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1.
Pharmaceutics ; 14(5)2022 Apr 21.
Article in English | MEDLINE | ID: mdl-35631497

ABSTRACT

P2X7R is a purinergic receptor with broad expression throughout the body, especially in immune system cells. P2X7R activation causes inflammatory mediators to release, including interleukin-1ß (IL-1ß), the processing and release of which are critically dependent on this ion channel activation. P2X7R's therapeutic potential augments the discovery of new antagonistic compounds. Thus, we investigated whether the Eugenia sulcata essential oil could block P2X7R activity. The essential oil (ESO) dose-dependently inhibited ATP-promoted PI uptake and IL-1ß release with an IC50 of 113.3 ± 3.7 ng/mL and 274 ± 91 ng/mL, respectively, and the essential oil nanoemulsion (ESON) improved the ESO inhibitory effect with an IC50 of 81.4 ± 7.2 ng/mL and 62 ± 2 ng/mL, respectively. ESO and ESON reversed the carrageenan-activated peritonitis in mice, and ESON exhibited an efficacy higher than ESO. The majority substance from essential oil, ß-caryophyllene, impaired the ATP-evoked PI uptake and IL-1ß release with an IC50 value of 26 ± 0.007 ng/mL and 97 ± 0.012 ng/mL, respectively. Additionally, ß-caryophyllene reduced carrageenan-induced peritonitis, and the molecular modeling and computational simulation predicted the intermolecular interactions in the P2X7R situs. In silico, results indicated ß-caryophyllene as a potent allosteric P2X7R antagonist, although this substance may present toxic effects for humans. These data confirm the nanoemulsion of essential oil from E. sulcata as a promisor biotechnology strategy for impaired P2X7R functions and the inflammatory response.

2.
An. acad. bras. ciênc ; 89(2): 1111-1120, Apr.-June 2017. tab, graf
Article in English | LILACS | ID: biblio-886682

ABSTRACT

ABSTRACT Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.


Subject(s)
Humans , Phenols/analysis , Flavonoids/analysis , Myrtaceae/chemistry , Cell Proliferation/drug effects , Antioxidants/pharmacology , Picrates , Biphenyl Compounds , Brazil , Cell Line, Tumor , Oxygen Radical Absorbance Capacity , Indicators and Reagents , Acetates/pharmacology , Acetates/chemistry
3.
An Acad Bras Cienc ; 89(2): 1111-1120, 2017.
Article in English | MEDLINE | ID: mdl-28489194

ABSTRACT

Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.


Subject(s)
Antioxidants/pharmacology , Cell Proliferation/drug effects , Flavonoids/analysis , Myrtaceae/chemistry , Phenols/analysis , Plant Extracts/pharmacology , Tannins/analysis , Acetates/chemistry , Acetates/pharmacology , Biphenyl Compounds , Brazil , Cell Line, Tumor , Humans , Indicators and Reagents , Oxygen Radical Absorbance Capacity , Picrates , Plant Leaves/chemistry , Reference Values , Reproducibility of Results , Spectrophotometry
4.
Rev. bras. farmacogn ; 24(3): 316-321, May-Jun/2014. tab
Article in English | LILACS | ID: lil-719457

ABSTRACT

Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is popularly known as "camboim-amarelo" and was collected at Restinga de Jurubatiba (RJ, Brazil). Leaves from this species were submitted to hydrodistillation to extract its essential oil. Monoterpenes were the main compounds found (53.9%), and 1,8-cineole was the major constituent (38.4%). Studies were carried out to evaluate the effects of this essential oil on the development of two species of agricultural pests (Oncopeltus fasciatus and Dysdercus peruvianus). The essential oil was considered effective against D. peruvianus and O. fasciatus, causing mortality in both insects. The LD50 values (µg/insect) observed were 112.44 µg/insect (O. fasciatus) and 309.64 µg/insect (D. peruvianus) after one day of treatment, and 72.18 µg/insect (O. fasciatus) and 94.42 µg/insect (D. peruvianus) after 22 days of treatment. The present study reports for the first time the bioinsecticidal activity of essential oil of Myrciaria floribunda leaves, and provides important data regarding the use of essential oils in complementary programs for pest control.

