Evaluation of Ilex guayusa and Piper marginatum Extract Cytotoxicity on Human Dental Pulp Mesenchymal Stem Cells.

BACKGROUND: Amelogenesis imperfecta is a hereditary disorder affecting dental enamel. Among its phenotypes, hypocalcified AI is characterized by mineral deficiency, leading to tissue wear and, consequently, dental sensitivity. Excessive fluoride intake (through drinking water, fluoride supplements, toothpaste, or by ingesting products such as pesticides or insecticides) can lead to a condition known as dental fluorosis, which manifests as stains and teeth discoloration affecting their structure. Our recent studies have shown that extracts from Colombian native plants, Ilex guayusa and Piper marginatum, deposit mineral ions such as phosphate and orthophosphate into the dental enamel structure; however, it is unknown whether these extracts produce toxic effects on the dental pulp. OBJECTIVE: To assess cytotoxicity effects on human dental pulp stem cells (hDPSCs) exposed to extracts isolated from I. guayusa and P. marginatum and, hence, their safety for clinical use. METHODS: Raman spectroscopy, fluorescence microscopy, and flow cytometry techniques were employed. For Raman spectroscopy, hDPSCs were seeded onto nanobiochips designed to provide surface-enhanced Raman spectroscopy (SERS effect), which enhances their Raman signal by several orders of magnitude. After eight days in culture, I. guayusa and P. marginatum extracts at different concentrations (10, 50, and 100 ppm) were added. Raman measurements were performed at 0, 12, and 24 h following extract application. Fluorescence microscopy was conducted using an OLIMPUS fv1000 microscope, a live-dead assay was performed using a kit employing a BD FACS Canto TM II flow cytometer, and data analysis was determined using a FlowJo program. RESULTS: The Raman spectroscopy results showed spectra consistent with viable cells. These findings were corroborated using fluorescence microscopy and flow cytometry techniques, confirming high cellular viability. CONCLUSIONS: The analyzed extracts exhibited low cytotoxicity, suggesting that they could be safely applied on enamel for remineralization purposes. The use of nanobiochips for SERS effect improved the cell viability assessment.

Essential oil from Piper tuberculatum Jacq. (Piperaceae) and its majority compound ß-caryophyllene: mechanism of larvicidal action against Aedes aegypti (Diptera: Culicidae) and selective toxicity.

Synthetic insecticides have been the primary approach in controlling Aedes aegypti; however, their indiscriminate use has led to the development of resistance and toxicity to non-target animals. In contrast, essential oils (EOs) are alternatives for vector control. This study investigated the mechanism of larvicidal action of the EO and ß-caryophyllene from Piper tuberculatum against A. aegypti larvae, as well as evaluated the toxicity of both on non-target animals. The EO extracted from P. tuberculatum leaves was majority constituted of ß-caryophyllene (54.8%). Both demonstrated larvicidal activity (LC50 of 48.61 and 57.20 ppm, p < 0.05), acetylcholinesterase inhibition (IC50 of 57.78 and 71.97 ppm), and an increase in the production of reactive oxygen and nitrogen species in larvae after exposure to the EO and ß-caryophyllene. Furthermore, EO and ß-caryophyllene demonstrate no toxicity to non-target animals Toxorhynchites haemorrhoidalis, Anisops bouvieri, and Diplonychus indicus (100% of survival rate), while the insecticide α-cypermethrin was highly toxic (100% of death). The results demonstrate that the EO from P. tuberculatum and ß-caryophyllene are important larvicidal agents.

Two new species of the hyperdiverse geometrid moth genus Eois (Lepidoptera, Geometridae, Larentiinae) from Ecuador, with descriptions of early stages.

The hyperdiverse geometrid genus Eois Hübner, estimated to encompass more than 1,000 species, is among the most species-rich genera in all of Lepidoptera. While the genus has attracted considerable attention from ecologists and evolutionary biologists in recent decades, limited progress has been made on its alpha taxonomy. This contribution focuses on the Olivacea clade, whose monophyly has been recognized previously through molecular analyses. We attempt to define the clade from a morphological perspective and recognize the following species based on morphology and genomic data: E.olivacea (Felder & Rogenhofer); E.pseudolivacea Doan, sp. nov.; E.auruda (Dognin), stat. rev.; E.beebei (Fletcher, 1952), stat. rev.; E.boliviensis (Dognin), stat. rev.; and E.parumsimii Doan, sp. nov. Descriptions and illustrations of the immature stages of E.pseudolivacea reared from Piper (Piperaceae) in Ecuador are provided.

