Diversity and Allelopathic Potential of Weeds among Panamanian Coffee Crops

Worldwide, coffee is one of the most highly consumed and produced crops. Coffee production is a significant activity in the Panamanian economy, mainly in rural communities and among indigenous groups in the Chiriquí province highlands. Weeds growing alongside coffee plants can provoke considerable economic losses for producers by interfering with the growth, development and yield of coffee crop in cultivated areas. Designing an effective program to control weeds depends on identifying the different species found in the coffee plantations. The objective of this study was to assess the biological diversity and negative allelopathic potential of weeds in a coffee field to generate enough information that would better allow farmers to control them. As a result, we identified forty-two different species of weeds in all sampling transects within the study area. Emilia sonchifolia and Impatiens walleriana were the most abundant. In respect to phytotoxic activity, Emilia sonchifolia and Hyptis capitata showed the highest activity against the seed germination of dicotyledonous species Amaranthus hypochondriacus, exhibiting IC50 values of 160 and 178 µg mL−1 , respectively. Finally, we proceeded to evaluate the organic extracts of two coffee weeds in a panel of bioassays to demonstrate to the farmers that weeds may also have useful applications for human health. Borreria verticillata showed antimalaric activity while Blechum pyramidatum displayed inhibition of the α-glucosidase enzyme. These results allow us to propose a rational and systematic management of coffee weedsWorldwide, coffee is one of the most highly consumed and produced crops. Coffee production is a significant activity in the Panamanian economy, mainly in rural communities and among indigenous groups in the Chiriquí province highlands. Weeds growing alongside coffee plants can provoke considerable economic losses for producers by interfering with the growth, development and yield of coffee crop in cultivated areas. Designing an effective program to control weeds depends on identifying the different species found in the coffee plantations. The objective of this study was to assess the biological diversity and negative allelopathic potential of weeds in a coffee field to generate enough information that would better allow farmers to control them. As a result, we identified forty-two different species of weeds in all sampling transects within the study area. Emilia sonchifolia and Impatiens walleriana were the most abundant. In respect to phytotoxic activity, Emilia sonchifolia and Hyptis capitata showed the highest activity against the seed germination of dicotyledonous species Amaranthus hypochondriacus, exhibiting IC50 values of 160 and 178 µg mL−1 , respectively. Finally, we proceeded to evaluate the organic extracts of two coffee weeds in a panel of bioassays to demonstrate to the farmers that weeds may also have useful applications for human health. Borreria verticillata showed antimalaric activity while Blechum pyramidatum displayed inhibition of the α-glucosidase enzyme. These results allow us to propose a rational and systematic management of coffee weed

α-Glucosidase Inhibitor Isolated from Blechum pyramidatum

Blechum pyramidatum (Lam.) Urb. is a species of extensive medicinal use in the American continent. In fact, antidiabetic and anticancer preparations from this plant have been patented in Mexico, even though their active constituents are not yet known. It was recently discovered that B. pyramidatum inhibits the action of the -glucosidase enzyme, thereby corroborating the antidiabetic properties attributed to this plant. The primary purpose of this study was to identify and characterize the -glucosidase inhibitors from this species. Bioassay-guided fractionation of a crude extract of B. pyramidatum led to the isolation of a main - glucosidase inhibitor, Palmitic acid (IC50 237.5). This compound was identified by both spectroscopic and spectrometric analysis. Its inhibitory activity was similar to that of the antidiabetic drug acarbose (IC50 241.6 µM), which was used as a positive control in our bioassay. Kinetic analysis established that palmitic acid acted as a competitive inhibitor. Docking analysis predicted that this compound binds to the same site as acarbose does in the human intestinal α‑glucosidase (PDB: 3TOP). The presence of palmitic acid in B. pyramidatum and its potent inhibitory activity against α‑glucosidase enzyme provides solid evidence to support the antidiabetic use of this plant in traditional medicinBlechum pyramidatum (Lam.) Urb. is a species of extensive medicinal use in the American continent. In fact, antidiabetic and anticancer preparations from this plant have been patented in Mexico, even though their active constituents are not yet known. It was recently discovered that B. pyramidatum inhibits the action of the -glucosidase enzyme, thereby corroborating the antidiabetic properties attributed to this plant. The primary purpose of this study was to identify and characterize the -glucosidase inhibitors from this species. Bioassay-guided fractionation of a crude extract of B. pyramidatum led to the isolation of a main - glucosidase inhibitor, Palmitic acid (IC50 237.5). This compound was identified by both spectroscopic and spectrometric analysis. Its inhibitory activity was similar to that of the antidiabetic drug acarbose (IC50 241.6 µM), which was used as a positive control in our bioassay. Kinetic analysis established that palmitic acid acted as a competitive inhibitor. Docking analysis predicted that this compound binds to the same site as acarbose does in the human intestinal α‑glucosidase (PDB: 3TOP). The presence of palmitic acid in B. pyramidatum and its potent inhibitory activity against α‑glucosidase enzyme provides solid evidence to support the antidiabetic use of this plant in traditional medici

