Effects of different drying methods on quality of male flowers of Eucommia ulmoides based on color and chemical composition / 中国中药杂志

To study the effects of different drying methods on the quality of male flowers of Eucommia ulmoides(MFOEU), we treated fresh MFOEU samples with drying in the shade(DS), vacuum freeze drying(VFD), high-or low-temperature hot air drying(HTHAD, LTHAD), microwave drying(MD), and vacuum drying(VD), respectively. The color, total flavonoid content, total polysaccharide content, and main active components such as geniposide, geniposidic acid, rutin, chlorogenic acid, galuteolin, pinoresinol diglucoside, and aucubin in MFOEU were taken as the evaluation indicators. The quality of MFOEU was comprehensively evaluated by entropy weight method combined with color index method, partial least squares discriminant analysis and content clustering heat map. The experimental results showed that VFD and DS basically kept the original color of MFOEU. The MFOEU treated with MD had higher content of total polysaccharides, phenylpropanoids, lignans, and iridoids. The MFOEU treated with LTHAD had higher content of total flavonoids and that treated with VD had lower content of active components. According to the results of comprehensive evaluation, the quality of MFOEU dried with different methods followed the order of MD>HTHAD>VFD>LTHAD>DS>VD. Considering the color of MFOEU, the suitable drying methods were DS and VFD. Considering the color, active components, and economic benefits of MFOEU, MD was the suitable drying method. The results of this study are of a reference value for the determination of suitable methods for MFOEU processing in the producing areas.

Therapeutic potential of rutin in male infertility: A mini review / 中西医结合学报

Male infertility has become a problem worldwide, and recent research has emphasized the development of more effective therapy options. Among natural compounds, rutin has been widely studied for its potential to treat dysfunction related to male infertility, including a reduction in sperm quality, spermatogenesis disruption and structural disruption in the testis. A thorough review of scientific literature published in several databases, including Google Scholar, PubMed/MEDLINE and Scopus, was used to synthesize the present state of research on the role of rutin in male reproductive health. Rutin has been shown to possess antiapoptotic, antioxidant and anti-inflammatory activities, among others, which are crucial in the management of male infertility. Numerous investigations have shown that rutin protects against male infertility and have explored the underlying mechanisms involved. The present review, therefore, assesses the therapeutic mechanisms involved in male infertility treatment using rutin. Rutin was able to mitigate the induced oxidative stress, apoptosis, inflammation, and related physiological processes that can cause testicular dysfunction. Please cite this article as: Rotimi DE, Elebiyo TC, Ojo OA. Therapeutic potential of rutin in male infertility: A mini review. J Integr Med. 2023; 21(2): 130-135.

Quality by design (Qbd) approach to develop stability indicating HPLC method for estimation of rutin in chitosan-sodium alginate nanoparticles

Rutin is a flavonoid glycoside, mainly consists of phenolic compounds, responsible for many biological activities. The objective of the present study was to develop and validate a precise, simple, robust, rapid and reliable reverse phase high -performance liquid chromatography (RP-HPLC) technique by using Qbd approach for evaluating the rutin in nanoparticles. Central composite design (CCD) was employed for optimizing the experimental conditions of RP-HPLC method. Buffer pH, methanol content in the mobile phase composition, flow rate, and wavelength were selected as independent variables whereas retention time, peak area, and asymmetry factor was selected as dependent variables. The retention time, peak area and asymmetric factor of rutin by using optimized independent variables were found to be 3.75 min, 1014.79 mV, and 1.26 respectively. The limit of detection and limit of quantitation values were found to be 0.005 µg/mL and 0.15 µg/mL respectively. For confirming linearity, accuracy, precision, and robustness, the optimized assay condition was validated as per ICH guidelines. The proposed method, which was optimized by QbD approach was found to be a suitable method for analyzing the rutin in chitosan-sodium alginate nanoparticles.

