Publications by authors named "Saleh Bahashwan"

23 Publications

  • Page 1 of 1

The detection of SARS-CoV-2 in outpatient clinics and public facilities during the COVID-19 pandemic.

J Med Virol 2021 05 10;93(5):2955-2961. Epub 2021 Feb 10.

Department of Medical Laboratory Technology, College of Applied Medical Sciences, Taibah University, Madinah, Kingdom of Saudi Arabia.

The transmission of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) can occur through an airborne route, in addition to contaminated surfaces and objects. In hospitals, it has been confirmed by several studies that SARS-CoV-2 can contaminate surfaces and medical equipment especially in hospitals dedicated to coronavirus disease 2019 (COVID-19) patients. The aim of this study was to detect the contamination of hands, objects, and surfaces in isolation rooms and also in outpatients' clinics in hospitals and polyclinics. Environmental contamination of public high-touch surfaces in public facilities was also investigated during an active COVID-19 pandemic. Random swabs were also taken from public shops, pharmacies, bakeries, groceries, banknotes, and automated teller machines (ATMs). Samples were analyzed for SARS-CoV-2 positivity using real-time polymerase chain reaction. In the COVID-19 regional reference hospital, only 3 out of 20 samples were positive for SARS-CoV-2 RNA. Hand swabs from SARS-CoV-2-positive patients in isolation rooms were occasionally positive for viral RNA. In outpatients' clinics, door handles were the most contaminated surfaces. Dental chairs, sinks, keyboards, ophthalmoscopes, and laboratory equipment were also contaminated. Although no positive swabs were found in shops and public facilities, random ATM swabs returned a positive result for SARS-CoV-2. Although there is no longer a focus on COVID-19 wards and isolation hospitals, more attention is required to decontaminate frequently touched surfaces in health-care facilities used by patients not diagnosed with COVID-19. Additionally, high-touch public surfaces such as ATMs require further disinfection procedures to limit the transmission of the infection.
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http://dx.doi.org/10.1002/jmv.26819DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8014553PMC
May 2021

Generation of Combinatorial Lentiviral Vectors Expressing Multiple Anti-Hepatitis C Virus shRNAs and Their Validation on a Novel HCV Replicon Double Reporter Cell Line.

Viruses 2020 09 18;12(9). Epub 2020 Sep 18.

Department of Molecular Medicine, University of Padua, 35121 Padua, Italy.

Despite the introduction of directly acting antivirals (DAAs), for the treatment of hepatitis C virus (HCV) infection, their cost, patient compliance, and viral resistance are still important issues to be considered. Here, we describe the generation of a novel JFH1-based HCV subgenomic replicon double reporter cell line suitable for testing different antiviral drugs and therapeutic interventions. This cells line allowed a rapid and accurate quantification of cell growth/viability and HCV RNA replication, thus discriminating specific from unspecific antiviral effects caused by DAAs or cytotoxic compounds, respectively. By correlating cell number and virus replication, we could confirm the inhibitory effect on the latter of cell over confluency and characterize an array of lentiviral vectors expressing single, double, or triple cassettes containing different combinations of short hairpin (sh)RNAs, targeting both highly conserved viral genome sequences and cellular factors crucial for HCV replication. While all vectors were effective in reducing HCV replication, the ones targeting viral sequences displayed a stronger antiviral effect, without significant cytopathic effects. Such combinatorial platforms as well as the developed double reporter cell line might find application both in setting-up anti-HCV gene therapy approaches and in studies aimed at further dissecting the viral biology/pathogenesis of infection.
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http://dx.doi.org/10.3390/v12091044DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7551853PMC
September 2020

The metabolic disorders associated with chronic consumption of soft and energy drinks in rats.

Acta Biochim Pol 2020 Mar;67(1):79-84

1Department of Pharmacology and Toxicology (subdivision of Biochemistry), College of Pharmacy, Taibah University, Medina, Kingdom of Saudi Arabia; 2Department of Biochemistry, Faculty of Pharmacy, Minia University, Minia, Egypt.

Background: Energy Drinks (EDs) and Soft Drinks (SDs) are widely consumed among adolescents and young adults. These drinks contain variable amounts of caffeine which is a central nervous system stimulator; in addition to sugar, taurine, vitamins and herbal extracts. Several adverse effects have been reported for the excessive consumption of caffeine and sugar.

Aim: This work aimed at providing a comparison between the effect of chronic consumption of both drinks on metabolism biochemically as well as at the histopathological level.

