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1.
J Indian Soc Pedod Prev Dent ; 38(3): 238-246, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33004721

RESUMO

Background: Controlling cariogenic biofilm formation by plant extracts could add to preventive strategies to dental caries. Objective: To evaluate in vitro the role of Aerva Sanguinolenta ethanolic extract on biofilm-induced microbial human enamel demineralization. Methodology: The prepared enamel sections of study group (SG), positive control group (PCG), and negative control group (NCG) were immersed in 2 ml of 0.2% ethanolic extract of A. sanguinolenta, 0.12% chlorhexidine, and distilled water, respectively, for 2 min before subjecting to closed batch culture technique utilizing mono- or dual-species culture media of Streptococcus mutans and Lactobacillus acidophilus. Quantification of biofilm and demineralization of enamel was performed by crystal violet (CV) assay and scanning electron microscope (SEM) attached to energy-dispersive X-ray analysis, respectively. Statistical Analysis: Two-way ANOVA and Tukey's test were used for analysis. Results: CV assay of biofilm recorded the highest and lowest optical absorbance value in NC3 (2.728660) and PC3 (0.364200), respectively. Thus, biofilm formation is highest in NCG and lowest among PCG. Surface roughness and porosity in enamel are greatest among NCG and lowest among SG as evident by SEM. Wt% of calcium (S3 47.7170) and phosphorus ion (S3 22.7330) was highest in SG, closely resembling that of B enamel (Ca = 41.9530, P = 19.6650). Wt% of oxygen is lowest in SG (S3 28.8920) and resembles baseline O2 (37.4950). Thus, the amount of biofilm formation is moderate and amount of demineralization of enamel is least among SGs. Conclusion: Enamel exposed to 2 ml of 0.2% solution of A. sanguinolenta for 2 min could fairly inhibit formation of biofilm and positively inhibit underlying demineralization in cariogenic environment.


Assuntos
Amaranthaceae , Cárie Dentária , Desmineralização do Dente/prevenção & controle , Biofilmes , Esmalte Dentário , Humanos , Extratos Vegetais/farmacologia
2.
Phytomedicine ; 78: 153296, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32890913

RESUMO

BACKGROUND: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has extensively and rapidly spread in the world, causing an outbreak of acute infectious pneumonia. However, no specific antiviral drugs or vaccines can be used. Phillyrin (KD-1), a representative ingredient of Forsythia suspensa, possesses anti-inflammatory, anti-oxidant, and antiviral activities. However, little is known about the antiviral abilities and mechanism of KD-1 against SARS-CoV-2 and human coronavirus 229E (HCoV-229E). PURPOSE: The study was designed to investigate the antiviral and anti-inflammatory activities of KD-1 against the novel SARS-CoV-2 and HCoV-229E and its potential effect in regulating host immune response in vitro. METHODS: The antiviral activities of KD-1 against SARS-CoV-2 and HCoV-229E were assessed in Vero E6 cells using cytopathic effect and plaque-reduction assay. Proinflammatory cytokine expression levels upon infection with SARS-CoV-2 and HCoV-229E infection in Huh-7 cells were measured by real-time quantitative PCR assays. Western blot assay was used to determine the protein expression of nuclear factor kappa B (NF-κB) p65, p-NF-κB p65, IκBα, and p-IκBα in Huh-7 cells, which are the key targets of the NF-κB pathway. RESULTS: KD-1 could significantly inhibit SARS-CoV-2 and HCoV-229E replication in vitro. KD-1 could also markedly reduce the production of proinflammatory cytokines (TNF-α, IL-6, IL-1ß, MCP-1, and IP-10) at the mRNA levels. Moreover, KD-1 could significantly reduce the protein expression of p-NF-κB p65, NF-κB p65, and p-IκBα, while increasing the expression of IκBα in Huh-7 cells. CONCLUSIONS: KD-1 could significantly inhibit virus proliferation in vitro, the up-regulated expression of proinflammatory cytokines induced by SARS-CoV-2 and HCoV-229E by regulating the activity of the NF-кB signaling pathway. Our findings indicated that KD-1 protected against virus attack and can thus be used as a novel strategy for controlling the coronavirus disease 2019.


Assuntos
Anti-Inflamatórios/farmacologia , Antivirais/farmacologia , Betacoronavirus/efeitos dos fármacos , Coronavirus Humano 229E/efeitos dos fármacos , Infecções por Coronavirus , Glucosídeos/farmacologia , NF-kappa B/metabolismo , Pandemias , Pneumonia Viral , Animais , Chlorocebus aethiops , Coronavirus/efeitos dos fármacos , Infecções por Coronavirus/metabolismo , Infecções por Coronavirus/virologia , Citocinas/metabolismo , Forsythia/química , Humanos , Fitoterapia , Extratos Vegetais/farmacologia , Pneumonia Viral/metabolismo , Pneumonia Viral/virologia , Síndrome Respiratória Aguda Grave/virologia , Transdução de Sinais/efeitos dos fármacos , Células Vero , Replicação Viral/efeitos dos fármacos
3.
Virol J ; 17(1): 136, 2020 09 09.
Artigo em Inglês | MEDLINE | ID: mdl-32907596

