STAT3 Inhibitory Activities of Lignans Isolated from the Stems of <i>Lindera obtusiloba</i> Blume

• Main Authors: Eun-Jae Park (Author), Hee Ju Lim (Author), Hyung Jin Lim (Author), Bong-Sik Yun (Author), Soyoung Lee (Author), Seung-Jae Lee (Author), Seung Woong Lee (Author)
• Format: Book
• Published: MDPI AG, 2023-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/scipharm91040056; 2218-0532; 0036-8709
• Keywords: <i>Lindera obtusiloba</i> Blume; Lignan; IL-6; JAK2; STAT3; Pharmacy and materia medica; RS1-441
• Source: Scientia Pharmaceutica, Vol 91, Iss 4, p 56 (2023)

<i>Lindera obtusiloba</i> Blume has several activities, such as anti-inflammatory, anti-allergic, anti-tumor, anti-wrinkle, and antioxidant activities. Interleukin-6 (IL-6) is a classic pro-inflammatory cytokine that is associated with various functions, such as proliferation, invasion, inflammatory responses and functions within antioxidant defense systems. In this study, we investigated IL-6-induced STAT3 activation of lignan compounds isolated from <i>L. obtusiloba</i>. The structures of the isolated compounds were elucidated via spectroscopic nuclear magnetic resonance (NMR) and electrospray ionization mass spectrometry (ESI-MS). As a result, seven lignans were identified from <i>L. obtusiloba</i>. All the isolated compounds (<b>1</b>-<b>7</b>) were evaluated for their IL-6-induced STAT3 inhibitory effects in Hep3B cells using a luciferase reporter assay. Of the isolates, compounds <b>1</b> and <b>5</b> showed inhibitory effects against IL-6-stimulated STAT3 activation. Furthermore, the mRNA expression levels of inflammation-related genes such as CRP, IL-1b, and SOCS3 were significantly reduced by exposure to compounds <b>1</b> and <b>5</b>. The protein levels of p-STAT3 and p-JAK2 in IL-6-induced U266 cells were regulated in the presence of lignans derived from <i>Lindera obtusiloba</i> by Western blot assay. Based on the results, this study of <i>L. obtusiloba</i> demonstrates that the species has promise as a bioactive candidate for the treatment of IL-6-induced STAT3-related disease.