Modulation of Gut Microbiota, and Morphometry, Blood Profiles and performance of Broiler Chickens Supplemented with Piper aduncum, Morinda citrifolia, and Artocarpus altilis leaves Ethanolic Extracts.

Bioactive plants such as P. aduncum, M. citrifolia, and A. altilis might improve intestinal health as an alternative to antibiotic growth promoters. The objective of this study was to determine the effect of the ethanolic extracts (EEs) of these plants on the intestinal health of broiler chickens. Cobb 500 chickens (n = 352) were distributed into eight treatments with four replicates and 11 chickens each. T1 received a base diet, and T2 received a base diet with 0.005% zinc bacitracin. T3, T5, and T7 were supplemented with 0.005% of P. aduncum, M. citrifolia, and A. altilis EE in the diet while T4, T6, and T8 with 0.01% of the extract. The EEs were supplemented with drinking water from 1 to 26 days of age. The following parameters were evaluated: hematological profiles at 28 days of age, blood metabolites profiles at 14, 21, and 28 days; Escherichia coli, Staphylococcus aureus, and Lactobacillus sp. abundance in the ileum mucosa and content at 21 and 28 days, and histomorphometry of the duodenum, jejunum, and ileum mucosa at 14, 21, and 28 d. Final weight (FW), weight gain (WG), feed intake (FI), and feed conversion rate (FCR) were evaluated at seven, 21, and 33 days of age. M. citrifolia and A. altilis EE at 0.01% increased blood glucose levels at 21 and 28 days of age, respectively, and P. aduncum and M. citrifolia EE at 0.01% increased triglycerides at 28 days of age; in addition, this EE did not have any effect on the AST and ALT profiles. The depths of the Lieberkühn crypts and the villi length to the crypt's depth ratio increased with age on supplementation with 0.01% M. citrifolia and A. altilis EE at 21 days of age (p < 0.05). In addition, the depth of the crypts increased at 28 days of age (p < 0.05) in chickens supplemented with 0.01% A. altilis EE. The 0.01% M. citrifolia EE in diet decreased in the Staphylococcus aureus population in the ileal microbiota (p < 0.05). The FW and WG during the fattening and in the three stages overall increased, and the FCR decreased; however, the FI and the carcass yield did not change in the broiler chickens supplemented with 0.01% M. citrifolia EE (p < 0.05). Conclusively, the M. citrifolia EE at 0.01% of the diet improved intestinal health and thus the performance indices of the broiler chickens and did not have a detrimental effect on any of the parameters evaluated, so it is postulated as a potential alternative to AGP in poultry.

Lignans Isolated from Piper truncatum Act as New Potent Antitrypanosomal Compounds.

The hexane extract from twigs of Piper truncatum Vell (Piperaceae) displayed activity against Trypanosoma cruzi and was subjected to chromatographic steps to afford six dibenzylbutyrolactolic lignans, being four knowns: cubebin (1), (-)-9α-O-methylcubebin (2), (+)-9ß-O-methylcubebinin (3) and 3,4-dimethoxy-3,4-demethylenedioxycubebin (4) as well as two new, named truncatin A (5) and B (6). Initially, in vitro activity against trypomastigotes was evaluated and compounds 1, 4 and 6 exhibited EC50 values of 41.6, 21.0 and 39.6 µM, respectively. However, when tested against amastigotes, the relevant clinical form in the chronic phase of Chagas disease, compounds 1-6 displayed activities with EC50 values ranging from 1.6 to 13.7 µM. In addition, the mammalian cytotoxicity of compounds 1-6 was evaluated against murine fibroblasts (NCTC). Compounds 2, 3 and 4 exhibited reduced toxicity against NCTC cells (CC50>200 µM), resulting in SI values of>21.9,>14.5 and>121.9, respectively. Compound 4 showed the highest potency with an SI value twice superior to that determined by the standard drug benznidazole (SI>54.6) against the intracellular amastigotes. These data suggest that lignan 4 can be considered a possible scaffold for designing a new drug candidate for Chagas disease.

