Cytotoxicity of Nine Medicinal Plants from San Basilio de Palenque (Colombia) on HepG2 Cells.

The utilization of plants with medicinal properties is deeply rooted in the traditional knowledge of diverse human populations. This study aims to investigate the cytotoxicity of nine plants commonly used by communities in San Basilio de Palenque, Bolivar (Colombia), for managing inflammation-related illnesses. Hydroethanolic extracts from various plant parts such as roots, stems, barks, or leaves were prepared through a process involving drying, powdering, and maceration in an ethanol-water (7:3) solution. The extracts were subsequently freeze-dried and dissolved in DMSO for the bioassays. Cytotoxicity against the human hepatoma HepG2 cell line was assessed using the MTT assay, with extract concentrations ranging from 0 to 500 µg/mL and treatment durations of 24 and 48 h. The total phenolic content of the nine extracts varied from 96.7 to 167.6 mg GAE/g DT. Among them, eight hydroethanolic extracts from Jatropha gossypiifolia L., Piper peltatum L., Malachra alceifolia, Verbesina turbacensis, Ricinus communis, Desmodium incanum, and Dolichandra unguis-cati showed low toxicity (IC50 > 500 µg/mL, 24 h) against HepG2 cells. On the other hand, the extracts of Aristolochia odoratissima L. (IC50 = 95.7 µg/mL) and Picramnia latifolia (IC50 = 128.9 µg/mL) demonstrated the highest cytotoxicity against the HepG2 cell line, displaying a modest selectivity index when compared to the HEKn cell line after 48 h of treatment. These findings suggest that medicinal plants from San Basilio de Palenque, particularly Picramnia latifolia and Aristolochia odoratissima, have potential activity against cancer cells, highlighting their potential for further research and development.

Deleterious Effects of Cymbopogon nardus (L.) Essential Oil on Life Cycle and Midgut of the Natural Predator Ceraeochrysa claveri (Navás, 1911) (Neuroptera: Chrysopidae).

Cymbopogon nardus (citronella) essential oil (EO) has been widely used in the cosmetic and food industry due to its repellent and fumigant properties. The aim of this study was to evaluate its effects on the life cycle and midgut morphology of the natural predator Ceraeochrysa claveri. Larvae were fed on sugarcane borer eggs (Diatraea saccharalis) pretreated with citronella EO solutions (1-100 µg/mL in methanol, 5 s) or solvent and air-dried at room temperature for 30 min. Larval and pupal stage duration, the percentage of emergence of the insect, and malformed insects were recorded. One day after adults emerged from their cocoons, adult insects were used to obtain their midgut and analyzed using light microscopy. The chemical composition of C. nardus EO revealed that citronellal (25.3%), citronellol (17.9%), geraniol (11.6%), elemol (6.5%), δ-cadinone (3.6%), and germacrene D (3.4%) were the predominant compounds. Exposure to the EO produced a significant change in development duration for third instar and prepupa of the insect. The observed alterations in the lifecycle included prepupae with no cocoon formation, dead pupa inside the cocoon, and malformed adults. Several injuries in the midgut epithelium of exposed adults were registered, such as detachment of columnar cells leaving only swollen regenerative cells fixed on the basement membrane, and the formation of epithelial folds. In summary, these data suggest that C. nardus oil has adverse effects on the life cycle and midgut morphology of a beneficial predator.

Cytoprotective, Antiproliferative, and Anti-Oxidant Potential of the Hydroethanolic Extract of Fridericia chica Leaves on Human Cancer Cell Lines Exposed to α- and ß-Zearalenol.

