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Synthesis, reactions, and spectral characterization of some new biologically active compounds derived from thieno[2,3-c]pyrazole-5-carboxamide

Research Abstract

The starting compound 4-amino-3-methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-
5-carboxamide (1), that has been previously synthesized according to the literature
procedure, underwent a reaction with the anhydride of phthalic acid
either in AcOH or DMF to give isoindolinylpyrazole-5-carboxamide 3 and
pyrazolothienopyrimidoisoindoledione 4, respectively. Also, it was subjected to
react with diethylmalonate followed by hydrazinolysis by hydrazine hydrate to
yield the pyrazolothienopyrimidinyl acetohydrazide 5. The carbohydrazide
derivative 5 was used as a key intermediate for the preparation of other new
heterocyclic systems containing pyrazolylacetyl pyrazolothienopyrimidines
and pyrazolothieno-pyrimidotriazepine compounds 6–11. The structures of
these new heterocycles have been characterized by using analytical and spectroscopic
analyses (IR, 1H-NMR, 13C-NMR and MS). Some derivatives of the
synthesized compounds exhibited remarkable antibacterial and antifungal
activities against many bacterial and fungal strains.

Research Authors
Ahmed F. Saber, Remon M. Zaki, Adel M. Kamal El-Dean, Shaban M. Radwan
Research Department
Research Journal
Journal of Heterocyclic Chemistry
Research Member
Research Pages
pp. 238–247
Research Publisher
Wiley
Research Rank
1
Research Vol
Vol. 57
Research Website
https://doi.org/10.1002/jhet.3769
Research Year
2020

Cytoprotective effect of Nigella sativa seed on 4-nonylphenol-induced
renal damage in the African catfish (Clarias gariepinus)

Research Abstract

4-Nonylphenol (4-NP) is a nephrotoxic substance that is highly prevalent in aquatic environments. Nigella
sativa seed (NSS) has many biological activities and is widely used throughout the world as a
medicinal product. Therefore, in the present study, we investigated the cytoprotective effect of NSS on 4-
NP-induced renal damage in African catfish (Clarias gariepinus). Thirty fish were divided into five equal
groups: an untreated control group and four groups that were challenged with 4-NP at a dose of
0.1 mg L1 of aquarium water and fed a basal diet supplemented with 0%, 1%, 2.5%, and 5% NSS,
respectively, for 3 weeks. Histological, histochemical, and ultrastructural features of the kidney were
then assessed as biomarkers for renal tissue damage. Our results confirmed that 4-NP was a potent
cytotoxic agent for the kidney tissue and induced renal damage, with 4-NP-intoxicated fish showing
necrosis in the epithelial cells of the renal corpuscles, renal proximal convoluted tubules, and intertubular
hematopoietic tissue, as well as loss of or a decrease in microvilli, a decrease in mitochondria,
and an increase in the lysosomes in the epithelial cells of the proximal convoluted tubules. The kidneys of
4-NP-intoxicated fish also showed increased numbers of Perls’ Prussian blue-positive melanomacrophage
centers and intraepithelial T-lymphocytes in the proximal convoluted tubules and plasma cells.
The administration of NSS to 4-NP-challenged fish significantly minimized the cytotoxic effect of 4-NP,
maintaining the normal kidney structure, with concentrations of 2.5% and 5% of feed being most effective
for protecting the kidney against 4-NP-induced renal damage.

Research Authors
Mahmoud Abd-Elkareem a, Nasser S. Abou Khalil b, Alaa El-Din H. Sayed c,
Research Department
Research Journal
Chemosphere
Research Member
Research Pages
127379
Research Publisher
ElSevier
Research Rank
1
Research Vol
259
Research Website
https://www.sciencedirect.com/science/article/pii/S0045653520315721?via%3Dihub
Research Year
2020

Cytoprotective effect of Nigella sativa seed on 4-nonylphenol-induced
renal damage in the African catfish (Clarias gariepinus)