RESUMO

BACKGROUND: Coronaviruses (CoVs) were long thought to only cause mild respiratory and gastrointestinal symptoms in humans but outbreaks of Middle East Respiratory Syndrome (MERS)-CoV, Severe Acute Respiratory Syndrome (SARS)-CoV-1, and the recently identified SARS-CoV-2 have cemented their zoonotic potential and their capacity to cause serious morbidity and mortality, with case fatality rates ranging from 4 to 35%. Currently, no specific prophylaxis or treatment is available for CoV infections. Therefore we investigated the virucidal and antiviral potential of Echinacea purpurea (Echinaforce®) against human coronavirus (HCoV) 229E, highly pathogenic MERS- and SARS-CoVs, as well as the newly identified SARS-CoV-2, in vitro. METHODS: To evaluate the antiviral potential of the extract, we pre-treated virus particles and cells and evaluated remaining infectivity by limited dilution. Furthermore, we exposed cells to the extract after infection to further evaluate its potential as a prophylaxis and treatment against coronaviruses. We also determined the protective effect of Echinaforce® in re-constituted nasal epithelium. RESULTS: In the current study, we found that HCoV-229E was irreversibly inactivated when exposed to Echinaforce® at 3.2 µg/ml IC50. Pre-treatment of cell lines, however, did not inhibit infection with HCoV-229E and post-infection treatment had only a marginal effect on virus propagation at 50 µg/ml. However, we did observe a protective effect in an organotypic respiratory cell culture system by exposing pre-treated respiratory epithelium to droplets of HCoV-229E, imitating a natural infection. The observed virucidal activity of Echinaforce® was not restricted to common cold coronaviruses, as both SARS-CoV-1 and MERS-CoVs were inactivated at comparable concentrations. Finally, the causative agent of COVID-19, SARS-CoV-2 was also inactivated upon treatment with 50µg/ml Echinaforce®. CONCLUSIONS: These results show that Echinaforce® is virucidal against HCoV-229E, upon direct contact and in an organotypic cell culture model. Furthermore, MERS-CoV and both SARS-CoV-1 and SARS-CoV-2 were inactivated at similar concentrations of the extract. Therefore we hypothesize that Echinacea purpurea preparations, such as Echinaforce®, could be effective as prophylactic treatment for all CoVs due to their structural similarities.


Assuntos
Antivirais/farmacologia , Betacoronavirus/efeitos dos fármacos , Coronavirus Humano 229E/efeitos dos fármacos , Infecções por Coronavirus/tratamento farmacológico , Coronavirus/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Linhagem Celular , Chlorocebus aethiops , Resfriado Comum/tratamento farmacológico , Resfriado Comum/virologia , Infecções por Coronavirus/virologia , Humanos , Coronavírus da Síndrome Respiratória do Oriente Médio/efeitos dos fármacos , Pandemias , Pneumonia Viral/tratamento farmacológico , Pneumonia Viral/virologia , Vírus de RNA/efeitos dos fármacos , Ensaios Clínicos Controlados Aleatórios como Assunto , Síndrome Respiratória Aguda Grave/tratamento farmacológico , Síndrome Respiratória Aguda Grave/virologia , Células Vero
4.
Anticancer Res ; 40(9): 5015-5024, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32878789

RESUMO

BACKGROUND/AIM: Despite being a rare disease, melanoma is considered the most dangerous skin cancer due to its highly invasive and aggressive nature, and still requires for more effective treatments. The aim of this study was to evaluate the in vitro anti-melanoma potential of Ephedranthus pisocarpus R.E.Fr. (Annonaceae), a popular Brazilian plant with medicinal properties. MATERIALS AND METHODS: Initially, the ethanolic extract (EtOH) was obtained from E. pisocarpus leaves and later partitioned using increasing polarity solvents. The anti-melanoma potential of E. pisocarpus was assessed by spectrophotometry and its cytotoxicity determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and confocal microscopy. RESULTS: We demonstrated that the EtOH extract and fractions from E. pisocarpus had a moderate photoprotective action (FPS 3.0-5.0) against UVA radiation. Interestingly, the dichloromethane fraction presented higher anti-melanoma activity against B16-F10 (IC50=46.8 µg/ml) and SK-MEL-28 cells (IC50=40.1 µg/ml) and lesser toxicity on normal cells. Additionally, our study reported that spathulenol, one of the major constituents from E. pisocarpus, acts through an apoptosis-dependent mechanism in SK-MEL-28 cells. CONCLUSION: The present study demonstrated, for the first time, the in vitro anti-melanoma potential of E. pisocarpus against melanoma cells.


Assuntos
Annonaceae/química , Antineoplásicos Fitogênicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Brasil , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citotoxicidade Imunológica , Relação Dose-Resposta a Droga , Hemólise , Humanos , Melanoma Experimental , Camundongos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
5.
Anticancer Res ; 40(9): 5201-5210, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32878808

RESUMO

BACKGROUND/AIM: Persimmon (Diospyros kaki L.) leaves are popular as a tea infusion in Asia and their main active ingredients are flavonoids. The present study aimed to explore the anticancer properties of flavonoids isolated from persimmon leaves (PLF). MATERIALS AND METHODS: We investigated the in vitro anti-proliferative activity of PLF against several human cancer cell lines. Apoptosis and intracellular reactive oxygen species (ROS) induced by PLF were accessed using high-content analysis with florescent staining. The ability of PLF to scavenge free radicals was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. RESULTS: PLF demonstrated significant inhibition of proliferation of liver, breast, and colorectal cancer cells in vitro. PLF induced apoptosis and increased intracellular ROS levels in HCT116 (colorectal cancer) and HepG2 (liver cancer) cells. In addition, PLF showed strong free radical scavenging ability. CONCLUSION: The anti-proliferation activity of PLF against cancer cells was related to the induction of apoptosis and oxidative stress.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Diospyros/química , Flavonoides/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Flavonoides/química , Flavonoides/isolamento & purificação , Humanos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Espécies Reativas de Oxigênio/metabolismo
6.
PLoS One ; 15(8): e0236633, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32785249

