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1.
Biol Open ; 12(8)2023 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-37581305

RESUMO

This review highlights the largely understudied behavior of gliding locomotion, which is exhibited by a diverse range of animals spanning vertebrates and invertebrates, in air and in water. The insights in the literature gained from January 2022 to December 2022 continue to challenge the previously held notion of gliding as a relatively simple form of locomotion. Using advances in field/lab data collection and computation, the highlighted studies cover gliding in animals including seabirds, flying lizards, flying snakes, geckos, dragonflies, damselflies, and dolphins. Altogether, these studies present gliding as a sophisticated behavior resulting from the interdependent aspects of morphology, sensing, environment, and likely selective pressures. This review uses these insights as inspiration to encourage researchers to revisit gliding locomotion, both in the animal's natural habitat and in the laboratory, and to investigate questions spanning gliding biomechanics, ecology, sensing, and the evolution of animal flight.


Assuntos
Lagartos , Odonatos , Animais , Asas de Animais/anatomia & histologia , Locomoção , Voo Animal , Fenômenos Biomecânicos
2.
Molecules ; 27(7)2022 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-35408703

RESUMO

Three rings 2-hydroxypyridine liquid crystalline compounds have been prepared and fully characterized. The mesomorphic behavior of the prepared compounds has been investigated in terms of differential scanning calorimetry (DSC) and polarized optical microscopy (POM). Moreover, a comparative study between the prepared compounds and previously reported analogs has been discussed in terms of the orientation and position of the mesogenic core, in addition to the direction of the terminal alkyl chains. Furthermore, a detailed computational approach has been studied to illustrate the effect of geometrical and dimensional parameters on the type of the enhanced texture and the mesomorphic range and stability. The results of the DFT study revealed that the orientation of the mesogen could affect the mesomorphic behavior and this has been attributed in terms of the degree of the polarizability of the linking groups. This result has been confirmed by calculation of the net dipole moment and the molecular electrostatic potential that show how the mesogen orientation and position could impact the molecular charge separation. Finally, the effect of the pyridyl group has been also investigated in terms of the calculated aromaticity index and the π-π stacking.


Assuntos
Cristais Líquidos , Varredura Diferencial de Calorimetria , Ésteres , Cristais Líquidos/química , Bases de Schiff/química , Espectroscopia de Infravermelho com Transformada de Fourier
3.
Int J Mol Sci ; 22(19)2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34638665

RESUMO

Matrix metalloproteinases (MMPs) are key signaling modulators in the tumor microenvironment. Among MMPs, MMP-2 and MMP-9 are receiving renewed interest as validated druggable targets for halting different tumor progression events. Over the last decades, a diverse range of MMP-2/9 inhibitors has been identified starting from the early hydroxamic acid-based peptidomimetics to the next generation non-hydroxamates. Herein, focused 1,2,4-triazole-1,2,3-triazole molecular hybrids with varying lengths and decorations, mimicking the thematic features of non-hydroxamate inhibitors, were designed and synthesized using efficient protocols and were alkylated with pharmacophoric amines to develop new Mannich bases. After full spectroscopic characterization the newly synthesized triazoles tethering Mannich bases were subjected to safety assessment via MTT assay against normal human fibroblasts, then evaluated for their potential anticancer activities against colon (Caco-2) and breast (MDA-MB 231) cancers. The relatively lengthy bis-Mannich bases 15 and 16 were safer and more potent than 5-fluorouracil with sub-micromolar IC50 and promising selectivity to the screened cancer cell lines rather than normal cells. Both compounds upregulated p53 (2-5.6-fold) and suppressed cyclin D expression (0.8-0.2-fold) in the studied cancers, and thus, induced apoptosis. 15 was superior to 16 in terms of cytotoxic activities, p53 induction, and cyclin D suppression. Mechanistically, both were efficient MMP-2/9 inhibitors with comparable potencies to the reference prototype hydroxamate-based MMP inhibitor NNGH at their anticancer IC50 concentrations. 15 (IC50 = 0.143 µM) was 4-fold more potent than NNGH against MMP-9 with promising selectivity (3.27-fold) over MMP-2, whereas 16 was comparable to NNGH. Concerning MMP-2, 16 (IC50 = 0.376 µM) was 1.2-fold more active than 15. Docking simulations predicted their possible binding modes and highlighted the possible structural determinants of MMP-2/9 inhibitory activities. Computational prediction of their physicochemical properties, ADMET, and drug-likeness metrics revealed acceptable drug-like criteria.


