Tamoxifen Citrate (TC) is the standard endocrine therapy for estrogen receptor (ER) positive breast cancer. TC is a selective estrogen receptor modulator (SERM) whose estrogenic properties in uterus have been linked to increased side effects like blood clots, endometrial polyps and cancer. Therefore, significant amount of research has been carried out to develop tamoxifen loaded nano-formulations with a preferential accumulation in tumor tissue rather than healthy tissues. Synthetic high-density lipoproteins (sHDL) are novel nanocarriers with inherent active-targeting ability towards tumor cells through the ligand–receptor interaction between apolipoprotein A-I (Apo A-I) and scavenger receptor class B type I (SR-BI) overexpressed in various malignant cells. The current study was carried out to investigate whether encapsulation of TC in sHDL could improve the cytotoxic effect of TC against malignant cells. For this purpose, the cytotoxicity of TC-sHDL was evaluated in MCF-7 cell line in vitro. MTT assay demonstrated the increased cytotoxicity of TC-sHDL against cancer cells as compared with the cytotoxic effect of the free drug.
{"title":"Tamoxifen Citrate- loaded synthetic high-density lipoproteins: Assessment of cellular toxicity in breast cancer cells","authors":"Ameerah A. Radhi, Wedad K. Ali, Fitua Al-Saedi","doi":"10.32947/ajps.v23i1.987","DOIUrl":"https://doi.org/10.32947/ajps.v23i1.987","url":null,"abstract":"Tamoxifen Citrate (TC) is the standard endocrine therapy for estrogen receptor (ER) positive breast cancer. TC is a selective estrogen receptor modulator (SERM) whose estrogenic properties in uterus have been linked to increased side \u0000effects like blood clots, endometrial polyps and cancer. Therefore, significant amount of research has been carried out to develop tamoxifen loaded nano-formulations with a preferential accumulation in tumor tissue rather than healthy tissues. \u0000Synthetic high-density lipoproteins (sHDL) are novel nanocarriers with inherent active-targeting ability towards tumor cells through the ligand–receptor interaction between apolipoprotein A-I (Apo A-I) and scavenger receptor class B type I (SR-BI) overexpressed in various malignant cells. The current study was carried out to investigate whether encapsulation of TC in sHDL could improve the cytotoxic effect of TC against malignant cells. For this purpose, the cytotoxicity of TC-sHDL was evaluated in MCF-7 cell line in vitro. MTT assay demonstrated the increased cytotoxicity of TC-sHDL against cancer cells as compared with the cytotoxic effect of the free drug.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"151 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76795930","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}
A simple, accurate and rapid method was developed for routine determination of trace elements in blood serum. The method based on the direct determination for Cr, Se, Ge, and V in hypothyroidism patients before therapy. By using atomic absorption spectrometry with graphite surface coated and uncoated pyrolysis GF-AAS, and a mixture of palladium nitrate and magnesium nitrate as the matrix modifier, with deuterium background correction and no sample pretreatment except dilution was necessary. This permitted direct determination hence the risk of sample contamination was reduced. Further, the use of graphite surface-coated GF-AAS decreased the ashing and atomization temperatures of Cr, Ge, and V to values that were lesser than the corresponding values obtained using uncoated pyrolysis GF-AAS, by 100°C; in case of Se, the atomization temperature decreased to a value that was 200°C lesser than that obtained using uncoated pyrolysis GF-AAS. A mixture of (3µL) palladium nitrate, and (2µL) magnesium nitrate was successfully applied to improve the sensitivity, reproducibility, recovery, limit of detection and the accuracy of the measurements. The correlation coefficients of the calibration curves of Cr, Se, Ge, and V were found to be (0.9999, 0.9999, 0.9995 and 0.9999) respectively, the relative standard deviation of the measurements for Cr, Se, Ge and V were (0.027, 0.075, 0.054 and 0.068) respectively. The statistical analysis of the acquired data showed acceptable accuracy. The analyses thus performed indicated that the levels of serum trace elements Cr, Se, Ge, and V in hypothyroidism patients were lower than those in the control group.
