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1.
Photochem Photobiol Sci ; 23(5): 853-869, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38613600

RESUMO

Synthetic sunscreen offers protection against excessive exposure to ultraviolet (UV) radiation from the sun, and protects the skin from possible damage. However, they have low efficacy against the formation of reactive oxygen species (ROS), which are highly reactive molecules that can be generated in the skin when it is exposed to UV radiation, and are known to play a role in oxidative stress, which can contribute to skin aging and damage. Thus, there is an ongoing search for sunscreens that do not have these negative effects. One promising source for these is natural products. Therefore, the current patent review summarizes topical formulations made from natural compounds that have antioxidant properties and can be used as photoprotective or anti-aging agents, either using a single natural extract or a combination of extracts. The review reports basic patent information (applicant country, type of applicant, and year of filing) and gives details about the invention, including its chemical composition, and the in vitro and in vivo tests performed. These patents describe natural products that can be used to protect the skin and validate their efficacy, and safety, in addition to standardizing their formulations. The compositions described illustrate the consistent innovation in the use of natural products to protect against UV damage and photoaging disorders, a promising field which is receiving growing global recognition.


Assuntos
Produtos Biológicos , Protetores Solares , Raios Ultravioleta , Protetores Solares/farmacologia , Protetores Solares/química , Humanos , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Raios Ultravioleta/efeitos adversos , Patentes como Assunto , Pele/efeitos dos fármacos , Pele/efeitos da radiação , Envelhecimento da Pele/efeitos dos fármacos , Envelhecimento da Pele/efeitos da radiação , Antioxidantes/farmacologia , Antioxidantes/química , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química
2.
AAPS PharmSciTech ; 25(7): 212, 2024 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-39242428

RESUMO

UV radiation causes long- and short-term skin damage, such as erythema and skin cancer. Therefore, the use of sunscreens is extremely important. However, concerns about UV filter safety have prompted exploration into alternative solutions, with nanotechnology emerging as a promising avenue. This systematic review identified 23 experimental studies utilizing nanocarriers to encapsulate sunscreens with the aim of enhancing their efficacy and safety. Polymeric and lipid nanoparticles are frequently employed to encapsulate both organic and inorganic UV filters along with natural antioxidants. Nanocarriers have demonstrated benefits including reduced active ingredient usage, increased sun protection factor, and mitigated photoinstability. Notably, they also decreased the skin absorption of UV filters. In summary, nanocarriers represent a viable strategy for improving sunscreen formulations, offering enhanced physicochemical properties and bolstered photoprotective effects, thereby addressing concerns regarding UV filter safety and efficacy in cosmetic applications.


Assuntos
Nanopartículas , Nanotecnologia , Protetores Solares , Raios Ultravioleta , Animais , Humanos , Antioxidantes/administração & dosagem , Antioxidantes/química , Antioxidantes/farmacologia , Portadores de Fármacos/química , Lipídeos/química , Nanopartículas/química , Nanotecnologia/métodos , Polímeros/química , Pele/metabolismo , Pele/efeitos dos fármacos , Absorção Cutânea/efeitos dos fármacos , Fator de Proteção Solar , Protetores Solares/química , Protetores Solares/administração & dosagem , Raios Ultravioleta/efeitos adversos
3.
J Microencapsul ; 40(7): 475-490, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37698545

RESUMO

Osteoarthritis is considered a degenerative joint disease that is characterised by inflammation, chronic pain, and functional limitation. The increasing development of nanotechnology in drug delivery systems has provided new ideas and methods for osteoarthritis therapy. This review aimed to evaluate patents that have developed innovations, therapeutic strategies, and alternatives using nanotechnology in osteoarthritis treatment. The results show patents deposited from 2015 to November 2021 in the online databases European Patent Office and World Intellectual Property Organisation. A total of 651 patents were identified for preliminary assessment and 16 were selected for full reading and discussion. The evaluated patents are focused on the intraarticular route, oral route, and topical route for osteoarthritis treatment. The intraarticular route presented a higher patent number, followed by the oral and topical routes, respectively. The development of new technologies allows us to envision a promising and positive future in osteoarthritis treatment.