RESUMO

The induction of general plant defense responses following the perception of external elicitors is now regarded as the first level of the plant immune response. Depending on the involvement or not of these molecules in pathogenicity, this induction of defense is called either Pathogen-Associated Molecular Pattern (PAMP) Triggered Immunity or Pattern Triggered Immunity-both abbreviated to PTI. Because PTI is assumed to be a widespread and stable form of resistance to infection, understanding the mechanisms driving it becomes a major goal for the sustainable management of plant-pathogen interactions. However, the induction of PTI is complex. Our hypotheses are that (i) the recognition by the plant of PAMPs vs non-PAMP elicitors leads to specific defense profiles and (ii) the responses specifically induced by PAMPs target critical life history traits of the pathogen that produced them. We thus analyzed, using a metabolomic approach coupled with transcriptomic and hormonal analyses, the defense profiles induced in potato foliage treated with either a Concentrated Culture Filtrate (CCF) from Phytophthora infestans or two non-PAMP preparations, ß-aminobutyric acid (BABA) and an Ulva spp. Extract, used separately. Each elicitor induced specific defense profiles. CCF up-regulated sesquiterpenes but down-regulated sterols and phenols, notably α-chaconine, caffeoyl quinic acid and rutin, which decreased spore production of P. infestans in vitro. CCF thus induces both defense and counter-defense responses. By contrast, the Ulva extract triggered the synthesis of a large-spectrum of antimicrobial compounds through the phenylpropanoid/flavonoid pathways, while BABA targeted the primary metabolism. Hence, PTI can be regarded as a heterogeneous set of general and pathogen-specific responses triggered by the molecular signatures of each elicitor, rather than as a uniform, non-specific and broad-spectrum set of general defense reactions.


Assuntos
Resistência à Doença/imunologia , Doenças das Plantas/imunologia , Imunidade Vegetal/imunologia , Solanum tuberosum/imunologia , Aminobutiratos/farmacologia , Resistência à Doença/efeitos dos fármacos , Flavonoides/biossíntese , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Interações Hospedeiro-Patógeno/genética , Interações Hospedeiro-Patógeno/imunologia , Fenóis/metabolismo , Phytophthora infestans/imunologia , Phytophthora infestans/patogenicidade , Doenças das Plantas/microbiologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Imunidade Vegetal/efeitos dos fármacos , Sesquiterpenos/metabolismo , Solanum tuberosum/crescimento & desenvolvimento , Solanum tuberosum/microbiologia , Esteróis/metabolismo , Ulva/química
7.
PLoS One ; 15(8): e0236879, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32790676

RESUMO

Benign prostatic hyperplasia (BPH) is a progressive pathological condition associated with proliferation of prostatic tissues, prostate enlargement, and lower-urinary tract symptoms. However, the mechanism underlying the pathogenesis of BPH is unclear. The aim of this study was to investigate the protective effects of a combination of Stauntonia hexaphylla and Cornus officinalis (SC extract) on a testosterone propionate (TP)-induced BPH model. The effect of SC extract was examined in a TP-induced human prostate adenocarcinoma cell line. Male Sprague-Dawley rats were randomly divided into 5 groups (n = 6) for in vivo experiments. To induce BPH, all rats, except those in the control group, were administered daily with subcutaneous injections of TP (5 mg/kg) and orally treated with appropriate phosphate buffered saline/drugs (finasteride/saw palmetto/SC extract) for 4 consecutive weeks. SC extract significantly downregulated the androgen receptor (AR), prostate specific antigen (PSA), and 5α-reductase type 2 in TP-induced BPH in vitro. In in vivo experiments, SC extract significantly reduced prostate weight, size, serum testosterone, and dihydrotestosterone (DHT) levels. Histologically, SC extract markedly recovered TP-induced abnormalities and reduced prostatic hyperplasia, thereby improving the histo-architecture of TP-induced BPH rats. SC extract also significantly downregulated AR and PSA expression, as assayed using immunoblotting. Immunostaining revealed that SC extract markedly reduced the 5α-reductase type 2 and significantly downregulated the expression of proliferating cell nuclear antigen. In addition, immunoblotting of B-cell lymphoma 2 (Bcl-2) family proteins indicated that SC extract significantly downregulated anti-apoptotic Bcl-2 and markedly upregulated pro-apoptotic B cell lymphoma-associated X (Bax) expression. Furthermore, SC treatment significantly decreased the Bcl-2/Bax ratio, indicating induced prostate cell apoptosis in TP-induced BPH rats. Thus, our findings demonstrated that SC extract protects against BPH by inhibiting 5α-reductase type 2 and inducing prostate cell apoptosis. Therefore, SC extract might be useful in the clinical treatment of BPH.


