Anti-Inflammatory Activity and Mechanism of Isookanin, Isolated by Bioassay-Guided Fractionation from Bidens pilosa L.

Abstract

Bidens pilosa L. (Asteraceae) has been used historically in traditional Asian medicine and is known to have a variety of biological effects. However, the specific active compounds responsible for the individual pharmacological effects of Bidens pilosa L. (B. pilosa) extract have not yet been made clear. This study aimed to investigate the anti-inflammatory phytochemicals obtained from B. pilosa. We isolated a flavonoids-type phytochemical, isookanin, from B. pilosa through bioassay-guided fractionation based on its capacity to inhibit inflammation. Some of isookanin’s biological properties have been reported; however, the anti-inflammatory mechanism of isookanin has not yet been studied. In the present study, we evaluated the anti-inflammatory activities of isookanin using lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. We have shown that isookanin reduces the production of proinflammatory mediators (nitric oxide, prostaglandin E2) by inhibiting the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated macrophages. Isookanin also inhibited the expression of activator protein 1 (AP-1) and downregulated the LPS-induced phosphorylation of p38 mitogen-activated protein kinase (MAPK) and c-jun NH2-terminal kinase (JNK) in the MAPK signaling pathway. Additionally, isookanin inhibited proinflammatory cytokines (tumor necrosis factor-a (TNF-α), interleukin-6 (IL-6), interleukin-8 (IL-8), and interleukin-1β (IL-1β)) in LPS-induced THP-1 cells. These results demonstrate that isookanin could be a potential therapeutic candidate for inflammatory disease.

Anti-inflammatory and neuroprotective activity of Viphyllin a standardized extract of β-caryophyllene from black pepper (Piper Nigrum L) and its associated mechanisms in mouse macrophage cells and Human Neuroblastoma SH-SY5Y cells

“…All these elements stimulate the development of inflammation and worsen the inflammation over the harmonious interaction with further inflammatory intermediaries and there are reports that in variety of inflammatory ailments including asthma and colitis the expression levels of PGE2 and NO is elevated [15–17]. Our study revealed that Viphyllin efficiently inhibited the secretion of PGE2 and NO, and proinflammatory cytokines in LPS-challenged macrophages at safer dose, our findings are consistent with earlier published studies [18, 19]. COX-2.…”

Meroterpenoids Possessing Diverse Rearranged Skeletons with Anti‐inflammatory Activity from the Mangrove‐Derived Fungus Penicillium sp. HLLG‐122

“…The tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) can significantly promote the progression of inflammation. [26] Thus, the levels of TNF-α and IL-6 in the LPS-stimulated RAW 264.7 cell were determined by ELISA. As showed in Figure 7, when the RAW 264.7 cells were pretreated with compound 11, the levels of TNF-α, and IL-6 induced by LPS were dose-dependently downregulated.…”

Isookanin Inhibits PGE2-Mediated Angiogenesis by Inducing Cell Arrest through Inhibiting the Phosphorylation of ERK1/2 and CREB in HMEC-1 Cells

“…Many natural compounds—for example, resveratrol, curcumin, or quercetin—can target a wide variety of molecules, implying that natural products might be effective inhibitors [ 42 ]. Isookanin is a phenolic flavonoid component contained in some plants, such as Asteraceae [ 26 ] and Leguminosae [ 28 ], and its anti-inflammatory efficacy and mechanism of action have already been revealed in our previous research [ 29 ].…”

“…Isookanin (C 15 H 12 O 6 , molecular weight: 288.3) is a phenolic flavonoid presented in Bidens extract [ 26 ]. It has been reported that isookanin possesses some biological properties, including antioxidative [ 27 , 28 ] and anti-diabetic properties [ 27 ], anti-inflammatory effects [ 29 ] and an ability to inhibit α-amylase [ 26 ]. However, the antiangiogenic effects and mechanism thereof have not been studied yet.…”