Assuntos
Sistemas de Liberação de Medicamentos , Osteoartrite , Humanos , Nanotecnologia , Osteoartrite/tratamento farmacológico
4.
Molecules ; 28(11)2023 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-37298941

RESUMO

Pain is one of the most prevalent and difficult to manage symptoms in cancer patients, and conventional drugs present a range of adverse reactions. The development of ß-cyclodextrins (ß-CD) complexes has been used to avoid physicochemical and pharmacological limitations due to the lipophilicity of compounds such as p-Cymene (PC), a monoterpene with antinociceptive effects. Our aim was to obtain, characterize, and measure the effect of the complex of p-cymene and ß-cyclodextrin (PC/ß-CD) in a cancer pain model. Initially, molecular docking was performed to predict the viability of complex formation. Afterward, PC/ß-CD was obtained by slurry complexation, characterized by HPLC and NMR. Finally, PC/ß-CD was tested in a Sarcoma 180 (S180)-induced pain model. Molecular docking indicated that the occurrence of interaction between PC and ß-CD is favorable. PC/ß-CD showed complexation efficiency of 82.61%, and NMR demonstrated PC complexation in the ß-CD cavity. In the S180 cancer pain model, PC/ß-CD significantly reduced the mechanical hyperalgesia, spontaneous nociception, and nociception induced by non-noxious palpation at the doses tested (p < 0.05) when compared to vehicle differently from free PC (p > 0.05). Therefore, the complexation of PC in ß-CD was shown to improve the pharmacological effect of the drug as well as reducing the required dose.


Assuntos
Dor do Câncer , Ciclodextrinas , Neoplasias , beta-Ciclodextrinas , Humanos , Camundongos , Animais , Simulação de Acoplamento Molecular , beta-Ciclodextrinas/química , Dor/tratamento farmacológico , Dor/etiologia , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Analgésicos/química , Solubilidade
5.
Mycopathologia ; 187(5-6): 535-546, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36194378

RESUMO

Candida auris is responsible for hospital outbreaks worldwide. Some C. auris isolates may show concomitant resistance to azoles, echinocandins, and polyenes, thereby possibly leaving clinicians with few therapeutic options. In addition, this multi-drug-resistant yeast is difficult to identify with conventional methods and has the ability to persist on environmental surfaces causing hospital-acquired infections. The development of new treatment options and tools for identification is critical to control, prevent, and establish an early diagnosis of this emerging pathogen. The aim of this study was to perform a critical patent review to explore and identify the latest advances in therapeutic strategies as well as diagnostic methods for C. auris. A total of 19 patents were identified for a preliminary assessment from the Espacenet database. Three patents were excluded as they were out of focus for this review according to their abstract and/or description. The final selection covered 16 patents, which were surveyed by country, year and classified as treatment or diagnostic methods for C. auris. As noted in the patent reading, in recent years, the interest of academic, government and industry sectors have shown an increasing tendency focused on research and development of new therapeutic molecules and diagnostic methods to combat this emerging pathogen.


Assuntos
Candidíase , Farmacorresistência Fúngica Múltipla , Candida , Candidíase/diagnóstico , Candidíase/tratamento farmacológico , Candidíase/epidemiologia , Candida auris , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Testes de Sensibilidade Microbiana
6.
AAPS PharmSciTech ; 23(6): 170, 2022 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-35729366

RESUMO

UV radiation can cause damages, such as erythema, skin photoaging, and carcinogenesis. The adoption of protective measures against sun exposure is essential to prevent these damages, and the interest in using natural substances as an alternative for photoprotection is growing. Thus, hesperetin with antioxidant, anti-inflammatory, and anticancer properties is a promising substance to be used with photochemopreventive action and to protect the skin from damage induced by UV radiation. Therefore, the present study aimed to develop a topical formulation based on AAMVPC gel containing hesperetin and evaluate its photoprotective effect on the skin of rats exposed to UVA-UVB radiation. The animals were submitted to the irradiation protocol UVA-UVB, and at the end, erythema, lipid peroxidation, and activity of the antioxidant enzyme catalase and superoxide dismutase were evaluated. Additionally, it evaluated the activity of myeloperoxidase and histological changes. The formulation presented a rheological and spreadability profile suitable for cutaneous application. In vivo results demonstrated that the topical formulation of AAMVPC gel containing hesperetin at a concentration of 10% protected the skin from damage induced by UVA-UVB radiation, with the absence of erythema, lipid lipoperoxidation, and inflammation (low myeloperoxidase activity), and increased catalase and superoxide dismutase activities. The morphology and architecture of the dermo-epidermal tissue of these animals were like those observed under normal conditions (non-irradiated animals). Thus, the results showed that hesperetin was able to protect the animals' skin against UV radiation-induced skin damage and the protection mechanisms may be related to the antioxidant and anti-inflammatory properties of this natural product.


