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1.
Molecules ; 26(12)2021 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-34204457

RESUMO

Mitragyna speciosa Korth (kratom) is known for its psychoactive and analgesic properties. Mitragynine is the primary constituent present in kratom leaves. This study highlights the utilisation of the green accelerated solvent extraction technique to produce a better, non-toxic and antinociceptive active botanical extract of kratom. ASE M. speciosa extract had a dry yield (0.53-2.91 g) and showed a constant mitragynine content (6.53-7.19%) when extracted with organic solvents of different polarities. It only requires a shorter extraction time (5 min) and a reduced amount of solvents (less than 100 mL). A substantial amount of total phenolic (407.83 ± 2.50 GAE mg/g and flavonoids (194.00 ± 5.00 QE mg/g) were found in ASE kratom ethanol extract. The MTT test indicated that the ASE kratom ethanolic leaf extract is non-cytotoxic towards HEK-293 and HeLa Chang liver cells. In mice, ASE kratom ethanolic extract (200 mg/kg) demonstrated a better antinociceptive effect compared to methanol and ethyl acetate leaf extracts. The presence of bioactive indole alkaloids and flavonols such as mitragynine, paynantheine, quercetin, and rutin in ASE kratom ethanolic leaf extract was detected using UHPLC-ESI-QTOF-MS/MS analysis supports its antinociceptive properties. ASE ethanolic leaf extract offers a better, safe, and cost-effective choice of test botanical extract for further preclinical studies.


Assuntos
Mitragyna/química , Extratos Vegetais/química , Alcaloides de Triptamina e Secologanina/isolamento & purificação , Animais , Células HEK293 , Células HeLa , Humanos , Masculino , Camundongos , Mitragyna/metabolismo , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Alcaloides de Triptamina e Secologanina/química , Solventes/química
2.
Molecules ; 26(12)2021 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-34208560

RESUMO

Pectis elongata is found in the northern and northeastern regions of Brazil. It is considered a lemongrass due to its citric scent. The remarkable citral content and the wide antimicrobial properties and bioactive features of this terpene make this essential oil (EO) eligible for several industrial purposes, especially in cosmetics and phytotherapics. However, to address the problems regarding citral solubility, nano-emulsification is considered a promising strategy thanks to its improved dispersability. Thus, in this paper we propose a low-energy approach for the development of citral-based nano-emulsions prepared with P. elongata EO. The plant was hydrodistillated to produce the EO, which was characterized with a gas chromatograph coupled to mass spectrometry. The nano-emulsion prepared by a non-heated water titrating (low-energy) method was composed of 5% (w/w) EO, 5% (w/w) non-ionic surfactants and 90% (w/w) deionized water and was analyzed by dynamic light scattering. Levels of citral of around 90% (neral:geranial-4:5) were detected in the EO and no major alteration in the ratio of citral was observed after the nano-emulsification. The nano-emulsion was stable until the 14th day (size around 115 nm and polydispersity index around 0.2) and no major alteration in droplet size was observed within 30 days of storage. Understanding the droplet size distribution as a function of time and correlating it to concepts of compositional ripening, as opposing forces to the conventional Ostwald ripening destabilization mechanism, may open interesting approaches for further industrial application of novel, low-energy, ecofriendly approaches to high citral essential oil-based nano-emulsions based on lemongrass plants.


Assuntos
Monoterpenos Acíclicos/isolamento & purificação , Emulsões/química , Óleos Voláteis/isolamento & purificação , Monoterpenos Acíclicos/química , Brasil , Cymbopogon/química , Cromatografia Gasosa-Espectrometria de Massas , Monoterpenos/química , Óleos Voláteis/química , Extratos Vegetais/isolamento & purificação , Tensoativos/química , Água/química
3.
Molecules ; 26(12)2021 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-34208750

RESUMO

Entamoeba histolytica (protozoan; family Endomoebidae) is the cause of amoebiasis, a disease related to high morbidity and mortality. Nowadays, this illness is considered a significant public health issue in developing countries. In addition, parasite resistance to conventional medicinal treatment has increased in recent years. Traditional medicine around the world represents a valuable source of alternative treatment for many parasite diseases. In a previous paper, we communicated about the antiprotozoal activity in vitro of the methanolic (MeOH) extract of Ruta chalepensis (Rutaceae) against E. histolytica. The plant is extensively employed in Mexican traditional medicine. The following workup of the MeOH extract of R. chalepensis afforded the furocoumarins rutamarin (1) and chalepin (2), which showed high antiprotozoal activity on Entamoeba histolytica trophozoites employing in vitro tests (IC50 values of 6.52 and 28.95 µg/mL, respectively). Therefore, we offer a full scientific report about the bioguided isolation and the amebicide activity of chalepin and rutamarin.


