RESUMO
Abstract Due to the severe side effects revealed by most of the currently used antidiabetic medicines, search for finding new and safe drugs to manage diabetes is continued. Naphthoquinones possessing strong antioxidant properties have been employed as candidates for diabetes therapy. Present study is aimed at finding the antioxidant and hypoglycaemic potential of some novel derivatives of 2-phenylamino-1,4-naphthoquinones (PAN) including chloro, nitro, methyl and bromo (5a-d) derivatives synthesized by single pot experiment. Product crystals were purified by TLC and characterized by FT-IR. The antioxidant potential of the compounds was assayed through DPPH radical scavenging and reducing power activities noted as UV-vis. absorbance. The DPPH assay has showed the powerful antioxidant activity of nitro and bromo derivatives, while the nitro derivative showed the significant reduction potential towards FRAP assay. Hypoglycaemic potential of the compounds was studied in rat animal model. All synthesized compounds revealed better hypoglycaemic activity; however, the chloro-derivative exhibited the more potent hypoglycaemic activity showing about 43% reduction in the mean blood glucose levels of the treated animals. As the bioreduction of naphthoquinones may be influenced by changing its redox properties, it has been noticed that the e-donating resonance effect (+R) of chloro group has shown the significant effects on biological activity through stabalization of its imine form which limits the potential of generation of free radicals during bioreduction of quinones and thus has been proposed as the reason of its hypoglycaemic activity. Future studies employing the properties of e-donating groups of PAN may optimize the drug-receptor interaction for better drug designing and drug development strategies against diabetes and also for the clinical trials.
Resumo Em razão dos graves efeitos colaterais causados pela maioria dos medicamentos antidiabéticos atualmente utilizados, continua a busca por novos medicamentos seguros para o controle do diabetes. As naftoquinonas, que possuem fortes propriedades antioxidantes, têm sido empregadas como candidatas à terapia do diabetes. O presente estudo visa encontrar o potencial antioxidante e hipoglicemiante de alguns novos derivados de 2-fenilamino-1,4-naftoquinonas (PAN), incluindo derivados de cloro, nitro, metil e bromo (5a-d) sintetizados por experimento em pote único. Os cristais do produto foram purificados por TLC e caracterizados por FT-IR. O potencial antioxidante dos compostos foi testado por meio de atividades de sequestro de radicais DPPH e redução de energia observada como absorção no UV-vis. O ensaio DPPH mostrou a poderosa atividade antioxidante dos derivados nitro e bromo, enquanto o derivado nitro mostrou o potencial de redução significativo para o ensaio FRAP. O potencial hipoglicêmico dos compostos foi estudado em modelo animal de rato. Todos os compostos sintetizados revelaram melhor atividade hipoglicemiante; no entanto, o derivado cloro apresentou atividade hipoglicêmica mais potente, com redução de 43% nos níveis médios de glicose no sangue dos animais tratados. Como a biorredução de naftoquinonas pode ser influenciada pela alteração de suas propriedades redox, notou-se que o efeito da doação eletrônica por ressonância (+R) do grupo cloro tem sido significativo na atividade biológica por meio da estabilização de sua forma imina, que limita o potencial de geração de radicais livres durante a biorredução de quinonas, e, portanto, tem sido proposto como a razão de sua atividade hipoglicemiante. Estudos futuros empregando as propriedades de grupos de doação eletrônica de PAN podem otimizar a interação droga-receptor para melhor planejamento de medicamentos e estratégias de desenvolvimento de medicamentos contra o diabetes e também para os ensaios clínicos.
RESUMO
Due to the severe side effects revealed by most of the currently used antidiabetic medicines, search for finding new and safe drugs to manage diabetes is continued. Naphthoquinones possessing strong antioxidant properties have been employed as candidates for diabetes therapy. Present study is aimed at finding the antioxidant and hypoglycaemic potential of some novel derivatives of 2-phenylamino-1,4-naphthoquinones (PAN) including chloro, nitro, methyl and bromo (5a-d) derivatives synthesized by single pot experiment. Product crystals were purified by TLC and characterized by FT-IR. The antioxidant potential of the compounds was assayed through DPPH radical scavenging and reducing power activities noted as UV-vis. absorbance. The DPPH assay has showed the powerful antioxidant activity of nitro and bromo derivatives, while the nitro derivative showed the significant reduction potential towards FRAP assay. Hypoglycaemic potential of the compounds was studied in rat animal model. All synthesized compounds revealed better hypoglycaemic activity; however, the chloro-derivative exhibited the more potent hypoglycaemic activity showing about 43% reduction in the mean blood glucose levels of the treated animals. As the bioreduction of naphthoquinones may be influenced by changing its redox properties, it has been noticed that the e-donating resonance effect (+R) of 'chloro' group has shown the significant effects on biological activity through stabalization of its imine form which limits the potential of generation of free radicals during bioreduction of quinones and thus has been proposed as the reason of its hypoglycaemic activity. Future studies employing the properties of e-donating groups of PAN may optimize the drug-receptor interaction for better drug designing and drug development strategies against diabetes and also for the clinical trials.
