Inducible nitric oxide synthase (iNOS) is a crucial enzyme involved in monocyte cell response towards inflammation, and it is responsible for the production of sustained amounts of nitric oxide. This free radical molecule is involved in the defense against pathogens; nevertheless, its continuous and dysregulated production contributes to the development of several pathological conditions, including inflammatory and autoimmune diseases. In the present study, we investigated the effects of two new iNOS inhibitors, i.e., 4-(ethanimidoylamino)-N-(4-fluorophenyl)benzamide hydrobromide (FAB1020) and N-{3-[(ethanimidoylamino)methyl]benzyl}-l-prolinamidedihydrochloride (CM554), on human LPS-stimulated monocytes, using the 1400 W compound as a comparison. Our results show that CM544 and FAB1020 are selective and decrease cytotoxicity, IL-6 secretion and LPS-stimulated monocyte migration. Furthermore, the modulation of iNOS, nitrotyrosine and Nrf2 were analyzed at the protein level. Based on the collected preliminary results, the promising therapeutic value of the investigated compounds emerges, as they appear able to modulate the pro-inflammatory LPS-stimulated response in the low micromolar range in human monocytes.
机构:
Taif Univ, Coll Appl Med Sci, Dept Clin Lab Sci, POB 11099, At Taif 21944, Saudi ArabiaTaif Univ, Coll Appl Med Sci, Dept Clin Lab Sci, POB 11099, At Taif 21944, Saudi Arabia
机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Gao, Wan-Jiao
;
Liu, Jian-Xin
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机构:
Hunan Univ Med, Sch Pharmaceut Sci, Huaihua City, Hunan, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Liu, Jian-Xin
;
Xie, Yie
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Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Xie, Yie
;
Luo, Pei
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Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Luo, Pei
;
Liu, Zhong-Qiu
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机构:
Guangzhou Univ Chinese Med, Joint Lab Translat Canc Res Chinese Med, Minist Educ Peoples Republ China, Guangzhou, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Liu, Zhong-Qiu
;
Liu, Liang
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机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R China
Guangzhou Univ Chinese Med, Joint Lab Translat Canc Res Chinese Med, Minist Educ Peoples Republ China, Guangzhou, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Liu, Liang
;
Zhou, Hua
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机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R China
Guangzhou Univ Chinese Med, Joint Lab Translat Canc Res Chinese Med, Minist Educ Peoples Republ China, Guangzhou, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
机构:
Taif Univ, Coll Appl Med Sci, Dept Clin Lab Sci, POB 11099, At Taif 21944, Saudi ArabiaTaif Univ, Coll Appl Med Sci, Dept Clin Lab Sci, POB 11099, At Taif 21944, Saudi Arabia
机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Gao, Wan-Jiao
;
Liu, Jian-Xin
论文数: 0引用数: 0
h-index: 0
机构:
Hunan Univ Med, Sch Pharmaceut Sci, Huaihua City, Hunan, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Liu, Jian-Xin
;
Xie, Yie
论文数: 0引用数: 0
h-index: 0
机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Xie, Yie
;
Luo, Pei
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h-index: 0
机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Luo, Pei
;
Liu, Zhong-Qiu
论文数: 0引用数: 0
h-index: 0
机构:
Guangzhou Univ Chinese Med, Joint Lab Translat Canc Res Chinese Med, Minist Educ Peoples Republ China, Guangzhou, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Liu, Zhong-Qiu
;
Liu, Liang
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h-index: 0
机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R China
Guangzhou Univ Chinese Med, Joint Lab Translat Canc Res Chinese Med, Minist Educ Peoples Republ China, Guangzhou, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Liu, Liang
;
Zhou, Hua
论文数: 0引用数: 0
h-index: 0
机构:
Macau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China
Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macao, Peoples R China
Guangzhou Univ Chinese Med, Joint Lab Translat Canc Res Chinese Med, Minist Educ Peoples Republ China, Guangzhou, Peoples R ChinaMacau Univ Sci & Technol, Fac Chinese Med, Taipa, Macao, Peoples R China