Epidemiological studies have revealed that a diet rich in plant-derived foods has a protective effect on human health. Identifying bioactive dietary constituents is an active area of scientific investigation that may lead to new drug discovery. Kaempferol (3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) is a flavonoid found in many edible plants (e.g. tea, broccoli, cabbage, kale, beans, endive, leek, tomato, strawberries and grapes) and in plants or botanical products commonly used in traditional medicine (e.g. Ginkgo biloba, Tilia spp, Equisetum spp, Moringa oleifera, Sophora japonica and propolis). Some epidemiological studies have found a positive association between the consumption of foods containing kaempferol and a reduced risk of developing several disorders such as cancer and cardiovascular diseases. Numerous preclinical studies have shown that kaempferol and some glycosides of kaempferol have a wide range of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial, anticancer, cardioprotective, neuroprotective, antidiabetic, anti-osteoporotic, estrogenic/antiestrogenic, anxiolytic, analgesic and antiallergic activities. In this article, the distribution of kaempferol in the plant kingdom and its pharmacological properties are reviewed. The pharmacokinetics (e.g. oral bioavailability, metabolism, plasma levels) and safety of kaempferol are also analyzed. This information may help understand the health benefits of kaempferol-containing plants and may contribute to develop this flavonoid as a possible agent for the prevention and treatment of some diseases.

A review on the dietary flavonoid kaempferol.

A review of anti-infective and anti-inflammatory chalcones.

Epidemiological evidence suggests that flavonoids may play an important role in the decreased risk of chronic diseases associated with a diet rich in plant-derived foods. Flavonoids are also common constituents of plants used in traditional medicine to treat a wide range of diseases. The purpose of this article is to summarize the distribution and biological activities of one of the most common flavonoids: luteolin. This flavonoid and its glycosides are widely distributed in the plant kingdom; they are present in many plant families and have been identified in Bryophyta, Pteridophyta, Pinophyta and Magnoliophyta. Dietary sources of luteolin include, for instance, carrots, peppers, celery, olive oil, peppermint, thyme, rosemary and oregano. Preclinical studies have shown that this flavone possesses a variety of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial and anticancer activities. The ability of luteolin to inhibit angiogenesis, to induce apoptosis, to prevent carcinogenesis in animal models, to reduce tumor growth in vivo and to sensitize tumor cells to the cytotoxic effects of some anticancer drugs suggests that this flavonoid has cancer chemopreventive and chemotherapeutic potential. Modulation of ROS levels, inhibition of topoisomerases I and II, reduction of NF-kappaB and AP-1 activity, stabilization of p53, and inhibition of PI3K, STAT3, IGF1R and HER2 are possible mechanisms involved in the biological activities of luteolin.

Distribution and biological activities of the flavonoid luteolin.

Alkaloids mimicking the structures of monosaccharides are now believed to be widespread in plants and microorganisms, and these sugar mimics inhibit glycosidases because of a structural resemblance to the sugar moiety of the natural substrate. Naturally occurring sugar mimics with a nitrogen in the ring are classified into five structural classes: polyhydroxylated piperidines, pyrrolidines, indolizidines, pyrrolizidines and nortropanes. Glycosidases are involved in a wide range of important biological processes, such as intestinal digestion, post-translational processing of glycoproteins and the lysosomal catabolism of glycoconjugates. The realization that alkaloidal sugar mimics might have enormous therapeutic potential in many diseases such as viral infection, cancer and diabetes has led to increasing interest and demand for these compounds. Most of these effects can be shown to result from the direct or indirect inhibition of glycosidases. The glycosphingolipid (GSL) storage diseases are relatively rare hereditary disorders that are severe in nature and frequently fatal. Possible strategies for the treatment of these lysosomal storage diseases include enzyme replacement therapy, gene therapy and substrate deprivation. Recently, quite a new therapy for lysosomal storage diseases has been reported, namely a ‘chemical chaperone therapy’ for Fabry disease. In this report, the structural basis for the specificity of inhibition of alkaloidal sugar mimics and their current and potential application to biomedical problems will be reviewed.

Sugar-mimic glycosidase inhibitors: natural occurrence, biological activity and prospects for therapeutic application

Plant phenolics: recent advances on their biosynthesis, genetics, and ecophysiology.

