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      • KCI등재

        Inhibitory potential of rutin and rutin nano-crystals against Helicobacter pylori, colon cancer, hemolysis and Butyrylcholinesterase in vitro and in silico

        Qanash Husam,Al-Rajhi Aisha M. H.,Almashjary Majed N.,Basabrain Ammar A.,Hazzazi Mohannad S.,Abdelghany Tarek M. 한국응용생명화학회 2023 Applied Biological Chemistry (Appl Biol Chem) Vol.66 No.-

        Despite the vital activity of many compounds, they lack that effectiveness due to their low solubility in water. Unfortunately, for this reason, rutin often leads to low tissue permeability and insufficient bioavailability, which has greatly limited its pharmacological utility. Therefore, the present investigation is designed to overcome this problem by formulating the rotin to rotin nanocrystals (RNCs) with studying their some pharmacological applications in vitro and in silico. RNCs were created via the ultrasonication approach and showed a spherical shape via Transmission electron microscopy with a mean particle size of 27 nm. RNCs reflected inhibitory action against Helicobacter pylori with an inhibition zone (IZ) of 22.67 mm compared to rutin (IZ of 18 mm) and standard control (IZ of 19.5 mm). RNCs exhibited less minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) (7.8 µg/mL) than rutin (62.5 µg/mL). The MBC/MIC index of rutin and RNCs indicated their bactericidal properties. RNCs were more acutely (92.12%) than rutin (85.43%) for inhibition the H. pylori biofilm formation. A promising half maximal inhibitory concentration (IC50) (6.85 µg/mL) was recorded using RNCs for urease inhibition compared to the IC50 value of rutin (97.8 µg/mL). The activity of rutin and RNCs was tested against cancer cells of human colon cancer (HT-29) and normal Vero cells. IC50 values of RNCs were less 168.23 ± 1.15 µg/mL and 297.69 ± 4.23 µg/mL than the IC50 values of rutin 184.96 ± 4.33 µg/mL and 335.31 ± 2.02 µg/mL against HT-29 cells and normal Vero cells, respectively. Different percentages (72.2, 77.3, and 81.9%) of hemolysis inhibition were recorded using RNCs, but 63.6, 68.9, 73.6, and 80.6% were obtained using rutin at 600, 800, and 1000 µg/mL, respectively. Butyrylcholinesterase (BChE) inhibition % was documented at a lower IC50 value for RNCs (12.74 µg/mL) than the IC50 of rutin (18.15 µg/mL). The target molecule underwent molecular docking research against H. pylori [Protein Data Bank (PDB) code: 4HI0], HT-29 cells (PDB code: 2HQ6), and BChE (PDB code: 6EMI) in order to enhance the interactions between rutin and the chosen receptors and to estimate its molecular operating environment (MOE) affinity scoring. Rutin has predicted strong binding interactions and potent activity against the examined proteins 4HI0, 2HQ6, and 6EMI with low binding scores of − 7.47778 kcal/mol, − 7.68511 kcal/mol, and − 9.50333 kcal/mol, respectively.

      • KCI등재

        In vitro repress of breast cancer by bio-product of edible Pleurotus ostreatus loaded with chitosan nanoparticles

        Al-Rajhi Aisha M. H.,Ghany Tarek M. Abdel 한국응용생명화학회 2023 Applied Biological Chemistry (Appl Biol Chem) Vol.66 No.-

