Click for new scientific resources and news about Corona[COVID-19]

Paper Information

Journal:   IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES   DECEMBER 2013 , Volume 16 , Number 12; Page(s) 1238 To 1244.
 
Paper: 

SYNTHESIS, ANTI-INFLAMMATORY AND ANTI- NOCICEPTIVE ACTIVITIES AND CYTOTOXIC EFFECT OF NOVEL THIAZOLIDIN-4-ONES DERIVATIVES AS SELECTIVE CYCLOOXYGENASE (COX-2) INHIBITORS

 
 
Author(s):  MOALLEM SEYED ADEL, IMENSHAHIDI MOHSEN, SHAHINI NARGES, JAVAN AHMAD REZA, KARIMI MOHSEN, ALIBOLANDI MONA, GHANDADI MORTEZA, ETEMAD LEILA, MOTAMEDSHARIATY VAHIDEHSADAT, HOSSEINI TOKTAM, HADIZADEH FARZIN*
 
* BIOTECHNOLOGY RESEARCH CENTER, MASHHAD UNIVERSITY OF MEDICAL SCIENCES, MASHHAD, IRAN
 
Abstract: 

Objective (s): Nowadays, COX-2 inhibitors such as valdecoxib are removed from the market because of their cardiovascular toxicity and their potential to increase the risk of strokes. In response to this, medicinal chemists have attempted to synthesize new classes of COX-2 Inhibitors.
Materials and Methods: In this study, three novel analogues of thiazolidin-4-ones derivatives 2a-c were synthesized. The ability of these compounds to inhibit ovine COX-1 and COX-2 (0.2- 0.8 ?M) was determined using a colorimetric method. The cytotoxic effect of the synthesized compounds (25-100
mM) was also investigated by measuring their cytotoxicity against Caco-2 and MCF-7 cell lines using MTT assay. Cell apoptosis was determined by flow cytometry. Writhing test (7.5-75 mg/kg) was used to examine the antinociceptive effects in mice. The effect of the analogues against acute inflammation (7.5-75 mg/kg) was also studied using xylene-induced ear edema test in mice.
Results: The synthesized compounds showed a weak capacity to inhibit the proliferation of Caco-2 and MCF-7 cell lines. The COX-2 inhibition potency and selectivity index for test compounds 2a–b were as follows; celecoxib>2b>2a. On the other hand, all three analogues exhibited strong antinociceptive activity against acetic acid-induced writhing. The anti-inflammatory and antinociceptive effects of the analogues were markedly more than positive control, celecoxib.
Conclusion: This study demonstrates that the antinociceptive and anti-inflammatory activity profiles exhibited by the novel synthesized compounds are independent from their COX-2 inhibitory potencies. The found antinociceptive and anti-inflammatory effects can be caused by interaction with other target; independent from COX-2. Accordingly, the compounds 2a-c could serve as lead compounds to develop novel anti-inflammation and antinociceptive drugs.

 
Keyword(s): ANTINOCICEPTIVE, ANTI-INFLAMMATORY, ANTICANCER, CELECOXIB, COX-2 INHIBITOR, THIAZOLIDIN-4-ONES
 
 
References: 
  • ندارد
  •  
 
Click to Cite.
APA: Copy

MOALLEM, S., & IMENSHAHIDI, M., & SHAHINI, N., & JAVAN, A., & KARIMI, M., & ALIBOLANDI, M., & GHANDADI, M., & ETEMAD, L., & MOTAMEDSHARIATY, V., & HOSSEINI, T., & HADIZADEH, F. (2013). SYNTHESIS, ANTI-INFLAMMATORY AND ANTI- NOCICEPTIVE ACTIVITIES AND CYTOTOXIC EFFECT OF NOVEL THIAZOLIDIN-4-ONES DERIVATIVES AS SELECTIVE CYCLOOXYGENASE (COX-2) INHIBITORS. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 16(12), 1238-1244. https://www.sid.ir/en/journal/ViewPaper.aspx?id=405650



Vancouver: Copy

MOALLEM SEYED ADEL, IMENSHAHIDI MOHSEN, SHAHINI NARGES, JAVAN AHMAD REZA, KARIMI MOHSEN, ALIBOLANDI MONA, GHANDADI MORTEZA, ETEMAD LEILA, MOTAMEDSHARIATY VAHIDEHSADAT, HOSSEINI TOKTAM, HADIZADEH FARZIN. SYNTHESIS, ANTI-INFLAMMATORY AND ANTI- NOCICEPTIVE ACTIVITIES AND CYTOTOXIC EFFECT OF NOVEL THIAZOLIDIN-4-ONES DERIVATIVES AS SELECTIVE CYCLOOXYGENASE (COX-2) INHIBITORS. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES. 2013 [cited 2021May06];16(12):1238-1244. Available from: https://www.sid.ir/en/journal/ViewPaper.aspx?id=405650



IEEE: Copy

MOALLEM, S., IMENSHAHIDI, M., SHAHINI, N., JAVAN, A., KARIMI, M., ALIBOLANDI, M., GHANDADI, M., ETEMAD, L., MOTAMEDSHARIATY, V., HOSSEINI, T., HADIZADEH, F., 2013. SYNTHESIS, ANTI-INFLAMMATORY AND ANTI- NOCICEPTIVE ACTIVITIES AND CYTOTOXIC EFFECT OF NOVEL THIAZOLIDIN-4-ONES DERIVATIVES AS SELECTIVE CYCLOOXYGENASE (COX-2) INHIBITORS. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, [online] 16(12), pp.1238-1244. Available: https://www.sid.ir/en/journal/ViewPaper.aspx?id=405650.



 
  pdf-File
Yearly Visit 91
 
Latest on Blog
Enter SID Blog