Assuntos
Peroxidase , Raios Ultravioleta , Animais , Anti-Inflamatórios/metabolismo , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Catalase , Hesperidina , Hidrogéis/metabolismo , Estresse Oxidativo , Peroxidase/metabolismo , Peroxidase/farmacologia , Ratos , Pele/metabolismo , Superóxido Dismutase/metabolismo , Superóxido Dismutase/farmacologia , Raios Ultravioleta/efeitos adversos
7.
Crit Rev Biotechnol ; 41(2): 229-248, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33530749

RESUMO

Fungal biofilms, such as Candida albicans biofilms, are capable of surviving in hostile environments owing to their remarkable ability to adhere to surfaces and their tolerance to chemical interventions. Currently, therapeutic treatment options are few, making these biofilm-based infections problematic particularly due to their great tolerance to conventional antimicrobial drugs, thus causing serious health and economic problems. Therefore, the development of new drugs and antibiofilm specific therapies for the prevention and treatment of antifungal to eradicate biofilms are needed. This study was aimed at carrying out a patent review analysis to identify the innovation trends, and to explore the latest antifungal drugs and the specific therapeutic strategies available for the treatment of fungal biofilms. The present patent review was carried out using the Espacenet database, using the key words "biofilm and antifungal," from 2002 to December 2019. Through this review, it was possible to identify that most of the patent contents refer to new synthetic drugs derived from natural products and associations thereof with existing antifungal drugs. Methods and biomaterials for the treatment and prevention of fungal biofilms, mainly for C. albicans biofilms, which is the most isolated and studied fungal species, were also disclosed. The lack of scientific and technical information on the biofilm eradication subject is remarkable and further confirmed by the small number of patents identified in this survey.


Assuntos
Anti-Infecciosos , Preparações Farmacêuticas , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Biofilmes , Candida albicans
8.
Drug Dev Ind Pharm ; 47(4): 673-684, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33826439

RESUMO

PURPOSE: The last two decades have seen the emergence of several viral outbreaks. Some of them are the severe acute respiratory syndrome (SARS), Middle East respiratory syndrome (MERS), and severe acute respiratory syndrome 2 (SARS-CoV2) - the cause of the coronavirus disease 2019 (COVID-19). Ever, vaccines for emergency use have been authorized for the control and prevention of COVID-19. Currently, there is an urgent need to develop a vaccine for prophylaxis of COVID-19 and for other future epidemics. METHODS: This review describes patented vaccines for SARS and MERS-CoV and vaccines developed and approved for emergency use against the new coronavirus (COVID-19). The European Patent Office and the World Intellectual Property Organization were the patent databases used using specific terms. In addition, another search was carried out in the Clinical Trials in search of ongoing clinical studies focused on the COVID-19 vaccine. RESULTS: The patent search showed that most vaccines are based on viral vector platforms, nucleic acids, or protein subunits. The review also includes an overview of completed and ongoing clinical trials for SARS-CoV-2 in several countries. CONCLUSION: The information provided here lists vaccines for other types of coronavirus that have been used in the development of vaccines for COVID-19.


Assuntos
COVID-19 , Vacinas , Vacinas contra COVID-19 , Humanos , RNA Viral , SARS-CoV-2
9.
AAPS PharmSciTech ; 22(2): 72, 2021 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-33575845

RESUMO

Since January 2020, the World Health Organization announces COVID-19 outbreak a case of public health emergency of international interest, and declaring it a pandemic on March. Due to the high transmission of this disease, rate precautions have been implemented, such as the use of masks by the population, personal protective equipment (PPE), and safety protocols, mainly to health workers. Thus, we performed a patent review to evaluate the current patents related to the protective mask. The review was carried out in the patent database in the period of May 2019 to May 2020. After the process of screening and eligibility, 563 patents were selected for our analysis according to the aim of the study which used masks such as a PPE against dust particles and pathogens, mostly when it is about airborne transmission, such as viruses and bacteria. Here, an overview of the main materials used in the mask manufacturing and their efficiency was described. The results of the review showed that most of the masks used cotton, nylon, silver fiber fabrics, among others as fabrics to develop the masks. It also makes an analysis of masks composed of nanotechnology which provide high filtration efficiency. Moreover, the review also brought possibilities of masking the population, which already have been done in countries such as China and Korea and ways of sterilization for reuse of PPE during COVID-19 outbreak. Thus, this review can further researchers in the developing of masks to decrease the spread of a pandemic disease. Graphical abstract.