{"title":"Determination of Cr, Se, Ge, and V in Hypothyroidism Patients by Using Graphite Furnace Atomic Absorption Spectrometry and mixture matrix modification","authors":"Halah Hamid Hammadi","doi":"10.32947/ajps.v23i1.986","DOIUrl":"https://doi.org/10.32947/ajps.v23i1.986","url":null,"abstract":"A simple, accurate and rapid method was developed for routine determination of trace elements in blood serum. The method based on the direct determination for Cr, Se, Ge, and V in hypothyroidism patients before therapy. By using atomic absorption spectrometry with graphite surface coated and uncoated pyrolysis GF-AAS, and a mixture of palladium nitrate and magnesium nitrate as the matrix modifier, with deuterium background correction and no sample pretreatment except dilution was necessary. This permitted direct determination hence the risk of sample contamination was reduced. Further, the use of graphite surface-coated GF-AAS decreased the ashing and atomization temperatures of Cr, Ge, and V to values that were lesser than the corresponding values obtained using uncoated pyrolysis GF-AAS, by 100°C; in case of Se, the atomization temperature decreased to a value that was 200°C lesser than that obtained using uncoated pyrolysis GF-AAS. \u0000A mixture of (3µL) palladium nitrate, and (2µL) magnesium nitrate was successfully applied to improve the sensitivity, reproducibility, recovery, limit of detection and the accuracy of the measurements. The correlation coefficients of the calibration curves of Cr, Se, Ge, and V were found to be (0.9999, 0.9999, 0.9995 and 0.9999) respectively, the relative standard deviation of the measurements for Cr, Se, Ge and V were (0.027, 0.075, 0.054 and 0.068) respectively. The statistical analysis of the acquired data showed acceptable accuracy. The analyses thus performed indicated that the levels of serum trace elements Cr, Se, Ge, and V in hypothyroidism patients were lower than those in the control group.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84396476","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}
Ola Ali Nassr, Mohammed Mahmood Mohammed, Hind abdulkhaliq Showman
Background: Psychiatric symptoms are common during pregnancy, potentially leading to an increased risk of adverse birth outcomes. Studies assessing the impact of depression and/or anxiety on adverse birth outcomes in Iraq are currently lacking. This study aims to determine whether depression and/or anxiety is independently associated with preterm birth (PTB) and low birth weight (LBW). Methods: A prospective cohort study included 352 pregnant women from outpatient clinics of Al-Yarmouk hospital and private clinics in Baghdad, Iraq from March 2021 to February 2022 using a convenience sampling. They were screened for depression using Edinburgh Postnatal Depression Scale (EPDS) during pregnancy and followed up to assess adverse birth outcomes. Multivariable logistic regression was used to determine predictors associated with adverse birth outcomes. Results: The prevalence of PTB and LBW was 7.7% and 11.6%, respectively. After adjustment of all potential sociodemographic, clinical and obstetric confounders, depression was independently associated with giving birth to LBW neonate (odd ratio (OR):3.64; 95% confidence interval (CI) 1.70, 7.79), but not PTB. Prevalence of LBW in depressed was 21.2% compared to 7.7% for non-depressed. LBW was also associated with a history of LBW and PTB. In contrast, anxiety did not seem to affect birth outcomes. Conclusion: Depression during pregnancy, regardless of the trimester, is independently associated with a higher likelihood of giving birth to LBW neonates (OR: 3.64; 95% CI 1.70, 7.79). Effective interventions that target maternal depression are vital to decrease morbidity and mortality associated with LBW.