Evaluation of antiparasitic, anticancer, antimicrobial and hypoglycemic properties of organic extracts from Panamanian mangrove plants

To investigate 33 organic extracts of mangrove plants for: antiparasitic, anticancer, and antibacterial activities, as well as their ability to inhibit the activity of the 毩-glucosidase enzyme. Methods: Leaves from all different plant mangrove species located in five mangrove zones of the Pacific coast of Panama were collected according to standard procedures. Qualitative phytochemical analysis of the organic extracts was performed by thin layer chromatography. The antiparasitic activity against Plasmodium falciparum, Trypanosoma cruzi and Leishmania donovani, toxicity against Artemia salina, anticancer activity in MCF-7 cell line, and antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa of all organic extract were investigated according protocols stablished in our institution. Finally, the ability to inhibit the enzymatic activity of 毩-glucosidase was evaluated by monitoring the hydrolysis of p-nitrophenyl 毩-Dglucopyranoside. Results: Thirty-three different samples belonging to nine different species of vascular plants with seeds of true mangroves were collected. Triterpenoids, phenolics, and tannins were the main groups of compounds found in the sampled mangroves. Saponins, quinones, and coumarins were found in less than 50% of the samples. Laguncularia racemosa showed moderate activity against Plasmodium falciparum. None of the extracts presented anticancer activity. Rhizophora mangle exhibited potent activity against Staphylococcus aureus and Bacillus subtilis [(90.41±7.33)% and (96.02±6.14)% of inhibition]; Avicennia germinans and Conocarpus erectus had activity against Escherichia coli [(71.17±6.15)% and (60.60±5.13)% of inhibition, respectively]. About 60% of the mangroves showed 毩-glucosidase inhibitory activity. In particular, extracts from Laguncularia racemosa, Pelliciera rhizophorae, Conocarpus erectus, Mora oleifera, and Tabebuia palustris species showed 毩-glucosidase inhibitory potential, with IC50 values of (29.45±0.29), (20.60±0.70), (730.06±3.74), (25.59±0.37), and (853.39±5.30) µg/mL, respectively. Conclusions: Panamanian mangroves are mainly a promising potential source of hypoglycemic compounds, specifically 毩-glucosidase inhibitors. These results highlight the therapeutic virtues of extracts from American mangrove plants.To investigate 33 organic extracts of mangrove plants for: antiparasitic, anticancer, and antibacterial activities, as well as their ability to inhibit the activity of the 毩-glucosidase enzyme. Methods: Leaves from all different plant mangrove species located in five mangrove zones of the Pacific coast of Panama were collected according to standard procedures. Qualitative phytochemical analysis of the organic extracts was performed by thin layer chromatography. The antiparasitic activity against Plasmodium falciparum, Trypanosoma cruzi and Leishmania donovani, toxicity against Artemia salina, anticancer activity in MCF-7 cell line, and antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa of all organic extract were investigated according protocols stablished in our institution. Finally, the ability to inhibit the enzymatic activity of 毩-glucosidase was evaluated by monitoring the hydrolysis of p-nitrophenyl 毩-Dglucopyranoside. Results: Thirty-three different samples belonging to nine different species of vascular plants with seeds of true mangroves were collected. Triterpenoids, phenolics, and tannins were the main groups of compounds found in the sampled mangroves. Saponins, quinones, and coumarins were found in less than 50% of the samples. Laguncularia racemosa showed moderate activity against Plasmodium falciparum. None of the extracts presented anticancer activity. Rhizophora mangle exhibited potent activity against Staphylococcus aureus and Bacillus subtilis [(90.41±7.33)% and (96.02±6.14)% of inhibition]; Avicennia germinans and Conocarpus erectus had activity against Escherichia coli [(71.17±6.15)% and (60.60±5.13)% of inhibition, respectively]. About 60% of the mangroves showed 毩-glucosidase inhibitory activity. In particular, extracts from Laguncularia racemosa, Pelliciera rhizophorae, Conocarpus erectus, Mora oleifera, and Tabebuia palustris species showed 毩-glucosidase inhibitory potential, with IC50 values of (29.45±0.29), (20.60±0.70), (730.06±3.74), (25.59±0.37), and (853.39±5.30) µg/mL, respectively. Conclusions: Panamanian mangroves are mainly a promising potential source of hypoglycemic compounds, specifically 毩-glucosidase inhibitors. These results highlight the therapeutic virtues of extracts from American mangrove plants

