RESUMO: "Produtos naturais inibidores da enzima conversora de angiotensina (ECA).Uma revisão entre 1980 -2000". A inibição da Enzima Conversora da Angiotensina (ECA) é um alvo terapêutico moderno e efi caz no tratamento da hipertensão arterial. Na cascata enzimática que envolve o sistema renina-angiotensina, a ECA promove a remoção dos aminoácidos histidilleucina da angiotensina I para formar o octapeptídio angiotensina II, a qual é fi siologicamente ativa em diversos sistemas, e considerado como um dos mais potentes vasoconstrictores endógenos conhecido. Portanto, uma racionalidade no tratamento da hipertensão seria administrar drogas ou compostos de origem natural que inibam seletivamente a ECA. O presente estudo constitui uma revisão da literatura sobre plantas e moléculas de origem natural com potencial anti-hipertensivo, baseado na inibição in vitro da ECA. A revisão referencia 321 plantas, partes usadas, tipo de extrato e se é ativo ou não. Inclui ainda o nome de 158 compostos isolados de plantas superiores, esponjas e algas marinhas, fungos e venenos de cobra. Alguns aspectos de pesquisa recente com produtos naturais direcionados à produção de drogas anti-hipertensivas também são discutidos. Nesta revisão 148 referências foram consultadas.Unitermos: Enzima conversora da angiotensina, efeito anti hipertensivo, agentes hipotensivos. ABSTRACT: Inhibition of Angiotensin Converting Enzyme (ACE) is a modern therapeutic targetin the treatment of hypertension. Within the enzyme cascade of the renin-angiotensin system, ACE removes histidyl-leucine from angiotensin I to form the physiologically active octapeptide angiotensin II, one of the most potent known vasoconstrictors. Therefore, a rationale for treating hypertension would be to administer drugs or natural compounds which selectively inhibit ACE. The present work constitutes a review of the literature of plants and chemically defi ned molecules from natural sources with in vitro anti-hypertensive potential based on the inhibition of ACE. The review refers to 321 plants, the parts utilized, type of extract and whether they are active or not. It includes also the names of 158 compounds isolated from higher plants, marine sponges and algae, fungi and snake venom. Some aspects of recent research with natural products directed to produce anti-hypertensive drugs are discussed. In this review, 148 references were cited.

RESUMO: Das partes aéreas de Herissantia tiubae (K. Schum.) Brizicky foram isolados, através de métodos cromatográfi cos, dois fl avonóides glicosilados, canferol 3,7-di-O-α-L-ramnopiranosídeo e canferol 3-β-O-D-(6''-E-p-cumaroil) glicosídeo. As estruturas foram identifi cadas com o uso de técnicas espectroscópicas de IV, RMN 1 H e 13 C incluindo métodos bidimensionais, além de comparações com dados da literatura. O canferol 3,7-di-O-α-L-ramnopiranosídeo foi submetido a testes farmacológicos preliminares com a fi nalidade de avaliar o seu efeito sobre o sistema cardiovascular.Unitermos: Herissantia tiubae, Malvaceae, fl avonóides, atividade cardiovascular. C NMR spectroscopy, including two dimensional techniques, together with comparison with literatura data. Preliminary tests were carried out with kaempferol 3,7-di-O-α-L-rhamnopyranoside in order to study its possible cardiovascular effect.

1 The aim of this work was to study the effects of N-salicyloyltryptamine (STP), a novel anticonvulsant agent, on voltage-gated ion channels in GH3 cells. 2 In this study, we show that STP at 17 mM inhibited up to 59.2710.4% of the I to and 73.178.56% of the I KD K þ currents in GH3 cells. Moreover, the inhibitory activity of the drug STP on K þ currents was dose-dependent (IC 50 ¼ 34.678.14 mM for I to ) and partially reversible after washing off. 3 Repeated stimulation at 1 Hz (STP at 17 mM) led to the total disappearance of I to current, and an enhancement of I KD . 4 In the cell-attached configuration, application of STP to the bath increased the open probability of large-conductance Ca 2 þ -activated K þ channels. 5 STP at 17 mM inhibited the L-type Ca 2 þ current by 54.977.50% without any significant changes in the voltage dependence. 6 STP at 170 mM inhibited the TTX-sensitive Na þ current by 22.172.41%. At a lower concentration (17 mM), no effect on I Na was observed. 7 The pharmacological profile described here might contribute to the neuroprotective effect exerted by this compound in experimental 'in vivo' models.