Assuntos
Apoptose/efeitos dos fármacos , Colestenona 5 alfa-Redutase/química , Extratos Vegetais/farmacologia , Hiperplasia Prostática/prevenção & controle , Substâncias Protetoras/uso terapêutico , Inibidores de 5-alfa Redutase/química , Inibidores de 5-alfa Redutase/farmacologia , Inibidores de 5-alfa Redutase/uso terapêutico , Animais , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Colestenona 5 alfa-Redutase/metabolismo , Cornus/química , Cornus/metabolismo , Regulação para Baixo/efeitos dos fármacos , Humanos , Masculino , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Folhas de Planta/metabolismo , Antígeno Prostático Específico/sangue , Hiperplasia Prostática/etiologia , Substâncias Protetoras/farmacologia , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Ranunculales/química , Ranunculales/metabolismo , Ratos , Ratos Sprague-Dawley , Propionato de Testosterona/efeitos adversos
8.
Toxicon ; 186: 182-190, 2020 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-32822735

RESUMO

Snakebites produce several toxic effects in victims, such as hemorrhage, tissue necrosis, hemostatic, renal, or cardiotoxic alterations, inflammation, and death. To counteract these symptoms, antivenom is the official treatment. Although such therapy prevents death, it does not efficiently neutralize necrosis or other local effects, leading to amputation or morbidities of the affected limb. Therefore, the search for better and more efficient therapies deserves attention; further, plants have been used to ameliorate a number of diseases and medical conditions, including snakebites, for many years. Thus, the aim of this work was to evaluate the antivenom effect of the crude extract, fractions (aqueous and diethyl acetate), and subfractions derived from the aqueous fraction (P1, P2, P3, and P4) of the plant Stryphnodendron adstringens against in vitro (coagulation and proteolytic) and in vivo (edema, hemorrhage, and myotoxic) activities caused by Bothrops jararacussu venom. Overall, all extracts inhibited the toxic effect of B. jararacussu venom, but with different potencies, regardless of whether plant samples were incubated together with venom or injected before or after venom injection into animals; the crude extract and aqueous fraction were found to be the most effective. Indeed, phytochemical and mass spectrometry analysis of S. adstringens samples revealed the presence of flavonols, tannins, and saponins. In conclusion, the plant S. adstringens may represent a promising natural source of molecules to treat the toxic effects associated with envenomation by B. jararacussu snakebites.


Assuntos
Bothrops , Venenos de Crotalídeos/toxicidade , Fabaceae , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Animais , Antivenenos , Edema , Hemorragia , Mordeduras de Serpentes
9.
PLoS One ; 15(8): e0231612, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32810139

RESUMO

The recent focus is on the analysis of biological activities of extracts from thirteen folk medicinal plants from arid and semi-arid zones of Balochistan, Pakistan. Only a small proportion of them have been scientifically analyzed. Therefore the present investigation explores the biochemical and bioactive potential of different plant parts. Superoxide dismutase was detected maximum in Fagonia indica, (184.7±5.17 units/g), ascorbate peroxidase in Tribulus pentandrus (947.5±12.5 units/g), catalase and peroxidase were higher in Peganum harmala (555.0±5.0 and 2597.8±0.4 units/g, respectively). Maximum esterase and α-amylase activity was found in Zygophyllum fabago (14.3±0.44 and 140±18.8 mg/g, respectively). Flavonoid content was high in T. pentandrus (666.1±49 µg/ml). The highest total phenolic content and tannin was revealed in F. olivieri (72125±425 and 37050±1900 µM/g, respectively). The highest value of ascorbic acid was depicted in F. bruguieri (F.b.N) (448±1.5 µg/g). Total soluble proteins and reducing sugars were detected higher in P. harmala (372.3±54 and 5.9±0.1 mg/g, respectively). The maximum total antioxidant capacity was depicted in Tetraena simplex (16.9±0.01 µM/g). The highest value of lycopene and total carotenoids exhibited in T. terrestris (7.44±0.2 and 35.5±0.0 mg/g, respectively). Chlorophyll contents were found maximum in T. pentandrus var. pterophorus (549.1±9.9, 154.3±10, and 703.4±20.2 ug/g, respectively). All taxa exhibited anti-inflammatory activity and anti-diabetic potential. Z. eurypterum seeds exhibited the highest anti-inflammatory potential (96%), along with other taxa indicated (96-76%) activity when compared with the standard drug diclofenac sodium (79%). Seeds of T. pentandrus (85%) exhibited the highest anti-diabetic activity. The other taxa also exhibited inhibitory activity of α-amylase ranging from (85-69%) compared with Metformin (67%) standard drug. Phytochemical screening revealed that selected taxa proved to be the potential source of natural antioxidants and could further be explored for in-vivo studies and utilized in pharmaceutical industries as potent therapeutic agents validating their ethno-pharmacological uses.


