RI75, a curcumin analogue, inhibits tumor necrosis factor-α and interleukin-6 production and exhibits antiallodynic and antiedematogenic activities in mice

Curcumin and its analogues exhibited anti-inflammatory activity in different experimental models. Recently, we synthesized (2 E ,3 E )-3-buten-2-one-4-(4-hydroxy-3-methoxyphenyl)-2-(4-(4-methoxyphenyl)-2-thiazolyl)hydrazone (RI75), a curcumin analogue with a thiazolyl hydrazone moiety. In the presen...

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Published in:	Inflammopharmacology Vol. 30; no. 2; pp. 505 - 515
Main Authors:	Costa, Sarah O. A. M., Rodrigues, Ianny B., Braga, Alysson V., Barbosa, Bárbara C. M., Silva, Roger R. L., Rodrigues, Felipe F., Melo, Ivo S. F., Morais, Marcela Í., Castro, Brenda F. M., Júnior, Armando S. Cunha, Maltarollo, Vinícius G., Oliveira, Renata B., Coelho, Márcio M., Machado, Renes R.
Format:	Journal Article
Language:	English
Published:	Cham Springer International Publishing 01-04-2022
Subjects:	Allergology Animals Biomedical and Life Sciences Biomedicine Curcumin - analogs & derivatives Curcumin - pharmacology Dermatology Disease Models, Animal Edema - drug therapy Edema - metabolism Gastroenterology Hyperalgesia - drug therapy Hyperalgesia - metabolism Immunology Inflammation - chemically induced Interleukin-6 - antagonists & inhibitors Interleukin-6 - biosynthesis Mice Neuralgia - drug therapy Neuralgia - metabolism Original Article Pharmacology/Toxicology Rheumatology Tumor Necrosis Factor-alpha - antagonists & inhibitors Tumor Necrosis Factor-alpha - biosynthesis RI75 Pain Cytokines Curcumin analogues Curcumin Inflammation Thiazolyl hydrazone derivative
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Summary:	Curcumin and its analogues exhibited anti-inflammatory activity in different experimental models. Recently, we synthesized (2 E ,3 E )-3-buten-2-one-4-(4-hydroxy-3-methoxyphenyl)-2-(4-(4-methoxyphenyl)-2-thiazolyl)hydrazone (RI75), a curcumin analogue with a thiazolyl hydrazone moiety. In the present study, we investigated the effects induced by RI75 in different models of inflammation and pain in mice, as well as some underlying mechanisms. Pre-treatment with RI75 (40 mg/kg, intraperitoneal; i.p.) or curcumin (40 mg/kg, i.p.) reduced the mechanical allodynia and paw edema induced by intraplantar (i.pl) injection of carrageenan. RI75 antiallodynic activity was reduced by pre-treatment with naltrexone (5 and 10 mg/kg, i.p.) and cyproheptadine (10 mg/kg, i.p.), but not glibenclamide (20 and 40 mg/kg, i.p.). In a model of neuropathic pain, a single i.p. administration of RI75 (40 mg/kg) or curcumin (40 mg/kg) attenuated the ongoing mechanical allodynia induced by repeated administrations of paclitaxel. Pre-treatment with RI75 (40 mg/kg, i.p.) or curcumin (40 mg/kg, i.p.) also reduced tumor necrosis factor-α and interleukin-6 production and myeloperoxidase activity induced by carrageenan. The results of the present study demonstrate that RI75, a synthetic curcumin analogue, exhibits antiallodynic and antiedematogenic activities. Activation of opioidergic and serotonergic mechanisms and reduced production of inflammatory mediators and neutrophil recruitment may underlie RI75 activities.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0925-4692 1568-5608
DOI:	10.1007/s10787-021-00913-9