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The study investigated the effects of cultivating Tridax procumbens in hydroponic conditions with different concentrations of copper ions, aiming to understand the physiological changes and the impact on the biosynthesis of secondary metabolites. The treatments consisted of a completely randomized design, with five increasing concentrations of copper (T0 = 0.235, T1 = 12.5, T2 = 25, T3 = 50, T4 = 100 µmol L-1 of Cu), under controlled conditions for 36 days. Analysis of bioactive compounds in leaves was performed by HPLC-DAD and ESI-MS. Several phenolic compounds, alkaloids, phytosterols and triterpenoids were identified, demonstrating the plant's metabolic plasticity. The highest dose of copper (100 µmol L-1) significantly promoted voacangine, the most predominant compound in the analyses. Notably, 66.7% of the metabolites that showed an increase in concentration, were phenolic compounds. Furthermore, treatments with 12.5 and 25 µmol L-1 of copper were identified as promoting the biosynthesis of phytosterols and triterpenoids. These biochemical adaptations can play a fundamental role in the survival and development of plants in environments contaminated by metals, and from this it is possible to determine cultivation techniques that maximize the biosynthesis of the compound of interest.
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Cobre , Folhas de Planta/metabolismo , Asteraceae/metabolismo , Fitosteróis/metabolismoRESUMO
Fridericia chica is an Amazonian plant used to treat stomach disorders. However, the pharmacological activity of flavonoids in the extract has yet to be investigated. Therefore, we considered that a flavonoid-rich F. chica subfraction (FRS) has gastroprotective functions. For this, before the induction of gastric ulcers with ethanol or piroxicam, the rats received vehicle (water), omeprazole (30 mg/kg), or FRS (30 mg/kg), and the ulcer area was measured macro and microscopically, and the antisecretory action was investigated in pylorus-ligated rats. In addition, the roles of nitric oxide (NO) and nonprotein sulfhydryl compounds (NP-SH) in the gastroprotective effects of FRS were studied. FRS reduced ethanol- and piroxicam-induced ulcerations by 81% and 77%, respectively, as confirmed histologically. Antioxidant effects were observed for FRS through the maintenance of GSH and LPO levels, and the SOD and CAT activity similar to those found in the nonulcerated group. Moreover, FRS avoided the increase in MPO activity and TNF, IL-6, IL-4 and IL-10 levels. Moreover, mucin staining increased in ulcerated rats receiving FRS, and the pharmacological mechanism gastroprotective seems to involve the NO and NP-SH in addition to antisecretory actions. The chemical study by mass spectrometry confirmed the presence of flavonoids in FRS, and molecular docking studies have shown that these compounds interact with cyclooxygenase-1 and NO synthase. Furthermore, there was no indication that FRS had cytotoxic effects. Our results support the popular use of F. chica, and we conclude that the gastroprotection effect promoted by FRS can be attributed to the combined effect of the flavonoids.
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Antiulcerosos , Antioxidantes , Flavonoides , Extratos Vegetais , Plantas Medicinais , Ratos Wistar , Úlcera Gástrica , Animais , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/prevenção & controle , Ratos , Extratos Vegetais/farmacologia , Masculino , Antiulcerosos/farmacologia , Antiulcerosos/isolamento & purificação , Plantas Medicinais/química , Antioxidantes/farmacologia , Óxido Nítrico/metabolismo , Fabaceae/química , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Simulação de Acoplamento MolecularRESUMO
Wounds or chronic injuries are associated with high medical costs so, develop healing-oriented drugs is a challenge for modern medicine. The identification of new therapeutic alternatives focuses on the use of natural products. Therefore, the main goal of this study was to evaluate the healing potential and anti-inflammatory mechanism of action of extracts and the main compounds derived from Myrciaria plinioides D. Legrand leaves. The antimicrobial activity of leaf extracts was analyzed. Cell viability, cytotoxicity and genotoxicity of plant extracts and compounds were also assessed. Release of pro- and anti-inflammatory cytokines and TGF-ß by ELISA, and protein expression was determined by Western Blot. The cell migration and cell proliferation of ethanol and aqueous leaf extracts and p-coumaric acid, quercetin and caffeic acid compounds were also evaluated. The aqueous extract exhibited antibacterial activity and, after determining the safety concentrations in three assays, we showed that this extract induced p38-α MAPK phosphorylation and the same extract and the p-coumaric acid decreased COX-2 and caspase-3, -8 expression, as well as reduced the TNF-α release and stimulated the IL-10 in RAW 264.7 cells. In L929 cells, the extract and p-coumaric acid induced TGF-ß release, besides increasing the process of cell migration and proliferation. These results suggested that the healing properties of Myrciaria plinioides aqueous extract can be associated to the presence of phenolic compounds, especially p-coumaric acid, and/or glycosylated metabolites.