Biogenic Ag2O nanoparticles with "Hoja Santa" (Piper auritum) extract: characterization and biological capabilities.

The 'sacred leaf' or "Hoja Santa" (Piper auritum Kunth) has a great value for Mexican culture and has gained popularity worldwide for its excellent properties from culinary to remedies. To contribute to its heritage, in this project we proposed the green synthesis of silver oxide nanoparticles (Ag2O NPs) using an extract of "Hoja Santa" (Piper auritum) as a reducing and stabilizing agent. The synthesized Ag2O NPs were characterized by UV-Visible spectroscopy (plasmon located at 405 nm), X-ray diffraction (XRD) (particle size diameter of 10 nm), scanning electron microscopy (SEM) (particle size diameter of 13.62 ± 4.61 nm), and Fourier-transform infrared spectroscopy (FTIR) (functional groups from "Hoja Santa" attached to nanoparticles). Antioxidant capacity was evaluated using DPPH, ABTS and FRAP methods. Furthermore, the antimicrobial activity of NPs against a panel of clinically relevant bacterial strains, including both Gram-positive (Staphylococcus aureus) and Gram-negative bacteria (Salmonella Enteritidis and Escherichia coli O157:H7), was over 90% at concentrations of 200 µg/mL. Additionally, we assessed the antibiofilm activity of the NPs against Pseudomonas aeruginosa (reaching 98% of biofilm destruction at 800 µg/mL), as biofilm formation plays a crucial role in bacterial resistance and chronic infections. Moreover, we investigated the impact of Ag2O NPs on immune cell viability, respiratory burst, and phagocytic activity to understand their effects on the immune system.

Essential Oils from the Genus Piper Promote Antinociception by Modulating TRP Channels and Anti-Inflammatory Effects in Adult Zebrafish.

The Piper genus, known for its pharmacological potential, comprises 2,263 species primarily found in tropical regions. Despite recent advancements in pain therapies, the demand for more effective and well-tolerated analgesics and anti-inflammatories, particularly for chronic pain, remains. This study assessed the effects of essential oils from Piper caldense, Piper mosenii, and Piper mikanianum on nociceptive behavior induced by formalin and capsaicin, as well as their anti-inflammatory impact induced by carrageenan, using adult zebrafish models. Results indicated non-toxic essential oils with antinociceptive properties in both neurogenic and inflammatory phases of formalin-induced nociception through interaction with the TRPA1 receptor. Additionally, P. mosenii essential oil also blocked the nociceptive effect of capsaicin, a TRPV1 receptor agonist. Furthermore, essential oils from P. caldense and P. mikanianum exhibited significant anti-inflammatory effects by reducing carrageenan-induced abdominal edema. These findings highlight the pharmacological potential of Piper's essential oils as antinociceptive and anti-inflammatory agents.

Improving Strength and Fatigue Resistance in Post-Polio Syndrome Individuals with REAC Neurobiological Treatments.

Post-Polio Syndrome (PPS) is a chronic condition characterized by the emergence of new symptoms and functional decline in individuals who previously had polio. Despite advances in medical understanding, management of PPS remains challenging. This study aimed to evaluate the use of neurobiological modulation treatments using Radio Electric Asymmetric Conveyer (REAC) technology on fatigue and muscle strength. An open-label study was conducted with 17 patients submitted to four neuromodulation protocols: Neuro Postural Optimization (NPO), Neuro Psycho Physical Optimization (NPPO), Neuro Psycho Physical Optimization-Cervico Brachial (NPPO-CB), and Neuromuscular Optimization (NMO). The Time Up and Go (TUG) test, Handgrip Strength Test, and Revised Piper Fatigue Scale (RPFS) were used to assess participants' fatigue and muscle strength, being applied at the beginning and end of each protocol. The results obtained from the improvement in strength, physical endurance, and particularly the RPFS behavioral dimension, affective dimension, and psychological sensory dimension, through the utilization of REAC neurobiological modulation treatments, highlight this correlation. These results suggest that these treatments could be considered as a potential therapeutic approach for PPS.

