Antioxidant and antidiabetic activity and phytoconstituents of lichen extracts with temperate and polar distribution.

The objective of this research was to characterize the chemical composition of ethanolic extracts of the lichen species Placopsis contortuplicata, Ochrolechia frigida, and Umbilicaria antarctica, their antioxidant activity, and enzymatic inhibition through in vitro and molecular docking analysis. In total phenol content, FRAP, ORAC, and DPPH assays, the extracts showed significant antioxidant activity, and in in vitro assays for the inhibition of pancreatic lipase, α-glucosidase, and α-amylase enzymes, together with in silico studies for the prediction of pharmacokinetic properties, toxicity risks, and intermolecular interactions of compounds, the extracts evidenced inhibitory potential. A total of 13 compounds were identified by UHPLC-ESI-QTOF-MS in P. contortuplicata, 18 compounds in O. frigida, and 12 compounds in U. antarctica. This study contributes to the knowledge of the pool of bioactive compounds present in lichens of temperate and polar distribution and biological characteristics that increase interest in the discovery of natural products that offer alternatives for treatment studies of diseases related to oxidative stress and metabolic syndrome.

Chemical Fingerprinting, Aorta Endothelium Relaxation Effect, and Enzymatic Inhibition of Canelo (Drimys winteri J. R. Forst. & G. Forst, (D.C) A. Gray, Family Winteraceae) Fruits.

Drimys winteri J.R. Forst. & G. Forst (D.C) G. Gray, var. chilensis (canelo) is an endemic tree from Chile. Since pre-Columbian times, it has produced a fruit known as the canelo pepper, (pimienta de canelo) or Foye pepper, which can be used as a spice. The chemical and biological analysis of canelo fruits is reported for the first time in this study, that is, its phenolic fingerprinting by UHPLC-PDA- Q-orbitrap MS, the antioxidant activity, the enzymatic inhibitory activity, and its relaxation effects on rat aorta. The proximal composition and the mineral content (Ca: 1.45 ± 0.03 mg/100 g; Mg: 7.72 ± 0.03 mg/100 g; Fe: 4.54 ± 0.21 mg/100 g; Zn: 2.99 ± 0.02 mg/100 g; Mn: 1.08 ± 0.03 mg/100 g; Cu: 0.82 ± 0.02 mg/100 g; K: 53.03 ± 0.20 mg/100 g; Na: 0.087 ± 0.00 mg/100 g) are also reported. The canelo fruits showed a total phenolic content of 57.33 ± 0.82 mg GAE/g dry weight. In addition, the total flavonoid content was 38.42 ± 1.32 mg equivalent of QE/g dry weight. The antioxidant activity was evaluated by employing DPPH and ABTS methods (IC50 of 6.65 ± 0.5 and 9.5 ± 0.05 µg/mL, respectively), ORAC (25.33 ± 1.2 µmol Trolox/g dry plant) and FRAP (45.56 ± 1.32 µmol Trolox/g dry plant). The enzymatic inhibition of acetylcholinesterase, butyrylcholinesterase, and tyrosinase (IC50: 1.94 ± 0.07, 2.73 ± 0.05, and 9.92 ± 0.05 µg extract/mL, respectively) is also reported. Canelo extract led to an 89% relaxation of rat aorta. Our results confirm that D. winteri fruits are a rich source of secondary metabolites and can inhibit enzymes associated with neurodegenerative diseases; the results also suggest that canelo may induce a potentially hypotensive effect in rat aorta. The study demonstrates the medicinal properties of canelo fruit and spice.

Antioxidant, Antiproliferative and Anti-Enzymatic Capacities, Nutritional Analysis and UHPLC-PDA-MS Characterization of Ungurahui Palm Fruits (Oenocarpus bataua Mart) from the Peruvian Amazon.

