Inhibitory Effects of Cucurbitane-Type Triterpenoids from <i>Momordica charantia</i> Fruit on Lipopolysaccharide-Stimulated Pro-Inflammatory Cytokine Production in Bone Marrow-Derived Dendritic Cells

• Main Authors: Thao Quyen Cao, Nguyen Viet Phong, Jang Hoon Kim, Dan Gao, Hoang Le Tuan Anh, Viet-Duc Ngo, Le Ba Vinh, Young Sang Koh, Seo Young Yang
• Format: Article
• Language: English
• Published: MDPI AG 2021-07-01
• Series: Molecules
• Subjects: <i>Momordica charantia</i>; bioactive compound; anti-inflammatory effect; triterpenoid
• Online Access: https://www.mdpi.com/1420-3049/26/15/4444

The bitter melon, <i>Momordica charantia</i> L., was once an important food and medicinal herb. Various studies have focused on the potential treatment of stomach disease with <i>M</i>. <i>charantia</i> and on its anti-diabetic properties. However, very little is known about the specific compounds responsible for its anti-inflammatory activities. In addition, the in vitro inhibitory effect of <i>M</i>. <i>charantia</i> on pro-inflammatory cytokine production by lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells (BMDCs) has not been reported. Phytochemical investigation of <i>M</i>. <i>charantia</i> fruit led to the isolation of 15 compounds (<b>1</b>−<b>15</b>). Their chemical structures were elucidated spectroscopically (one- and two-dimensional nuclear magnetic resonance) and with electrospray ionization mass spectrometry. The anti-inflammatory effects of the isolated compounds were evaluated by measuring the production of the pro-inflammatory cytokines interleukin IL-6, IL-12 p40, and tumor necrosis factor α (TNF-α) in LPS-stimulated BMDCs. The cucurbitanes were potent inhibitors of the cytokines TNF-α, IL-6, and IL-12 p40, indicating promising anti-inflammatory effects. Based on these studies and in silico simulations, we determined that the ligand likely docked in the receptors. These results suggest that cucurbitanes from <i>M</i>. <i>charantia</i> are potential candidates for treating inflammatory diseases.