Development, characterization and anti - Mycobacterium tuberculosis activity of solid lipid nanoparticles for oral Piper corcovadensis roots extract delivery / Desarrollo, caracterización y actividad anti - Mycobacterium tuberculosis de nanopartículas lipídicas sólidas para la administración oral de extracto de raíces de Piper corcovadensis

The present study thus aimed at the development and physicochemical characterization of solid lipid nanoparticles loaded with crude extract of Piper corcovadensis roots (SLN - CEPc) and chitosan - coated solid lipid nanoparticles loaded with crude extract of P. corcovadensis roots (C - SLN - CEPc), as well as the determination of its antimycobacterial activity against Mycobacterium tuberculosis H37Rv, its cytotoxicity against the Vero cell line and evaluation in the hemolysis assay. Both formulat ions containing the encapsulated extract showed high encapsulation efficiency, formed by a monodispersed system with small and spherical particles, and there was no aggregation of particles. In the biological assays, SLN - CEPc and C - SLN - CEPc showed promisin g anti - M. tuberculosis activity with a minimum inhibitory concentration (MIC) of 12.5 µg/mL, whereas the cytotoxic concentrations obtained at 50% (CC 50 ) in Vero cells were 60.0 and 70.0 µg/mL, respectively. Therefore, nanoencapsulation showed satisfactory results, justifying its usage in the development of new products.

El presente estudio apuntó al desarrollo y caracterización fisicoquímica de na nopartículas lípidas en estado sólido, cargadas con extracto crudo de raíz de Piper c orcovadensis (SLN - CEPc) y nanopartículas lípidas en estado sólido cubiertas con quitosano cargadas co n extracto crudo de raíz de P. corcovadensis (C - SLN - CEPc), así como la determinación de su actividad antimico bacterial contra Mycobacterium tuberculosis H37Rv, su citotoxicidad contra la línea celular Vero y su evaluación en ensayo de hemólisis. Ambas formulaciones que contenían el extracto encapsulado mostraron alta eficien cia de encapsulación, formado por un sistema monodispersado con pequeñas partículas esféricas, y no hubo agregación de partículas. En los ensayos biológicos, SLN - CEPc y C - SLN - CEPc mostraron un a prometedora actividad anti - M. tuberculosis con una mínima conc entración inhibitoria (MIC) de 12,5 µg/mL, mientras que las concentraciones citotóxicas obtenidas al 50% (CC 50 ) en células Vero estuvo en 60,0 y 70,0 µg/mL, respectivamente. Por lo tanto, la nanoencapsulación mostró resultados satisfactorios, justificando su uso en el desarrollo de nuevos productos.

The Antitumor Activity of Piplartine: A Review.

Cancer is a worldwide health problem with high mortality in children and adults, making searching for novel bioactive compounds with potential use in cancer treatment essential. Piplartine, also known as piperlongumine, is an alkamide isolated from Piper longum Linn, with relevant therapeutic potential. Therefore, this review covered research on the antitumor activity of piplartine, and the studies reported herein confirm the antitumor properties of piplartine and highlight its possible application as an anticancer agent against various types of tumors. The evidence found serves as a reference for advancing mechanistic research on this metabolite and preparing synthetic derivatives or analogs with better antitumor activity in order to develop new drug candidates.

Bioactive Compounds from P. pertomentellum That Regulate QS, Biofilm Formation and Virulence Factor Production of P. aeruginosa.

Pseudomonas aeruginosa is an opportunistic pathogen responsible for many nosocomial infections. This bacterium uses Quorum Sensing (QS) to generate antimicrobial resistance (AMR) so its disruption is considered a novel approach. The current study describes the antibiofilm and QS inhibitory potential of extract and chemical components from Piper pertomentellum. The methodo- logy included the phytochemical study on the aerial part of the species, the determination of QS inhibition efficacy on Chromobacterium violaceum and the evaluation of the effect on biofilm formation and virulence factors on P. aeruginosa. The phytochemical study led to the isolation and identification of a new piperamide (ethyltembamide 1), together with four known amides (tembamide acetate 2, cepharadione B 3, benzamide 4 and tembamide 5). The results indicated that the ethanolic extract and some fractions reduced violacein production in C. violaceum, however, only the ethanolic extract caused inhibition of biofilm formation of P. aeruginosa on polystyrene microtiter plates. Finally, the investigation determined that molecules (1-5) inhibited the formation of biofilms (50% approximately), while compounds 2-4 can inhibit pyocyanin and elastase production (30-50% approximately). In this way, the study contributes to the determination of the potential of extract and chemical constituents from P pertomentellum to regulate the QS system in P. aeruginosa.

