The LABEXTRACT plant extract bank, featuring diverse members of the Myrtaceae family from Brazilian hot spot regions, provides a promising avenue for bioprospection. Given the pivotal roles of the ...Spike protein and 3CL
and PL
proteases in SARS-CoV-2 infection, this study delves into the correlations between the Myrtaceae species from the Atlantic Forest and these targets, as well as an antiviral activity through both
and
analyses. The results uncovered notable inhibitory effects, with
and
standing out, while
proved to be multitarget, presenting inhibition values above 72% in the three targets analyzed. All extracts inhibited viral replication in Calu-3 cells (EC
was lower than 8.3 µg·mL
). Chemometric analyses, through LC-MS/MS, encompassing prediction models and molecular networking, identified potential active compounds, such as myrtucommulones, described in the literature for their antiviral activity. Docking analyses showed that one undescribed myrtucommulone (m/z 841 M - H
) had a higher fitness score when interacting with the targets of this study, including ACE2, Spike, PL
and 3CL
of SARS-CoV-2. Also, the study concludes that Myrtaceae extracts, particularly from
and
, exhibit promising inhibitory effects against crucial stages in SARS-CoV-2 infection. Compounds like myrtucommulones emerge as potential anti-SARS-CoV-2 agents, warranting further exploration.
Natural products are an important source of bioproducts with pharmacological properties. Here we investigate the components of leaves from M. tomentosa Benth. (Fritsch) (Chrysobalanaceae) and its ...effects on bacterial cell growth, biofilm production and macrophage activity.
The effect of the different leaf extracts against bacterial cell growth was performed using the microdilution method. The most active extract was analyzed by mass spectrometry, and its effect on bacterial biofilm production was evaluated on polystyrene plates. The extract effect on macrophage activity was tested in the RAW264.7 cell line, which was stimulated with different concentrations of the extract in the presence or absence of LPS.
We show that the ethyl acetate (EtOAc) extract was the most effective against bacterial cell growth. EtOAc extract DI-ESI (-)MS
analysis showed the presence of a glycosylated flavonoid tentatively assigned as myricetin 3-O-xylosyl-rhamnoside (MW 596). Also, the EtOAc extract increased biofilm formation by S. aureus and inhibited cytokine and NO production induced by LPS in RAW macrophages.
M. tomentosa flavonoid-enriched EtOAc extract presented a bactericidal and anti-inflammatory pharmacological potential.
Zika virus (ZIKV) is involved in the etiology of serious nervous system pathologies. Currently, there are no specific and effective vaccines or antiviral drugs to prevent the diseases caused by ZIKV. ...This study aimed to assess the activity of flavonoids present in crude hydroethanolic extract (CHE) and fractions obtained from B. holophylla leaves against ZIKV. O-glycosylated flavonoids were characterized by high-performance liquid chromatography coupled with high-resolution mass spectrometry (LC-HRMS/MS). The cytotoxic concentration and the effective concentration for 50% of the cells (CC50 and EC50, respectively) were determined, and the selectivity index (SI) was calculated. Molecular networks were constructed based on the chemical composition of the samples and global antiviral activity data using the Global Natural Products Social Molecular Networking (GNPS) platform. Protein–ligand docking was performed in the NS2B-NS3 protease, NS3 helicase, and NS5 methyltransferase of the ZIKV. CHE showed greater antiviral activity at a multiplicity of infection (MOI) of 1.0, with an EC50 of 11.93 µg/mL, SI = 13.38, and reduced cytopathic effects. Molecular networks indicated that O-glycosylated flavonoids are responsible for the activity against ZIKV, being quercetin-O-deoxyhexoside more selective and effective. Molecular docking confirmed the inhibitory activity of quercetin-O-deoxyhexoside, which showed an affinity for the tested targets, especially for NS2B-NS3 protease. The results showed that B. holophylla has flavonoids with potential for future therapeutic applications against ZIKV.
Snakebite envenomation (SBE) is the world's most lethal neglected tropical disease. Bothrops jararaca is the species that causes the greatest number of SBEs in the South and Southeastern of Brazil. ...The main symptoms are local (inflammation, edema, hemorrhage, and myonecrosis) and systemic (hemorrhage, hemostatic alterations with consumptive coagulopathy, and death) effects. Species of the genus Siparuna, Siparunaceae, are used in folk and traditional medicine to treat SBE. However, limited information is available concerning Brazilian Siparuna species against SBE.