5.
Cardiovasc Ultrasound ; 8: 6, 2010 Mar 16.
Article in English | MEDLINE | ID: mdl-20233431

ABSTRACT

Thromboembolism is a major cause of death in cancer patients. The association between paraneoplastic hypercoagulability of oncological patients and long-term central venous catheters (CVC) may result in CVC associated thrombosis. Patent Foramen Ovale (PFO), especially when associated with atrial septal aneurysm (ASA) is a risk factor for paradoxical embolism. We report a case of paradoxical embolism with stroke in an oncological patient with a huge CVC thrombus playing "ping-pong" with an hypermobile ASA with a PFO. We review the management of hypercoagulability in oncologic patients and discuss the potential role of routine transthoracic echocardiography before the implantation of long term central venous catheters to identify predisposing conditions to paradoxical embolism and select patients for anticoagulant therapy.


Subject(s)
Echocardiography, Transesophageal , Embolism, Paradoxical/diagnostic imaging , Embolism, Paradoxical/etiology , Upper Extremity Deep Vein Thrombosis/complications , Upper Extremity Deep Vein Thrombosis/diagnostic imaging , Adenocarcinoma/complications , Adenocarcinoma/drug therapy , Antineoplastic Agents/administration & dosage , Blood Coagulation Disorders/etiology , Colonic Neoplasms/complications , Colonic Neoplasms/drug therapy , Fatal Outcome , Female , Heart Atria , Humans , Middle Aged , Vena Cava, Superior
6.
J Am Coll Cardiol ; 54(25): 2430-4, 2009 Dec 15.
Article in English | MEDLINE | ID: mdl-20082934

ABSTRACT

OBJECTIVES: This retrospective multicenter registry evaluated the safety and feasibility of left ventricular (LV) support with the Impella 2.5 (Abiomed Europe GmbH, Aachen, Germany) during high-risk percutaneous coronary intervention (PCI). BACKGROUND: Patients with complex or high-risk coronary lesions, such as last remaining vessel or left main lesions, are increasingly being treated with PCI. Because periprocedural hemodynamic compromise and complications might occur rapidly, many of these high-risk procedures are being performed with mechanical cardiac assistance, particularly in patients with poor LV function. The Impella 2.5, a percutaneous implantable LV assist device, might be a superior alternative to the traditionally used intra-aortic balloon pump. METHODS: The Europella registry included 144 consecutive patients who underwent a high-risk PCI. Safety and feasibility end points included incidence of 30-day adverse events and successful device function. RESULTS: Patients were older (62% >70 years of age), 54% had an LV ejection fraction < or = 30%, and the prevalence of comorbid conditions was high. Mean European System for Cardiac Operative Risk Evaluation score was 8.2 (SD 3.4), and 43% of the patients were refused for coronary artery bypass grafting. A PCI was considered high-risk due to left main disease, last remaining vessel disease, multivessel coronary artery disease, and low LV function in 53%, 17%, 81%, and 35% of the cases, respectively. Mortality at 30 days was 5.5%. Rates of myocardial infarction, stroke, bleeding requiring transfusion/surgery, and vascular complications at 30 days were 0%, 0.7%, 6.2%, and 4.0%, respectively. CONCLUSIONS: This large multicenter registry supports the safety, feasibility, and potential usefulness of hemodynamic support with Impella 2.5 in high-risk PCI.


Subject(s)
Angioplasty, Balloon, Coronary , Coronary Artery Disease/therapy , Heart-Assist Devices , Ventricular Dysfunction, Left/therapy , Aged , Blood Transfusion/statistics & numerical data , Comorbidity , Coronary Artery Disease/mortality , Europe/epidemiology , Feasibility Studies , Female , Hemorrhage/epidemiology , Humans , Male , Myocardial Infarction/epidemiology , Registries , Retrospective Studies , Risk Assessment , Severity of Illness Index , Stroke/epidemiology , Stroke Volume , Ventricular Dysfunction, Left/mortality
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