Synergism in Two-Component Insecticides with Dillapiole against Fall Armyworm.

The fall armyworm (Spodoptera frugiperda), a polyphagous insect pest, is a major threat to food production, rapidly spreading through all the tropical areas in the world. Resistance has developed to the control protocols used so far (pyrethroids, organophosphorus, and genetically modified plants), and alternative strategies must be found. The bioactivity in essential oils is usually associated with the major constituents, but synergistic interactions among the constituents (even minor ones) can improve the levels of activity considerably. Herein, we tested the insecticidal activity of several constituents of the essential oil from Piper aduncum, an Amazonian Piperaceae, both separately and as binary mixtures, through their application on the dorsal side of the larva pronotum. Dillapiole proved to be, isolated, the most active compound in this oil (LD50 = 0.35 ppm). In binary mixtures, a strong synergistic effect was observed for the pairs of dillapiole with ß-caryophyllene (LD50 = 0.03 ppm), methyl eugenol (LD50 = 0.05 ppm), and α-humulene (LD50 = 0.05 ppm). In some cases, however, antagonism was recorded, as for dillapiole + ß-pinene (LD50 = 0.44 ppm). The use of binary mixtures of essential oil constituents as low-environmental-toxicity insecticides allows a fine tuning of the insecticidal activity, and the exploitation of synergy effects.

Composición química y actividad Butirilcolinesterasa selectiva del aceite esencial de Piper arboreum Aubl. de Ecuador / Chemical composition and selective BuChE activity of the essential oil of Piper arboreum Aubl. from Ecuador

The aim of this study was to identify the chemical composition of the Piper arboreum Aubl. essential oil (EO), and to evaluate its inhibitory activity in vitro against the enzymes butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE). The EO was obtained by steam distillation of the leaves, which were collected in Pindal canton of the Loja province in southern Ecuador. The chemical composition was analyzed using the gas chromatography technique coupled to a mass spectrometry detector (GC-MS) and gas chromatography coupled to a flame ionization detector (GC-FID). A total of 41 compounds were identified, the major components found in the oil were limonene (31,46%), ß-selinene (12,01%), (E)-caryophyllene (7,53%), bicyclogermacrene (6,72%), germacrene D (3,83%) and ß-elemene (3,63%). In in vitro analyzes, the EO showed high selective inhibition for BuChE with an IC50 inhibition value of 29,3±3,3 µg/mL. By contrast, the EO was not active against the AChE enzyme (IC50was 100,1±15,2 µg/mL).

El objetivo del presente estudio consistió en identificar la composición química del aceite esencial de la especie Piper arboreum Aubl. y evaluar su actividad inhibitoria in vitro frente a las enzimas butirilcolinesterasa (BuChE) y acetilcolinesterasa (AChE). El aceite esencial (AE) se obtuvo mediante destilación por arrastre de vapor de las hojas de la planta, que se colectaron en el cantón Pindal de la provincia de Loja al sur de Ecuador. La composición química se analizó mediante la técnica de cromatografía de gases acoplado a un detector de espectrometría de masas (GC-MS) y cromatografía de gases acoplado a un detector de ionización de llama (GC-FID). Se identificaron en total 41 compuestos, siendo los mayoritarios, el limoneno (31,46%), ß-selineno (12,01%), (E)-cariofileno (7,53%), biciclogermacreno (6,72%), germacreno D (3,83%) y ß-elemeno (3,63%). En los análisis in vitro, el AE mostró una alta inhibición selectiva para BuChE con un valor de inhibición CI50 de 29,3±3,3 µg/mL. Por el contrario,el AE no resultó activo frente a la enzima AChE con un valor de inhibión CI50= 100,1±15,2 µg/mL.

Plant Extracts from the Yucatan Peninsula in the In Vitro Control of Curvularia lunata and Antifungal Effect of Mosannona depressa and Piper neesianum Extracts on Postharvest Fruits of Habanero Pepper.

