Development and Evaluation of Vaginal Suppository Containing Althaea officinalis L. Polysaccharide Extract

Abstract Intrauterine adhesions cause several gynecological problems. Althaea officinalis L. roots known as marshmallows contain polysaccharides (M.P.) which possess anti-inflammatory and anti-ulcerogenic activities also can form a bio-adhesive layer on damaged epithelial membranes prompting healing processes. Vaginal formulations of herbal origin are commonly applied to relieve cervico-uterine inflammation. Herein, we aim to develop and evaluate vaginal suppositories containing polysaccharides isolated from the A. officinalis root. Six formulations (four P.E.G.-based and two lipid-based suppositories containing 25% and 50% M.P.) met standard requirements, which were then subjected to qualitative and quantitative evaluation. All suppositories exhibited acceptable weights, hardness, content uniformity, melting point, and disintegration time, which fall within the acceptable recommended limits. Higher concentrations of M.P. in PEG-bases moderately increased the hardness (p<0.05). PEG-formulations showed content uniformity>90% of the average content while it was 75-83% for suppocire formulations. All formulations disintegrated in<30minutes. In-vitro release test revealed that M.P. release from 25%-MP formulations was higher than that of 50%-M.P. suppositories. Overall, results revealed the feasibility of preparing P.E.G.-or lipid-based suppositories containing M.P., which met the B.P. quality requirement

A network pharmacology approach to assess Reno-protective and -curative effects of methanolic extract of Malva neglecta Wallr in gentamicin induced renal toxicity rat model

Abstract The aim of present study was to explore protective and curative effects of Malve neglecta on kidneys. In silco study with network pharmacology was performed to find out potential target organs, genes and cellular cell lines which confirmed kidneys as target organ of phyto-constituents present in Malva neglecta extract. Gentamicin (40 mg/kg, i.p) was given to induce renal toxicity. Prophylactic study was performed with 300-, 600- and 900 mg/kg doses to find out nephro-protective and -curative effects and curative potential was evaluated at 900 mg/kg dose. Renal function biomarkers, blood urea, BUN, serum creatinine and uric acid, and oxidative stress measuring biomarkers, SOD, CAT, GSH and MDA levels in kidney homogenate were quantified at the end of study. Treatment groups showed decrease in blood urea, BUN, serum creatinine and uric acid levels dose dependently and curative group also showed decline in these biomarkers. SOD, CAT, GSH levels were increased and MDA level decreased in treatment groups significantly as compared to toxic control which revealed the role of oxidative stress in renal damage and anti-oxidant power of MN. Data suggested that use of MN along with drugs causing renal toxicity may prove beneficial due to its nephro- protective and curative effects.

Stomatal size, ploidy and polyembryony in Eriotheca Stellate Trichome Species Complex (Bombacoideae - Malvaceae) in the Cerrados of Brazil.

Geographic parthenogenesis, range expansion of apomictic plants after climate changes, has been described for Northern Hemisphere gametophytic apomicts. But similar trends have been observed for sporophytic apomicts of Cerrado, the savannas in Brazil. Eriotheca pubescens is a common Cerrado tree, an agamic complex of either hexaploid/polyembryonic apomicts or tetraploid/monoembryonic sexual individuals. Some populations have been described as a new species, Eriotheca estevesiae, all included in the Eriotheca Stellate Trichome Species Complex (ESTSC). Since breeding systems and ploidy are clearly associated with polyembryony and stomatal size, we used these ancillary features to map the reproductive and ploidy level traits of E. pubescens and E. estevesiae. Leaves and seeds were collected from individuals of 19 populations. Seeds were evaluated for the presence of polyembryony and leaves for stomatal measurements. Eight populations were monoembryonic while another eight were polyembryonic and for other three, the embryonic pattern was not readily verified. E. pubescens polyembryonic and hexaploid populations formed a homogeneous group, but monoembryonic plants were more variable. E. estevesiae populations were monoembryonic with smaller stomata. In contrast, some E. pubescens monoembryonic populations further south presented larger stomata. Despite these outliers, possibly mixed populations, stomatal size and embryonic pattern differed from northern to southern populations. Embryonic pattern and stomatal size indicated that northernmost populations of Eriotheca STSC (E. estevesiae) are diploid and sexual. Southernmost populations, mostly polyembryonic and with large stomata, are hexaploid and apomictic. This is in agreement with geographic parthenogenesis and range expansion of apomictic lineages to southern habitats available after the last glacial maximum.

Ameliorating effect of Malva Neglecta on hyperglycemia and hyperlipidemia in diabetic rats

The plant, Malva neglecta wallr., is widely consumed for medicinal and nutritional purposes. The current study was carried out to assess the hypoglycemic and antihyperlipidemic potential of aqueous methanolic extract of M. neglecta. Chemical evaluation of the extract was performed by high pressure liquid chromatography. Oral glucose tolerance test (OGTT) was done in diabetic rats pre-exposed to 250, 500 and 750 mg/kg plant extract via the oral route. For hypoglycemic and biochemical study, the same therapy was administered to alloxan induced diabetic rats for 14 days. The standard control group received Glibenclamide (5 mg/kg). Ferulic acid, p-coumaric acid and other phenolic acids were detected and estimated in the extract. Administration of the plant extract significantly reduced blood glucose level in diabetic rats subjected to OGTT. The plant extract lowered the fasting blood glucose and alpha amylase, and prevented the damage to pancreas. It also corrected dyslipidemia in diabetic animals following 14 days therapy. Hence, this experimental study establishes the fact that M. neglecta exhibited significant antidiabetic and antihyperlipidemic activities in alloxan induced diabetic rats.

Complete chloroplast genomes of three important species, Abelmoschus moschatus, A. manihot and A. sagittifolius: Genome structures, mutational hotspots, comparative and phylogenetic analysis in Malvaceae.