Fridericia chica (Bignoniaceae) is a Colombian Caribbean plant with numerous health benefits, including properties such as wound healing, immune system stimulation, and antioxidant capacity, among others. Mycotoxins alpha-zearalenol (α-ZEL) and beta-zearalenol (ß-ZEL) are phase I metabolites of zearalenone, a natural product involved in endocrine disruption and cell proliferation processes. This study aimed to investigate the cytotoxic potential of the hydroethanolic extract of F. chica leaves (HEFc) and determine their protective effects against proliferation induced by α-ZEL and ß-ZEL on human hepatoma HepG2, lung cancer Calu-1, and primary normal human epidermal keratinocytes, neonatal (HEKn). The cytotoxicity of HEFc was measured in a range from 4 to 1000 µg/mL and from 0.4 to 100 µM for both α-ZEL and ß-ZEL. Cell production of intracellular ROS was monitored using the H2-DCFDA probe. The cells exposed to HEFc presented IC50 of 128, 249, and 602 µg/mL for the HepG2, Calu-1, and HEKn cells, respectively. A greater selectivity was seen in HepG2 cells [selectivity index (SI) = 3.5] than in Calu-1 cells (SI = 2.4). Cells treated with mycotoxins remained viable during the first day, and cell proliferation increased at low tested concentrations (0.4-6.3 µM) in all three cell lines. However, after 48 h treatment, cells exposed to 50 and 100 µM of α-ZEL and ß-ZEL displayed decreased viability. HEFc at 16 µg/mL was able to give some protection against cytotoxicity induced by high concentrations of ß-ZEL in HepG2, reducing also cell proliferation elicited at low levels of α-ZEL and ß-ZEL. ROS production was not observed in cells treated with this HEFc concentration; however, it prevented ROS formation induced by treatment with 50 µM α-ZEL or ß-ZEL. In summary, HEFc isolated from plants grown in northern Colombia displayed promising results against cell proliferation and oxidative stress caused by mycotoxins.

Photoprotective Agents Obtained from Aromatic Plants Grown in Colombia: Total Phenolic Content, Antioxidant Activity, and Assessment of Cytotoxic Potential in Cancer Cell Lines of Cymbopogon flexuosus L. and Tagetes lucida Cav. Essential Oils.

Photoprotective agents obtained from plants provide benefits for the health of the skin. The present study aims to assess the total phenolic content (TPC) and in vitro UV-protective properties of twelve essential oils (EOs) from plants grown in Colombia and to evaluate the antioxidant and cytotoxic potential of two species identified as photoprotective potentials: Cymbopogon flexuosus and Tagetes lucida. The composition of EOs was studied by GC/MS. The cytotoxicity of both EOs was examined using an MTT assay, and an H2-DCFDA probe was employed to estimate the intracellular production of ROS in HepG2 and Calu-1 cells. Major constituents (≥10%) were neral, geranial, geranyl acetate in C. flexuosus and estragole in T. lucida. The TPC for C. flexuosus and T. lucida EOs were ≥10 mg GAE/g of byproduct. Both EOs showed photoprotective properties (SPFin vitro: 13−14), and long-wavelength UVA protection (λc > 370 nm). HepG2 and Calu-1 cells exposed to C. flexuosus exhibited antiproliferative activity (˂50%) at 125 µg/mL, while T. lucida was at 250 and 500 µg/mL. The IC50 values for C. flexuosus were 75 and 100 µg/mL in HepG2 and Calu-1 cells, respectively, whereas those for T. lucida were >250 µg/mL. These EOs achieved significant inhibitory effects (between 15.6 and 40.4%) against H2O2-induced oxidative stress. The results showed that EO compounds recognized as antioxidants could counteract the effects elicited by H2O2.

Protective Effects of the Hydroethanolic Extract of Fridericia chica on Undifferentiated Human Neuroblastoma Cells Exposed to α-Zearalenol (α-ZEL) and ß-Zearalenol (ß-ZEL).