Plant extracts are a valuable alternative for the control of phytopathogenic fungi in horticultural crops. In the present work, the in vitro antifungal effect of ethanol and aqueous extracts from different vegetative parts of 40 native plants of the Yucatan Peninsula on Curvularia lunata ITC26, a pathogen of habanero pepper (Capsicum chinense), and effects of the most active extracts on postharvest fruits were investigated. Among these, the ethanol extracts of Mosannona depressa (bark from stems and roots) and Piper neesianum (leaves) inhibited 100% of the mycelial growth of C. lunata. The three extracts were partitioned between acetonitrile and n-hexane. The acetonitrile fraction from M. depressa stem bark showed the lowest mean inhibitory concentration (IC50) of 188 µg/mL against C. lunata. The application of this extract and its active principle α-asarone in the postharvest fruits of C. chinense (500 µg/mL) was shown to inhibit 100% of the severity of the infection caused by C. lunata after 11 days of contact. Both samples caused the distortion and collapse of the conidia of the phytopathogen when observed using electron microscopy at 96 h. The spectrum of M. depressa enriched antifungal action is a potential candidate to be a botanical fungicide in the control of C. lunata in cultivating habanero pepper.

Piper nigrum extract suppresses tumor growth and enhances the antitumor immune response in murine models of breast cancer and melanoma.

Although the antitumor effect of P. nigrum has been widely studied, research related to its possible immunomodulatory effects is relatively scarce. Here, the antitumor and immunomodulatory activity of an ethanolic extract of P. nigrum were evaluated in the murine models of 4T1 breast cancer and B16-F10 melanoma. In vitro evaluations showed that the P. nigrum extract has cytotoxic activity, induces apoptotic cell death, and has a pro-oxidant effect in both cell lines, but it regulates glucose uptake differently in both lines, decreasing it in 4T1 but not in B16-F10. P. nigrum extract significantly reduced tumor size in both models and decreased the occurrence of macrometastases in 4T1 model. Evaluation of immune subpopulations by flow cytometry revealed that the P. nigrum extract significantly increases the frequency of dendritic cells and activated CD8+ T cells and decreases the frequency of myeloid-derived suppressor like cells and Tregs in the tumor microenvironment of both models but with different dynamics. Our findings strongly suggest that the P. nigrum extract exerts immunomodulatory functions, slightly related to the modulation of cellular energy metabolism, which could ultimately contribute to the promising antitumor effect of P. nigrum.

Actividad antiinflamatoria in vitro de Plantago major L. y Piper aduncum L. sobre la fosfolipasa A2 del veneno de la serpiente Lachesis muta muta / In vitro anti-inflammatory activity of Plantago major L. and Piper aduncum L. on phospholipase A2 from the venom of snake Lachesis muta muta

Objetivo. Evaluar la actividad inhibitoria in vitro de los extractos de Plantago major «llantén» y Piper aduncum «matico» sobre Fosfolipasa A2 (PLA2) del veneno de la serpiente Lachesis muta muta. Materiales y métodos. Esta investigación fue de tipo explicativa con diseño experimental. Se recolectaron hojas de P. major y P. aduncum en la provincia de Huarochirí en Lima, Perú. Se prepararon extractos alcohólicos diluidos en agua destilada y se realizaron los ensayos fitoquímicos, la cuantificación de fenoles y flavonoides, la cromatografía de capa fina (CCF) en celulosa y la actividad enzimática con PLA2. Se analizó la capacidad de inhibir la PLA2 con los extractos en estudio y sus fracciones. Para el análisis estadístico se utilizó la prueba de Kruskal Wallis y comparaciones múltiples de Bonferroni. Resultados. Tanto en P. major como en P. aduncum se identificó cualitativamente la presencia de fenoles, flavonoides y taninos; además, P. aduncum presentó saponinas. La inhibición de la actividad de la PLA2 del veneno por el extracto total de P. major fue del 45,3%, y sus fracciones mostraron valores de inhibición: LLF-1 con 31,1%, LLF-2 con 66,3% y LLF-3 con 65,5%. En P. aduncum, los valores de inhibición para el extracto total fueron de 86,9%, y sus fracciones presentaron inhibiciones: MF-1 con 34,3%, MF-2 con 67,1% y MF-3 con 54,9%. El análisis estadístico demostró diferencias significativas en la inhibición de la PLA2 (p=0,009) por los extractos. Conclusión. Los ensayos realizados demostraron una asociación entre el efecto antiinflamatorio de los extractos y la inhibición de la PLA2.

