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Guaco, a native and perennial Brazilian liana, is one of the medicinal plants most widely commercialized in the Brazilian market. The major bioactive compounds in guaco leaves are coumarin and o-coumaric acid, along with kaurene-type diterpenes. Two Mikania species, M. laevigata and M. glomerata, are both treated as guaco in the Brazilian pharmacopeia and are commercialized indiscriminately, although they can be distinguished by the shape of the leaves and by the characteristic coumarin aroma of M. laevigata. We used DNA barcoding, chromosome counting and chemical analysis to study guaco germplasm accessions from collections in 10 Brazilian states. ETS and ITS sequences failed to distinguish most guaco accessions identified as M. glomerata and M. laevigata regardless of geographical origin, suggesting that M. glomerata and M. laevigata are recently diverged species. The chromosome number 2n = 36 was observed in all guaco accessions. In guaco accessions grown under experimental conditions, two chemical phenotypes were found: phenotype G-I, containing moderate coumarin content (644–755 mg/100 g) and high levels of kaurenoic acid (771–881 mg/100 g) and phenotype G-II, containing high levels of coumarin (1123–1309 mg/100 g) and low levels of kaurenoic acid (160–334 mg/100 g). None of the M. glomerata accessions produced coumarin in satisfactory levels (all

Introduction: The traditional antimalarial tea Artemisia annua, indicated for centuries in China to treat fevers, is again arousing interest for the treatment of malaria due to improvements attained in the plant composition by a few Institutions throughout the world, including the State University of Campinas (UNICAMP), Brazil, increasing its principal component by more than 100 times as from standard varieties, giving 1% in artemisinin and an expressive biomass yield such as 2 tons of dried leaves/hectare. Clinical trials carried out with this material in African countries have proven its therapeutic potential for a new generation of Artemisia tea in the treatment of falciparum malaria. In addition to artemisinin, recent studies have identified and quantified other compounds present in the crude extract and characterized their contributions to the anti-malarial efficacy, including their action against chloroquine-resistant strains. The majority of the clinical trials carried out with Artemisia tea in African countries have shown that the control of the parasitaemia is efficient in the initial treatment period, but few trials have followed the patients up to the 28th day. This first clinical trial carried out in Brazil with the A. annua infusion, after toxicological trials that defined the safety of this form of medication. Methods: The therapeutic efficacy of the tea was measured in patients with falciparum malaria over 28 days, comparing it with the current first-line treatment namely artemether-lumefantrine (Coartem?). The trial was carried out in controlled groups according to official protocol approved by the National Ethics in Research Committee (CONEP: 77/ 2011) and a rigorous control of the 17 patients with non-serious cases of falciparum malaria, recruited in the following three municipalities of the State of Para, Brazil: Tucurui, Goianesia do Para and Anajas. The tea group received the infusion prepared in the proportion of 1.25 g of dry leaves of the variety CPQBA with 1% artemisinin for 250 mL of just boiled water, taken every 6 hours for 7 days, giving a total of approximately 175 mg of artemisinin, whilst the artemether-lumefantrine (Coartem?) group received a total of 525 mg of artemisinin equivalent to artemether. Results: The parasitaemia by the tea treatment became negative in the first days, even though it was administered with a dose that was one third of the recommended dose of artemisinin. However, as in the case artemisinin or artesunate monotherapies, 57.1% of the patients treated with the A. annua tea presented type I resistance, with a return of the parasitaemia around the 14th or 21st day. The other patients in the tea group showed type II/III resistance without manifestation of any serious signs or symptoms. In these cases, according to the protocol, the patients were redirected for treatment with artemether-lumefantrin (Coartem?) with subsequent negativity of the parisitaemia. Discussion: The fact that the efficacy of the tea with 1/3 of the dose of artemisinin was similar to that of the full dose of this medication infers that other compounds present in the crude extract, probably flavonoids, had contributed to the negativity of the parasitaemia at the start of the treatment. Considering that the positive control group, where the compound derived from artemisinin (artemether) was associated with another antimalarial agent (lumefantrine), presented excellent efficacy throughout the entire control of the cure, future trials with the A. annua tea should use the same strategy of association with another antimalarial agent, preferably from A. annua itself, in order to extend its therapeutic action during the whole control period. The Artemisia annua tea in the form standardized and used in this research, should not substitute the most efficient treatment, but could be considered as an emergency therapeutic resource in the first hours of symptoms as a function of its availability, anti-inflammatory action and lack of side effects. Other regimes and standardizations deserve investigation, mainly those with a high content of arteannuin B, as occurs in the initial cultivation phase.