背景:精神症状在怀孕期间很常见，可能导致不良出生结局的风险增加。目前缺乏评估伊拉克抑郁和/或焦虑对不良出生结果影响的研究。本研究旨在确定抑郁和/或焦虑是否与早产(PTB)和低出生体重(LBW)独立相关。方法:前瞻性队列研究纳入了2021年3月至2022年2月期间来自伊拉克巴格达Al-Yarmouk医院门诊和私人诊所的352名孕妇。她们在怀孕期间使用爱丁堡产后抑郁量表(EPDS)进行抑郁筛查，并随访评估不良分娩结果。使用多变量逻辑回归来确定与不良出生结局相关的预测因素。结果:PTB和LBW患病率分别为7.7%和11.6%。在对所有潜在的社会人口统计学、临床和产科混杂因素进行调整后，抑郁症与LBW新生儿的出生独立相关(奇数比(OR):3.64;95%置信区间(CI) 1.70, 7.79)，但PTB除外。抑郁症患者的LBW患病率为21.2%，而非抑郁症患者为7.7%。LBW还与LBW和PTB病史相关。相比之下，焦虑似乎并不影响分娩结果。结论:妊娠期抑郁与分娩LBW新生儿的可能性较高独立相关(OR: 3.64;95% ci 1.70, 7.79)。针对产妇抑郁症的有效干预措施对于降低与LBW相关的发病率和死亡率至关重要。
{"title":"Impact of antenatal depressive and anxiety symptoms on adverse birth outcomes in Baghdad, Iraq: a prospective cohort study","authors":"Ola Ali Nassr, Mohammed Mahmood Mohammed, Hind abdulkhaliq Showman","doi":"10.32947/ajps.v23i1.988","DOIUrl":"https://doi.org/10.32947/ajps.v23i1.988","url":null,"abstract":"Background: Psychiatric symptoms are common during pregnancy, potentially leading to an increased risk of adverse birth outcomes. Studies assessing the impact of depression and/or anxiety on adverse birth outcomes in Iraq are currently lacking. This study aims to \u0000 \u0000determine whether depression and/or anxiety is independently associated with preterm birth (PTB) and low birth weight (LBW). \u0000Methods: A prospective cohort study included 352 pregnant women from outpatient clinics of Al-Yarmouk hospital and private clinics in Baghdad, Iraq from March 2021 to February 2022 using a convenience sampling. They were screened for depression using Edinburgh Postnatal Depression Scale (EPDS) during pregnancy and followed up to assess adverse birth outcomes. Multivariable logistic regression was used to determine predictors associated with adverse birth outcomes. \u0000Results: The prevalence of PTB and LBW was 7.7% and 11.6%, respectively. After adjustment of all potential sociodemographic, clinical and obstetric confounders, depression was independently associated with giving birth to LBW neonate (odd ratio (OR):3.64; 95% confidence interval (CI) 1.70, 7.79), but not PTB. Prevalence of LBW in depressed was 21.2% compared to 7.7% for non-depressed. LBW was also associated with a history of LBW and PTB. In contrast, anxiety did not seem to affect birth outcomes. \u0000Conclusion: Depression during pregnancy, regardless of the trimester, is independently associated with a higher likelihood of giving birth to LBW neonates (OR: 3.64; 95% CI 1.70, 7.79). Effective interventions that target maternal depression are vital to decrease morbidity and mortality associated with LBW. ","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91328052","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}
Sarah Abdul-Razzaq makki, Shakir M. Alwan, Mayada H. Al-Qaissy
Levofloxacin carboxamides with certain amino acids were prepared through an amide linkage to the amino acid (glycine, histidine, or serine). These carboxamides were subjected to an in silico molecular docking evaluation on DNA gyrase to predict their antibacterial activity using the GOLD suite. The binding affinities were very significant and encouraged the synthesis of the suggested carboxamides for intensive evaluation. These carboxamides were also subjected to Swiss ADME software to predict their ADME parameters. Levofloxacin carboxamides were prepared in high yield, and their chemical structures were confirmed by spectral analysis, such as 1H-NMR, 13C-NMR and FT-IR spectroscopy. Antibacterial activities were evaluated for the new carboxamides against two G-ve (Klebsiella and P. aeruginosa) and one G+ve (Streptococcus pneumonia) bacteria. When compared to levofloxacin, all of the synthesized carboxamides 1-3 demonstrated good activity against three types of bacteria. These carboxamides showed significant antibacterial activities against S. pneumoniae and lower activities against Klebsiella.
