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":null,"pages":null},"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":null,"pages":null},"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":null,"pages":null},"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":null,"pages":null},"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":null,"pages":null},"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":null,"pages":null},"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}
Acute kidney injury (AKI) is characterized by a sudden loss of kidney function that is established by increased serum creatinine levels and decreased urinary output. AKI is one of a group of functional kidney conditions known as acute kidney disease and disorders (AKD), which can vary in severity and self-limiting to severe and chronic. Adminstrations of glycerol generate significant elevation in serum urea and creatinine that’s mean occurance of functional abnormalities in the kidney. Vinpocetine drug has many pharmacological targets with multiple action, phosphodiesterase inhibiters-1(PDE-1) inhibitor, a voltage-gated sodium channel, and Inhibitory kinase B (IKK) are 3 main molecule targets of vinpocetine. PDE1 has been implicated in the regulation of vasoconstriction, vascular and cardiac structure remodeling, and neuro-transmission. Cilostazol, a phosphodiesterase (PDE) III inhibitors, that widely used for many cases such as reduces direct vascular injury via different mechanism, such as vasodilation and antiplatelet action, anti-inflammation and platelet-leukocyte interaction minimisation, and inhibition of vascular proliferation via up-regulation of hepatocyte growth factors. In present study, we looked at the effect and mechanism of the drugs vinpocetine and cilostazol in an animal model of glycerol-induced AKI. Experiment done during the 14-day trial, rats were divided into five groups: the control group received 2ml/kg normal saline; the induction group received 10ml/kg intramuscular glycerol injection; the vinpocetine group received 5mg/kg via gavage for 14 days and on day 7 given glycerol IM, the cilostazol group received 50mg/kg for 14 days and on day 7 given glycerol IM, and the combination group received half dose vinpocetine (2.5mg/kg) and cilostazol (25mg/kg). We discovered that the induction group had higher levels of urea and creatinine, as well as increased inflammation and oxidative stress, and that their renal tissue showed morphological changes typical of AKI, whereas the combination groups reduced glycerol induce acute renal damage. This revealed that vinpocetine and cilostazol can reinforce renal rat protection by reducing serum urea and creatinine and improving histopathological changes.
{"title":"Renoprotective effect of vinpocetine and cilostazol on glycerol induced renal injury in male rats","authors":"Duaa Ahmed, Ghaith Ali Jasim","doi":"10.32947/ajps.v22i4.947","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.947","url":null,"abstract":" Acute kidney injury (AKI) is characterized by a sudden loss of kidney function that is established by increased serum creatinine levels and decreased urinary output. AKI is one of a group of functional kidney conditions \u0000known as acute kidney disease and disorders (AKD), which can vary in severity and self-limiting to severe and chronic. Adminstrations of glycerol generate significant elevation in serum urea and creatinine that’s mean occurance of functional abnormalities in the kidney. Vinpocetine drug has many pharmacological targets with multiple action, phosphodiesterase inhibiters-1(PDE-1) inhibitor, a voltage-gated sodium channel, and Inhibitory kinase B (IKK) are 3 main molecule targets of vinpocetine. PDE1 has been implicated in the regulation of vasoconstriction, vascular and cardiac structure remodeling, and neuro-transmission. Cilostazol, a phosphodiesterase (PDE) III inhibitors, that widely used for many cases such as reduces direct vascular injury via different mechanism, such as vasodilation and antiplatelet action, anti-inflammation and platelet-leukocyte interaction minimisation, and inhibition of vascular proliferation via up-regulation of hepatocyte growth factors. In present study, we looked at the effect and mechanism of the drugs vinpocetine and cilostazol in an animal model of glycerol-induced AKI. Experiment done during the 14-day trial, rats were divided into