Assuntos
COVID-19 , Máscaras , Pandemias , Pacientes , Equipamento de Proteção Individual , Bases de Dados Factuais , Humanos
10.
Rev Panam Salud Publica ; 44: e108, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33042199

RESUMO

OBJECTIVE: To estimate the prevalence of SARS-CoV-2 antibodies in an asymptomatic population in the state of Sergipe, Brazil.
. METHODS: This cross-sectional study with stratified sampling (sex and age) included serological immunofluorescent tests for IgM and IgG on samples from 3 046 asymptomatic individuals. Sample collection was performed in wet-markets of the 10 most populous cities of Sergipe, Brazil. Exclusion criteria included symptomatic individuals and health workers. The presence of comorbidities was registered.
. RESULTS: Of the 3 046 participants, 1 577 (51.8%) were female and 1 469 (48.2%) were male; the mean age was 39.76 (SD 16.83) years old. 2 921 tests were considered valid for IgM and 2 635 for IgG. Of the valid samples, 347 (11.9% [CI 10.7%-13.1%]) tested positive for IgM and 218 (8.3% [CI 7.2%-9.4%]) tested positive for IgG. Women over 40 had the highest prevalence for IgM (group C, p=0.006; group D p=0.04). The capital Aracaju displayed the highest prevalence for both antibodies; 83 (26.3% [CI 21.6%-31.6%]) tested positive for IgM and 35 (14.6% [CI 10.4%-19.7%]) for IgG. The most prevalent comorbidities were hypertension (64/123 individuals) and diabetes (29/123).
. CONCLUSIONS: A high prevalence of SARS-CoV-2 antibodies was found among asymptomatic persons in Sergipe. Women over 40 showed the highest rates. The capital, Aracaju, displayed the highest seroprevalence. Surveys like this one are important to understand how the virus spreads and to help authorities to plan measures to control it. Repeated serologic testing are required to track the progress of the epidemic.


OBJETIVO: estimar la prevalencia de anticuerpos dirigidos contra el SARS-CoV-2 en una población asintomática del estado de Sergipe, Brasil. MÉTODOS: estudio transversal con muestreo estratificado (por sexo y edad) que incluyó pruebas serológicas de inmunofluorescencia para IgM e IgG en muestras de 3 046 individuos asintomáticos. La recolección de muestras se realizó en los mercados húmedos de las 10 ciudades más pobladas de Sergipe, Brasil. Se excluyó a los individuos sintomáticos y a los trabajadores de la salud. Se registró la presencia de comorbilidades. RESULTADOS: De los 3 046 participantes, 1 577 (51,8%) eran mujeres y 1 469 (48,2%) varones; la edad promedio fue de 39,76 (SD 16,83) años. Se consideraron válidas 2 921 pruebas para la IgM y 2 635 para la IgG. De las muestras válidas, 347 (11,9% [CI 10,7%-13,1%]) resultaron positivas para IgM y 218 (8,3% [CI 7,2%-9,4%]) para IgG. Las mujeres mayores de 40 años tuvieron la mayor prevalencia de IgM (grupo C, p=0,006; grupo D, p=0,04). Aracaju, la capital del estado, mostró la mayor prevalencia para ambos anticuerpos; 83 (26,3% [CI 21,6%-31,6%]) resultaron positivas para IgM y 35 (14,6% [CI 10,4%-19,7%]) para IgG. Las comorbilidades más frecuentes fueron la hipertensión (64/123 individuos) y la diabetes (29/123). CONCLUSIONES: Se encontró una alta prevalencia de anticuerpos contra el SARS-CoV-2 en personas asintomáticas en Sergipe. Las mujeres mayores de 40 años mostraron las tasas más altas. La capital, Aracaju, mostró la mayor seroprevalencia. Las encuestas como esta son importantes para comprender cómo se propaga el virus y para ayudar a las autoridades a planificar medidas de control. Se requieren pruebas serológicas repetidas para dar seguimento al progreso de la epidemia.

