PMID- 25655391 OWN - NLM STAT- MEDLINE DCOM- 20160418 LR - 20181113 IS - 1573-2576 (Electronic) IS - 0360-3997 (Linking) VI - 38 IP - 4 DP - 2015 Aug TI - Anti-inflammatory Effects of Aspalathin and Nothofagin from Rooibos (Aspalathus linearis) In Vitro and In Vivo. PG - 1502-16 LID - 10.1007/s10753-015-0125-1 [doi] AB - Aspalathin (Asp) and nothofagin (Not) are two major active dihydrochalcones found in green rooibos, which have been reported for their anti-oxidant activity. Here, we investigated the anti-inflammatory effects and underlying mechanisms of Asp and Not against lipopolysaccharide (LPS)-mediated vascular inflammatory responses. The anti-inflammatory activities of Asp and Not were determined by measuring permeability, monocytes adhesion and migration, and activation of pro-inflammatory proteins in LPS-activated human umbilical vein endothelial cells (HUVECs) and mice. We found that each compound inhibited LPS-induced barrier disruption, expression of cell adhesion molecules (CAMs), and adhesion/transendothelial migration of neutrophils to human endothelial cells. Asp and Not also suppressed LPS-induced hyperpermeability and leukocyte migration in vivo. Furthermore, each compound suppressed the production of tumor necrosis factor-alpha (TNF-alpha) or interleukin (IL)-6 and the activation of nuclear factor-kappaB (NF-kappaB) or extracellular regulated kinases (ERK) 1/2 by LPS. Moreover, treatment with each compound resulted in reduced LPS-induced lethal endotoxemia. These results suggest that Asp and Not posses anti-inflammatory functions by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases. FAU - Lee, Wonhwa AU - Lee W AD - College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, Kyungpook National University, 80 Dahak-ro, Buk-gu, Daegu, 702-701, Republic of Korea. FAU - Bae, Jong-Sup AU - Bae JS LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - United States TA - Inflammation JT - Inflammation JID - 7600105 RN - 0 (Anti-Inflammatory Agents) RN - 0 (Chalcones) RN - 0 (Inflammation Mediators) RN - 0 (aspalathin) RN - 0 (nothofagin) SB - IM MH - Animals MH - Anti-Inflammatory Agents/*pharmacology MH - Cell Movement/drug effects/physiology MH - Chalcones/*pharmacology MH - Dose-Response Relationship, Drug MH - Human Umbilical Vein Endothelial Cells/drug effects/metabolism MH - Humans MH - Inflammation Mediators/*antagonists & inhibitors/*metabolism MH - Male MH - Mice MH - Mice, Inbred C57BL MH - Neutrophils/drug effects/metabolism EDAT- 2015/02/07 06:00 MHDA- 2016/04/19 06:00 CRDT- 2015/02/07 06:00 PHST- 2015/02/07 06:00 [entrez] PHST- 2015/02/07 06:00 [pubmed] PHST- 2016/04/19 06:00 [medline] AID - 10.1007/s10753-015-0125-1 [doi] PST - ppublish SO - Inflammation. 2015 Aug;38(4):1502-16. doi: 10.1007/s10753-015-0125-1.