Abelmoschus is an economically and phylogenetically valuable genus in the family Malvaceae. Owing to coexistence of wild and cultivated form and interspecific hybridization, this genus is controversial in systematics and taxonomy and requires detailed investigation. Here, we present whole chloroplast genome sequences and annotation of three important species: A. moschatus, A. manihot and A. sagittifolius, and compared with A. esculentus published previously. These chloroplast genome sequences ranged from 163121 bp to 163453 bp in length and contained 132 genes with 87 protein-coding genes, 37 transfer RNA and 8 ribosomal RNA genes. Comparative analyses revealed that amino acid frequency and codon usage had similarity among four species, while the number of repeat sequences in A. esculentus were much lower than other three species. Six categories of simple sequence repeats (SSRs) were detected, but A. moschatus and A. manihot did not contain hexanucleotide SSRs. Single nucleotide polymorphisms (SNPs) of A/T, T/A and C/T were the largest number type, and the ratio of transition to transversion was from 0.37 to 0.55. Abelmoschus species showed relatively independent inverted-repeats (IR) boundary traits with different boundary genes compared with the other related Malvaceae species. The intergenic spacer regions had more polymorphic than protein-coding regions and intronic regions, and thirty mutational hotpots (≥200 bp) were identified in Abelmoschus, such as start-psbA, atpB-rbcL, petD-exon2-rpoA, clpP-intron1 and clpP-exon2.These mutational hotpots could be used as polymorphic markers to resolve taxonomic discrepancies and biogeographical origin in genus Abelmoschus. Moreover, phylogenetic analysis of 33 Malvaceae species indicated that they were well divided into six subfamilies, and genus Abelmoschus was a well-supported clade within genus Hibiscus.

Nuclear phylogeography of the temperate tree species Chiranthodendron pentadactylon (Malvaceae): Quaternary relicts in Mesoamerican cloud forests.

BACKGROUND: The Mexican hand tree or Canac (Chiranthodendron pentadactylon) is a temperate tree species of cloud and pine-oak forests of southern Mexico and Guatemala. Its characteristic hand-shaped flower is used in folk medicine and has constituted the iconic symbol of the Sociedad Botánica de México since 1940. Here, the evolutionary history of this species was estimated through phylogeographic analyses of nuclear DNA sequences obtained through restriction site associated DNA sequencing and ecological niche modeling. Total genomic DNA was extracted from leaf samples obtained from a representative number (5 to 10 per sampling site) of individuals distributed along the species geographic range. In Mexico, population is comprised by spatially isolated individuals which may follow the trends of cloud forest fragmentation. By contrast, in Guatemala Chiranthodendron may constitute a canopy dominant species near the Acatenango volcano. The distributional range of this species encompasses geographic provinces separated by the Isthmus of Tehuantepec. The objectives of the study were to: (i) estimate its genetic structure to define whether the observed range disjunction exerted by the Isthmus of Tehuantepec translates into separate populations, (ii) link population divergence timing and demographic trends to historical climate change, and (iii) test hypotheses related to Pleistocene refugia. RESULTS: Patterns of genetic diversity indicated high levels of genetic differentiation between populations separated by the Isthmus. The western and eastern population diverged approximately 0.873 Million years ago (Ma). Demographic analyses supported a simultaneous split from an ancestral population and rapid expansion from a small stock approximately 0.2 Ma corresponding to a glacial period. The populations have remained stable since the LIG (130 Kilo years ago (Ka)). Species distribution modelling (SDM) predicted a decrease in potential distribution in the Last Interglacial (LIG) and an increase during the Last Glacial Maximum (LGM) (22 Ka), Mid-Holocene (6 Ka) and present times. CONCLUSIONS: Divergence time estimations support the hypothesis that populations represent Quaternary relict elements of a species with broader and northernmost distribution. Pleistocene climatic shifts exerted major influence on the distribution of populations allowing dispersion during episodes of suitable climatic conditions and structuring during the first interglacial with a time period length of 100 Kilo years (Kyr) and the vicariant influence of the Isthmus. Limited demographic expansion and population connectivity during the LGM supports the moist forest hypothesis model.

MaGenDB: a functional genomics hub for Malvaceae plants.

Malvaceae is a family of flowering plants containing many economically important plant species including cotton, cacao and durian. Recently, the genomes of several Malvaceae species have been decoded, and many omics data were generated for individual species. However, no integrative database of multiple species, enabling users to jointly compare and analyse relevant data, is available for Malvaceae. Thus, we developed a user-friendly database named MaGenDB (http://magen.whu.edu.cn) as a functional genomics hub for the plant community. We collected the genomes of 13 Malvaceae species, and comprehensively annotated genes from different perspectives including functional RNA/protein element, gene ontology, KEGG orthology, and gene family. We processed 374 sets of diverse omics data with the ENCODE pipelines and integrated them into a customised genome browser, and designed multiple dynamic charts to present gene/RNA/protein-level knowledge such as dynamic expression profiles and functional elements. We also implemented a smart search system for efficiently mining genes. In addition, we constructed a functional comparison system to help comparative analysis between genes on multiple features in one species or across closely related species. This database and associated tools will allow users to quickly retrieve large-scale functional information for biological discovery.

[New records of medicinal plants in Tibet].

By the fourth survey of Chinese medicinal resources, new medicinal plants records of 2 genera and 5 species were reported in Tibet. They are two genera Rhynchoglossum and Asteropyrum, and five species including Rh. obliquum, A. peltatum, Urena repanda, Schefflera khasiana and Mimulus tenellus. All the voucher specimens are preserved in Herbarium of Tibet Agriculture and Animal Husbandry University.