Ungurahui, or Patawa, fruits are a popular fruit and medicinal food used in the Amazon. Here, we have studied nine natural populations of ungurahui from the Peruvian Amazon regarding their nutritional and biological activities, including metal composition, proximal analyses, cytotoxic, antioxidant and cholinesterase inhibition activities. Twenty-four compounds have been detected in these Peruvian natural populations by UHPLC-MS, including nine phenolic acids (peaks 1-6, 8, 9 and 11), four C-glycosyl flavonoids (peaks 12, 16, 17 and 18), two flavonols (peaks 7 and 10), one flavanol (peak 15), three anthocyanins (peaks 13, 14 and 22) and five resveratrol derivatives (peaks 19-21, 23 and 24). Sample 9, Tunaants, showed the highest DPPH clearing capacity regarding the content of Trolox equivalents (2208.79 µmol Trolox/g), but an ORAC test of the sample collected in San Lorenzo showed the highest clearing activity (1222.28 µmol Trolox/g) and the sample collected in Allpahuayo Mishana showed the most powerful ABTS (1803.72 µmol Trolox/g). The sample from Jenaro Herrera was the most powerful in AChe inhibition (IC50 2.05 ± 0.03 µg/mL), followed by the sample from Contamana (IC50 2.43 ± 0.12 µg/mL). In BChE inhibition, the sample from Palestina was the most active (4.42 ± 0.06 µg/mL), followed by samples from Tunaants and San Lorenzo. The differences among bioactivities can be related to the different growing conditions of the populations of ungurahui. The palm tree fruit proved to be a good source of natural antioxidants and dietary fatty acids, and their consumption represents an alternative for the prevention of neurodegenerative or related non-chronic transmittable diseases.

UHPLC-MS Characterization, and Antioxidant and Nutritional Analysis of Cocoa Waste Flours from the Peruvian Amazon.

Cocoa (Theobroma cacao) is a food product used worldwide and a key raw material for chocolate manufacturing. Cocoa possesses bioactive compounds such as methylxanthines, flavonoids, procyanidins, and related molecules with medicinal or health-promoting properties. Cocoa shell and pod husk have been proposed as a by-product with several interesting bioactivities, and the gummy residue or glue (a sticky, gluey by-product known as "mucilage" in Spanish) is used to produce liquors and is eaten as a food in Perú. However, little is known about the chemical composition and bioactivity of flours made from Peruvian cocoa ecotype wastes such as those from the vein and pod husk of the fruits. This study aimed to characterize the in vitro antioxidant properties and nutritional values of flours made from the waste from a special ecotype of cocoa (CCN-51). The chemical fingerprinting was performed using UHPLC-HESI orbitrap mass spectrometry and allowed the detection of 51 compounds. GC-FID was used for the determination of individual fatty acid contents, and the antioxidant activity was assessed by several assays (DPPH, FRAP, and ABTS). The flours obtained were composed of a good amount of dietary fiber, carbohydrates, and minerals, as well as several bioactive polyphenolic compounds, fatty acids, and amino acids with nutraceutical properties, making the flours a rich and promising food as well as a good source for the preparation of functional foods or nutraceuticals.

UHPLC-MS Chemical Fingerprinting and Antioxidant, Enzyme Inhibition, Anti-Inflammatory In Silico and Cytoprotective Activities of Cladonia chlorophaea and C. gracilis (Cladoniaceae) from Antarctica.

The lichen species Cladonia chlorophaea and C. gracilis (Cladoniaceae) are widely distributed in the island archipelago of maritime Antarctica and represent a natural resource of scientific interest. In this work, the metabolomic characterization of the ethanolic extracts of these species and the determination of the antioxidant activity, enzymatic inhibition and anti-inflammatory potential of selected compounds on the 5-lipoxygenase enzyme by molecular docking and cytoprotective activity in the SH-SY5Y cell line were carried out. Nineteen compounds were identified by liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry (UHPLC-ESI-QTOF-MS) in each of the species. The contents of phenolic compounds, antioxidant activity, the inhibition of cholinesterases (acetylcholinesterase and butyrylcholinesterase) and digestive enzymes (α-glucosidase and pancreatic lipase) were variable among species, with better results in C. chlorophaea. Molecular docking evidenced significant binding affinities of some compounds for the 5-lipoxygenase enzyme, together with outstanding pharmacokinetic properties. Both extracts were shown to promote cell viability and a reduction in reactive oxygen species production in an H2O2-induced oxidative stress model. This study contributes to the chemical knowledge of the Cladonia species and demonstrates the biological potential for the prevention and promising treatment of central nervous system pathologies, inflammatory disorders and metabolic alterations.

Antihyperlipidemic and Antioxidant Capacities, Nutritional Analysis and UHPLC-PDA-MS Characterization of Cocona Fruits (Solanum sessiliflorum Dunal) from the Peruvian Amazon.

