with mixture of mycorrhizal and mycrobein at full dose of NPK.
{"title":"EFFECT OF CHEMICAL FERTILIZATION, BIOFERTILIZER AND THIDIAZURON ON GROWTH AND YIELD OF CELERY (APIUM GRAVEOLENS L.) PLANT.","authors":"S. Sallam","doi":"10.21608/ajps.2019.64102","DOIUrl":"https://doi.org/10.21608/ajps.2019.64102","url":null,"abstract":"This study was conducted duringtwo successive seasons of 2014-2015 and 2015-2016 at Biotechnology Department, Phytochemistry Department and Farm of Applied Research Center of Medicinal Plants (ARCMP) affiliated to the National Organization for Drug Control And Research (NODCAR). The present work aimed to investigate the effect of inoculation Apium graveolens L. seeds with arbuscular mycorrhizal fungi (my) and/or microbein (mi) biofertilizer and foliar spray plants with Thidiazuron (TDZ) combined with chemical fertilizer at half or full dose of NPK on number of spores Am fungi (kg soil-1), AM fungi colonization , enzymatic activities (dehydrogenase activity [µg TPF/g dry soil/day] & Nitrogenase activity [nmol C2H4/g rhizosphere/ hour]), growth parameters (fresh weight of shoots per plant (g), fresh weight of roots per plant (g), dry weight of shoots per plant (g), dry weight of roots per plant (g), Plant height (cm), number of umbel per plant [at full flowering stage] & dry weight of fruits per plant [at harvest stage]) and chemical composition (plant pigments [chlorophyll a, chlorophyll b and carotenoides], macro elements content (%), total carbohydrates, and crude protein). The results in both seasons showed that, the highest values of number of AM fungi spores (kg soil-1) in celery (Apium graveolens L.) roots, AM fungi colonization %, enzymatic activities, growth parametersand chemical composition obtained at inoculating seeds with mixture of mycorrhizal and mycrobein at full dose of NPK.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88430675","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 : 2019-03-01DOI: 10.21608/ajps.2019.64115
Y. Haddad
Radiotherapy is one of the most important strategies in cancer treatment. Seriously, radiotherapy resulted in premature ovarian failure (POF) and infertility, Radiotherapy depends on the generation of reactive oxygen species (ROS) in cancer cells as a result of water radiolysis leading to induction of oxidative stress and diminution of antioxidant defense mechanisms and within this process, healthy tissues are also damaged. Moreover, germ cells seem to be much more susceptible to oxidative stress induced by radiotherapy than somatic cells. Seriously, ROS generated by ionizing radiation are capable of inducing tissue apoptosis by direct and indirect pathways leading to oxidative damage of cellular macromolecules (mainly DNA, proteins and lipids). Curiously, apoptosis was identified as the mechanism responsible for oocyte loss caused by radiotherapy. Soybeans products contain high amounts of isoflavones known as soy phytoestrogens which act as natural selective estrogen receptor modulators (SERMs). The most prominant phytoestrogen in soybean is genistein (GEN), which shows estrogenic properties through estrogen receptor beta (ER-β) binding. GEN has different pharmacological properties through its chemoprotective activity against cancers and cardiovascular diseases. GEN was also reported to protect against acute myelotoxicity, intestinal, lung, and testicular injuries-induced by radiation. The radioprotective effects of GEN was attributed to its antioxidant, anti-apoptotic, anti-inflammatoryand anti-fibrotic activities. Concerning its effects on the ovaries, previous report confirmed the protective effect of GEN against ovarian carcinogenesis. Also, GEN slowed down follicular development, considerably improving the ovarian follicular stock and extend the ovarian lifespan. In this context, GEN was documented to delay ovarian ageing and prolong ovarian reproductive life, besides its protective effect against chemotherapy and radiotherapy induced ovarian toxicity.