Assuntos
Furocumarinas/isolamento & purificação , Ruta/metabolismo , Amebicidas/isolamento & purificação , Amebicidas/farmacologia , Antiprotozoários/farmacologia , Benzopiranos/metabolismo , Entamoeba histolytica/efeitos dos fármacos , Entamoeba histolytica/patogenicidade , Furocumarinas/farmacologia , Concentração Inibidora 50 , Medicina Tradicional , México , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
4.
J Mol Model ; 27(8): 221, 2021 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-34236507

RESUMO

Natural products have served human life as medications for centuries. During the outbreak of COVID-19, a number of naturally derived compounds and extracts have been tested or used as potential remedies against COVID-19. Tetradenia riparia extract is one of the plant extracts that have been deployed and claimed to manage and control COVID-19 by some communities in Tanzania and other African countries. The active compounds isolated from T. riparia are known to possess various biological properties including antimalarial and antiviral. However, the underlying mechanism of the active compounds against SARS-CoV-2 remains unknown. Results in the present work have been interpreted from the view point of computational methods including molecular dynamics, free energy methods, and metadynamics to establish the related mechanism of action. Among the constituents of T. riparia studied, luteolin inhibited viral cell entry and was thermodynamically stable. The title compound exhibit residence time and unbinding kinetics of 68.86 ms and 0.014 /ms, respectively. The findings suggest that luteolin could be potent blocker of SARS-CoV-2 cell entry. The study shades lights towards identification of bioactive constituents from T. riparia against COVID-19, and thus bioassay can be carried out to further validate such observations.


Assuntos
Antivirais/farmacologia , COVID-19/tratamento farmacológico , Luteolina/farmacologia , Simulação de Dinâmica Molecular , Extratos Vegetais/farmacologia , SARS-CoV-2/efeitos dos fármacos , Internalização do Vírus/efeitos dos fármacos , Enzima de Conversão de Angiotensina 2/metabolismo , Antivirais/isolamento & purificação , Antivirais/metabolismo , Sítios de Ligação , COVID-19/virologia , Interações Hospedeiro-Patógeno , Humanos , Cinética , Lamiaceae/química , Luteolina/isolamento & purificação , Luteolina/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/metabolismo , Ligação Proteica , Conformação Proteica , Receptores Virais/metabolismo , SARS-CoV-2/patogenicidade , Glicoproteína da Espícula de Coronavírus/metabolismo
5.
Pharm Biol ; 59(1): 696-703, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: covidwho-1263613

RESUMO

CONTEXT: COVID-19 is a novel coronavirus that causes a severe infection in the respiratory system. Nigella sativa L. (Ranunculaceae) is an annual flowering plant used traditionally as a natural food supplement and multipurpose medicinal agent. OBJECTIVE: The possible beneficial effects of N. sativa, and its constituent, thymoquinone (TQ) on COVID-19 were reviewed. METHODS: The key words including, COVID-19, N. sativa, thymoquinone, antiviral effects, anti-inflammatory and immunomodulatory effects in different databases such as Web of Science (ISI), PubMed, Scopus, and Google Scholar were searched from 1990 up to February 2021. RESULTS: The current literature review showed that N. sativa and TQ reduced the level of pro-inflammatory mediators including, IL-2, IL-4, IL-6, and IL-12, while enhancing IFN-γ. Nigella sativa and TQ increased the serum levels of IgG1 and IgG2a, and improved pulmonary function tests in restrictive respiratory disorders. DISCUSSION AND CONCLUSIONS: These preliminary data of molecular docking, animal, and clinical studies propose N. sativa and TQ might have beneficial effects on the treatment or control of COVID-19 due to antiviral, anti-inflammatory and immunomodulatory properties as well as bronchodilatory effects. The efficacy of N. sativa and TQ on infected patients with COVID-19 in randomize clinical trials will be suggested.


Assuntos
Anti-Inflamatórios/farmacologia , Antivirais/farmacologia , Benzoquinonas/farmacologia , COVID-19/tratamento farmacológico , Nigella sativa , Extratos Vegetais/farmacologia , SARS-CoV-2/efeitos dos fármacos , Animais , Anti-Inflamatórios/isolamento & purificação , Antivirais/isolamento & purificação , Benzoquinonas/isolamento & purificação , COVID-19/imunologia , COVID-19/metabolismo , COVID-19/virologia , Citocinas/metabolismo , Humanos , Sistema Imunitário/efeitos dos fármacos , Sistema Imunitário/imunologia , Sistema Imunitário/metabolismo , Sistema Imunitário/virologia , Mediadores da Inflamação/metabolismo , Pulmão/efeitos dos fármacos , Pulmão/imunologia , Pulmão/metabolismo , Pulmão/virologia , Nigella sativa/química , Extratos Vegetais/isolamento & purificação , SARS-CoV-2/imunologia , SARS-CoV-2/patogenicidade
6.
J Food Sci ; 86(7): 2978-2989, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34155646

RESUMO

Passion fruit rind is a waste product from the beverage industry that is rich in anthocyanins that can be potentially applied as a natural colorant. However, the inherent instability of anthocyanins causes rapid discoloration. In this study, the cyanidin-3-glucoside (C-3-G) in passion fruit rind was extracted using 50% ethanol and converted into nonbleachable pigments by reaction with Oolong tea extracts and acetaldehyde. Reactions over 70 days formed high concentrations of stable nonbleachable pigments (3.07-6.68 absorbance unit [A.U.], in total) such as pyranoanthocyanins, as well as oligomeric and polymeric pigments with ethyl-linked bridges. In C-3-G and acetaldehyde reaction, positive relations were found among acetaldehyde concentration, color density, and nonbleachable pigment concentrations. As for reactions with C-3-G and Oolong tea extract combined with acetaldehyde, greater color density and greater concentrations of nonbleachable pigments (10.80-12.34, 4.25-4.40 A.U., respectively) were formed compared with acetaldehyde alone. In addition, the antioxidant capabilities of the extracts were enhanced after reaction with Oolong tea extracts. The results of this study show a useful method to enhance the stability of anthocyanins from passion fruit rind and also provide greater economic value to this waste product. PRACTICAL APPLICATION: Ripened passion fruits contain a high concentration of anthocyanins in their rind. These anthocyanins can be optimally extracted by ultrasonic assisted solvent extraction to provide stable pigments by inducing acetaldehyde (a volatile compound often found in foods and beverages) into the anthocyanins. These stable pigments have a greater reddish hue in solution than the anthocyanin extracted from the rind and are more stable over a greater pH range. In addition, these stable pigments can be potentially used as colorant throughout the food and cosmetic industry to provide high economical values.