To investigate the correlation between the compounds present in the extracts of five Siparuna species as potential agents against proteolytic activity, plasma coagulation, and phospholipase A2 (PLA2) activity caused by B. jararaca venom, using data obtained by UHPLC-MS/MS, biological activity, and multivariate statistics.
The ethanol extracts from leaves of S. ficoides, S. decipiens, S. glycycarpa, S. reginae, and S. cymosa were fractionated by liquid-liquid extraction using different solvents of increasing polarity (hexane, dichloromethane, ethyl acetate, and n-butanol), affording their respective extracts, totaling 25 samples that were assayed through in vitro plasma coagulation and proteolytic activity assays. Moreover, the extracts were analyzed by UHPLC-MS/MS, using electrospray ionization (ESI) and atmospheric-pressure chemical ionization (APCI) in negative and positive ionization modes. The data was processed in MZmine v. 2.53 and evaluated by multivariate statistical tests (PLS) using the software UnscramblerX v. 10.4. These data were also used to build molecular networks (GNPS), and some ions of interest could be annotated using the library of molecules on the GNPS platform.
A total of 19 extracts inhibited B. jararaca-induced plasma coagulation, with emphasis on S. cymosa and S. reginae (800 s). The inhibition of the proteolytic activity was also promising, ranging from 16% (S. glycycarpa) to 99% (S. cymosa, S. decipiens, and S. reginae). In addition, most extracts from S. cymosa and S. reginae inhibited 70–90% of PLA2 activity. Based on data from positive mode APCI analyses, it was possible to obtain a statistic model with reliable predictive capacity which exhibited an average R2 of 0.95 and a Q2 of 0.88, indicating a robust fit. This process revealed five ions, identified as the alkaloids: coclaurine (1), stepholidine (2) O-methylisopiline (3), nornantenine (4) and laurolitsine (5). This is the first study to evidence the potential antivenom of alkaloids from Siparuna species.
Altogether, our results give support to the popular use of Siparuna extracts in SBE accidents, suggesting their potential as an alternative or complementary strategy against envenoming by B. jararaca venom. The predicted ions in the chemometric analysis for the assayed activities can also be correlated with the blocking activity and encourage the continuation of this study for possible isolation and testing of individual compounds on the used models.
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•Siparuna spp. are used in folk medicine to counter snakebite envenomation in tropics.•Siparuna extracts inhibited B. jararaca snake venom proteolytic activity (30–96%).•Siparuna extracts inhibit B. jararaca venom-induced plasma coagulation (75–800s).•Siparuna extracts can inhibit up to 90% of PLA2 of B. jararaca activity.•Five alkaloids in the PLSr model are candidates with potential antivenom activity.
Siparuna species are used in Brazilian Folk Medicine for the treatment and prophylaxis of colds, fever, headache, gastrointestinal disorders and rheumatic pain.
This study aimed to investigate a ...possible anti-influenza activity of 25 extracts from leaves of Amazonian S. cristata, S. decipiens, S. glycycarpa, S. reginae and S. sarmentosa based on their folk medicinal uses as well as to investigate their metabolic fingerprinting. The chemical composition of the active extracts was further dereplicated.
The chemical composition of the crude EtOH extracts from five Siparuna species were investigated by ESI (±) LC-QTOF-MS2. Organic extracts were obtained by liquid-liquid partition with solvents of increasing polarity, generating 25 extracts which were subjected to a quick DI-ESI (±) IT-MS fingerprint analysis. These extracts were tested against influenza virus replication and cellular toxicity using MDCK cells and influenza A/Michigan/45/2015 (H1N1)pdm09 virus. The compounds in the active BuOH extracts from S. glycycarpa and S. sarmentosa were annotated by ESI (±) LC-QTOF-MS2.
Analysis of the EtOH extracts revealed the presence of alkaloids and flavonoids, in the positive and negative ionization modes. Out of the 25 organic extracts screened for their antiviral activity, the BuOH extracts from S. glycycarpa and S. sarmentosa were the most active, inhibiting 96.0 ± 1.3% and 89.5 ± 0.8% of influenza virus replication 24 h post-infection. These inhibitory effects were maintained until 72hpi. Alkaloids, O- and C-flavonoid glycosides, dihydrochalcones and a procyanidin dimer were annotated in these extracts.
