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1.
Shafia Shafiq Ronok Zahan Samina Yesmin Alam Khan Md. Sabbir Mahmud Md Abu Reza Sarah M. Albogami Mohammed Alorabi Michel De Waard Hebatallah M. Saad Jean-Marc Sabatier Tarannum Naz Gaber El-Saber Batiha 《Molecules (Basel, Switzerland)》2022,27(20)
Litsea glutinosa (L. glutinosa) is considered an evidence-based medicinal plant for the treatment of cancer, the leading cause of death worldwide. In our study, the in vitro antioxidant and in vivo anticancer properties of an essential ethno-medicinal plant, L. glutinosa, were examined using non-toxic doses and a phytochemical analysis was executed using gas-chromatography–mass-spectrometry. The in vitro antioxidant study of the L. glutinosa methanolic extract (LGBME) revealed a concentration-dependent antioxidant property. The bark extract showed promising antioxidant effects in the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay. The strongest antioxidant activity was demonstrated at the maximum concentration (50 µg/mL). The IC50 values of the LGBME and BHT were 5.51 and 5.01 µg/mL, respectively. At the same concentration, the total antioxidant capacity of the LGBME was 0.161 µg/mL and the ferric reducing antioxidant power assay result of the LGBME was 1.783 µg/mL. In the cytotoxicity study, the LD50 of the LGBME and gallic acid were 24.93 µg/mL and 7.23 µg/mL, respectively. In the in vivo anticancer-activity studies, the LGBME, particularly at a dose of 150 mg/kg/bw, showed significant cell-growth inhibition, decreased tumor weight, increased mean survival rate, and upregulated the reduced hematological parameters in EAC (Ehrlich’s ascites carcinoma)-induced Swiss albino mice. The highest cell-growth inhibition, 85.76%, was observed with the dose of 150 mg/kg/bw. Furthermore, the upregulation of pro-apoptotic genes (p53, Bax) and the downregulation of anti-apoptotic Bcl-2 were observed. In conclusion, LGBME extract has several bioactive phytoconstituents, which confirms the antioxidant and anticancer properties of L. glutinosa. 相似文献
2.
Sarosh Iqbal Nimra Naveed Shaikh Khalid Mohammed Khan Shumaila Kiran Sehrish Naz Zaheer Ul-Haq Shahnaz Perveen M. Iqbal Choudhary 《Molecules (Basel, Switzerland)》2022,27(22)
Currently the discovery and development of potent β-glucuronidase inhibitors is an active area of research due to the observation that increased activity of this enzyme is associated with many pathological conditions, such as colon cancer, renal diseases, and infections of the urinary tract. In this study, twenty-seven 2-aminopyrimidine derivatives 1–27 were synthesized by fusion of 2-amino-4,6-dichloropyrimidine with a variety of amines in the presence of triethylamine without using any solvent and catalyst, in good to excellent yields. All synthesized compounds were characterized by EI-MS, HREI-MS and NMR spectroscopy. Compounds 1–27 were then evaluated for their β-glucuronidase inhibitory activity, and among them, compound 24 (IC50 = 2.8 ± 0.10 µM) showed an activity much superior to standard D-saccharic acid 1,4-lactone (IC50 = 45.75 ± 2.16 µM). To predict the binding mode of the substrate and β-glucuronidase, in silico study was performed. Conclusively, this study has identified a potent β-glucuronidase inhibitor that deserves to be further studied for the development of pharmaceutical products. 相似文献
3.
Marva Sandhu Hafiz Muhammad Irfan Shahid Ali Shah Madiha Ahmed Iffat Naz Muhammad Akram Humaira Fatima Ayesha Shuja Farooq 《Molecules (Basel, Switzerland)》2022,27(14)
Oxidative stress (OS) and c-Jun N-terminal kinase (JNK) are both key indicators implicated in neuro-inflammatory signalling pathways and their respective neurodegenerative diseases. Drugs targeting these factors can be considered as suitable candidates for treatment of neuronal dysfunction and memory impairment. The present study encompasses beneficial effects of a naturally occurring triterpenoid, friedelin, against scopolamine-induced oxidative stress and neurodegenerative pathologies in mice models. The treated animals were subjected to behavioural tests i.e., Y-maze and Morris water maze (MWM) for memory dysfunction. The underlying mechanism was determined via western blotting, antioxidant enzymes and lipid profile analyses. Molecular docking studies were carried out to predict the binding modes of friedelin in the binding pocket of p-JNK protein. The results reveal that scopolamine caused oxidative stress by (1) inhibiting catalase (CAT), peroxidase enzyme (POD), superoxide dismutase (SOD), and reduced glutathione enzyme (GSH); (2) the up-regulation of thiobarbituric acid reactive substances (TBARS) in mice brain; and (3) affecting the neuronal synapse (both pre- and post-synapse) followed by associated memory dysfunction. In contrast, friedelin administration not only abolished scopolamine-induced oxidative stress, glial cell activation, and neuro-inflammation but also inhibited p-JNK and NF-κB and their downstream signaling molecules. Moreover, friedelin administration improved neuronal synapse and reversed scopolamine-induced memory impairment accompanied by the inhibition of β-secretase enzyme (BACE-1) to halt amyloidogenic pathways of amyloid-β production. In summary, all of the results show that friedelin is a potent naturally isolated neuro-therapeutic agent to reverse scopolamine-induced neuropathology, which is characteristic of Alzheimer’s disease. 相似文献
4.