Methods: Adult albino rats were randomly divided into three groups and treated for 4 weeks. Animals received water (control, group 1), 12.5 ml/kg/day of either Pepsi® (SD, group 2) or Power Horse® (ED, group 3). All animals had free access to water and standard animal chow.

Results: ED and SD groups showed a significant weight gain compared to control. ED animals showed a significant increase in serum urea, hyperlipidemia and hyperglycemia in comparison to control and SD groups. Serum uric acid significantly increased in ED and SD groups. ED group showed congestion and inflammation in their renal tissues in addition to splenomegaly and increased phagocyte infiltration.

Conclusion: The high caffeine-sugar content in ED exerts a more significant influence on the metabolic pathways than SDs. Both increase the incidence of cardiovascular diseases and tissue inflammation due to their effect on lipid profile and blood glucose. The other ingredients in EDs may play a role in the observed metabolic disturbances. Chronic use of EDs should be especially discouraged to avoid these negative effects.
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http://dx.doi.org/10.18388/abp.2020_2914DOI Listing
March 2020

Apremilast prevent doxorubicin-induced apoptosis and inflammation in heart through inhibition of oxidative stress mediated activation of NF-κB signaling pathways.

Pharmacol Rep 2018 Sep 29;70(5):993-1000. Epub 2018 Mar 29.

Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Background: Doxorubicin is an effective, potent and commonly used anthracycline-related anticancer drug; however, cardiotoxicity compromises its therapeutic potential. Apremilast, a novel phosphodiesterase type 4-inhibitor, reported to have anti-inflammatory effects and modulating many inflammatory mediators.

Methods: The present study investigated the influence of apremilast against doxorubicin-induced cardiotoxicity in male Wistar rats. A total, 24 animals were divided into four groups of six animal each. Group 1, served as control and received normal saline. Group 2 animals, received doxorubicin (20 mg kg, ip). Group 3 and 4, treatment group, received doxorubicin (20 mg kg, ip) with the same schedule as group-2, plus apremilast (10 and 20 mg kg day, po) respectively. Oxidative stress, caspase-3 enzyme activity, gene expression and protein expression were tested.

Results: The results of the present study demonstrated that administration of apremilast reversed doxorubicin-induced cardiotoxicity.

Conclusion: These findings suggested that apremilast can attenuate doxorubicin-induced cardiotoxicity via inhibition of oxidative stress mediated activation of nuclear factor-kappa B signaling pathways.
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http://dx.doi.org/10.1016/j.pharep.2018.03.009DOI Listing
September 2018

Apremilast prevent doxorubicin-induced apoptosis and inflammation in heart through inhibition of oxidative stress mediated activation of NF-κB signaling pathways.

Pharmacol Rep 2018 Oct 29;70(5):993-1000. Epub 2018 Mar 29.

Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Background: Doxorubicin is an effective, potent and commonly used anthracycline-related anticancer drug; however, cardiotoxicity compromises its therapeutic potential. Apremilast, a novel phosphodiesterase type 4-inhibitor, reported to have anti-inflammatory effects and modulating many inflammatory mediators.

Methods: The present study investigated the influence of apremilast against doxorubicin-induced cardiotoxicity in male Wistar rats. A total, 24 animals were divided into four groups of six animal each. Group 1, served as control and received normal saline. Group 2 animals, received doxorubicin (20mgkg, ip). Group 3 and 4, treatment group, received doxorubicin (20mgkg, ip) with the same schedule as group-2, plus apremilast (10 and 20mgkgday, po) respectively. Oxidative stress, caspase-3 enzyme activity, gene expression and protein expression were tested.

Results: The results of the present study demonstrated that administration of apremilast reversed doxorubicin-induced cardiotoxicity.

Conclusion: These findings suggested that apremilast can attenuate doxorubicin-induced cardiotoxicity via inhibition of oxidative stress mediated activation of nuclear factor-kappa B signaling pathways.
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http://dx.doi.org/10.1016/j.pharep.2018.03.009DOI Listing
October 2018

Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives.