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Anti-Inflamatórios , Movimento Celular , Extratos Vegetais , Folhas de Planta , Cicatrização , Extratos Vegetais/farmacologia , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Cicatrização/efeitos dos fármacos , Camundongos , Células RAW 264.7 , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Linhagem Celular , Citocinas/metabolismo , Myrtaceae/química , Ácidos Cumáricos/farmacologia , Ácidos Cumáricos/isolamento & purificação , Antibacterianos/farmacologia , Antibacterianos/isolamento & purificaçãoRESUMO
Fabiana punensis S. C. Arroyo is a subshrub or shrub that is indigenous to the arid and semiarid region of northern Argentina and is known to possess several medicinal properties. The objective of this study was to optimize the extraction conditions so as to maximize the yield of bioactive total phenolic compound (TPC) and flavonoids (F) of F. punensis' aerial parts by using non-conventional extraction methods, namely ultrasound-assisted extraction, UAE, and microwave-assisted extraction, MAE, and to compare the biological activities and toxicity of optimized extracts vs. conventional extracts, i.e., those gained by maceration. Response Surface Methodology (RSM) was used to apply factorial designs to optimize the parameters of extraction: solid-to-liquid ratio, extraction time, ultrasound amplitude, and microwave power. The experimental values for TPC and F and antioxidant activity under the optimal extraction conditions were not significantly different from the predicted values, demonstrating the accuracy of the mathematical models. Similar HPLC-DAD patterns were found between conventional and UAE- and MAE-optimized extracts. The main constituents of the extracts correspond to phenolic compounds (flavonoids and phenolic acids) and apigenin was identified. All extracts showed high scavenger capacity on ABTSâ¢+, O2â¢- and H2O2, enabling the inhibition of the pro-inflammatory enzymes xanthine oxidase (XO) and lipoxygenase (LOX). They also showed an antimutagenic effect in Salmonella Typhimurium assay and cytotoxic/anti-proliferative activity on human melanoma cells (SKMEL-28). Toxicological evaluation indicates its safety. The results of this work are important in the development of efficient and sustainable methods for obtaining bioactive compounds from F. punensis for the prevention of chronic degenerative diseases associated with oxidative stress, inflammation, and DNA damage.
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Antioxidantes , Micro-Ondas , Fenóis , Componentes Aéreos da Planta , Extratos Vegetais , Fenóis/química , Fenóis/farmacologia , Fenóis/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Componentes Aéreos da Planta/química , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Humanos , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Ondas Ultrassônicas , Fracionamento Químico/métodos , Xantina Oxidase/antagonistas & inibidores , Xantina Oxidase/metabolismoRESUMO
Ethnobotany approached through ethnoeducation allows for the preservation of the cultural heritage of indigenous communities. In this way, the ethnobotanical knowledge of primary school students from the Paniquita Indigenous Community was recognized, regarding the cultural knowledge of medicinal plants and their significance in the conservation of the biocultural heritage. This research had a qualitative, ethnographic approach. The sample consisted of ten students who were part of a focus group, ethnobotanical walks, and participatory workshops with drawings since they stimulate students' creative and dynamic thinking and strengthen interculturality. Twenty-one plants were reported, which are used to relieve sore throats, headaches, and stomach aches, as well as to treat diarrhea and fever, to prevent flu, and as a purgative. All the medicinal plants mentioned grow in the community and are either cultivated or wild, which also shows the students' knowledge of the ir territory. These findings reflect the importance of ethno-education and ethnobotany at school and how historical reconstruction processes are generated from these settings, where indigenous ancestral knowledge is made visible.
