Ameliorating effects of ethanol extract of root bark of Salacia nitida on blood electrolyte and renal perturbations in Plasmodium berghei-infected mice

Abstract Malaria, a disease of public health concern is a known cause of kidney failure, and dependence on herbal medicines for its treatment is increasing due to the high cost of drugs. So this study is designed to evaluate the ameliorating effect of ethanol extract from Salacia nitida root bark on electrolyte and renal perturbations in Plasmodium berghei-infected mice. Thirty malariainfected mice divided into five groups of six mice each and another group of six uninfected mice were used for the study. 280, 430, and 580 mg/kg of extract were given to infected mice in groups B, C, and D, 4 mg/kg of artesunate given to group E mice, and 4 ml/kg of physiological saline given to group A and uninfected group F mice for five days. Serum Na+, K+, HCO3, Cl-, TB, urea, creatinine, BUN concentrations, and BUN/creatinine ratio were determined using standard methods. Results showed significant increases (p < 0.05) in Na+, K+, and HCO3 and decreases in Cl-, TB, urea, creatinine, BUN, and BUN/creatinine ratio in the infected treated mice in groups B - E. This study showed that ethanol extract of S. nitida root bark is efficient in the treatment of renal disorders and blood electrolyte perturbations

Changes in activities of antioxidant enzymes in radish (Raphanus sativus) seedlings in response to allelopathic effect of safflower (Carthamus tinctorius)

Abstract ROS (Reactive Oxygen Species) production is a usual plant reaction to environmental stresses such as allelopathy. Plants possess antioxidant enzymes to scavenge cells and resist against the ROS. This study was conducted to evaluate changes in antioxidant enzymes (CAT, GPX, APX) in radish seedlings in response to allelopathic effect of safflower root and shoot residues grown under normal irrigation and drought stress. Safflower allelopathic effect led to an increase in antioxidant enzymes activities. GPX activity increased more than CAT and APX. Radish seedlings exposed to safflower residue grown under drought stress showed more antioxidant enzymes activities. Root residues enhanced the activities of antioxidant enzymes greater than shoot. Seedlings exposed to root residues grown under drought stress had the highest level of antioxidant enzymes activities.

Tacinga inamoena vegetal drug characterization using phytochemistry, pharmacopoeial methods and thermoanalytical techniques

Tacinga inamoena (K. Schum.) N.P. Taylor & Stuppy, also known as quipá, is a native cactus of the Caatinga used in traditional medicine to treat urethral infections and inflammation. This study aimed to determine the physicochemical characteristics of vegetal drug obtained from the roots of T. inamoena. Analytical techniques and phytochemical tests were used, such as thermal analysis, qualitative and semiquantitative determination of secondary metabolites and spectroscopy at the infrared region. The powder of the vegetal drug met the parameters established by the Brazilian Pharmacopoeia, except for compressibility, which was low. On the thermogravimetric curve, three events related to the mass loss were verified, which correlate with the vegetal drug quality control and play a part in their standardization. The qualitative screening suggested the presence of alkaloids, flavonoids and terpenes. The infrared spectrum reinforced the presence of hydroxyl, carbonyl, and ether groups. In the semiquantitative screening, a concentration for total polyphenols of 65 mg equivalent to gallic acid g-1 to the crude ethanol extract (CEE) was obtained. On the correlation of flavonoid content to seasonality, a concentration was obtained of 3.3 mg equivalent to quercetin g-1 to the CEE obtained during the drought period and of 10.6 mg equivalent to quercetin g-1 to the CCE obtained during the rainy season. In T. inamoena, the presence of important classes of secondary metabolites, which are associated with the pharmacognostic characterization, aids the authentication and quality control of vegetal drugs of importance in traditional Brazilian medicine.