Cocona fruits are a popular food and medicinal fruit used mainly in the Amazon and several countries of South America for the preparation of several food products such as drinks, jams and milk shakes. In this study five ecotypes of cocona native to Peru have been studied regarding their nutritional and antioxidants values plus antihyperlipidemic activities. Seventy bioactive compounds have been detected in Peruvian cocona ecotypes including several phenolic acids, aminoacids and flavonoids; of those six were spermidines, (peaks 1, 2, 25, 26, 38 and 39), thirteen were aminoacids, (peaks 3-9, 11-13, 16, 17, 22-24), eighteen flavonoids (peaks 28, 30-32 45,46, 48-53 56, 57, 61 and 64-66), twelve were phenolics (peaks 19, 21, 27, 29, 34, 35, 36, 42, 43, 44, 54, and 59), two carotenoids, (peak 62 and 63), eight were lipid derivatives (peaks 37, 55, 58, 60 and 67-70), one sugar (peak 47), four terpenes (peaks 33, 40, 41 and 47), two amides, (peaks 10 and 18), one aldehyde, (peak 15), and three saturated organic acids, (peaks 4, 5 and 20). Hypercholesterolemic rats administered with pulp of the ecotypes CTR and SRN9 showed the lowest cholesterol and triglyceride levels after treatment (126.74 ± 6.63; 102.11 ± 9.47; 58.16 ± 6.64; 61.05 ± 4.00 mg/dL, for cholesterol, triglycerides, high-density lipoprotein and low-density lipoprotein respectively, for the group treated with SRN9 pulp, and 130.09 ± 8.55; 108.51 ± 10.04; 57.30 ± 5.72; and 65.41 ± 7.68 mg/dL, for cholesterol, triglycerides, HDL and LDL lipoproteins respectively for the group treated with CTR pulp). The ecotypes proved to be good sources of natural antioxidants and their consumption represent an alternative for the prevention of atherosclerosis.

Nutritional evaluation and human health-promoting potential of compounds biosynthesized by native microalgae from the Peruvian Amazon.

A plausible strategy to mitigate socioeconomic problems in the Peruvian Amazon is through the sustainable exploitation of biodiversity resources, such as native microalgae. Several studies worldwide affirm that these microorganisms are excellent sources of higher value products for human nutrition and possess health-promoting biochemicals, but these attributes are unknown for the native microalgae of Peru. Therefore, the aim of this investigation was to evaluate the nutritional and human health-promoting potential of compounds biosynthesized by native microalgae from the Peruvian Amazon. Ten native microalgae strains of the groups cyanobacteria and chlorophyta were cultured in BG-11 medium and their biomass harvested and dried. Standardized methods were then used to determine proximate composition, fatty acids and amino acids composition, antioxidant activity, and total phenolic content. All ten microalgae strains produce primary nutrients, the entire spectrum of essential amino acids, essential fatty acids, and 3 of the 10 microalgae strains produced eisosapentaenoic acid. Additionally, all microalgae strains exhibited antioxidant activities and contained phenolic compounds. In conclusion, native microalgae strains from the Peruvian Amazon analyzed in this study possess the ability to biosynthesize and accumulate several nutrients and compounds with human health-promoting potential.

Male sexual enhancers from the Peruvian Amazon.

ETHNOPHARMACOLOGICAL RELEVANCE: Selected Peruvian Amazon plants are macerated into sugar cane distillates to prepare alcoholic beverages used to improve male sexual performance. The tree bark from Campsiandra angustifolia Spruce ex Benth (Fabaceae), Swartzia polyphylla DC (Fabaceae), Minquartia guianensis Aubl. (Olacaceae) and Thynantus panurensis (Bureau) Sandwith (Bignoniaceae) usually are used as crude drugs in mixtures of several ingredients. AIM OF STUDY: Describe the chemical composition of the most traded traditional male enhancer beverages, namely "Levántate Lazaro" and "Siete veces sin sacarla", and their single crude drug constituents, as well as their inhibitory activity towards the enzyme phosphodiesterase-5. The presence of pro-sexual drugs such as Sildenafil® and derivatives was assessed in the samples. MATERIALS AND METHODS: Single plant constituents and the preparation mixtures were purchased in the Mercado Belen (Iquitos, Peru). Chemical profiling was carried out by HPLC-DAD-ESI-MS/MS. The extracts were assessed for phosphodiesterase-5 inhibition. The occurrence of pro-sexual drugs was determined by HPLC-DAD-ESI-MS/MS. RESULTS: Chemical profiling allowed the identification of condensed tannins as the main constituents of C. angustifolia and S. polyphylla, hydrolysable tannins for M. guianensis, and C-glycosides for T. panurensis. The traditional preparations showed similar composition compared to the crude drugs. At 200 µg/mL, the traditional preparation "Levántate Lázaro" and "Siete veces sin sacarla" inhibited the phosphodiesterase-5 by 49.88% and 27.90%, respectively. No adulterations with pro-sexual drugs were found in the samples. From the crude drugs, low effect was found for the extracts of S. polyphylla and T. panurensis and high activity for C. angustifolia which inhibited the enzyme by 89.37% and 81.32% at 200 and 100 µg/mL, respectively. CONCLUSION: The traditional preparations used to improve sexual performance in the Peruvian Amazon showed activity as phosphodiesterase-5 inhibitors. The most active ingredient of the traditional preparations was C. angustifolia, with some contribution from T. panurensis. These results encourage additional studies, including animal models to confirm the male enhancer effect of the preparations.