{"title":"In Silico Molecular Docking, Synthesis and Preliminary Evaluation of Antibacterial Activity of Levofloxacin Carboxamides with Certain Amino Acids","authors":"Sarah Abdul-Razzaq makki, Shakir M. Alwan, Mayada H. Al-Qaissy","doi":"10.32947/ajps.v23i1.984","DOIUrl":"https://doi.org/10.32947/ajps.v23i1.984","url":null,"abstract":"Levofloxacin carboxamides with certain amino acids were prepared through an amide linkage to the amino acid (glycine, histidine, or serine). These carboxamides were subjected to an in silico molecular docking evaluation on \u0000 \u0000DNA gyrase to predict their antibacterial activity using the GOLD suite. The binding affinities were very significant and encouraged the synthesis of the suggested carboxamides for intensive evaluation. These carboxamides were also subjected to Swiss ADME software to predict their ADME parameters. Levofloxacin carboxamides were prepared in high yield, and their chemical structures were confirmed by spectral analysis, such as 1H-NMR, 13C-NMR and FT-IR spectroscopy. Antibacterial activities were evaluated for the new carboxamides against two G-ve (Klebsiella and P. aeruginosa) and one G+ve (Streptococcus pneumonia) bacteria. When compared to levofloxacin, all of the synthesized carboxamides 1-3 demonstrated good activity against three types of bacteria. These carboxamides showed significant antibacterial activities against S. pneumoniae and lower activities against Klebsiella.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87938871","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}
Anastrozole (ANZ) is a potent non-steroidal aromatase II inhibitor (AI) used to decrease or delay the progression of breast tumor growth in some women. Since ANZ could be delivered transdermally due to its physicochemical characteristics as (log p of 3.5, aqueous solubility of 0.5 mg /mL, low dosage and half-life of 46.8 hr.) so, it could be used as a modelling drug evaluation of ethosomes, the current study aimed to formulate ANZ loaded ethosomes and evaluate the formulated ethosomes for particle size and PDI, entrapment efficiency and in vitro release profile. Film hydration method was used to prepare ANZ-loaded ethosoms. using different ratios of phospholipid (Soy phosphatidyl choline) and ethanol at variables probe sonication energy and time ratios. polydispersity index and particle size were used to evaluate the prepared ANZ-loaded ethosoms. The optimized formula of ethosomes which contain (1% Soy phosphatidyl choline,20% ethanol subjected to 300watt sonication energy with 1/3 sonication on /off ratio) was studied for in vitro drug release. It had 127.75±0.36 nm particle diameter and 74.7136 ± 3.457 % entrapment efficiency, the release kinetics obey Korsmeyer-Peppas and non-Fickian release as R2=0.9779 and n=0.737. The ratios of Soy phosphatidyl choline, ethanol, sonication energy and duration had a significant impact on the particle size of ethosomes at (p0.05). The preformulating analysis of Powder X-ray diffraction (P-XRD) indicate amorphous ethosomes. Fourier transform infrared (FTIR) showed the inertness among components.
{"title":"Formulation and in-vitro Evaluation of Ethosomes using Anastrozole as a Modeling Drug","authors":"Neven Nasef AlEbadi, M. Al-lami","doi":"10.32947/ajps.v22i4.971","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.971","url":null,"abstract":"Anastrozole (ANZ) is a potent non-steroidal aromatase II inhibitor (AI) used to decrease or delay the progression of breast tumor growth in some women. Since ANZ could be delivered transdermally due to its physicochemical characteristics as (log p of 3.5, aqueous solubility of 0.5 mg /mL, low dosage and half-life of 46.8 hr.) so, it could be used as a modelling drug evaluation of ethosomes, the current study aimed to formulate ANZ loaded ethosomes and evaluate the formulated ethosomes for particle size and PDI, entrapment efficiency and in vitro release profile. Film hydration method was used to prepare ANZ-loaded ethosoms. using different ratios of phospholipid (Soy phosphatidyl choline) and ethanol at variables probe sonication energy and time ratios. \u0000 polydispersity index and particle size were used to evaluate the prepared ANZ-loaded ethosoms. The optimized formula of ethosomes which contain (1% Soy phosphatidyl choline,20% ethanol subjected to 300watt sonication energy with 1/3 sonication on /off ratio) was studied for in vitro drug release. It had 127.75±0.36 nm particle diameter and 74.7136 ± 3.457 % entrapment efficiency, the release kinetics obey Korsmeyer-Peppas and non-Fickian release as R2=0.9779 and n=0.737. \u0000 The ratios of Soy phosphatidyl choline, ethanol, sonication energy and duration had a significant impact on the particle size of ethosomes at (p0.05). The preformulating analysis of Powder X-ray diffraction (P-XRD) indicate amorphous ethosomes. Fourier transform infrared (FTIR) showed the inertness among components.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76068925","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}