Research Abstract

4-Nonylphenol (4-NP) is a nephrotoxic substance that is highly prevalent in aquatic environments. Nigella
sativa seed (NSS) has many biological activities and is widely used throughout the world as a
medicinal product. Therefore, in the present study, we investigated the cytoprotective effect of NSS on 4-
NP-induced renal damage in African catfish (Clarias gariepinus). Thirty fish were divided into five equal
groups: an untreated control group and four groups that were challenged with 4-NP at a dose of
0.1 mg L1 of aquarium water and fed a basal diet supplemented with 0%, 1%, 2.5%, and 5% NSS,
respectively, for 3 weeks. Histological, histochemical, and ultrastructural features of the kidney were
then assessed as biomarkers for renal tissue damage. Our results confirmed that 4-NP was a potent
cytotoxic agent for the kidney tissue and induced renal damage, with 4-NP-intoxicated fish showing
necrosis in the epithelial cells of the renal corpuscles, renal proximal convoluted tubules, and intertubular
hematopoietic tissue, as well as loss of or a decrease in microvilli, a decrease in mitochondria,
and an increase in the lysosomes in the epithelial cells of the proximal convoluted tubules. The kidneys of
4-NP-intoxicated fish also showed increased numbers of Perls’ Prussian blue-positive melanomacrophage
centers and intraepithelial T-lymphocytes in the proximal convoluted tubules and plasma cells.
The administration of NSS to 4-NP-challenged fish significantly minimized the cytotoxic effect of 4-NP,
maintaining the normal kidney structure, with concentrations of 2.5% and 5% of feed being most effective
for protecting the kidney against 4-NP-induced renal damage.

Research Authors
Mahmoud Abd-Elkareem a, Nasser S. Abou Khalil b, Alaa El-Din H. Sayed c,
Research Journal
Chemosphere
Research Pages
127379
Research Publisher
ElSevier
Research Rank
1
Research Vol
259
Research Website
https://www.sciencedirect.com/science/article/pii/S0045653520315721?via%3Dihub
Research Year
2020

Cytoprotective effect of Nigella sativa seed on 4-nonylphenol-induced
renal damage in the African catfish (Clarias gariepinus)

Research Abstract

4-Nonylphenol (4-NP) is a nephrotoxic substance that is highly prevalent in aquatic environments. Nigella
sativa seed (NSS) has many biological activities and is widely used throughout the world as a
medicinal product. Therefore, in the present study, we investigated the cytoprotective effect of NSS on 4-
NP-induced renal damage in African catfish (Clarias gariepinus). Thirty fish were divided into five equal
groups: an untreated control group and four groups that were challenged with 4-NP at a dose of
0.1 mg L1 of aquarium water and fed a basal diet supplemented with 0%, 1%, 2.5%, and 5% NSS,
respectively, for 3 weeks. Histological, histochemical, and ultrastructural features of the kidney were
then assessed as biomarkers for renal tissue damage. Our results confirmed that 4-NP was a potent
cytotoxic agent for the kidney tissue and induced renal damage, with 4-NP-intoxicated fish showing
necrosis in the epithelial cells of the renal corpuscles, renal proximal convoluted tubules, and intertubular
hematopoietic tissue, as well as loss of or a decrease in microvilli, a decrease in mitochondria,
and an increase in the lysosomes in the epithelial cells of the proximal convoluted tubules. The kidneys of
4-NP-intoxicated fish also showed increased numbers of Perls’ Prussian blue-positive melanomacrophage
centers and intraepithelial T-lymphocytes in the proximal convoluted tubules and plasma cells.
The administration of NSS to 4-NP-challenged fish significantly minimized the cytotoxic effect of 4-NP,
maintaining the normal kidney structure, with concentrations of 2.5% and 5% of feed being most effective
for protecting the kidney against 4-NP-induced renal damage.

Research Authors
Mahmoud Abd-Elkareem a, Nasser S. Abou Khalil b, Alaa El-Din H. Sayed c,
Research Journal
Chemosphere
Research Pages
127379
Research Publisher
ElSevier
Research Rank
1
Research Vol
259
Research Website
https://www.sciencedirect.com/science/article/pii/S0045653520315721?via%3Dihub
Research Year
2020

Hepato-nephrotoxicity in late juvenile of Oreochromis niloticus exposed to
gibberellic acid: Ameliorative effect of Spirulina platensis