Acta Pharm 2017 Sep;67(3):407-414

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Triazinopyrazolothieno pyrimidine derivatives 1-5 were evaluated for their anti-inflammatory, analgesic and anticancer activities and acute toxicity. Anti-inflammatory activity of the compounds was studied using the carrageenan test. All tested compounds showed analgesic activity, 3-methoxycarbonyl-4,6-dimethyl-8-[(N-methylindolyl)methyl] pyrimido [5',4':4,5]thieno [3',2'-3,4]pyrazolo [5,1-c]triazine (4) showed activity comparable to that of diclofenac. Compounds 1-5 were also screened for anticancer activity on a human lung cancer cell line (A549) and a human prostate cancer cell line (DU145) using the MTT micro-cultured tetrazolium assay method. Compound 4 showed also significant anticancer activity against both cancer cell lines, comparable to that of doxorubicin. The most active compounds were tested for their acute toxicity and median lethal doses were evaluated.
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http://dx.doi.org/10.1515/acph-2017-0022DOI Listing
September 2017

Knowledge, awareness, and attitudes toward antibiotic use and antimicrobial resistance among Saudi population.

Int J Clin Pharm 2016 Oct 29;38(5):1261-8. Epub 2016 Aug 29.

Department of Social and Clinical Pharmacy, Faculty of Pharmacy, Charles University, 50005, Prague, Hradec Kralove, Czech Republic.

Background Inappropriate use of antibiotics is a public health problem of great concern. Objective To evaluate knowledge of antibiotics, race, gender and age as independent risk factors for self-medication. Setting Residents and population from different regions of Saudi Arabia. Methods We conducted a cross sectional survey study among residents. Data were collected between June 2014 to May, 2015 from 1310 participants and data were recorded anonymously. The questionnaire was randomly distributed by interview of participants and included sociodemographic characteristics, antibiotics knowledge, attitudes and behavior with respect to antibiotics usage. Main outcome measure Population aggregate scores on questions and data were analyzed using univariate logistic regression to evaluate the influence of variables on self-prescription of antibiotics. Results The response rate was 87.7 %. A cumulative 63.6 % of participants reported to have purchased antibiotics without a prescription from pharmacies; 71.1 % reported that they did not finish the antibiotic course as they felt better. The availability of antibiotics without prescription was found to be positively associated with self-medication (OR 0.238, 95 % CI 0.17-0.33). Of those who used prescribed or non-prescribed antibiotics, 44.7 % reported that they kept left-over antibiotics from the incomplete course of treatment for future need. Interestingly, 62 % of respondents who used drugs without prescription agreed with the statement that antibiotics should be access-controlled prescribed by a physician. We also found significant association between storage, knowledge/attitudes and education. Conclusions The overall level of awareness on antibiotics use among residents in Saudi Arabia is low. This mandates public health awareness intervention programs to be implemented on the use of antibiotics.
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http://dx.doi.org/10.1007/s11096-016-0362-xDOI Listing
October 2016

Airway oxidative stress causes vascular and hepatic inflammation via upregulation of IL-17A in a murine model of allergic asthma.

Int Immunopharmacol 2016 May 5;34:173-182. Epub 2016 Mar 5.

Department of Pharmacology & Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Oxidants are generated in asthmatic airways due to infiltration of inflammatory leukocytes and resident cells in the lung. Reactive oxygen species (ROS) such as hydrogen peroxide and superoxide radical may leak into systemic circulation when generated in uncontrolled manner and may impact vasculature. Our previous studies have shown an association between airway inflammation and systemic inflammation; however so far none has investigated the impact of airway oxidative inflammation on hepatic oxidative stress and Th1/Th2/Th17 cytokine markers in liver/vasculature in a murine model of asthma. Therefore, this study investigated the contribution of oxidative stress encountered in asthmatic airways in modulation of systemic/hepatic Th1/Th2/Th17 cytokines balance and hepatic oxidative stress. Mice were sensitized intraperitoneally with cockroach extract (CE) in the presence of aluminum hydroxide followed by several intranasal (i.n.) challenges with CE. Mice were then assessed for systemic/hepatic inflammation through assessment of Th1/Th2/Th17 cytokines and oxidative stress (iNOS, protein nitrotyrosine, lipid peroxides and myeloperoxidase activity). Challenge with CE led to increased Th2/Th17 cytokines in blood/liver and hepatic oxidative stress. However, only Th17 related pro-inflammatory markers were upregulated by hydrogen peroxide (H2O2) inhalation in vasculature and liver, whereas antioxidant treatment, N-acetyl cysteine (NAC) downregulated them. Hepatic oxidative stress was also upregulated by H2O2 inhalation, whereas NAC attenuated it. Therefore, our study shows that airway oxidative inflammation may contribute to systemic inflammation through upregulation of Th17 immune responses in blood/liver and hepatic oxidative stress. This might predispose these patients to increased risk for the development of cardiovascular disorders.
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http://dx.doi.org/10.1016/j.intimp.2016.03.003DOI Listing
May 2016

Rutin Attenuates Carfilzomib-Induced Cardiotoxicity Through Inhibition of NF-κB, Hypertrophic Gene Expression and Oxidative Stress.