five groups: the control group received 2ml/kg normal saline; the induction group received 10ml/kg intramuscular glycerol injection; the vinpocetine group received 5mg/kg via gavage for 14 days and on day 7 given glycerol IM, the cilostazol group received 50mg/kg for 14 days and on day 7 given glycerol IM, and the combination group received half dose vinpocetine (2.5mg/kg) and cilostazol (25mg/kg). We discovered that the induction group had higher levels of urea and creatinine, as well as increased inflammation and oxidative stress, and that their renal tissue showed morphological changes typical of AKI, whereas the combination groups reduced glycerol induce acute renal damage. This revealed that vinpocetine and cilostazol can reinforce renal rat protection by reducing serum urea and creatinine and improving histopathological changes.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74202934","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}
Study of the pharmacological activity of new heterocyclic scaffolds becomes a passion of many medicinal chemists around the world. 1,2,4-thiadiazine 1,1-dioxide derivatives are one of the heterocyclic derivatives that haveattracted researchers' attention since the early 1940's. In spite of this, however, the study of the pharmacological activities of this nucleus remains scant and needs to shed lighter on it. Therefore, in this review, the authors in this review collected all the families that included this nucleus whose biological activities were studied for the period between 1993 and 2020 in order to get an idea of the effectiveness of these compounds and highlighted the most effective ones. In addition, knowing the pharmacological aspects that had not been studied previously to focus more on them in the future by interested researchers.
{"title":"Study the pharmacological potential of 1,2,4-thiadiazine 1,1-dioxides: A minireview","authors":"Hiba Ali Hasan, Mesoun A. A. Al-Nubi Al-Sudani","doi":"10.32947/ajps.v22i4.951","DOIUrl":"https://doi.org/10.32947/ajps.v22i4.951","url":null,"abstract":"Study of the pharmacological activity of new heterocyclic scaffolds becomes a passion of many medicinal chemists around the world. 1,2,4-thiadiazine 1,1-dioxide derivatives are one of the heterocyclic derivatives that haveattracted researchers' attention since the early 1940's. In spite of this, however, the study of the pharmacological activities of this nucleus remains scant and needs to shed lighter on it. Therefore, in this review, the authors in this review collected all the families that included this nucleus whose biological activities were studied for the period between 1993 and 2020 in order to get an idea of the effectiveness of these compounds and highlighted the most effective ones. In addition, knowing the pharmacological aspects that had not been studied previously to focus more on them in the future by interested researchers.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74164455","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 Saad Hamdan, Yassir Mustafa Kamal, Huda Jaber Waheed
Methotrexate is used in the treatment of cancer, psoriasis, rheumatoid arthritis and several other disorders. It has a hepatotoxic potential side effect. Patients who have no access to alternative medications face a serious challenge as a result. The current study aimed to assess the apoptotic potential of methotrexate on liver cells and evaluate the hepatoprotective activity of the potent antioxidant astaxanthin, by downregulation of apoptotic biomarkers caspase 9 and caspase 3. A model of methotrexate-induced liver toxicity was employed on male rats. Thirty-six rats were divided into six groups; a negative control group, methotrexate induction group given (20 mg/kg) on day 13, three groups pretreated with astaxanthin in ascending doses (50, 75 and 100 mg/kg) for 14 days before methotrexate, and a conventional therapy group pretreated with silymarin (200mg/kg). The use of methotrexate significantly increased liver tissue caspase 9 and caspase 3 compared to the negative control. On the other side, astaxanthin used in all three doses significantly normalized these biomarkers. This study revealed that since astaxanthin significantly decreased caspase 9 and caspase 3 that are involved in the apoptotic pathway, it could be used as pretreatment in patients treated with methotrexate to alleviate its hepatotoxicity.
