Chenopodium quinoa Willd. and Amaranthus hybridus L.: Ancestral Andean Food Security and Modern Anticancer and Antimicrobial Activity.

The species Chenopodium quinoa Willd. and Amaranthus hybridus L. are Andean staples, part of the traditional diet and gastronomy of the people of the highlands of Colombia, Ecuador, Peru, Bolivia, northern Argentina and Chile, with several ethnopharmacological uses, among them anticancer applications. This review aims to present updated information on the nutritional composition, phytochemistry, and antimicrobial and anticancer activity of Quinoa and Amaranth. Both species contribute to food security due to their essential amino acid contents, which are higher than those of most staples. It is highlighted that the biological activity, especially the antimicrobial activity in C. quinoa, and the anticancer activity in both species is related to the presence of phytochemicals present mostly in leaves and seeds. The biological activity of both species is consistent with their phytochemical composition, with phenolic acids, flavonoids, carotenoids, alkaloids, terpenoids, saponins and peptides being the main compound families of interest. Extracts of different plant organs of both species and peptide fractions have shown in vitro and, to a lesser degree, in vivo activity against a variety of bacteria and cancer cell lines. These findings confirm the antimicrobial and anticancer activity of both species, C. quinoa having more reported activity than A. hybridus through different compounds and mechanisms.

Exploring the Antioxidant Potential of Tragia volubilis L.: Mitigating Chemotherapeutic Effects of Doxorubicin on Tumor Cells.

Several plants of the genus Tragia L. have shown antibacterial, fungicidal, and antiproliferative activity, among other types of activities; however, most species of the genus have not been investigated. Tragia volubilis L. is native to tropical America and Africa, and although it has been reported as medicinal in the literature, it has not been thoroughly investigated. In this study, the phytochemical screening, isolation, and identification of compounds and the determination of the antioxidant activity of the aqueous extract of Tragia volubilis L. and its partitions were carried out. Ethyl acetate and n-butanol partitions of the extract present high antioxidant activity according to the Antioxidant Activity Index. Due to their activity, these partitions were tested on RKO cells as a representative model, both individually and in combination with Doxorubicin. It was found that the partitions significantly reduced the effect of Doxorubicin, as well as the expression of proteins involved in DNA damage and cell death. While the reduction of the chemotherapeutic effect of Doxorubicin on tumor cells may not be a desired outcome in therapeutic settings, the findings of the study are valuable in revealing the antioxidant potential of Tragia volubilis L. and its partitions. This highlights the importance of carefully regulating the application of antioxidants, especially in the context of cancer chemotherapy.

Crystal Structure, Hirshfeld Surface Analysis, and Biological Activities of Schiff-Base Derivatives of 4-Aminoantipyrine.

Eight Schiff bases, synthesized by the reaction of 4-aminoantipyrine with different cinnamaldehydes, were studied in the solid state by using vibrational spectroscopy (IR) and X-ray diffraction techniques. The analysis was extended to the solution phase through ultraviolet-vis, fluorescence spectroscopy, and cyclic voltammetry. Finally, the crystal structures of four compounds (3b, 3d, 3g, and 3h) were determined and studied. In addition to the experimental study, theoretical calculations using the semiempirical method PM6/ZDO were performed to understand better the compound's molecular properties, UV-vis, and infrared spectra. The primary difference is the angular conformation of the terminal phenyl rings around the corresponding linking C-N and C-C σ-bonds. Furthermore, as a result of extended bonding, the > C=N- azomethine group-containing Cpyr-N=(CH)-(CR)=(CH)-Cbz chain (with R=H for 3b, 3d, and 3h, and R=CH3 for 3g) is planar, nearly coplanar, with the mean plane of the pyrazole ring. Hirshfeld surface (HS) analysis was used to investigate the crystal packing and intermolecular interactions, which revealed that intermolecular C-H···O and C-H···N hydrogen bonds, π···π stacking, and C-H···π and C=O···π interactions stabilize the compounds. The energy contributions to the lattice energies of potential hydrogen bonds were primarily dispersive and repulsive. All derivatives were tested in vitro on LPS-stimulated mouse macrophages to assess their ability to suppress the LPS-induced inflammatory responses. Only a slight reduction in the level of NO production was found in activated macrophages treated with 3h. Additionally, the derivatives were tested for antimicrobial activity against several clinical bacteria and fungi strains, including three biofilm-forming microorganisms. Nevertheless, only Schiff base 3f showed interesting antibacterial activities with minimum inhibitory concentration (MIC) values as low as 15.6 µM against Enterobacter gergoviae. On the other hand, Schiff base 3f and, to a lesser extent, 3b and 3h showed antifungal activity against clinical isolates of Candida. The lowest MIC value was for 3f against Candida albicans (15.6 µM). It is interesting to note that the same Schiff bases exhibit the highest activity in both biological evaluations.