Assuntos
Antocianinas/química , Corantes/química , Passiflora/química , Extratos Vegetais/química , Acetaldeído , Antocianinas/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Corantes/isolamento & purificação , Frutas/química , Extratos Vegetais/isolamento & purificação
7.
Molecules ; 26(10)2021 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-34070150

RESUMO

Hepatic fibrosis would develop into cirrhosis or cancer without treating. Hence, it is necessary to study the mechanism and prevention methods for hepatic fibrosis. Gynostemma pentaphyllum is a traditional medicinal material with a high medicinal and health value. In this study, nineteen compounds obtained from G. pentaphyllum were qualitative and quantitative by HPLC-FT-ICR MS and HPLC-UV, respectively. Among them, the total content of 19 gypenosides accurately quantified reaches 72.21 mg/g and their anti-proliferation against t-HSC/Cl-6 cells indicated compound 19 performed better activity (IC50: 28.1 ± 2.0 µM) than the other compounds. Further network pharmacology study demonstrated that compound 19 mainly plays an anti-fibrosis role by regulating the EGFR signaling pathway, and the PI3K-Akt signaling pathway. Overall, the verification result indicated that compound 19 appeared to be nontoxic to LO2, was able to modulate the PI3K/Akt signal, led to subG1 cells cycle arrest and the activation of mitochondrial-mediated apoptosis of t-HSC/Cl-6 cells for anti-hepatic fibrosis.


Assuntos
Gynostemma/química , Cirrose Hepática/tratamento farmacológico , Cirrose Hepática/prevenção & controle , Terapia de Alvo Molecular , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Ontologia Genética , Humanos , Cirrose Hepática/patologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Mapas de Interação de Proteínas/efeitos dos fármacos
8.
Molecules ; 26(9)2021 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-34066895

RESUMO

Water lily (Nuphar) bioactive extracts have been widely used in traditional medicine owing to their multiple applications against human ailments. Phyto-active Nuphar extracts and their purified and synthetic derivatives have attracted the attention of ethnobotanists and biochemists. Here, we report that 6,6'-dihydroxythiobinupharidine (DTBN), purified from extracts of Nuphar lutea (L.) Sm. leaves, is an effective inhibitor of the kinase activity of members of the protein kinase C (PKC) family using in vitro and in silico approaches. We demonstrate that members of the conventional subfamily of PKCs, PKCα and PKCγ, were more sensitive to DTBN inhibition as compared to novel or atypical PKCs. Molecular docking analysis demonstrated the interaction of DTBN, with the kinase domain of PKCs depicting the best affinity towards conventional PKCs, in accordance with our in vitro kinase activity data. The current study reveals novel targets for DTBN activity, functioning as an inhibitor for PKCs kinase activity. Thus, this and other data indicate that DTBN modulates key cellular signal transduction pathways relevant to disease biology, including cancer.


Assuntos
Alcaloides/farmacologia , Isoenzimas/antagonistas & inibidores , Nuphar/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Proteína Quinase C/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Cristalografia por Raios X , Células HEK293 , Humanos , Concentração Inibidora 50 , Isoenzimas/química , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ligação Proteica , Proteína Quinase C/química , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos
9.
Turkiye Parazitol Derg ; 45(2): 101-107, 2021 06 07.
Artigo em Inglês | MEDLINE | ID: mdl-34103285