Assuntos
Medicina Tradicional/métodos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Anti-Inflamatórios , Antioxidantes/farmacologia , Flavonoides/farmacologia , Paquistão , Fenóis/farmacologia , Compostos Fitoquímicos , Plantas Medicinais/química
10.
Life Sci ; 258: 118222, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32768577

RESUMO

AIMS: We previously reported that fenugreek-derived 4-hydroxyisoleucine ameliorates insulin resistance via regulation of TNF-α converting enzyme (TACE) expression. In the present study, we further investigate the effects and mechanisms of fenugreek on obesity-induced inflammation and insulin signaling in the high-fat diet (HFD)-challenged obese mice. MAIN METHODS: After 12 weeks of HFD intervention, mice were treated with the low or high dosages of fenugreek. Serum levels of glucose, insulin, lipid profile, inflammation cytokines, and adipokines were detected. Macrophage infiltration and adipose tissue morphology were observed. Western blot was conducted to investigate the expressions of inactive rhomboid 2 (iRhom2) and TACE as well as other signaling pathways in subcutaneous adipose tissue. KEY FINDINGS: We showed that fenugreek significantly suppressed body weight gain and fat accumulation in HFD-challenged obese mice. Meanwhile, fasting glucose, insulin, and HOMA-IR in fenugreek-treated mice were remarkably decreased, which were properly explained by fenugreek-induced activation of the insulin receptor signaling pathway. Moreover, the anti-inflammatory properties of fenugreek were shown by the decrease of systemic and local expressions of pro-inflammatory cytokines as well as reduced macrophage infiltration into adipose tissue. Additionally, fenugreek markedly deactivated NF-κB and JNK pathways. Finally, we demonstrated that fenugreek strikingly repressed the transcriptions and expressions of iRhom2 and TACE. SIGNIFICANCE: Fenugreek shows an encouraging and promising property in ameliorating insulin resistance and suppressing inflammation in obesity, which might be realized by fenugreek-mediated inhibition of iRhom2/TACE axis-facilitated TNF-α release from adipocytes.


Assuntos
Proteína ADAM17/antagonistas & inibidores , Proteínas de Transporte/antagonistas & inibidores , Mediadores da Inflamação/antagonistas & inibidores , Resistência à Insulina/fisiologia , Obesidade/tratamento farmacológico , Trigonella , Proteína ADAM17/sangue , Animais , Proteínas de Transporte/sangue , Relação Dose-Resposta a Droga , Regulação para Baixo/efeitos dos fármacos , Regulação para Baixo/fisiologia , Inflamação/sangue , Inflamação/tratamento farmacológico , Mediadores da Inflamação/sangue , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/sangue , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Sementes
11.
PLoS One ; 15(8): e0235723, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32797045

RESUMO

Mixtures of drugs often have greater therapeutic value than any of their constituent drugs alone, and such combination therapies are widely used to treat diseases such as cancer, malaria, and viral infections. However, developing useful drug mixtures is challenging due to complex interactions between drugs. Natural substances can be fruitful sources of useful drug mixtures because secondary metabolites produced by living organisms do not often act in isolation in vivo. In order to facilitate the study of interactions within natural substances, a new analytical method to quantify interactions using data generated in the process of bioassay-guided fractionation is presented here: the extract fractional inhibitory concentration index (EFICI). The EFICI method uses the framework of Loewe additivity to calculate fractional inhibitory concentration values by which interactions can be determined for any combination of fractions that make up a parent extract. The EFICI method was applied to data on the bioassay-guided fractionation of Lechea mucronata and Schinus terebinthifolia for growth inhibition of the pathogenic bacterium Acinetobacter baumannii. The L. mucronata extract contained synergistic interactions (EFICI = 0.4181) and the S. terebinthifolia extract was non-interactive overall (EFICI = 0.9129). Quantifying interactions in the bioassay-guided fractionation of natural substances does not require additional experiments and can be useful to guide the experimental process and to support the development of standardized extracts as botanical drugs.


Assuntos
Antibacterianos/farmacologia , Produtos Biológicos/farmacologia , Extratos Vegetais/farmacologia , Infecções por Acinetobacter/tratamento farmacológico , Acinetobacter baumannii/efeitos dos fármacos , Anacardiaceae/química , Antibacterianos/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Fracionamento Químico , Descoberta de Drogas , Avaliação Pré-Clínica de Medicamentos/métodos , Sinergismo Farmacológico , Humanos , Extratos Vegetais/isolamento & purificação
12.
Mikrobiyol Bul ; 54(3): 463-478, 2020 Jul.
Artigo em Turco | MEDLINE | ID: mdl-32755521

