Rho-Iso-Alpha Acids and Tetrahydro-Iso-Alpha Acids Are Selective Protein Kinase Inhibitors Which Potently Reduce Inflammation in Macrophages in Vitro and in the Collagen-Induced Rheumatoid Arthritis Model in Vivo

Pharmacokinetics of reduced iso-α-acids in volunteers following clear bottled beer consumption

“…These preliminary IAA pharmacokinetic studies demonstrated that IAA compounds can be detected and suggests that the structurally similar reduced IAA may also be able to be targeted. Furthermore, there have been toxicity [19] and pharmacokinetic studies investigating reduced IAA, particularly RIAA and TIAA, due to their possible medicinal properties such as weight loss, antidiabetic, anti-carcinogenic and anti-inflammatory [7,8,[20][21][22][23]. Of these, two studies detected RIAA and TIAA in New Zealand white rabbits [7], and one measured RIAA in humans [8], confirming those reduced IAA groups examined were indeed bioavailable.…”

The Promising Ability of Humulus lupulus L. Iso-α-acids vs. Diabetes, Inflammation, and Metabolic Syndrome: A Systematic Review

“…In fact, in vitro investigations proved that both RIAA and THIAA (1-20 μg/mL) dose-dependently reduced NF-kB nuclear translocation and abundancy in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages [50]. This activity was shown to be similar to that of parthenolide, a natural NF-κB inhibitor that works through the inhibition of NF-κB activation and releases from the cytoplasmatic IkB complex [50,51]. Furthermore, RIAA and THIAA inhibited several protein kinases involved in LPS-triggered activation of toll-like receptors (TLRs).…”

Isohumulones from hops (Humulus lupulus) and their potential role in medical nutrition therapy

“…In 2005 Tripp reported the unique antiinflammatory potential and putative mechanism of action of the isohumulones [23,24]. Babish et al screened 208 chemically characterized phytochemical extracts for antiinflammatory and antidiabetic activity and found that the iso-alpha acids derived from hops and proanthocyanidins from Acacia nilotica were among the most active natural compounds influencing both inflammation and insulin signaling pathways [25].…”