Estudo da variação ontogenética de princípios ativos de Leonurus sibiricus L. e suas ações farmacológicas

Author(s)

Nilsa Sumie Yamashita Wadt

• Document type: Doctoral Thesis
• Press: São Paulo.
• Institution: Universidade de São Paulo (USP). Conjunto das Químicas (IQ e FCF) (CQ/DBDCQ)
• Defense date: 2000-04-11

Examining board members

Elfriede Marianne Bacchi; Jairo Kenupp Bastos; Jose Jorge Neto; Seizi Oga; Jayme Antonio Aboin Sertie

• Advisor: Elfriede Marianne Bacchi

Abstract

Leonurus sibiricus L. (family Lamiaceae), is native to Asia, nevertheless this species is so adaptaded in Brazil that we can consider it Brazilian. lts application in gynecological diseases in known for centuries in China; in Brazil, its used as antispasmodics, antireumatic, against mataria fever, but its popular use is a topical antiinflammatory, in state of São Paulo. ln this work we did the follow up of flavonoids \'s contents, in different time of the year as well as in different phases of development of this herb. We could verify that, in adequate conditions of culture, the species produce a greater amount of green mass and thus a greater amount of flavonoids. We chose to work only with the leaves and not with the aerial parts, as shown in the bibliography, so that we could keep track of these specimen since the germination until the frutification, collecting from these specimen the seeds for next culture, thus decreasing the genotipical variation. The pharmacological activities tested were: antiulcer, antimicrobial, antioxidant, anti-inflammatory and also toxicity evaluation, subchronic and acute, including DL50. Regarding the antioxidant activity, despite the thin layer chromatography result indicate the antioxidant substances, in vitro test (MDA), the Q1/2 was 53&#181;g/mL, while the &#945;-tocopherol was 12,10&#181;g/mL. These results only show that, having tested the hidroalcoolic extract by 70%, the components which indicate antioxidant action may be found in inferior concentration, or this extract contains not only antioxidant components but also pro-oxidant ones. The anti-inflammatory action was tested in three models: induction of the granuloma, paw edema induced by carragenin, croton oil dermatitis, observing that in 360mg/kg dose, all of the models showed positive responses. ln the two first models, the administration via was intraperitoneal. According to the induction granuloma model, topical and oral via, no inflammation inhibition occured. Regarding the croton oil dermatitis, not only the hidroalcoolic extract by 70% but also the aqueous extract of L sibiricus, demonstrated positive responses in 0,014mg/ear dose (360mg/kg). These models apply mainly in acute topical action, which confirms the popular use as a topical antiinflammatory. ln the antiulcer action results,the extract shows positive result only in levei Ili ulcerations (hemorrhagic), which can be considered of the nonsteroidal anti-inflammatory, presents an ulcerogenic action as a side effect. The antimicrobial action, once the freezedryed hidroalcoholic extract 70º/o displayed a growth inhibition for the Staphy/ococcus aureus, Candida albicans, Pseudomonas aeruginosa, with minimum inhibitory concentration (MIC), 0,1 mg/mL<MIC<0,5mg/mL, of the extract. Having already tested the chloroform fraction (EC), etil acetate (ACet), ethanolic (EET), aqueous (EA) of L sibiricus, the inhibition ofmicrobial growth occured only for the Staphylococcus aureus, in fractions EC, EACet, EET, with 0,1mg/mL<MIC<0,5mg/mL; regarding the aqueous fraction the result was negative. These results suggest the sinergism action among the extract components, since it was observed a decrease of microbial growth inhibition after the fraction. The extract indicated a fairly low toxicity in the acute and subchronical tests, with DL50 3,999/kg, intraperitoneal via, which can be considered non-toxic. (AU)