Antidiabetic activity evaluation of Onobrychis species on alloxan-induced diabetic mice

In the current study, four Onobrychis species, O. albiflora Hub.-Mor., O. argyrea Boiss. subsp. argyrea Boiss., O. galegifolia Boiss., and O. tournefortii (Willd.) Desv. were collected from Anatolia to be evaluated for their antidiabetic activities. Methanol water extracts of the aerial parts were used for experiments. An alloxan-induced diabetic mice test model was used. Phytochemical analysis of the tested extracts was investigated using the HPLC method. The highest activity was observed with treatment of O. albiflora aerial part extract. Significant decrements were detected in the blood glucose levels as follows: 180.83±47.48 and 252.83±50.47mg/dL at 100 mg/kg and 200 mg/kg doses of O. albiflora, respectively, when compared to the isotonic saline solution control group, eliciting a blood glucose level of 494.20±27.32. Among the tested standard compounds, rutin and isoquercetin were detected in the examined species. The highest amount of rutin (1.1981±0.0017%) and isoquercetin (0.7318±0.0197%) were found in O. albiflora and O. argyrea subsp. argyrea, respectively. Antidiabetic activities of the tested Onobrychis species seem to indicate a possible correlation with their rutin and isoquercetin contents. Therefore, rutin and isoquercetin may be the antidiabetic compounds that contribute to the antidiabetic activity of the tested Onobrychis species.

Desenvolvimento, caracterização e avaliação da formação de complexos de inclusão de rutina, avobenzona e ρ-metoxicinamato de octila na presença de ciclodextrinas / Development, characterization and evaluation of inclusion complexes between rutin, avobenzone and octyl ρ-methoxycinnamate with cyclodextrins

A radiação UV pode causar danos à pele humana, e, evitar estes danos, é uma preocupação crescente para a população e um desafio à comunidade científica. Para uma ação efetiva de fotoproteção, a associação de filtros, como avobenzona (BMBM) e ρ-metoxicinamato de octila (EHMC), são empregados. Devido à semelhança estrutural com os filtros solares químicos, a rutina (RUT), tal como outros flavonoides, apresenta atividade fotoprotetora. Apesar da disponibilidade de diferentes classes de filtros solares, o desenvolvimento de fotoprotetores contendo filtros químicos é um desafio, devido à instabilidade inerente a certos filtros orgânicos. As ciclodextrinas (CDs) são oligossacarídeos cíclicos, de formato tronco-cônico, cuja estrutura externa é hidrófilica e sua cavidade interna central hidrofóbica, com a capacidade de acomodar substâncias lipofílicas, formando complexos de inclusão. A formação dos complexos de inclusão pode levar à alterações de propriedades físico-químicas da molécula hóspede, tais como, solubilidade, fotoestabilidade e biodisponibilidade. O objetivo deste trabalho foi desenvolver, caracterizar e avaliar a formação de complexos de inclusão entre RUT, BMBM e EHMC e as CDs (HPßCD e SBEßCD). Os complexos de inclusão (RUT:HPßCD, RUT:SBEßCD, BMBM:HPßCD, BMBM:SBEßCD, EHMC:HPßCD e EHMC:SBEßCD) foram obtidos pelo método de liofilização e quantificados por cromatografia líquida de alta eficiência (CLAE). Os sistemas binários foram caracterizados em solução, pelo método de equilíbrio de solubilidade, e, no estado sólido, empregando calorimetria exploratória diferencial (DSC), termogravimetria (TG/DTG) e difração de raios-X de pó (PDRX). As substâncias isoladas e os complexos binários foram avaliados quanto à fotoestabilidade em estado sólido, e, em solução. Incremento na solubilidade (X mcg mL-1) foi observado para os complexo RUT:HPßCD (4,13x); RUT:SBEßCD (4,38x); BMBM:HPßCD (43,3x); BMBM:SBEßCD (53,3x); EHMC:HPßCD (12,7x); e EHMC:SBEßCD (70,0x). Os ensaios de DSC, TG/DTG, e P-DRX indicaram a formação de complexos de inclusão para os todos os sistemas, onde a supressão dos eventos endotérmicos característicos das substâncias isoladas foram observados; porém, nos complexos de BMBM, a presença de avobenzona livre no meio foi detectada, sugerindo, que a complexação não foi completa. A formação dos complexos de inclusão promoveu o aumento da fotoestabilidade em todos os sistemas avaliados, tanto no estado sólido, como em solução. Os resultados reportados neste estudo, indicaram que a complexação de substâncias fotoprotetoras com HPßCD e SBEßCD, pode representar, uma estratégia promissora quanto ao aumento da solubilidade e da fotoestabilidade