Assuntos
Ácidos Hidroxâmicos/farmacologia , Bases de Mannich/farmacologia , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/metabolismo , Inibidores de Metaloproteinases de Matriz/farmacologia , Triazóis/farmacologia , Antineoplásicos/farmacologia , Células CACO-2 , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Humanos , Micro-Ondas , Simulação de Acoplamento Molecular , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
4.
Chemometr Intell Lab Syst ; 217: 104421, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-34538993

RESUMO

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a pandemic fatal infection with no known treatment. The severity of the disease and the fast viral mutations forced the scientific community to search for potential solution. Here in the present manuscript, some benzofused1,2,3triazolesulfonamide hybrids were synthesized and evaluated for their anti- SARS-CoV-2 activity using in silico prediction then the most potent compounds were assessed using in-Vitro analysis. The in-Silico study was assessed against RNA dependent RNA polymerase, Spike protein S1, Main protease (3CLpro) and 2'-O-methyltransferase (nsp16). It was found that 4b and 4c showed high binding scores against RNA dependent RNA polymerase reached -8.40 and -8.75 â€‹kcal/mol, respectively compared to the approved antiviral (remdesivir -6.77 â€‹kcal/mol). Upon testing the binding score with SARS-CoV-2 Spike protein it was revealed that 4c exhibited the highest score (-7.22 â€‹kcal/mol) compared to the reference antibacterial drug Ceftazidime (-6.36 â€‹kcal/mol). Surprisingly, the two compounds 4b and 4c showed the highest binding scores against SARS-CoV-2 3CLpro (-8.75, -8.48 â€‹kcal/mol, respectively) and nsp16 (- 8.84 and - 8.89 â€‹kcal/mol, respectively) displaying many types of interaction with all the enzymes binding sites. The derivatives 4b and 4c were examined in vitro for their potential anti-SARS-CoV-2 and it was revealed that 4c was the most promising compound with IC50 reached 758.8108 â€‹mM and complete (100%) inhibition of the binding of SARS-CoV-2 virus to human ACE2 can be accomplished by using 0.01 â€‹mg.

5.
Ann Parasitol ; 67(1): 117-121, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34022782

RESUMO

Thirty-five white-spotted geckos, Tarentola annularis were collected from Shendi area, River Nile State, Sudan, between June and September 2019 and examined for the presence of haemoparasites infection. Six (17.14%) geckos were found to be positive for intra erythrocytic haemogregarine (Apicomplexa: Haemogregarinidae) species with a mean overall infection intensity of 1.20% ± 0.32 and parasitemia level between ~0.70% and ~1.70%. However, most parasite gamonts were found intracellular, and no damage on the infected erythrocytes was observed. The prevalence of infection between adult and juvenile geckos was significantly different (P = 0.012); however, no substantial difference between males and females was found. On the other hand, the mean intensity of infection did not differ between adult and juvenile geckos. In conclusion, no obvious negative impact on the local T. annularis gecko community was observed due to haemogregarine species infection.


Assuntos
Eucoccidiida , Lagartos , Parasitos , Animais , Feminino , Masculino , Prevalência , Sudão/epidemiologia
6.
Ann Parasitol ; 66(1): 115­118, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32199004

RESUMO

Three hundred and sixty fecal samples of stray dogs were collected between July and December 2018, from open grounds of Shendi city and two suburbs (Gulia and Musiab), River Nile State, Sudan, and were examined for helminthic infections. The results showed 43 (11.9%) of the samples were positive for at least one species of helminth. A total of four helminth species were identified, including two nematodes (Ancylostoma caninum and Trichuris vulpis) and two cestodes (Dipylidium caninum and Taenia spp.). Taenia spp. was found to be the most common helminth infection in stray dogs (6.7%) followed by D. caninum (3.1%), while the least was the nematode, A. caninum (0.8%). The prevalence of infection among stray dogs in the suburbs was found to be higher than those in the city; however, there was no statistical significance (P = 0.07). In conclusion, stray dogs in Shendi area were found to be harboring several important zoonotic helminthes such as A. caninum and Taenia spp.; this shows the necessity of stray dog population management in this area as they present a health risk to the community.


Assuntos
Doenças do Cão , Helmintíase Animal , Helmintos , Enteropatias Parasitárias , Animais , Doenças do Cão/epidemiologia , Doenças do Cão/parasitologia , Cães/parasitologia , Fezes/parasitologia , Helmintíase Animal/epidemiologia , Helmintíase Animal/parasitologia , Helmintos/isolamento & purificação , Enteropatias Parasitárias/epidemiologia , Enteropatias Parasitárias/veterinária , Prevalência , Sudão/epidemiologia
7.
Iran J Parasitol ; 12(2): 284-291, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28761490

RESUMO

BACKGROUND: Schistosomiasis is a debilitating disease, infects millions of people in tropical and subtropical regions. This study assessed the situation of the urinary schistosomiasis among schoolchildren of the Alsaial Alsagair village, Sudan. METHODS: A cross-sectional survey was carried out in 2016, in the Alsaial Alsagair village, and 385 samples of urine were collected and processed using the centrifugation/sedimentation technique. RESULTS: The overall prevalence and intensity of the disease among the pupils studied were 1.82% and 40.1 eggs/10ml urine, respectively. The prevalence of infection among male pupils was 3.1%, and for females was 0.52%, while the intensity among males was 42.3 eggs/10ml and for females was 27 eggs/10ml urine. No significant difference in the disease prevalence between the 7-10 yr age group and the 11-14 yr age group was found, while the over 14 yr age group was found to be free from infection. However, a considerably higher intensity of the parasite was found among the 7-10 yr age group compared to the other age group infected. A high prevalence and intensity of infection was observed among pupils who were active in swimming and working in the fields. Most of the pupils interviewed were found to be unaware of the disease and the prevalence and intensity of the infection was found to be higher among the group who were aware of the disease. CONCLUSION: Findings show the need for an integrated control program against urinary schistosomiasis including the treatment of all infected children and the implementation of a health education program.

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