Purpose To develop an anesthetic mucoadhesive film containing Acmella oleracea (jambu) extract for topical use on oral mucosa. Methods Ethanolic extracts from aerial parts of jambu were prepared by maceration. Pigment removal was obtained by adsorption with activated carbon. Three mucoadhesive films were developed using a film casting method: 10 or 20% of crude jambu extract (10% JB and 20% JB), and 10% of crude jambu extract treated with activated carbon (10% JBC). The mucoadhesive films were characterized regarding their uniformity, thickness, pH, and spilanthol content, and their stability was evaluated during 120 days. Gas chromatography was used to quantify the amount of spilanthol. In vitro tests determined the permeation of spilanthol across pig esophageal epithelium mucosa in Franz diffusion cells. Topical anesthetic efficacy was assessed in vivo using a tail flick test in mice. Results The three mucoadhesive films showed physical stability and visual appearances suitable for use on oral mucosa. The permeation study revealed that the spilanthol from 10% JBC presented higher flux and permeability coefficient values, compared to 10% or 20% JB (p < 0.001). Moreover, 10% JBC showed better topical anesthetic efficacy than the other films (p < 0.01). Conclusion Mucoadhesive film containing crude extract of jambu treated with activated carbon is a potential alternative for oral, topical use, encouraging future clinical studies.

Despite numerous studies with the Piper genus, there are no previous results reporting in vitro or in vivo Piper regnellii (Miq.) C. DC. var. regnellii anticancer activity. The aim of this study was to investigate P. regnellii in vitro and in vivo anticancer activity and further identify its active compounds. In vitro antiproliferative activity was evaluated in 8 human cancer cell lines: melanoma (UACC-62), breast (MCF7), kidney (786-0), lung (NCI-H460), prostate (PC-3), ovary (OVCAR-3), colon (HT29), and leukemia (K-562). Total growth inhibition (TGI) values were chosen to measure antiproliferative activity. Among the cell lines evaluated, eupomatenoid-5 demonstrated better in vitro antiproliferative activity towards prostate, ovary, kidney, and breast cancer cell lines. In vivo studies were carried out with Ehrlich solid tumor on Balb/C mice treated with 100, 300, and 1000 mg/kg of P. regnellii leaves dichloromethane crude extract (DCE), with 30 and 100 mg/kg of the active fraction (FRB), and with 30 mg/kg of eupomatenoid-5. The i. p. administration of DCE, FRB, and eupomatenoid-5 significantly inhibited tumor progression in comparison to control mice (saline). Therefore, this study showed that neolignans of Piper regnellii have promising anticancer activity. Further studies will be undertaken to determine the mechanism of action and toxicity of these compounds.