Em razão dos graves efeitos colaterais causados pela maioria dos medicamentos antidiabéticos atualmente utilizados, continua a busca por novos medicamentos seguros para o controle do diabetes. As naftoquinonas, que possuem fortes propriedades antioxidantes, têm sido empregadas como candidatas à terapia do diabetes. O presente estudo visa encontrar o potencial antioxidante e hipoglicemiante de alguns novos derivados de 2-fenilamino-1,4-naftoquinonas (PAN), incluindo derivados de cloro, nitro, metil e bromo (5a-d) sintetizados por experimento em pote único. Os cristais do produto foram purificados por TLC e caracterizados por FT-IR. O potencial antioxidante dos compostos foi testado por meio de atividades de sequestro de radicais DPPH e redução de energia observada como absorção no UV-vis. O ensaio DPPH mostrou a poderosa atividade antioxidante dos derivados nitro e bromo, enquanto o derivado nitro mostrou o potencial de redução significativo para o ensaio FRAP. O potencial hipoglicêmico dos compostos foi estudado em modelo animal de rato. Todos os compostos sintetizados revelaram melhor atividade hipoglicemiante; no entanto, o derivado cloro apresentou atividade hipoglicêmica mais potente, com redução de 43% nos níveis médios de glicose no sangue dos animais tratados. Como a biorredução de naftoquinonas pode ser influenciada pela alteração de suas propriedades redox, notou-se que o efeito da doação eletrônica por ressonância (+R) do grupo "cloro" tem sido significativo na atividade biológica por meio da estabilização de sua forma imina, que limita o potencial de geração de radicais livres durante a biorredução de quinonas, e, portanto, tem sido proposto como a razão de sua atividade hipoglicemiante. Estudos futuros empregando as propriedades de grupos de doação eletrônica de PAN podem otimizar a interação droga-receptor para melhor planejamento de medicamentos e estratégias de desenvolvimento de medicamentos contra o diabetes e também para os ensaios clínicos.
Assuntos
Ratos, Modelos Animais, Diabetes Mellitus, Desenvolvimento de Medicamentos, Hipoglicemiantes, AntioxidantesRESUMO
Due to the severe side effects revealed by most of the currently used antidiabetic medicines, search for finding new and safe drugs to manage diabetes is continued. Naphthoquinones possessing strong antioxidant properties have been employed as candidates for diabetes therapy. Present study is aimed at finding the antioxidant and hypoglycaemic potential of some novel derivatives of 2-phenylamino-1,4-naphthoquinones (PAN) including chloro, nitro, methyl and bromo (5a-d) derivatives synthesized by single pot experiment. Product crystals were purified by TLC and characterized by FT-IR. The antioxidant potential of the compounds was assayed through DPPH radical scavenging and reducing power activities noted as UV-vis. absorbance. The DPPH assay has showed the powerful antioxidant activity of nitro and bromo derivatives, while the nitro derivative showed the significant reduction potential towards FRAP assay. Hypoglycaemic potential of the compounds was studied in rat animal model. All synthesized compounds revealed better hypoglycaemic activity; however, the chloro-derivative exhibited the more potent hypoglycaemic activity showing about 43% reduction in the mean blood glucose levels of the treated animals. As the bioreduction of naphthoquinones may be influenced by changing its redox properties, it has been noticed that the e-donating resonance effect (+R) of 'chloro' group has shown the significant effects on biological activity through stabalization of its imine form which limits the potential of generation of free radicals during bioreduction of quinones and thus has been proposed as the reason of its hypoglycaemic activity. Future studies employing the properties of e-donating groups of PAN may optimize the drug-receptor interaction for better drug designing and drug development strategies against diabetes and also for the clinical trials.