11.
AAPS PharmSciTech ; 21(5): 184, 2020 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-32632735

RESUMO

Fibromyalgia (FM) is a chronic disease that has as main characteristic generalized musculoskeletal pain, which can cause physical and emotional problems to patients. However, pharmacological therapies show side effects that hamper the adhesion to treatment. Given this, (-)-linalool (LIN), a monoterpene with several therapeutic properties already reported in scientific literature as anti-depressive, antinociceptive, anti-inflammatory, and antihyperalgesic also demonstrated therapeutic potential in the treatment of FM. Nevertheless, physicochemical limitations as high volatilization and poor water-solubility make its use difficult. In this perspective, this present research had performed the incorporation of LIN into polymeric nanocapsules (LIN-NC). Size, morphology, encapsulation efficiency, cytotoxicity, and drug release were performed. The antihyperalgesic effect of LIN-NC was evaluated by a chronic non-inflammatory muscle pain model. The results demonstrated that the polymeric nanocapsules showed particle size of 199.1 ± 0.7 nm with a PDI measurement of 0.13 ± 0.01. The drug content and encapsulation efficiency were 13.78 ± 0.05 mg/mL and 80.98 ± 0.003%, respectively. The formulation did not show cytotoxicity on J774 macrophages. The oral treatment with LIN-NC and free-LIN increased the mechanical withdrawal threshold on all days of treatment in comparison with the control group. In conclusion, LIN-NC is a promising proposal in the development of phytotherapy-based nanoformulations for future clinical applications.


Assuntos
Monoterpenos Acíclicos/administração & dosagem , Anti-Inflamatórios/administração & dosagem , Fibromialgia/tratamento farmacológico , Nanocápsulas , Polímeros/administração & dosagem , Monoterpenos Acíclicos/farmacocinética , Monoterpenos Acíclicos/uso terapêutico , Animais , Anti-Inflamatórios/farmacocinética , Liberação Controlada de Fármacos , Humanos , Tamanho da Partícula , Solubilidade
12.
Z Naturforsch C J Biosci ; 72(3-4): 93-97, 2017 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-28107177

RESUMO

Aristolochia trilobata L. is an aromatic plant, popularly known as "mil-homens", and its essential oil (EO) is generally used to treat colic, diarrhea and dysentery disorders. We evaluated the antinociceptive effect of A. trilobata stem EO and of its major compound, the (R)-(-)-6-methyl-5-hepten-2-yl acetate (sulcatyl acetate: SA), using acetic acid (0.85%)-induced writhing response and formalin-induced (20 µL of 1%) nociceptive behavior in mice. We also evaluated the EO and SA effect on motor coordination, using the rota-rod apparatus. EO (25, 50 and 100 mg/kg) or SA (25 and 50 mg/kg) reduced nociceptive behavior in the writhing test (p<0.001). EO (100 mg/kg) and SA (25 and 50 mg/kg) decreased the nociception on the first phase of the formalin test (p<0.05). On the second phase, EO (25: p<0.01; 50: p<0.05 and 100 mg/kg: p<0.001) and SA (25 and 50 mg/kg; p<0.001) reduced the nociceptive response induced by formalin. EO and SA were not able to cause changes in the motor coordination of animals. Together, our results suggest that EO has an analgesic profile and SA seems to be one of the active compounds in this effect.


Assuntos
Analgésicos/farmacologia , Aristolochia/química , Heptanol/farmacologia , Óleos Voláteis/isolamento & purificação , Caules de Planta/química , Acetatos/antagonistas & inibidores , Acetatos/farmacologia , Analgésicos/isolamento & purificação , Animais , Heptanol/análogos & derivados , Heptanol/isolamento & purificação , Masculino , Camundongos , Óleos Voláteis/química , Medição da Dor , Extratos Vegetais/química , Desempenho Psicomotor/efeitos dos fármacos , Teste de Desempenho do Rota-Rod
13.
AAPS PharmSciTech ; 18(1): 49-57, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27073031

RESUMO

This study evaluated three different methods for the formation of an inclusion complex between alpha- and beta-cyclodextrin (α- and ß-CD) and limonene (LIM) with the goal of improving the physicochemical properties of limonene. The study samples were prepared through physical mixing (PM), paste complexation (PC), and slurry complexation (SC) methods in the molar ratio of 1:1 (cyclodextrin:limonene). The complexes prepared were evaluated with thermogravimetry/derivate thermogravimetry, infrared spectroscopy, X-ray diffraction, complexation efficiency through gas chromatography/mass spectrometry analyses, molecular modeling, and nuclear magnetic resonance. The results showed that the physical mixing procedure did not produce complexation, but the paste and slurry methods produced inclusion complexes, which demonstrated interactions outside of the cavity of the CDs. However, the paste obtained with ß-cyclodextrin did not demonstrate complexation in the gas chromatographic technique because, after extraction, most of the limonene was either surface-adsorbed by ß-cyclodextrin or volatilized during the procedure. We conclude that paste complexation and slurry complexation are effective and economic methods to improve the physicochemical character of limonene and could have important applications in pharmacological activities in terms of an increase in solubility.