Made available in DSpace on 2018-11-26T17:06:36Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-01-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) The Brazilian forests have one of the world's biggest biodiversities. Achyrocline satureioides (macela) and Acmella oleracea (jambu) are native species from Brazil with a huge therapeutic potential, with proved anti-inflammatory and anesthetic action, respectively. The jambu's crude extract after depigmentation with activated charcoal and macela's essential oil were incorporated in a film made with hydroxyethyl cellulose. Those films were evaluated by mechanical test using a texturometer and anti-inflammatory and anesthetic activities by in vivo tests: wound healing and antinociceptive. The film containing the highest concentration of depigmented jambu's extract and macela's essential oil obtained an anesthesia time of 83.6 (+/- 28.5) min longer when compared with the positive control EMLA (R); the same occurred with the wound healing test; the film containing the highest concentration had a higherwound contraction (62.0%+/- 12.1) compared to the positive control allantoin and the histopathological analysis demonstrated that it increases collagen synthesis and epidermal thickening. The results demonstrate that the films have a potential use in skin wounds, pressure sore, and infected surgical wounds treatment. Univ Estadual Campinas, Chem Biol & Agr Res Ctr CPQBA, Campinas, SP, Brazil Univ Estadual Campinas, Dept Biochem & Tissue Biol, Biol Inst, Campinas, SP, Brazil Sao Paulo State Univ, Inst Biosci, Dept Biol, Rio Claro, SP, Brazil Sao Paulo State Univ, Inst Biosci, Dept Biol, Rio Claro, SP, Brazil FAPESP: 2016/13776-5

Background Essential oils (EO) obtained from twenty medicinal and aromatic plants were evaluated for their antimicrobial activity against the oral pathogens Candida albicans, Fusobacterium nucleatum, Porphyromonas gingivalis, Streptococcus sanguis and Streptococcus mitis. Methods The antimicrobial activity of the EO was evaluates by microdilution method determining Minimal Inhibitory Concentration. Chemical analysis of the oils compounds was performed by Gas chromatography–mass spectrometry (CG-MS). The most active EO were also investigated as to their actions on the biolfilm formation. Results The most of the essential oils (EO) presented moderate to strong antimicrobial activity against the oral pathogens (MIC - Minimal Inhibitory Concentrations values between 0.007 and 1.00 mg/mL). The essential oil from Coriandrum sativum inhibited all oral species with MIC values from 0.007 to 0.250 mg/mL, and MBC/MFC (Minimal Bactericidal/Fungicidal Concentrations) from 0.015 to 0.500 mg/mL. On the other hand the essential oil of C. articulatus inhibited 63.96% of S. sanguis biofilm formation. Through Scanning Eletronic Microscopy (SEM) images no changes were observed in cell morphology, despite a decrease in biofilm formation and changes on biofilm structure. Chemical analysis by Gas Chromatography – Mass Spectrometry (GC-MS) of the C. sativum essential oil revealed major compounds derivatives from alcohols and aldehydes, while Cyperus articulatus and Aloysia gratissima (EOs) presented mono and sesquiterpenes. Conclusions In conclusion, the crude oil from C. articulatus exhibited the best results of antimicrobial activity e ability to control biofilm formation. The chemical analysis showed the presence of terpenes and monoterpenes such as a-pinene, a-bulnesene and copaene. The reduction of biofilms formation was confirmed from SEM images. The results of this research shows a great potential from the plants studied as new antimicrobial sources.

Arrabidaea chica (H&B) Verlot is a plant popularly known as Pariri and this species is a known source of anthocyanins, flavonoids and tannins. This report describes an approach involving enzymatic treatment prior to extraction procedures to enhance A chica crude extract anticancer activity. Anticancer activity in human cancer cell lines in vitro using a 48 h SRB cell viability assay was performed to determine growth inhibition and cytotoxic properties. The final extraction yield without enzyme treatment was higher (24.28%) compared to the enzyme-treated material (19.03%), with an enhanced aglycones anthocyanin ratio as determined by HPLC- DAD and LC-MS with direct infusion.