A series of nine novel 4, 5-dihydro-1H- pyrazole-1-yl acetate derivatives (IVa-i) by Shahlaa et al. was investigated in vitro for their antiproliferative activity against two cancer cell lines, breast cancer cell line (MCF-7) and lung cancer cell lines (A549), According to the cytotoxicity effect of these compounds, IVa, IVc and IVi compounds have antiproliferative effect with percentage (81.30%, 87.4% & 54.66%) respectively at 72h treatment on MCF-7 cell line compared to other compounds, these results indicate that the new compound IVc have the higher antiproliferative percent comparable to tamoxifen as a standard anti-tumour for oestrogen receptor positive breast cancer cell line after 72h followed by IVa after 72h (83.31%). cytotoxicity effect of compound IVb was highest among tested compounds on lung cancer cell line (A549) with antiproliferative percentage (58.49% & 75.04%) at 48 & 72h respectively, but it is less than erlotinib as a standard anti-tumour for lung cancer cell line cytotoxicity effect (77.10% & 82.46%) at these times. three compounds (IVa, IVc & IVi) have antiproliferative effect on breast cancerous cell line (MCF-7) and compound (IVc) have inhibition percentage comparable to that of the authorized medication Tamoxifen. One compound (IVb) had antiproliferative activity, but less than that of erlotinib on lung cancerous cell line (A549) and there is good agreement between our docking results and the experimental results.
{"title":"Pharmacological Evaluation of New 4, 5-dihydro-1H- Pyrazole-1-yl acetate Derivatives as anti-cancer agents","authors":"Shahlaa Zuhair Abdul-Majeed, Monther Faisal Mahdi, Suhad Faisal Hatem Al-Mugdadi","doi":"10.32947/ajps.v22i4.963","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.963","url":null,"abstract":"A series of nine novel 4, 5-dihydro-1H- pyrazole-1-yl acetate derivatives (IVa-i) by Shahlaa et al. was investigated in vitro for their antiproliferative activity against two cancer cell lines, breast cancer cell line (MCF-7) and lung cancer cell lines (A549), According to \u0000 \u0000the cytotoxicity effect of these compounds, IVa, IVc and IVi compounds have antiproliferative effect with percentage (81.30%, 87.4% & 54.66%) respectively at 72h treatment on MCF-7 cell line compared to other compounds, these results indicate that the new compound IVc have the higher antiproliferative percent comparable to tamoxifen as a standard anti-tumour for oestrogen receptor positive breast cancer cell line after 72h followed by IVa after 72h (83.31%). cytotoxicity effect of compound IVb was highest among tested compounds on lung cancer cell line (A549) with antiproliferative percentage (58.49% & 75.04%) at 48 & 72h respectively, but it is less than erlotinib as a standard anti-tumour for lung cancer cell line cytotoxicity effect (77.10% & 82.46%) at these times. three compounds (IVa, IVc & IVi) have antiproliferative effect on breast cancerous cell line (MCF-7) and compound (IVc) have inhibition percentage comparable to that of the authorized medication Tamoxifen. One compound (IVb) had antiproliferative activity, but less than that of erlotinib on lung cancerous cell line (A549) and there is good agreement between our docking results and the experimental results.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86186164","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}
Oxazine and thiazine are heterocyclic organic compounds that have a wide range of pharmacological applications. In this study, some chalcone derivatives (1–5) were synthesized based on the reaction of an equal amount of p-substituted acetophenone and terephthalaldehyde in a basic medium. Oxazine derivatives (6-10) and thiazine derivatives (11–15) are synthesized from the reactions of chalcones (1-5) with urea and thiourea, respectively, in a basic medium. The newly synthesized compounds were identified using various physical techniques like 1H-NMR and FT-IR spectra, in addition to docking analysis for some of these derivatives. Finally, these compounds were tested for their biological activity, IC50, and % of PC3 cell line viability as markers of anticancer activity.