{"title":"Astaxanthin effect on apoptotic biomarkers in methotrexate-induced liver injury","authors":"Sarah Saad Hamdan, Yassir Mustafa Kamal, Huda Jaber Waheed","doi":"10.32947/ajps.v22i3.888","DOIUrl":"https://doi.org/10.32947/ajps.v22i3.888","url":null,"abstract":"Methotrexate is used in the treatment of cancer, psoriasis, rheumatoid arthritis and several other disorders. It has a hepatotoxic potential side effect. Patients who have no access to alternative medications face a serious \u0000 \u0000challenge as a result. The current study aimed to assess the apoptotic potential of methotrexate on liver cells and evaluate the hepatoprotective activity of the potent antioxidant astaxanthin, by downregulation of apoptotic biomarkers caspase 9 and caspase 3. \u0000A model of methotrexate-induced liver toxicity was employed on male rats. Thirty-six rats were divided into six groups; a negative control group, methotrexate induction group given (20 mg/kg) on day 13, three groups pretreated with astaxanthin in ascending doses (50, 75 and 100 mg/kg) for 14 days before methotrexate, and a conventional therapy group pretreated with silymarin (200mg/kg). \u0000The use of methotrexate significantly increased liver tissue caspase 9 and caspase 3 compared to the negative control. On the other side, astaxanthin used in all three doses significantly normalized these biomarkers. This study revealed that since astaxanthin significantly decreased caspase 9 and caspase 3 that are involved in the apoptotic pathway, it could be used as pretreatment in patients treated with methotrexate to alleviate its hepatotoxicity.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80176800","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}
Zaman Mahmood Jasim, Ghaith Ali Jasim, Ibrahim Saleh Abbas
Rosa canina belongs to rosacea family. Rosa. canina has a high concentration of phyto-constituents such as flavonoids, carotenoids, triterpene and vitamins as vitamin C, E, and A Rosa canina have an anti-inflammatory and antioxidant effects. The antioxidant effect belongs to presence of large quantities of phytochemicals such as flavonoids and polyphenols. Rosa canina has been used for arthritis gout, osteoarthritis, urinary tract disorder, diabetes, inflammation and cancer. After grinding the leaves of Rosa canina, they are extracted by using ethanol solvent (cold extraction method), then the extract concentrated by rotary evaporator at 40 c° and leaving it to dry. Median lethal dose (LD50) has been examined on 84 mice (male and female) divided into seven groups, each one contains 12 (6 male and 6 female). The animals were monitored for signs and any behavior changes after administration of Rosa canina ethanol extract. Acute toxicity study was done on 20 rats (male and female for fourteen days. The weight of animals was taken at day 0, 7, and 14. At day fourteen, relative organ weight as well as histopathological examination for (heart, liver, spleen, kidney, lung, abdominal stomach, testes and ovaries) were taken. In addition to the serum biochemical tests for) blood glucose, urea, creatinine, ALT, AST and total bilirubin (were done at day fourteen. The result of this study, indicated that lethal dose 50 was 16.527 gram/kilogram. Acute toxicity study, revealed that there is no significant difference between relative organ weight of controlled and treated groups for all organs that were selected and mentioned above. In addition, there is no significant difference between serum biochemical tests for both controlled and treated groups. Finally, no changes have been found between controlled and treated groups regarding histopathology examination due to the p value was P ˃ 0.05. Conclusion According to the presented study, ethanol extract of Rosa canina showed wide range of safety depending on the result of lethal dose 50h (16.527 g/kg). Therefore, the extract considered nontoxic. No cytotoxic effect appeared by using ethanol extract of Rosa canina in acute toxicity study. This belongs to the results obtained, which include no significant difference between control and treated male and female rats in biochemistry tests and histopathological examination.