Agrobacterium rhizogenes-mediated transformation of Hypericum sinaicum L. for the development of hairy roots containing hypericin

Hypericum sinaicum L. is an endangered Egyptian medicinal plant of high importance due to the presence of naphthodianthrones (hypericins), which have photodynamic properties and pharmaceutical potential. We sought to assess H. sinaicum ability to develop hairy roots that could be cultured in contained conditions in vitro and used as a source for hypericin production. We used four A. rhizogenes strains differing in their plasmids and chromosomal backgrounds to inoculate excised H. sinaicum root, stem and leaf explants to induce hairy root development. Additionally, inoculum was applied to shoots held in Rockwool cubes supporting their stand after removal of the root system. All explant types were susceptible to A. rhizogenes although stem explants responded more frequently (over 90%) than other explant types. The A4 and A4T A. rhizogenes strains were highly, and equally effective in hairy root induction on 66-72% of explants while the LBA1334 strain was the most effective in transformation of shoots. Sonication applied to explants during inoculation enhanced the frequency of hairy root development, the most effective was 60 s treatment doubling the percentage of explants with hairy roots. However, shoot transformation was the most effective approach as shoots developed hairy roots within 10 days after inoculation. Molecular analyses confirmed that the established hairy root cultures in vitro were indeed obtained due to a horizontal gene transfer from bacteria. These cultures grew fast and the hypericin content in hairy roots was about two fold higher than in H. sinaicum plants as determined by HPLC.

Análogos sintéticos da cheferina I: interação com íons metálicos divalentes e o seu efeito na internalização celular e nas atividades anticandida e candidacida / Synthetic analogues of Shepherin I: interaction with metal divalent ions and their effect on cellular internalization and on anticandidal/candidacidal activitie

O desenvolvimento de resistência antimicrobiana e a consequente seleção de microrganismos multirresistentes consolidam-se como grandes ameaças à saúde global. Neste contexto, a busca por novas drogas antimicrobianas/microbicidas é fundamental e compostos como os peptídeos antimicrobianos (AMPs) tornaram-se alvos atraentes. Os AMPs são compostos químicos de massa molar média e grande diversidade estrutural, produzidos por todos os seres vivos e com capacidade de inibir o crescimento de e/ou matar microrganismos. O AMP Cheferina I (Chef I) foi isolado das raízes de Capsella bursa-pastoris e é resultado da proteólise de uma proteína da família das proteínas ricas em glicina, que em plantas estão relacionadas às funções de defesa e cicatrização. O nosso grupo de pesquisa foi pioneiro no desenvolvimento e estudo de análogos truncados amidados deste AMP atípico rico em glicina (67,9%) e histidina (28,6%), que se mostraram ativos frente às diferentes cepas de Candida e a S. cerevisiae pela internalização/ação celular acompanhada de manutenção da integridade da membrana plasmática; o análogo amidado (Chef Ia) e o análogo marcado com 5(6)-carboxifluoresceína/FAM (FAM-Chef Ia) tiveram as suas atividades antifúngicas potencializadas por íons Zn2+. Este trabalho deu continuidade ao estudo do efeito dos íons metálicos divalentes Zn2+, Cu2+, Ca2+ e Mg2+ nas atividades anticandida/fungistática e candidacida/fungicida a diferentes pHs e forças iônicas, estruturas e localizações intracelulares destes análogos. Os resultados na ausência de íons em pH 5,1 revelaram maior atividade do análogo fluorescente em relação à do não fluorescente. Neste mesmo pH, as atividades anticandida e candidacida de Chef Ia foram influenciadas negativamente pelos íons Ca2+ e Mg2+ (2-4 vezes) enquanto que, na presença de íons Zn2+ as atividades anticandida de ambos os análogos foram aumentadas (Chef Ia: 8-64 vezes; FAM-Chef Ia: 4-32 vezes). Os íons Cu2+ aumentaram a atividade anticandida de Chef Ia (2-4 vezes), mas não a do análogo fluorescente, mas as atividades candidacidas de ambos foram melhoradas (Chef Ia: 2-8 vezes; FAM-Chef Ia: 2 vezes). Em pH 5,1, os íons Zn2+ mantiveram a atividade anticandida de Chef Ia em alta força iônica, mas só FAM-Chef Ia exibiu atividade candidacida. Em pH 7,4 ambos análogos foram inativos em baixa e alta forças iônicas na ausência e presença de Zn2+ ou Cu2+. As maiores porcentagens de folhas-ß-antiparalelas e dobras foram observadas no espectro de DC de Chef Ia em pH 7,4, sendo que aqueles registrados em pH 5,1 e 7,4 em presença de íons Zn2 e Cu2+ indicaram a formação de quelatos estruturalmente distintos. Ambos os peptídeos são bioquelantes em potencial, sendo as proporções peptídeo: íon obtidas as seguintes: FAM-Chef Ia = 1:2 para Cu2+, 1:10 para Zn2+; Chef Ia = 1:1 para Cu2+. A análise da internalização celular de FAM-Chef Ia permitiu a suposição de dois mecanismos de internalização (translocação direta e endocitose), sendo que nas células vivas a presença de Zn2+ afetou negativamente a translocação direta (p 0,0343) e potencializou a endocitose (p 0,0002)