Saberes ancestrales sobre el uso de flora y fauna en la comunidad indígena Tikuna de Cushillo Cocha, zona fronteriza Perú-Colombia-Brasil / Ancestral knowledge about the use of flora and fauna in the Tikuna indigenous community of Cushillo Cocha, Peru-Colombia-Brazil border area

En el presente estudio se reportan los conocimientos ancestrales indígenas (etnoconocimientos) de la comunidad indígena Tikuna de Cushillo Cocha. La comunidad está ubicada en la provincia de Ramón Castilla, al nororiente de la Región Loreto, Perú. La recolección de datos se realizó a través de talleres participativos, entrevistas y recorridos biológicos para realizar la recolectar de especies vegetales, observar a animales in situ, acompañados por los pobladores con experiencia y conocimiento de su territorio. Un total de 247 especies de flora y fauna fueron registradas. En etnobotánica se identificaron 101 especies, en siete categorías de uso asignados por los pobladores, siendo las categorías de alimentación y medicinal las de mayor representatividad. Para el caso de etnozoología se identificaron 146 especies, que son utilizadas en seis categorías, siendo las de mayor relevancia las categorías de alimentación y mascotas. Se evidenció que el bosque es la fuente principal para la alimentación, cura de enfermedades, elaboración de artesanías, como mascotas para la venta y plantas como ornamentales, todo esto con importante aceptación por parte de la población indígena.

Anti-inflammatory activity of animal oils from the Peruvian Amazon.

ETHNOPHARMACOLOGICAL RELEVANCE: Animal oils and fats from the fishes Electrophorus electricus and Potamotrygon motoro, the reptiles Boa constrictor, Chelonoidis denticulata (Geochelone denticulata) and Melanosuchus niger and the riverine dolphin Inia geoffrensis are used as anti-inflammatory agents in the Peruvian Amazon. The aim of the study was to assess the topic anti-inflammatory effect of the oils/fats as well as to evaluate its antimicrobial activity and fatty acid composition. MATERIALS AND METHODS: The oils/fats were purchased from a traditional store at the Iquitos market of Belen, Peru. The topic anti-inflammatory effect was evaluated by the mice ear edema induced by arachidonic acid (AA) and 12-O-tetradecanoylphorbol-13-acetate (TPA) at the dose of 3mg oil/ear. Indomethacine and nimesulide were used as reference anti-inflammatory drugs. The application resembles the traditional topical use of the oils. The antimicrobial effect of the oils/fats was assessed by the microdilution test against reference strains of Escherichia coli, Staphylococcus aureus and Salmonella enteritidis. The fatty acid composition of the oils/fats (as methyl esters) was determined by GC and GC-MS analysis after saponification. RESULTS: All oils/fats showed topic anti-inflammatory activity, with better effect in the TPA-induced mice ear edema assay. The most active drugs were Potamotrygon motoro, Melanosuchus niger and Geochelone denticulata. In the AA-induced assay, the best activity was found for Potamotrygon motoro and Electrophorus electricus oil. The oil of Electrophorus electricus also showed a weak antimicrobial effect with MIC values of 250 µg/mL against Escherichia coli ATCC 25922 and Salmonella enteritidis-MI. The main fatty acids in the oils were oleic, palmitic and linoleic acids. CONCLUSIONS: Topical application of all the oils/fats investigated showed anti-inflammatory activity in the mice ear edema assay. The effect can be related with the identity and composition of the fatty acids in the samples. This study gives support to the traditional use of animal oils/fats as ant-inflammatory agents in the Peruvian Amazon. However, new alternative should be encouraged due to the conservation status of several of the animal sources of the crude drugs.