The inhibitory effect against influenza A(H1N1)pdm09 virus replication shown by Amazonian Siparuna species corroborates the use of these plants in Brazilian Folk Medicine, showing their potential as anti-influenza agents. These promising results stimulate the continuation of this study with the aim of isolating the compound(s) responsible for this bioactivity, thus contributing to a better knowledge of those species and to the research of natural products with potential anti-influenza activity.
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Characteristics such as calcareous morphology and life cycle are used to understand the ecology of calcified rhodophytes. However, there is limited information regarding their chemical profiles and ...biological activities. Therefore, a systematic review (PRISMA) was conducted to assess the influence of the chemistry of calcareous rhodophytes on ecological interactions in the marine environment. The keywords used were: "Chemical AND Ecology OR Interaction OR Response OR Defense OR Effect OR Cue OR Mediated OR Induce" AND "Red Seaweed" OR "Red Macroalgae" OR Rhodophy? AND Calcified OR Calcareous in Science Direct, Scielo, PUBMED, Springer, Web of Science, and Scopus. Only English articles within the proposed theme were considered. Due to the low number of articles, another search was conducted with three classes and 16 genera. Finally, 67 articles were considered valid. Their titles, abstracts, and keywords were analyzed using IRaMuTeQ through factorial, hierarchical and similarity classification. Most of the studies used macroalgae thallus to evaluate chemical mediation while few tested crude extracts. Some substances were noted as sesquiterpene (6-hydroxy-isololiolide), fatty acid (heptadeca5,8,11-triene) and dibromomethane. The articles were divided into four classes: Herbivory, Competition, Settlement/Metamorphosis, and Epiphytism. Crustose calcareous algae were associated with studies of Settlement/Metamorphosis, while calcified algae were linked to herbivory. Thus, the importance of chemistry in the ecology of these algae is evident,and additional studies are needed to identify the substances responsible for ecological interactions. This study collected essential information on calcified red algae, whose diversity appears to be highly vulnerable to the harmful impacts of ongoing climate change.Characteristics such as calcareous morphology and life cycle are used to understand the ecology of calcified rhodophytes. However, there is limited information regarding their chemical profiles and biological activities. Therefore, a systematic review (PRISMA) was conducted to assess the influence of the chemistry of calcareous rhodophytes on ecological interactions in the marine environment. The keywords used were: "Chemical AND Ecology OR Interaction OR Response OR Defense OR Effect OR Cue OR Mediated OR Induce" AND "Red Seaweed" OR "Red Macroalgae" OR Rhodophy? AND Calcified OR Calcareous in Science Direct, Scielo, PUBMED, Springer, Web of Science, and Scopus. Only English articles within the proposed theme were considered. Due to the low number of articles, another search was conducted with three classes and 16 genera. Finally, 67 articles were considered valid. Their titles, abstracts, and keywords were analyzed using IRaMuTeQ through factorial, hierarchical and similarity classification. Most of the studies used macroalgae thallus to evaluate chemical mediation while few tested crude extracts. Some substances were noted as sesquiterpene (6-hydroxy-isololiolide), fatty acid (heptadeca5,8,11-triene) and dibromomethane. The articles were divided into four classes: Herbivory, Competition, Settlement/Metamorphosis, and Epiphytism. Crustose calcareous algae were associated with studies of Settlement/Metamorphosis, while calcified algae were linked to herbivory. Thus, the importance of chemistry in the ecology of these algae is evident,and additional studies are needed to identify the substances responsible for ecological interactions. This study collected essential information on calcified red algae, whose diversity appears to be highly vulnerable to the harmful impacts of ongoing climate change.
Snakebite envenomation (SBE) is the world's most lethal neglected tropical disease. Bothrops jararaca is the species that causes the greatest number of SBEs in the South and Southeastern of Brazil. ...The main symptoms are local (inflammation, edema, hemorrhage, and myonecrosis) and systemic (hemorrhage, hemostatic alterations with consumptive coagulopathy, and death) effects. Species of the genus Siparuna, Siparunaceae, are used in folk and traditional medicine to treat SBE. However, limited information is available concerning Brazilian Siparuna species against SBE.