{"title":"GENISTEIN AS RADIOPROTECTIVE AGAINST PREMATURE OVARIAN FAILURE","authors":"Y. Haddad","doi":"10.21608/ajps.2019.64115","DOIUrl":"https://doi.org/10.21608/ajps.2019.64115","url":null,"abstract":"Radiotherapy is one of the most important strategies in cancer treatment. Seriously, radiotherapy resulted in premature ovarian failure (POF) and infertility, Radiotherapy depends on the generation of reactive oxygen species (ROS) in cancer cells as a result of water radiolysis leading to induction of oxidative stress and diminution of antioxidant defense mechanisms and within this process, healthy tissues are also damaged. Moreover, germ cells seem to be much more susceptible to oxidative stress induced by radiotherapy than somatic cells. Seriously, ROS generated by ionizing radiation are capable of inducing tissue apoptosis by direct and indirect pathways leading to oxidative damage of cellular macromolecules (mainly DNA, proteins and lipids). Curiously, apoptosis was identified as the mechanism responsible for oocyte loss caused by radiotherapy. Soybeans products contain high amounts of isoflavones known as soy phytoestrogens which act as natural selective estrogen receptor modulators (SERMs). The most prominant phytoestrogen in soybean is genistein (GEN), which shows estrogenic properties through estrogen receptor beta (ER-β) binding. GEN has different pharmacological properties through its chemoprotective activity against cancers and cardiovascular diseases. GEN was also reported to protect against acute myelotoxicity, intestinal, lung, and testicular injuries-induced by radiation. The radioprotective effects of GEN was attributed to its antioxidant, anti-apoptotic, anti-inflammatoryand anti-fibrotic activities. Concerning its effects on the ovaries, previous report confirmed the protective effect of GEN against ovarian carcinogenesis. Also, GEN slowed down follicular development, considerably improving the ovarian follicular stock and extend the ovarian lifespan. In this context, GEN was documented to delay ovarian ageing and prolong ovarian reproductive life, besides its protective effect against chemotherapy and radiotherapy induced ovarian toxicity.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"117 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80380430","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 : 2019-03-01DOI: 10.21608/ajps.2019.64110
G. Mohamed
Pseudomonas aeruginosa was the most frightening pathogen that emergence in health facilities with increasing antibiotic resistance. Nanoparticles have reported as non-antibiotic therapeutic agents, that are highly effective in the treatment of P. aeruginosa infections. Combination therapy of nanoparticles and antibiotics considered an alternative therapeutic approach for restoring antibiotic activity. To achieve that goal, we used the synthetic silver nanoparticles in a combined form with ciprofloxacin against MDR P. aeruginosa. Fifty bacterial isolates that collected from different infection sites were confirmed as P. aeruginosa by detection of algD gene and Exotoxin A genes. Antibiotic sensitivity of P. aeruginosa strains was assessed by single diskdiffusion method. The most prevelant phenotype among P. aeruginosa were recorded. The synthetic nanoparticles AgNPs and ZnONPs were tested against all P. aeruginosa strains. minimum inhibitory conc (MIC) of ciprofloxacin and AgNPS was determined using microdilution method for 24 selected P. aeruginosa strains and in the range from 160-1280, 6-12mg/l, respectively. In vitro, the synergistic activity of ciprofloxacin and AgNPs was achieved in all combinations. Our finding approved that combination therapy depend on using nanoparticles considered a promising tool used to restore the activity of antibiotics.
{"title":"COMBINATION OF CIPROFLOXACIN AND SILVER NANOPARTICLES FOR TREATMENT OF MULTI-DRUG RESISTANT PSEUDOMONAS AERUGINOSA IN EGYPT","authors":"G. Mohamed","doi":"10.21608/ajps.2019.64110","DOIUrl":"https://doi.org/10.21608/ajps.2019.64110","url":null,"abstract":"Pseudomonas aeruginosa was the most frightening pathogen that emergence in health facilities with increasing antibiotic resistance. Nanoparticles have reported as non-antibiotic therapeutic agents, that are highly effective in the treatment of P. aeruginosa infections. Combination therapy of nanoparticles and antibiotics considered an alternative therapeutic approach for restoring antibiotic activity. To achieve that goal, we used the synthetic silver nanoparticles in a combined form with ciprofloxacin against MDR P. aeruginosa. Fifty bacterial isolates that collected from different infection sites were confirmed as P. aeruginosa by detection of algD gene and Exotoxin A genes. Antibiotic sensitivity of P. aeruginosa strains was assessed by single diskdiffusion method. The most prevelant phenotype among P. aeruginosa were recorded. The synthetic nanoparticles AgNPs and ZnONPs were tested against all P. aeruginosa strains. minimum inhibitory conc (MIC) of ciprofloxacin and AgNPS was determined using microdilution method for 24 selected P. aeruginosa strains and in the range from 160-1280, 6-12mg/l, respectively. In vitro, the synergistic activity of ciprofloxacin and AgNPs was achieved in all combinations. Our finding approved that combination therapy depend on using nanoparticles considered a promising tool used to restore the activity of antibiotics.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"76 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84196153","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 : 2019-03-01DOI: 10.21608/ajps.2019.64108
M. Zaki
Phytochemical investigations of Dovyalis caffra (leaves and twigs) revealed a new dovyalicin-type spermidine alkaloid, named Dovyalicin G (1); which was identified as (E)-N-(4-(1,5-diazocan-1-yl)butyl)-N-methyltetradec-2-enamide, along with previously isolated β-sitosterol (2) and Hentriacontan-1-ol (3). The structures were established using ESI/MS, EI/MS, 1H NMR, APT NMR, and two-dimensional NMR experiments. In addition to the biological studies of the different plant extracts including cytotoxicity, topoisomerase II inhibition, antimicrobial, and in-vitro anti-inflammatory activities. Screening of 5-lipoxygenase (5-LOX) and Cyclooxygenase-1 (COX-1) and -2 (COX-2) inhibition to evaluate anti-inflammatory activity were performed. The alkaloid fraction showed good antimicrobial activity against studied microorganisms and remarkable cytotoxic activities against studied cell lines (Besides, total methanolic and petroleum ether extracts). The total methanolic extract showed strong COX- inhibition activity and selectivity toward COX-2, comparing with celecoxib.