Cardiovasc Toxicol 2017 01;17(1):58-66

Department of Pharmacology and Toxicology, College of Pharmacy, Taibah University, Madinah, Kingdom of Saudi Arabia.

Carfilzomib is a proteasome inhibitor, commonly used in multiple myeloma, but its clinical use may be limited due to cardiotoxicity. This study was aimed to evaluate the influence of rutin in carfilzomib-induced cardiotoxicity in rats. Wistar albino male rats weighing 200-250 g (approximately 10 weeks old) were taken for this study. Animals were divided into four groups of six animals each. Group 1 served as normal control (NC), received normal saline; group 2 animals received carfilzomib (dissolved in 1 % DMSO) alone; group 3 animals received rutin (20 mg/kg) + carfilzomib; and group 4 animals received rutin (40 mg/kg) + carfilzomib. Hematological changes, biochemical changes, oxidative stress, hypertrophic gene expression, apoptotic gene expression, NFκB and IκB-α protein expression and histopathological evaluation were done to confirm the finding of carfilzomib-induced cardiotoxicity. Treatment with rutin decreased the carfilzomib-induced changes in cardiac enzymes such as lactate dehydrogenase, creatine kinase (CK) and CK-MB. For the assessment of cardiotoxicity, we further evaluated cardiac hypertrophic gene and apoptotic gene expression such as α-MHC, β-MHC and BNP and NF-κB and p53 gene expression, respectively, using RT-PCR. Western blot analysis showed that rutin treatment prevented the activation of NF-κB by increasing the expression of IκB-α. Rutin also attenuated the effects of carfilzomib on oxidant-antioxidant including malondialdehyde and reduced glutathione. Histopathological study clearly confirmed that rutin attenuated carfilzomib-induced cardiotoxicity in rats.
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http://dx.doi.org/10.1007/s12012-015-9356-5DOI Listing
January 2017

Riboflavin attenuates lipopolysaccharide-induced lung injury in rats.

Toxicol Mech Methods 2015 11;25(5):417-23. Epub 2015 Sep 11.

b Department of Pharmacology and Toxicology , College of Pharmacy, Taibah University , Medina , KSA.

Riboflavin (vitamin B2) is an easily absorbed micronutrient with a key role in maintaining health in humans and animals. It is the central component of the cofactors flavin adenine dinucleotide (FAD) and flavin mononucleotide (FMN) and is therefore required by all flavoproteins. Riboflavin also works as an antioxidant by scavenging free radicals. The present study was designed to evaluate the effects of riboflavin against acute lungs injury induced by the administration of a single intranasal dose (20 μg/rat) of lipopolysaccharides (LPS) in experimental rats. Administration of LPS resulted in marked increase in malondialdehyde (MDA) level (p < 0.01) and MPO activity (p < 0.001), whereas marked decrease in glutathione (GSH) content (p < 0.001), glutathione reductase (GR) (p < 0.001) and glutathione peroxidase (p < 0.01) activity. These changes were significantly (p < 0.001) improved by treatment with riboflavin in a dose-dependent manner (30 and 100 mg/kg, respectively). Riboflavin (100 mg/kg, p.o.) showed similar protective effects as dexamethasone (1 mg/kg, p.o.). Administration of LPS showed marked cellular changes including interstitial edema, hemorrhage, infiltration of PMNs, etc., which were reversed by riboflavin administration. Histopathological examinations showed normal morphological structures of lungs tissue in the control group. These biochemical and histopathological examination were appended with iNOS and CAT gene expression. The iNOS mRNA expression was increased significantly (p < 0.001) and levels of CAT mRNA expression was decreased significantly (p < 0.001) in the animals exposed to LPS, while treatment with riboflavin significantly (p < 0.01) improved expression of both gene. In conclusion, the present study clearly demonstrated that riboflavin caused a protective effect against LPS-induced ALI. These results suggest that riboflavin may be used to protect against toxic effect of LPS in lungs.
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http://dx.doi.org/10.3109/15376516.2015.1045662DOI Listing
July 2016

Oxidative airway inflammation leads to systemic and vascular oxidative stress in a murine model of allergic asthma.