Umar Farooq Sara Khan Sadia Naz Tanveer A. Wani Syed Majid Bukhari Abullahi Tunde Aborode Sohail Anjum Shahzad Seema Zargar 《Molecules (Basel, Switzerland)》2022,27(15)
(1) Background: Achillea mellifolium belongs to a highly reputed family of medicinal plants, with plant extract being used as medicine in indigenous system. However, limited data is available regarding the exploitation of the medicinal potential of isolated pure compounds from this family; (2) Methods: A whole plant extract was partitioned into fractions and on the basis of biological activity, an ethyl acetate fraction was selected for isolation of pure compounds. Isolated compounds were characterized using different spectroscopic techniques. The compounds isolated from this study were tested for their medicinal potential using in-vitro enzyme assay, coupled with in-silico studies; (3) Results: Three new acrylic acid derivatives (1–3) have been isolated from the ethyl acetate fraction of Achillea mellifolium. The characterization of these compounds (1–3) was carried out using UV/Vis, FT-IR, 1D and 2D-NMR spectroscopy (1H-NMR, 13C-NMR, HMBC, NOESY) and mass spectrometry. These acrylic acid derivatives were further evaluated for their enzyme inhibition potential against urease from jack bean and α glucosidase from Saccharomyces cerevisiae, using both in-silico and in-vitro approaches. In-vitro studies showed that compound 3 has the highest inhibition against urease enzyme (IC50 =10.46 ± 0.03 μΜ), followed by compound 1 and compound 2 with percent inhibition and IC50 value of 16.87 ± 0.02 c and 13.71 ± 0.07 μΜ, respectively, compared to the standard (thiourea-IC50 = 21.5 ± 0.01 μΜ). The investigated IC50 value of compound 3 against the urease enzyme is two times lower compared to thiourea, suggesting that this compound is twice as active compared to the standard drug. On the other hand, all three compounds (1–3) revealed mild inhibition potential against α-glucosidase. In-silico molecular docking studies, in combination with MD simulations and free energy, calculations were also performed to rationalize their time evolved mode of interaction inside the active pocket. Binding energies were computed using a MMPBSA approach, and the role of individual residues to overall binding of the inhibitors inside the active pockets were also computed; (4) Conclusions: Together, these studies confirm the inhibitory potential of isolated acrylic acid derivatives against both urease and α-glucosidase enzymes; however, their inhibition potential is better for urease enzyme even when compared to the standard. 相似文献
5.
Aydin Tavman Naz M. Agh-Atabay Sadik Guner Fahrettin Gucin Basaran Dulger 《Transition Metal Chemistry》2007,32(2):172-179
2-(5-H/Me/Cl-1H-benzimidazol-2-yl)-phenol ligands form 1:1 electrolytes, 5-coordinate monometallic complexes with iron(III) nitrate. The geometry of the [Fe(L)(OH)(H2O)2](NO3) complexes was derived from theoretical calculation in DGauss/DFT level (DZVP basis set) on CACHE. In all of the complexes
the ligands are bidentate, via one imine nitrogen atom and phenolate oxygen atom. The coordination is completed with a hydroxide ion, and two water molecules,
adopting a distorted square pyramidal geometry. The structures of the compounds were confirmed on the basis of elemental analysis,
molar conductivity, magnetic moment, FT-Raman, FT-IR (mid-IR, far-IR), EPR and u.v.–vis. The antimicrobial activities of the
free ligands, their hydrochloride salts, and the complexes were evaluated using the disk diffusion method in dimethyl sulfoxide
(DMSO) as well as the minimal inhibitory concentration (MIC) dilution method, against nine bacteria and the results are compared
with several known antibiotic agents. Antifungal activities were reported for Candida albicans, Kluyveromyces fragilis, Rhodotorula rubra, Debaryomyces hansenii, Hanseniaspora guilliermondii, and the results were referenced against nystatin, ketaconazole, and clotrimazole antifungal agents. In most cases, the compounds
tested showed broad-spectrum (Gram+ & Gram− bacteria) activities that were either more active or as potent as the references. 相似文献
6.
Hasan M. Khan Shagufta Naz Safia Tabassum 《Journal of Radioanalytical and Nuclear Chemistry》2011,289(1):225-229
Aqueous solution of crystal violet has been evaluated spectrophotometrically as a gamma-ray chemical dosimeter. The response
of the chemical dosimetric system has also been investigated under different environmental conditions, such as light and temperature.