Antiparasitic Compounds from the Panamanian Marine Bacterium Pseudomonas aeruginosa

Fractionation of the ethyl acetate extract of the bacterium Pseudomonas aeruginosa led to the isolation of five compounds, cyclo –(L-Phe-L-Pro) (1), 3-heptyl-3-hydroxy-1,2,3,4-tetrahydroquinoline-2.4-dione (2), 2-heptyl-4-hydroxyquinoline (3), 2-nonyl-4-hydroxyquinoline (4), and 1-phenazinecarboxylic acid (5). The structures of compounds 1-5 were established by spectroscopic analyses. Compounds 2 4 produced inhibition on the growth of Plasmodium falciparum, with IC50 values of 3.47, 2.57 and 2.79 μg/mL, respectively. Compounds 3-4 had activity against Trypanosoma cruzi, with IC50 values of 3.66 and 3.99 μg/mL. Finally, all compounds were found inactive when tested against Leishmania donovani at 10 μg/mL.Fractionation of the ethyl acetate extract of the bacterium Pseudomonas aeruginosa led to the isolation of five compounds, cyclo –(L-Phe-L-Pro) (1), 3-heptyl-3-hydroxy-1,2,3,4-tetrahydroquinoline-2.4-dione (2), 2-heptyl-4-hydroxyquinoline (3), 2-nonyl-4-hydroxyquinoline (4), and 1-phenazinecarboxylic acid (5). The structures of compounds 1-5 were established by spectroscopic analyses. Compounds 2 4 produced inhibition on the growth of Plasmodium falciparum, with IC50 values of 3.47, 2.57 and 2.79 μg/mL, respectively. Compounds 3-4 had activity against Trypanosoma cruzi, with IC50 values of 3.66 and 3.99 μg/mL. Finally, all compounds were found inactive when tested against Leishmania donovani at 10 μg/mL

Screening and evaluation of antiparasitic and in vitro anticancer activities of Panamanian endophytic fungi

Many compounds produced by fungi have relevant pharmaceutical applications. The purpose of this study was to collect and isolate endophytic fungi from different regions of Panama and then to test their potential therapeutic activities against Leishmania donovani, Plasmodium falciparum, and Trypanosoma cruzi as well as their anticancer activities in MCF-7 cells. Of the 25 fungal isolates obtained, ten of them had good anti-parasitic potential, showing selective activity against L. donovani; four had significant anti-malarial activity; and three inhibited the growth of T. cruzi. Anticancer activity was demonstrated in four isolates. Of the active isolates, Edenia sp. strain F0755, Xylaria sp. strain F1220, Aspergillus sp. strain F1544, Mycoleptodiscus sp. strain F0194, Phomopsis sp. strain F1566, Pycnoporus sp. strain F0305, and Diaporthe sp. strain F1647 showed the most promise based on their selective bioactivity and lack of toxicity in the assays.Many compounds produced by fungi have relevant pharmaceutical applications. The purpose of this study was to collect and isolate endophytic fungi from different regions of Panama and then to test their potential therapeutic activities against Leishmania donovani, Plasmodium falciparum, and Trypanosoma cruzi as well as their anticancer activities in MCF-7 cells. Of the 25 fungal isolates obtained, ten of them had good anti-parasitic potential, showing selective activity against L. donovani; four had significant anti-malarial activity; and three inhibited the growth of T. cruzi. Anticancer activity was demonstrated in four isolates. Of the active isolates, Edenia sp. strain F0755, Xylaria sp. strain F1220, Aspergillus sp. strain F1544, Mycoleptodiscus sp. strain F0194, Phomopsis sp. strain F1566, Pycnoporus sp. strain F0305, and Diaporthe sp. strain F1647 showed the most promise based on their selective bioactivity and lack of toxicity in the assays