Int Immunopharmacol 2015 May 3;26(1):237-45. Epub 2015 Apr 3.

Department of Pharmacology and Toxicology, College of Pharmacy, Taibah University, Medina, Saudi Arabia.

Oxidant-antioxidant imbalance plays an important role in repeated cycles of airway inflammation observed in asthma. It is when reactive oxygen species (ROS) overwhelm antioxidant defenses that a severe inflammatory state becomes apparent and may impact vasculature. Several studies have shown an association between airway inflammation and cardiovascular complications; however so far none has investigated the link between airway oxidative stress and systemic/vascular oxidative stress in a murine model of asthma. Therefore, this study investigated the contribution of oxidative stress encountered in asthmatic airways in modulation of vascular/systemic oxidant-antioxidant balance. Rats were sensitized intraperitoneally with ovalbumin (OVA) in the presence of aluminum hydroxide followed by several intranasal (i.n.) challenges with OVA. Rats were then assessed for airway and vascular inflammation, oxidative stress (ROS, lipid peroxides) and antioxidants measured as total antioxidant capacity (TAC) and thiol content. Challenge with OVA led to increased airway inflammation and oxidative stress with a concomitant increase in vascular inflammation and oxidative stress. Oxidative stress in the vasculature was significantly inhibited by antioxidant treatment, N-acetyl cysteine; whereas hydrogen peroxide (H2O2) inhalation worsened it. Therefore, our study shows that oxidative airway inflammation is associated with vascular/systemic oxidative stress which might predispose these patients to increased cardiovascular risk.
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http://dx.doi.org/10.1016/j.intimp.2015.03.032DOI Listing
May 2015

Androgen receptor antagonists and anti-prostate cancer activities of some newly synthesized substituted fused pyrazolo-, triazolo- and thiazolo-pyrimidine derivatives.

Int J Mol Sci 2014 Nov 24;15(11):21587-602. Epub 2014 Nov 24.

Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

A series of substituted pyrazole, triazole and thiazole derivatives (2-13) were synthesized from 1-(naphtho[1,2-d]thiazol-2-yl)hydrazine as starting material and evaluated as androgen receptor antagonists and anti-prostate cancer agents. The newly synthesized compounds showed potent androgen receptor antagonists and anti-prostate cancer activities with low toxicity (lethal dose 50 (LD50)) comparable to Bicalutamide as reference drug. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, 13C-NMR, and MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD50 values and pharmacological activities of the synthesized compounds are reported.
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http://dx.doi.org/10.3390/ijms151121587DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4264242PMC
November 2014

Protection against tacrolimus-induced cardiotoxicity in rats by olmesartan and aliskiren.

Toxicol Mech Methods 2014 Dec 23;24(9):697-702. Epub 2014 Sep 23.

Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University , Riyadh , KSA .

Context: Tacrolimus (TAC), a calcineurin inhibitor, is commonly used as an immunosuppressive agent in organ transplantation, but its clinical use may be limited due to cardiotoxicity. Olmesartan (OLM; angiotensin receptor blocker) and aliskiren (ALK; renin inhibitor) may attenuate cardiotoxicity induced by TAC by inhibition of renin-angiotensin aldosterone system.

Objective: The aim of this study was to evaluate the effect of OLM and ALK on TAC-induced cardiotoxicity.

Materials And Methods: Male Wistar albino rats weighing 200-250 g (10-12 weeks old) were used in this study. Animals were divided into four groups. Group 1 received normal saline, group 2 received TAC (2 mg/kg, intraperitoneally for 14 d), group 3 received OLM (2 mg/kg, p.o. for 28 d) + TAC and group 4 received ALK (50 mg/kg, p.o. for 28 d) + TAC. TAC-induced cardiotoxicity was assessed biochemically and histopathologically.

Results: Treatment with OLM or ALK decreased the TAC-induced changes in biochemical markers of cardiotoxicity such as serum aspartate transaminase, creatine kinase and lactate dehydrogenase. OLM or ALK also attenuated the effects of TAC on oxidant-antioxidant parameters such as malondialdehyde, reduced glutathione and catalase. Histopathological and ultrastructural studies showed that OLM or ALK also attenuated TAC-induced cardiotoxicity.