La etnobotánica abordada desde la etnoeducación permite mantener el legado cultural de los pueblos originarios. De esta manera, se reconoció el conocimiento etnobotáni co de los estudiantes de primaria de la Comunidad Indígena Paniquita, sobre el conocimiento cultural de las plantas medicinales y su importancia para la conservación del patrimonio biocultural. La investigación tuvo un enfoque cualitativo y etnográfico. La muestra estuvo conformada por diez estudiantes que formaron parte de un grupo focal, caminatas etnobotánicas y talleres participativos con dibujos, ya que estimulan el pensamiento creativo y dinámico de los estudiantes y fortalecen la interculturalidad. Se reportaron 21 plantas que se utilizan para aliviar dolores de garganta, cabeza y estómago, así como para tratar la diarrea y la fiebre, para prevenir la gripe y como purgante. Todas las plantas medicinales mencionadas crecen en la comunidad y son cultivadas o silvestres, lo que también demuestra el conocimiento que los estudiantes tienen de su territorio. Estos hallazgos reflejan la importancia de la etnoeducación y la etnobotánica en la escuela y cómo se generan procesos de reconstrucción histórica desde estos escenarios, donde se visibiliza el conocimiento ancestral indígena.
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Humanos , Plantas Medicinais , Estudantes , Indígenas Sul-Americanos , Etnobotânica , Colômbia , Medicina TradicionalRESUMO
Leaves of Croton stipulaceuswere extracted (EHex, ECHCl3and EEtOH extracts) to assesstheir antioxidant potential, anti-inflammatory activity in murine models and acute toxicity. EEtOH showed the highest effect in DPPH (37.80% inhibition), FRAP (1065.00 ± 55.30 µmolFe2+) and total polyphenols (231.24 ± 9.05 meq AG/gM). EHex was the most active, ~ 50% inhibition of TPA-induced ear edema; while EEtOH (dose of 2 mg/ear) showed the highest inhibition in the chronic model (97% inhibition), and inhibited MPO activity (48%). In carrageenan-induced edema, ECHCl3(dose 500 mg/kg) was the most active. None of the extracts showed acute toxicity (LD50) at 2 g/kg (p.o.). This work is the first report that supports the traditional use of C. stipulaceusas an anti-inflammatory.
De las hojas de Croton stipulaceusse obtuvieron diferentes extractos (EHex, ECHCl3y EEtOH) evaluando el potencial antioxidante y la actividad antiinflamatoria en modelos murinos y la toxicidad aguda. El EEtOH mostró mayor efecto en DPPH (37.80% inhibición), FRAP (1065.00 ± 55.30 µmolFe2+) y polifenolestotales (231.24 ± 9.05 meq AG/gM). El EHex fue el más activo, cercano al 50% de inhibición del edema auricular inducido con TPA; mientras que el EEtOH (dosis de 2 mg/oreja) mostró la mayor inhibición en el modelo crónico (97% inhibición), e inhibió la actividad de la MPO (48%). En el edema inducido con carragenina, el ECHCl3(dosis 500 mg/kg) fue el más activo. Ninguno de los extractos mostró una toxicidad aguda (DL50) mayor a 2 g/kg (p.o). Este trabajo es el primer reporte que sustenta el uso tradicional de C. stipulaceuscomo antiinflamatorio.