RESUMO

Objective: Natural plant products are considered as a source of novel and effective compounds for the treatment of leishmaniasis. In this study, the in vitro activities of essential oils obtained from Origanum dubium (OD), Origanum majorana (OM), Salvia fruticosa (SF) and Laurus nobilis (LN) plants in Northern Cyprus were investigated against Leishmania tropica. Methods: Leishmania tropica strain (MHOM/TR/2012/CBCL-LT) was obtained. RPMI-1640 was added to 96-well plates in 100 µL aliquots, 100 µg/mL essential oil was added to the first well of each row and serial 2-fold dilutions were performed. A promastigote suspension was pipetted into all wells, and the plates were incubated. The promastigotes were enumerated using a haemocytometer. Results: OD essential oil was effective at killing all promastigotes at a minimum inhibitor height (MIC)=0.2 µg/mL and had high activity at the lowest concentrations. Both SF and LN oils had MIC=1.56 µg/mL and LD50=0.78 µg/mL. SF was observed to impair promastigote morphology at the lowest concentrations, while LN did not exert any effect at concentrations <0.2 µg/mL. OM essential oil was found to have a MIC=3.13 µg/mL and a LD50=1.56 µg/mL. Conclusion: All tested essential oils inhibited promastigotes of Leishmania tropica. OD essential oil demonstrated the highest anti-leishmanial activity. Amaç: Bitkilerden elde edilen dogal ürünlerin leishmaniasis tedavisi için yeni ve etkili bilesiklerin üretilmesine öncülük edecegi düsünülmektedir. Çalismamizda, Kuzey Kibris'ta yetisen Origanum dubium (OD), Origanum majorana (OM), Salvia fruticosa (SF) ve Laurus nobilis (LN) bitkilerinden elde edilen uçucu yaglarin Leishmania tropica'ya karsi in vitro etkinlikleri arastirilmistir. Yöntemler: Çalismamizda, Leishmania tropica susu (MHOM/TR/2012/CBCL-LT) kullanildi. Düz tabanli 96'lik plaklarda, tüm kuyucuklara 100 µL RPMI-1640 ve ilk kuyucuklara 100 µg/mL uçucu yaglar eklenerek, seri dilüsyonlari yapildi. Ardindan tüm kuyucuklara Leishmania tropica promastigot süspansiyonundan pipetlendi ve inkübe edildi. Hemositometre yöntemiyle promastigotlarin sayisi incelendi. Bulgular: OD yaginin minimum inhibitör konsantrasyonu (MIK)=0,2 µg/mL'de tüm promastigotlari öldürürken, en düsük konsantrasyonlarda bile etkili oldugu görülmüstür. SF ve LN uçucu yaglarinin ikisinde de MIK=1,56 µg/mL, LD50=0,78 µg/mL olarak saptanmistir. SF'nin en düsük konsantrasyonlarinin bile promastigot morfolojisini bozdugu görülürken, Laurus nobilis'in ise 0,2 µg/mL'den sonraki konsantrasyonlarda etkisini kaybettigi belirlenmistir. OM uçucu yaginin MIK=3,13 µg/mL, LD50=1,56 µg/mL oldugu görülmüstür. Sonuç: Kullanilan tüm uçucu yaglarin Leishmania tropica promastigotlarini inhibe ettigi görülürken, en yüksek anti-leishmanial etkinlik Origanum dubium uçucu yaginda bulunmustur.


Assuntos
Antiprotozoários/farmacologia , Leishmania tropica/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Vegetais/farmacologia , Antiprotozoários/isolamento & purificação , Chipre , Laurus/química , Leishmaniose/tratamento farmacológico , Leishmaniose/parasitologia , Dose Letal Mediana , Óleos Voláteis/isolamento & purificação , Origanum/química , Testes de Sensibilidade Parasitária , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Óleos Vegetais/isolamento & purificação , Salvia/química
10.
Pharm Biol ; 59(1): 696-703, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34110959

RESUMO

CONTEXT: COVID-19 is a novel coronavirus that causes a severe infection in the respiratory system. Nigella sativa L. (Ranunculaceae) is an annual flowering plant used traditionally as a natural food supplement and multipurpose medicinal agent. OBJECTIVE: The possible beneficial effects of N. sativa, and its constituent, thymoquinone (TQ) on COVID-19 were reviewed. METHODS: The key words including, COVID-19, N. sativa, thymoquinone, antiviral effects, anti-inflammatory and immunomodulatory effects in different databases such as Web of Science (ISI), PubMed, Scopus, and Google Scholar were searched from 1990 up to February 2021. RESULTS: The current literature review showed that N. sativa and TQ reduced the level of pro-inflammatory mediators including, IL-2, IL-4, IL-6, and IL-12, while enhancing IFN-γ. Nigella sativa and TQ increased the serum levels of IgG1 and IgG2a, and improved pulmonary function tests in restrictive respiratory disorders. DISCUSSION AND CONCLUSIONS: These preliminary data of molecular docking, animal, and clinical studies propose N. sativa and TQ might have beneficial effects on the treatment or control of COVID-19 due to antiviral, anti-inflammatory and immunomodulatory properties as well as bronchodilatory effects. The efficacy of N. sativa and TQ on infected patients with COVID-19 in randomize clinical trials will be suggested.


Assuntos
Anti-Inflamatórios/farmacologia , Antivirais/farmacologia , Benzoquinonas/farmacologia , COVID-19/tratamento farmacológico , Nigella sativa , Extratos Vegetais/farmacologia , SARS-CoV-2/efeitos dos fármacos , Animais , Anti-Inflamatórios/isolamento & purificação , Antivirais/isolamento & purificação , Benzoquinonas/isolamento & purificação , COVID-19/imunologia , COVID-19/metabolismo , COVID-19/virologia , Citocinas/metabolismo , Humanos , Sistema Imunitário/efeitos dos fármacos , Sistema Imunitário/imunologia , Sistema Imunitário/metabolismo , Sistema Imunitário/virologia , Mediadores da Inflamação/metabolismo , Pulmão/efeitos dos fármacos , Pulmão/imunologia , Pulmão/metabolismo , Pulmão/virologia , Nigella sativa/química , Extratos Vegetais/isolamento & purificação , SARS-CoV-2/imunologia , SARS-CoV-2/patogenicidade
11.
Toxins (Basel) ; 13(3)2021 03 22.
Artigo em Inglês | MEDLINE | ID: mdl-33809838

RESUMO

The evolutionary arms race between plants and herbivores has led, over millions of years, to the production of many substances that prevent plants from being over-eaten by plant-feeding animals [...].


