New pyrazolone derivatives, synthesis, characterization, and neuroprotective effect against PTZ- induced neuroinflammation in mice

سال انتشار: 1401
نوع سند: مقاله ژورنالی
زبان: انگلیسی
مشاهده: 172

فایل این مقاله در 9 صفحه با فرمت PDF قابل دریافت می باشد

استخراج به نرم افزارهای پژوهشی:

لینک ثابت به این مقاله:

شناسه ملی سند علمی:

JR_IJBMS-25-12_003

تاریخ نمایه سازی: 25 آبان 1401

چکیده مقاله:

Objective(s): The study was aimed at synthesis of the new derivatives of the pyrazolone nucleus, and their spectroscopic and pharmacological analysis and evaluation. Materials and Methods: Three series of compounds, with ۲-picolinic acid (I a-d), ۳-picolinic acid (II a-d), and ۴-picolinic acid (III a-d) were synthesized and characterized by FT-IR, ۱HNMR, ۱۳C NMR, elemental, and melting points. The new compounds were then evaluated for their anti-oxidant, anti-inflammatory, and anti-epileptic potential. The hind paw edema model was used to screen anti-inflammatory potential, while the anticonvulsant effect was evaluated by employing the acute model of anti-epileptic activity. The in vivo anti-oxidant potential was determined through glutathione (GSH), glutathione-S-transferase (GST), catalase, and lipid peroxidase enzyme (LPO) assays. The expression of key biomarkers involved in inflammation and neuroprotection, including tumor necrotic factors alpha (TNF-α) and phosphorylated nuclear factor kappa B (NF-κB), was detected through enzyme-linked immunosorbent assay (ELISA) and Western blot analysis. Results: The tested compounds showed anti-oxidant potential. The selected compounds exhibited good anti-inflammatory potential. The PTZ-induced elevation of these inflammatory mediators and oxidative stress were ameliorated significantly by the selected compound Ic. Results of molecular analysis (ELISA and Western blot analysis) for potent compound Ic showed a prominent inhibitory effect against neuroinflammatory mediators, including TNF-α and NF-κB. Conclusion: It is concluded that the derivative Ic ameliorated PTZ-induced seizures, oxidative stress, and inflammatory cascades by regulating the NF-κB/ TNF-α/ROS pathway.

کلیدواژه ها:

Anticonvulsant ، Anti-inflammatory ، Anti-oxidant ، Enzyme-linked - immunosorbent assay (ELISA) ، Pyrazolone ، Western blot

نویسندگان

Madiha Kanwal

Department of Pharmaceutical Chemistry, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

Sadia Sarwar

Department of Pharmacognosy, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

Humaira Nadeem

Department of Pharmaceutical Chemistry, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

Athar Ata

Department of Chemistry, University of Manitoba, Canada

Fawad Shah

Department of Pharmacology, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

Sumra Malik

Department of Pharmaceutical Chemistry, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

Saima Maqsood

Department of Pharmaceutical Chemistry, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

Ghulam Miana

Department of Pharmaceutical Chemistry, Riphah International University, Islamabad, Pakistan, ۴۴۰۰۰

مراجع و منابع این مقاله:

لیست زیر مراجع و منابع استفاده شده در این مقاله را نمایش می دهد. این مراجع به صورت کاملا ماشینی و بر اساس هوش مصنوعی استخراج شده اند و لذا ممکن است دارای اشکالاتی باشند که به مرور زمان دقت استخراج این محتوا افزایش می یابد. مراجعی که مقالات مربوط به آنها در سیویلیکا نمایه شده و پیدا شده اند، به خود مقاله لینک شده اند :
  • Orabi EA, Orabi MAA, Mahross MH, Abdel-Hakim M. Computational investigation ...
  • Anderson RC. The chemistry of heterocyclic compounds. pyrazolones, pyrazolidones, and ...
  • Ahsan MJ, Khalilullah H, Stables JP, Govindasamy J. Synthesis and ...
  • Brogden RN. Pyrazolone derivatives. Drugs ۱۹۸۶; ۳۲:۶۰-۷۰ ...
  • Brune K. The early history of non-opioid analgesics. Acute Pain ...
  • Knorr L. Einwirkung von acetessigester auf phenylhydrazin. Ber Deutsch Chem ...
  • Abdel-Aziz M, Abuo-Rahma GE-DA, Hassan AA. Synthesis of novel pyrazole ...
  • Khalifa MM, Abdelbaky NA. Synthesis of new imidazolyl acetic acid ...
  • Sun ZQ, Meng FH, Tu LX, Sun L. Myricetin attenuates ...
  • McMurray KM, Distler MG, Sidhu PS, Cook JM, Arnold LA, ...
  • Queda F, Calò S, Gwizdala K, Magalhães JD, Cardoso SM, ...
  • Dede F, Karadenizli S, Ozsoy OD, Eraldemir FC, Sahin D, ...
  • Singh N, Saha L, Kumari P, Singh J, Bhatia A, ...
  • Wang H, Yan H, Wang K, Wang J. Dynamic regulation ...
  • Bhattacharya A, Derecki NC, Lovenberg TW, Drevets WC. Role of ...
  • Young I, Woodside J. Anti-oxidants in health and disease. J ...
  • Nimse SB, Pal D. Free radicals, natural antioxidants, and their ...
  • Chen Y, Xiao H, Zheng J, Liang G. Structure-thermodynamics-antioxidant activity ...
  • Wright JS, Johnson ER, DiLabio GA. Predicting the activity of ...
  • Melov S, Ravenscroft J, Malik S, Gill MS, Walker DW, ...
  • Rajendran P, Nandakumar N, Rengarajan T, Palaniswami R, Gnanadhas EN, ...
  • Sidhaye R, Dhanawade A, Manasa K, Aishwarya G. Synthesis, antimicrobial ...
  • Eldehna ME, Fares M, Abdel-Aziz MM, Abdel Aziz HA ...
  • Design, Synthesis and Antitubercular Activity of Certain NicotinicAcid Hydraziides. Molecules ...
  • Patel JB, Sen DJ. Synthesis and biological evaluation of some ...
  • Hasan SR, Hossain MM, Akter R, Jamila M, Mazumder MEH, ...
  • Li Y-C, Xian Y-F, Ip S-P, Su Z-R, Su J-Y, ...
  • Blakaj DM, McConnell KJ, Beveridge DL, Baranger AM. Molecular dynamics ...
  • Rana I, Khan N, Ansari MM, Shah FA, ud Din ...
  • Al Kury LT, Zeb A, Abidin ZU, Irshad N, Malik ...
  • Khan A, Shal B, Naveed M, Shah FA, Atiq A, ...
  • Hadwan MH. Simple spectrophotometric assay for measuring catalase activity in ...
  • Irshad N, Khan A-u, Iqbal MS. Antihypertensive potential of selected ...
  • Anwar T, Nadeem H, Sarwar S, Naureen H, Ahmed S, ...
  • Surati KR, Sathe PA. Schiff base pyrazolone complexes of iron ...
  • K Okla M, Alamri SA, Alaraidh IA, AL‐ghamdi AA, Soufan ...
  • Minnelli C, Laudadio E, Galeazzi R, Rusciano D, Armeni T, ...
  • Vallés SL, Blanco AM, Pascual M, Guerri C. Chronic ethanol ...
  • Alfonso-Loeches S, Pascual-Lucas M, Blanco AM, Sanchez-Vera I, Guerri C. ...
  • نمایش کامل مراجع