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Animais , Ratos , Extratos Vegetais/administração & dosagem , Croton/química , Inflamação/tratamento farmacológico , Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem , Fenóis/análise , Extratos Vegetais/química , Folhas de Planta , Modelos Animais de Doenças , Anti-Inflamatórios/química , Antioxidantes/químicaRESUMO
This study investigates Cystobasidium benthicum (Cb) probiotic yeast and Cyrtocarpa edulis (Ce) fruit dietary effects, single (0.5 %) or combined (Cb:Ce, 0.25:0.25 %), on growth performance, humoral immunity in serum and skin mucus, and intestinal morphology of Nile tilapia (Oreochromis niloticus) after 14 and 28 days. The Cb group presented the highest (P < 0.05) specific growth rate, weight gain, and absolute growth rate with respect to the control group. Immunological assays indicated that Cb, Ce and Cb:Ce groups increased serum nitric oxide concentration compared to the control group (P < 0.05). Cb and Cb:Ce groups showed the highest serum myeloperoxidase enzyme activity at day 14 and 28, respectively (P < 0.05); whereas, Cb:Ce group had the highest (P < 0.05) myeloperoxidase activity in skin mucus. The superoxide dismutase enzyme activity was unaffected. On day 28, Cb, Ce, and Cb:Ce groups showed higher and lower (P < 0.05) catalase enzyme activity in serum and skin mucus, respectively, compared with the control group. Only the Cb group had higher (P < 0.05) total protein concentration in serum (day 14) and skin mucus (day 14 and 28) with respect to the control group. The lysozyme activity in serum (day 28) and skin mucus (day 14) was higher (P < 0.05) in the Cb group compared to the control group. Only the skin mucus of Ce group showed bactericidal activity against Aeromonas dhakensis (P < 0.05). Histological studies indicated that Cb and Cb:Ce groups increased microvilli height, and Cb, Ce and Cb:Ce augmented goblet cell area at day 14 compared to the control group (P < 0.05). At day 28, microvilli height was higher in all groups and the number of intraepithelial leukocytes increased in Cb and Ce groups with respect to the control group (P < 0.05). The ex vivo assay revealed that A. dhakensis in leukocytes decreased cell viability similar to the control group (P < 0.05). A principal component analysis (PCA) confirmed the results. In conclusion, C. benthicum in the diet was the best supplement to improve the growth and immunity of Nile tilapia.
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Ração Animal , Ciclídeos , Dieta , Frutas , Probióticos , Animais , Probióticos/administração & dosagem , Ciclídeos/crescimento & desenvolvimento , Ciclídeos/imunologia , Dieta/veterinária , Peroxidase/metabolismo , Óxido Nítrico/metabolismo , Intestinos/microbiologia , Intestinos/imunologia , Pele , Imunidade Humoral , Muco/metabolismo , Superóxido Dismutase/metabolismo , Catalase/metabolismoRESUMO
Neglected diseases are a group of infectious diseases, many of them parasitic, that mainly affect the poorest populations with limited access to health services, especially those living in remote rural areas and slums. According to the World Health Organization (WHO), neglected diseases put the lives of more than 200 million people at risk, and treatment is made difficult by the occurrence of resistance to existing medications, as well as the high level of toxicity. In this way, the potential of multitarget compounds is highlighted, defined as compounds designed to modulate multiple targets of relevance to disease, with the overall goal of enhancing efficacy and/or improving safety. Thus, the objective of our study is to evaluate existing multitarget compound approaches for neglected diseases, with an emphasis on Leishmaniasis, Chagas Disease, and Arboviruses. A literature review was performed by searching the database "Web of Sciences". In relation to the diseases covered in this work, Leishmaniasis, individually, was the one that presented the largest number of articles (11) that dealt with the topic, which can be justified by the high prevalence of this disease in the world, the second most common disease was Dengue, followed by Chagas disease, Chikungunya virus, and Zika virus. Furthermore, the multitarget potential of phenolic compounds was observed in all diseases under study, with the mechanisms related to the nucleus and transcription being the most reported mechanisms. From this perspective, it is worth highlighting the effectiveness of approaches related to multitarget drugs in discovering new therapeutic agents for neglected diseases.
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Doença de Chagas , Leishmaniose , Doenças Negligenciadas , Humanos , Doenças Negligenciadas/tratamento farmacológico , Doença de Chagas/tratamento farmacológico , Leishmaniose/tratamento farmacológico , Infecções por Arbovirus/tratamento farmacológico , Terapia de Alvo Molecular , AnimaisRESUMO
Aim: To identify potential antischistosomal agents through 3D pharmacophore-based virtual screening of US FDA approved drugs.Materials & methods: A comprehensive virtual screening was conducted on a dataset of 10,000 FDA approved drugs, employing praziquantel as a template. Promising candidates were selected and assessed for their impact on Schistosoma mansoni viability in vitro and in vivo using S. mansoni infected mice.Results & conclusion: Among the selected drugs, betamethasone and doxazosin demonstrated in vitro efficacy, with effective concentration 50% (EC50) values ranging from 35 to 60 µM. In vivo studies revealed significant (>50%) reductions in worm burden for both drugs. These findings suggest that betamethasone and doxazosin hold promise for repurposing in treating schistosomiasis. Additionally, the study showcases a useful approach for identifying new antischistosomal drugs.
