Characterization of Sparstolonin B, a Chinese Herb-derived Compound, as a Selective Toll-like Receptor Antagonist with Potent Anti-inflammatory Properties

A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.

Histamine mediates its physiological function through binding to four known histamine receptors. Here, we describe the first selective antagonist of the histamine H4 receptor, the newest member of the histamine receptor family, and provide evidence that such antagonists have anti-inflammatory activity in vivo. 1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120) has a K(i) of 4...

P 147: Role of Sparstolonin B in Intracerebral Hemorrhage-Induced Inflammatory Brain Injury: Blocking the Formation of TLR2/TLR4 Heterodimer

Intra-cerebral hemorrhage (ICH) is a particularly severe type of stroke accounting for 10–15 % of all strokes and is associated with a mortality rate of 30–50%. Neuroinflammation contributes to ICH-induced secondary brain injury and understanding the mechanisms causing neuroinflammation can be helpful to find new treatments of ICH. Recent studies demonstrated that toll like receptor...

The Anti-angiogenic Effects of Sparstolonin B

Sparstolonin B (SsnB) is a novel bioreactive compound isolated from Sparganium stoloniferum, an herb historically used in Traditional Chinese Medicine as an anti-tumor agent. SsnB has demonstrated anti-inflammatory properties, inhibiting Toll-like receptor mediated inflammation in isolated macrophages and in mice. Angiogenesis, the process of new capillary formation from existing blood vessels,...

Antiviral Response Than Toll-Like Receptor Toll-Like Receptor 3 Mediates a More Potent

CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.

The prostaglandin (PG) EP(4) receptor subtype is expressed by peripheral sensory neurons. Although a potential role of EP(4) receptor in pain has been suggested, a limited number of selective ligands have made it difficult to explore the physiological functions of EP(4) or its potential as a new analgesic target. Here, we describe the in vitro and in vivo pharmacology of a novel EP(4) receptor ...