Discussion And Conclusion: These results suggest that OLM as well as ALK has protective effects against TAC-induced cardiotoxicity; implying that angiotensin receptor blocker or renin inhibitor, respectively, may counteract cardiotoxicity associated with immunosuppressant use.
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http://dx.doi.org/10.3109/15376516.2014.963773DOI Listing
December 2014

Modulatory effects of meloxicam on cardiotoxicity and antitumor activity of doxorubicin in mice.

Cancer Chemother Pharmacol 2014 Sep 23;74(3):559-69. Epub 2014 Jul 23.

Department of Pharmacology and Toxicology, College of Pharmacy, Taibah University, P.O. Box 30001, El-Madinah, El-Munaworah, Saudi Arabia,

Purpose: This study was undertaken to assess the possible modulatory effects and mechanisms of meloxicam, a cyclooxygenase-2 inhibitor, on the antitumor activity and cardiotoxicity of doxorubicin in a mice model of mammary carcinoma.

Methods: Solid tumor mass was developed in female albino mice using Ehrlich carcinoma cells. Forty mice-bearing tumor were divided randomly into four groups for treatment: with saline, meloxicam 10 mg/kg, doxorubicin 5 mg/kg and meloxicam 1 h ahead of doxorubicin, twice weekly for 2 weeks. Tumor volume was followed up and cardiac protective utility was estimated via measuring heart and serum parameters.

Results: Meloxicam expressed a non-significant increase in doxorubicin antitumor activity. Conversely, meloxicam significantly (p < 0.01) mitigated doxorubicin-induced elevation of serum cardiac enzymes [creatine kinase, lactate dehydrogenase and troponin-I]; cardiac lipid peroxidations marker; cardiac active caspase-3 content; and cardiac prostaglandin E2 content. Meloxicam significantly abrogated doxorubicin-induced disturbance in heart histology and relative heart weight to body weight. Meloxicam normalized doxorubicin-induced suppression in heart antioxidant enzymes activities and gene expressions [superoxide dismutase, glutathione peroxidase (GSH-Px) and catalase], and heart GSH content. In addition, meloxicam ameliorated doxorubicin-induced disturbance in phase II metabolizing enzyme, cardiac quinone reductase (QR), at activity level and mRNA expression.

Conclusion: Meloxicam protects heart against doxorubicin toxicity without affecting its antitumor activity against solid mammary cancer model in mice. This protective effect is attributed to antioxidant effect, antiradical effect, antiinflammatory action, antiapoptotic effect and induction of QR enzyme.
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http://dx.doi.org/10.1007/s00280-014-2544-3DOI Listing
September 2014

Synthesis and pharmacological activities of some new triazolo- and tetrazolopyrimidine derivatives.

Molecules 2013 Dec 6;18(12):15051-63. Epub 2013 Dec 6.

Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawara 3893, Saudi Arabia.

A new series of fused triazolo- and tetrazolopyrimidine derivatives 2-14 were synthesized and their anti-inflammatory and ulcerogenic activities were evaluated. The pharmacological screening showed that many of these obtained compounds have good anti-inflammatory activities, comparable to the reference drug. The toxicity of the compounds was also assayed via the determination of their LD50 values. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, MS spectral data and elemental analysis.
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http://dx.doi.org/10.3390/molecules181215051DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269734PMC
December 2013

Anti-parkinsonism, hypoglycemic and anti-microbial activities of new poly fused ring heterocyclic candidates.

Int J Biol Macromol 2013 Jun 15;57:165-73. Epub 2013 Mar 15.

Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

A new series of poly fused pyrazolothienopyrimidine derivatives (2-14) were synthesized and their anti-parkinsonism, hypoglycemic and anti-microbial activities were evaluated. Some of the newly synthesized compounds exhibited better pharmacological and biological activities than the reference controls with low concentrations. The structures of newly synthesized compounds were confirmed by chemical, elemental and spectroscopic evidences. The detailed synthesis, spectroscopic data, and pharmacological activities were reported.
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http://dx.doi.org/10.1016/j.ijbiomac.2013.03.019DOI Listing
June 2013

Pharmacological activities of some new polycyclic triazolopyrazolopyridazine derivatives.

Int J Biol Macromol 2012 Jul-Aug;51(1-2):7-17. Epub 2012 May 8.

Pharmacy Department, College of Medical Rehabilitation Sciences, Taibah University, Madinah Munawara, Saudi Arabia.