Discovering new treatments for #schistosomiasis is crucial [Formula: see text]. Our study used virtual screening to identify potential antischistosomal drugs from US FDA approved compounds [Formula: see text]. Promising results in vitro and in vivo. [Formula: see text] #drugdiscovery #tropicaldiseases.
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Schistosoma mansoni , United States Food and Drug Administration , Animais , Camundongos , Schistosoma mansoni/efeitos dos fármacos , Estados Unidos , Aprovação de Drogas , Esquistossomicidas/farmacologia , Esquistossomicidas/química , Esquistossomicidas/uso terapêutico , Esquistossomose mansoni/tratamento farmacológico , Modelos Moleculares , Humanos , FarmacóforoRESUMO
Fungi are a source of a variety of secondary metabolites of importance in different areas of biotechnology. Several compounds have been characterized with antioxidant, antimicrobial, and anti-inflammatory activity from fungi of the division of the Ascomycota, among which is the species Daldinia eschscholtzii, an endophyte fungus of pantropical distribution. In this study, we evaluated the effect of an ointment made with D. eschscholtzii on the wound healing of BALB/c mice. The species was corroborated using a molecular marker Internal Transcribed Spacer (ITS1 and ITS4). The extracts and dust of the fungus were considered nontoxic as they caused a mortality of <15% in the nematode Panagrellus redivivus, and experimental ointments had no adverse effects on the skin of BALB/c mice. Wounds treated with the D. eschscholtzii ointments had 99.9-100% wound contraction after 17 days, which was similar to commercial healing (positive control). As such, the ointment of D. eschscholtzii is a natural alternative to improve wound healing.
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Camundongos Endogâmicos BALB C , Pomadas , Cicatrização , Animais , Cicatrização/efeitos dos fármacos , Camundongos , Pele/efeitos dos fármacos , Masculino , Modelos Animais de Doenças , Humanos , Ascomicetos/química , FemininoRESUMO
This study aimed to investigate the effect of including mouse feed with different concentrations (5, 10, or 20%) of Pereskia aculeata Miller (PAM) leaves on the morphology and development of preantral ovarian follicles and ovarian stromal cell density. The oral toxicity was performed using repeated dose toxicity assays subdivided into experiments of 30 days and 90 days of treatment. After the experiments, the ovaries of each animal were collected and submitted to classical histology. At 30 and 90 days, there was an equivalent percentage of normal, primordial, and developing follicles (P > 0.05) between PAM treatments compared to the control. Regarding the different stages of follicular development, after 90 days, there was a higher percentage (P < 0.05) of developing follicles only in the control group compared to day 30. The PAM 5% treatment was the only one that affected the cell density in the stroma after 90 days of treatment. Thus, we observed that supplementing the diet with P. aculeata did not pose any risk concerning animal consumption; specifically, there were no toxic reproductive effects observed from adding Pereskia aculeata Miller to the mouse diet.
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Plant cell, tissue, and organ cultures (PCTOC) have been used as experimental systems in basic research, allowing gene function demonstration through gene overexpression or repression and investigating the processes involved in embryogenesis and organogenesis or those related to the potential production of secondary metabolites, among others. On the other hand, PCTOC has also been applied at the commercial level for the vegetative multiplication (micropropagation) of diverse plant species, mainly ornamentals but also horticultural crops such as potato or fruit and tree species, and to produce high-quality disease-free plants. Moreover, PCTOC protocols are important auxiliary systems in crop breeding crops to generate pure lines (homozygous) to produce hybrids for the obtention of polyploid plants with higher yields or better performance. PCTOC has been utilized to preserve and conserve the germplasm of different crops or threatened species. Plant genetic improvement through genetic engineering and genome editing has been only possible thanks to the establishment of efficient in vitro plant regeneration protocols. Different companies currently focus on commercializing plant secondary metabolites with interesting biological activities using in vitro PCTOC. The impact of omics on PCTOC is discussed.