To investigate the correlation between the compounds present in the extracts of five Siparuna species as potential agents against proteolytic activity, plasma coagulation, and phospholipase A
(PLA
) activity caused by B. jararaca venom, using data obtained by UHPLC-MS/MS, biological activity, and multivariate statistics.
The ethanol extracts from leaves of S. ficoides, S. decipiens, S. glycycarpa, S. reginae, and S. cymosa were fractionated by liquid-liquid extraction using different solvents of increasing polarity (hexane, dichloromethane, ethyl acetate, and n-butanol), affording their respective extracts, totaling 25 samples that were assayed through in vitro plasma coagulation and proteolytic activity assays. Moreover, the extracts were analyzed by UHPLC-MS/MS, using electrospray ionization (ESI) and atmospheric-pressure chemical ionization (APCI) in negative and positive ionization modes. The data was processed in MZmine v. 2.53 and evaluated by multivariate statistical tests (PLS) using the software UnscramblerX v. 10.4. These data were also used to build molecular networks (GNPS), and some ions of interest could be annotated using the library of molecules on the GNPS platform.
A total of 19 extracts inhibited B. jararaca-induced plasma coagulation, with emphasis on S. cymosa and S. reginae (800 s). The inhibition of the proteolytic activity was also promising, ranging from 16% (S. glycycarpa) to 99% (S. cymosa, S. decipiens, and S. reginae). In addition, most extracts from S. cymosa and S. reginae inhibited 70-90% of PLA
activity. Based on data from positive mode APCI analyses, it was possible to obtain a statistic model with reliable predictive capacity which exhibited an average R
of 0.95 and a Q
of 0.88, indicating a robust fit. This process revealed five ions, identified as the alkaloids: coclaurine (1), stepholidine (2) O-methylisopiline (3), nornantenine (4) and laurolitsine (5). This is the first study to evidence the potential antivenom of alkaloids from Siparuna species.
Altogether, our results give support to the popular use of Siparuna extracts in SBE accidents, suggesting their potential as an alternative or complementary strategy against envenoming by B. jararaca venom. The predicted ions in the chemometric analysis for the assayed activities can also be correlated with the blocking activity and encourage the continuation of this study for possible isolation and testing of individual compounds on the used models.
Ampelozizyphus amazonicus Ducke, known as "saracura‐mirá" in the Amazon rainforest, is valued for its traditional use in malaria prevention and treatment. The plant's roots and bark are employed for ...these purposes, while the wood is often overlooked. Given the global importance of leishmaniasis, research focused on A. amazonicus anti‐Leishmania amazonensis potential. The ethyl acetate extract from the bark (EAEB) exhibited the most effective inhibition of intracellular amastigote growth with IC50 7.0 µg.mL‐1 but showed high toxicity (CC50 9.0 µg.mL‐1). The wood ethanol (EW) and ethyl acetate (EAEW) extracts demonstrated promising results against L. amazonensis with IC50 15.8 µg.mL‐1 and 10.0 µg.mL‐1, CC50 50.5 µg.mL‐1 and 22.7 µg.mL‐1, respectively. High‐speed countercurrent chromatography combined with mass spectrometry off‐line detection was employed for the bioassay‐guided fractionation of EAEB and EAEW using HEMWat as solvent system. These extracts showed to be rich in saponins and triterpenes, besides minor glycosylated flavonoids. HSCCC was effective in obtaining high purity fractions, leading to the identification of a di‐glycosylated triterpene saponin from EAEB, and melaleucic acid from EAEW. These findings highlight A. amazonicus as a potential source for developing new therapeutic alternatives for leishmaniasis and HSCCC as a technique enabling better separation efficiency of complex saponin matrices.
Tétano em equino: Relato de caso Pereira, André Luis de Araújo; Gonçalves, Talia Fabrício; Dantas, Jackson Brendo Gomes ...
