The aim of this study was to determine, first, the chemical composition of
(Griseb) Moldenke essential oil, from leaves harvested in central Chile; and second, its antioxidant and cytotoxic activity. ...Eight compounds were identified via gas chromatography-mass spectrometry (GC-MS) analyses, with the most representative being
-carvone (91.03%),
-limonene (4.10%), and dihydrocarvone (1.07%). For
essential oil, antioxidant assays (2,2-diphenyl-1-picrylhydrazyl (DPPH), H
O
, ferric reducing antioxidant power (FRAP), and total reactive antioxidant potential (TRAP)) showed good antioxidant activity compared to commercial antioxidant controls; and anti-proliferative assays against three human cancer cell lines (colon, HT-29; prostate, PC-3; and breast, MCF-7) determined an IC
of 5.85, 6.74, and 9.53 µg/mL, and selectivity indices of 4.75, 4.12, and 2.92 for HT-29, PC-3, and MCF-7, respectively. We also report on assays with CCD 841 CoN (colon epithelial). Overall, results from this study may represent, in the near future, developments for natural-based cancer treatments.
This work reports on the development of an efficient and ecofriendly ultrasound assisted method for the high yield synthesis (70.0–94.0%) of eighteen oxyalkylated derivatives of ...2′,4′-dihydroxychalcone. Synthesized compounds were subjected to in vitro biological assays against HT-29 (colorectal), MCF-7 (breast), and PC-3 (prostate) human tumor cell lines, these cell lines are among the ten most aggressive malignancies diagnosed in the world. Cytotoxicity evaluations showed that four of the synthesized compounds exhibited moderate to very high toxic activity against MCF-7 (IC50 = 8.4–34.3 μM) and PC-3 (IC50 = 9.3–29.4 μM) – comparable to 5-fluorouracil (IC50 16.4–22.3 μM). The same compounds only showed moderate activity against HT-29 (IC50 15.3–36.3 μM), closer to daunorubicin (IC50 15.1 μM). Next, although selectivity index (SI) of compounds was weak, compound 18 exhibited a remarkable and selective cytotoxic activity (5.8–10.57) against cancer cells. Outside of these, most compounds significantly reduced cell survival, increased reactive oxygen species (ROS) and caspase activity, and decreased mitochondrial membrane permeability. In this sense, a portion of anti-proliferative activity is due to apoptosis. Notwithstanding, due to its remarkable response, chalcone 18 may be a potential alternative as a chemotherapeutic anti-carcinogen.
•Synthesis by ultrasound irradiation represent an efficient and ecofriendly method.•Compound 18 exhibited a selective cytotoxic activity against cancer cells.•Oxyalkylated chalcones may be a potential alternative as a chemotherapeutic agent.
is a native South American plant used ancestrally by Mapuche people to treat gastrointestinal ailments.
flower extracts are rich in molecules with therapeutic potential, including the sesquiterpene ...lactone leptocarpin, which displays cytotoxic effects against various cancer types in vitro. However, the combination of active molecules in these extracts could offer a hitherto unexplored potential for targeting cancer. In this study, we investigated the effect of
flower extracts on the proliferation, survival, and spread parameters of gastric cancer cells in vitro. Gastric cancer (AGS and MKN-45) and normal immortalized (GES-1) cell lines were treated with different concentrations of
flower extracts (DCM, Hex, EtOAc, and EtOH) and we determined the changes in proliferation (MTS assay, cell cycle analysis), cell viability/cytotoxicity (trypan blue exclusion assay, DEVDase activity, mitochondrial membrane potential MMP, and clonogenic ability), senescence (β-galactosidase activity) and spread potential (invasion and migration assays using the Boyden chamber approach) in all these cells. The results showed that the DCM, EtOAc, and Hex extracts display a selective antitumoral effect in gastric cancer cells by affecting all the cancer parameters tested. These findings reveal an attractive antitumoral potential of
flower extracts by targeting several acquired capabilities of cancer cells.