Research Abstract

The current work intended to inspect the hepato-nephrotoxicity of gibberellic acid (GA3) in juvenile of
Oreochromis niloticus as well as the possibility of restoration after dietary addition of different concentrations of
Spirulina platensis (SP). Fishes were evenly assorted into five groups: Group I assigned as control, Group II fed on
basal diet and exposed to 150 mg/L gibberellic acid (GA3). The 3rd, 4th, and 5th groups exposed to150 mg/L
gibberellic acid (GA3) and previously fed for two months on SP supplemented diets at levels of 5, 20, and 100 g/
kg, respectively. Fish serum were utilized to check glucose, total protein, hepatic and renal functions, enzymatic
and non-enzymatic antioxidants activities (superoxide dismautase; SOD, catalase; CAT, and total antioxidant
capacity; TAC) as well as histopathological alterations in liver and kidney. The results showed that creatinine,
uric acid, liver enzymes, glucose, total protein, SOD, and CAT were significantly elevated in GA3-treated group.
Liver of GA3-treated fish manifested some histopathological changes (hypertrophy, cytoplasmic vacuolization,
and apoptotic cells with pyknotic nuclei, necrosis, dilated blood sinusoids, and lymphocytic aggregation around
the central veins). Kidney of GA3-exposed fish revealed edema of the epithelium lining of some renal tubules and
some showed vacuolar degeneration and dissociation. Hypertrophy in the glomerulus was observed with dilated
blood capillaries. SP supplementation restored these biochemical, antioxidants, and histological changes near to
control levels. This improvement was higher with 100 g/kg SP showing concentration dependency. According to
this study we can conclude that SP supplementation can improve the hepato- and nephrotoxicity caused by GA3
exposure indicating its role as potent antioxidant food additive.

Research Authors
Alaa El-Din H. Sayeda,⁎, Elham A. AbdAllahb, Mohamed Hamedc, Hamdy A.M. Solimand
Research Department
Research Journal
Pesticide Biochemistry and Physiology
Research Member
Research Pages
104600
Research Publisher
ElSevier
Research Rank
1
Research Vol
167
Research Website
https://www.sciencedirect.com/science/article/pii/S004835752030095X?via%3Dihub
Research Year
2020

Comprehensive assessment of benthic diatom (Amphora coffeaeformis ) as a feed additive in Nile tilapia (Oreochromis niloticus ) diet

Research Abstract

Four hundred and fifty Nile tilapia (Oreochromis niloticus), each weighing ca. 4 g, were
randomly allocated into five equal groups in triplicate. The first group acts as control
(A0). A1, A2, A3 and A4 groups were fed on rations supplemented with diatom,
Amphora coffeaeformis, at 2.5, 5.0, 7.5 and 10%, respectively, for 63 days. Assessment
of fish growth, biochemical composition, erythrocyte alterations, gonadal maturation,
serum biomarkers, and liver and intestinal pathogens was carried out to identify
fish welfare. Fish were challenged by Aeromonas hydrophila injection for an additional
14 days; then, mortality rate and some blood parameters were monitored. Results
demonstrated that Amphora sp. insignificantly impacted fish growth, but it induced
significant depletion in lipid content. Blood smear investigation indicated erythrocyte
alterations in A4 group compared with A0 group. Male gonadosomatic index and
relative fecundity demonstrated an increment in A3 and A4 groups respectively. A
boost in fish immunity of A3 group was demonstrated through serum biomarkers and
pathogenic bacterial identification in liver and intestine compared with other groups.
Cumulative mortality of stressed fish was 90% in the A0 group and decreased to 30%
in the A3 group. Blood analysis of stressed fish indicated higher tolerance in the A3
group. In conclusion, Amphora sp. can be used as an immunostimulant for increasing
disease resistance under stress conditions.

Research Authors
Norhan E. Saleh
Rania F. Ismail
Alaa El‐Din H. Sayed
Eman H. Zaghloul
Hosam Saleh
Research Department
Research Journal
Aquaculture Research
Research Member
Research Pages
1-14
Research Publisher
Wiley
Research Rank
1
Research Vol
NULL
Research Website
https://onlinelibrary.wiley.com/doi/full/10.1111/are.14686
Research Year
2020

Bisphenol-A induced antioxidants imbalance and cytokines alteration leading to immune suppression during larval development of Labeo rohita

Research Abstract

Recently, the oxidative stress and immunotoxicity biomarkers have been extensively used in embryotoxicity using fish embryos
as promising models especially after exposure to chemical-like environmental estrogens. Bisphenol-A (BPA) is an estrogenic
endocrine disruptor and is ubiquitous in the aquatic environment. Larvae of Labeo rohita were exposed to low concentrations of
BPA(10, 100, 1000 μg/l) for 21 days. Innate immune system, antioxidants parameters, and developmental alterations were used
as biomarkers. Exposure to BPA caused developmental abnormalities including un-inflated swim bladder, delayed yolk sac
absorption, spinal curvature, and edema of pericardium. Lipid peroxidation increased and activity of catalase (p < 0.05), superoxide
dismutase (p < 0.05), and glutathione peroxidase (p < 0.01) decreased after exposure to BPA. Level of reduced glutathione
also decreased (p < 0.05) in BPA-exposed group. Lower expression of tumor necrosis factor-α (p < 0.05) and interferon-γ
(p < 0.001) was observed in BPA-exposed groups while expression of interleukin-10 increased (p < 0.05) in larvae exposed to
10 μg/l BPA. Moreover, exposure of BPA caused a concentration-dependent increase in expression of heat shock protein 70
(p < 0.05). The present study showed that the exposure to BPA in early life stages of Labeo rohita caused oxidative stress and
suppress NF-κB signaling pathway leading to immunosuppression. The results presented here demonstrate the cross talk between
heat shock protein 70 and cytokines expression.

