Lee, Sung Jin Lee, Sang Hyuk Lee, Heesu Shin, Myoung-Sook Jae Wook Lee 2024-01-12T02:32:32Z 2024-01-12T02:32:32Z 2023-01-20 2023-02 1661-6596 https://pubs.kist.re.kr/handle/201004/75816 This study aimed to synthesize and evaluate the anti-inflammatory activity of 3-substituted-indolin-2-one derivatives. Cell viability of 3-substituted-indolin-2-one derivatives was measured with the EZ-Cytox reagent; interleukin (IL)-6, tumor necrosis factor (TNF)-α, and inducible NOS mRNA levels were measured using Taqman qRT-PCR; pro-inflammatory cytokine IL-6 and TNF-α levels were determined using ELISA kits; the phosphorylation of Akt, JNK, ERK, p38, p65, and IκB protein levels were measured by immunoblotting. Among the nineteen 3-substituted-indolin-2-one derivatives synthesized, 3-(3-hydroxyphenyl)-indolin-2-one showed the highest anti-inflammatory activity, inhibiting the nitric oxide production related to inflammation, suppressing the production of TNF-α and IL-6 in a concentration-dependent manner and mRNA expression. Moreover, 3-(3-hydroxyphenyl)-indolin-2-one significantly inhibited lipopolysaccharide (LPS)-induced signal pathways such as the Akt, MAPK, and NF-κB signaling pathways. Our findings revealed that a 3-substituted-indolin-2-one derivative, 3-(3-hydroxyphenyl)-indolin-2-one, possesses excellent anti-inflammatory activity and can be considered for future research. English Multidisciplinary Digital Publishing Institute (MDPI) Design, Synthesis, and Biological Evaluation of 3-Substituted-Indolin-2-One Derivatives as Potent Anti-Inflammatory Agents Article 10.3390/ijms24032066 1 International Journal of Molecular Sciences, v.24, no.3, pp.1 - 15 International Journal of Molecular Sciences 24 3 1 15 Y scie scopus 000929791800001 2-s2.0-85147894896 Biochemistry & Molecular Biology Chemistry, Multidisciplinary Biochemistry & Molecular Biology Chemistry NF-KAPPA-B MAP KINASE SCAFFOLD AURONE INHIBITORS DISEASE INFLAMMATION EXPRESSION SULFURETIN SYNTHASE 3-substituted-indolin-2-one derivatives inflammation macrophages cytokines