RESUMO:A realização de estudos farmacológicos é fundamental para comprovar a eficácia do uso de plantas medicinais pela população para o tratamento de doenças e descobrir novos fitoterápicos. Palavras-chave: Maytenus rigida, bom nome, Celastraceae, atividade antibacteriana, plantas medicinais ABSTRACT: Evaluation of the antimicrobial activity of Maytenus rigida Mart. (Celastraceae).Ppharmacological studies are essential to prove the effectiveness of using medicinal plants to treat diseases and discover new phytotherapics. This study aimed to evaluate the antimicrobial potential of ethanol and ethyl acetate extracts of "bom-nome" (Maytenus rigida Mart.) against Staphylococcus aureus ATCC 25923, three samples of multiresistant Staphylococcus aureus isolated from patients with nosocomial infections, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and Salmonella sp. (228-R-Tet, 118-R-Sut and 01-S) isolated from water environment, using the agar diffusion test. Both extracts showed in vitro antimicrobial activity against all S. aureus strains, presenting 400 mg mL -1 minimum inhibitory concentration (MIC). However, these products did not show activity against strains of the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa and Salmonella sp.

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The N-salicyloyltryptamine (NST) is an indole derivative compound analogue to the alkaloid N-benzoyltryptamine. In the present study, the antiedematogenic activity of NST was investigated in animal models. Firstly, the acute toxicity for NST was assessed according to the OECD Guideline no. 423. The potential NST-induced antiedematogenic activity was evaluated by carrageenan-induced paw edema in rats, as well as by dextran-, compound 48/80-, histamine-, serotonin-, capsaicine-, and prostaglandin E2-induced paw edema in mice. The effect of NST on compound 48/80-induced ex vivo mast cell degranulation on mice mesenteric bed was investigated. No death or alteration of behavioral parameters was observed after administration of NST (2000 mg/kg, i.p.) during the observation time of 14 days. The NST (100 and 200 mg/kg, i.p.) inhibited the carrageenan-induced edema from the 1st to the 5th hour (**p<0.01; ***p<0.001). The edematogenic activity induced by dextran, compound 48/80, histamine, serotonin, capsaicin, and prostaglandin E2 was inhibited by NST (100 mg/kg, i.p.) throughout the observation period (**p<0.01; ***p<0.001). The pretreatment with NST (50, 100 or 200 mg/kg, i.p) attenuates the compound 48/80-induced mast cell degranulation (**p<0.01; ***p<0.001). Thus, the inhibition of both mast cell degranulation and release of endogenous mediators are probably involved in the NST-induced antiedematogenic effect.

We investigated the antinociceptive and nerve excitability effects of the N-salicyloyltryptamine (NST) NST-treated mice exhibited a significant decrease in the number of writhes when 100 and 200 mg/kg (i.p.) were administered (i.p.). This effect was not antagonized by naloxone (1.5 mg/kg, i.p.). NST inhibited the licking response of the injected paw when 100 and 200 mg/kg were administered (i.p.) to mice in the first and second phases of the formalin test. Because the antinociceptive effects could be associated with neuronal excitability inhibition, we performed the single sucrose gap technique and showed that NST (3.57 mM) significantly reduced (29.2%) amplitude of the compound action potential (CAP) suggesting a sodium channel effect induced by NST. Our results demonstrated an antinociceptive activity of the NST that could be, at least in part, associated to the reduction of the action potential amplitude. NST might represent an important tool for pain management.

Four known flavones, 5-hydroxyauranetin, araneosol, calycopterin and sarothrin, were isolated from the aerial parts of Herissantia tiubae (K. Schum) Brizicky (Malvaceae). Their structures were identified by the use of spectroscopic methods such as IR, UV, and mainly nuclear magnetic resonance, which included two-dimensional techniques ( 1 H-1 H COSY, NOESY, HETCOR, and HMBC). This is the first reported isolation of these compounds from the genus Herissantia.