Modificações estruturais e reológicas em chocolate amargo devido à alteração do tipo de gordura utilizada / Structural and rheological changes in bitter chocolate due to the change in the type of fat used

O chocolate é conhecido mundialmente, proveniente do fruto do cacaueiro (Theobroma cacao) normalmente consumido em forma de barra, mas também podendo ser usado de inúmeras formas como coberturas, recheios dentre outras. Um importante componente na produção do chocolate é a gordura utilizada, uma vez que esta é responsável pela textura, brilho e características organolépticas do produto. O objetivo deste trabalho foi utilizar a manteiga de cupuaçu (proveniente do fruto da Theobroma grandiflorum) na elaboração de chocolate amargo. Para tanto a manteiga de cacau foi substituída de forma parcial e total. Foram desenvolvidas duas formulações de chocolate padrão com liquor de cacau (P1) e com cacau em pó (P2), e quatro formulações com substituição parcial da manteiga de cacau por manteiga de cupuaçu a partir de P2(F1 e F2) e de P1 (F3 e F4). As amostras elaboradas e os ingredientes (líquor de cacau, cacau em pó, manteiga de cacau e manteiga de cupuaçu) foram avaliadas por análise térmica (DSC-Differential Scanning Calorimetry), reologia, tamanho de partícula, composição em ácidos graxos e em triacilgliceróis, índice de temperagem e índice de resfriamento, bem como testes de acompanhamento de 112 dias como cor, atividade de água e textura. A manteiga de cupuaçu apresentou maior quantidade de ácido oleico quando comparada com a manteiga de cacau, aproximadamente 11,5%, e também características reológicas diferentes dos padrões: tensões iniciais variaram de 3,4 ± 0,3 a 7,9 ± 2,0 Pa para as amostras e 2,9 ± 1,4 a 6,2 ± 0,7 Pa para os padrões; viscosidade de 1,6 ± 0,1 a 2,9 ± 0,4 Pa*s para as amostras e 1,9 ± 0,8 a 2,9 ± 0,9 Pa*s para os padrões; tamanho de partícula das amostras de 21 ± 2 a 22 ± 2 µm, padrões de 20 ± 2 a 34 ± 4 µm. Durante os 112 dias de estudo de prateleira: Aw variou de 0,405 ± 0,03 a 0,424 ± 0,02 nas amostras e 0,399 ± 0,03 no padrão; textura variou de 16,3 ± 1,2 a 31,6 ± 2,0 N para as amostras e 25,9 ± 3,0 a 28,6 ± 7,2 N para os padrões; WI variou de 24,1 ± 0,6 a 25,4 ± 0,3 para as amostras e 23,0 ± 0,4 a 23,9 ± 0,8 para os padrões; ΔE variou de 0,4 a 2,2 para as amostras e de 0,5 a 1,2 para os padrões. Concluiu-se que: A variação do líquor de cacau para cacau em pó acarretou aumentando do tempo total de processo em aproximadamente 15 min. Os chocolates com maior teor de manteiga de cupuaçu apresentaram aumento em triacilglicerol C54, com redução de POP e POS. A faixa de fusão dos chocolates com maiores porcentagens de manteiga de cupuaçu (F3 e F4) foi maior do que para chocolates formulados apenas com manteiga de cacau (P1 e P2). A manteiga de cupuaçu tem relação direta com a queda da tensão inicial e da viscosidade (sem diferença significativa, p<0,05) nos chocolates produzidos. O baixo ponto de fusão do ácido oleico contido na manteiga de cupuaçu alterou a temperatura final e o valor do índice de temperagem nas amostras com maior teor de manteiga de cupuaçu (F3 e F4)

The chocolate is known worldwide, coming from the fruit of the cacao (Theobroma cacao) normally consumed in the form of a bar, but also can be used in countless ways like coverings, fillings among others. An important component in the production of chocolate is the fat used, since it is responsible for the texture, brightness and organoleptic characteristics of the product. The objective of this work was to use cupuassu butter (from the fruit of Theobroma grandiflorum) in elaboration of bitter chocolate. For this purpose, the cocoa butter was partially and totally replaced. Two formulations of standard chocolate with cocoa liquor (P1) and with cocoa powder (P2) were developed, and four formulations with partial replacement of cocoa butter by cupuassu butter from P2 (F1 and F2) and P1 (F3 and F4). The elaborated samples and the ingredients (cocoa liquor, cocoa powder, cocoa butter and cupuassu butter) were evaluated by DSC, rheology, particle size, fatty acid composition and triacylglycerol, temperature index and cooling index, as well as follow-up tests of 112 days such as color, water activity and texture. The cupuassu butter presented a higher amount of oleic acid when compared to cocoa butter, approximately 11.5%, and also different rheological characteristics of the standards: initial tensions ranged from 3.4 ± 0.3 to 7.9 ± 2, 0 Pa for the samples and 2.9 ± 1.4 to 6.2 ± 0.7 Pa for the standards; viscosity of 1.6 ± 0.1 to 2.9 ± 0.4 Pa*s for the samples and 1.9 ± 0.8 to 2.9 ± 0.9 Pa*s for the standards; sample particle size from 21 ± 2 to 22 ± 2 µm, patterns from 20 ± 2 to 34 ± 4 µm. During the 112 days of shelf study: Aw ranged from 0.405 ± 0.03 to 0.424 ± 0.02 in the samples and 0.399 ± 0.03 in the standard; texture ranged from 16.3 ± 1.2 to 31.6 ± 2.0 N for the samples and 25.9 ± 3.0 to 28.6 ± 7.2 N for the standards; WI ranged from 24.1 ± 0.6 to 25.4 ± 0.3 for the samples and 23.0 ± 0.4 to 23.9 ± 0.8 for the standards; ΔE ranged from 0.4 to 2.2 for the samples and from 0.5 to 1.2 for the standards. It was concluded that: The variation of cocoa liquor to cocoa powder increased the total process time by approximately 15 min. The chocolates with higher content of cupuassu butter presented increase in triacylglycerol C54, with reduction of POP and POS. The melting range of chocolates with higher percentages of cupuassu butter (F3 and F4) was higher than for chocolates formulated with cocoa butter alone (P1 and P2). Cupuassu butter is directly related to the drop in initial tension and viscosity (without significant difference, p <0.05) in the chocolates produced. The low melting point of the oleic acid contained in the cupuassu butter altered the final temperature and the temperature index value in the samples with the highest cupuassu butter content (F3 and F4)