Flavonoid Composition and Antioxidant Activity of Tragia volubilis L. Methanolic Extract.

Several species from the genus Tragia L. in the family Euphorbiaceae are part of the ethnomedicine of traditional cultures, and have a variety of uses. Tragia volubilis L. is a species spread through tropical America and Africa with several ethnomedical uses, particularly for wound healing and reproductive issues. In this study, we assess the phytochemical composition and antioxidant activity of the methanolic extract of the aerial parts of T. volubilis collected in southern Ecuador. The phytochemical screening of the extract shows the preliminary presence of carbohydrates, alkaloids, flavonoids, and tannins. The extract shows an Antioxidant Activity Index of 1.14, interpreted as strong antioxidant activity. Four flavonoid compounds were isolated through chromatographic procedures and identified through NMR spectroscopy: avicularin, quercitrin, afzelin, and amentoflavone. The biological activity of these compounds matches the ethnopharmacological uses of the species. This is the first phytochemical study of T. volubilis and supports its traditional medicinal uses.

Peach Palm (Bactris gasipaes Kunth.): Ancestral Tropical Staple with Future Potential.

A pre-Columbian staple, Bactris gasipaes Kunth. is a palm tree domesticated around 4000 years ago, so appreciated that a Spanish chronicler wrote in 1545, "only their wives and children were held in higher regard" by the Mesoamerican natives. The peach palm is an integral part of the foodways and gastronomy of Ecuador, Colombia, Bolivia, Peru, Brazil, and other tropical American countries; meanwhile, it is almost unknown in the rest of the world, except for hearts of palm. Although abundant, the species faces anthropogenic threats. The purpose of this study is to describe and summarize the physicochemical, nutritional, and bioactive characteristics of the peach palm and its two main alimentary products: hearts of palm and fruits, highlighting the functional and antioxidant potential of the latter, showing both ancestral and modern uses. There is active research on peach palm products and coproducts that aim for better, more sustainable uses of its traditional and recently found properties. The review and presentation of studies on this strategically relevant species can motivate the protection of endangered populations and stimulate new lines of research to advance development in the food, pharmaceutical, and cosmetic industries, with fair trade, sustainable development goals, and adaptation to climate change in mind.

Xylosma G. Forst. Genus: Medicinal and Veterinary Use, Phytochemical Composition, and Biological Activity.

Xylosma G. Forst. is a genus of plants belonging to the Salicaceae family with intertropical distribution in America, Asia, and Oceania. Of the 100 accepted species, 22 are under some level of conservation risk. In this review, around 13 species of the genus used as medicinal plants were found, mainly in Central and South America, with a variety of uses, among which antimicrobial is the most common. There is published research in chemistry and pharmacological activity on around 15 of the genus species, centering in their antibacterial and fungicidal activity. Additionally, a variety of active phytochemicals have been isolated, the most representative of which are atraric acid, xylosmine and its derivatives, and velutinic acid. There is still ample field for the validation and evaluation of the activity of Xylosma extracts, particularly in species not yet studied, and concerning uses other than antimicrobial and for the identification and evaluation of their active compounds.

Tragia L. Genus: Ethnopharmacological Use, Phytochemical Composition and Biological Activity.