Assuntos
Hipoglicemiantes, Naftoquinonas, Animais, Antioxidantes/química, Antioxidantes/farmacologia, Hipoglicemiantes/farmacologia, Naftoquinonas/farmacologia, Oxirredução, Ratos, Espectroscopia de Infravermelho com Transformada de FourierRESUMO
BACKGROUND: To evaluate the efficacy of probiotics in the treatment of gingivitis. METHODS: MEDLINE, EMBASE and CENTRAL were searched up to May 2019. Randomized controlled clinical trials (RCTs) and/or controlled clinical trials were considered. Studies consisting of ≥10 patients per group clinically diagnosed with gingivitis were selected that compared the efficacy of probiotics in any form with placebo. The primary outcome measure was bleeding on probing (BOP) and gingival index (GI), while the secondary outcome measure was plaque index (PI). Forest plots were created reporting weighted mean difference (WMD) of outcomes with 95% confidence intervals (CI). RESULTS: A total of 10 double-blind placebo-parallel RCTs were included. All studies showed that probiotic administration was effective in the treatment of gingivitis at follow-up. The mean percentage of BOP ranged from 11.87% to 21.7% in the probiotics group and from 15% to 33% in the placebo groups at follow-up, respectively. Considering the effects of Lactobacillus reuteri, the overall mean difference for GI (WMD = -0.48, 95% CI = -1.69 to 0.72, P = 0.42) and PI (WMD = 0.18, 95% CI = -0.23 to 0.61, P = 0.37) did not show any statistical significance between probiotic and placebo groups. CONCLUSIONS: The outcomes of this review show weak evidence to support the use of probiotics in reducing inflammatory periodontal parameters in gingivitis. Significant heterogeneity and limited available data may reduce the impact of these conclusions.
Assuntos
Gengivite, Probióticos/uso terapêutico, Índice de Placa Dentária, Humanos, Índice Periodontal, Resultado do TratamentoRESUMO
OBJECTIVE: The aim of this study was to investigate EDC-assisted collagen crosslinking effect with different concentrations of tiopronin-protected gold (TPAu) nanoparticles on demineralized dentine. METHODS: TPAu nanoparticles were fabricated from 0.31-g tetrachloroauric acid and 0.38-g of N-(2-mercaptopropionyl) glycine (2.4-mmol). Then co-dissolved using 35-mL of 6:1 methanol/acetic acid and mixed using NaBH4. EDC (0.3-M) was conjugated to TPAu nanoparticles at TPAU/EDC-0.25:1, and TPAU/EDC-0.5:1 treatment formulations ratios. Dentin specimens treated with 0.3-M EDC solution alone or left untreated were used as control. Nanoparticles formulations were characterized in term of particles morphology and size, Zeta potential, thermogravimetric analysis and small-angle X-ray scattering. Dentin substrates were characterized in term of TEM investigation, dentin proteases characterization, hydroxyproline liberation, elastic modulus measurement, Raman analysis and confocal microscopy viewing. RESULTS: TEM evaluation of tiopronin protected gold nanoparticles dispersion revealed nano-clusters formations in both groups. However, based on our TEM measurements, the particle-size was ranging from Ë20 to 50 nm with spherical core-shape which were almost similar for both TPAu/EDC ratios (0.5:1 and 0.25:1). Zeta potential measurements indicate negative nanoparticles surface charge. SAXS profiles for both formulations, suggest a typical profile for uni-lamellar nanoparticles. Superior dentin collagen cross-linking effect was found with the TPAu/EDC nanoparticles formulations compared to the control and EDC treated groups. SIGNIFICANCE: Cross-linking of dentin collagen using TPAu coupled with EDC through TPAu/EDC nanoparticles formulations is of potential significance in improving the biodegradation resistance, proteases inhibition, mechanical and structural stability of demineralized dentin substrates. In addition, the cross-linking effect is dependent on TPAu/EDC ratio, whereas higher cross-linking effect was found at TPAu/EDC ratio of 0.5:1.
Assuntos
Nanopartículas Metálicas, Tiopronina, Colágeno, Reagentes de Ligações Cruzadas, Dentina, Ouro, Espalhamento a Baixo Ângulo, Difração de Raios XRESUMO
This study aimed to evaluate the efficacy of metformin as an adjunct to scaling and root planing (SRP) in the treatment of chronic periodontitis. Electronic searches were conducted in databases (MEDLINE, EMBASE, Cochrane Central Register of Controlled Trials and Cochrane Oral Health Group Trials Register databases) up to August 2017. Randomized clinical trials with data in comparison between adjunctive locally delivered metformin use to SRP and placebo in each group and a follow-up period of at least 6 months, were included. Primary outcomes included clinical attachment level, while secondary outcomes were bone defect (BD) fill and reduction in probing depth. The weighted mean differences (WMD) of outcomes and 95% confidence intervals (CI) for each variable were calculated using the random effects model. Five clinical studies were included in the qualitative synthesis and 3 studies were included for meta-analysis. All the included studies showed significant BD fill, probing depth reduction and clinical attachment level gain with adjunctive locally delivered metformin compared to SRP alone. Considering the effects of adjunctive metformin as compared to SRP, a high degree of heterogeneity for BD fill (Q value = 7.03, P = .02, I2 = 71.55%) was noticed among both the groups. Meta-analysis showed a statistically significant clinical attachment level gain (WMD = -2.83, 95% CI = -3.32 to -2.34, P < .001), BD fill (WMD = -2.96, 95% CI = -3.99 to -1.93, P < .001) and probing depth reduction (WMD = -3.11, 95% CI = -3.63 to -2.59, P < .001) for SRP + metformin treatment vs SRP. Adjunctive use of metformin delivery in periodontal treatment appears to be effective in BD fill, reducing probing depth and gain in clinical attachment level. Further multicentered randomized clinical trials are warranted in future to prove additional benefits of metformin as an adjunct to SRP in the treatment of chronic periodontitis.