In continuation of our previous work, a novel series of polycyclic derivatives were synthesized and their anti-inflammatory, analgesic and antimicrobial activities were evaluated. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). Some of the newly compounds exhibited better biological and pharmacological activities than the reference controls with low toxicity (LD(50)). The structure of the new compounds has been established on the bases of chemical and spectroscopic evidences. The detailed synthesis, spectroscopic data, LD(50) and pharmacological activities of the synthesized compounds were reported.
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http://dx.doi.org/10.1016/j.ijbiomac.2012.05.002DOI Listing
October 2012

Changes in phospholipid composition, protein content and chemical properties of flaxseed oil during development.

Plant Physiol Biochem 2012 May 10;54:1-5. Epub 2012 Feb 10.

Laboratoire de Biochimie des Lipides, Département de Biologie, Faculté des Sciences de Tunis, 2092 ELmanar, Tunisia.

The aim of the present research is to investigate the effect of harvest date on the composition of flaxseed. Samples were collected at regular intervals from 7 to 56 days after flowering (DAF) and analyzed for phospholipid composition, storage protein content and chemical properties. Phospholipid (PL) percentage of the total lipid decreased from 32.72% on the 7th DAF to 2.55% on the 56th DAF. The most phospholipids present in flaxseed were phosphatidylinositol (PI), phosphatidylethanolamine (PE) and lysophosphatidylcholine (LPC) which were highly unsaturated and rich in linolenic and linoleic acids, comprising together 60% of the total fatty acids. Chemical investigation of flaxseed oil showed overall a decrease in UV absorbance (K(232) and K(270)), acid value, free fatty acid content and an increase in peroxide value and storage protein content with development. At full maturity, flaxseed contained 29% proteins on a dry weight basis (DW %).
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http://dx.doi.org/10.1016/j.plaphy.2012.02.008DOI Listing
May 2012

Androgen receptor antagonists and anti-prostate cancer activities of some synthesized steroidal candidates.

Chem Pharm Bull (Tokyo) 2011 ;59(11):1363-8

Department of Pharmacy, College of Health Science, Taibah University, Madinah 3893, Saudi Arabia.

In continuation of our previous work, a novel series of steroid derivatives were synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Twenty-one heterocyclic derivatives containing a cyanopyrane ring fused to a steroidal moiety were conveniently synthesized and screened for their antagonistic, antiandrogen and prostate anticancer activities comparable to that of bicalutamide as the reference control. Some of the compounds exhibited better antagonistic, antiandrogen and prostate anticancer activities than the reference controls. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). Synthetic steroidal structures fused to a substituted cyanopyrane ring seem to be a promising approach in the search for novel leads for potent antagonistic, antiandrogen and prostate anticancer agents.
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http://dx.doi.org/10.1248/cpb.59.1363DOI Listing
March 2012

Abrogation of cisplatin-induced nephrotoxicity in mice by alpha lipoic acid through ameliorating oxidative stress and enhancing gene expression of antioxidant enzymes.

Eur J Pharmacol 2011 Oct 13;668(1-2):278-84. Epub 2011 Jul 13.

Department of Medical Laboratories Technology, Faculty of Applied Medical Sciences, Taibah University, Madinah, Saudi Arabia.

Cisplatin is chemotherapeutic drug used in treatment of malignancies. However, its clinical utility is limited by nephrotoxicity. The purpose of present study is to investigate biochemical and molecular effects of alpha lipoic acid (ALA) to protect against cisplatin-induced nephrotoxicity in mice. Cisplatin (12 mg/kg/day) was administered i.p. for 4 days. Group of mice were given ALA (20 mg/kg/day) for 18 days. Another set were administered ALA for 4 days before and 14 days after cisplatin intoxication. The results obtained revealed that kidney/body weight ratio of cisplatin-treated mice was increased by +40%. ALA intake declined the ratio by -19%. Serum creatinine and urea levels were increased in cisplatin-treated mice by +375% and +69%, respectively. These changes were moved to normalcy upon ALA intake. Cisplatin treatment elevated malondialdehyde (MDA) by 27 fold and declined reduced glutathione (GSH) by -49%. Cisplatin decreased catalase, superoxide dismutase (SOD) and glutathione peroxidase (GPx) enzymes by -47%, -49% and -59%, respectively. ALA decreased the MDA by -286% and increased the GSH, catalase, SOD and GPx levels by +60%, +81%, +90% and +38%, respectively. ALA increased mRNA expression of catalase, CuZn SOD and GPx genes near to normalcy compared to cisplatin-treated mice. Cisplatin-treated mice increased caspase-3-activity by +223%, nitric oxide (NO) by +74% and inducible nitric oxide synthase (iNOS) by 10 fold. ALA intake declined these changes by -43%, -45% and -73%, respectively. ALA may play renoprotective role on cisplatin-induced nephrotoxicity through antioxidant and antiapoptotic mechanisms combined with initiation of mRNA expression of antioxidant genes.
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http://dx.doi.org/10.1016/j.ejphar.2011.06.051DOI Listing
October 2011

