handelin

Handelin is a guaianolide dimer from Chrysanthemum boreale that has potent anti-inflammatory activity by down-regulating NF-κB signaling and pro-inflammatory cytokine production[1].

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Handelin (Compound 1; 10-40 μM; RAW 264.7 cells) treatment suppresses the LPS-induced (1 μg/mL) overexpression of iNOS and COX-2 protein levels in a concentration-dependent manner. Handelin also suppresseS the induction of pro-inflammatory cytokines TNF-α and IL-1β in LPS-stimulated RAW 264.7 cells. Handelin also suppresses the activation of mitogen-activated protein kinases, including ERK and JNK signaling[1]. Handelin (Compound 1; 10-40 μM; RAW 264.7 cells) treatment significantly reduces the iNOS and COX-2 mRNA levels in LPS- stimulated RAW 264.7 cells. The transcriptional activity of NF-κB stimulated with LPS is also suppressed by Handelin. In addition, the LPS-stimulated upregulation of miRNA-155 expression is suppressed by Handelin[1]. RT-PCR[1] Cell Line: RAW 264.7 cells Concentration: 10 μM, 20 μM, 40 μM Incubation Time: 5 hours Result: iNOS and COX-2 mRNA levels were significantly reduced. The transcriptional activity of NF-κB stimulated with LPS was also suppressed and the LPS-stimulated upregulation of miRNA-155 expression was also suppressed. Western Blot Analysis[1] Cell Line: RAW 264.7 cells Concentration: 10 μM, 20 μM, 40 μM Incubation Time: Result: Suppressed the LPS-induced overexpression of iNOS and COX-2 protein levels in a concentration-dependent manner. Suppressed the induction of pro-inflammatory cytokines TNF-α and IL-1β, and also also suppressed the activation of mitogen-activated protein kinases, including ERK and JNK signaling in LPS-stimulated RAW 264.7 cells.

Handelin (Compound 1; 10-20 mg/kg; oral administration; for 30 mintues; male Sprague-Dawley rats) treatment inhibits acute inflammation in carrageenan-induced paw edema model. The serum level of IL-1β is also inhibited by Handelin in a carrageenan-induced paw edema model [1]. Animal Model: Male Sprague-Dawley (SD) rats (150-170 g, 5 weeks old) injected with carrageenan[1] Dosage: 10 mg/kg, 20 mg/kg Administration: Oral administration; for 30 mintues Result: Inhibited acute inflammation in carrageenan-induced paw. The serum level of IL-1β was also inhibited.

[1]. Y Pyee, et al. Suppression of inflammatory responses by handelin, a guaianolide dimer from Chrysanthemum boreale, via downregulation of NF-κB signaling and pro-inflammatory cytokine production. J Nat Prod. 2014 Apr 25;77(4):917-24.