A series of novel dihydrochalcone derivatives 2-7 were synthesized from dihydroisorcordoin 1 which was isolated from the aerial parts of Adesmia balsamica. The structures of all compounds were ...confirmed by
1
H NMR,
13
C NMR, and HRMS. Their anti-oomycete activity was evaluated in vitro against Saprolegnia parasitica and Saprolegnia diclina. Some of the newly synthesized compounds exhibited better anti-oomycete activities at low values compared with bronopol and fluconazole as positive controls. Among them, compound 7 exhibited strong activity, with minimum inhibitory concentration and minimum oomyceticidal concentration values of 75 and 100 μg/mL, respectively.
•The thermal performance of ZrO2 nanofluids through two heat exchangers is studied.•ZrO2 nanofluids enhance heat transfer in laminar and turbulent flow.•Analysis reveals enhanced heat transfer ...performance and moderate pressure drops.•A new Nusselt correlation for nanofluids is proposed with deviations under 15 %.•ZrO2 nanofluids show promising potential for ground heat exchangers.
The improvement in heat transfer equipment plays a significant role to enhance the overall performance of many systems and a wide variety of industrial processes. Heat exchangers are widely used in many of these applications and, with the aim of limiting the growing of energy demand, further improvement is needed. A low-enthalpy geothermal system is commonly constituted by a ground heat exchanger, a heat pump unit, and indoor heating/cooling units. In the ground heat exchanger circuit, the heat exchange occurs between the fluid of the wellbore and the ground through a tubular section similar to that of the inner tube of a Double-Tube Heat Exchanger (DTHE), and between the fluid of the wellbore and the refrigerant of the heat pump in the evaporator/condenser, which is typically a Plate Heat Exchanger (PHE). The use of new nano-enhanced heat transfer fluids featuring improved properties, known as nanofluids, has been proposed as a potential solution for energy efficiency improvement. This study aims to analyse the feasibility of ZrO2 nanofluids based on a propylene glycol:water 10:90 vol% mixture as working fluids in heat transfer applications, focusing on renewable energy systems such as low-enthalpy geothermal installations. The heat transfer performance and hydrodynamic behaviour of four new ZrO2-based nanofluids at nanoparticle mass concentrations of 0.25, 0.50, 0.75, and 1.0 wt% are analysed and compared with the base fluid. Tests through a PHE and a DTHE were performed, and convective heat transfer coefficients and pressure drops were obtained in laminar and turbulent regimes. Increases of the convective heat transfer coefficients up to 123 % and 8.8 % were found for the nanofluids in comparison to the base fluid for laminar flow in the PHE and for turbulent flow in the DTHE, respectively. Finally, a dimensionless analysis was carried out through Nusselt and Reynolds numbers and Darcy friction factor.
The purpose of the article is to support the main role of an effective public policy of innovation, science and technology, oriented to contribute to productive development and social inclusion. To ...this objective, a strong conceptual framework is adopted that emerges from the threefold failure: market, system and State. It supports policy´s key components such as: governance and focus on science, innovation, and productive development. There is awareness that in the world there exists a set of methods, models and techniques that facilitate the achievement of seemingly contradictory objectives. Among the challenges presented, note is made of the support of science, innovation, and productive development to post-conflict Colombian nation and territory and to the economy´s informal sector.
El propósito de este artículo es sustentar la centralidad de una efectiva política pública de innovación, ciencia y tecnología con miras a contribuir al desarrollo productivo y la inclusión social. Para ello se adopta un marco conceptual robusto que, partiendo de la triple falla (mercado, sistema y Estado), sustenta componentes clave de la política como son la gobernanza y la focalización en ciencia, innovación y desarrollo productivo. Hay conciencia de que en el mundo existe un conjunto de métodos, modelos y técnicas que facilitan la consecución de objetivos aparentemente contradictorios. Entre los retos planteados, cabe mencionar, en los niveles nacional y territorial, el apoyo de la ciencia, la innovación y el desarrollo productivo al posconflicto colombiano y del sector informal de la economía.