Preliminary in vitro assessment of the potential toxicity and antioxidant activity of Ceiba speciosa (A. St.-Hill) Ravenna (Paineira)

ABSTRACT The bark tea of Ceiba speciosa, a tropical tree of the Malvaceae family, is used in the Northwestern Region of Rio Grande do Sul state, Brazil, to reduce blood cholesterol levels. However, there are no scientific data on the efficacy and safety of this plant. The aim of the present study was to evaluate the in vitro antioxidant and toxic potential of bark extracts of C. speciosa. We performed a preliminary phytochemical analysis by high-performance liquid chromatography-diode array detection (HPLC-DAD) and evaluated the oxidative damage to proteins and lipids, the radical scavenging effect, and genotoxicity of the lyophilized aqueous extract (LAECs) and the precipitate obtained from the raw ethanol extract (Cs1). The phytochemical profile demonstrated the presence of phenolic and flavonoid compounds. The LAECs and Cs1 prevented damage to lipids and proteins at concentrations of 50 and 10 µg/mL. They also showed a scavenging effect on 2,2-diphenyl-1-pricril-hydrazyl (DPPH) radicals in a concentration-dependent manner. Furthermore, no genotoxic effect was observed at concentrations of 10, 5 and 2 µg/mL in the Comet assay. The present study is the first evaluation regarding the characterization of C. speciosa and its safety, and the results demonstrate its antioxidant potential and suggest that its therapeutic use may be relatively safe.

Revisiting the phylogeny of Bombacoideae (Malvaceae): Novel relationships, morphologically cohesive clades, and a new tribal classification based on multilocus phylogenetic analyses.

Bombacoideae (Malvaceae) is a clade of deciduous trees with a marked dominance in many forests, especially in the Neotropics. The historical lack of a well-resolved phylogenetic framework for Bombacoideae hinders studies in this ecologically important group. We reexamined phylogenetic relationships in this clade based on a matrix of 6465 nuclear (ETS, ITS) and plastid (matK, trnL-trnF, trnS-trnG) DNA characters. We used maximum parsimony, maximum likelihood, and Bayesian inference to infer relationships among 108 species (∼70% of the total number of known species). We analyzed the evolution of selected morphological traits: trunk or branch prickles, calyx shape, endocarp type, seed shape, and seed number per fruit, using ML reconstructions of their ancestral states to identify possible synapomorphies for major clades. Novel phylogenetic relationships emerged from our analyses, including three major lineages marked by fruit or seed traits: the winged-seed clade (Bernoullia, Gyranthera, and Huberodendron), the spongy endocarp clade (Adansonia, Aguiaria, Catostemma, Cavanillesia, and Scleronema), and the Kapok clade (Bombax, Ceiba, Eriotheca, Neobuchia, Pachira, Pseudobombax, Rhodognaphalon, and Spirotheca). The Kapok clade, the most diverse lineage of the subfamily, includes sister relationships (i) between Pseudobombax and "Pochota fendleri" a historically incertae sedis taxon, and (ii) between the Paleotropical genera Bombax and Rhodognaphalon, implying just two bombacoid dispersals to the Old World, the other one involving Adansonia. This new phylogenetic framework offers new insights and a promising avenue for further evolutionary studies. In view of this information, we present a new tribal classification of the subfamily, accompanied by an identification key.

Efeito dos compostos fenólicos do camu-camu e do cupuaçu no desenvolvimento da obesidade e diabetes mellitus tipo 2 / Effects of camu camu and cupuassu phenolic compounds on obesity and type 2 diabetes mellitus development