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Células Vegetais , Técnicas de Cultura de Tecidos , Técnicas de Cultura de Células/métodos , Produtos Agrícolas/genética , Produtos Agrícolas/crescimento & desenvolvimento , Melhoramento Vegetal/métodos , Células Vegetais/metabolismo , Desenvolvimento Vegetal/genética , Plantas/genética , Plantas/metabolismo , Técnicas de Cultura de Tecidos/métodosRESUMO
An efficient procedure for in vitro propagation of Herreria salsaparrilha Martius was established from single-node explants (fourth and fifth nodes from apex to the base) derived from donor plants maintained under shading-house conditions. After surface sterilization, explants are inoculated in test tubes containing 15 mL of Murashige and Skoog (MS) medium without growth regulators. Cultures are maintained under 35 µmol m-2 s-1 irradiance, a 16/8-h light/dark light regime, at 26 ± 2 °C. The subcultures are carried out under the same conditions, adding 6-benzyladenine 1.0 mg/L and Phytagel® 2.8 g/L. Shoots are elongated and rooted by transferring individual shoots to half-strength MS medium without growth regulators. After 25-30 days, elongated rooted shoots are transferred to plastic pots containing 25-30 mL of sterile distilled water, covered with a transparent plastic bag, and kept under the same growth room conditions for 2 days. Plants are transferred to cups containing autoclaved and washed sand and kept in a shading house (50% light interception) for acclimatization. True-to-type adult plants were successfully recovered under ex vitro conditions.
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Aclimatação , Brotos de Planta , Brotos de Planta/crescimento & desenvolvimento , Plantas Medicinais/química , Meios de Cultura/química , Raízes de Plantas/crescimento & desenvolvimentoRESUMO
Plants are a core part of cultural identity, as part of a diet, decorations, ceremonies, or as medicinal agents. Empirical knowledge regarding plants and their healing potential has existed worldwide for centuries. With the advance of science and technology, not only is the refinement of such sources or isolation of specific compounds possible, but these compounds can also be characterized based on their natural occurrence. Besides their importance for plant metabolism and structure, polysaccharides have been demonstrated to have substantial positive human health impacts on inflammation, metabolism, oxidative stress, and others. As an inherent part of plant cell walls, many polysaccharides from medicinal herbs, such as fructans, glucans, and pectins, have been extracted and analyzed for their structure and function. However, a review summarizing a significant portion of these studies was still unavailable. This review helps to fill the knowledge gap between polysaccharide bioactivity, their structure, and their plant matrix sources, focusing on historical medicinal usage.
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BACKGROUND: Colonization with Helicobacter pylori (H. pylori) has a strong correlation with gastric cancer, and the virulence factor CagA is implicated in carcinogenesis. Studies have been conducted using medicinal plants with the aim of eliminating the pathogen; however, the possibility of blocking H. pylori-induced cell differentiation to prevent the onset and/or progression of tumors has not been addressed. This type of study is expensive and time-consuming, requiring in vitro and/or in vivo tests, which can be solved using bioinformatics. Therefore, prospective computational analyses were conducted to assess the feasibility of interaction between phenolic compounds from medicinal plants and the CagA oncoprotein. AIM: To perform a computational prospecting of the interactions between phenolic compounds from medicinal plants and the CagA oncoprotein of H. pylori. METHODS: In this in silico study, the structures of the phenolic compounds (ligands) kaempferol, myricetin, quercetin, ponciretin (flavonoids), and chlorogenic acid (phenolic acid) were selected from the PubChem database. These phenolic compounds were chosen based on previous studies that suggested medicinal plants as non-drug treatments to eliminate H. pylori infection. The three-dimensional structure model of the CagA oncoprotein of H. pylori (receptor) was obtained through molecular modeling using computational tools from the I-Tasser platform, employing the threading methodology. The primary sequence of CagA was sourced from GenBank (BAK52797.1). A screening was conducted to identify binding sites in the structure of the CagA oncoprotein that could potentially interact with the ligands, utilizing the GRaSP online platform. Both the ligands and receptor were prepared for molecular docking using AutoDock Tools 4 (ADT) software, and the simulations were carried out using a combination of ADT and AutoDock Vina v.1.2.0 software. Two sets of simulations were performed: One involving the central region of CagA with phenolic compounds, and another involving the carboxy-terminus region of CagA with phenolic compounds. The receptor-ligand complexes were then analyzed using PyMol and BIOVIA Discovery Studio software. RESULTS: The structure model obtained for the CagA oncoprotein exhibited high quality (C-score = 0.09) and was validated using parameters from the MolProbity platform. The GRaSP online platform identified 24 residues (phenylalanine and leucine) as potential binding sites on the CagA oncoprotein. Molecular docking simulations were conducted with the three-dimensional model of the CagA oncoprotein. No complexes were observed in the simulations between the carboxy-terminus region of CagA and the phenolic compounds; however, all phenolic compounds interacted with the central region of the oncoprotein. Phenolic compounds and CagA exhibited significant affinity energy (-7.9 to -9.1 kcal/mol): CagA/kaempferol formed 28 chemical bonds, CagA/myricetin formed 18 chemical bonds, CagA/quercetin formed 16 chemical bonds, CagA/ponciretin formed 13 chemical bonds, and CagA/chlorogenic acid formed 17 chemical bonds. Although none of the phenolic compounds directly bound to the amino acid residues of the K-Xn-R-X-R membrane binding motif, all of them bound to residues, mostly positively or negatively charged, located near this region. CONCLUSION: In silico, the tested phenolic compounds formed stable complexes with CagA. Therefore, they could be tested in vitro and/or in vivo to validate the findings, and to assess interference in CagA/cellular target interactions and in the oncogenic differentiation of gastric cells.