PUBVET,
07/2019, Letnik:
13, Številka:
6
Journal Article
Recenzirano
Odprti dostop
This work aimed to report the clinical case of a female horse of the Paint horse race, approximately six years old, attended at the University Veterinary Hospital of the Federal University of Piauí, ...with clinical tetanus. Disease caused by toxins, tetanospasmin and tetanolysin, produced by gram-positive and anaerobic bacteria Clostridium tetani. Because it is a toxic disease with high infection power, it can affect some domestic species, but its epidemiology is more related to equines. For infection to occur and clinical signs of the disease occur, there must be a gateway, such as an injury, or direct contact with secretions from other already infected animals. The animal once infected has clinical signs such as limb rigidity, labial trismus, muscle stiffness, muscle spasms, hyperesthesia, and tail lift. In view of the clinical signs presented, a case of tetanus was diagnosed. The treatment was then started using metronidazole tablets at a dose of 25mg/kg, every 8 hours for 5 days; thiocolchicoside tablets at a dose of 0.05 mg/kg/SID for 5 days; tetanus serum (50,000 IU/animal), every 24 hours for 5 days; and washing the right posterior limb wound daily with water, hydrogen peroxide and topical application of fenitrothion for seven consecutive days. The improvement was gradual and significant with the animal responding very well to the treatment, obtaining expected results, restoring the patient's health. After being discharged after seven days of intensive treatment.
Este trabajo objetivó relatar el caso clínico de una hembra equina de la raza Paint horse, de aproximadamente seis años, atendida en el Hospital Veterinario Universitario de la Universidad Federal de Piauí, con cuadro clínico de tétano. Enfermedad causada por las toxinas, tetanaspasmina y tetanolisina, producidas por la bacteria gram-positiva y anaeróbica Clostridium tetani. Por ser una enfermedad tóxica de alto poder de infección, puede acometer algunas especies domésticas, pero su epidemiología está más ligada a los equinos. Para que ocurra la infección y surgimiento de los signos clínicos de la enfermedad, es necesario que haya una puerta de entrada, como una herida, o contacto directo con secreciones de otros animales ya infectados. El animal una vez infectado presenta signos clínicos como: rigidez de los miembros, trismo labial, rigidez muscular, espasmos musculares, hiperestesia y levantamiento de la cola. Ante los signos clínicos presentados, se diagnosticó un caso de tétano. Se inició luego el tratamiento, utilizando metronidazol comprimidos a la dosis de 25 mg/kg, cada 8 horas durante 5 días; tiocolchicosídeos comprimidos en la dosis de 0,05 mg/kg/SID durante 5 días; suero antitetánico (50.000 UI / animal), cada 24 horas por 5 días; y realizándose el lavado de la herida del miembro posterior derecho diariamente con agua, agua oxigenada y aplicación tópica de fenitrothion por siete días consecutivos. La mejora fue gradual y significativa con el animal respondiendo muy bien al tratamiento, obteniendo resultados esperados, restableciendo la salud del paciente. Teniendo alta médica después de siete días de tratamiento intensivo.
Este trabalho objetivou relatar o caso clínico de uma fêmea equina da raça Paint horse, de aproximadamente seis anos de idade, atendido no Hospital Veterinário Universitário da Universidade Federal do Piauí, com quadro clínico de tétano. Doença causada pelas toxinas, tetanospasmina e tetanolisina, produzidas pela bactéria gram-positiva e anaeróbia Clostridium tetani. Por ser uma doença tóxica de alto poder de infecção, ela pode acometer algumas espécies domésticas, porém sua epidemiologia está mais ligada a equinos. Para que ocorra a infecção e surgimento dos sinais clínicos da doença, é necessário que haja uma porta de entrada, como um ferimento, ou contato direto com secreções de outros animais já infectados. O animal uma vez infectado apresenta sinais clínicos como: rigidez dos membros, trismo labial, rigidez muscular, espasmos musculares, hiperestesia e levantar da cauda. Diante dos sinais clínicos apresentados, diagnosticou-se um caso de tétano. Iniciou-se em seguida o tratamento, utilizando-se metronidazol comprimidos na dose de 25mg/Kg, a cada 8 horas durante 5 dias; tiocolchicosídeo comprimidos na dose de 0,05 mg/Kg/SID durante 5 dias; soro antitetânico (50.000 UI/animal), a cada 24 horas por 5 dias; e realizando-se a lavagem da ferida do membro posterior direito diariamente com água, água oxigenada e aplicação tópica de fenitrothion por sete dias consecutivos. A melhora foi gradativa e significativa com o animal respondendo muito bem ao tratamento, obtendo resultados esperados, restabelecendo a saúde do paciente. Tendo alta médica após sete dias de tratamento intensivo.
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