UV radiation may cause demage on human skin, and preventing it, is an increasing worry for the population and a challenge to the scientific community. For an effective action of photoprotection, the association of filters, like avobention (BMBM) and octyl ρ-methoxycinnamate (EHMC), are used. Due to the structural similarity with the chemical solar filters, the rutin (RUT), like other flavonoids, shows photoprotective activity. Despite the availability of different classes of sunscreens, the development of photoprotectors containing chemical filters is a challenge, due to the inherent instability of certain organic filters. The cyclodextrins (CD) are cyclic oligosaccharides of truncated conical structure, which external structure is hydrophilic and its internal central hydrophobic cavity, with capacity to accommodate lipophilic substances, forming inclusion complexes. The formation of the inclusion complexes can lead to changes in physicalchemical properties of the host molecule, such as, solubility, photostability and bioavailability. The objective of this work was to develop, characterize and evaluate the formation of the inclusion complexes between RUT, BMBM and EHMC and the CDs (HPßCD and SBEßCD). The inclusion complexes (RUT:HPßCD, RUT:SBEßCD, BMBM:HPßCD, BMBM:SBEßCD, EHMC:HPßCD and EHMC:SBEßCD) were obtained by the lyophilization method and quantified by high performance liquid chromatography (HPLC). The binary systems were characterized in solution, by solubility equilibrium method and in solid state, using differential scanning calorimetry (DSC), thermogravimetry (TG/DTG) and powder X-ray diffraction (P-XRD). The isolated substances and binary complexes were evaluated the photostability in solid state, and in solution. The increase in solubility (X mcg mL-1) was observed for the complexes RUT:HPßCD (4.13x); RUT:SBEßCD (4.38x); BMBM:HPßCD (43.3x); BMBM:SBEßCD (53.3x); EHMC:HPßCD (12.7x); and EHMC:SBEßCD (70.0x). The analysis of DSC, TG/DTG, and P-DRX indicated the formation of inclusion complexes for all systems, where the suppression of the endothermic events characteristic of the isolated substances were observed; however, in the BMBM complexes, the presence of free avobenzone was detected, suggesting that the complexation was not complete. The formation of inclusion complexes promoted the increase of photostability in all evaluated systems, as in solid state as in solution. The results reported in this study indicated that the complexation of photoprotective substances with (HPßCD e SBEßCD). may represent a promising strategy for increasing solubility and photostability

Fotoprotetores bioativos multifuncionais contendo rutina, octil dimetil PABA e avobenzona: caracterização físico-química, funcional e eficácia clínica / Bioactive sunscreens containing rutin, octyl dimethyl PABA and avobenzone: physicochemical, functional and clinical characterization

A exposição crônica à radiação solar pode contribuir para o aparecimento do câncer de pele, sendo o uso de fotoprotetores um fator primordial na prevenção desses efeitos deletérios. Atualmente, substâncias bioativas tais como a rutina têm sido foco de interesse da comunidade científica graças às suas propriedades fotoprotetoras e antioxidantes, que podem promover aumento dos valores de FPS, além de conferir características multifuncionais às formulações. Achados in vitro recentes indicam que a rutina, quando incorporada em emulsões fotoprotetoras óleo em água, promove aumento da atividade antioxidante e aumento do FPS. No entanto, a realização de estudos clínicos é fundamental para confirmar e quantificar esses resultados, já que a metodologia in vitro possui baixa repetibilidade e ausência de correlação com ensaios in vivo, principalmente quando as formulações analisadas apresentam substâncias antioxidantes em sua composição. O objetivo deste estudo foi avaliar pela primeira vez a atividade da rutina frente ao FPS e sua segurança clínica através da comparação de formulações fotoprotetoras contendo rutina 0.1% (w/w), avobenzona 3.0% (w/w) e octil dimetil PABA 8.0% (w/w) com uma preparação similar sem o composto bioativo. Adicionalmente, hidratação cutânea, FPS in vitro e atividade antioxidante da rutina em associação com outros filtros foram investigados. O perfil de segurança das formulações qualificou as fórmulas para os testes de eficácia clínica. O teste de DPPH confirmou a capacidade antioxidante da rutina, demonstrando cerca de 40% de aumento na capacidade de sequestro de radicais livres na presença do composto bioativo. A rutina em combinação com os filtros UV aumentou o FPS clínico de 7.30 ± 0.60 para 12.37 ± 1.13, o que representa cerca de 70% de aumento. Os resultados encontrados provam que a rutina em combinação com outros filtros pode aumentar significativamente o valor do FPS e que a mesma é segura para uso clínico