Assuntos
Extratos Vegetais/farmacologia , Plantas Tóxicas/metabolismo , Toxinas Biológicas/farmacologia , Animais , Humanos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Plantas Tóxicas/toxicidade , Toxinas Biológicas/isolamento & purificação , Toxinas Biológicas/toxicidade
12.
Respir Res ; 22(1): 99, 2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: covidwho-1169963

RESUMO

BACKGROUND: COVID-19 pneumonia has been associated with severe acute hypoxia, sepsis-like states, thrombosis and chronic sequelae including persisting hypoxia and fibrosis. The molecular hypoxia response pathway has been associated with such pathologies and our recent observations on anti-hypoxic and anti-inflammatory effects of whole aqueous extract of Adhatoda Vasica (AV) prompted us to explore its effects on relevant preclinical mouse models. METHODS: In this study, we tested the effect of whole aqueous extract of AV, in murine models of bleomycin induced pulmonary fibrosis, Cecum Ligation and Puncture (CLP) induced sepsis, and siRNA induced hypoxia-thrombosis phenotype. The effect on lung of AV treated naïve mice was also studied at transcriptome level. We also determined if the extract may have any effect on SARS-CoV2 replication. RESULTS: Oral administration AV extract attenuates increased airway inflammation, levels of transforming growth factor-ß1 (TGF-ß1), IL-6, HIF-1α and improves the overall survival rates of mice in the models of pulmonary fibrosis and sepsis and rescues the siRNA induced inflammation and associated blood coagulation phenotypes in mice. We observed downregulation of hypoxia, inflammation, TGF-ß1, and angiogenesis genes and upregulation of adaptive immunity-related genes in the lung transcriptome. AV treatment also reduced the viral load in Vero cells infected with SARS-CoV2. CONCLUSION: Our results provide a scientific rationale for this ayurvedic herbal medicine in ameliorating the hypoxia-hyperinflammation features and highlights the repurposing potential of AV in COVID-19-like conditions.


Assuntos
Anti-Inflamatórios/farmacologia , COVID-19/tratamento farmacológico , Reposicionamento de Medicamentos , Hipóxia/tratamento farmacológico , Justicia, Planta , Pulmão/efeitos dos fármacos , Extratos Vegetais/farmacologia , Pneumonia/prevenção & controle , Fibrose Pulmonar/tratamento farmacológico , Sepse/tratamento farmacológico , Animais , Anti-Inflamatórios/isolamento & purificação , Bleomicina , COVID-19/metabolismo , COVID-19/virologia , Ceco/microbiologia , Ceco/cirurgia , Citocinas/genética , Citocinas/metabolismo , Modelos Animais de Doenças , Hipóxia/genética , Hipóxia/metabolismo , Subunidade alfa do Fator 1 Induzível por Hipóxia/genética , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Prolina Dioxigenases do Fator Induzível por Hipóxia/genética , Prolina Dioxigenases do Fator Induzível por Hipóxia/metabolismo , Mediadores da Inflamação/metabolismo , Justicia, Planta/química , Ligadura , Pulmão/metabolismo , Pulmão/microbiologia , Pulmão/patologia , Masculino , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Extratos Vegetais/isolamento & purificação , Pneumonia/genética , Pneumonia/metabolismo , Pneumonia/microbiologia , Fibrose Pulmonar/induzido quimicamente , Fibrose Pulmonar/genética , Fibrose Pulmonar/metabolismo , Interferência de RNA , RNA Interferente Pequeno/genética , RNA Interferente Pequeno/metabolismo , Sepse/genética , Sepse/metabolismo , Sepse/microbiologia , Transcriptoma
13.
Respir Res ; 22(1): 99, 2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-33823870

RESUMO

BACKGROUND: COVID-19 pneumonia has been associated with severe acute hypoxia, sepsis-like states, thrombosis and chronic sequelae including persisting hypoxia and fibrosis. The molecular hypoxia response pathway has been associated with such pathologies and our recent observations on anti-hypoxic and anti-inflammatory effects of whole aqueous extract of Adhatoda Vasica (AV) prompted us to explore its effects on relevant preclinical mouse models. METHODS: In this study, we tested the effect of whole aqueous extract of AV, in murine models of bleomycin induced pulmonary fibrosis, Cecum Ligation and Puncture (CLP) induced sepsis, and siRNA induced hypoxia-thrombosis phenotype. The effect on lung of AV treated naïve mice was also studied at transcriptome level. We also determined if the extract may have any effect on SARS-CoV2 replication. RESULTS: Oral administration AV extract attenuates increased airway inflammation, levels of transforming growth factor-ß1 (TGF-ß1), IL-6, HIF-1α and improves the overall survival rates of mice in the models of pulmonary fibrosis and sepsis and rescues the siRNA induced inflammation and associated blood coagulation phenotypes in mice. We observed downregulation of hypoxia, inflammation, TGF-ß1, and angiogenesis genes and upregulation of adaptive immunity-related genes in the lung transcriptome. AV treatment also reduced the viral load in Vero cells infected with SARS-CoV2. CONCLUSION: Our results provide a scientific rationale for this ayurvedic herbal medicine in ameliorating the hypoxia-hyperinflammation features and highlights the repurposing potential of AV in COVID-19-like conditions.