In the present study the response has been measured at two wavelengths; 588 nm (λmax of the irradiated solution) and 500 nm. The response of the crystal violet dosimeter was linear in the dose range of 50–550 Gy
at pH 5.6 when absorption measurements were made at 588 and 500 nm. The response of the crystal violet dosimeter during post-irradiation
storage at room temperature in dark showed slight decrease in absorbance at 588 and 510 nm but the response was almost stable
at 460 nm. For higher doses, the change in the response was greater as compared to the low doses. Post-irradiation stability
during diffused sunlight showed significant decrease in the response for higher dose at 588 and 510 nm and slower decrease
in the response for lower dose at the above mentioned wavelengths. However the response was almost stable up to 97 days at
460 nm for higher and lower doses. At 4 °C, the decrease in the absorbance was slower at 588 and 510 nm while the response
was almost constant at 460 nm. At higher temperatures, such as 40 °C, the decrease in the absorbance was greater at 588 and
510 nm while at 460 nm the absorbance was almost constant for about 3 months. 相似文献
7.
Melek Naz Guven Ece Akyol Fatma Demir Duman Havva Yagci Acar Ozlem Karahan Duygu Avci 《Journal of polymer science. Part A, Polymer chemistry》2017,55(19):3195-3204
Incorporation of bisphosphonate/bisphosphonic acid groups in dental monomer structures should increase interaction of these monomers with dental tissue as these groups have strong affinity for hydroxyapatite. Therefore, new urea dimethacrylates functionalized with bisphosphonate (1a, 1b) and bisphosphonic acid (2a, 2b) groups are synthesized and evaluated for dental applications. Monomers 1a and 1b are synthesized from 2‐isocyanatoethyl methacrylate (IEM) and two bisphosphonated amines (BPA1 and BPA2), prepared as reported elsewhere. Selective dealkylation of the bisphosphonate ester groups of 1a and 1b using trimethylsilyl bromide (TMSBr) gives monomers (2a and 2b) with bisphosphonic acid functionality. X‐ray diffractometer (XRD), Raman spectroscopy, and X‐ray photoelectron spectroscopy (XPS) analyses of monomer‐treated HAP particles show that 2a induces formation of stable monomer‐calcium salts, similar to 10‐methacryloyloxydecyl dihydrogen phosphate (MDP), with higher chemical interaction than 2b. The photopolymerization studies indicate good copolymerizability with commercial dental monomers. In vitro studies on NIH 3T3 mouse embryonic fibroblast cells have clearly shown that the tested monomers (1b and 2b) are not toxic according to the MTT standards. All these properties make these monomers suitable as biocompatible cross‐linkers/adhesives for dental applications. © 2017 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2017 , 55, 3195–3204 相似文献
8.
Effects of porous medium have been investigated on the steady flow of a third grade fluid between two stationary porous plates. The continuity and momentum equations along with modified Darcy??s law are used for the development of mathematical problem. The governing nonlinear problem is solved by a homotopy analysis method. The dimensionless velocity and shear stresses at the plates are analyzed. 相似文献
9.
Farah Naz Bibimaryam Mousavi Zhixiong Luo Christia Jabbour Philippe M. Heynderickx Somboon Chaemchuen Francis Verpoort 《应用有机金属化学》2019,33(5)
A series of spray dried zeolitic imidazolate frameworks (ZIFs = ZIF‐8, ZIF‐67, and Zn/Co‐ZIF) are used as a catalyst for the bulk ring‐opening polymerization of δ‐valerolactone without any co‐catalyst to generate polyvalerolactone. Interestingly, using the same catalyst under the same reaction conditions could manipulate the structure of the product polymer, and thus its physical properties. Thus, using a dried substrate leads to the formation of the cyclic polymer while a linear polymer was formed on using the commercially available substrate. An activated monomer mechanism has been suggested where the propagating zinc alkoxide undergoes an intramolecular transesterification to release cyclic or linear polyvalerolactone. The ROP of δ‐VL without drying shows that the polymeric zwitterions have little tendency to cyclize in the presence of moisture. At 140 °C, ZIF‐8 shows a superior catalytic activity resulting in the production of cyclic polyvalerolactone having a high molecular weight as compared to ZIF‐67 or Zn/Co‐ZIF due to the presence of highly active sites. The catalyst could be recycled and reused without any significant loss of catalytic activity. 相似文献
10.
Saba NAZ Muhammad SALMAN Usman ALI Imran JAVAID Syed Ahtsham-ul-Haq BOKHARY 《数学学报(英文版)》2014,30(7):1145-1160
In this paper,we consider the family of generalized Petersen graphs P(n,4).We prove that the metric dimension of P(n,4) is 3 when n ≡ 0(mod 4),and is 4 when n = 4k + 3(k is even).For n ≡ 1,2(mod 4) and n = 4k + 3(k is odd),we prove that the metric dimension of P(n,4) is bounded above by 4.This shows that each graph of the family of generalized Petersen graphs P(n,4)has constant metric dimension. 相似文献