Chemo-evolutionary polarizations in the Lamiiflorae

The present study discusses the evolutionary status of Moraceae, from the perspective of chemical features of phenolic micromolecules. A chemosystematics analysis points to affinities between genera and tribe belonging to the Moraceae family, by correlation of the protection parameters of micromolecule hydroxyls resulting from the mixed pathway (acetate/shikimate) and the shikimate pathway. The phenylpropanoid and aromatic polyketide hydroxyl groups are mainly protected by prenylation and methylation mechanisms. A chemometric analysis (grouping and factor analyses) was used to evaluate the evolutionary relationships of the Moraceae genera and tribe, and it was possible to establish taxonomic relationships for the systematic characterization of the Moraceae family through the chemosystematic data. The results of the chemosystematic study suggest evidence that the Trilepisium genus is inadequately classified in the Dorstenia tribe and that the Streblus genus does not belong to the Moreae tribe. In addition, this chemosystematic study confirms the advanced status of Moraceae and legitimization of intrafamiliar classification.

Chemosystematic Aspects of the Moraceae Family: Phenylpropanoids and Aromatic Polyketides

The chemical composition of essential oils isolated by hydrodistillation from ripe fruits and leaves of Pourouma cecropiifolia Martius, Pourouma mollis Trecul and Pourouma velutina Martius ex Miguel was determined by GC and GC/MS. From ripe fruits of P. cecropiifolici Martius, 24 compounds were identified, accounting for 73.8% of the oil. Oxygenated monoterpenes were found to be an important group of constituents with linalool (3.1%) predominating. A new monoterpene, 2-methoxγ-1,7,7-trimethylbicyclo[2.2.1]hept-2-ene (2-methoxybornylene), was tentatively identified by mass spectrometry. In addition, 29, 37 and 26 constituents were identified in the leaf oils of P. cecropiifolia, P. mollis and P. velutina, respectively. Aliphatic alcohols, aldehydes and esters (C3-C9) were quantitatively the most significant components. (Z)-3-Hexenol was clearly the dominant product occurring in contents of 26.7%, 22.3% and 3.2%, respectively. The major sesquiterpene hydrocarbons in the analyzed oils were β-caryoph...

Essential Oil Composition of Brazilian Pourouma Species

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"Sapium glandulatum Complex" (Euphorbiaceae)

Stifftia chrysantha J.C. Mikan e uma planta pertencente a familia Asteraceae cujo principal uso pela populacao e o ornamental e atualmente se encontra sob risco moderado de extincao. E sabido que a planta foi utilizada no tratamento de afeccoes respiratorias por quilombolas. O objetivo deste estudo foi investigar o potencial efeito antimicrobiano de diferentes extratos de S. chrysantha contra algumas especies de micobacterias e formas promastigotas de duas especies de Leishmania. Os testes foram realizados in vitro utilizando MTT ou Resazurina em metodos colorimetricos, de acordo com o microrganismo avaliado. Os resultados mostraram baixa atividade dos extratos contra as culturas de micobacterias. Por outro lado, um efeito inibidor do crescimento foi observado noextrato metanolico das folhas e no extrato hexânico da casca contra as culturas de promastigotas de L. amazonensis (CI50 = 55,16 mg/mL extrato metanolico and 38,61 mg/mL extrato hexânico) and L. chagasi (CI50 = 72,05 mg/mL extrato hexânico). Novos estudos sao necessarios para descobrir as substâncias responsaveis pela inibicao do crescimento das formas promastigotas.Evaluation of in vitro antileishmanial and antimycobacterial activities of Stifftia chrysantha J.C. Mikan extractsStifftia chrysantha J.C. Mikan is a plant that belongs to Asteraceae family, mainly used for ornamental purposes and it is moderately endangered to die out nowadays. It is known this plant has been used on the treatment of respiratory affections by quilombo communities (Brazilian hinterland settlement founded by people of African origin). The aim of this study was to investigate the potential antimicrobial effect of different extracts from S. chrysantha against some species of mycobacterias and promastigote forms of two Leishmania sp. In vitro assays were performed using colorimetric methods with  3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide or Resazurin, according to the microorganism evaluated. The results showed low activity of extracts against mycobacterial cultures. On the other hand, a growth inhibitory effect was observed in the methanol extract from leaves and on the hexane extract from bark against promastigote culture of L. amazonensis (IC50 = 55.16 mg/mL methanol extract and 38.61mg/mL hexane extract) and L. chagasi (IC50 = 72.05 mg/mL hexane extract). New studies are necessary to discover the substances that were responsible for the growth inhibition of promastigote forms.

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Maria Auxiliadora Coelho Kaplan

Papers

Chemo-evolutionary polarizations in the Lamiiflorae

Chemosystematic Aspects of the Moraceae Family: Phenylpropanoids and Aromatic Polyketides

Essential Oil Composition of Brazilian Pourouma Species

"Sapium glandulatum Complex" (Euphorbiaceae)

Evaluation of in vitro antileishmanial and antimycobacterial activities of Stifftia chrysantha J.C. Mikan extracts