The development of antimicrobial resistance and the consequent selection of multiresistant microorganisms have become major threats to global health. In this context, the search for new antimicrobial/microbicidal drugs is crucial and the antimicrobial peptides (AMPs) have been seen as attractive targets. AMPs are chemical compounds of medium molecular mass and high structural diversity produced by all living beings, capable of inhibiting the growth of microorganisms and killing them. The AMP Shepherin I (Shep I) was isolated from the roots of Capsella bursa-pastoris, being a bioactive peptide encrypted in a glycine-rich protein from a family that in plants are strictly related to defense and healing functions. Our research group has pioneered the development and study of amidated truncated analogues of this atypical glycine- (67.9%) and histidine-rich (28.6%) AMP, which has shown activity against different strains of Candida and S. cerevisiae through cellular internalization with maintenance of the plasma membrane integrity. The amide analogue (Chef Ia) and its fluorescent analog labeled with 5 (6) - carboxyfluorescein / FAM (FAM-Chef Ia) had their antifungal activities potentiated by Zn2+ ions, so the present work continued examining the effect of the divalent metallic ions Zn2+, Cu2+, Ca2+ and Mg2+ on the anticandidal/fungistatic and candidacidal/fungicide activities at different pHs and ionic forces, structures and intracellular locations of these analogues. The results in the absence of those ions at pH 5.1 revealed that the fluorescently labelled analog was more potent than the nonfluorescent. At the same pH, Shep Ia anticandidal and candidacidal activities were negatively influenced by Ca2+ and Mg2+ ions (2-4 fold), whereas in the presence of Zn2+ ions the anticandidal activities of both analogues were increased (Shep Ia: 8-64 fold, FAM- Shep Ia: 4-32 fold). Cu2+ ions increased Shep Ia anticandidal activity (2-4 fold) but not that of FAM-Shep Ia, nevertheless, the candidacidal activities of both analogues were increased (Shep Ia: 2-8 fold, FAM-Shep Ia: 2 fold). Also at pH 5.1, the Zn2+ ions helped retaining the anticandidal activity of Shep Ia at high ionic strength, although only FAM-Shep Ia exhibited candidacidal activity. At pH 7.4 both analogues were inactive at low and high ionic strengths in the absence or presence of Zn2+ or Cu2+. The highest percentages of antiparallel ß-sheet and turns were observed in Shep Ia CD spectrum at pH 7.4, while those recorded at pH 5.1 and 7.4 in the presence of Zn2+ or Cu2+ ions indicated the formation of structurally different chelates. Both peptides are potential biochelates, with the following peptide:ion ratios: FAM-Shep Ia = 1: 2 for Cu2+, 1:10 for Zn2+; Shep Ia = 1: 1 for Cu2+. The analysis of the cellular internalization of FAM-Chef Ia allowed the assumption of two mechanisms of internalization (direct translocation and endocytosis) and in the living cells the presence of Zn2+ negatively affected the direct translocation (p 0.0343) and potentiated endocytosis (p 0.0002)

