Synthesis of DAAS derivatives and their enhancement of HL-60 leukemia cell differentiation.

DAAS is the diacetoxy acetal derivative of a-santonin and induces HL-60 cell differentiation into granulocytes. In this report, we investigated the structure-activity relationship (SAR) of DAAS derivatives in the differentiation of human HL-60 leukemia cells. Although its derivatives themselves had less effect on HL-60 cell differentiation than DAAS, the monoacetyl derivative, 2, mainly induced HL-60 cell differentiation. Moreover, compound 2 synergistically enhanced all-trans retinoic acid (ATRA)-induced HL-60 cell differentiation when combined with 50 nM ATRA, a well-known differentiation inducer. This enhancing effect is similar to that of DAAS in ATRA-induced differentiation.

Studies on the antiinflammatory, antipyretic and analgesic activities of santonin.

Santonin, a sesquiterpene lactone, commonly found in the plants of the family Compositae was found to show significant antiinflammatory activity on acute inflammatory processes. The activity profile of santonin closely resembled that of a standard non-steroidal antiinflammatory drug, diclofenac sodium. It also showed a significant inhibitory effect on granuloma formation; however, this effect of santonin was less pronounced as compared to diclofenac sodium. Santonin caused a significant antipyretic effect in mice, which was found to be independent of the route of administration of the drug. It also increased the hot plate reaction time of treated mice, similar to morphine.

Evaluación comparativa entre ácido kaínic, santonina y adipato de piperazina solos y asociados como antihelmínticos: terapétuica y tolerancia / Comparative evaluation between kainic acid, santonine and piperazine adipate alone and combined as antihelminthes: therapeutics and tolerance

Se estudió a la población escolar de una zona endémica para geohelmintiasis mediante estudios coproparasitoscópicos, utilizando el método de flotación. Se seleccionaron con 200 pacientes que presentaban parasitosis por Ascaris lumbricoides, Trichuris trichiura y uncinaria. En un estudio posterior se valoraron por el método de frotis fecal de Kato Katz, además de realizar tres estudios por el método de raspado anal con cinta de celulosa engomada. Los pacientes se dividieron en cinco grupos y se les administró en una sola dosis: grupo 1, santonina a concentración de 66.6 mg/10 ml; grupo 2, adipato de piperazina a concentración de 1333.2 mg/10 ml, grupo 3, ácido Kaínico a concentración de 6.6 mg/10 ml; grupo 4, combinación de santonina 33.3 mg/10 ml, piperazina 666.6 mg/10 ml y ácido Kaínico 3.3 mg/10 ml, y grupo 5, adipato de piperazina a concentración de 2666.4 mg/10ml. Posterior al tratamiento se practicaron nuevamente los exámenes mencionados a manera de control. Los resultados demostraron que la combinación de ácido Kaínico, piperazina y santonina es mejor en el control de la helmintiasis que los fármacos utilizados en forma independiente