Fridericia chica (Bignoniaceae) is a traditional medicinal plant. The aim of this research was to determine the protective effects of the hydroethanolic extract from the F. chica leaves (HEFc) against the cytotoxicity of zearalenone (α-ZEL) and ß-ZEL on SH-SY5Y cells. Free radical scavenging activity of HEFc was evaluated using the DPPH method. The cytotoxicity of both zearalenone metabolites and HEFc was examined using MTT test, as was the cytoprotective effects of the HEFc on cells treated with these mycotoxins. The chemical composition of HEFc was determined using UPLC-QTOF-MS/MS. HEFc elicited good DPPH radical scavenging activity following a concentration-dependent relationship. Cells exposed to α-ZEL exhibited a viability ˂50% after 48 h of treatment (25 and 50 µM), while those exposed to ß-ZEL showed viability ˂50% (100 µM) and ˂25% (25-100 µM) after 24 and 48 h of exposure, respectively. HEFc showed a significant increase in cell viability after exposure to α-ZEL (25 and 50 µM) and ß-ZEL (6-100 µM) (p < 0.05). UPLC-QTOF-MS/MS analyses allowed the identification of 10 phytochemical components in the HEFc. In short, the hydroethanolic extract of F. chica grown in Colombian Caribbean can protect against the effects of mycotoxins and it is a valuable source of compounds with antioxidant properties.

The aqueous extract of Fridericia chica grown in northern Colombia ameliorates toxicity induced by Tergitol on Caenorhabditis elegans.

The aqueous extract of fallen leaves from Fridericia chica (Bonpl.) L.G. Lohmann is utilized as a remedy in communities at northern Colombia. Traditional uses include wound healing, gastrointestinal inflammation, leukemia and psoriasis, among others. The aims of this research were to evaluate the potential of the aqueous extract of fallen leaves of F. chica (AEFchica) to inhibit ethoxylated nonylphenol (Tergitol)-induced toxicity in Caenorhabditis elegans; and to identify its main components. The pharmacological properties of AEFchica was evaluated using a Tergitol-induced toxicity model in Caenorhabditis elegans. Lethality, locomotion, reproduction, and DAF-16 nuclear translocation were quantified. The chemical composition of AEFchica was carried out using ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. AEFchica induced very little lethality on C. elegans (5.6%) even at high concentrations (10,000 µg/mL). The extract had no effect on locomotion impairing induced by ethoxylated nonylphenol. However, AEFchica (1000 µg/mL) abrogated Tergitol-induced mortality, recovering up to 53.3% of the nematodes from lethality induced by 10 mM Tergitol. Similarly, it also blocked Tergitol-dependent reproduction inhibition (82.1% recovery), as well as DAF-16 nuclear translocation (>95%), suggesting a prominent role on oxidative stress control. The chemical analysis indicated the presence of a great variety of molecules with known antioxidant, metabolic and immune modulator properties, such as hydroxylated methoxy flavones, N-methyl-1-deoxynojirimycin, and rehmaionoside A. In short, the aqueous extract of F. chica protects C. elegans from the deleterious effects of Tergitol on lethality, reproduction and oxidative stress involving DAF-16-mediated pathway. This extract is a promising source of bioactive phytochemicals for multi-target pharmacological purposes.

Biomonitoring of Mercury, Cadmium and Selenium in Fish and the Population of Puerto Nariño, at the Southern Corner of the Colombian Amazon.

Heavy metals threaten communities near biodiversity hotspots, as their protein sources come from the environment. This study assessed Hg, Cd, and Se concentrations in fish, as well as the magnitude of exposure and hematological conditions of adult citizens from Puerto Nariño (Colombian Amazon). Among fish samples, greater Hg concentrations were found in higher trophic level species, including Rhaphiodon vulpinus (880 ± 130 ng/g) and Pseudoplatystoma tigrinum (920 ± 87 ng/g). These species presented the highest hazard quotients and lowest Se:Hg molar ratios among those studied, showing their consumption represents a health risk to consumers. Moreover, some samples of Mylossoma duriventre and Prochilodus magdalenae had Cd levels greater than the regulated limit (100 ng/g). The average total Hg (T-Hg) concentrations in human hair and blood were 5.31 µg/g and 13.7 µg/L, respectively. All hair samples exceeded the 1.0 µg/g threshold set by the USEPA, whereas 93% of the volunteers had T-Hg blood levels greater than 5 µg/L, suggesting elevated exposure. The mean Cd level was 3.1 µg/L, with 21% of samples surpassing 5 µg/L, value at which mitigating actions should be taken. Eighty-four percent of participants presented Se deficiencies (<100 µg/L). There was a significant association between fish consumption and T-Hg in hair (ρ = 0.323; p = 0.032) and blood (ρ = 0.381; p = 0.011). In this last matrix, Se correlated with Cd content, whereas lymphocytes were inversely linked to Hg concentrations. The results of this study show that there is  extensive exposure to Hg in fish, the consumption of which may promote detrimental impacts on hematology parameters within the community.