Composição química e atividade inseticida do extrato acetônico de Piper alatabaccum Trel & Yuncker (Piperaceae) sobre Hypothenemus hampei Ferrari / Chemical constituents and insecticidal activity of the crude acetonic extract of Piper alatabaccum Trel & Yuncker (Piperaceae) on Hypothenemus hampei Ferrari

O presente trabalho teve como objetivo investigar a composição química e avaliar a atividade inseticida do extrato acetônico das raízes de Piper alatabaccum sobre Hypothenemus hampei. As raízes foram coletadas no campus da Universidade Federal de Rondônia, em Porto Velho-RO. Diluições de 100,0, 50,0, 25,0, 5,0 e 0,5 mg mL-1 foram utilizadas para exposição na superfície contaminada e aplicação tópica. No teste de repelência, utilizou-se as diluições de 25,0 e 100,0 mg mL-1. As avaliações ocorreram durante 48 horas após a exposição ao extrato. O extrato foi eficiente na mortalidade em aplicação tópica e superfície contaminada, não sendo eficiente no efeito de repelência. Estes resultados apontam para o elevado potencial inseticida do extrato de P. alatabaccum no controle de H. hampei. Identificou-se cinco compostos, sendo três amidas, dihydropiplartine piperovatina e piplartina, e duas flavona, 3',4',5,5',7 pentamethoxyflavone e 5,5',7-trimetóxi-3',4'-methylenedioxyflavone.

The purpose of this work was to investigate the chemical composition and to evaluate the insecticidal activity of the acetonic extract of Piper alatabaccum roots on Hypothenemus hampei. Roots of P. alatabaccum were collected at the University of Rondônia in Porto Velho-RO. Dilutions of 100.0, 50.0, 25.0, 5.0 and 0.5 mg mL-1 were used for exposition in the contaminated surface and for topical application. For the repellence test, 25.0 and 100.0 mg mL-1 dilutions were used. The evaluations occurred during 48 hours after exposure to the extract. The extract was efficient in terms of mortality, but no repellence was observed in the bioassays. These results pointed out the high insecticidal potential of the P. alatabaccum extract to control H. hampei. Five compounds, three amids, piperovatine, dihydropiplartine and piplartine, and two flavones, 3',4',5,5',7-pentamethoxyflavone and 5,5',7-trimethoxy-3',4' methylenedioxyflavone were identified.

Avaliação da toxicidade aguda e da atividade cicatrizante dos extratos etanólicos das folhas e raízes da Memora nodosa (Silva Manso) Miers (Bignoniaceae) / Evaluation of acute and healing activity of ethanol extracts of Memora nodosa (Silva Manso) Miers (Bignoniaceae) leaves and roots

Memora nodosa (Silva Manso) Miers é uma espécie da flora do Cerrado cujas folhas e caules são utilizados popularmente no tratamento de feridas e úlceras externas, enquanto as raízes são empregadas para dores abdominais e no tratamento da sarna. O objetivo desse trabalho foi avaliar a toxicidade aguda dos extratos etanólicos das folhas e raízes nas doses de 2000 e 5000 mg kg-1 em ratos e camundongos e a atividade cicatrizante das soluções aquosas contendo 2% desses extratos em feridas cutâneas em ratos. A contração das bordas das feridas foi avaliada por análises histológicas e morfométricas após 4, 7 e 14 dias de tratamento e por reação imunohistoquímica após 7 dias de tratamento. Os extratos etanólicos das folhas e raízes não apresentaram toxicidade na dose de 2000 mg kg-1 para ratos e camundongos e na dose de 5000 mg kg-1 para ratos. Nos camundongos, a dose de 5000 mg kg-1 dos extratos das folhas e raízes provocou alterações histológicas no fígado. Não foram observadas diferenças significativas na contração das feridas entre os grupos tratados com os extratos das folhas e das raízes e o controle após 4 e 7 dias de tratamento. Após 14 dias de tratamento, 50% dos animais tratados com o extrato das raízes apresentaram reepitelização total das feridas e reconstrução parcial dos anexos. A alantoína, isolada do extrato etanólico da raiz, pode ser considerada como um dos metabólitos secundários responsáveis pela aceleração da reepitelização.