Schistosoma mansoni changes the activity of phase II drug-metabolizing enzymes: role of praziquantel as antibilharzial drug.

Drug Metab Lett 2010 Aug;4(3):134-8

Department of Clinical Biochemistry, Faculty of Medicine, PO Box 30001, Taibah University, Al-Madinah, Saudi Arabia.

Schistosomiasis is one of the major health problems in many developing countries and causes liver damage. In addition, under the influence of schistosomiasis most of the endogenous toxic compounds can be conjugated with glutathione via glutathione S-transferase. Therefore, the present study showed the effect of Schistosoma mansoni after 20, 30, 45, 60, and 75 days post-infection on the activity of glutathione-S-transferase (GST) and glutathione reductase (GR), and on the levels of glutathione [GSH] in the livers of male mice. In addition, anti-schistosomal drug (praziquantel) was administered orally [60 mg/kg body weight] for three consecutive days before decapitation of the infected mice at each time point. In the present, depletion of GSH levels was observed at 45, 60 and 75 days post-infection. However, treatment of infected mice at 45, 60, and 75 days post-infection with praziquantel for three consecutive days before decapitation at each time point restored the increased GSH levels to their normal values compared with control groups. Inhibition of GST and induction of GR activities in the livers of S. mansoni-infected mice at all time-points were restored to their normal levels after praziquantel treatment. It is concluded that S. mansoni infection changed the activities of GST, GR and GSH levels. Moreover, it has been found that praziquantel treatment of S. mansoni-infected mice restored such alterations to their normal values and this recovery could alleviate the deleterious effects of S. mansoni infection. In addition, the present study could provide new evidence to the damage occurred in livers of S. mansoni-infected hosts. Also, it is suggested that praziquantel is the best drug of choice for schistosoma mansoni treatment.
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http://dx.doi.org/10.2174/187231210791698447DOI Listing
August 2010

Schistsoma Mansoni Changes the Activity of Glutathione S-Transferase and Glutathione Levels in the Liver of Male Mice: Role of Praziquantel as Anti-Schistosomal Drug.

Drug Metab Lett 2010 Jun 15. Epub 2010 Jun 15.

Department of Clinical Biochemistry, Faculty of Medicine, PO Box 30001, Taibah University, Al-Madinah, Saudi Arabia.

Schistosomiasis is one of the major health problems in many developing countries and causes liver damage. In addition, under the influence of schistosomaisis, most of the endogenous toxic compounds can be conjugated with glutathione via glutathione S-transferase. Therefore, the present study showed the effect of Schistosoma mansoni after 20, 30, 45, 60, and 75 days post-infection on the activity of glutathione-S-transferase (GST) and glutathione reductase (GR), and on the levels of glutathione [GSH] in the livers of male mice. In addition, anti-schistosomal drug (praziquantel) was administered orally [60 mg/kg body weight] for three consecutive days before decapitation of the infected mice at each time point. In the present, depletion of GSH levels was observed at 45, 60 and 75 days post-infection. However, treatment of infected mice at 45, 60, and 75 days post-infection with praziquantel for three consecutive days before decapitation at each time point restored the increased GSH levels to their normal values compared with control groups. Inhibition of GST and induction of GR activities in the livers of S. mansoni-infected mice at all time-points were restored to their normal levels after praziquantel treatment. It is concluded that S. mansoni infection changed the activities of GST, GR and GSH levels. Moreover, it has been found that praziquantel treatment of S. mansoni-infected mice restored such alterations to their normal values and this recovery could alleviate the deleterious effects of S. mansoni infection. In addition, the present study could provide new evidence to the damage occurred in livers of S. mansoni-infected hosts. Also, it is suggested that praziquantel is the best drug of choice for schistosoma mansoni treatment.
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June 2010
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