PGE2 production

The different furanones 104 were tested for their potency as inhibitors of PGE2 production both in transfected Chinese hamster ovarian (CHO) cells expressing human COX-2 and in human whole blood. Compound 104r proved to be an orally active and selective COX-2 inhibitor that is devoid of the ulcerogenic effect at >100 times the dose for antiinflammatory, analgesic, and antipyretic effects (99BMC3187). 

The plant is strongly aromatic on account of an essential oil which comprises cis-a-ocimene (25.11%), 3,7-dimethyl-l,6-octadien-3 ol (16.85%), and trans-nerolidol (13.89%), hence the use of the plant in aromatherapy. A methanolic extract of bark of Litsea cubeba (Lour.) Pers. and its fractions (0.01 mg/mL) from bark inhibit NO and PGE2 production in LPS-activated RAW 264.7 macrophages without significant cytotoxicity at less than 0.01 mg/mL concentration. The methanol extract decreased the enzymatic activity of myeloperoxidase (0.05 mg/mL). These findings suggest that L. cubeba is beneficial for inflammatory conditions and may contain compound(s) with anti-inflammatory properties (63). Can we expect the vasorelaxant laurotetanine (64) isolated from the plant to exert such activity ... 

JP-8-induced systemic immunosuppression is explained in part by modulation of cytokine and inflammatory pathways. Within 48 hours of a single dermal application of JP-8 (300 pL), serum IL-10 levels increase significantly to nearly 3000 pg/mL [36], As IL-10 is known to suppress DTH responses [64,65], it is likely that modulation of this cytokine contributes to JP-8 s immunotoxicity. Furthermore, splenic T-cell proliferative responses are significantly decreased in JP-8 exposed mice, yet this effect is reversed following neutralization of IL-10, administration of IL-12, or inhibition of prostaglandin E2 (PGE2) production [60], Additional studies demonstrated suppression... 

Jaksic, A. et al., Cis-urocanic acid synergizes with histamine for increased PGE2 production by human keratinocytes Link to indomethacin-inhibitable UVB-induced immunosuppression, Photochem. Photobiol. 61, 303-309, 1995. 

Ballou, L.R., Chao, C.P., Holness, M.A., Barker, S.C., and Raghow, R., 1992, Interleukin-1-mediated PGE2 production and sphingomyelin metabolism. Evidence for the regulation of cyclooxygenase gene expression by sphingosine and ceramide. J.Biol.Chem. 267 20044-20050. 

Several fatty acids and derivatives were isolated from the dichloromethane extract of Angelica pubescens Maxim f. biserrata Shan et Yuan (Umbelliferae) by following in vitro 5-LOX and COX-1 inhibitory assays. Linoleic acid showed potent inhibition against PGE2 production from purified COX-1 enzyme. Falcarindiol, which is an acetylenic alcohol, showed higher potency against LOX than COX (Table 3) [122]. Linolenic acid is an... 

Jolad, S.D., Lantz, R.C., Solyom, A.M., Chen, G.J., Bates, R.B. and Timmermann, B.N. (2004) Fresh organically grown ginger (Zingiber officinale) composition and effects on LPS-induced PGE2 production. Phytochemistry 65(1 3), 1 937-1954. 

Excisanin A (kaurane diterpene) Isodonjaponicus (Lamiaceae) l iNOS expression [blocks LPS-induced macrophage NFkB activation, iNOS COX-2 expression NO PGE2 production]... 

The kinin-kallikrein system (kinin system) is a poorly delineated system of blood proteins that plays a role in inflammation, blood-pressure control, coagulation and pain. Kinins are small peptides produced from kininogen by kallikrein, which are subsequently degraded by kininases. They act on phospholipase and increase arachidonic acid release and thus prostaglandin (PGE2) production. 

Nonsteroidal anti-inflammatory drugs (NSAlDs) nonselectively inhibit the activities of both COX-1 and COX-2. Out of concern for the gastrointestinal side effects of NSAID, scientists have discovered and developed many specific COX-2 inhibitors that facilitate a safer choice for controlling inflammatory diseases (73). Eor example, NS-398, a selective COX-2 inhibitor, has been shown to reduce tension (mechanical stress)-induced PGE2 production from periodontal ligament cell cultures (74). 

Attur MG, Patel R,ThakkerG,Vyas P, Levartovsky D, Patel P, Naqvi S, Raza R, Patel K, Abramson D, Bruno G, Abramson SB, Amin AR. Differential antl-Inflammatory effects of immunosuppressive drugs cyclosporin, rapamycin and FK-506on inducible nitric oxide synthase, nitric oxide, cyclooxygenase-2 and PGE2 production. Inflamm Res 2000 49 20-26. 

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