Screening and evaluation of antiparasitic and in vitro anticancer activities of Panamanian endophytic fungi

Parasitic infections are major causes of human chronic diseases in most countries of the tropics. The parasites include protozoa and helminths, infect billions of people, and the resulting diseases cause debilitating injuries such as blind ness and disfigurement, or death in millions of people. According to World Health Organization (WHO) estimates, 25% of the human population is infected with parasitic worms. However, attempts to develop vaccines against these pathogens have been frustrated by the difficulty of cultivating the parasites in the laboratory, the complexity of their multicellular organization and—in many species—their multistage development, in addition to their impressive antigenic variability [http://www.who.int/vaccine_research/diseases/ soa_parasitic/en/index.html]. Malaria is the most dangerous parasitic disease, as evidenced by the high rates of complications and mortality caused by the most fatal species, Plasmodium falciparum [15]. Chagas disease, or American trypanosomiasis, is a potentially life-threatening two-phase illness caused by the protozoan Trypanosoma cruzi. The acute phase persists for about two months after infection; symptoms are absent or mild and can include fever, headache, enlarged lymph glands, pallor, muscle pain, difficulty in breathing, swelling, and abdominal or chest pain. In the chronic phase, the parasites reside mainly in the heart and digestive muscle, resulting in cardiac disorders in up to 30% of patients and digestive, neurological, or mixed pathologies in up to 10%. Eventually, the infection can lead to sudden death or heart failure, caused by progressive destruction of cardiac muscle [10,15]. Leishmaniasis, a worldwide disease, is caused by several species of the flagellated protozoan parasite Leishmania. In its more severe forms, the disease causes serious disfigurement and may be fatal. The WHO estimates a worldwide prevalence of leishmaniasis of approximately 12 million cases, with an annual mortality of about 60,000 and approximately 350 million people at risk. The expansion of leishmaniasis and the alarming rise in the number of cases has been attributed to environmental changes, such as deforestation, dam construction, new irrigation schemes, and the migration of non-immune individuals to endemic areas [10,15]. At the same time, the frequency of drug-resistant parasites has greatly increased and most treatments involve highly toxic drugs. In addition, the chemotherapeutic agents used in patients with these diseases have lacked effectiveness. Thus, there is an urgent need to search for novel drugs from previously unexplored sources, including natural products, to combat the global health problems posed by parasitic infections. Cancer is another major cause of mortality worldwide; in 2008, it accounted for 7.6 million deaths. According to WHO forecasts, an increase to 11 million deaths annually is expected by 2030. The prevalence is higher in low and middle-income countries. As a part of the on-going research activities, the Panamanian International Cooperative Biodiversity Group (ICBG) [17] recently decided to explore endophytic fungi as a source of molecules with antiparasitic and anticancer bioactivities [18,21,22]. Within the ICBG program, we have assayed the antiparasitic and in vitro anticancer activities of 25 isolates, while also analyzing the effect of the culture medium on the production of secondary metabolites by Panamanian endophytic fungi. The results of these studies are reported and discussed hereinParasitic infections are major causes of human chronic diseases in most countries of the tropics. The parasites include protozoa and helminths, infect billions of people, and the resulting diseases cause debilitating injuries such as blind ness and disfigurement, or death in millions of people. According to World Health Organization (WHO) estimates, 25% of the human population is infected with parasitic worms. However, attempts to develop vaccines against these pathogens have been frustrated by the difficulty of cultivating the parasites in the laboratory, the complexity of their multicellular organization and—in many species—their multistage development, in addition to their impressive antigenic variability [http://www.who.int/vaccine_research/diseases/ soa_parasitic/en/index.html]. Malaria is the most dangerous parasitic disease, as evidenced by the high rates of complications and mortality caused by the most fatal species, Plasmodium falciparum [15]. Chagas disease, or American trypanosomiasis, is a potentially life-threatening two-phase illness caused by the protozoan Trypanosoma cruzi. The acute phase persists for about two months after infection; symptoms are absent or mild and can include fever, headache, enlarged lymph glands, pallor, muscle pain, difficulty in breathing, swelling, and abdominal or chest pain. In the chronic phase, the parasites reside mainly in the heart and digestive muscle, resulting in cardiac disorders in up to 30% of patients and digestive, neurological, or mixed pathologies in up to 10%. Eventually, the infection can lead to sudden death or heart failure, caused by progressive destruction of cardiac muscle [10,15]. Leishmaniasis, a worldwide disease, is caused by several species of the flagellated protozoan parasite Leishmania. In its more severe forms, the disease causes serious disfigurement and may be fatal. The WHO estimates a worldwide prevalence of leishmaniasis of approximately 12 million cases, with an annual mortality of about 60,000 and approximately 350 million people at risk. The expansion of leishmaniasis and the alarming rise in the number of cases has been attributed to environmental changes, such as deforestation, dam construction, new irrigation schemes, and the migration of non-immune individuals to endemic areas [10,15]. At the same time, the frequency of drug-resistant parasites has greatly increased and most treatments involve highly toxic drugs. In addition, the chemotherapeutic agents used in patients with these diseases have lacked effectiveness. Thus, there is an urgent need to search for novel drugs from previously unexplored sources, including natural products, to combat the global health problems posed by parasitic infections. Cancer is another major cause of mortality worldwide; in 2008, it accounted for 7.6 million deaths. According to WHO forecasts, an increase to 11 million deaths annually is expected by 2030. The prevalence is higher in low and middle-income countries. As a part of the on-going research activities, the Panamanian International Cooperative Biodiversity Group (ICBG) [17] recently decided to explore endophytic fungi as a source of molecules with antiparasitic and anticancer bioactivities [18,21,22]. Within the ICBG program, we have assayed the antiparasitic and in vitro anticancer activities of 25 isolates, while also analyzing the effect of the culture medium on the production of secondary metabolites by Panamanian endophytic fungi. The results of these studies are reported and discussed herei