Assuntos
Anti-Inflamatórios/farmacologia , COVID-19/tratamento farmacológico , Reposicionamento de Medicamentos , Hipóxia/tratamento farmacológico , Justicia, Planta , Pulmão/efeitos dos fármacos , Extratos Vegetais/farmacologia , Pneumonia/prevenção & controle , Fibrose Pulmonar/tratamento farmacológico , Sepse/tratamento farmacológico , Animais , Anti-Inflamatórios/isolamento & purificação , Bleomicina , COVID-19/metabolismo , COVID-19/virologia , Ceco/microbiologia , Ceco/cirurgia , Citocinas/genética , Citocinas/metabolismo , Modelos Animais de Doenças , Hipóxia/genética , Hipóxia/metabolismo , Subunidade alfa do Fator 1 Induzível por Hipóxia/genética , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Prolina Dioxigenases do Fator Induzível por Hipóxia/genética , Prolina Dioxigenases do Fator Induzível por Hipóxia/metabolismo , Mediadores da Inflamação/metabolismo , Justicia, Planta/química , Ligadura , Pulmão/metabolismo , Pulmão/microbiologia , Pulmão/patologia , Masculino , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Extratos Vegetais/isolamento & purificação , Pneumonia/genética , Pneumonia/metabolismo , Pneumonia/microbiologia , Fibrose Pulmonar/induzido quimicamente , Fibrose Pulmonar/genética , Fibrose Pulmonar/metabolismo , Interferência de RNA , RNA Interferente Pequeno/genética , RNA Interferente Pequeno/metabolismo , Sepse/genética , Sepse/metabolismo , Sepse/microbiologia , Transcriptoma
14.
Mar Drugs ; 19(4)2021 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-33920324

RESUMO

Menopause, caused by decreases in estrogen production, results in symptoms such as facial flushing, vaginal atrophy, and osteoporosis. Although hormone replacement therapy is utilized to treat menopausal symptoms, it is associated with a risk of breast cancer development. We aimed to evaluate the estrogenic activities of Spartina anglica (SA) and its compounds and identify potential candidates for the treatment of estrogen reduction without the risk of breast cancer. We evaluated the estrogenic and anti-proliferative effects of extracts of SA and its compounds in MCF-7 breast cancer cells. We performed an uterotrophic assay using an immature female rat model. Among extracts of SA, belowground part (SA-bg-E50) had potent estrogenic activity. In the immature female rat model, the administration of SA-bg-E50 increased uterine weight compared with that in the normal group. Among the compounds isolated from SA, 1,3-di-O-trans-feruloyl-(-)-quinic acid (1) had significant estrogenic activity and induced phosphorylation at serine residues of estrogen receptor (ER)α. All extracts and compounds from SA did not increase MCF-7 cell proliferation. Compound 1 is expected to act as an ERα ligand and have estrogenic effects, without side effects, such as breast cancer development.


Assuntos
Fitoestrógenos/farmacologia , Extratos Vegetais/farmacologia , Poaceae/metabolismo , Útero/efeitos dos fármacos , Animais , Neoplasias da Mama/patologia , Proliferação de Células/efeitos dos fármacos , Receptor alfa de Estrogênio/agonistas , Receptor alfa de Estrogênio/metabolismo , Feminino , Humanos , Ligantes , Células MCF-7 , Estrutura Molecular , Tamanho do Órgão , Fitoestrógenos/isolamento & purificação , Fitoestrógenos/toxicidade , Componentes Aéreos da Planta/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Raízes de Plantas/metabolismo , Poaceae/crescimento & desenvolvimento , Ratos Sprague-Dawley , Relação Estrutura-Atividade , Útero/crescimento & desenvolvimento , Útero/metabolismo
15.
Mar Drugs ; 19(5)2021 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-33925208

RESUMO

Walleye dermal sarcoma virus (WDSV) is a type of retrovirus, which affects most of the adult walleye fishes during the spawning time. The virus causes multiple epithelial tumors on the fish's skin and fins that are liable for more than 50% of the mortality rate of fish around the world. Till now, no effective antiviral drug or vaccine candidates have been developed that can block the progression of the disease caused by the pathogen. It was found that the 582-amino-acid (aa) residues long internal structural gag polyprotein of the virus plays an important role in virus budding and virion maturation outside of the cell. Inhibition of the protein can block the budding and virion maturation process and can be developed as an antiviral drug candidate against the virus. Therefore, the study aimed to identify potential natural antiviral drug candidates from the tropical mangrove marine plant Avicennia alba, which will be able to block the budding and virion maturation process by inhibiting the activity of the gag protein of the virus. Initially, a homology modeling approach was applied to identify the 3D structure, followed by refinement and validation of the protein. The refined protein structures were then utilized for molecular docking simulation. Eleven phytochemical compounds have been isolated from the marine plant and docked against the virus gag polyprotein. Three compounds, namely Friedlein (CID244297), Phytosterols (CID12303662), and 1-Triacontanol (CID68972) have been selected based on their docking score -8.5 kcal/mol, -8.0 kcal/mol and -7.9 kcal/mol, respectively, and were evaluated through ADME (Absorption, Distribution, Metabolism and Excretion), and toxicity properties. Finally, molecular dynamics (MD) simulation was applied to confirm the binding stability of the protein-ligands complex structure. The ADME and toxicity analysis reveal the efficacy and non-toxic properties of the compounds, where MD simulation confirmed the binding stability of the selected three compounds with the targeted protein. This computational study revealed the virtuous value of the selected three compounds against the targeted gag polyprotein and will be effective and promising antiviral candidates against the pathogen in a significant and worthwhile manner. Although in vitro and in vivo study is required for further evaluation of the compounds against the targeted protein.