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Background: Uncaria tomentosa (Willd. ex Schult.) DC. (Rubiaceae) is traditionally used by Amazonian indigenous groups to treat inflammatory diseases. To date, there are no systematic reviews and meta-analyses on the use of U. tomentosa for inflammation control in animals supporting the traditional knowledge about this species. This study was conducted to evaluate the effect of U. tomentosa extracts in modulating inflammatory mediators and to determine which types of inflammatory diseases can be treated by this species. Methods: We conducted a systematic review and meta-analysis of preclinical studies published before 26 July 2023, identified in PubMed, Embase, and Scopus. Four independent reviewers extracted the data and assessed the risks of bias. The effects of U. tomentosa on inflammatory diseases and the inflammatory mediators involved were extracted from the studies. Standardized mean differences (SMD) and 95% confidence intervals (95%CI) of the outcomes were estimated. The meta-analyses were conducted using RevMan 5.4 (Cochrane Collaboration). This protocol was registered in PROSPERO (CRD42023450869). Results: Twenty-four of 523 studies were included. U. tomentosa extracts decreased the cytokines interleukin (IL)-6 (SMD: -0.72, 95%CI: -1.15, -0.29, p = 0.001) and transcription factor nuclear factor kappa-B (NF-κB) (SMD: -1.19, 95%CI: -1.89, -0.48, p = 0.001). However, the extracts did not significantly alter IL-1 (SMD: -0.16, 95%CI: -0.87, +0.56, p = 0.67), IL-10 (SMD: -0.05, 95%CI:-0.35, 0.45, p = 0.80), or tumor necrosis factor-alpha (TNF-α) levels (SMD: 0.18, 95%CI: -0.25, 0.62, p = 0.41). Conclusion: Many extracts of stem bark, roots, and leaves of U. tomentosa, mostly aqueous and hydroethanolic, exhibited anti-inflammatory and/or immunomodulatory activities and low toxicity. The extracts decreased NF-κB and IL-6. These findings suggest that this species has the potential to treat inflammatory diseases in which these markers are increased, according to the ethnopharmacological use. These activities are not related to a specific class of compounds.Systematic Review Registration: https://www.crd.york.ac.uk/prospero/display_record.php?RecordID=450869, Identifier CRD42023450869.
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Despite the vast global botanical diversity, the pharmaceutical development of herbal medicinal products (HMPs) remains underexploited. Of over 370,000 described plant species, only a few hundred are utilized in HMPs. Most of these have originated from traditional use, and only a minority come from megadiverse countries. Exploiting the pharmacological synergies of the hundreds of compounds found in poorly studied plant species may unlock new therapeutic possibilities, enhance megadiverse countries' scientific and socio-economic development, and help conserve biodiversity. However, extensive constraints in the development process of HMPs pose significant barriers to transforming this unsatisfactory socio-economic landscape. This paper proposes a roadmap to overcome these challenges, based on the technology readiness levels (TRLs) introduced by NASA to assess the maturity of technologies. It aims to assist research entities, manufacturers, and funding agencies from megadiverse countries in the discovery, development, and global market authorization of innovative HMPs that comply with regulatory standards from ANVISA, EMA, and FDA, as well as WHO and ICH guidelines.
