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Peedikayil Arshida Thottile,Lee Jiseong,Abdelgawad Mohamed A.,Ghoneim Mohammed M.,Shaker Mohamed E.,Selim Samy,Kumar Sunil,Dev Sanal,Kim Hoon,Mathew Bijo 한국응용생명화학회 2023 Applied Biological Chemistry (Appl Biol Chem) Vol.66 No.-
Monoamine oxidases (MAOs) regulate neurotransmitters, and changes in their regulation lead to neurogenerative diseases (NDs). Therefore, MAO inhibitors are used to treat NDs. Ferulic acid, a phenolic compound found in various plant species, has been demonstrated to have a variety of biological functions, including anti-inflammatory, anticancer, and neuroprotective effects. In this study, ten ferulic acid hydrazide derivatives (FA1–FA10) were synthesized, and their ability to inhibit monoamine oxidase (MAO) enzymes was tested. Six candidates demonstrated a more pronounced pattern of inhibitory action against MAO-B than against MAO-A. FA3 had the highest inhibitory efficacy in MAO-B inhibition (IC50 value of 1.88 μM), followed by FA9 (2.08 μM). FA3 has a Ki of 1.92 ± 0.73 μM. A reversibility experiment of MAO-B inhibition by FA3 was conducted using dialysis, and the recovery pattern showed FA3 was a reversible MAO-B inhibitor with a similar recovery to safinamide, a reversible reference inhibitor. These results indicate that FA3 is an effective reversible MAO-B inhibitor. In molecular dynamics and docking, FA3 paired with pi-pi stacking helped stabilize the protein ligand in the active site of MAO-B. According to this study, lead compounds can be used as therapeutic agents to treat neurological conditions, such as Parkinson's disease (PD).
A Bioactive Fraction from Streptomyces sp. Enhances Maize Tolerance against Drought Stress
Warrad Mona,Hassan Yasser M.,Mohamed Mahmoud S.M,Hagagy Nashwa,Al-Maghrabi Omar A,Selim Samy,Saleh Ahmed M.,AbdElgawad Hamada 한국미생물·생명공학회 2020 Journal of microbiology and biotechnology Vol.30 No.8
Drought stress is threatening the growth and productivity of many economical crops. Therefore, it is necessary to establish innovative and efficient approaches for improving crop growth and productivity. Here we investigated the potentials of the cell-free extract of Actinobacteria (Ac) isolated from a semi-arid habitat (Al-Jouf region, Saudi Arabia) to recover the reduction in maize growth and improve the physiological stress tolerance induced by drought. Three Ac isolates were screened for production of secondary metabolites, antioxidant and antimicrobial activities. The isolate Ac3 revealed the highest levels of flavonoids, antioxidant and antimicrobial activities in addition to having abilities to produce siderophores and phytohormones. Based on seed germination experiment, the selected bioactive fraction of Ac3 cell-free extract (F2.7, containing mainly isoquercetin), increased the growth and photosynthesis rate under drought stress. Moreover, F2.7 application significantly alleviated drought stress-induced increases in H2O2, lipid peroxidation (MDA) and protein oxidation (protein carbonyls). It also increased total antioxidant power and molecular antioxidant levels (total ascorbate, glutathione and tocopherols). F2.7 improved the primary metabolism of stressed maize plants; for example, it increased in several individuals of soluble carbohydrates, organic acids, amino acids, and fatty acids. Interestingly, to reduce stress impact, F2.7 accumulated some compatible solutes including total soluble sugars, sucrose and proline. Hence, this comprehensive assessment recommends the potentials of actinobacterial cell-free extract as an alternative ecofriendly approach to improve crop growth and quality under water deficit conditions.
Khaled R. A. Abdellatif,Mohamed A. Abdelgawad,Heba A. H. Elshemy,Shahinda S. R. Alsayed 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.11
Anovel series of 2-pyrazoline derivatives 13a–l wassynthesized via aldol condensation of 4-substituted acetophenoneswith appropriately substituted aldehydes followed by cyclizationof the formed chalcones with 4-hydrazinobenzenesulfonamidehydrochloride. The chemical structures of the targetpyrazoline derivatives were proved by means of IR, 1HNMR, 13CNMR, mass spectroscopy and elemental analyses data. All thesynthesized compounds were evaluated for their cyclooxygenaseselectivity, anti-inflammatory and ulcerogenic liability. Whilecompounds 13e, 13h and 13i showed moderate COX-2 selectivityin vitro and good anti-inflammatory activity in vivo, compound13i showed the highest anti-inflammatory activity that isvery close in potency to the reference drug (celecoxib) with bettergastric profile than celecoxib.