对香鸽(Dovyalis caffra)叶片和细枝的植物化学研究发现了一种新的Dovyalicin型亚精胺生物碱，命名为Dovyalicin G (1);鉴定为(E)- n-(4-(1,5-重氮烷-1-基)丁基)- n-甲基四tradec-2-enamide，以及先前分离的β-谷甾醇(2)和Hentriacontan-1-ol(3)。通过ESI/MS、EI/MS、1H NMR、APT NMR和二维NMR实验建立了结构。此外，不同植物提取物的生物学研究包括细胞毒性、拓扑异构酶II抑制、抗菌和体外抗炎活性。筛选5-脂氧合酶(5-LOX)和环氧合酶-1 (COX-1)和-2 (COX-2)抑制物以评估抗炎活性。生物碱部分对所研究的微生物具有良好的抑菌活性，对所研究的细胞系具有显著的细胞毒活性(此外，总甲醇和石油醚提取物)。与塞来昔布相比，总甲醇提取物对COX-2具有较强的抑制活性和选择性。
{"title":"NEW DOVYALICIN-TYPE SPERMIDINE ALKALOID FROM DOVYALIS CAFFRA (WARB.); FAMILY: SALICACEAE, CULTIVATED IN EGYPT","authors":"M. Zaki","doi":"10.21608/ajps.2019.64108","DOIUrl":"https://doi.org/10.21608/ajps.2019.64108","url":null,"abstract":"Phytochemical investigations of Dovyalis caffra (leaves and twigs) revealed a new dovyalicin-type spermidine alkaloid, named Dovyalicin G (1); which was identified as (E)-N-(4-(1,5-diazocan-1-yl)butyl)-N-methyltetradec-2-enamide, along with previously isolated β-sitosterol (2) and Hentriacontan-1-ol (3). The structures were established using ESI/MS, EI/MS, 1H NMR, APT NMR, and two-dimensional NMR experiments. In addition to the biological studies of the different plant extracts including cytotoxicity, topoisomerase II inhibition, antimicrobial, and in-vitro anti-inflammatory activities. Screening of 5-lipoxygenase (5-LOX) and Cyclooxygenase-1 (COX-1) and -2 (COX-2) inhibition to evaluate anti-inflammatory activity were performed. The alkaloid fraction showed good antimicrobial activity against studied microorganisms and remarkable cytotoxic activities against studied cell lines (Besides, total methanolic and petroleum ether extracts). The total methanolic extract showed strong COX- inhibition activity and selectivity toward COX-2, comparing with celecoxib.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"158 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82921260","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 : 2019-03-01DOI: 10.21608/ajps.2019.64106
A. Adel
Liver fibrosis is a common health problem that is associated with mortality and morbidity worldwide. The inappropriate tissue repair of damaged liver results in over-synthesis and deposition of fibrillar collagen. It is usually associated with progressive pathological and biochemical changes that ultimately lead to structural and metabolic abnormalities and hepatic scarring. If not properly treated, liver fibrosis may develop to cirrhosis and hepatocellular carcinoma within few years. Blocking this progression, therefore, could be an effective and potential strategy for survival. The only effective approach to treating advanced liver fibrosis is transplantation. Understanding its etiology and pathophysiology, however, could help to investigate therapeutic pathophysiology based treatment of liver fibrogenesis. Recently several promising natural based treatment methods interfering with cytokines signaling pathway involved in fibrogenesis have been investigated offering new potential therapeutic intervention. The aim of the present updated review is to identify the natural antifibrotic options that have been studied in animal models with liver fibrosis for the treatment of this pathological conditions enabling prevention or at least regression of its progression.
{"title":"NATURALLY DERIVED COMPOUNDS USED FOR PREVENTION OR REGRESSION OF EXPERIMENTALLY INDUCED LIVER FIBROSIS","authors":"A. Adel","doi":"10.21608/ajps.2019.64106","DOIUrl":"https://doi.org/10.21608/ajps.2019.64106","url":null,"abstract":"Liver fibrosis is a common health problem that is associated with mortality and morbidity worldwide. The inappropriate tissue repair of damaged liver results in over-synthesis and deposition of fibrillar collagen. It is usually associated with progressive pathological and biochemical changes that ultimately lead to structural and metabolic abnormalities and hepatic scarring. If not properly treated, liver fibrosis may develop to cirrhosis and hepatocellular carcinoma within few years. Blocking this progression, therefore, could be an effective and potential strategy for survival. The only effective approach to treating advanced liver fibrosis is transplantation. Understanding its etiology and pathophysiology, however, could help to investigate therapeutic pathophysiology based treatment of liver fibrogenesis. Recently several promising natural based treatment methods interfering with cytokines signaling pathway involved in fibrogenesis have been investigated offering new potential therapeutic intervention. The aim of the present updated review is to identify the natural antifibrotic options that have been studied in animal models with liver fibrosis for the treatment of this pathological conditions enabling prevention or at least regression of its progression.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90792734","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：