Research Authors
Mehwish Faheem; Muhammad Adeel, Saba Khaliq, Khalid P. Lone & Alaa El-Din-H-Sayed
Research Department
Research Journal
Environmental Science and Pollution Research

ٍ
Research Member
Research Pages
1-10
Research Publisher
Springer
Research Rank
1
Research Vol
100
Research Website
https://link.springer.com/article/10.1007/s11356-020-08959-y#citeas
Research Year
2020

Generating non-locality correlation via 2-photon resonant interaction of dissipative two-qubit system with coherent field

Research Abstract

In this paper, we introduce analytically the TC-model of two qubits interacting with a coherent
cavity eld via 2-photon process under the intrinsic dissipation e ect. The interaction between the coherent cavity eld and the two qubits, which are initially in an uncorrelated state, leads to generate non-locality qubit-qubit correlations. These correlations are investigated by using trace-norm measurement-induced nonlocality and Bures distance entanglement. It is found that the sudden appearance and sudden disappearance of the qubit-qubit entanglement depend not only on the intrinsic noise but also on the initial coherence intensity. The generated non-locality correlations and their stationary values may be controlled by the physical parameters of the intrinsic noise and the initial coherent eld state.

Research Authors
Abdel-Baset A. Mohamed
Mostafa Hashem
Moataz M. Elkhateeb
Abdel-Shafy F. Obada
Research Department
Research Journal
The European Physical Journal D
Research Member
Research Pages
130
Research Publisher
Springer Nature
Research Rank
1
Research Vol
74
Research Website
https://doi.org/10.1140/epjd/e2020-10115-7
Research Year
2020

Generating non-locality correlation via 2-photon resonant interaction of dissipative two-qubit system with coherent field

Research Abstract

In this paper, we introduce analytically the TC-model of two qubits interacting with a coherent
cavity eld via 2-photon process under the intrinsic dissipation e ect. The interaction between the coherent cavity eld and the two qubits, which are initially in an uncorrelated state, leads to generate non-locality qubit-qubit correlations. These correlations are investigated by using trace-norm measurement-induced nonlocality and Bures distance entanglement. It is found that the sudden appearance and sudden disappearance of the qubit-qubit entanglement depend not only on the intrinsic noise but also on the initial coherence intensity. The generated non-locality correlations and their stationary values may be controlled by the physical parameters of the intrinsic noise and the initial coherent eld state.

Research Authors
Abdel-Baset A. Mohamed
Mostafa Hashem
Moataz M. Elkhateeb
Abdel-Shafy F. Obada
Research Department
Research Journal
The European Physical Journal D
Research Pages
130
Research Publisher
Springer Nature
Research Rank
1
Research Vol
74
Research Website
https://doi.org/10.1140/epjd/e2020-10115-7
Research Year
2020

Generating non-locality correlation via 2-photon resonant interaction of dissipative two-qubit system with coherent field

Research Abstract

In this paper, we introduce analytically the TC-model of two qubits interacting with a coherent
cavity eld via 2-photon process under the intrinsic dissipation e ect. The interaction between the coherent cavity eld and the two qubits, which are initially in an uncorrelated state, leads to generate non-locality qubit-qubit correlations. These correlations are investigated by using trace-norm measurement-induced nonlocality and Bures distance entanglement. It is found that the sudden appearance and sudden disappearance of the qubit-qubit entanglement depend not only on the intrinsic noise but also on the initial coherence intensity. The generated non-locality correlations and their stationary values may be controlled by the physical parameters of the intrinsic noise and the initial coherent eld state.

Research Authors
Abdel-Baset A. Mohamed
Mostafa Hashem
Moataz M. Elkhateeb
Abdel-Shafy F. Obada
Research Department
Research Journal
The European Physical Journal D
Research Member
Research Pages
130
Research Publisher
Springer Nature
Research Rank
1
Research Vol
74
Research Website
https://doi.org/10.1140/epjd/e2020-10115-7
Research Year
2020
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