A incidência da obesidade e do diabetes do tipo 2 tomou proporções epidêmicas nos últimos anos, atingindo bilhões de indivíduos em todo o mundo. A descoberta de formas inovadoras capazes de reduzir as alterações metabólicas associadas a estas doenças é fundamental para minimizar o seu impacto na qualidade de vida da população e na economia dos países. Muitos estudos têm demonstrado que os compostos bioativos de alimentos possuem efeitos benéficos à saúde. O camu-camu e o cupuaçu são frutas nativas da região amazônica com potencial agroeconômico ainda inexplorado, que contêm um grande número de compostos fitoquímicos que podem atuar sobre o metabolismo corporal. Desta forma, o objetivo deste estudo foi verificar os efeitos dos compostos fenólicos de extratos do camu-camu e do cupuaçu no desenvolvimento da obesidade e do diabetes tipo 2 em ensaios in vivo e in vitro, e identificar os possíveis metabólitos envolvidos nestes efeitos. Os extratos ricos em compostos fenólicos da polpa comercial destes frutos foram extraídos em fase sólida, caracterizados por cromatografia líquida de alta eficiência (CLAE/DAD) e avaliados quanto à inibição da atividade de enzimas digestivas in vitro. Os extratos obtidos foram então testados em duas diferentes concentrações (2,25 e 4,5 mg de equivalentes de catequina/Kg de peso corporal para o cupuaçu; 7 e 14 mg de equivalentes de ácido gálico/Kg de peso corporal para o camu camu) em um modelo animal de obesidade e resistência insulínica induzida por dieta com alto teor de lipídios e sacarose em camundongos C57BL/6J. Foram investigados os efeitos destes compostos sobre as homeostases glicídica e lipídica através de análises séricas, testes de tolerância à insulina e à glicose e conteúdo de lipídios hepáticos e fecais. O extrato do camu camu apresentou flavonóis, ácido elágico e elagitaninos em sua composição. A suplementação com o extrato de compostos fenólicos do camu camu reduziu o ganho de peso corporal e diminuiu a intolerância à glicose e à insulina, independente da dose administrada. No entanto, a administração destes extratos não apresentou efeitos sobre o metabolismo lipídico. Estes resultados foram associados a um possível efeito de saciedade, com consequente redução da ingestão da dieta e da glicolipotoxicidade, e com um efeito anti-inflamatório devido à diminuição dos níveis de proteína C reativa. Já o extrato de cupuaçu apresentou flavanóis, flavonas e proantocianidinas em sua composição. A suplementação com o extrato de cupuaçu na maior dose testada melhorou a homeostase da glicose e principalmente dos lipídios, protegendo o tecido hepático dos danos causados pela dieta com alto teor de lipídios e sacarose. Estes efeitos foram associados à inibição de enzimas digestivas, com consequente menor absorção de lipídios provenientes da dieta, reduzindo assim a resistência à insulina no fígado, a hiperglicemia e a dislipidemia. Ainda, foi avaliada a distribuição de metabólitos no trato gastrointestinal de camundongos após a administração aguda do extrato de cupuaçu. Foi possível identificar a complexa mistura de polifenóis presentes no extrato de cupuaçu ao longo do trato gastrointestinal, que posteriormente foi metabolizada pela microbiota. Entre os metabólitos encontrados estão as agliconas hipolaetina e isoscutelareína, e os metabolitos microbianos da epicatequina como o 3,4-diHPP-2-ol e a 5-(3,4-dihidroxiphenil)-γ-valerolactona. De acordo com estes resultados, as diferenças na composição de compostos fenólicos encontradas entre os extratos das duas frutas foram responsáveis pelos diferentes resultados nos protocolos in vivo e a identificação dos metabólitos microbianos possibilita o conhecimento dos compostos possivelmente implicados nos efeitos benéficos. Novos estudos podem contribuir para um melhor entendimento dos mecanismos, bem como quais metabólitos estão associados aos efeitos benéficos que os compostos presentes nestas duas frutas apresentaram neste estudo

The incidence of obesity and type 2 diabetes reached epidemic proportions in recent years, arriving to billions of people around the world. The discovery of innovative ways that can reduce the metabolic abnormalities associated with these diseases is essential to minimize its impact on the population's quality of life and the economy of the countries. Many studies have demonstrated that food bioactive compounds have beneficial health effects. Camu-camu and cupuassu are native fruits of the Amazon region with unexplored agroeconomic potential, which contain a large number of phytochemical compounds that can act on body metabolism. Thus, the objective of this study was verify the effects of phenolic compounds of camu-camu and cupuassu extracts on the development of obesity and type 2 diabetes in vivo and in vitro, and identfy the possible metabolites involved in these effects. The phenolic compound-rich extracts were obtained from commercial frozen fruit pulps by solid phase extraction, characterized by high-performance liquid chromatography (HPLC/DAD) and evaluated for inhibition of digestive enzymes activities in vitro. Then, the extracts were tested at two different doses (2.25 and 4.5 mg catechin equivalents/kg body weight for cupuassu; 7 and 14 mg of gallic acid equivalents/kg body weight for camu camu) in an animal model (C57BL/6J mice) of obesity and insulin resistance induced by high fat high sucrose diet. The effects of extract supplementation on glucose and lipid homeostasis were assessed by serum analysis, insulin and glucose tolerance tests in mice, and contents of fat in liver and fecal samples. Camu camu extract presented flavonols, ellagic acid and ellagitannins in its composition. Supplementation with camu camu phenolic extract reduced weight gain and decreased glucose and insulin intolerance independent of the dose administered. However, no effects on lipid metabolism were found. These findings were associated with a possible effect of satiety with a consequent reduction in energy intake and glicolipotoxicity, and anti-inflammatory properties. Cupuassu extract presented flavanols, flavones and proanthocyanidins in its composition. Supplementation with cupuacu extract at the highest dose improved glucose homeostasis and plasmatic lipid levels, protecting the liver tissue from damage caused by diet rich in lipids and sucrose. These effects were associated with inhibition of digestive enzymes, with consequent lower absorption of lipids from the diet, thereby reducing the insulin resistance in the liver, the hyperglycemia and dyslipidemia. Furthermore, the distribution of metabolites in the gastrointestinal tract of mice was evaluated after acute administration of cupussu extract by HPLC-ESI-QTOF. We identified the complex mixture of polyphenols present in cupuassu extract along the gastrointestinal tract, which was subsequently metabolized by the intestinal microbiota. Among detected metabolites are hypolaetin and isoscutellarein aglycones and microbial metabolites of epicatechin as 3,4-diHPP-2-ol and 5-(3,4-dihydroxyphenyl)-γvalerolactone. According to these results, the differences in the composition of phenolic compounds found between the two fruit extracts were responsible for the different effects in vivo and identification of microbial metabolites enables the knowledge of the compounds potentially implicated in the beneficial effects. New studies can contribute to a better understanding of the metabolism and mechanisms of action

Atividades antinociceptiva e antiinflamatória do extrato etanólico de Luehea divaricata / Antinociceptive and anti-inflammatory activities of Luehea divaricate ethanol extract