In this study, we aimed to evaluate two sets of sesquiterpene-aryl derivatives linked by an ester bond, their cytotoxic activities, and their capacity to activate caspases 3/7 and inhibit human ...topoisomerase I (TOP1). A total of 13 compounds were synthesized from the natural sesquiterpene (-)-drimenol and their cytotoxic activity was evaluated in vitro against three cancer cell lines: PC-3 (prostate cancer), HT-29 (colon cancer), MCF-7 (breast cancer), and an immortalized non-tumoral cell line (MCF-10). From the results, it was observed that
was the most promising compound due to its cytotoxic effect on three cancer cell lines and its selectivity,
was 100-fold more selective than 5-FU in MCF-7 and 20-fold in PC-3. It was observed that
also induced apoptosis by caspases 3/7 activity using a Capsase-Glo-3/7 assay kit and inhibited TOP1. A possible binding mode of
in a complex with TOP1-DNA was proposed by docking and molecular dynamics studies. In addition,
was predicted to have a good pharmacokinetic profile for oral administration. Therefore, through this study, it was demonstrated that the drimane scaffold should be considered in the search of new antitumoral agents.
In this study, the essential oil (EO) from
was analyzed by GC/MS and safrole (
) was identified as the major metabolite
, was subjected to direct reactions on the oxygenated groups in the aromatic ...ring and in the side chain, and eight compounds (
to
) were obtained by the process. EO and compounds
-
were subjected to biological assays on 24 strains of the genus
, specifically of the species 12
and 12
. EO showed a significant effect against
strains. Compound
presents the highest activity against two resistant strains, with minimum inhibitory concentration (MIC) and minimum oomyceticidal concentration (MOC) values of 25 to 100 and 75 to 125 µg/mL, respectively. The results show that compound
exhibited superior activities compared to the commercial controls bronopol and azoxystrobin used to combat these pathogens.
Tomato crops can be affected by several infectious diseases produced by bacteria, fungi, and oomycetes. Four phytopathogens are of special concern because of the major economic losses they generate ...worldwide in tomato production;
subsp.
and
pv.
, causative agents behind two highly destructive diseases, bacterial canker and bacterial speck, respectively; fungus
f. sp.
that causes Fusarium Wilt, which strongly affects tomato crops; and finally,
spp., which affect both potato and tomato crops. Polygodial (
), drimenol (
), isonordrimenone (
), and nordrimenone (
) were studied against these four phytopathogenic microorganisms. Among them, compound
, obtained from
Forst, and synthetic compound
are shown here to have potent activity. Most promisingly, the results showed that compounds
and
affect
growth at minimal inhibitory concentrations (MIC) values of 16 and 32 µg/mL, respectively, and high antimycotic activity against
and
spp. with MIC of 64 µg/mL. The results of the present study suggest novel treatment alternatives with drimane compounds against bacterial and fungal plant pathogens.
Resinous exudate obtained from the aerial parts of Adesmia boronioides Hook.f. were evaluated to determine anti-phytopathogenic effects. Briefly, resinous exudate was obtained by dipping fresh plant ...material in dichloromethane; chemical composition was determined by GC-MS; and minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were evaluated against four phytopathogenic bacteria. Resinous exudate yield was 8.5% (resin/fresh plant), of which esquel-6-en-9-one (14.25%), esquel-7-en-9-one (5.86%), and veratric acid (2.59%) were the effective antibacterial compounds. Tested against Pectobacterium carotovorum subsp. carotovora, Erwinia amylovora, Bacillus subtilis, and Pseudomonas syringae, MICs and MBCs ranged from 16 to 128 µg/mL and 32-256 µg/mL, respectively. These results provide initial evidence that resinous bush A. boronioides is a new and alternative source of substances with agricultural interest.
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