Tragia L. is a genus of plants belonging to the Euphorbiaceae family with worldwide intertropical distribution, composed of more than 150 species. In this literature review, 26 species of the genus used as medicinal plants were found, mainly in East Africa and the Indian subcontinent, with a variety of uses among which antibacterial, anti-inflammatory, anticancer and reproductive health are most common. Research has been done on a few of the species, mostly those of the Old World, with emphasis on four of them: Tragia involucrata Linn., Tragia spathulata Benth., Tragia benthamii Baker and Tragia plukenetii Radcl.-Sm., confirming several ethnomedicinal claims. Moreover, a variety of active phytochemicals have been isolated, mainly ethers, hydrocarbons, flavonoids and sterols. There is ample field for the evaluation of the activity of Tragia extracts and essential oils and the identification of their active compounds, particularly of the New World species, for which there is still very little research.

Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis.

This work focuses on the search and development of drugs that may become new alternatives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We then characterized their potential application in therapeutic use. For this, the in vitro biological activities against three eukaryotic models-S. cerevisiae, five cancer cell lines, and the parasite L. mexicana-were evaluated. In addition, cytotoxicity against non-cancerous mammalian cells has been evaluated and other properties of interest have been characterized, such as genotoxicity, antioxidant properties and, in silico predictive adsorption, distribution, metabolism, and excretion (ADME). The results that we present here represent a first screening, indicating two derivatives of bis(spiropyrazolone)cyclopropanes as good candidates for the treatment of leishmaniasis. They have good specificity against parasites with respect to mammalian cells.

Synthesis of 4,4'-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ols) and evaluation of their antioxidant and anticancer activities.

BACKGROUND: Pyrazoles have attracted particular attention due to the diverse biological activities associated with this heterocyclic system, and some have been shown to be cytotoxic to several human cell lines. Several drugs currently on the market have this heterocycle as the key structural motif, and some have been approved for the treatment of different types of cancer. RESULTS: 4,4'-(Arylmethylene)bis(1H-pyrazol-5-ols) derivatives 3a-q were synthetized by a three components reaction of 3-methyl-1-phenyl-5-pyrazolone (1) with various benzaldehydes 2 catalyzed by sodium acetate at room temperature. The structures of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR) and were evaluated for their radical scavenging activity by DPPH assay and tested in vitro on colorectal RKO carcinoma cells in order to determine their cytotoxic properties. All 4,4'-(arylmethylene)bis(1H-pyrazol-5-ols) derivatives 3a-q were synthetized in high to excellent yield, and pure products were isolated by simple filtration. All compounds have good radical scavenging activity, and half of them are more active than ascorbic acid used as standard. CONCLUSION: Several derivatives proved to be cytotoxic in the RKO cell line. In particular, compound 3i proved to be a very potent scavenger with an IC50 of 6.2 ± 0.6 µM and exhibited an IC50 of 9.9 ± 1.1 µM against RKO cell. Autophagy proteins were activated as a survival mechanism, whereas the predominant pathway of death was p53-mediated apoptosis.

Enfermedades Genéticas: Xeroderma pigmentoso. Amor a media noche (2017) / Genetic Diseases: Xeroderma pigmentosum. Midnight Sun (2017)

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Phytochemical Study and Evaluation of the Cytotoxic Properties of Methanolic Extract from Baccharis obtusifolia.

Some species of the Baccharis genus have been shown to possess important biomedical properties, including cytotoxic activity. In this study, we examined the cytotoxic effect of methanol extract from Baccharis obtusifolia (Asteraceae) in cancer cell lines of prostate (PC-3), colon (RKO), astrocytoma (D-384), and breast (MCF-7). The methanolic extract displayed the largest substantial cytotoxic effect in lines of colon cancer (RKO) and cerebral astrocytoma (D-384). Chromatographic purification of the B. obtusifolia methanolic extract led to the isolation and identification of 5,4'-dihydroxy-7-methoxyflavone (1) and 5-hydroxy-7,4'-dimethoxyflavone (2) compounds of the flavonoid type.

Cytotoxic, antioxidative, genotoxic and antigenotoxic effects of Horchata, beverage of South Ecuador.

