Antioxidant potential, anti-inflammatory activity, antidiabetic and cardioprotective effect of Microsechium helleri (Peyr. ) Cong / Potencial antioxidante, actividad anti-inflamatoria, efecto antidiabético y cardioprotector de Microsechium helleri (Peyr. ) Cong

Microsechium helleri (Cucurbitaceae) has been used in ethnopharmacological as a lotion to prevent hair loss, diuretic and cathartic, in the region of central Veracruz, Mexico is used as antidiabetic. The antioxidant properties of the hexanic (EHex), chloroformic (ECHCl3) and ethanolic (EEtOH) extracts, were evaluated by 2,2diphenyl-1-pychrylhydrazyl (DPPH) test, the Ferric Reducing/Antioxidant Power (FRAP) and the total phenolic content test. The anti-inflammatory effect was evaluated in the acute ear edema induced with phorbol 12-myristate 13-acetate (TPA) in mouse and the hypoglycemic and cardioprotective effects of the EEtOH were determined in rats. The EEtOH was the most active in the antioxidant potential DPPH test and the ECHCl3 was the best in the FRAP assay and the total polyphenols content. In the anti-inflammatory assay, the ECHCl3 showed the most activity. The EEtOH had the decreased the glucose levels and reduced myocardial damage. The results support the use of this plant in folk medicine in Mexico as antioxidant, anti-inflammatory, hypoglycemic and cardioprotective.

Microsechium helleri (Cucurbitaceae) se utiliza en etnofarmacología como una loción para prevenir la caída del cabello, como diurético y catártico, en la región del centro de Veracruz, México es usado como antidiabético. Las propiedades antioxidantes de los extractos hexánico (EHex), clorofórmico (ECHCl3) y etanólico (EEtOH), se evaluaron mediante la prueba de 2,2difenil-1-psililhidrazilo (DPPH), el poder reductor férrico/poder antioxidante (FRAP) y el contenido fenólico total. El efecto anti-inflamatorio se evaluó en el edema agudo de la oreja inducido con forbol 12-miristato 13-acetato (TPA) en ratones y se determinaron los efectos hipoglucémicos y cardioprotectores del EEtOH en ratas. El EEtOH fue el más activo en la prueba DPPH de potencial antioxidante y el ECHCl3 fue el mejor en el ensayo FRAP y el contenido total de polifenoles. En el ensayo antiinflamatorio, el ECHCl3 mostró la mayor actividad. El EEtOH disminuyó los niveles de glucosa y redujo el daño miocárdico. Los efectos hipoglucémicos y cardioprotector del extracto de EEtOH se determinaron en ratas, donde el extracto disminuyó los niveles de glucosa y redujo el daño miocárdico. Los resultados apoyan el uso de esta planta en la medicina popular en México como antioxidante, anti-inflamatorio, hipoglucemiante y cardioprotector.

A QSAR study on a series of simplified digitalis-like compounds acting on Na+,K+-ATPase

Among the cardiotonics (agents against congestive heart failure), the most important group is of the digitalis cardiac glycosides, but since these compounds suffer from a low therapeutic index, attention has been paid to investigating safer cardiotonic agents through the inhibition of Na+,K+-ATPase, the mechanism by which the digitalis cardiac glycosides elicit their action. Recently, a series of perhydroindenes were studied for their Na+,K+-ATPase inhibition activity. We report here a QSAR study on them to investigate the physicochemical and structural properties of the molecules that govern their activity in order to rationalize the structural modification to have more potent drugs. A multiple regression analysis reveals a significant correlation between the Na+,K+-ATPase inhibition activity of the compounds and Kier’s first order valence molecular connectivity index of their R5-substituents and some indicator parameters, suggesting that the R5-substituents of the compounds containing atoms with low valence and high saturation and the R1-substituents having =N−O− moiety will be conducive to the activity.

Participação de um agente adrenérgico não peptídico na ação inotrópica positiva da fração polar da Bryopsis pennata / Participation of a non-peptide adrenergic agent on positive inotropic effect of the polar fraction of Bryopsis pennata

As algas marinhas representam uma rica fonte de compostos bioativos, algumas delas precursoras de ferramentas farmacológicas e de substâncias potencialmente úteis para o desenvolvimento de novos fármacos. A macroalga Bryopsis pennata, Cloroficea pertencente à ordem Caulerpales, sin. Bryopsidales é uma espécie tropical encontrada em diversos costões rochosos. Essa espécie produz uma defesa química tóxica para organismos herbívoros e potencial de se tornar invasiva e dominante em condições ambientais favoráveis. Este trabalho é uma investigação do efeito cardiotônico da fração polar da B. pennata .O cultivo, em ambiente controlado destituído de contaminantes, foi realizado no intuito de comparar seus efeitos com os efeitos da alga coletada. O efeito cardiotônico cronotrópico positivo em tiras ventriculares de anuros ficou fortemente evidenciado nos testes com frações polares de algas coletadas e cultivadas, não apresentando diferenças significativas entre as frações. O propranolol antagonizou o efeito cardiotônico e enzimas endopeptidases não reagiram com a fração polar da B. pennata. Testes bioquímicos demonstraram que a fração com efeito cardiotônico é de caráter ácido e apresenta peso molecular menor que 10.000 daltons.

Marine algae are a rich source of bioactive compounds and some of them have shown to be useful for the development of new pharmacological tools and medicines. Bryopsis pennata, (Clorofícea, Caulerpales, sin. Bryopsidales) is a marine algae that can be found in the Southeastern Brazilian coast and elsewhere. The species produces a toxic chemical defense to the herbivorous organisms and possesses a potential to become invasive and dominant in favorable environmental conditions.The present study is about the investigation of the cardiotonic effect of the polar extract of B. pennata. The cultive in laboratory without any contaminants was made to compare studies performed with the collected algae extracts and the ones cultivated effect. The cardiotonic effect in the anurou’s ventricular strips was strongly unequivocal when it was tested with the polar extracts from the collected and cultivated algae. The propranolol antagonized polar effects of these algae and the endopeptidase enzyme did not change the effects of polar extracts of Bryopsis pennata. Biochemical tests showed that the polar fraction presenting the inotropic cardiac activity weighs less than 10.000 Daltons and has an acid character.

Electric field mapping and structure-activity relationship for cardiotonic activities of medorinone and some of its analogs.

Medorinone 5-methyl-1,6-napthyridin-2(1H)-one and some of its analogs having varying degrees of cardiotonic potency have been studied by molecular orbital and electric field mapping methods. Ground state geometries of the molecules were optimized using the MNDO molecular orbital method. Hybridization displacement charges (HDC) combined with Löwdin charges as well as Mulliken charges were used for electric field mapping around the molecules. Electric fields near the O2 site of medorinone and its analogs correlate well with their observed cardiotonic potencies. This result is in agreement with certain pharmacological models for cardiotonics.