{"title":"Synthesis A New Bis Oxazine and Thiazine Derivatives and Study Their Biological Activities","authors":"Dina Saleem M. Ameen","doi":"10.32947/ajps.v22i4.962","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.962","url":null,"abstract":"Oxazine and thiazine are heterocyclic organic compounds that have a wide range of pharmacological applications. In this study, some chalcone derivatives (1–5) were synthesized based on the reaction of an equal amount of p-substituted acetophenone and terephthalaldehyde in a basic medium. Oxazine derivatives (6-10) and thiazine derivatives (11–15) are synthesized from the reactions of chalcones (1-5) with urea and thiourea, respectively, in a basic medium. The newly synthesized compounds were identified using various physical techniques like 1H-NMR and FT-IR spectra, in addition to docking analysis for some of these derivatives. Finally, these compounds were tested for their biological activity, IC50, and % of PC3 cell line viability as markers of anticancer activity.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"96 10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87687962","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}
Furqan M. Abdulelah, Mohammed M. Mohammed, Rabab Hassan Baaker
Mucopolysaccharidosis I (MPS I) or Hurler and Mucopolysaccharidosis VI (MPS VI) or Maroteaux-Lamy syndrome are infrequent genetic disorder inherited as an autosomal recessive disease attributed to genetic variants genetic variant causing α-L iduronidase (IDUA) and arylsulfatase B (ARSB)enzyme deficiency, respectively. Here, two cases of children suffering from MPS disorder were described, the first case was MPS I while the second case was MPS VI and both cases were treated with allogenic Hematopoietic Stem Cell Transplantation approach in order to limit skeletal deterioration and retard neurocognitive alterations and hence, improve the quality of life of affected children. Following Transplantations outcomes reveal a full engraftment of donor cells as well as improvement of recipient enzymatic activity, enzyme replacement therapy post-transplantation will augment transplantation clinical outcomes. Transplantation will be more successful if the disease diagnosed early before the severe irreversible symptoms ensue.
{"title":"Case study of two Iraqi patients with Mucopolysaccharidosis (Hurler syndrome \"type I\" and Maroteaux-Lamy syndrome \"type VI\") treated with Hematopoietic Stem Cell Transplantation (HSCT)","authors":"Furqan M. Abdulelah, Mohammed M. Mohammed, Rabab Hassan Baaker","doi":"10.32947/ajps.v22i4.958","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.958","url":null,"abstract":"Mucopolysaccharidosis I (MPS I) or Hurler and Mucopolysaccharidosis VI (MPS VI) or Maroteaux-Lamy syndrome are infrequent genetic disorder inherited as an autosomal recessive disease attributed to genetic \u0000 \u0000variants genetic variant causing α-L iduronidase (IDUA) and arylsulfatase B (ARSB)enzyme deficiency, respectively. Here, two cases of children suffering from MPS disorder were described, the first case was MPS I while the second case was MPS VI and both cases were treated with allogenic Hematopoietic Stem Cell Transplantation approach in order to limit skeletal deterioration and retard neurocognitive alterations and hence, improve the quality of life of affected children. Following Transplantations outcomes reveal a full engraftment of donor cells as well as improvement of recipient enzymatic activity, enzyme replacement therapy post-transplantation will augment transplantation clinical outcomes. Transplantation will be more successful if the disease diagnosed early before the severe irreversible symptoms ensue.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72945691","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}
Background Antidepressant drugs are most commonly used for management of depressive disorders. Antidepressant drugs used in psychiatric clinics may affect the electrical activity of the heart which may induce fatal cardiac events. Objectives The purpose of the current study is to reveal the outcomes of escitalopram use for short period of time on the ECG records applying the prolongation of (heart-rate corrected interval for assessing ventricular repolarization) QTc and (corrected JT interval) JTc intervals as a predictor of the negative effects of antidepressants. Methods Twenty-eight patients with major depressive disorder and 20 healthy participants were recruited. Parameters such as weight, height, and blood pressure measurements were determined. Electrocardiographic (ECG) records and echocardiographic records [for ejection fraction (%)] were obtained before administration of escitalopram and after 4 weeks of treatment with daily escitalopram 10 mg. The intervals of JTc and QTc and the voltage criteria (R wave-V5 and S wave-V1) were measured. Results Patients with depression had a significantly prolonged interval of JTc and small-voltage criterion of the ventricles. Escitalopram significantly improves the prolongation in JTc and non-significantly ameliorate the voltage criterion. There is no significant alteration in the parameter of ejection fraction. Conclusion Irregularities in ECG records were observed in patients with major depressive disorder, and treatment with escitalopram for short period is associated with favorable results rather than negative effects. The evaluation of JTc interval in patients with depression is more suitable than QTc measurement in estimation of the effects of escitalopram.
