Danielle T.M. Costa

Bio: Danielle T.M. Costa is an academic researcher from Universidade Federal de Santa Catarina. The author has contributed to research in topics: Aristolochia. The author has an hindex of 1, co-authored 2 publications receiving 21 citations.

Chromenes from leaves of Calea pinnatifida and evaluation of their leishmanicidal activity

Abstract: Calea pinnatifida (R. Br.) Less., Asteraceae, is popularly known as “quebra-tudo”, “cipo-cruz” or “aruca”. This species is used in the folk medicine for the treatment of stomach pain, giardiasis and amoebiasis. The aim of this study was to isolate and identify chromenes from leaves of C. pinnatifida and evaluate their leishmanicidal activity. A fraction from leaves of C. pinnatifida was analyzed for their chemical constituents, resulting in the isolation and characterization of four known chromenes: 6-acetyl-7-hydroxy-2,2-dimethylchromene (1), 6-acetyl-7-methoxy-2,2-dimethylchromene (2), 6-(1-hydroxyethyl)-7-methoxy-2,2-dimethylchromene (3) and 6-(1-ethoxyethyl)-7-methoxy-2,2-dimethylchromene (4). Structure identification of isolated compounds involved analysis of spectral data of 1D and 2D-NMR. The isolated compounds are here reported for the first time in C. pinnatifida, and the chromenes 1 and 3 show a moderate leishmanicidal activity.

Chemical Constituents and Pharmacology properties of Aristolochia triangularis: a south brazilian highly-consumed botanical with multiple bioactivities.

Abstract: Aristolochia triangularis Cham., is one of the most frequently used medicinal plant in Southern Brazil. Preparations containing the leaves and/or stems are traditionally used as anti-inflammatory, diuretic, as well as antidote against snakebites. This study screened A. triangularis extracts, fractions and isolated compounds for different bioactivities. A weak antiproliferative activity against human lung cancer cell line (A549) was observed only for chloroform fraction obtained from stems (CFstems - CC50: 2.93 µg/mL). Also, a moderate antimicrobial activity against Staphylococcus aureus was detected just for chloroform fraction obtained from leaves (CFleaves -13-16 mm inhibition zone). Additionally, two semi-purified fractions (CFstems-4 and CFleaves-4) selectively inhibited HSV-1 replication (IC50 values of 0.40 and 2.61 µg/mL, respectively), while only CFleaves showed promising results against Leishmania amazonensis. Fractionation of extracts resulted in the isolation of one neolignan (-) cubebin and one lignan (+) galbacin. However, these compounds are not responsible for the in vitro bioactivities herein detected. The presence of aristolochic acid I and aristolochic acid II in the crude ethanol extract of stems (CEEstems) and leaves (CEEleaves) was also investigated. The HPLC analysis of these extracts did not display any peak with retention time or UV spectra comparable to aristolochic acids I and II.

Identification and characterization of antibacterial compound(s) of cockroaches (Periplaneta americana)

Abstract: Infectious diseases remain a significant threat to human health, contributing to more than 17 million deaths, annually. With the worsening trends of drug resistance, there is a need for newer and more powerful antimicrobial agents. We hypothesized that animals living in polluted environments are potential sources of antimicrobials. Under polluted milieus, organisms such as cockroaches encounter different types of microbes, including superbugs. Such creatures survive the onslaught of superbugs and are able to ward off disease by producing antimicrobial substances. Here, we characterized antibacterial properties in extracts of various body organs of cockroaches (Periplaneta americana) and showed potent antibacterial activity in crude brain extract against methicillin-resistant Staphylococcus aureus and neuropathogenic Escherichia coli K1. The size-exclusion spin columns revealed that the active compound(s) are less than 10 kDa in molecular mass. Using cytotoxicity assays, it was observed that pre-treatment of bacteria with lysates inhibited bacteria-mediated host cell cytotoxicity. Using spectra obtained with LC-MS on Agilent 1290 infinity liquid chromatograph, coupled with an Agilent 6460 triple quadruple mass spectrometer, tissues lysates were analysed. Among hundreds of compounds, only a few homologous compounds were identified that contained the isoquinoline group, chromene derivatives, thiazine groups, imidazoles, pyrrole-containing analogs, sulfonamides, furanones, and flavanones and known to possess broad-spectrum antimicrobial properties and anti-inflammatory, anti-tumour, and analgesic properties. Further identification, characterization, and functional studies using individual compounds can act as a breakthrough in developing novel therapeutics against various pathogens including superbugs.