Unprotected chronic exposure to solar radiation can contribute to premature skin cancer and sunscreens are a key factor to avoid those detrimental effects. Currently, there is a growing interest in the photoprotector and antioxidant potential of bioactive substances, such as rutin, that could help to increase the SPF value and add multifunctional characteristics to the formulations. Recent in vitro findings indicated that rutin, when incorporated in oil-in-water photoprotective emulsions can provide antioxidant activity and SPF increase. However, clinical studies are fundamental to determine this activity duo to in vitro methodology lack of repeatability and correlation between the in vivo data, especially when the analyzed formulas contain antioxidant substances. The aim of this study was to evaluate for the first time to date the rutin in vivo SPF and clinical safety by comparing sunscreens formulations containing rutin 0.1% (w/w), butyl methoxydibenzoylmethane 3.0% (w/w) and octyl dimethylPABA 8.0% (w/w) with a similar bioactive-free preparation. Additionally, skin hydration, in vitro SPF and in vitro antioxidant activity of rutin, in association with the UV filters were investigated. The safety profile of the formulations under sun-exposed skin conditions qualified the formulas for clinical efficacy assays. DPPH test confirmed rutin antioxidant properties, demonstrating about 40% increase in radical scavenging potential when the bioactive compound was present. Rutin in combination with the UV filters increased the clinical SPF from 7.30 ± 0.60 to 12.37 ± 1.13, representing about 70% growth in the SPF value. The results obtained proved that rutin in combination with UV filters can improve the SPF value significantly and is safe for clinical use

Aplicação de planejamento fatorial na oxidação de óleos contendo diferentes tipos de ácidos graxos ômega 3 / The use of factorial design to evaluate the oxidation of oils containing differents types of omega 3 fatty acids

Óleos contendo alta proporção de ácidos graxos ômega-3 (n-3 FA) têm sido aplicados na formulação de alimentos ou comercializados como suplementos, com a finalidade de reduzir o risco cardiovascular, principalmente devido aos seus efeitos hipotriglicêmicos e anti-inflamatórios. No entanto, a susceptibilidade à oxidação dos n-3 FA é elevada, levando à formação de vários produtos secundários, incluindo alguns tóxicos e potencialmente aterogênicos. Por esta razão, compostos naturais com propriedades antioxidantes têm sido investigados com o objetivo de melhorar a estabilidade oxidativa dos óleos com alta proporção de n-3 FA. Neste estudo, avaliou-se a capacidade antioxidante de dois compostos naturais (ácido sinápico e hidrato de rutina) utilizando-se um modelo acelerado para oxidar os óleos. Foram combinados cinco indutores (Temperatura; Ferro- Fe2+; 2,2'-Azobis dicloridrato de 2-amidinopropano - AAPH; ascorbil palmitato - AP e 2,2'-azobis -2,4-dimetilvaleronitrilo - AMVN) em um delineamento fatorial (25-1) com ½ fração de "resolução V" para acelerar a oxidação de três óleos (linhaça, Echium e peixe) contendo diferentes fontes de n-3 FA: ácido α-linolênico (ALA), ácido estearidônico (SDA) e ácido eicosapentaenóico (EPA) + ácido docosahexaenóico (DHA), respectivamente. Não houve diferença entre os marcadores de oxidação (LOOH e TBARS) estimados pelos modelos e os valores observados experimentalmente. Os indutores AMVN e Fe2+ foram os principais fatores responsáveis pelo aumento da concentração de TBARS. Os valores dos marcadores oxidativos obtidos 48 h após a indução foram semelhantes ou superiores àqueles observados nas amostras oxidadas a 60°C por 15 dias, sendo ambos maiores que os valores observados nas amostras de óleo frescas. Entre os compostos voláteis formados pela oxidação de diferentes fontes de n-3 FA, (E, E) 2,4 -heptadienal, (E, E) 2,4-decadienal, decanal, undecanal e (E) -2-undecenal foram identificados em todas as amostras, podendo ser utilizados como marcadores oxidativos mais específicos. Utilizando o modelo de oxidação acelerada, o hidrato de rutina melhorou a estabilidade oxidativa do óleo de peixe, provavelmente devido à presença de grupos catecol em sua estrutura química. Este estudo contribuiu para que ensaios mais rápidos fossem realizados na avaliação do efeito antioxidante de novas moléculas aplicadas em óleos funcionais comestíveis