Assuntos
Cicloexenos/química , Terpenos/química , alfa-Ciclodextrinas/química , beta-Ciclodextrinas/química , Cromatografia Gasosa/métodos , Limoneno , Espectroscopia de Ressonância Magnética/métodos , Espectrometria de Massas/métodos , Modelos Moleculares , Solubilidade , Espectrofotometria Infravermelho/métodos , Termogravimetria/métodos , Difração de Raios X/métodos
14.
BMC Complement Altern Med ; 14: 514, 2014 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-25539576

RESUMO

BACKGROUND: The present study was carried out to evaluate antioxidant, antinociceptive and anti-inflammatory activities of essential oil from R. maritima (RMO) in experimental protocols. METHODS: The essential oil from the roots and rhizomes of RMO were obtained by hydrodistillation using a Clevenger apparatus, and analyzed by gas chromatography/mass spectrometry (GC/MS). Here, we evaluated free radical scavenging activities and antioxidant potential of RMO using in vitro assays for scavenging activity against hydroxyl radicals, hydrogen peroxide, superoxide radicals, and nitric oxide. The total reactive antioxidant potential (TRAP) and total antioxidant reactivity (TAR) indexes and in vitro lipoperoxidation were also evaluated. The ability of RMO to prevent lipid peroxidation was measured by quantifying thiobarbituric acid-reactive substances (TBARS). NO radical generated at physiological pH was found to be inhibited by RMO, that showed scavenging effect upon SNP-induced NO production at all concentrations. Antinociceptive and anti-inflammatory properties were evaluated by acetic acid writhing reflex, Formalin-induced nociception and Carrageenan-induced edema test. RESULTS: The majors compounds identified was remirol (43.2%), cyperene (13.8%), iso-evodionol (5.8%), cyperotundone (5.7%), caryophyllene oxide (4.9%), and rotundene (4.6%). At the TRAP assay, RMO concentration of 1 mg.mL(-1) showed anti-oxidant effects and at concentration of 1 and 10 ng.mL(-1) RMO showed pro-oxidant effect. RMO at 1 mg.mL(-1) also showed significant anti-oxidant capacity in TAR measurement. Concentrations of RMO from 1 ng.mL(-1) to 100 µg.mL(-1) enhanced the AAPH-induced lipoperoxidation. RMO reduced deoxyribose oxidative damage, induced by the Fenton reaction induction system, at concentrations from 1 ng.mL(-1) to 100 µg.mL(-1). We observed that RMO caused a significant increase in rate of adrenaline auto-oxidation. On the other hand RMO did not present any scavenging effect in H2O2 formation in vitro. The results of this study revealed that RMO has both peripheral and central analgesic properties. The RMO, all doses, orally (p.o.) administered significantly inhibited (p < 0.05, p < 0.01 and p < 0.001) the acetic acid-induced writhings and two phases of formalin-induced nociception in mice. CONCLUSION: The RMO demonstrated antioxidant and analgesic profile which may be related to the composition of the oil.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Cyperaceae/química , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Analgésicos/química , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Antioxidantes/química , Antioxidantes/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Cromatografia Gasosa-Espectrometria de Massas , Masculino , Camundongos , Óleos Voláteis/química , Óleos Voláteis/uso terapêutico , Oxirredução/efeitos dos fármacos , Óleos de Plantas/química , Óleos de Plantas/uso terapêutico , Superóxido Dismutase/metabolismo
15.
Int J Mol Sci ; 16(1): 547-63, 2014 Dec 29.
Artigo em Inglês | MEDLINE | ID: mdl-25551603

RESUMO

O. basilicum leaves produce essential oils (LEO) rich in monoterpenes. The short half-life and water insolubility are limitations for LEO medical uses. ß-Cyclodextrin (ß-CD) has been employed to improve the pharmacological properties of LEO. We assessed the antihyperalgesic profile of LEO, isolated or complexed in ß-CD (LEO/ß-CD), on an animal model for fibromyalgia. Behavioral tests: mice were treated every day with either LEO/ß-CD (25, 50 or 100 mg/kg, p.o.), LEO (25 mg/kg, p.o.), tramadol (TRM 4 mg/kg, i.p.) or vehicle (saline), and 60 min after treatment behavioral parameters were assessed. Therefore, mice were evaluated for mechanical hyperalgesia (von Frey), motor coordination (Rota-rod) and muscle strength (Grip Strength Metter) in a mice fibromyalgia model. After 27 days, we evaluated the central nervous system (CNS) pathways involved in the effect induced by experimental drugs through immunofluorescence protocol to Fos protein. The differential scanning analysis (DSC), thermogravimetry/derivate thermogravimetry (TG/DTG) and infrared absorption spectroscopy (FTIR) curves indicated that the products prepared were able to incorporate the LEO efficiently. Oral treatment with LEO or LEO-ßCD, at all doses tested, produced a significant reduction of mechanical hyperalgesia and we were able to significantly increase Fos protein expression. Together, our results provide evidence that LEO, isolated or complexed with ß-CD, produces analgesic effects on chronic non-inflammatory pain as fibromyalgia.


