Salacia impressifolia (Miers) A. C. Smith (family Celastraceae) is a traditional medicinal plant found in the Amazon Rainforest known as “miraruíra”, "cipó-miraruíra" or “panu” and is traditionally ...used to treat dengue, flu, inflammation, pain, diabetes, male impotency, renal affections, rheumatism and cancer. Aim of the study: The aim of this study was to investigate in vitro and in vivo anti-leukemia activity of the stem bark of S. impressifolia in experimental models. Materials and methods: The in vitro cytotoxic activity of extracts, fractions and quinonemethide triterpenes (22-hydroxytingenone, tingenone and pristimerin) from the stem bark of S. impressifolia in cultured cancer cells was determined. The in vivo antitumor activity of the ethyl acetate extract (EAE) and of its fraction (FEAE.3) from the stem bark of S. impressifolia was assessed in C.B-17 severe combined immunodeficient (SCID) mice engrafted with human promyelocytic leukemia HL-60 cells. Results: The extract EAE, its fraction FEAE.3, and quinonemethide triterpenes exhibited potent cytotoxicity against cancer cell lines, including in vitro anti-leukemia activity against HL-60 and K-562 cells. Moreover, extract EAE and its fraction FEAE.3 inhibited the in vivo development of HL-60 cells engrafted in C.B-17 SCID mice. Tumor mass inhibition rates were measured as 40.4% and 81.5% for the extract EAE (20 mg/kg) and for its fraction FEAE.3 (20 mg/kg), respectively. Conclusions: Ethyl acetate extract and its fraction from the stem bark of S. impressifolia exhibit in vitro and in vivo anti-leukemia activity that can be attributed to their quinonemethide triterpenes. These data confirm the ethnopharmacological use of this species and may contribute to the development of a novel anticancer herbal medicine.
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Context. Capella (α Aur) is one of the few binaries in the sky with two cool giant stars. With spectral types of G8III and G0III, the two components appear at different but distinct stages in their ...evolution. The G0 secondary star is a Hertzsprung-gap giant, and the G8 primary star is thought to be a clump giant. Aims. We present a new measure of the carbon 12C/13C isotope ratio of the primary component of Capella using high-resolution R ≈ 250 000 spectra obtained with the Potsdam Echelle Polarimetric and Spectroscopic Instrument (PEPSI) with both the Vatican Advanced Technology Telescope (VATT) and the Large Binocular Telescope (LBT). Methods. Signal-to-noise ratios of up to 2 700 were obtained by averaging nightly spectra. These average spectra were used to disentangle the two binary components. The isotope ratio was derived with the use of spectrum synthesis from the CN lines at 8004 Å. Results. We found that the 12C/13C ratio of the primary component of Capella is 17.8 ± 1.9. Our measurement precision is now primarily limited by the spectral-line data and by the grid-step size of the model atmospheres rather than the data. The separated spectrum of the secondary component does not show distinguishable 12CN and 13CN lines because of its vsini and higher temperature. Conclusions. Our new 12C/13C value is significantly lower than the previous value of 27 ± 4 but now agrees better with the recent model prediction of 18.8–20.7.
Acute myeloid leukemia (AML) is a very heterogeneous group of disorders with large differences in the percentage of immature blasts that presently are classified according to the specific mutations ...that trigger malignant proliferation among thousands of mutations reported thus far. It is an aggressive disease for which few targeted therapies are available and still has a high recurrence rate and low overall survival. The main reason for AML relapse is believed to be due to leukemic stem cells (LSCs) that have unlimited self-renewal capacity and long residence in a quiescent state, which promote greater resistance to traditional therapies for this cancer. AML LSCs have low oxidative stress levels, which appear to be caused by a combination of low mitochondrial activity and high activity of ROS-removing pathways. In this sense, oxidative stress has been thought to be an important new potential target for the treatment of AML patients, targeting the eradication of AML LSCs. The aim of this review is to discuss some drugs that induce oxidative stress to direct new goals for future research focusing on redox imbalance as an effective strategy to eliminate AML LSCs.
