Antipsoriatic activity

Bhatia A, Singh B, Wadhwa S, Raza K, Katare OP. Novel phospholipid-based topical formulations of tamoxifen Evaluation for antipsoriatic activity using mouse-tail model. Pharm Dev Technol. 19(2)... 

Immunomodulator. Antiviral and antiinflammatory agent. Exhibits antipsoriatic activity. Also used against other autoimmune diseases such as arthritis, eczema and systemic lupus erythematosus. Viscous oil. [a]o -12 (neat). 1.4687. Log P -1.31 (calc). Low toxicity and no serious side effects, but requires large therapeutic dosage. 

A few drugs depend for their therapeutic action upon light activation. Included in this review are dithranol, which has been suggested to exert its antipsoriatic action in this way, and the psoralens, which have long been used in combination with sunbathing to treat various skin conditions and now are also used against surface cancers. 

Anthralin (59), used clinically as an antipsoriatic, inhibited human ISN (7 /zM) the oxidation products of (59) (the corresponding quinone and dimer) were not active [164]. A non-specific antioxidant effect was suggested, since co-oxidation of LTB4 and mouse ear 12-LO were inhibited at similar concentrations [165]. However, some other phenolic polycyclic aromatic compounds appear more specific in their actions. 

Mechanism of Action A topical agent that binds DNA, inhibiting synthesis of nucleic protein, and reduces mitotic activity. Therapeutic Effect Results in damage to DNA sugar and enhances membrane lipid peroxidation, which may play a critical role in the antipsoriatic action. 

Muller, K. and K. Ziereis. 1994. The antipsoriatic Mahonia aquifolium and its active consitutents. I. Pro- and antioxidant properties and inhibition of 5-lipoxygenase. Planta Med. 60 421-424. 

Van de Kerkhof, P.C.M., Biological activity of vitamin D analogues in the skin, with special reference to antipsoriatic mechanisms, Br. J. Dermatol., 132, 675, 1995. 

Prokopenko et al described that some naphthoquinones normalized or increased the immune response in rats after intensive physical load. The naphthoquinones induced the development of immunostimulating properties in heavy red blood cells by direct action on cell membranes or indirectly through proteolytic enzymes secreted by hepatocytes [212]. Other activities described for several naphthoquinones related to lapachol are antipsoriatic [213], larvicidal and insecticidal, [214-215] molluscicidal [216], and mutagenicity in salmonella [217]. The potential use of lapachol in cosmetics has been published too [218]. 

Anthrahn possesses antiproliferative activity on human ker-atinocytes, inhibiting DNA synthesis by intercalation between DNA strands." It induces nuclear factor-KB (NF-kB) in murine ker-atinocytes. Since NF-kB is involved in the transcription of proin-flammatory cytokines such as IL-6, IL-8, and TNF-a, these findings may be helpful in explaining the irritant properties of anthralin. Other hypotheses support the role of anthralin-generated free radicals in producing both antipsoriatic effects and irritation. 

AA - 861) inhibited the biosynthesis of LTD, LTB, and 5-HETE in RBL-1 extracts at a concentration of 1 pM (70-80% inh.). Bay 0 8278 (14)inhibits the formation of LO products 5-HETE, 12-HETE, 15-HETE, LTB, and its isomer in rabbit and human PMN s. LC-6 (15) has the ability to inhibit AA 5-LO activity. A correlation was observed between known antipsoriatic drugs (resorcinol, salicyclic acid, anthralin, AA, ETYA, mycophenolic acid, trans-retinoic acid and etretinate) and their inhibitory activity with soybean LO. Calmodulin (CM) antagonists trifluoroperamine, chlorpromazlne and dlphenylbutlamlne inhibited 5-LO from RBL-1 cells with potencies (IC-q 5.6, 9.6 and 8.3 pM, respectively) similar to those reported for their CM antagonism. 13-cis retinoic acid (Ro 4-3780) is a selective inhibitor of 5-LO with an of 9 pM. ... 

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