Assuntos
Analgésicos/uso terapêutico , Fibromialgia/tratamento farmacológico , Monoterpenos/uso terapêutico , Ocimum basilicum/química , Óleos Voláteis/uso terapêutico , Proteínas Proto-Oncogênicas c-fos/genética , beta-Ciclodextrinas/química , Analgésicos/administração & dosagem , Analgésicos/química , Analgésicos/isolamento & purificação , Animais , Sistema Nervoso Central/efeitos dos fármacos , Sistema Nervoso Central/metabolismo , Sistema Nervoso Central/fisiopatologia , Fibromialgia/genética , Fibromialgia/fisiopatologia , Força da Mão , Hiperalgesia/tratamento farmacológico , Hiperalgesia/genética , Hiperalgesia/fisiopatologia , Masculino , Camundongos , Monoterpenos/administração & dosagem , Monoterpenos/química , Monoterpenos/isolamento & purificação , Atividade Motora/efeitos dos fármacos , Óleos Voláteis/administração & dosagem , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Folhas de Planta/química , Regulação para Cima/efeitos dos fármacos
16.
Molecules ; 19(9): 14496-527, 2014 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-25221871

RESUMO

Chronic diseases such as cancer, diabetes, neurodegenerative and cardiovascular diseases are characterized by an enhanced state of oxidative stress, which may result from the overproduction of reactive species and/or a decrease in antioxidant defenses. The search for new chemical entities with antioxidant profile is still thus an emerging field on ongoing interest. Due to the lack of reviews concerning the antioxidant activity of lichen-derived natural compounds, we performed a review of the antioxidant potential and mechanisms of action of natural compounds isolated from lichens. The search terms "lichens", "antioxidants" and "antioxidant response elements" were used to retrieve articles in LILACS, PubMed and Web of Science published until February 2014. From a total of 319 articles surveyed, 32 met the established inclusion and exclusion criteria. It was observed that the most common isolated compound studied was usnic acid, cited in 14 out of the 32 articles. The most often described antioxidant assays for the study of in vitro antioxidant activity were mainly DPPH, LPO and SOD. The most suggested mechanisms of action were scavenging of reactive species, enzymatic activation and inhibition of iNOS. Thus, compounds isolated from lichens are possible candidates for the management of oxidative stress, and may be useful in the treatment of chronic diseases.


Assuntos
Elementos de Resposta Antioxidante , Antioxidantes/química , Líquens/química , Neoplasias/tratamento farmacológico , Antioxidantes/farmacologia , Benzofuranos/metabolismo , Compostos de Bifenilo/administração & dosagem , Compostos de Bifenilo/química , Sequestradores de Radicais Livres/metabolismo , Humanos , Oxirredução , Estresse Oxidativo , Picratos/administração & dosagem , Picratos/química
17.
Recent Pat Anticancer Drug Discov ; 19(2): 137-145, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-36788702

RESUMO

BACKGROUND: Cannabis use for tumor treatment has been explored in several areas, and its potential for tumor remission is currently being studied after the discovery of the endogenous cannabinoid. OBJECTIVE: The study aimed to conduct a critical patent review to identify and explore the latest advances and therapeutic strategies using Cannabis to treat cancer. METHODS: The research was carried out in the free and online database Espacenet, using the descriptors "cancer" and "Cannabis or cannabidiol" in the title or abstract. A total of 95 patents were identified for preliminary evaluation in the database. Six duplicate patents were excluded, 12 referring to traditional Chinese medicine and 36 with a title in disagreement with the scope of this review. In addition the final selection involved 21 patents that were in line with the objective of the study. RESULTS: As observed in the reading of patents, the interest of pharmaceutical industries and researchers and the development of new products to fight cancer have increased in recent years. The main cannabinoids present in the patents are tetrahydrocannabinol, cannabidiol, and hemp. Moreover, the patents were classified and the main applicant countries were the United States followed by Japan, with a higher filing rate in 2019 and, mainly by the industry. CONCLUSION: In conclusion we can say that, the importance of parliamentary approval in the cultivation and investments that, in addition to bringing innovation to the industrial sector, enriches research in the area, contributing to the creation of new medicines.