Embryonic exposure to an aqueous coal dust extract results in gene expression alterations associated with the development and function of connective tissue and the hematological system, immunological and inflammatory disease, and cancer in zebrafish.

Coal mining is one of the economic activities with the greatest impact on environmental quality. At all stages contaminants are released as particulates such as coal dust. The first aim of this study was to obtain an aqueous coal dust extract and characterize its composition in terms of trace elements by ICP-MS. In addition, the developmental toxicity of the aqueous coal extract was evaluated using zebrafish (Danio rerio) after exposure to different concentrations (0-1000 ppm; µg mL-1) to establish acute toxicity, morphology and transcriptome changes. Trace elements within the aqueous coal dust extract present at the highest concentrations (>10 ppb) included Sr, Zn, Ba, As, Cu and Se. In addition, Cd and Pb were found in lower concentrations. No significant difference in mortality was observed (p > 0.05), but a delay in hatching was found at 0.1 and 1000 ppm (p < 0.05). No significant differences in morphological characteristics were observed in any of the treatment groups (p > 0.05). Transcriptomic results of zebrafish larvae revealed alterations in 77, 61 and 1376 genes in the 1, 10, and 100 ppm groups, respectively. Gene ontology analysis identified gene alterations associated with the development and function of connective tissue and the hematological system, as well as pathways associated with apoptosis, the cell cycle, transcription, and oxidative stress including the MAPK signaling pathway. In addition, altered genes were associated with cancer; connective tissue, muscular, and skeletal disorders; and immunological and inflammatory diseases. Overall, this is the first study to characterize gene expression alterations in response to developmental exposure to aqueous coal dust residue from coal mining with transcriptome results signifying functions and systems to target in future studies.

Low blood lead levels impair intellectual and hematological function in children from Cartagena, Caribbean coast of Colombia.

Lead produces numerous biochemical and physiological changes in humans, including hematological disorders, toxic effects on the central nervous system and in the function of several organs. The aim of this study was to determine blood lead levels (BLL) in children from Cartagena, Colombia, associating those with hematological and liver damage markers, the intelligence quotient (IQ), as well as with gene expression of the aminolevulinate dehydratase (ALAD), superoxide dismutase 1 (SOD1), gamma interferon (INF-γ), tumor necrosis factor (TNF) and tumor protein (p53). To achieve this purpose, 118 blood samples were collected from children 5-16 years old, with their respective informed consent from their parents. BLL was measured by atomic absorption; hematological parameters were obtained with automated systems; plasma was utilized to analyze hepatic toxicity markers, alanine aminotransferase (ALT), gamma-glutamyltransferase (γ-GT) and alkaline phosphatase (ALP); the Kaufman Brief Intelligence Test (K-BIT) was administered to measure the IQ; and gene expression was quantified from blood RNA. The mean BLL was 1.7±0.3µg/dL. A low proportion of the children (3.4%) had BLL above the CDC recommended limit (5µg/dL). BLL were correlated weakly, but negatively with child age, weight, height, body mass index, platelets wide distribution, mean platelet volume, γ-GT and IQ. There were not significant changes in the expression of evaluated genes. These results support the hypothesis that BLL below 5µg/dL may still be a detrimental factor on children's cognitive abilities, development and hematology, in line with recent concerns that there is no safe level of pediatric lead exposure.

Toxicity of Naphthalene and Benzene on Tribollium castaneum Herbst.