Usos tradicionales, fitoquímica y farmacología de la bolsa mullaca (Physalis angulata L. ) / Physalis angulata L. (bolsa mullaca): usos tra-dicionais, fitoquímica e farmacologia / Physalis angulata L. (bolsa mullaca): a review of its traditional uses, chemistry and pharmacology

Physalis angulata es una hierba anual usada ampliamente, en la medicina popular para el tratamiento de una variedad de patologías. La presente revisión muestra las investigaciones realizadas durante los últimos 30 años, sobre sus usos tradicionales, componentes químicos y farmacología de esta especie. Los estudios referidos a los usos tradicionales, muestran que la especie es conocida por propiedades antimaláricas, antiinflamatorias y en el tratamiento de postparto. Así mismo se muestran los diferentes experimentos farmacológicos de ensayos in vitro y de modelos in vivo que se han realizado, la identificación de sus constituyentes fitoquímicos con importancia medicinal, siendo los principales las fisalinas y los witanólidos. Los estudios farmacológicos revelan que tiene actividad antiparasitaria, antiinflamatoria, antimicrobiana, antinociceptiva, antimalárica, antileishmania, inmunosupresora, antiasmática, diurética y antitumoral, validando de esta manera sus usos tradicionales y demostrando el gran potencial que tiene esta especie, para un mayor desarrollo dentro de la industria farmacéutica (AU)

Physalis angulata é uma erva anual amplamente utilizada na medicina popular para o tratamento de uma variedade de patologias. A presente revisão mostra a investigação realizada durante os últimos 30 anos sobre os seus usos tradicionais, constituintes químicos e farmacologia. Os estudos relacionados com os usos tradicionais mostram que P. angulata é conhecida pelas suas propriedades antimaláricas, anti-inflamatórias e no tratamento do pós-parto. Também se apresentam diferentes ensaios farmacológicos realizados in vitro e em modelos in vivo, bem como a identificação dos seus constituintes químicos com importância medicinal, principalmente as fisalinas e os witanólidos. Os estudos farmacológicos revelam que tem actividade antiparasitária, anti-inflamatória, antimicrobiana, anti-nociceptiva, antimalárica, antileishmania, imunossupressora, anti-asmática, diurética e antitumoral, validando desta maneira os seus usos tradicionais e demonstrando o grande potencial desta espécie para um maior desenvolvimento na área da industria farmacêutica

Physalis angulata is an annual herb widely used in popular medicine for the treatment of a variety of pathologies. This review shows research over the last 30 years, about traditional uses, chemical constituents and pharmacology of this specie. The studies related to traditional uses show that P. angulata is known for its antimalarial, anti-inflammatory and post-partum treating properties. It presents the different pharmacological experiments in vitro and in vivo models that have been made, also the identification of phytochemical constituents with medicinal importance, the main being physalins and withanolides. Pharmacological studies have shown antiparasitic, anti-inflammatory, antimicrobial, antinociceptive, antimalarial, antileishmanial, immunosuppressive, antiasthmatic diuretic, and antitumor activities, thus validating its traditional uses and demonstrating the great potential of this specie for further development within the pharmaceutical industry (AU)

Physalis angulata L. (Bolsa Mullaca): a review of its traditional uses, chemistry and pharmacology / Physalis angulata L. (Bolsa Mullaca): revisión de usos tradicionales, química y farmacología

Physalis angulata is a specie of the Solanaceae family, which edible fruit is used in several countries of tropical and subtropical regions of the world as medicinal and fruit-tree. This review shows research over the last 30 years, about traditional uses, chemical constituents and pharmacology of this specie. The studies related to traditional uses show that P. angulata is known for its antimalarial, anti-inflammatory and post-partum treating properties. It presents the different pharmacological experiments in vitro and in vivo models that have been made, also the identification of phytochemical constituents with medicinal importance, the main being physalins and withanolides. Pharmacological studies have shown antiparasitic, anti-inflammatory, antimicrobial, antinociceptive, antimalarial, antileishmanial, immunosuppressive, antiasthmatic diuretic, and antitumor activities, thus validating its traditional uses and demonstrating the great potential of this specie for further development within the pharmaceutical industry.

Physalis angulata, es una especie de la familia Solanaceae, de frutos comestibles, que en diferentes países de regiones tropicales y subtropicales del mundo utilizan como medicinal y frutal. La presente revisión muestra las investigaciones realizadas durante los últimos 30 años, sobre los usos tradicionales, componentes químicos y farmacología de esta especie. Los estudios referidos a los usos tradicionales, muestran que la especie es conocida por propiedades antimaláricas, antiinflamatorias y en el tratamiento de postparto. Se muestran los diferentes experimentos farmacológicos de ensayos in vitro y modelos in vivo que se han realizado, asimismo la identificación de sus constituyentes fitoquímicos con importancia medicinal, siendo los principales las fisalinas y los witanólidos. Los estudios farmacológicos revelan que tiene actividad antiparasitaria, antiinflamatoria, antimicrobiana, antinociceptiva, antimalárica, antileishmania, inmunosupresor, antiasmático, diurético y antitumoral, validando de esta manera sus usos tradicionales y demostrando el gran potencial que tiene esta especie para un mayor desarrollo dentro de la industria farmacéutica.