BACKGROUND: "Horchata" is an herbal mixture infusion consumed in Southern Ecuador; 66% of its plants are anti-inflammatory medicinal plant, and 51% are analgesics. Anti-inflammatory substances can prevent carcinogenesis mediated by cytotoxic effects and can prevent DNA damage. The aim of this study was to evaluate the cytotoxicity and apoptotic/antigenotoxic effects of horchata as well as its mechanism. METHODS: Nine different varieties of horchata were prepared in the traditional way and then freeze-dried. Phytochemical screening tested for the presence of secondary metabolites using standard procedures and antioxidant activities. The cytotoxic activity was evaluated on cerebral astrocytoma (D-384), prostate cancer (PC-3), breast cancer (MCF-7), colon cancer (RKO), lung cancer (A-549), immortalized Chinese hamster ovary cells (CHO-K1), and human peripheral blood lymphocytes via a MTS assay. The pro-apoptotic effects were evaluated with Anexin V/Propidium Iodide and western blot of Bax, Bcl-2, TP53, and TP73. Induction and reduction of ROS were assessed by fluorimetry. Genotoxic and antigenotoxic effects were evaluated with a comet assay and micronuclei on binucleated cells. RESULTS: Five of nine horchatas had cytotoxic effects against D-384 while not affecting normal cells. These horchatas induce cell death by apoptosis modulated by p53/p73. In CHO-K1 cells, the horchatas decrease the damage induced by hydrogen peroxide and Mitomycin C measured in the comet and micronucleus assay respectively. CONCLUSIONS: The IC50 range of effective horchatas in D-384 was 41 to 122 µg·mL-1. This effect may be related to its use in traditional medicine (brain tonic). On the other hand, immortalized Chinese hamster ovary cells (CHO-K1) and lymphocytes did not show a cytotoxic effect. The most potent horchata induced apoptosis via a p53/p73-mediated mechanism. The horchatas present antigenotoxic properties, which may be related to the antioxidant capacity. Future studies on horchata components are necessary to understand the interactions and beneficial properties.

Natural Compounds as Modulators of Cell Cycle Arrest: Application for Anticancer Chemotherapies.

Natural compounds from various plants, microorganisms and marine species play an important role in the discovery novel components that can be successfully used in numerous biomedical applications, including anticancer therapeutics. Since uncontrolled and rapid cell division is a hallmark of cancer, unraveling the molecular mechanisms underlying mitosis is key to understanding how various natural compounds might function as inhibitors of cell cycle progression. A number of natural compounds that inhibit the cell cycle arrest have proven effective for killing cancer cells in vitro, in vivo and in clinical settings. Significant advances that have been recently made in the understanding of molecular mechanisms underlying the cell cycle regulation using the chemotherapeutic agents is of great importance for improving the efficacy of targeted therapeutics and overcoming resistance to anticancer drugs, especially of natural origin, which inhibit the activities of cyclins and cyclin-dependent kinases, as well as other proteins and enzymes involved in proper regulation of cell cycle leading to controlled cell proliferation.

"Horchata" drink in Southern Ecuador: medicinal plants and people's wellbeing.

BACKGROUND: The "horchata" is a herbal mixture infusion consumed in Southern Ecuador. It remains unknown how vendors group the plant species to sell them at traditional markets. This research documented the following: 1) a list of medicinal plant species sold for the drink; 2) the culturally important medicinal plant species; 3) the agreement among vendors regarding the medicinal plants species and their therapeutic use; and 4) the groups of medicinal plants sold for the preparation of "horchata." METHODS: Interviews were made to 185 vendors at 31 traditional markets in Loja province. Bunches of medicinal plants were purchased to identify the species and to prepare voucher specimens. Culturally important medicinal plants species were established with the Fidelity Level (FL) index. Agreement among vendors on the therapeutic use of medicinal plants was measured with the Factor of Informant Consensus (FIC) index. A cluster analysis was made to determine the groups of medicinal plants sold by market vendors to prepare the "horchata" drink. RESULTS: In Loja province, the "horchata" drink is consumed for its therapeutic uses. This study registered 33 families with 58 genera and 71 medicinal plant species, 50 of which are herbs and three are endemic to the Andean highlands of Ecuador. The FL index (46.1-96.3) determined 20 culturally important medicinal plant species. The highest FIC value (1.00) among vendors corresponds to four plant species employed each for a different therapeutic use. The cluster analysis identified a core group of 16 plant species which are essential to the drink and which likely interact to provide wellbeing. CONCLUSIONS: The "horchata" is a heritage drink in Loja province. The 71 medicinal plants species registered for this drink is the largest number reported to date, and they have a total of 32 therapeutic uses. The combined results of the FL and FIC indices, the cluster analysis, and the field observations reveal an agreement among vendors on 16 medicinal plant species and their therapeutic use. This core group of plants requires bioactivity and bioassays analyses to determine biomedicine benefits that would be based on their pharmacological properties.

