Psoriasis is a chronic inflammatory skin disease. Its treatment is based on the inhibition of proliferation of epidermal cells and interference in the inflammatory process. A new systemic antipsoriasis drug, which consists of dimethylfumarate and ethylhydrogenfumarate in the form of their calcium, magnesium and zinc salts has been introduced in Europe with successful results. In the present study, a homologous series of mono- and diesters of fumaric acid has been studied with respect to the sites and kinetics of presystemic ester degradation using pancreas extract, intestinal perfusate, intestinal homogenate and liver S9 fraction. In addition, intestinal permeability has been determined using isolated intestinal mucosa as well as Caco-2 cell monolayers, in order to obtain estimates of the fraction of the dose absorbed for these compounds. Relationships between the physicochemical properties of the fumaric acid esters and their biological responses were investigated. The uncharged diester dimethylfumarate displayed a high presystemic metabolic lability in all metabolism models. It also showed the highest permeability in the Caco-2 cell model. However, in permeation experiments with intestinal mucosa in Ussing-type chambers, no undegraded DMF was found on the receiver side, indicating complete metabolism in the intestinal tissue. The intestinal permeability of the monoesters methyl hydrogen fumarate, ethyl hydrogen fumarate, n-propylhydrogen fumarate and n-pentyl hydrogen fumarate increased with an increase in their lipophilicity, however, their presystemic metabolism rates likewise increased with increasing ester chain length. It is concluded that for fumarates, an increase in intestinal permeability of the more lipophilic derivatives is counterbalanced by an increase in first-pass extraction.

Abstract:The chemical composition of the essential oil of the leaves of Eucalyptus globulus (Myrtaceae) grown in North West Karnataka, has been analyzed by GC and GC/MS. Forty-eight constituents were identified, accounting 97.93% of the total oil. The major compounds were á-phellandrene (40.31%), á-pinene (13.71%), â-pinene (13.31%), ã-terpinene (9.61%) and 1,8-cineol (4.96%). The oil was rich in monoterpene hydrocarbons (81.14%).

The essential oil was isolated from the aerial parts of Phlomis bracteosa Royle ex Benth., a hairy erect herb. The leaves and flowers of this species are used as carminative, stimulant and locally known as ‘Ballikotu, Calba, Salba’ in Turkish traditional medicine. The antimicrobial activity of Phlomis bracteosa was studied using well diffusion method. The activity was tested against human pathogenic bacteria and fungi at different concentrations (0.25 μg/ml, 0.125 μg/ml and 0.062 μg/ml) of the essential oil. Keywords: Phlomis bracteosa; Lamiaceae; Antimicrobial activity DOI: http://dx.doi.org/10.3126/sw.v9i9.5521 SW 2011; 9(9): 63-65

No abstract