Naphthalene and benzene are widely-used volatile organic compounds. The aim of this research was to examine the toxicological effects of naphthalene and benzene against Tribolium castaneum as an animal model. Adult insects were exposed to these aromatic compounds to assess mortality after 4-48 h of exposure. The lethal concentration 50 (LC50) for naphthalene, naphthalin, and benzene were 63.6 µL/L, 20.0 µL/L, and 115.9 µL/L in air, respectively. Real-time polymerase chain reaction (PCR) analysis revealed expression changes in genes related to oxidative stress and metabolism [Glutathione S-Transferase (Gst), and Cytochrome P450 6BQ8 (Cyp6bq8)]; reproduction and metamorphosis [Hormone receptor in 39-like protein (Hr39), Ecdysone receptor: (Ecr), and Chitin synthase 2 (Chs2)]; and neurotransmission [Histamine-gated chloride channel 2 (Hiscl2)] in insects exposed for 4 h to 70.2 µL/L naphthalene. Adults exposed to benzene (80 µL/L; 4 h) overexpressed genes related to neurotransmission [GABA-gated anion channel (Rdl), Hiscl2, and GABA-gated ion channel (Grd)]; reproduction and metamorphosis [Ultraspiracle nuclear receptor (USP), Ecr; and Hr39]; and development (Chs2). The data presented here provides evidence that naphthalene and benzene inhalation are able to induce alterations on reproduction, development, metamorphosis, oxidative stress, metabolism, neurotransmission, and death of the insect.

Chemical and toxicological characterization of sediments along a Colombian shoreline impacted by coal export terminals.

Extraction, transport and utilization of coal spread out coal dust. Nowadays, Colombia is an important producer of this mineral in South America, being the Santa Marta area one of the largest coal exporting ports in the country. The aim of this work was to assess the pollutants levels and toxicity of shoreline sediments from this place. 16 PAHs and 46 elements were measured in nine locations during dry and rainy seasons. HepG2 cells were exposed to 1% sediment extracts and mRNA expression evaluated for selected genes. PAHs levels were greater during the rainy season. The highest ∑PAHs (89.9 ng g(-1)) appeared at a site located around 300 m far from the coast line at close proximity to the area where coal is loaded into cargo vessels for international shipments, being naphthalene the most abundant PAH. At Santa Marta Bay port, ∑PAHs were 62.8 ng g(-1) and 72.8 ng g(-1) for dry and rainy seasons, respectively, with greatest levels for fluoranthene. Based on sediment standards, most stations have poor condition regarding Cr, but moderate contamination on Cu, Pb and Zn. Sediments from the port and coal transport sites, the most polluted by PAHs and metals, induced CYP1A1 and NQO1 during the dry season. Data showed the sediments from this shoreline have bioactive chemicals that determine their toxicological profile.

Chemical composition and bioactivity of Piper auritum and P. multiplinervium essential oils against the red flour beetle, Tribolium castaneum (Herbst) / Composición química y bioactividad de los aceites esenciales de Piper auritum y P. multiplinervium contra el escarabajo rojo de la harina, Tribolium castaneum (Herbst)

Stored grain insects have shown resistance to synthetic insecticides, fact that has promoted the use of vegetable species for integrated pest management. Piper auritum and P. multiplinervium are two plants from the Piperaceae family present in the department of Chocó, Colombia, one of the most important hot spots of biodiversity in the world. This study was conducted to determine the repellent activity and toxicity of essential oils (EOs) isolated from these plants against Tribolium castaneum, using the area preference and contact toxicity methods, respectively. P. auritum EO presented greater repellency than P. multiplinervium, the first showed 100 percent lethality at minimum tested exposure period (24 h) whereas the second reached 16 percent at 72 h. EOs were analyzed by gas chromatography-mass spectrometry. P. auritum major components were safrole (93.2 percent) and miristicine (4.3 percent), whereas for P. multiplinervium were beta-elemene (9.0 percent), trans-beta-caryophyllene (5.3 percent) and caryophyllene oxide (4.1 percent). It is speculated that the repellent effect of P. auritum may be related to its safrole content, a known repellent. These results evidenced Piper species could be used for development of repellents against T. castaneum.