RESUMO Considerando os diferentes usos etnofarmacológicos apresentados pela planta Luehea divaricata, realizou-se este estudo com o objetivo de avaliar as atividades antinociceptiva e antinflamatória do extrato etanólico de suas folhas, em modelo animal, nas dosagens de 20, 40, 80 e 160 mg/Kg, por via oral. Foram realizados os seguintes testes: contorções abdominais induzidas pelo acido acético, placa quente, formalina e edema de pata induzido por carragenina. Foram utilizados camundongos Swiss (20-25 g) para os três primeiros testes e ratos Wistar (180-250 g), para o último, divididos em seis grupos de oito animais, totalizando 48 animais em cada parâmetro de avaliação. Os resultados foram analisados estatisticamente pela análise de variância a 5% de probabilidade, para verificar quais os tratamentos que diferiram entre si, e estes foram submetidos aos testes de Kruskall-Wallis e Student-Newman-Keuls. O extrato etanólico das folhas de L. divaricata (EEtOH-Ld), nas diferentes doses estudadas, apresentou significativa atividade antinociceptiva sobre a dor induzida quimicamente por injeções intraperitoneal de acido acético e intraplantar de formalina. Na dosagem de 160 mg/Kg, esse extrato apresentou ação analgésica central, aos 120 minutos de observação, no teste de placa quente e reduziu o edema de pata induzido pela administração de carragenina, uma hora após a administração do agente inflamatório, semelhante ao efeito produzido pelo fármaco padrão.

ABSTRACT Considering the different ethnopharmacological uses submitted by the plant Luehea divaricata, this study took place in order to evaluate the antinociceptive and anti-inflammatory activities of the ethanol extract of the leaves in an animal model, the dosages of 20, 40, 80 and 160 mg/kg by oral intake. The following tests were performed: writhing induced by acetic acid, hot plate, formalin, and paw edema induced by carrageenan. Swiss mice (20-25 g) were used for the first three tests and Wistar rats (180-250 g) for the last, divided into six groups, each of eight animals, totaling 48 animals for each assessment parameter. The results were statistically analyzed by analysis of variance at 5% probability to verify which treatments differ, and these were tested by Kruskal-Wallis and Student-Newman-Keuls. The ethanol extract of L. divaricataleaves (EEtOH-Ld) at the different studied doses showed significant antinociceptive activity on chemically induced pain by intraperitoneal injections of acetic acid and intraplantar formalin. At a dosage of 160 mg/kg, this extract showed a central analgesic action after 120 minutes of observation in the hot plate test and reduced action in the paw edema induced by carrageenan one hour after the administration of the inflammatory agent, similar to the effect produced by the standard drug.

Phytoconstituents from Sidastrum micranthum (A. St.-Hil.) Fryxell (Malvaceae) and antimicrobial activity of pheophytin a

abstract Sidastrum micranthum (A. St.-Hil.) Fryxell, a member of the Malvaceae family, is called malva preta in Brazil. As this species is commonly used to treat bronchitis, cough, and asthma, better knowledge of its chemical compounds is important. The phytochemical study of its hexane extract, using chromatographic techniques, led to isolation of six compounds: the triterpene isoarborinol, a mixture of sitosterol and stigmasterol, sitosterol-3-O-β-D-glucopyranoside, pheophytin a, and 132-hydroxy-(132-S)-pheophytin a. Structural identification of these compounds was carried out using spectroscopic methods such as IR and 1D and 2D NMR (HOMOCOSY, HMQC, HMBC, and NOESY). Compounds isolated from S. micranthum were screened for their in vitro antifungal and antibacterial activity against twenty fungal and bacterial standard strains. Pheophytin a exhibited antimicrobial action against all microorganisms tested.

resumo Sidastrum micranthum (A. St.-Hil.) Fryxell, pertencente à família Malvaceae, é conhecida no Brasil como "malva preta". A espécie é popularmente usada contra bronquite, tosse e asma, mostrando a relevância de conhecer melhor sua composição química. O estudo fitoquímico do extrato hexânico da espécie, utilizando técnicas cromatográficas, conduziu ao isolamento de seis compostos: o triterpeno isoarborinol, mistura de sitosterol e estigmasterol, sitosterol-3-O-β-D-glicopiranosídeo, feofitina a e de 132-hidroxi-(132-S)-feofitina a. A identificação estrutural destes compostos foi realizada com base em métodos espectroscópicos, tais como IV, RMN 1D e 2D (HOMOCOSY, HMQC, HMBC e NOESY). As substâncias isoladas de Sidastrum micranthum foram avaliadas quanto às suas atividades antimicrobianas in vitro, contra vinte cepas fúngicas e bacterianas. A feofitina a mostrou ação antimicrobiana contra todos os microrganismos testados.

Farmacologia e fitoquímica de extratos e formulações de Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. e Piper umbellatum L / Pharmacology and phytochemistry of extracts and formulations from Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. and Piper umbellatum L

Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. e Piper umbellatum L. são plantas nativas do Brasil, presentes no estado de São Paulo, com relatos de uso popular para atividade antiúlcera. Este trabalho teve como objetivo avaliar a atividade antiúlcera de J. caroba, J. decurrens e formulações de nanocápsulas contendo P. umbellatum. Também pretendeu-se caracterizar a fitoquímica de tais formulações e extratos. Adicionalmente, foi avaliada a toxicidade aguda e subaguda de J. caroba. Os extratos de Jacaranda apresentaram compostos fenólicos em seus perfis cromatográficos obtidos por CCD e CLAE, característicos para cada espécie. Os diferentes extratos de J. caroba variaram sua composição química conforme a procedência e idade da planta. As espécies J. decurrens e J. caroba de três diferentes regiões não apresentaram ação antiúlcera aguda em ratos em modelo de indução por etanol acidificado, embora o extrato e as frações de J. caroba apresentaram potencial atividade anti Helicobacter pylori, com CIM variando entre 125 e 1.000 µg/mL. O extrato de J. caroba não promoveu sintomas de toxicidade aguda e subaguda em ratos. A DL50 observada foi maior que 5.000 mg/kg. Não foram relatadas alterações significativas na aparência macroscópica e peso dos órgãos, porém houve indicação de atividade mutagênica em teste de Ames na linhagem TA98 de S. typhimurium, o qual apresentou uma tendência dose-resposta para concentrações entre 7,5 e 15,0 mg/placa após ativação metabólica (S9). A formulação de nanocápsulas de poli-ε- caprolactona com extrato de P. umbellatum apresentou partículas com diâmetro médio de 181,6 ± 0,9 nm e potencial zeta de -31 ± 4 mV. Através de análise por CLAE observou-se maior eficiência de encapsulamento para a porção mais apolar da fração, enquanto que os compostos mais polares ficaram dispersos no meio. As nanocápsulas poliméricas apresentaram atividade gastroprotetora mesmo sem a adição de ativos e tiveram sua atividade aumentada pela fração clorofórmica de P. umbellatum

Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. and Piper umbellatum L. are native plants in Brazil, present in the state of São Paulo, with popular usage reports for anti-ulcer activity. This study aimed to evaluate the anti-ulcer activity of J. caroba, J. decurrens and nanocapsules formulations containing P. umbellatum. Also, we intended to characterize the phytochemistry of such formulations and extracts. Additionally, we evaluated the acute and subacute toxicity of J. caroba. Extracts from Jacaranda presented phenolic compounds in their chromatographic profiles obtained by TLC and HPLC, with variations between species. Samples of J. caroba extracts showed different chemical composition according to the origin and age of the plant. The species J. decurrens and J. caroba from three different regions showed no acute anti-ulcer action when tested in rats by acidified ethanol induction model. However, extract and fractions from J. caroba showed potential anti Helicobacter pylori activity, with MIC ranging from 125 and 1,000 ug/mL. J. caroba extract did not cause symptoms of acute and subacute toxicity in rats. The DL50 was determined above 5,000 mg/kg. Also, there were no significant changes to the macroscopic appearance of organs or changes in their weights. Meanwhile, an indication of mutagenic activity was observed in the Ames test. The TA98 strain of S. typhimurium, showed a tendency of dose-response for concentrations between 7.5 and 15.0 mg/plate after metabolic activation (S9). The nanocapsules formulation of poly-ε-caprolactone containing P. umbellatum extract had an average particle diameter of 181.6 ± 0.9 nm and zeta potential of -31 ± 4 mV. HPLC analysis showed better entrapping efficiency for the more apolar portion of the fraction, while the more polar compounds were dispersed in the medium. The polymeric nanocapsules showed gastroprotective activity even without the addition of active molecules and had their activity increased by chloroform fraction of P. umbellatum

Atividade gastroprotetora do extrato etanólico de Pavonia alnifolia A. St. -Hil / Gastro protective activity of the Pavonia alnifolia A.St. -Hil. extract

RESUMO No Brasil, a família Malvaceae está representada por aproximadamente 200 espécies e algumas foram descritas como gastroproteroras. Pavonia alnifolia A.St.-Hil. (Malvaceae) foi selecionada após uma abordagem quimiossistemática, considerando-se sua potencial capacidade em prevenir lesões gástricas. Assim, a atividade gastroprotetora do extrato etanólico de caules de P. alnifolia foi avaliada utilizando o modelo de indução aguda da lesão gástrica por etanol acidificado em camundongos. Além disso, foram quantificados o teor de flavonóides, pelo método de cloreto de alumínio, e de polifenóis, pelo método Folin-Ciocalteu, uma vez que a relação desses componentes com a proteção gástrica foi evidenciada. Os ensaios apontaram redução acentuada das lesões gástricas em camundongos tratados com o extrato da planta em todas as doses ensaiadas (10, 100 e 300 mg/kg). Esse efeito pode estar relacionado com a presença de polifenóis, cujo teor encontrado foi 74,3 ± 7,5 µg equivalente de pirogalol/mg do material vegetal examinado e 82,7 ± 7,1 µg equivalente de pirogalol /mg da amostra no extrato preparado por percolação e teor de flavonoides totais, que por sua vez apresentou um resultado de 17,1 ± 1,4 µg/mg de extrato. O extrato apresentou proteção da mucosa gástrica e este efeito pode estar relacionado à presença dos polifenóis e flavonóides encontrados

ABSTRACT Gastro protective activity of the Pavonia alnifolia A.St.-Hil. extract. In Brazil, the Malvaceae family is represented by at about 200 species. Some of those species are known as gastro protective ones. The Pavonia alnifolia A.St.-Hil (Malvaceae) was selected after a chemosystematic approach. The gastro preventive activity of the ethanol extract of stems Pavonia alnifolia was evaluated through the use of the Ethanol:chlroridric acid model on mice. The quantification of the total flavonoids (aluminum chloride method) and total polyphenols (Folin-Ciocalteu method) was also performed since the relation of those components with gastric protection has been previously highlighted. The tests showed a significant reduction of the ulcer formation in the mice treated with the plant extract (10, 100 and 300 mg/kg). This effect may be related to the presence of polyphenols whose content was found to be 74.3 ± 7.5 µg/mg of vegetal material and 82.7 ± 7.1 µg/mg of crude extract and flavonoids, which in turn showed a content of 17.1 ± 1.4 µg/mg dry extract

On the relevance of molecular tools for taxonomic revision in Malvales, Malvaceae s.l., and Dombeyoideae.