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The function of the sense of taste is usually confined to the ability to perceive the flavor of food to assess and use the nutrients necessary for healthy survival and to discard those that may be harmful, toxic, or unpleasant. It is almost unanimously agreed that the perception of bitter taste prevents the consumption of toxins from plants, decaying foods, and drugs. Forty years ago, while practicing medicine in a rural area of the Colombian Amazon, I had an unexpected encounter with the Inga Indians. I faced the challenge of accepting that their traditional medicine was effective and that the medicinal plants they used had a real therapeutic effect. Wanting to follow a process of learning about medicinal plants on their terms, I found that, for them, the taste of plants is a primary and fundamental key to understanding their functioning. One of the most exciting results was discovering the therapeutic value of bitter plants. The present review aims to understand whether there is any scientific support for this hypothesis from the traditional world. Can the taste of plants explain their possible therapeutic benefit? In the last 20 years, we have made novel advances in the knowledge of the physiology of taste. Our purpose will be to explore these scientific advances to determine if the bitter taste of medicinal plants benefits human health.
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Ugni candollei, commonly known as white murta, is a native Chilean berry with a polyphenol composition that has been underexplored. This study aimed to establish a comprehensive profile of white murta polyphenols using ultra-performance liquid chromatography electrospray ionization Orbitrap mass spectrometry (UPLC-ESI-ORBITRAP MS). Additionally, it compared the efficacy of conventional extraction methods with emerging techniques such as deep eutectic solvent (DES) extraction and hot pressurized water extraction (HPWE). The analysis tentatively identified 107 phenolic compounds (84 of them reported for the first time for this cultivar), including 25 phenolic acids, 37 anthocyanins, and 45 flavonoids. Among the prominent and previously unreported polyphenols are ellagic acid acetyl-xyloside, 3-p-coumaroylquinic acid, cyanidin 3-O-(6'-caffeoyl-glucoside, and phloretin 2'-O-xylosyl-glucoside. The study found HPWE to be a promising alternative to traditional extraction of hydroxybenzoic acids, while DES extraction was less effective across all categories. The findings reveal that white murta possesses diverse phenolic compounds, potentially linked to various biological activities.
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ETHNOPHARMACOLOGICAL RELEVANCE: H. pectinata (L.) Poit, popularly known as "sambacaitá" or "canudinho", is a plant endemic to north-eastern Brazil. Its aerial parts, leaves and flowers have traditionally been used to treat gastrointestinal disorders, rhinopharyngitis, nasal congestion, bacterial and fungal infections, fever, colic, inflammation, and pain. AIM OF THE STUDY: The aim of this review was to provide information on the botanical characteristics, ethnomedicinal uses, phytochemistry and biological-pharmacological activities of H. pectinata. MATERIALS AND METHODS: This systematic review followed the Cochrane Handbook Collaboration and the PRISMA guidelines. The review question was what are the biological-pharmacological activities of H. pectinata presented in non-clinical studies. The search for articles was conducted in the Medline (via PubMed), Embase, Web of Science, Scopus, Virtual Health Library, SciELO, Google Scholar and the Brazilian Digital Library of Theses and Dissertations databases. Two reviewers independently selected the studies that met the inclusion criteria, extracted the data, and assessed the risk of bias of the included studies. RESULTS: 39 articles were included in this review, of which 19 reported in vitro experiments, 16 in vivo studies and 4 in vivo and in vitro experiments. H. pectinata is a plant widely used in folk medicine in north-eastern Brazil for the treatment of various ailments, such as respiratory diseases, gastrointestinal disorders, bacterial and fungal infections, and general inflammation. Supporting its popular use, several in vitro and in vivo pharmacological investigations of the essential oil and extract of H. pectinata have demonstrated their anti-inflammatory, antinociceptive, antioxidant, antidepressant, anticancer, hepatoregenerative, healing, and antimicrobial activities. H. pectinata has been reported to contain 75 bioactive constituents, comprising 9 flavonoids, 54 terpenes, and 12 other compounds. CONCLUSION: H. pectinata is a plant commonly used in traditional medicine. Phytochemically, it contains several bioactive constituents, including terpenes and flavonoids, and has been shown to have antinociceptive, anti-inflammatory, antimicrobial and antitumour activity, as well as hepatorregenerative and healing effects, and low toxicity.