The cytotoxicity of the dichloromethane crude extract (DCE), obtained from the aerial parts of Pothomorphe umbellata (L.) Miq (Piperaceae), was evaluated against nine human cancer cell lines (MCF-7, NCI-ADR/RES, OVCAR-3, PC-3, HT-29, NCI-H460, 786-O, UACC-62, K-562). The DCE presented antiproliferative activity with good potency against all cell lines at low concentrations (between 4.0 and 9.5 microg/mL) and with selectivity (1.55 microg/mL) for the leukemia cell line (K-652). DCE (100, 200, 300 and 400 mg/kg, ip) was also evaluated in the Ehrlich ascites tumor model. Both the survival number and the life span of the animals that died increased by at least 45 and 50%, respectively (8 animals per group), demonstrating P. umbellata extract potential anticancer activity. The results of the in vivo antitumor activity prompted the fractionation of the crude extract. The crude extract was submitted to dry column chromatography with dichloromethane-methanol (99:1). The column effluent fractions were extracted with methanol, dried under vacuum yielding fractions FR1 (less polar), FR2 (medium polarity), and FR3 (polar), which were analyzed for their growth inhibition or cytotoxic properties by a 48-h sulforhodamine B cell viability assay by measuring the total protein content. FR1 demonstrated high potency and cytotoxicity, a result compatible with the high toxicity of oxalic acid; FR2, containing 4-nerolidylcathecol, presented the lowest cytotoxic activity compared to the other two fractions but with selectivity for prostate cancer cell line; FR3, containing a mixture of steroids described in the literature as possessing various biological activities, also presented potent anticancer in vitro activity. These results suggest that P. umbellata DCE in vivo antitumor activity may be a consequence of the activity of different active principles.

Essential oils obtained from leaves of 29 medicinal plants commonly used in Brazil were screened against 13 different Escherichia coli serotypes. The oils were obtained by water-distillation using a Clevenger-type system and their minimal inhibitory concentration (MIC) were determined by microdilution method. Essential oil from Cymbopogon martinii exhibited a broad inhibition spectrum, presenting strong activity (MIC between 100 and 500 microg/mL) against 10 out of 13 Escherichia coli serotypes: three enterotoxigenic, two enteropathogenic, three enteroinvasive and two shiga-toxin producers. C. winterianus inhibited strongly two enterotoxigenic, one enteropathogenic, one enteroinvasive and one shiga-toxin producer serotypes. Aloysia triphylla also shows good potential to kill Escherichia coli with moderate to strong inhibition. Other essential oils showed antimicrobial properties, however with a more restricted action against the serotypes studied. Chemical analysis of Cymbopogon martinii essential oil performed by gas chromatography (GC) and gas chromatography/mass spectrometry (GC-MS) showed the presence of compounds with known antimicrobial activity, including geraniol, geranyl acetate and trans-cariophyllene, which tested separately, indicated geraniol as antimicrobial active compound. The significant antibacterial activity of Cymbopogon martinii oil suggests that they could serve as a source for compounds with therapeutic potential.

Oral candidiasis is an opportunistic fungal infection of the oral cavity with increasingly worldwide prevalence and incidence rates. Novel specifically-targeted strategies to manage this ailment have been proposed using essential oils (EO) known to have antifungal properties. In this study, we aim to investigate the antifungal activity and mode of action of the EO from Coriandrum sativum L. (coriander) leaves on Candida spp. In addition, we detected the molecular targets affected in whole-genome expression in human cells. The EO phytochemical profile indicates monoterpenes and sesquiterpenes as major components, which are likely to negatively impact the viability of yeast cells. There seems to be a synergistic activity of the EO chemical compounds as their isolation into fractions led to a decreased antimicrobial effect. C. sativum EO may bind to membrane ergosterol, increasing ionic permeability and causing membrane damage leading to cell death, but it does not act on cell wall biosynthesis-related pathways. This mode of action is illustrated by photomicrographs showing disruption in biofilm integrity caused by the EO at varied concentrations. The EO also inhibited Candida biofilm adherence to a polystyrene substrate at low concentrations, and decreased the proteolytic activity of Candida albicans at minimum inhibitory concentration. Finally, the EO and its selected active fraction had low cytotoxicity on human cells, with putative mechanisms affecting gene expression in pathways involving chemokines and MAP-kinase (proliferation/apoptosis), as well as adhesion proteins. These findings highlight the potential antifungal activity of the EO from C. sativum leaves and suggest avenues for future translational toxicological research.