Objective. To evaluate the in vitro inhibitory activity of Plantago major "llantén" and Piper aduncum "matico" extracts on phospholipase A2 (PLA2) from the venom of the snake Lachesis muta muta. Materials and methods. We carried out an explanatory study with experimental design. Leaves of P. major and P. aduncum were collected in the province of Huarochirí in Lima, Peru. Then, we prepared alcoholic extracts diluted in distilled water and conducted phytochemical assays, quantification of phenols and flavonoids, thin layer chromatography (TLC) on cellulose and enzymatic activity with PLA2. The ability to inhibit PLA2 with the extracts under study and their fractions was analyzed. The Kruskal Wallis test and Bonferroni multiple comparisons were used during statistical analysis. Results. Phenols, flavonoids and tannins were qualitatively identified in both P. major and P. aduncum; in addition, P. aduncum presented saponins. The inhibition of PLA2 activity of the venom by the total extract of P. major was 45.3%, and its fractions showed the following inhibition values: 31.1% for LLF-1, 66.3% for LLF-2 and 65.5% for LLF-3. The inhibition values for the total extract of P. aduncum were 86.9%, and its fractions showed the following inhibition rates: 34.3% for MF-1, 67.1% for MF-2 and 54.9% for MF-3. Statistical analysis showed significant differences in the inhibition of PLA2 (p=0.009) by the extracts. Conclusion. The tests demonstrated an association between the anti-inflammatory effect of the extracts and PLA2 inhibition.

Extraction, identification and antitumor activity in cell cultures of cubebin isolated from dry seeds Piper cubeba (Piperaceae).

The Pipercubeba, it is one spice, widely consumed in Europe, which has several bioactive molecules, between those a lignan named cubebin. Cubebin has several known biological activities, such as analgesic activity and anti-inflammatory, trypanocidal activity, leishmanicidal and antitumor activity. The objective of this study was to evaluate the antiproliferative activity "in vitro" cubebin in eight different human tumor cell lines. It was fully characterized by IR analysis, NMR, mass spectrometry, DSC, TGA, residual solvent and elemental analysis. The antitumor activity of cubebin was evaluated "in vitro" on eight different human tumor cell lineages. Cubebin showed GI50≤30µg/mL for lineage cell U251 (glioma CNS), 786-0 (kidney), PC-3 (prostate), HT-29 (colon rectum). For K562 cells (leukemia), cubebin presented GI50≤to 4.0mg/mL. For the other lineages cells, MCF-7 (breast) and NCI-H460 to cubebin can be considered inactive because of GI50>250mg/mL. Analyzing the selectivity index for cubebin, it can be observed that high selectivity of cubebin to K562 lineage cells (leukemia). Analyzing the cytotoxic potential of cubebin was observed that probably acts cubebin altering metabolism, inhibiting cell growth - a cytostatic effect, showing no cytocidal effect on any lineage cell.

Antibacterial Activity of the Essential Oil of Piper tuberculatum Jacq. Fruits against Multidrug-Resistant Strains: Inhibition of Efflux Pumps and ß-Lactamase.

Antimicrobial resistance has become a growing public health concern in recent decades, demanding a search for new effective treatments. Therefore, this study aimed to elucidate the phytochemical composition and evaluate the antibacterial activity of the essential oil obtained from the fruits of Piper tuberculatum Jacq. (EOPT) against strains carrying different mechanisms of antibiotic resistance. Phytochemical analysis was performed using gas chromatography-mass spectrometry (GC/MS). The antibacterial activity of EOPT and its ability to inhibit antibiotic resistance was evaluated through the broth microdilution method. The GC-MS analysis identified 99.59% of the constituents, with ß-pinene (31.51%), α-pinene (28.38%), and ß-cis-ocimene (20.22%) being identified as major constituents. The minimum inhibitory concentration (MIC) of EOPT was determined to assess its antibacterial activity against multidrug-resistant strains of Staphylococcus aureus (IS-58, 1199B, K2068, and K4100). The compound showed a MIC of ≥ 1024 µg/mL, suggesting a lack of intrinsic antibacterial activity. However, when the EOPT was associated with antibiotics and EtBr, a significant decrease in antibiotic resistance was observed, indicating the modulation of efflux pump activity. This evidence was corroborated with the observation of increased fluorescent light emission by the bacterial strains, indicating the involvement of the NorA and MepA efflux pumps. Additionally, the significant potentiation of ampicillin activity against the S. aureus strain K4414 suggests the ß-lactamase inhibitory activity of EOPT. These results suggest that the essential oil from P. tuberculatum fruits has antibiotic-enhancing properties, with a mechanism involving the inhibition of efflux pumps and ß-lactamase in MDR S. aureus strains. These findings provide new perspectives on the potential use of EOPT against antibiotic resistance and highlight the importance of Piper species as sources of bioactive compounds with promising therapeutic activities against MDR bacteria. Nevertheless, further preclinical (in vivo) studies remain necessary to confirm these in vitro-observed results.