{"title":"Electrocardiographic Changes in Patients with Depression after Using Escitalopram for a Short Period","authors":"Raz Muhammed HamaSalih, Rebwar Ghareeb Hama","doi":"10.32947/ajps.v22i4.950","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.950","url":null,"abstract":"Background \u0000Antidepressant drugs are most commonly used for management of depressive disorders. Antidepressant drugs used in psychiatric clinics may affect the electrical activity of the heart which may induce fatal cardiac events. \u0000Objectives \u0000The purpose of the current study is to reveal the outcomes of escitalopram use for short period of time on the ECG records applying the prolongation of (heart-rate corrected interval for assessing ventricular repolarization) QTc and (corrected JT interval) JTc intervals as a predictor of the negative effects of antidepressants. \u0000Methods \u0000Twenty-eight patients with major depressive disorder and 20 healthy participants were recruited. Parameters such as weight, height, and blood pressure measurements were determined. Electrocardiographic (ECG) records and echocardiographic records [for ejection fraction (%)] were obtained before administration of escitalopram and after 4 weeks of treatment with daily escitalopram 10 mg. The intervals of JTc and QTc and the voltage criteria (R wave-V5 and S wave-V1) were measured. \u0000Results \u0000Patients with depression had a significantly prolonged interval of JTc and small-voltage criterion of the ventricles. Escitalopram significantly improves the prolongation in JTc and non-significantly ameliorate the voltage criterion. There is no significant alteration in the parameter of ejection fraction. \u0000Conclusion \u0000Irregularities in ECG records were observed in patients with major depressive disorder, and treatment with escitalopram for short period is associated with favorable results rather than negative effects. The evaluation of JTc interval in patients with depression is more suitable than QTc measurement in estimation of the effects of escitalopram.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"94 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91466487","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}
Marwah Mohammed Salih Ali, Mayssaa Essam Abdalah, Bahir Abdul-Razzaq Mshimesh
Dihydrofolate reductase (DHFR) is a fundamental enzyme in producing the precursor of purines and pyrimidines for biosynthesis of DNA, RNA and amino acids at various stages. It is considered the key target for both anticancer and antimicrobial drug design. Terminalia chebula has unique phytoconstituents which are employed broadly in the development of medications against different diseases. It has been established that Terminalia chebula fruit could be used as therapeutic agent for cancer treatment. The aim of study was to evaluate the inhibitory effect of T. chebula fruit extract against DHFR enzyme activity and assessment the antioxidant and scavenging activity of T. chebula fruit extract, using DPPH and reducing activity tests Terminalia chebula fruits where extracted. The anti- DHFR enzyme activity was assessed in vitro for the four extracts of Terminalia chebula fruit and MTX. Phytochemical analysis of screening test, gas chromatography-mass spectrometry (GC-MS) analysis and high-performance liquid chromatography (HPLC) was done for the extract with highest biological activity. Antioxidant and radical scavenging activity of the extract with highest biological activity were evaluated via DPPH [1, 1-diphenyl-2-picrylhydrazyl (α, α-diphenyl-β-picrylhydrazyl] and reductive ability test. The percent of DHFR inhibiting activity for the cold methanolic extract was the highest and it was higher than that of MTX (96.0±1.4% vs. 89.0±1.1%, respectively), therefore, it was selected for the proceeding assay. Phytochemical analysis showed that the cold methanolic extract of T. chebula, showed a positive reaction for alkaloids, flavonoids, phenolic compounds, steroids