In this work, we describe a novel ruthenium-xanthoxylin complex, Ru(phen)
(xant)(PF
) (RXC), that can eliminate colorectal cancer (CRC) stem cells by targeting the chaperone Hsp90. RXC exhibits ...potent cytotoxicity in cancer cell lines and primary cancer cells, causing apoptosis in HCT116 CRC cells, as observed by cell morphology, YO-PRO-1/PI staining, internucleosomal DNA fragmentation, mitochondrial depolarization, and PARP cleavage (Asp214). Additionally, RXC can downregulate the HSP90AA1 and HSP90B1 genes and the expression of HSP90 protein, as well as the expression levels of its downstream/client elements Akt1, Akt (pS473), mTOR (pS2448), 4EBP1 (pT36/pT45), GSK-3β (pS9), and NF-κB p65 (pS529), implying that these molecular chaperones can be molecular targets for RXC. Moreover, this compound inhibited clonogenic survival, the percentage of the CRC stem cell subpopulation, and colonosphere formation, indicating that RXC can eliminate CRC stem cells. RXC reduced cell migration and invasion, decreased vimentin and increased E-cadherin expression, and induced an autophagic process that appeared to be cytoprotective, as autophagy inhibitors enhanced RXC-induced cell death. In vivo studies showed that RXC inhibits tumor progression and experimental metastasis in mice with CRC HCT116 cell xenografts. Taken together, these results highlight the potential of the ruthenium complex RXC in CRC therapy with the ability to eliminate CRC stem cells by targeting the chaperone Hsp90.
A steady supply of mineral raw materials is vital for the transition to a low-carbon, circular economy. The number of active mines in Europe has severely declined over the last century and half, ...giving rise to many abandoned mining waste sites and corresponding geological heritage. Also, the rise in minerals demand for large-scale deployment of renewable energy requires the continued and steady availability of key minerals. The supply risk associated with unpredicted geopolitical events needs to be eliminated/mitigated. Historical mine waste sites are the answer but evaluating mine waste is a lengthy and costly exercise. The study, undertaken in the Lousal Mine, used small unmanned aerial systems (sUASs) to model and determine mine waste volumes by generating orthomosaic maps with quick, inexpensive, and reliable results. Calculated mine waste volumes between 308,478 m3 and 322,455 m3 were obtained. XRD and p-XRF techniques determined the mineralogy and chemistry of waste, which varied from mineralization and host rocks with hydrothermal alteration and numerous neogenic sulphates (mostly gypsum, rhomboclase, ferricopiapite, coquimbite, and jarosite) related with supergene processes and weathering. The study shows the viability of using these sUASs to successfully model historical mine waste sites in an initial phase and for future monitoring programs.
Acute myeloid leukemia (AML) is the most lethal form of leukemia. Standard anti-AML treatment remains almost unchanged for decades. Tingenone (TG) and 22-hydroxytingenone (22-HTG) are quinonemethide ...triterpenes found in the Amazonian plant Salacia impressifolia (Celastraceae), with cytotoxic properties in different histological types of cancer cells. In the present work, we investigated the anti-AML action mechanism of TG and 22-HTG in the AML HL-60 cell line. Both compounds exhibited potent cytotoxicity in a panel of cancer cell lines. Mechanistic studies found that TG and 22-HTG reduced cell growth and caused the externalization of phosphatidylserine, the fragmentation of internucleosomal DNA and the loss of mitochondrial transmembrane potential in HL-60 cells. In addition, pre-incubation with Z-VAD(OMe)-FMK, a pan-caspase inhibitor, prevented TG- and 22-HTG-induced apoptosis, indicating cell death by apoptosis via a caspase-dependent pathway. The analysis of the RNA transcripts of several genes indicated the interruption of the cellular antioxidant system, including the downregulation of thioredoxin, as a target for TG and 22-HTG. The application of N-acetyl-cysteine, an antioxidant, completely prevented apoptosis induced by TG and 22-HTG, indicating activation of the apoptosis pathway mediated by oxidative stress. Moreover, TG and 22-HTG induced DNA double-strand break and phosphorylation of JNK2 (T183/Y185) and p38α (T180/Y182), and co-incubation with SP 600125 (JNK/SAPK inhibitor) and PD 169316 (p38 MAPK inhibitor) partially prevented apoptosis induced by TG and 22-HTG. Together, these data indicate that TG and 22-HTG are new candidate for anti-AML therapy targeting thioredoxin.
•TG and 22-HTG induce caspase-mediated apoptotic cell death.•TG and 22-HTG target oxidative stress through downregulation of thioredoxin.•TG and 22-HTG cause DNA damage.•TG and 22-HTG cause JNK/p38-mediated apoptosis.
Agricultural expansion as a main human activity has affected pollinator's habitat, causing spatial distribution changes. Meanwhile, pollinators still provide pollination service to improve crop ...production. However, their spatial response is unclear because of environmental changes. This study sought to estimate spatial distribution of crop production and pollinator's richness, which can provide insights as to how they interact with the environment. We acquired environmental variables from remote sensing images and used a stacked species distribution model to predict selected bee species richness and a crop simulation model to simulate and calculate soybean production at a regional scale in the Cerrado for the period 2000–2015. Then, we analyzed their potential relationship. The results showed that higher selected bee species richness and higher soybean production occurred in the southern Cerrado. From 2000/08 to 2008/15 period, the selected bee species richness significantly decreased in the western part of the state of Bahia, the state of Goiás, and the northern region of the state of Minas Gerais; while soybean production increased in the states of Mato Grosso, Goiás, Bahia, and Tocantins. Correlation results of selected bee species richness and soybean production showed that they do not follow a linear relationship during the study period. Our findings indicate that the modeling method we proposed is robust to estimate spatial distribution of bee species richness and soybean production in the Cerrado at the regional scale and that the environment has a stronger influence on selected bee species richness than on soybean production. Moreover, climate effects and agricultural expansion are the main factors that affect their spatial distribution and interaction. Finally, our methodology provides a novel spatial perspective to analyze the relationship between pollinator and agricultural expansion corresponding with the environment, but future work is needed to collect a more comprehensive data set to improve model results.