Los insectos de los granos almacenados han mostrado resistencia a los insecticidas sintéticos, hecho que ha promovido el uso de especies vegetales para el manejo integrado de plagas. Piper auritum y P. multiplinervium son dos plantas de la familia Piperaceae presentes en el departamento del Chocó, Colombia, uno de los puntos de biodiversidad más importantes del mundo. En este estudio fue determinada la actividad repelente y toxicidad de los aceites esenciales (AE) aislados de estas plantas contra Tribolium castaneum, utilizando el método de área de preferencia y toxicidad por contacto, respectivamente. El AE de P. auritum presentó mayor repelencia que el de P. multiplinervium, el primero mostró 100 percent de letalidad al menor tiempo de exposición (24 h), mientras que el segundo alcanzó el 16 percent a las 72 h. Los AEs fueron analizados por cromatografía de gases-espectrometría de masas. Los componentes principales de P. auritum fueron safrol (93.2 percent) y miristicina (4.3 percent), mientras que para P. multiplinervium fueron beta-elemene (9.0 percent), trans-beta-cariofileno (5.3 percent) y óxido de cariofileno (4.1 percent). Se cree que el efecto repelente de P. auritum puede estar relacionado con su contenido de safrol, un repelente conocido. Estos resultados evidencian que las especies de Piper podrían ser utilizadas para el desarrollo de repelentes contra T. castaneum.

Actividad repelente de los aceites esenciales de Lippia origanoides, Citrus sinensis, y Cymbopogon nardus cultivadas en Colombia frente a Tribolium castaneum, Herbst / Repellent activity of the essential oils from Lippia origanoides, Citrus sinensis, and Cymbopogon nardus cultivated in Colombia against Tribolium castaneum, Herbst

Objetivo: El objetivo de este estudio fue evaluar la actividad repelente de tres aceites esenciales (AE) y un repelente comercial frente a la especie Tribolium castaneum, Herbst, una de las principales plagas de cereales y productos almacenados. Materiales y métodos: La actividad repelente fue medida utilizando el método de área de preferencia, además fue determinada la concentración de aceite esencial capaz de repeler el 50% de los insectos (CR50). La prueba T pareada fue utilizada para encontrar diferencias significativas entre el número de insectos presentes en las áreas tratadas y no tratadas. Resultados: Todos los AEs mostraron actividad repelente contra T. castaneum, y la magnitud del efecto fue dependiente de la concentración utilizada. Los AE con mayor repelencia fueron los extraídos de Lippia origanoides y Citrus sinensis, mientras que el aceite con menor actividad fue el de Cymbopogon nardus. Discusión: Aunque en términos de CR50 el AE de C. nardus mostró actividad repelente inferior a la de L. origanoides y C. sinensis, el primero presentó una eficacia superior a la del producto comercial IR3535. Estos AEs han mostrado propiedades repelentes frente a organismos diferentes a T. castaneum, lo cual sugiere que su espectro de acción es amplio. Conclusiones: Los resultados han demostrado que los AEs de la flora colombiana son una fuente importante de repelentes, por lo que podrían ser usados para el control biológico de insectos.

Objective: The aim of this study was to evaluate the repellent activity of three essential oils (EO), and a commercial repellent against species Tribolium castaneum Herbst, a major pest of grain and stored products. Materials and methods: The repellent activity was measured using the area of preference method, as well as the concentration of essential oil that is capable of repelling 50% of the insects (RC50). A paired T test was used to find significant differences between the number of insects present in the treated and untreated areas. Results: All EOs showed repellent activity against T. castaneum, and the magnitude of the effect was dose-dependent. The AE with the highest repellence were those extracted from Lippia origanoides and Citrus sinensis, whereas the one with the lowest activity was that from Cymbopogon nardus. Discussion: Although in terms of RC50 the EO from C. nardus showed repellent activity lower than those registered for L. origanoides and C. sinensis, the first had a greater efficacy than that showed by the commercial product IR3535. These Eos have shown repellent properties against organism different from T. Castaneum, suggesting that they have a wide spectrum of action. Conclusions: The results have shown that EOs from Colombian flora are an important source of repellents, which could be used for biological control of insects.