Assuntos
Canabidiol , Canabinoides , Cannabis , Neoplasias , Humanos , Estados Unidos , Canabidiol/uso terapêutico , Patentes como Assunto , Canabinoides/uso terapêutico , Neoplasias/tratamento farmacológico
18.
Expert Rev Med Devices ; 21(1-2): 91-107, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38189146

RESUMO

INTRODUCTION: Osteoarthritis is a musculoskeletal disease that can lead to the loss and inability of those affected to perform normal daily functions, which leads to a decrease in quality of life. The main symptoms of osteoarthritis are tenderness, joint pain, stiffness, crepitus, limited movement, and local inflammation. AREAS COVERED: The selected patents were deposited from 2010 to April 2022 involving 57 documents that were in line with the study objective in the final selection. The patents were classified in years, country, and applicants. Also, the therapeutic fields that presented the most documents were electrical stimulation, phototherapy, and ultrasound, followed by magnetic, electromagnetic, and thermotherapy. Therefore, the most current therapies used in the documents are already on the market. EXPERT OPINION: Although the OA is cureless, non-surgical treatments are classified as the primary management approach for this disease. The pharmacological and non-pharmacological therapies are employed to reduce its prevalence and ensure the effectiveness of treatments. A strategy for relieving OA symptoms is non-pharmacological treatment, which can be based on exercise and patient education, combined with other alternative therapies. These therapies are used as supplements to the main OA treatments, enhancing the effectiveness of treatment outcomes.


Assuntos
Hipertermia Induzida , Osteoartrite , Humanos , Qualidade de Vida , Osteoartrite/terapia , Inflamação , Exercício Físico
19.
Crit Rev Ther Drug Carrier Syst ; 41(6): 57-88, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38804554

RESUMO

Major depressive disorder is considered one of the most common and prevalent diseases worldwide, affecting children, adults, and the elderly. Currently, several antidepressant drugs are available on the market, but the low adherence of patients due to the slow therapeutic response is a problem to be solved. In this way, cyclodextrins become an alternative to circumvent the limitations and improve the physicochemical and pharmacological properties of this class of drugs. Thus, the objective of this work is to carry out a current review of patents associating antidepressant drugs and cyclodextrins. The patent search was performed in two patent databases, the World Intellectual Property Organization and the European Patent Office using terms in the title and abstract fields and the international patent classification code for antidepressant drugs. In the end, 27 patent documents were selected and divided into three classifications, physical-chemical characterization study, pre-clinical in vivo trials, and clinical trials. The scientific evidence found in the patents considers the use of cyclodextrins as an important alternative to improve the therapeutic and physicochemical properties of antidepressant drugs, among the main improved properties are, solubility, stability, masking taste and odor, bioavailability.


Assuntos
Antidepressivos , Ciclodextrinas , Patentes como Assunto , Antidepressivos/química , Antidepressivos/farmacologia , Antidepressivos/administração & dosagem , Ciclodextrinas/química , Humanos , Animais , Solubilidade , Transtorno Depressivo Maior/tratamento farmacológico , Disponibilidade Biológica , Estabilidade de Medicamentos
20.
Vaccines (Basel) ; 12(8)2024 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-39204002

RESUMO

Tuberculosis (TB) is an ancient global public health problem. Several strategies have been applied to develop new and more effective vaccines against TB, from attenuated or inactivated mycobacteria to recombinant subunit or genetic vaccines, including viral vectors. This review aimed to evaluate patents filed between 2010 and 2023 for TB vaccine candidates. It focuses on viral vector-based strategies. A search was carried out in Espacenet, using the descriptors "mycobacterium and tuberculosis" and the classification A61K39. Of the 411 patents preliminarily identified, the majority were related to subunit vaccines, with 10 patents based on viral vector platforms selected in this study. Most of the identified patents belong to the United States or China, with a concentration of patent filings between 2013 and 2023. Adenoviruses were the most explored viral vectors, and the most common immunodominant Mycobacterium tuberculosis (Mtb) antigens were present in all the selected patents. The majority of patents were tested in mouse models by intranasal or subcutaneous route of immunization. In the coming years, an increased use of this platform for prophylactic and/or therapeutic approaches for TB and other diseases is expected. Along with this, expanding knowledge about the safety of this technology is essential to advance its use.

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