Assuntos
Periodontite Crônica/terapia, Raspagem Dentária, Metformina/administração & dosagem, Aplainamento Radicular, Bases de Dados Bibliográficas, Humanos, Ensaios Clínicos Controlados Aleatórios como Assunto, Resultado do TratamentoRESUMO
BACKGROUND AND OBJECTIVE: The aim of the present study was to compare clinical periodontal parameters and to assess the release of C-telopeptides pyridinoline cross-links (ICTP) and C-terminal crosslinked telopeptide (CTX) from gingival collagen of naswar (NW) and non-naswar (control) dippers. MATERIAL AND METHODS: Eighty-seven individuals (42 individuals consuming NW and 45 controls) were included. Clinical (plaque index, bleeding on probing, probing depth and clinical attachment loss) and radiographic (marginal bone loss) periodontal parameters were compared among NW and control groups. Gingival specimens were taken from subjects in NW and control groups, assessed for ICTP and CTX levels (using ELISA) and analyzed using micro-Raman spectroscopy. The significance of differences in periodontal parameters between the groups was determined using Kruskal-Wallis and Mann-Whitney U tests. The percent loss of dry mass over exposure time and the rate of release of ICTP and CTX from all groups were compared using the paired t-test to examine the effects of exposure time. RESULTS: Clinical and radiographic periodontal parameters were significantly higher in the NW group than the control group (P < .01). In the Raman spectrum, the strongest and sharpest band occurred at 1260 cm-1 amongst NW users. A Raman band at Amide I was observed with slight shifts in wave numbers. The rate of ICTP and CTX release was significantly higher in subjects from the NW group compared with those from the control group (P < .05). Both factors, the type of groups and time, had a significant effect on release of ICTP and CTX (P < .05). CONCLUSION: Within the limits of the present study, it may be concluded that clinical and radiographic periodontal parameters were worse among subjects in the NW group than in those of the control group. There is a higher degree of collagen breakdown in the connective tissue of subjects in the NW group as a result of naswar usage.
Assuntos
Colágeno Tipo I/metabolismo, Colágeno/metabolismo, Peptídeos/metabolismo, Tabaco sem Fumaça/efeitos adversos, Adulto, Perda do Osso Alveolar/diagnóstico por imagem, Perda do Osso Alveolar/patologia, Biomarcadores/metabolismo, Estudos de Casos e Controles, Índice de Placa Dentária, Gengiva/metabolismo, Humanos, Masculino, Perda da Inserção Periodontal/diagnóstico por imagem, Perda da Inserção Periodontal/patologia, Índice Periodontal, Bolsa Periodontal/diagnóstico por imagem, Bolsa Periodontal/patologia, Análise Espectral RamanRESUMO
There are no studies that have systematically reviewed the influence of involuntary cigarette smoke inhalation (ICSI) on the stability of implants. The aim of the present study was to perform a systematic review and meta-analysis of preclinical studies that assessed the influence of involuntary cigarette smoke inhalation ICSI on osseointegration. Indexed databases (PubMed, Google-Scholar, Scopus, EMBASE, and Web of Knowledge) were searched till September 2017. Titles and abstracts of studies identified using the above-described protocol were independently screened by 2 authors. Full-texts of studies judged by title and abstract to be relevant were independently evaluated for the stated eligibility criteria. Nine studies were included. Six studies showed that ICSI compromised bone area contact around implants. In 4 studies, peri-implant bone mineral density was significantly higher in the control group than among subjects exposed to ICSI. For the effects of ICSI on the osseointegration of dental implants, significant differences could be observed for bone-to-implant contact for test subjects in cancellous (Z=-4.08, p<0.001) and cortical bone (Z=-4.31, p<0.001) respectively. ICSI may negatively influence osseointegration of dental implants. It is imperative to educate patients about the negative effects of passive smoking on dental and systemic health.