In this article, we present an overview of changes to the taxonomy of Malvales. In traditional classifications, this order was variously circumscribed as including four main families (i.e., Malvaceae, Bombacaceae, Sterculiaceae, and Tiliaceae, also known now as "Core Malvales"), but major disagreements existed between different taxonomic treatments. Contributions from molecular data, new morpho-anatomical data, and progress in methodological approaches have recently led to a new broader concept of this order (namely, "expanded Malvales"). Now, expanded Malvales includes ten families (Neuradaceae, Thymelaeaceae, Sphaerosepalaceae, Bixaceae, Cistaceae, Sarcolaenaceae, Dipterocarpaceae, Cytinaceae, Muntingiaceae, Malvaceae s.l.) distributed among seven monophyletic lineages. All these families were previously considered to have malvalean affinities in some traditional treatments, except the holoparasitic and highly modified Cytinaceae. Although molecular evidence has clarified the Malvales taxonomy, the phylogenetic positions of Sarcolaenaceae, Thymelaeaceae, and Sphaerosepalaceae are still controversial and need new analyses focusing specifically on these families to assess their phylogenetic placement and their morphological evolution.In a phylogenetic context, molecular data combined with recent examination of morphological characters supported the hypothesis of a common origin of "core Malvales." However, these analyses also showed that the former families but Malvaceae s.s. were paraphyletic or polyphyletic. As a consequence, recent taxonomic treatments grouped taxa formerly included in "Core Malvales" in a broader concept of Malvaceae s.l. Additionally, the intrafamilial taxonomy has been deeply modified, and in its present circumscription, Malvaceae includes nine subfamilies (Grewioideae, Byttnerioideae, Sterculioideae, Dombeyoideae, Brownlowioideae, Tilioideae, Bombacoideae, Malvoideae, Helicteroideae) in two main lineages. Phylogenetic studies on subfamilial rearrangements have focused on the relationships between emblematic taxa such as Bombacoideae and Malvoideae (which form together the /Malvatheca lineage). However, our understanding of the phylogenetic relationships among and within taxa of the other subfamilies (e.g., Dombeyoideae, Tilioideae, and Sterculioideae) has not followed at the same pace. Despite recent investigations, the relationships between the subfamilies of Malvaceae s.l. remain controversial. As an example of these taxonomic issues, we review the systematic studies on Dombeyoideae, with special emphasis on taxa endemic to the Mascarene archipelago (Indian Ocean). Recent investigations have shown that several island endemic genera such as Trochetia, Ruizia, and Astiria (endemic to the Mascarenes) are nested within the mega-genus Dombeya. Consequently, the current taxonomy of this genus does not match the phylogeny and should be modified. Therefore, we propose three possible taxonomic schemes as part of an ongoing revision of the Mascarene Dombeyoideae. However, these taxonomic rearrangements should only be made after a broader study of the diversity in Madagascar and adjacent areas. This broader approach shall avoid possibly multiple and contradictory taxonomic revisions of restricted regions if they were each studied in isolation.

Genetic diversity in natural populations of Theobroma subincanum Mart. in the Brazilian Amazon.

The genus Theobroma, recently reclassified in the family Malvaceae, comprises some species with high economic potential, including the cupuí, Theobroma subincanum Mart., which has not yet been domesticated, and whose genetics and population structure are mostly unknown. This study aimed to assess the population structure and genetic diversity in natural populations of T. subincanum Mart., using inter-simple sequence repeat (ISSR) markers. A total of 59 individuals were sampled in three geographically separate populations, CFA, CMN, and CPT. Nei's genetic distance was estimated to characterize populations with the use of 13 polymorphic primers. The analysis of molecular variance revealed that the variability between populations (51.71%) was higher than that within populations (48.29%). Among the three populations, CPT showed the highest diversity index and percentage of polymorphism. The ISSR molecular markers were efficient and presented sufficient polymorphism to estimate genetic diversity in populations of T. subincanum Mart.

Chemical constituents from Glyphaea brevis and Monodora myristica: chemotaxonomic significance.

A chemical investigation of the Glyphaea brevis leaves and of the Monodora myristica fruits led to the identification of thirteen compounds, seven linear long-chain aliphatic compounds, 1, 2, 4, 6, and 9-11, three steroids, 3a, 3b, and 7, two triterpenes, 5a and 5b, and one polyol, 8. The compounds 2 and 8, previously mentioned in the literature, are here characterized by their complete (1)H- and (13)C-NMR assignments. This is the first report of a full NMR assignment for linear fatty acid esters of aliphatic primary alcohols and for meso-erythritol. Compound 5b and 8 were isolated for the first time from plant extracts of the Tiliaceae family, and compounds 9-11 from the Annonaceae plant family. Our results constitute the basis for further chemotaxonomic studies on the two species.

[Identification characters of leaf morphological and venation pattern of Abutilon indicum with its confused herb A. theophrasti].

OBJECTIVE: To study the identification characters of Abutilon indicum and its confused herb A. theophrasti and establish an identification method. METHOD: LMVP (leaf morphological-venation pattern for identification Chinese herbs), and QAERM (quantitatively analyze and evaluate reliability for the method of identification Chinese herbs) were applied for the study. RESULT: The main differences of the leaf of Abutilon indicum: leaf margin cilia short and not clear (75-200 microm), petiole top with long straight hairs (up to 1.0-1.2 cm), when the tertiary veins and intersecondary veins issue from the lower part of midrib, their angles of divergence usually were wide acute (65 degrees-80 degrees) and a few was about right angle (80 degrees-100 degrees). The main differences of the leaf of A. theophrasti: leaf margin cilia long and clear (200-500 microm), petiole top with short straight hairs (most 0.1-0.5 mm), when the tertiary veins and intersecondary veins issue from the lower part of midrib, their angles of divergence usually were about right angle (80 degrees-100 degrees) and a few was wide acute (65 degrees-80 degrees). With the mentioned three groups of key differences, the both plants could be successfully identified from each other. The accuracy of identification results (AC) was from 97.5% to 99.6%, the repeatability of identification results: agreement rate for observation (ARO) was 97.1% and Kappa value was 0.94. CONCLUSION: The established method is simple, rapid, economic and reliable.