and saponins. Besides, GC-MS analysis showed the presence of pyrogallol compound, while HPLC analysis recorded 3 major peaks with different retention times that were semi-identical to gallic acid, rutin and quercetin standard. The highest radical scavenging activity of T.chebula cold methanolic extract and ascorbic acid according to DPPH were (80.1±2.04% and 85.83±2.1%, respectively) at the maximum studied concentration (200μg/ml), where the activity of ascorbic acid was significantly higher (p≤0.05) than that of T.chebula. Meanwhile, the reductive ability of the cold extract was significantly higher (p ≤ 0.05) than that of vitamin E (0.72±0.15 and 0.41±0.08, respectively) at the maximum studied concentration (250μg/ml). These results suggesting the cold extract of Terminalia chebula has in vitro prominent anti-dihydrofolate reductase activity which is better than that of MTX.
{"title":"Phytochemical study and pharmacological activity of Terminalia chebula fruit extracts activity as Dihydrofolate Reductase enzyme inhibitors associated with antioxidant effect: In vitro study","authors":"Marwah Mohammed Salih Ali, Mayssaa Essam Abdalah, Bahir Abdul-Razzaq Mshimesh","doi":"10.32947/ajps.v22i4.948","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.948","url":null,"abstract":"Dihydrofolate reductase (DHFR) is a fundamental enzyme in producing the precursor of purines and pyrimidines for biosynthesis of DNA, RNA and amino acids at various stages. It is considered the key target for both anticancer and antimicrobial drug design. \u0000Terminalia chebula has unique phytoconstituents which are employed broadly in the development of medications against different diseases. It has been established that Terminalia chebula fruit could be used as therapeutic agent for cancer treatment. The aim of study was to evaluate the inhibitory effect of T. chebula fruit extract against DHFR enzyme activity and assessment the antioxidant and scavenging activity of T. chebula fruit extract, using DPPH and reducing activity tests Terminalia chebula fruits where extracted. The anti- DHFR enzyme activity was assessed in vitro for the four extracts of Terminalia chebula fruit and MTX. Phytochemical analysis of screening test, gas chromatography-mass spectrometry (GC-MS) analysis and high-performance liquid chromatography (HPLC) was done for the extract with highest biological activity. Antioxidant and radical scavenging activity of the extract with highest biological activity were evaluated via DPPH [1, 1-diphenyl-2-picrylhydrazyl (α, α-diphenyl-β-picrylhydrazyl] and reductive ability test. The percent of DHFR inhibiting activity for the cold methanolic extract was the highest and it was higher than that of MTX (96.0±1.4% vs. 89.0±1.1%, respectively), therefore, it was selected for the proceeding assay. Phytochemical analysis showed that the cold methanolic extract of T. chebula, showed a positive reaction for alkaloids, flavonoids, phenolic compounds, steroids and saponins. Besides, GC-MS analysis showed the presence of pyrogallol compound, while HPLC analysis recorded 3 major peaks with different retention times that were semi-identical to gallic acid, rutin and quercetin standard. The highest radical scavenging activity of T.chebula cold methanolic extract and ascorbic acid according to DPPH were (80.1±2.04% and 85.83±2.1%, respectively) at the maximum studied concentration (200μg/ml), where the activity of ascorbic acid was significantly higher (p≤0.05) than that of T.chebula. Meanwhile, the reductive ability of the cold extract was significantly higher (p ≤ 0.05) than that of vitamin E (0.72±0.15 and 0.41±0.08, respectively) at the maximum studied concentration (250μg/ml). These results suggesting the cold extract of Terminalia chebula has in vitro prominent anti-dihydrofolate reductase activity which is better than that of MTX. \u0000 ","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75283211","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：