Assuntos
Implantes Dentários, Osseointegração/fisiologia, Poluição por Fumaça de Tabaco/efeitos adversos, Animais, Densidade Óssea, Implantes Experimentais, RatosRESUMO
To evaluate the effects of orthodontic palatal plate therapy (OPPT) in the treatment of orofacial dysfunction in children with Down syndrome (DS). Indexed databases were searched. Clinical trials in DS allocated to test (treatment with palatal plates) versus control group (without palatal plates/special physiotherapy for orofacial stimulation) with follow-up of any time duration and assessing mouth closure, tongue position, active and inactive muscle function as outcomes. Study designs, subject demographics, frequency and duration of palatal plate therapy, method for assessment, follow-up period and outcomes were reported according to the PRISMA guidelines. Eight clinical studies were included. The risk of bias was considered high in three studies and moderate in 5 studies. The number of children with DS ranged between 9 and 42. The mean age of children with DS at the start of the study ranged between 2 months and 12 years. The duration of palatal plate therapy ranged between 4 months and 48 months. The follow-up period in all studies ranged from 12 to 58 months. All studies reported OPPT to be effective in improving orofacial disorders in children with DS. Most of the included studies suggest that palatal plate therapy in combination with physiotherapy/orofacial regulation therapy according to Castillo Morales/speech and language intervention seems to be effective in improving orofacial disorders in children with DS. However, the risk of bias of the included studies was high to moderate. Longitudinal trials with standardized evaluation methods, age of children at treatment initiation, treatment duration and standard orofacial outcomes are recommended.
Assuntos
Síndrome de Down/fisiopatologia, Músculos Faciais/fisiopatologia, Lábio/fisiopatologia, Terapia Miofuncional/instrumentação, Aparelhos Ortodônticos, Língua/fisiopatologia, Criança, Pré-Escolar, Humanos, LactenteRESUMO
OBJECTIVES: To assess the attitude and knowledge of family medicine practitioners (FMPs) towards the association between periodontal disease and obesity. MATERIALS AND METHODS: A cross-sectional study was performed and a 13-item survey questionnaire was given to FMPs practicing in 12 different teaching hospitals in Karachi, Pakistan. The questions were aimed at exploring the knowledge of FMP's regarding the association of obesity and periodontal disease and their attitude towards the association of obesity and periodontal disease. Chi-square and Spearman co-efficient were conducted to compare subgroups and correlate factors with the knowledge score of FMPs. RESULTS: A total of 314 questionnaires were completed (response rate = 92%). Median age of participants was 41 years and 57% were females. Almost 61% of FMPs answered all the knowledge questions correctly and 64% reported moderate understanding of the association between periodontal health and obesity. Nearly 73% FMPs inquired from obese patients regarding the periodontal disease and more than half (58%) refer patients to a dentist for evaluation. More than half of FMPs perform periodontal disease screening. Nearly all FMPs considered informing obese patients regarding periodontal disease as one of their roles. CONCLUSIONS: FMP's play an important role in the early diagnosis, prevention and treatment of periodontal conditions in obese patients. More than two thirds of FMPs showed good knowledge of the association of obesity and periodontal disease. The attitudes of FMPs towards assessing and referring obese patients at a risk of having periodontal disease were reassuring.
Assuntos
Atitude do Pessoal de Saúde, Conhecimentos, Atitudes e Prática em Saúde, Obesidade/complicações, Doenças Periodontais/complicações, Médicos de Família/estatística & dados numéricos, Adulto, Estudos Transversais, Medicina de Família e Comunidade, Feminino, Humanos, Masculino, Inquéritos e QuestionáriosRESUMO
Nicotine has been associated with vasoconstriction and an impaired cellular healing response. It is therefore likely that nicotine jeopardizes osseointegration. This systematic review and meta-analysis was performed to assess pre-clinical studies on the effect of nicotine on implant osseointegration. Databases were searched up to and including March 2016 for animal/non-human studies using the following Keywords: bone to implant contact; implant; nicotine; osseointegration; bone healing; and new bone formation. In total eight in vivo design studies were included and processed for data extraction. Five studies reported no significant influence of nicotine on healing around implants. Quantitative analysis of the effects of nicotine on the osseointegration of dental implants showed a significant difference in bone-to-implant contact between test and control subjects (Z=-2.49; P=0.014). From the studies included in the present review; it appears that nicotine has an effect on implant osseointegration.