Assuntos
Antivirais/farmacologia , Avicennia/química , Epsilonretrovirus/efeitos dos fármacos , Doenças dos Peixes/prevenção & controle , Extratos Vegetais/farmacologia , Infecções por Retroviridae/veterinária , Infecções Tumorais por Vírus/veterinária , Animais , Antivirais/isolamento & purificação , Epsilonretrovirus/metabolismo , Epsilonretrovirus/patogenicidade , Doenças dos Peixes/virologia , Produtos do Gene gag/antagonistas & inibidores , Produtos do Gene gag/metabolismo , Ligantes , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Extratos Vegetais/isolamento & purificação , Conformação Proteica , Infecções por Retroviridae/prevenção & controle , Infecções por Retroviridae/virologia , Relação Estrutura-Atividade , Infecções Tumorais por Vírus/prevenção & controle , Infecções Tumorais por Vírus/virologia , Liberação de Vírus/efeitos dos fármacos
16.
Molecules ; 26(5)2021 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-33806579

RESUMO

This paper aimed to investigate the potential antifungal influences of new alkaloids from Delphinium peregrinum L. var. eriocarpum Boiss. New Diterpenoid alkaloids Delcarpum (1), Hydrodavisine (4) and known alkaloids Peregrine (2), Delphitisine (3) were isolated by different chromatographic methods from the aerial parts of D. Peregrinum eriocarpum Boiss, which grows in Syria. The structures of alkaloids were proposed based on 1D NMR spectroscopy 1H-NMR, 13C-NMR, DEPT-135, DEPT-90, 2D NMR spectroscopy DQF-COSY, HMQC, EI-Ms mass spectrum, and IR spectroscopic measurements. The antifungal activity of the isolated alkaloids was evaluated against different dermatophyte fungal isolates compared with fluconazole. In the case of Peregrine (2) the minimum inhibitory concentrations(MICs) recorded 128-256, 32-64, and 32 for Epidermophyton floccosum, Microsporum canis, and Trichophyton rubrum, respectively, compared to 32-64, 16, and 32 µg/mL in the case of fluconazole, respectively. The MICs recorded on application of the four alkaloids mixture were 64, 32, and 16 in the case of E. floccosum, M. canis, and T. rubrum, respectively, which were significantly lower than that measured for each of the individual alkaloid and were compatible for fluconazole. In conclusion, MICs of the tested alkaloids showed a variable potential effect on the investigated fungal isolates. Peregrine (2) was the most effective alkaloid, however, the application of the mixture of alkaloids induced significant synergistic activity that was more pronounced than the application of individual ones.


Assuntos
Alcaloides/farmacologia , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Delphinium/química , Diterpenos/farmacologia , Epidermophyton/efeitos dos fármacos , Extratos Vegetais/farmacologia , Alcaloides/isolamento & purificação , Antifúngicos/isolamento & purificação , Cromatografia , Diterpenos/isolamento & purificação , Estrutura Molecular , Extratos Vegetais/isolamento & purificação
17.
Molecules ; 26(9)2021 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-33925545

RESUMO

The aim of this study was to valorize Thymus serpyllum herbal dust, a particular fraction distinguished as an industrial waste from filter-tea production. Pressurized liquid extraction (PLE) was used with the aim of overcoming certain obstacles of conventional extraction techniques in terms of shortening extraction time, reducing solvent consumption and energy costs, using "green" solvents and obtaining high yield and quality products. In order to optimize PLE of T. serpyllum herbal dust, the preliminary screening of the independent variables in order to define the most influential parameters and their domain was done first. After the screening, the optimization study using the face-centered central composite experimental design (CCD) with response surface methodology (RSM) was implemented. Additionally, taking into account the high awareness of the positive influence of antioxidants on the human health and associating it with high content of polyphenolic compounds in various members of Lamiaceae family, PLE has proven to be a great approach for antioxidants recovery from T. serpyllum herbal dust.


Assuntos
Antioxidantes/isolamento & purificação , Fenóis/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Thymus (Planta)/química , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Humanos , Fenóis/química , Extratos Vegetais/química , Solventes/química
18.
Nutrients ; 13(3)2021 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-33809720

RESUMO

The prevalence of acute respiratory infections and their impact on quality of life underlies the need for efficacious solutions that are safe, sustainable and economically viable. Polysaccharides in several (traditional) plant extracts have been shown to be immunostimulatory, and some studies suggest beneficial effects against respiratory infections. The aim of this study was to (i) identify the active polysaccharide constituents from affordable and renewable crops (bell pepper and carrot) using activity-guided fractionation, (ii) evaluate in vitro effects on innate immune responses (phagocytosis and cytokine secretion), microbiota modulation and production of short chain fatty acids, followed by (iii) the evaluation of effects of a bell pepper extract enriched for the active component in a human proof of concept study. We identified rhamnogalacturonan-I (RG-I) as the nutricophore responsible for the immunostimulatory activity with substantial structural and functional equivalence between bell pepper (bp) and carrot (c). The in vitro studies showed that bpRG-I and cRG-I comprise similar immune- and microbiota modulatory potential and the human study demonstrated that bpRG-I was well tolerated and enhanced innate immune responsiveness in vivo. This is an important step towards testing the efficacy of RG-I from bpRG-I or cRG-I in an infection trial in humans.