RESUMO

Malaria still remains to be a public health threat and one of the most important infectious diseases to get attention from World Health Organization. No domestic malaria cases have been reported on the island of Cyprus since 1948, as a result of successful elimination process. All of the malaria cases detected in recent years are imported cases. As known, hundreds of medicines are obtained from plants and traditional medicine are used in endemic places of malaria. The cause of malaria - Plasmodium parasites, are developing resistance to antimalarial drugs. Hence, research on plant extracts and essential oils have gained great interest in recent years to obtain new and safe agents/substances. In our study, it was aimed to investigate the in vivo antimalarial activities of essential oils obtained from Origanum dubium, Origanum majorana, Salvia fruticosa and Laurus nobilis plants which grows in Northern Cyprus against Plasmodium berghei - the rodent malaria agent. Plants were collected in appropriate seasons and were dried to obtain and analyze essential oils via Clevenger Apparatus system. L929 mouse fibroblast cell line and MTT [3-(4.5-dimethylthiazole-2-yl) -2.5-diphenyltetrazolium bromide] kit were used to determine the cytotoxic activities of the essential oils obtained. In our study, total of 36 mice (Balb/c) of 6 groups (6 mice in each group) were formed: chloroquine group (CG) (50 mg/kg) as malaria reference group, untreated control group (UTCG), O.dubium (OD) (20 mg/kg), O.majorana (OM) (20 mg/kg), S.fruticosa (SF) (20 mg/kg) and L.nobilis (LN) (20 mg/kg). The essential oils were given to mice infected with P.berghei strain orally on 0, 1, 2 and 3rd days (4 times in total). Blood was taken from the tail end of each mouse 24 hours after the last treatment and blood collection was continued every two days until the mice died. Withdrawn blood taken from the mice were prepared as a thin smear and stained with Giemsa. Then, parasitemia percentages in each smear were calculated. As a result of the cytotoxicity tests, cytotoxic activity was not found at 100 µg/ml (20 mg/kg) in all oils except OD essential oil. While the mice receiving chloroquine continued their lives with the disappearance of the parasite on the 6thday, the mice in the UTCG died on the 9th day. The parasitemia rate reached 35% in the OM group on the 23rd day, in the OD group on the 21st day and in the other groups (SF and LN) on the 14th day and the mice have died. In our study, the difference between the life span in all groups was found statistically significant (p≤ 0.001). As a result, the essential oils O.majorana (14 days increase according to UTCG) an endemic plant of Cyprus and O.dubium (12 days increase according to UTCG) which had an antimalarial effect, decreased parasitemia and increased the life span of mice more than two times, indicated that they could be a source for the acquisition of new antimalarial molecules.


Assuntos
Antimaláricos , Malária , Óleos Voláteis , Origanum , Extratos Vegetais , Animais , Antimaláricos/farmacologia , Antimaláricos/uso terapêutico , Chipre , Células Alimentadoras , Malária/tratamento farmacológico , Camundongos , Camundongos Endogâmicos BALB C , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Origanum/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Plasmodium berghei/efeitos dos fármacos
13.
J Environ Pathol Toxicol Oncol ; 39(2): 125-136, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32749122

RESUMO

Biofilms are a collective of multiple types of bacteria that develop on a variety of surfaces. Biofilm development results in heightened resistance to antibiotics. Quorum sensing plays an important role in biofilm development as it is one of the common communication mechanisms within cells, which balances and stabilizes the environment, when the amount of bacteria increases. Because of the important implications of the roles biofilms play in infectious diseases, it is crucial to investigate natural antibacterial agents that are able to regulate biofilm formation and development. Various studies have suggested that natural plant products have the potential to suppress bacterial growth and exhibit chemopreventive traits in the modulation of biofilm development. In this review, we discuss and collate potential antibiofilm drugs and biological molecules from natural sources, along with their underlying mechanisms of action. In addition, we also discuss the antibiofilm drugs that are currently under clinical trials and highlight their potential future uses.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Farmacorresistência Bacteriana/efeitos dos fármacos , Infecções/tratamento farmacológico , Extratos Vegetais/farmacologia , Antibacterianos/uso terapêutico , Biofilmes/crescimento & desenvolvimento , Interações Hospedeiro-Patógeno , Humanos , Infecções/microbiologia , Extratos Vegetais/uso terapêutico , Percepção de Quorum/efeitos dos fármacos
14.
J Environ Pathol Toxicol Oncol ; 39(2): 179-189, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32749126

RESUMO

Ginkgo biloba extract EGb761 conveys an anticancer effect, but little is known regarding its role in hepatocellular carcinoma (HCC). Our study aims to determine the anticancer effect of EGb761 on HCC cell lines and clarify the underlying molecular mechanism. We explore biological functions of EGb761 in HCC using morphological observation, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and cytotoxic analysis. We investigate the effects of EGb761 on proliferation and apoptosis of HCC cells using plate clone formation, proliferating cell nuclear antigen, and terminal deoxynucleotidyl transferase d-untranslated protein nick end labeling assays. Protein expressions of the NF-κB/p53 signal pathway were detected and identified using immunohistochemistry. The effect of EGb761 on the p53 signaling pathway was further confirmed by adding pifithrin (PFT)-α, an inhibitor of p53. We determine that EGb761 inhibits cell growth, reduces cell viability, and promotes apoptosis of HCC cells. In addition, EGb761 reduces proliferation and increases apoptosis of human hepatocellular carcinomas (HepG2) cells in a dose-dependent manner. We also find that EGb761 exerts an anticancer effect on HepG2 cells by activating p53 and inhibiting nuclear factor (NF)-κB signaling pathways. This study confirms that EGb761 inhibits proliferation and triggers apoptosis of HCC cells through the NF-κB/p53 signaling pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Extratos Vegetais/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Proliferação de Células/efeitos dos fármacos , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos , Proteína Supressora de Tumor p53/metabolismo
15.
Nutrients ; 12(9)2020 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-32854262

