Morelloflavone, a novel biflavonoid inhibitor of human secretory phospholipase A2 with anti-inflammatory activity

Non-toxic melanin production inhibitors from Garcinia livingstonei (Clusiaceae)

“…The activity of morelloflavone (1) as an antiinflammatory (Gil et al, 1997;Castardo et al, 2008) and antioxidant (Sanz et al, 1994;Deachathai et al, 2005;Hutadilok-Towatana et al, 2007) are well-documented; it has also been found to be a potent tyrosinase inhibitor (Masuda et al, 2005), anti-HIV-1 (Lin et al, 1997), and anti-bacterial (Verdi et al, 2004) agent, and to have antimalarial (Ngouamegne et al, 2008) and analgesic (Luzzi et al, 1997) properties. Isojacareubin (5) is known for its activity as an anticoagulant (Wu et al, 1998), and 6-deoxyisojacareubin (6) for its antifungal (Morel et al, 2002) and antibacterial (Kuete et al, 2007) properties, while sargaol (4) shows marked activity as an antioxidant (Nahas et al, 2007).…”

Ochnaflavone, Naturally Occurring Biflavonoid, Inhibits Phospholipase A2 Dependent Phosphatidylethanolamine Degradation in a CCl4-Induced Rat Liver Microsome

“…1), which was isolated from L. japonica, was found to be inhibitor of sPLA 2 -IIA from rat platelets, and similar results were also obtained with morelloflavone. 2,3) Recently, it was reported that this compound inhibits LPS-induced iNOS expression, which is mediated by ERK1/2 via NF-kB regulation, in RAW264.7 cells. 4) In addition, biflavonoids such as ginkgetin and ochnaflavone (OC) were reported to be dual inhibitor of cyclooxygenase-2 and 5-lipoxygenase from the mast cells as well as inhibit the release of the archidonic acid metabolites from the rat peritoneal macrophages stimulated by either phorbol ester or calcium ionophore, A 23187 .…”

Characterization of Secretory Type IIA Phospholipase A2 (sPLA2-IIA) as a Glycyrrhizin (GL)-Binding Protein and the GL-Induced Inhibition of the CK-II-Mediated Stimulation of sPLA2-IIA Activity in Vitro.

“…4) Recently, we reported that (i) three phospholipases A 2 (PLA 2 s) [PA2Y (Tf PL-X, 121 amino acid residues), PA21 (Tf PLA, 122 amino acid residues) and PA2B (lysine-49-PLA 2 , 122 amino acid residues)] are selectively purified from Habu snake venom as GL-binding proteins (gbPs); and (ii) PA2B is a GL-sensitive enzyme in vitro. 5) Therefore, it is of interest to examine the inhibitory effects of GL, glycyrrhetinic acid (GA) and a GA derivative (oGA) on the activity of secretory type IIA PLA 2 (sPLA 2 -IIA) purified from the synovial fluids of patients with rheumatoid arthritis, 6,7) because (i) sPLA 2 -IIA is a critical modulator of cytokine-mediated synovial inflammation in rheumatoid arthritis 8,9) ; and (ii) the amino acid sequence of sPLA 2 -IIA has a high homology with that of a GL-sensitive PA2B (Habu snake venom). 5) An attempt was made to selectively purify sPLA 2 -IIA from the rheumatoid synovial fluids as a gbP by means of GL-affinity column chromatography (HPLC), similar to the purification of gbPLA 2 s from Habu snake venom.…”