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Synthesis and evaluation of 2-cyano-3, 12-dioxooleana-1, 9(11)-en-28-oate-13β, 28-olide as a potent anti-inflammatory agent for intervention of LPS-induced acute lung injury / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.) ; (6): 347-354, 2017.
Article in English | WPRIM | ID: wpr-812106
ABSTRACT
The present study was designed to synthesize 2-Cyano-3, 12-dioxooleana-1, 9(11)-en-28-oate-13β, 28-olide (1), a lactone derivative of oleanolic acid (OA) and evaluate its anti-inflammatory activity. Compound 1 significantly diminished nitric oxide (NO) production and down-regulated the mRNA expression of iNOS, COX-2, IL-6, IL-1β, and TNF-α in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Further in vivo studies in murine model of LPS-induced acute lung injury (ALI) showed that 1 possessed more potent protective effects than the well-known anti-inflammatory drug dexamethasone by inhibiting myeloperoxidase (MPO) activity, reducing total cells and neutrophils, and suppressing inflammatory cytokines expression, and thus ameliorating the histopathological conditions of the injured lung tissue. In conclusion, compound 1 could be developed as a promising anti-inflammatory agent for intervention of LPS-induced ALI.
Subject(s)

Full text: Available Index: WPRIM (Western Pacific) Main subject: Oleanolic Acid / Bronchoalveolar Lavage Fluid / Lipopolysaccharides / Interleukin-6 / Tumor Necrosis Factor-alpha / Peroxidase / Drug Therapy / Allergy and Immunology / Cyclooxygenase 2 / Interleukin-1beta Type of study: Prognostic study Limits: Animals / Female / Humans / Male Language: English Journal: Chinese Journal of Natural Medicines (English Ed.) Year: 2017 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Oleanolic Acid / Bronchoalveolar Lavage Fluid / Lipopolysaccharides / Interleukin-6 / Tumor Necrosis Factor-alpha / Peroxidase / Drug Therapy / Allergy and Immunology / Cyclooxygenase 2 / Interleukin-1beta Type of study: Prognostic study Limits: Animals / Female / Humans / Male Language: English Journal: Chinese Journal of Natural Medicines (English Ed.) Year: 2017 Type: Article