In vitro antiproliferative activity of 3 H-spiro [1-benzofuran-2,1'-cyclohexane] derivatives / Actividad antiproliferativa in vitro de derivados de 3 H-spiro [1-benzofuran-2, 1'-cyclohexano]

The in vitro effect of the resinous exudate of Heliotropium filifolium, of the 3 H-spiro[1-benzofuran-2,1 '-cyclohexane] derivative called filifolinol 1, isolated from the resin and the semi-synthetic compounds filifolinone 2 and filifolinoic acid 3, obtained from filifolinol 1, were evaluated on the proliferation of an immortalized cell line, UCHT1, derived from rat thyroid. We evaluated the effect of these compounds on UCHT1 cell growth parameters by calculating doubling time; and toxicity using the LIVE/DEAD™ in vitro test. The results showed that the resin is not active, while filifolinone 2, filifolinoic acid 3 and filifolinol 1 produced a significant inhibition of cell doubling time, in concentrations equal or greater than 50, 25 and 75 uM, respectively. The LIVE/DEAD test showed no significant toxicity at these concentrations, compared to cultures kept in absence of compounds. These results suggest a possible cytostatic effect of these compounds, and could therefore constitute potential alternatives for antineoplasic therapy.

Se evaluó el efecto in vitro de la resina aislada desde Heliotropium filifolium y del derivado 3 H-spiro[1-benzofuran-2,1'-cyclohexano] llamado filifolinol 1, obtenido desde este exudado resinoso y los compuestos semi-sintéticos filifolinona 2 y ácido filifolinoico 3, obtenidos a partir de filifolinol 1, sobre la proliferación de la línea celular inmortal, UCHT1, derivada de tumor de tiroide de rata. Evaluamos el efecto de estos compuestos en el desarrollo celular de UCHT1 a través de los parámetros tiempo de doblaje y citotoxicidad usando el test LIVE/DEAD™ in vitro. Los resultados mostraron que la resina no presentó actividad y que filifolinona, ácido filifolinoico y filifolinol producen una inhibición significativa del tiempo de doblaje celular, en concentraciones iguales o superiores a 50, 25 y 75 uM, respectivamente. El test LIVE/DEAD no mostró toxicidad significativa en comparación con los cultivos mantenidos en ausencia de compuestos. Estos resultados sugieren un posible efecto citostático de estos compuestos y por lo tanto, constituirían alternativas potenciales para terapia antineoplásica.

Atividade antitumoral do Ageratum conyzoides L. (Asteraceae) / Antitumoral activity of the Ageratum conyzoides L. (Asteraceae)

O Ageratum conyzoides, vegetal conhecido popularmente no Brasil é constituído por várias substâncias químicas, dentre elas os flavonóides, aos quais já foi atribuída a atividade antitumoral. Neste estudo foi avaliado o efeito das frações clorofórmica e metanólica do extrato AcOEt das folhas sobre o crescimento do tumor de Ehrlich. Foi constatado que o tratamento com as frações metanólicas, nas doses de 50 mg/kg de peso foi eficaz, inibindo o crescimento tumoral. A porcentagem de inibição para a fração metanólica estabilizada foi de 69,84 por cento e de 68,25 por cento para a fração metanólica não estabilizada. Estudos posteriores se fazem necessários para esclarecer quais os mecanismos envolvidos nesta inibição do crescimento tumoral.

Ageratum conyzoides, a popular vegetal in Brazil, is composed by many chemical compounds, including flavonoids, and antitumoral activity has been attributed to it. In this assay the effect of chloroform and methanol fractions from EtOAc extract of the leaves on the growth of the Ehrlich tumor was evaluated. Under our experimental conditions we have observed that the treatment with methanol fractions, under the dosage of 50 mg/kg was efficient on inhibiting the tumoral growth. There was an inhibition percentage of 69.84 percent to the stabilized methanol fraction and 68.25 percent to the non-stabilized fraction. Further studies are necessary to clarify which mechanisms are involved in the inhibition of the tumoral growth.

Actividad proteolítica de extractos enzimáticos obtenidos de plantas de la familia Bromeliaceae / Proteolytic activity of enzymatic extracts from plants of the Bromeliaceae family

Las enzimas proteolíticas aisladas de plantas de la familia Bromeliaceae se utilizan ampliamente en la industria médica, biotecnológica y alimenticia. Los estudios realizados en los últimos años sobre la actividad contra metástasis y tumores de las cisteíno-proteasas hacen que se incremente el interés por explorar nuevas fuentes naturales de obtención de fitoproteasas. En el presente trabajo se evaluó la actividad proteolítica de extractos enzimáticos obtenidos a partir de diferentes órganos de plantas de la familia Bromeliaceae. Se colectaron y clasificaron cinco grupos. Las plantas que se colectaron pertenecen a 3 géneros de la mencionada familia: 3 grupos son del género Tillandsia, 1 es del género Guzmania y otro del género Hohenbergia. Los mayores índices de actividad específica (3,3 U/mg de proteínas) se obtuvieron en los preparados obtenidos a partir de diferentes órganos de Hohenbergia penduliflora Mez, de cuyos extractos obtenidos se evaluó la influencia del pH de extracción y la actividad específica fue superior al realizarla a pH 3 a partir de sus tallos.

The proteolytic enzymes isolated from the Bromeliaceae family are widely used in the medical, biotechnological, and food industries. The studies conducted in recent years on the activity against metastasis and cysteine-proteases, increase the interest in screening new natural sources of obtention of phytoproteases. In the present paper, the authors assessed the proteolytic activity of enzymatic extracts obtained from different organs of the Bromeliaceae family plants. Five groups were collected and classified. Plants obtained belong to three genuses of the above mentioned family: 3 groups are of genus Tillandsia , one of genus Guzmania , and the other of genus Hohenbergia . The highest rates of specific activity (3.3 U/mg of proteins) were attained in preparations obtained from different organs of Hohenbergia penduliflora Mez. from whose extracts the influence of extraction pH was assessed. The specific activity was greater on carrying it out at pH3, starting from their stalks.

Antitumor effect of Zhongjiefeng Injection on mice liver cancer Hep-A-22 and its toxicity / 中成药

Objective: To study antitumor activity of Zhongjiefeng Injection (Herba sarcandrae) on mice liver cancer Hep A 22 in vivo, in vitro and its toxic reaction in mice with Hep A 22 tumor Methods: The antitumor activity and toxicity of Zhongjiefeng Injection were determined in the mice with transplantable tumor (mice liver cancer Hep A 22), and the antitumor effect of Zhongjiefeng Injection on Hep A 22 cells in vitro were determined with MTT method. Conclusion: The experiment indicates that Zhongjiefeng Injection shows significant antitumon effect increase the indexes of immune organs and amounts of WBC.