Antiquorum and Antibiofilm Activities of Piper bogotense C. DC. against Pseudomonas aeruginosa and Identification of Bioactive Compounds.

The present study describes the anti-biofilm and quorum sensing (QS) inhibitory potential of extracts and chemical constituents from Piper bogotense. Antibiofilm potential was determined through crystal violet assay against Pseudomonas aeruginosa, while QS inhibition efficacy was determined through violacein inhibition assay using Chromobacterium violaceum as a bacterial model. Additionally, this study reports the effects of the chemical constituents isolated in P. bogotense against various virulent factors associated with QS, such as the percentage decrease in pyocyanin, elastase, and protease production. The chemical study led to the isolation and identification of two prenylated benzoic acids (1 and 2) and a prenylated hydroquinone 3, of which compounds 1 and 2 are reported for the first time for P. bogotense. The ethanolic extract and the DCM fraction from P. bogotense stand out for reducing violacein production in C. violaceum, as well as the biofilm formation in P. aeruginosa. Compounds 2 and 3 stand out for having the lowest violacein production (43.8% and 68.3%), as well as the lowest production of virulence factors such as elastase (60.2% and 51.4%) and pyocyanin (39.7% and 33.2%). These results demonstrate the potential of P. bogotense components to be used as an alternative control against multidrug-resistant P. aeruginosa.

Volatile Components, Antioxidant and Phytotoxic Activity of the Essential Oil of Piper acutifolium Ruiz & Pav. from Peru.

Piper acutifolium Ruiz & Pav is known as "matico" and belongs to the Piperaceae family, and in Peru it is traditionally used as an infusion or decoction to ameliorate wound healings or ulcers. In this study, the aim was to investigate the volatile components, the antioxidant profile, and the phytotoxic activity of the essential oil (EO) of P. acutifolium from Peru. To identify the phytoconstituents, the EO was injected into a Gas Chromatography-Mass Spectrometry (GC-MS) to obtain the chemical profile of the volatile components, followed by the antioxidant activity carried out by the reaction with three organic radicals (2,2-diphenyl-1-picrylhydrazyl (DPPH); 2,2'-azinobis-(3-ethylbenzothiazoline)-6- sulfonic acid (ABTS); ferric reducing/antioxidant power (FRAP)). Finally, the phytotoxic capabilities of the EO were tested on two model plants, Lactuca sativa seeds and Allium cepa bulbs. As a result, the analysis identified α-phellandrene as its main volatile chemical at 38.18%, followed by ß-myrcene (29.48%) and ß-phellandrene (21.88%). Regarding the antioxidant profile, the half inhibitory concentration (IC50) in DPPH was 160.12 ± 0.30 µg/mL, for ABTS it was 138.10 ± 0.06 µg/mL and finally in FRAP it was 450.10 ± 0.05 µg/mL. The phytotoxic activity demonstrated that the EO had high activity at 5% and 10% against L. sativa seed germination, the inhibition of root length, and hypocotyl length. Additionally, in A. cepa bulbs, the inhibition root length was obtained at 10%, both comparable to glyphosate, which was used as a positive control. The molecular docking on 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS) revealed that α-phellandrene had -5.8 kcal/mol, being near to glyphosate at -6.3 kcal/mol. The conclusion shows that the EO of P. acutifolium presented antioxidant and phytotoxic activity and might be useful as a bioherbicide in the future.