Marine Natural Products as Breast Cancer Resistance Protein Inhibitors

Breast cancer resistance protein (BCRP) is a protein belonging to the ATP-binding cassette (ABC) transporter superfamily that has clinical relevance due to its multi-drug resistance properties in cancer. BCRP can be associated with clinical cancer drug resistance, in particular acute myelogenous or acute lymphocytic leukemias. The overexpression of BCRP contributes to the resistance of several chemotherapeutic drugs, such as topotecan, methotrexate, mitoxantrone, doxorubicin and daunorubicin. The Food and Drugs Administration has already recognized that BCRP is clinically one of the most important drug transporters, mainly because it leads to a reduction of clinical efficacy of various anticancer drugs through its ATP-dependent drug efflux pump function as well as its apparent participation in drug resistance. This review article aims to summarize the different research findings on marine natural products with BCRP inhibiting activity. In this sense, the potential modulation of physiological targets of BCRP by natural or synthetic compounds offers a great possibility for the discovery of new drugs and valuable research tools to recognize the function of the complex ABC-transporters

Newton's Method

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α-Glucosidase inhibitors from a mangrove associated fungus, Zasmidium sp. strain EM5-10

Abstract Background Mangroves plants and their endophytes represent a natural source of novel and bioactive compounds. In our ongoing research on mangrove endophytes from the Panamanian Pacific Coast, we have identified several bioactive endophytic fungi. From these organisms, an isolate belonging to the genus Zasmidium (Mycosphaerellaceae) showed 91.3% of inhibition against α-glucosidase enzyme in vitro. Results Zasmidium sp. strain EM5-10 was isolated from mature leaves of Laguncularia racemosa, and its crude extract showed good inhibition against α-glucosidase enzyme (91.3% of inhibition). Bioassay-guided fractionation of the crude extract led to obtaining two active fractions: L (tripalmitin) and M (Fungal Tryglicerides Mixture). Tripalmitin (3.75 µM) showed better inhibitory activity than acarbose (positive control, IC50 217.71 µM). Kinetic analysis established that tripalmitin acted as a mixed inhibitor. Molecular docking and molecular dynamics simulations predicted that tripalmitin binds at the same site as acarbose and also to an allosteric site in the human intestinal α-glucosidase (PDB: 3TOP). Conclusions Zasmidium sp. strain EM5-10 represents a new source of bioactive substances that could possess beneficial properties for human health