蔷薇属酒渣鼻科。罗莎。狗玫瑰含有高浓度的植物成分，如类黄酮、类胡萝卜素、三萜和维生素C、E和a，狗玫瑰具有抗炎和抗氧化作用。其抗氧化作用是由于含有大量的植物化学物质，如类黄酮和多酚。Rosa canina已被用于关节炎痛风，骨关节炎，尿路紊乱，糖尿病，炎症和癌症。将犬蔷薇的叶子磨碎后，用乙醇溶剂(冷提取法)提取，然后用旋转蒸发器在40℃下浓缩，晾干。84只雄性和雌性小鼠被分为7组，每组12只(雄性和雌性各6只)，检测了致死中位剂量(LD50)。在给药后监测动物的体征和任何行为变化。对20只雄性和雌性大鼠进行了为期14天的急性毒性研究。分别于第0、7、14天测定动物体重。第14天，取相对脏器重量及组织病理学检查(心、肝、脾、肾、肺、腹、胃、睾丸、卵巢)。在第14天进行血糖、尿素、肌酐、谷丙转氨酶、谷丙转氨酶和总胆红素等血清生化试验。研究结果表明，致死剂量50为16.527 g / kg。急性毒性研究结果显示，所选各脏器的相对脏器重量在对照组和治疗组之间均无显著差异。此外，对照组和试验组血清生化指标无显著差异。最后，对照组和治疗组在组织病理学检查方面没有发现任何变化，p值为p < 0.05。结论犬玫瑰乙醇提取物在50h (16.527 g/kg)致死剂量范围内具有较宽的安全性。因此，提取物被认为是无毒的。在急性毒性研究中，野蔷薇乙醇提取物未出现细胞毒作用。这属于所获得的结果，即对照和处理的雄性和雌性大鼠在生物化学试验和组织病理学检查方面没有显著差异。
{"title":"Median lethal Dose and Acute Toxicity of Rosa canina L: In-Vivo Study","authors":"Zaman Mahmood Jasim, Ghaith Ali Jasim, Ibrahim Saleh Abbas","doi":"10.32947/ajps.v22i3.891","DOIUrl":"https://doi.org/10.32947/ajps.v22i3.891","url":null,"abstract":"Rosa canina belongs to rosacea family. Rosa. canina has a high concentration of phyto-constituents such as flavonoids, carotenoids, triterpene and vitamins as vitamin C, E, and A Rosa canina have an anti-inflammatory and antioxidant \u0000 \u0000effects. The antioxidant effect belongs to presence of large quantities of phytochemicals such as flavonoids and polyphenols. Rosa canina has been used for arthritis gout, osteoarthritis, urinary tract disorder, diabetes, inflammation and cancer. After grinding the leaves of Rosa canina, they are extracted by using ethanol solvent (cold extraction method), then the extract concentrated by rotary evaporator at 40 c° and leaving it to dry. Median lethal dose (LD50) has been examined on 84 mice (male and female) divided into seven groups, each one contains 12 (6 male and 6 female). The animals were monitored for signs and any behavior changes after administration of Rosa canina ethanol extract. Acute toxicity study was done on 20 rats (male and female for fourteen days. The weight of animals was taken at day 0, 7, and 14. At day fourteen, relative organ weight as well as histopathological examination for (heart, liver, spleen, kidney, lung, abdominal stomach, testes and ovaries) were taken. In addition to the serum biochemical tests for) blood glucose, urea, creatinine, ALT, AST and total bilirubin (were done at day fourteen. The result of this study, indicated that lethal dose 50 was 16.527 gram/kilogram. Acute toxicity study, revealed that there is no significant difference between relative organ weight of controlled and treated groups for all organs that were selected and mentioned above. In addition, there is no significant difference between serum biochemical tests for both controlled and treated groups. Finally, no changes have been found between controlled and treated groups regarding histopathology examination due to the p value was P ˃ 0.05. \u0000Conclusion \u0000According to the presented study, ethanol extract of Rosa canina showed wide range of safety depending on the result of lethal dose 50h (16.527 g/kg). Therefore, the extract considered nontoxic. No cytotoxic effect appeared by using ethanol extract of Rosa canina in acute toxicity study. This belongs to the results obtained, which include no significant difference between control and treated male and female rats in biochemistry tests and histopathological examination. \u0000 ","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78637351","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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