RESUMO

The 2019 novel coronavirus, SARS-CoV-2, producing the disease COVID-19 is a pathogenic virus that targets mostly the human respiratory system and also other organs. SARS-CoV-2 is a new strain that has not been previously identified in humans, however there have been previous outbreaks of different versions of the beta coronavirus including severe acute respiratory syndrome (SARS-CoV1) from 2002 to 2003 and the most recent Middle East respiratory syndrome (MERS-CoV) which was first identified in 2012. All of the above have been recognised as major pathogens that are a great threat to public health and global economies. Currently, no specific treatment for SARS-CoV-2 infection has been identified; however, certain drugs have shown apparent efficacy in viral inhibition of the disease. Natural substances such as herbs and mushrooms have previously demonstrated both great antiviral and anti-inflammatory activity. Thus, the possibilities of natural substances as effective treatments against COVID-19 may seem promising. One of the potential candidates against the SARS-CoV-2 virus may be Inonotus obliquus (IO), also known as chaga mushroom. IO commonly grows in Asia, Europe and North America and is widely used as a raw material in various medical conditions. In this review, we have evaluated the most effective herbs and mushrooms, in terms of the antiviral and anti-inflammatory effects which have been assessed in laboratory conditions.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antivirais/uso terapêutico , Produtos Biológicos/uso terapêutico , Infecções por Coronavirus/tratamento farmacológico , Fungos/química , Magnoliopsida/química , Plantas Medicinais/química , Pneumonia Viral/tratamento farmacológico , Agaricales/química , Anti-Inflamatórios/farmacologia , Antivirais/farmacologia , Basidiomycota/química , Betacoronavirus , Produtos Biológicos/farmacologia , Chlorella/química , Infecções por Coronavirus/virologia , Humanos , Pandemias , Fitoterapia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Pneumonia Viral/virologia , Síndrome Respiratória Aguda Grave/virologia
16.
An Acad Bras Cienc ; 92(4): e20190810, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32844991

RESUMO

This study was designed to investigate the effects of emulsion formulations of oleuropein isolated from ethanol extract of olive leaf in streptozotocin-diabetic rats. The rats were treated with the administration of the emulsion containing oleuropein at a low (150 mg/kg b.wt.) and high (225 mg/kg b.wt.) dose for 30 days. At the end of the study, blood samples were drawn from the heart of the rats to determine blood glucose, alanine transaminase, and aspartate transaminase levels. In addition, their liver tissues were dissected to determine the levels of glutathione and thiobarbituric acid-reactive substances, and superoxide dismutase activity. According to the results for both dose treatments, a statistically significant increase in superoxide dismutase activities and glutathione levels of the treated diabetic rats was observed when compared with those of the diabetic control rats. On the other hand, a statistically significant decrease in the levels of thiobarbituric acid-reactive substances, aspartate transaminase and alanine transaminase of the treated diabetic rats was determined. It should be highlighted that the administrations at the high dose were more effective compared to that of the low dose. Furthermore, a substantial decrease in the blood glucose levels of the diabetic rats exposed to the high dose was observed.


Assuntos
Diabetes Mellitus Experimental , Iridoides , Olea , Extratos Vegetais , Animais , Antioxidantes , Glicemia , Catalase , Etanol , Iridoides/farmacologia , Fígado , Extratos Vegetais/farmacologia , Folhas de Planta , Ratos , Ratos Wistar , Superóxido Dismutase
17.
PLoS One ; 15(7): e0236433, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32706801

RESUMO

Coptidis alkaloids are the primary active components of Coptis chinensis Franch. Clinical and pharmacodynamic studies have confirmed that Coptidis alkaloids have multiple therapeutic effects including anti-inflammatory, antioxidant and antitumor effects, and they are usually used to treat various inflammatory disorders and related diseases. Mouse bone marrow cells (BMCs) were isolated from BALB/c mice. Immune-mediated destruction of BMCs was induced by interferon (IFN) -γ. High-performance liquid chromatography-electrospray ionization/ mass spectrometry was used to analyze the ingredients of the aqueous extract from Coptis chinensis Franch. The results confirmed that Coptidis alkaloids were the predominant ingredients in the aqueous extract from Coptis chinensis. The functional mechanism of Coptidis alkaloids in inhibiting immune-mediated destruction of BMCs was studied in vitro. After Coptidis alkaloid treatment, the percentages of apoptotic BMCs and the proliferation and differentiation of helper T (Th) cells and regulatory T (Treg) cells were measured by flow cytometry. The expression and distribution of T-bet in BMCs were observed by immunofluorescence. Western blotting analysis was used to assay the expression of key molecules in the Fas apoptosis and Jak/Stats signaling pathways in BMCs. We identified five alkaloids in the aqueous extract of Coptis chinensis. The apoptotic ratios of BMCs induced by IFN-γ were decreased significantly after Coptidis alkaloid treatment. The levels of key molecules (Fas, Caspase-3, cleaved Caspase-3, Caspase-8 and Caspase-8) in Fas apoptosis signaling pathways also decreased significantly after treatment with low concentrations of Coptidis alkaloids. Coptidis alkaloids were also found to inhibit the proliferation of Th1 and Th17 cells and induce the differentiation of Th2 and Treg cells; further, the distribution of T-bet in BMCs was decreased significantly. In addition, the levels of Stat-1, phospho-Stat-1 and phospho-Stat-3 were also reduced after Coptidis alkaloid treatment. These results indicate that Coptidis alkaloids extracted by water decoction from Coptis chinensis Franch could inhibit the proliferation and differentiation of T lymphocytes, attenuate the apoptosis of BMCs, and suppress the immune-mediated destruction of the BMCs induced by pro-inflammatory cytokines.