Memora nodosa (Silva Manso) Miers is a Brazilian Cerrado species whose leaves and stems are commonly used to treat external wounds and ulcers and the roots are used for abdominal pain and to treat scabies. The purpose of this study was to evaluate the acute toxicity of ethanol extracts from the leaves and roots of M. nodosa at 2000 and 5000 mg kg-1 doses in rats and mice and to evaluate the healing activity of aqueous solutions containing 2% of these extracts on skin wounds in rats. The contraction of the wounds was evaluated by histological and morphometric analysis after 4, 7 and 14 days of treatment and by immunohistochemistry analysis after 7 days of treatment. The ethanol extracts of leaves and roots presented no toxicity at a 2000 mg kg-1 dose for rats and mice, and at a 5000 mg kg-1 dose for rats. Histological changes in the liver of mice were verified with a 5000 mg kg-1 dose of the leaf and root extracts. Macroscopic and histological differences were not observed in the contraction of wounds between the groups treated with leaf and root extracts and the control group after 4 and 7 days of treatment. After 14 days of treatment, 50% of the animals treated with the root extract presented total re-epithelialization of wounds and partial reconstruction of the annexes. Allantoin, isolated from the root ethanol extract, can be considered one of the secondary metabolites responsible for accelerating re-epithelialization.

Four cases of toxic liver injury associated with Dictamnus dasycarpus / 대한간학회지

We report four cases of toxic hepatitis that occurred after taking a decoction made by boiling down the root of Dictamnus dasycarpus. The four patients had a median age of 60 years, common symptoms of jaundice and general weakness, and stated that they had not consumed alcohol for at least 5 years. The markers of hepatitis A, B, and C were all negative in the patients. Abdominal ultrasonography revealed common bile ducts with normal diameters. Two of the cases were a mother and daughter, and the other two were sporadic. All of them had consumed a decoction made by boiling down the root of Dictamnus dasycarpus five or six times daily until several days before admission. Dictamnus dasycarpus induced liver injury presenting with a benign course lasting less than 1 month after cessation of the causative agent. We suggest that this natural product can cause acute hepatitis in rural areas.

Valores de DL50 em peixes e no rato tratados com pó de raízes de Derris spp e suas implicações ecotoxicológicas / LD50 in fish and rat produced by powdered roots of Derris spp and ecotoxicological implications

Os "timbós verdadeiros" (plantas do gênero Derris), originários da Amazônia Brasileira, tem demonstrado importância crescente por produzirem uma classe de compostos flavonoídicos relacionados à rotenona, que possuem atividade tóxica para peixes e mamíferos. Neste estudo foi determinado a dose letal 50% (DL50) do extrato alcoólico do pó de Derris spp para três espécies de peixes filogeneticamente diferentes e um mamífero roedor (rato). As DL50 de 2,6 microgramas/ml para Collosoma macropomum (tambaqui), 4,8 microgramas/ml para Oreochromis niloticus (tilápia), 14,2 microgramas/ml para Plecostomus sp (cascudo) e DL50 de 100,0 mg/kg para Rattus norvegicus (rato) denotam acentuadas diferenças entre os valores de DL50, principalmente entre os peixes e o rato. Isto possivelmente é devido a fatores farmaco-cinéticos que se relacionam com as diferentes barreiras teciduais encontradas pelos rotenóides quando administrados pela via oral em mamíferos