Asteraceae Plants as Sources of Compounds Against Leishmaniasis and Chagas Disease.

Abstract: Leishmaniasis and Chagas disease cause great impact on social and economic aspects of people living in developing countries. The treatments for these diseases are based on the same regimen for over 40 years, thus, there is an urgent need for the development of new drugs. In this scenario, Asteraceae plants (a family widely used in folk medicine worldwide) are emerging as an interesting source for new trypanocidal and leishmanicidal compounds. Herein, we provide a non-exhaustive review about the activity of plant-derived products from Asteraceae with inhibitory action toward Leishmania spp. and T. cruzi. Special attention was given to those studies aiming the isolation (or identification) of the bioactive compounds. Ferulic acid, rosmarinic acid, and ursolic acid (Baccharis uncinella DC.) were efficient to treat experimental leishmaniasis; while deoxymikanolide (Mikania micrantha) and (+)-15-hydroxy-labd-7-en-17-al (Aristeguietia glutinosa Lam.) showed in vivo anti-T. cruzi action. It is also important to highlight that several plant-derived products (compounds, essential oils) from Artemisia plants have shown high inhibitory potential against Leishmania spp., such as artemisinin and its derivatives. In summary, these compounds may help the development of new effective agents against these neglected diseases.

One-pot three-component protocol for the synthesis of indolyl-4H-chromene-3-carboxamides as antioxidant and antibacterial agents

Abstract: A series of newly synthesized 4-(1H-indol-3-yl)-2-methyl-N-phenyl-4H-chromene-3-carboxamide derivatives were achieved by one-pot reaction between salicylaldehydes, substituted acetoacetanilides, and indoles in methanol catalyzed by 1,4-diazabicyclo [2.2.2]octane (DABCO) (30 mol%) at room temperature. These chromene systems were constructed through Knoevenagel condensation followed by a nucleophilic substitution process. The valuable features of this protocol such as short reaction time, simple operational procedure, broad substrate scope, and high yield of products make it an efficient and promising synthetic strategy. For the first time, various substituted 4H-chromene-3-carboxamide derivatives using DABCO as a catalyst are reported. The synthesized compounds (4a–p) were evaluated in antioxidant and antibacterial studies. The derivatives 4c, 4d, 4k, 4l, and 4p showed good antioxidant activity. Among all the derivatives 4k, 4l, and 4p were found to be active against bacterial strains with MIC values ranging from 9.3 to 18.75 μg mL−1.

Previously undescribed antioxidative and anti-inflammatory chromenyls bearing 3H-isochromenone and furanyl-2H-chromenyl skeletons from the venerid clam, Paphia malabarica

Abstract: Previously undescribed chromenyl derivatives, characterized as 7-(2′-ethyl-1′-hydroxynonan-2′-yl)-6,7,8,8a-tetrahydro-3H-isochromen-1-(5H)-one (1) and 61-(3-((E)-31b-(furan-2′-yl)-prop-31b-en-31-yl)-4a,5,6,8a-tetrahydro-8-methyl-2H-chromen-6-yl)-ethyl-5′′-methyl-hexanoate (2) were isolated from ethyl acetate-methanol extract of yellow-foot bivalve clam, Paphia malabarica. Their structures have skeletons composed of isochromen-(5H)-one and furanyl-2H-chromenyl moieties, which are reported for the first time in marine organism. These were characterized by extensive one and two-dimensional nuclear magnetic resonance, infrared, and high-resolution mass spectroscopic experiments. The title compounds were evaluated for therapeutic potentials with regard to anti-inflammatory and antioxidant properties compared to known standards. These compounds exhibited comparable 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS+) radical scavenging activities with α-tocopherol (IC50 ~0.6–0.7 mg/mL). The significantly higher anti-5-lipoxygenase activity of the title compounds (IC50 0.76–0.82 mg/mL) than ibuprofen (IC50 0.93 mg/mL) indicated their potential anti-inflammatory properties. The selectivity indices (IC50 anti-cyclooxygenase-1/IC50anti-cyclooxygenase-2) of compounds 1 (1.19) and 2 (1.31) well established its safety profiles as an anti-inflammatory when compared to known drug, ibuprofen (0.44). The target bioactivities of chromenyl derivatives were guided by hydrophobic and electronic parameters. These compounds can be used as potential bioactive leads in functional food and medicinal applications.