Assuntos
Alcaloides/farmacologia , Células da Medula Óssea/efeitos dos fármacos , Coptis/metabolismo , Extratos Vegetais/farmacologia , Linfócitos T Auxiliares-Indutores/efeitos dos fármacos , Linfócitos T Reguladores/efeitos dos fármacos , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Células da Medula Óssea/patologia , Diferenciação Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Citocinas/imunologia , Medicamentos de Ervas Chinesas/farmacologia , Camundongos , Camundongos Endogâmicos BALB C , Linfócitos T Auxiliares-Indutores/patologia , Linfócitos T Reguladores/patologia
18.
Am J Trop Med Hyg ; 103(3): 960-964, 2020 09.
Artigo em Inglês | MEDLINE | ID: mdl-32705976

RESUMO

The world is currently facing a novel COVID-19 pandemic caused by SARS-CoV-2 that, as of July 12, 2020, has caused a reported 12,322,395 cases and 556,335 deaths. To date, only two treatments, remdesivir and dexamethasone, have demonstrated clinical efficacy through randomized controlled trials (RCTs) in seriously ill patients. The search for new or repurposed drugs for treatment of COVID-19 continues. We have witnessed anecdotal use of herbal medicines, including Artemisia spp. extracts, in low-income countries, and exaggerated claims of their efficacies that are not evidence based, with subsequent political controversy. These events highlight the urgent need for further research on herbal compounds to evaluate efficacy through RCTs, and, when efficacious compounds are identified, to establish the active ingredients, develop formulations and dosing, and define pharmacokinetics, toxicology, and safety to enable drug development. Derivatives from the herb Artemisia annua have been used as traditional medicine over centuries for the treatment of fevers, malaria, and respiratory tract infections. We review the bioactive compounds, pharmacological and immunological effects, and traditional uses for Artemisia spp. derivatives, and discuss the challenges and controversies surrounding current efforts and the scientific road map to advance them to prevent or treat COVID-19.


Assuntos
Artemisia , Betacoronavirus , Infecções por Coronavirus/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Pneumonia Viral/tratamento farmacológico , Ensaios Clínicos Controlados Aleatórios como Assunto , Artemisia/química , Humanos , Pandemias , Extratos Vegetais/farmacologia
19.
Arch Microbiol ; 202(9): 2437-2451, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32607726

RESUMO

A total of 15 samples of thalassotherapy products, distributed in Tunisia in their intact and final state of production, was analyzed to determine their microbiological safety status. The result shows the absence of pathogenic bacteria (Staphylococcus aureus, Candida albicans, Salmonella, Pseudomonas aeruginosa and coliforms). The incidence of contamination by Gram-positive Bacilli (mesophelic bacteria, aerobic and anaerobic spore forming bacteria, anaerobic sulphite-reducing bacteria) was found to be higher in products composed by mud and extract of alga. The biochemical and molecular identification of the major contaminant show that Bacilli were the most covered from 75% of the thalassotherapy products. Mineral analysis (organic matter, Fe, Mg, Ca, Na d K, Al, Si and Ti) shows strong composition on Aluminum and Silica. Cytotoxicity study of six thalassotherapy products and three essential oil extracts (Menthol, Clove and Eucalyptus) did not show any cytotoxic effect. Furthermore, antibacterial acitivity of 5 essentila oils, against 30 isolates of the genus Bacillus and 10 reference strains, has been characterized showing an interesting bactericidal potential of the extract of menthol and Eucalyptus.


Assuntos
Climatoterapia/normas , Qualidade de Produtos para o Consumidor , Sedimentos Geológicos/microbiologia , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/isolamento & purificação , Testes de Sensibilidade Microbiana , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Óleos Vegetais/farmacologia , Tunísia
20.
Rev Bras Parasitol Vet ; 29(2): e019819, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32609242

RESUMO

We investigated the in vitro acaricide activity of the methanolic extract (ME) and alkaloid-rich fraction (AF) of Prosopis juliflora on Rhipicephalus microplus and correlated this effect with acetylcholinesterase (AChE) inhibition. The acaricide activity was evaluated using adult and larval immersion tests. Also, we studied the possible interaction mechanism of the major alkaloids present in this fraction via molecular docking at the active site of R. microplus AChE1 (RmAChE1). Higher reproductive inhibitory activity of the AF was recorded, with effective concentration (EC50) four times lower than that of the ME (31.6 versus 121 mg/mL). The AF caused mortality of tick larvae, with lethal concentration 50% (LC50) of 13.8 mg/mL. Both ME and AF were seen to have anticholinesterase activity on AChE of R. microplus larvae, while AF was more active with half-maximal inhibitory concentration (IC50) of 0.041 mg/mL. The LC-MS/MS analyses on the AF led to identification of three alkaloids: prosopine (1), juliprosinine (2) and juliprosopine (3). The molecular docking studies revealed that these alkaloids had interactions at the active site of the RmAChE1, mainly relating to hydrogen bonds and cation-pi interactions. We concluded that the alkaloids of P. juliflora showed acaricide activity on R. microplus and acted through an anticholinesterase mechanism.


Assuntos
Alcaloides , Colinesterases , Extratos Vegetais , Prosopis , Rhipicephalus , Acaricidas/farmacologia , Alcaloides/farmacologia , Animais , Colinesterases/metabolismo , Cromatografia Líquida , Ativação Enzimática/efeitos dos fármacos , Larva , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Prosopis/química , Rhipicephalus/efeitos dos fármacos , Rhipicephalus/enzimologia , Espectrometria de Massas em Tandem
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