        Despite advances in early detection and therapy, cancer still is a significant health challenge with the highest priority for investigation. Breast cancer represents the most common cancerous disease among women in the world. The study’s purpose is to estimate the cytotoxic activity of the edible mushroom Pleurotus ostreatus extract (PE), chitosan nanoparticles (ChNPs), and PE loaded with ChNPs (PELChNPs), as well as to identify the molecular docking of the cytotoxicity of methyl gallate (MG) as a main component of the PE against breast cancer (MCF-7) cell line. High-performance liquid chromatography (HPLC) analysis of PE exhibited the existence of various phenolic and flavonoid compounds such as MG, gallic acid, chlorogenic acid, hesperetin, naringenin, rutin, and cinnamic acid. The proliferation of the MCF-7 cell line was inhibited at 1, 3.9, and 62.50 µg/mL of PELChNPs, PE, and ChNPs, respectively. PELChNPs were more effective against the MCF-7 cell line than PE, particularly at low concentrations. For instance, at 7.8 µg/mL of PELChNPs and PE, the inhibitory % of MCF-7 proliferation was 20.59±1.75% and 8.57±0.59%, respectively. At 15.6 µg/mL of PELChNPs and PE, the inhibitory % of MCF-7 proliferation was 51.37±1.09% and 25.18±1.64%, respectively. While there is slight difference in the inhibition % of MCF-7 cells (98.64±0.21 and 97.22±0.16%) at high concentration 500 µg/mL of PELChNPs and PE, respectively. IC50 was 15.25 ± 0.54 µg/mL, 46.27 ± 1.94 µg/mL, and 337.38 ± 13.68 µg/mL against MCF-7 cell line of PELChNPs, PE, and ChNPs, respectively. The value of IC50 documented the efficacy of PELChNPs compared with the IC50 (5.91 ± 0.43 µg/mL) of Vinblastine sulfate. Noticeable distortions were observed in the MCF-7 cell line mainly treated with PELChNPs, followed by PE alone. While ChNPs exhibited less effect on the morphology of the MCF-7 cell line. Antioxidant activity of ChNPs, PE, and PELChNPs was evaluated compared with Trolox, which reflected IC50 = 118.33 ± 4.02, 85.63 ± 3.96, 36.80 ± 2.52 and 24.74 ± 0.45 µg/mL. Methyl gallate binding interactions were assessed using molecular docking with the MOE-Dock tool against the target crystal structures of Breast cancer cell line 3HB5. The results shed light on how molecular modeling techniques can inhibit methyl gallate with possible uses in treating breast cancer.

      • KCI등재

        In situ green synthesis of Cu‑doped ZnO based polymers nanocomposite with studying antimicrobial, antioxidant and anti‑inflammatory activities

        Al-Rajhi Aisha M. H.,Yahya Rana,Bakri Marwah M.,Yahya Reham,Abdelghany T. M. 한국응용생명화학회 2022 Applied Biological Chemistry (Appl Biol Chem) Vol.65 No.3

        The use of eco-friendly methods for the synthesis of nanoparticles and its nano-composite has become a public demand nowadays to reduce the risks of chemical methods. In the current study, green synthesis of Cu-doped ZnO based polymers nan-ocomposite was performed. Various instrumental analysis including UV–vis, ATR-FTIR spectroscopy, XRD, SEM coupled with energy dispersive X-ray analysis, TEM and Thermal gravimetric were used to characterize nano-composite. Highly antibacterial activity of the synthesized nano-composite was recorded against tested microorganisms with promising efficacy against bacteria namely; Bacillus subtilis, Staphylococcus aureus, Enterococcus faecalis, Proteus vulgaris, Pseudomonas aeruginosa, Escherichia coli, Salmonella typhimurium and yeast (Candida albicans) but unfortunately not against black fungus (Mucor circinelloides) and filamentous fungi Aspergillus flavus and A. niger. Anti-inflammatory of nano-composite represented by hemolysis inhibition was observed at using low concentration (100 μg/mL) with enhancing 23.85% compared with free nano-composite while at high concentrations 500 and1000 μg/mL the anti-inflammatory activity was approximately similar with enhancing 3.91% and 1.99%, respectively. Antioxidant of the nano-composite was better than the antioxidant of free nano-composite at all tested concentrations, moreover the IC50 of the nano-composite (91.16 μg/mL) was less than the IC50, (203.65 μg/mL) of the free nano-composite.

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