Medicinal plants used as anthelmintics: Ethnomedical, pharmacological, and phytochemical studies.

Intestinal parasites delay mental and physical development in children. Infection with these parasites can result in complications during pregnancy and alter the health of newborns, which has long-term effects on educational attainment and economic productivity. The appearance of resistance against classical drug treatments generates interest in the development of new deworming alternatives. We think that research of new plants species may reveal potential antiparasitic compounds. This review is focused on the use of plants and secondary metabolites against intestinal parasites. We discuss the use of plants in traditional medicine and the use of plant secondary metabolites tried in in vitro and in vivo models when available.

Medicinal plants sold at traditional markets in southern Ecuador.

BACKGROUND: The traditional markets in southern Ecuador and within the Andean region are especially important for plant resource trading among local people, even since before Spanish colonization; therefore, ethnobotanical studies are currently necessary and important. These strategic spaces persist for the traditional medicine cultural value reflected in the higher consumption of medicinal plants, which span all socioeconomic levels of rural and urban people. The purpose of this study includes the following: 1) to create a novel list of medicinal plants sold at 33 traditional markets; 2) to establish medicinal plant use agreement amongst vendors with the Factor of Informant Consensus (FIC); and 3) to determine the most sold medicinal plant species using the Fidelity Level (FL). METHODS: This study focus on traditional markets ethnobotany utilizes the largest sample of medicinal plants market vendors up to date in Ecuador, interviewing them at 33 traditional markets, located within the Loja province. In order to determine the most sold medicinal plants and their ethnobotanical information, structured questionnaires and personal conversations were conducted with 196 medicinal plant vendors, and voucher specimens were created. Agreement among vendors about the therapeutic use of medicinal plants was measured using the FIC, and the most sold medicinal plant species were assessed with the FL. RESULTS AND DISCUSSION: This research registered 160 medicinal plant species, grouped in 126 genera and 57 families that were sold in 33 traditional markets. The uses of medicinal plants in southern Ecuador are related to a long history of traditional medicine health practices that has persisted until today as well as high plant diversity. The 53 therapeutic uses recorded were grouped into 12 medical categories that were adapted from the World Health Organization. Three medical categories shared the highest value for FIC = 0.92, which showed a high level of agreement of market vendors for 57 medicinal plant species sold to treat ailments related with digestive, dermatological, and sensorial systems. The FL index determined 11 culturally important medicinal plant species based on the reported uses by 40 or more market vendors. Two medicinal plant species had an FL = 100 %, Matricaria recutita and Gaiadendrum punctatum, used to treat digestive and respiratory systems ailments. CONCLUSIONS: In the Loja province, people continue to consume medicinal plant species sold at local markets to treat somatic and/or psychosomatic health ailments because sociocultural customs are strongly expressed in ancestral practices of wellbeing. When the largest values of FL (60.5 %-100 %) and FIC (0.81-0.92) indexes are combined, they demonstrated agreement among 196 market vendors in the use of seven medicinal plant species that were most sold for the 12 medical categories. This study stresses how important public policies are for the trade and quality of medicinal plant resources, particularly for local people practicing auto-medication. Reasons for the maintenance of traditional markets in southern Ecuador include lower cost of medicinal plants, confidence in traditional medicine, and/or sociocultural environment. In Ecuador, the sustainable management of wild medicinal plants diversity, particularly the most sold, is crucial for its conservation in nature.

Development of anticancer drugs based on the hallmarks of tumor cells.

Cancer remains a public health problem with a high unmet medical demand. However, in recent decades, the knowledge of several functional molecular and biological traits that distinguish tumor cells from normal cells, known as the hallmarks of cancer as described by Hannahan and Weinberg, has led to new and modern therapeutic approaches against this disease. Most cancer drugs are deliberately developed for specific molecular targets that involve these hallmarks. In this review, we address the currently available cancer drugs and development of new drugs from the perspective of their interaction with these hallmarks as well as the pathways and mechanisms involved.