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•Estimate interaction among pollinator, crop production and environment during 2000–2015.•Stacked SDMs was used to predict spatial distribution of selected bee species richness.•Crop simulation model simulated soybean production and visualized their spatial distribution.•Higher selected bee species richness and higher soybean production are in the southern Cerrado.
Aiming to test the capacity of retention of carotenoids in tissues, Lophiosilurus alexandri juveniles were fed diets containing 0, 25, 50, 100, 200, and 400 mg/kg of synthetic astaxanthin for 62 ...days. The inclusion of astaxanthin did not result in significant differences in growth, weight gain, apparent feed conversion, and feed efficiency of the fish. Blood biochemistry and liver histology did not change with the different treatments. At the level of 100 mg/kg of inclusion, there were the highest levels of carotenoids in the blood, and muscle and the smallest difference between the muscle x integument ratio.
Cytotoxic Alkaloids from the Stem of Xylopia laevigata Menezes, Leociley R A; Costa, Cinara O D Sousa; Rodrigues, Ana Carolina B da C ...
Molecules (Basel, Switzerland),
07/2016, Letnik:
21, Številka:
7
Journal Article
Recenzirano
Odprti dostop
Xylopia laevigata (Annonaceae), known locally as "meiú" or "pindaíba", is widely used in folk medicine in Northeastern Brazil. In the present work, we performed phytochemical analyses of the stem of ...X. laevigata, which led to the isolation of 19 alkaloids: (-)-roemerine, (+)-anonaine, lanuginosine, (+)-glaucine, (+)-xylopine, oxoglaucine, (+)-norglaucine, asimilobine, (-)-xylopinine, (+)-norpurpureine, (+)-N-methyllaurotetanine, (+)-norpredicentrine, (+)-discretine, (+)-calycinine, (+)-laurotetanine, (+)-reticuline, (-)-corytenchine, (+)-discretamine and (+)-flavinantine. The in vitro cytotoxic activity toward the tumor cell lines B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), K562 (human chronic myelocytic leukemia) and HL-60 (human promyelocytic leukemia) and non-tumor peripheral blood mononuclear cells (PBMCs) was tested using the Alamar Blue assay. Lanuginosine, (+)-xylopine and (+)-norglaucine had the highest cytotoxic activity. Additionally, the pro-apoptotic effects of lanuginosine and (+)-xylopine were investigated in HepG2 cells using light and fluorescence microscopies and flow cytometry-based assays. Cell morphology consistent with apoptosis and a marked phosphatidylserine externalization were observed in lanuginosine- and (+)-xylopine-treated cells, suggesting induction of apoptotic cell death. In addition, (+)-xylopine treatment caused G₂/M cell cycle arrest in HepG2 cells. These data suggest that X. laevigata is a potential source for cytotoxic alkaloids.
Insects have a close relationship with the humanity, in both positive and negative ways. Mosquito borne diseases kill millions of people and insect pests consume and destroy around US $40 billion ...worth of food each year. In contrast, insects pollinate at least two-thirds of all the food consumed in the world. In order to control populations of disease vectors and agricultural pests, researchers in entomology have developed numerous methods including chemical, biological and mechanical approaches. However, without the knowledge of the exact location of the insects, the use of these techniques becomes costly and inefficient. We are developing a novel sensor as a tool to control disease vectors and agricultural pests. This sensor, which is built from inexpensive commodity electronics, captures insect flight information using laser light and classifies the insects according to their species. The use of machine learning techniques allows the sensor to automatically identify the species without human intervention. Finally, the sensor can provide real-time estimates of insect species with virtually no time gap between the insect identification and the delivery of population estimates. In this paper, we present our solution to the most important challenge to make this sensor practical: the creation of an accurate classification system. We show that, with the correct combination of feature extraction and machine learning techniques, we can achieve an accuracy of almost 90
%
in the task of identifying the correct insect species among nine species. Specifically, we show that we can achieve an accuracy of 95
%
in the task of correctly recognizing if a given event was generated by a disease vector mosquito.
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