Assuntos
Capsicum/química , Daucus carota/química , Fatores Imunológicos/farmacologia , Pectinas/farmacologia , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Adulto , Idoso , Citocinas/metabolismo , Método Duplo-Cego , Feminino , Microbioma Gastrointestinal/efeitos dos fármacos , Humanos , Fatores Imunológicos/isolamento & purificação , Células Matadoras Naturais/efeitos dos fármacos , Células Matadoras Naturais/fisiologia , Masculino , Pessoa de Meia-Idade , Pectinas/isolamento & purificação , Fagocitose/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Estudo de Prova de Conceito , Adulto Jovem
19.
Molecules ; 26(9)2021 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-33926133

RESUMO

Combretum quadrangulare Kurz is widely used in folk medicine in Eastern Asia and is associated with various ethnopharmacological properties including hepatoprotective, antipyretic, analgesic, antidysenteric, and anthelmintic activities. Previous phytochemical investigations reported the presence of numerous triterpenes (mostly cycloartanes, ursanes, lupanes, and oleananes) along with dozens of flavonoids. However, the extracts of C. quadrangulare and isolated flavonoids have not been evaluated for their alpha-glucosidase inhibition. In the frame of our efforts dedicated to the chemical investigation of Vietnamese medicinal plants and their biological activities, a phytochemical study of the MeOH extract of the leaves of C. quadrangulare using bioactive guided isolation was undertaken. In this paper, the isolation and structure elucidation of twelve known compounds, 5-hydroxy-3,7,4'-trimethoxyflavone (1), ayanin (2), kumatakenin (3), rhamnocitrin (4), ombuin (5), myricetin-3,7,3',5'-tetramethyl ether (6), gardenin D (7), luteolin (12), apigenin (13), mearnsetin (14), isoorientin (15), and vitexin (16) were reported. Bromination was applied to compounds 2 and 3 to provide four new synthetic analogues 8-11. All isolated and synthesized compounds were evaluated for alpha-glucosidase inhibition and antibacterial activity. Compounds 4 and 5 showed moderate antibacterial activity against methicillin-resistant Staphylococcus aureus while others were inactive. All compounds failed to reveal any activity toward extended spectrum beta-lactamase-producing Escherichia coli. Compounds 2, 4, 6-9, and 11-14 showed good alpha-glucosidase inhibition with IC50 values in the range of 30.5-282.0 µM. The kinetic of enzyme inhibition showed that 8 and 11 were noncompetitive type inhibition against alpha-glucosidase. In silico molecular docking model indicated that compounds 8 and 11 were potential inhibitors against enzyme α-glucosidase.


Assuntos
Combretum/química , Flavonas/química , Flavonas/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Relação Dose-Resposta a Droga , Flavonas/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Ligação de Hidrogênio , Ligantes , Modelos Moleculares , Conformação Molecular , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade
20.
Mar Drugs ; 19(3)2021 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-33808933

RESUMO

In this work, a non-toxic chitosan-based carrier was constructed via genipin activation and applied for the immobilization of tannase. The immobilization carriers and immobilized tannase were characterized using Fourier transform infrared spectroscopy and thermogravimetric analysis. Activation conditions (genipin concentration, activation temperature, activation pH and activation time) and immobilizations conditions (enzyme amount, immobilization time, immobilization temperature, immobilization pH, and shaking speed) were optimized. The activity and activity recovery rate of the immobilized tannase prepared using optimal activation and immobilization conditions reached 29.2 U/g and 53.6%, respectively. The immobilized tannase exhibited better environmental adaptability and stability. The immobilized tannase retained 20.1% of the initial activity after 12 cycles and retained 81.12% of residual activity after 30 days storage. The catechins composition analysis of tea extract indicated that the concentration of non-ester-type catechins, EGC and EC, were increased by 1758% and 807% after enzymatic treatment. Biological activity studies of tea extract revealed that tea extract treated with the immobilized tannase possessed higher antioxidant activity, higher inhibitory effect on α-amylase, and lower inhibitory effect on α-glucosidase. Our results demonstrate that chitosan activated with genipin could be an effective non-toxic carrier for tannase immobilization and enhancing biological activities of tea extract.


Assuntos
Antioxidantes/farmacologia , Camellia sinensis , Hidrolases de Éster Carboxílico/metabolismo , Quitosana/química , Portadores de Fármacos , Inibidores de Glicosídeo Hidrolases/farmacologia , Iridoides/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , Antioxidantes/isolamento & purificação , Antioxidantes/metabolismo , Camellia sinensis/metabolismo , Hidrolases de Éster Carboxílico/química , Composição de Medicamentos , Estabilidade Enzimática , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/metabolismo , Temperatura , Fatores de Tempo , alfa-Amilases/metabolismo
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