Modulação da hemostasia por inibição enzimática exercida por folhas de Averrhoa carambola

Herbal medicines represent an advantageous alternative for the prevention and treatment of several diseases when compared to allopathic medicines. Averrhoa carambola (Oxalidaceae) is a plant rich in phenolic compounds and popularly known for its medicinal properties such as anti-inflammatory, antioxidant, and hypoglycemic. Different enzymes of the human organism participate in physiological processes which involve hemostasis, inflammation, and formation of new tissue. These enzymes are highlighted as pharmaceutical targets for the treatment of numerous pathologies. The present work evaluated the aqueous and ethanolic extracts from A. carambola leaves on phospholipase, hemolytic, caseinolytic, thrombolytic, coagulant, and fibrinogenolytic activities induced by phospholipases A2 and proteases. Phenolic compounds and total flavonoids were quantified in the aqueous and ethanolic extracts of the leaves of Averrhoa carambola. These extracts were evaluated, in vitro, on phospholipase, proteolytic, hemolytic, thrombolytic and fibrinogenolytic activities induced by snake venoms. The results confirm the pharmacological potential of A. carambola since the extracts were able to modulate all evaluated activities related to hemostasis through inhibitions or potentiation of the enzymatic activities (phospholipases A2 and proteases). The constituents of A. carambola may act interfering in processes such as coagulation, thrombus dissolution, and fibrinogenolysis.Os medicamentos fitoterápicos representam uma alternativa vantajosa para a prevenção e tratamento de diversas doenças quando comparados aos medicamentos alopáticos. Averrhoa carambola (Oxalidaceae) é uma planta rica em compostos fenólicos e popularmente conhecida por suas propriedades medicinais como anti-inflamatória, antioxidante e hipoglicêmica. Diferentes enzimas do organismo humano participam de processos fisiológicos que envolvem hemostasia, inflamação e formação de novos tecidos. Essas enzimas são destacadas como alvos farmacêuticos para o tratamento de inúmeras patologias. O presente trabalho avaliou os extratos aquoso e etanólico das folhas de A. carambola sobre as atividades fosfolipásica, hemolítica, caseinolítica, trombolítica, coagulante e fibrinogenolítica induzidas por fosfolipases A2 e proteases. Compostos fenólicos e flavonoides totais foram quantificados nos extratos aquoso e etanólico das folhas de A. carambola. Esses extratos foram avaliados, in vitro, sobre as atividades fosfolipásica, proteolítica, hemolítica, trombolítica e fibrinogenolítica induzidas por peçonhas de serpentes. Os resultados confirmam o potencial farmacológico de A. carambola uma vez que os extratos foram capazes de modular todas as atividades avaliadas relacionadas à hemostasia por meio de inibições ou potencialização das atividades enzimáticas (fosfolipases A2 e proteases). Os constituintes de A. carambola podem atuar interferindo em processos como coagulação, dissolução de trombos e fibrinogenólise

Testes de citogenética vegetal podem prever efeitos tóxicos em células humanas: efeitos genotóxicos e mutagênicos da peçonha do escorpião Tityus serrulatus em células vegetais e humanas

The effects of Tityus serrulatus venom was accessed on the cell cycle and genetic material of the Lactuca sativa L. and compared with the damages to human leukocytes, in order to evaluate the genotoxic and mutagenic potential of toxins on cell types very different. The occurrence of cell cycle alterations and DNA fragmentation was evaluated in Lactuca sativa. Incubations of venom with human leukocytes were also held with subsequent evaluation of cell proliferation index, micronucleus and fragmented DNA. The T. serrulatus venom showed cytogenotoxic, reducing mitotic index and induced alterations in the cell cycle and micronuclei formation. The occurrence of cell death was evidenced by the detection of condensed nuclei, positive TUNEL signals, and presence of DNA fragmentation on lettuce cells. The scorpion venom induced DNA fragmentation and micronuclei in leukocytes. Further, the role of peptides and proteases from this venom in inducing the observed damage was discussed.Os efeitos da peçonha de Tityus serrulatus foram avaliados no ciclo celular e material genético da Lactuca sativa L. e comparados com os danos a leucócitos humanos, a fim de avaliar o potencial genotóxico e mutagênico de toxinas em tipos celulares muito diferentes.. Também foram realizadas incubações de peçonha com leucócitos humanos com posterior avaliação do índice de proliferação celular, micronúcleo e DNA fragmentado. A peçonha de T. serrulatus mostrou-se citogenotóxica, reduzindo o índice mitótico e induzindo alterações no ciclo celular vegetal e formação de micronúcleos. A ocorrência de morte celular foi evidenciada pela detecção de núcleos condensados, sinais TUNEL positivos e presença de fragmentação de DNA em células de alface. A peçonha do escorpião induziu fragmentação de DNA e micronúcleos em leucócitos. Além disso, o papel dos peptídeos e proteases desta peçonha na indução do dano observado foi discutido

Thrombolysis, clotting, and genotoxic activities modulated by essential oils extracted from Lippia alba

The composition and pharmacological properties of Lippia alba (Mill.) (L. alba) (Verbenaceae) flower and leaf essential oils (EO) were determined in this study. The major constituents in the flower EO were geranial (49.83%) and neral (32.75%), and in the leaf EO were geranial (38.06%), neral (31.02%), and limonene (18.03%). Flower EO inhibited thrombolysis induced by Bothrops moojeni (B. moojeni) and Lachesis muta muta (L. muta muta) venoms (0.05-1.2 µL mL-1). When tested against L. muta muta venom, the protective effect was smaller in both EO. The EOs prolonged the clotting time induced by L. muta muta venom and a procoagulant effect was observed on B. moojeni. In the comet assay, the flower EO presented anti-genotoxic action (damage frequency of only 11.6 - 34.9%) against the L. muta muta venom. The positive control (Doxorubicin) and the venom alone presented a damage frequency of 80.3% and 70.7%, respectively. The flower EO protected DNA from damage induced by L. muta muta venom. L. alba leaf and flower EOs presented anti-genotoxic actio

Achyrocline satureioides (Lam.) DC extracts acting as enzyme modulators: digestion, inflammation, and hemostasis

Achyrocline satureioides is popularly known for its richness in phenolic compounds and medicinal properties (anti-inflammatory, analgesic, and hepatoprotective). The present study aimed at broadening the knowledge about the pharmacological potential exerted by the aqueous and ethanolic extracts of A. satureioides. These extracts were characterized by HPLC and tested for their modulatory action on phospholipases A2 and proteases of snake venoms. In addition, they were tested on the activities of digestive enzymes. Snake venoms were used as tools since they have enzymes with high functional and structural homology to human enzymes. The results demonstrate that the extracts of A. satureioides act as enzymatic inhibitors or potentiators, interfering in processes related to the hemostasis, such as coagulation and thrombus dissolution. In addition, the anti-genotoxic activity and inhibitions exerted on digestive enzymes suggests their potential use in the prevention and/or treatment of several pathologies. New studies could provide information on how the compounds present in the extracts and the different enzymes interact