Oils containing a high proportion of omega-3 fatty acids (n-3 FA) have been used in the formulation of foods or sold as supplements, aiming to reduce cardio-vascular risks, mainly due to their hypotriglycemic and anti-inflammatory effects. However, n-3 FA are highey susceptible to oxidation, leading to the formation of several products, including some toxic and potentially atherogenic. For this reason, natural products with antioxidant properties have been investigated to improve the oxidative stability of oils with a high proportion of n-3 FA. This study evaluated the antioxidant capacity of two natural compounds (sinapic acid and rutin hydrate), using an accelerated model to oxidize the oils. Five inducers were combined (Temperature, Iron-Fe2+, 2,2'-Azobis (2-amidinopropane) dihydrochloride-AAPH, Ascorbyl palmitate-AP and 2,2'-azobis-2,4-dimethylvaleronitrile-AMVN) in a factorial design (25-1) ½ fraction of "resolution V" to accelerate the oxidation of three oils (flaxseed, Echium and fish) containing different sources of n-3 FA: α-linolenic acid (ALA), stearidonic acid (SDA) and eicosapentaenoic acid (EPA) + docosahexaenoic acid (DHA), respectively. There was no difference between the oxidation markers (LOOH and TBARS) estimated by the regression models and the values experimentally observed. The inducers AMVN and Fe2+ were the main factors responsible for the increase of TBARS concentration. The values of the oxidation markers obtained 48h after the induction were similar to or higher than those obtained when the samples were oxidized at 60°C for 15 days, both being more elevated than the values observed in the fresh oils. Among the volatile compounds formed by the oxidation of different sources of n-3 FA, (E, E) 2,4-heptadienal, (E, E) 2,4-decadienal, decanal, undecanal and (E)-2-undecenal were identified in all samples, and could be used as more specific oxidation markers. Using the accelerated model, rutin hydrate improved the oxidative stability of fish oil, probably due to the presence of catechol groups in its chemical structure. This study showed that faster anays could be performed to evaluate the antioxidant effect of new molecules applied on edible functional oils

Rutin restores adenosine deaminase activity in serum and the liver and improves biochemical parameters in streptozotocin-induced diabetic rats / Rutina restaura a atividade da Adenosina desaminase no soro e no fígado e melhora os parâmetros bioquímicos em ratos diabéticos induzidos por estreptozotocina

ABSTRACT denosine deaminase (ADA) is a critical control point in the regulation of adenosine levels. This study aimed to investigate the effects of a polyphenolic flavonoid, rutin, on the activity of ADA in serum, the cerebral cortex, liver, kidney, and biochemical parameters in diabetic rats. The animals were divided into four groups (n=6) for the following treatments: control; diabetic (streptozotocin 55 mg/kg); diabetic with rutin (100 mg/kg/day); diabetic with glibenclamide (10 mg/kg/day). After 30 days, ADA activity and biochemical parameters were analyzed. The ADA activity in the serum was significantly elevated in the diabetic group compared to the control group (p<0.01). The treatment with rutin prevented the increase in ADA activity in the STZ-induced rats when compared to control group. Our data showed that rutin reduced glucose, LDL levels, and hepatic enzymes in comparison with the control group. These results demonstrate that the increase of ADA activity observed in diabetic rats may be an important indicator of the immunopathogenesis of hyperglycemic disorders and suggest that rutin is important for regulating the enzymatic activities associated with immune, hyperglycemic, and inflammatory response in diabetes mellitus.

RESUMO A Adenosina desaminase (ADA) representa um ponto de controle crítico na regulação dos níveis de adenosina. A rutina, um flavonóide polifenólico presente em muitas plantas, foi testado para verificar a sua influência na atividade da ADA no soro, córtex cerebral, fígado rim e parâmetros bioquímicos em ratos diabéticos. Os animais foram divididos em quatro grupos cada grupo com 6 animais), tal como: controle; diabética (estreptozotocina 55 mg/kg); diabética + rutina (100 mg/kg/dia); diabético + glibenclamida (10 mg/kg/dia). Após 30 dias foram analisadas a atividade da ADA sérica e tecidual e parâmetros bioquímicos. A atividade de ADA no soro foi significativamente elevada no grupo diabético quando comparado ao grupo controle (p<0,01). O tratamento com Rutina preveniu o aumento na atividade da ADA nos ratos diabéticos, quando comparado com o grupo controle. Os resultados mostraram que a rutina reduziu a glicose, os níveis de LDL e as enzimas hepáticas, em comparação com o grupo controle. Estes resultados mostram que o aumento da atividade da ADA observado em ratos diabéticos pode ser um indicador importante da imuno-patogênese de perturbações hiperglicêmicas e sugerem que a Rutina é importante na regulação das atividades enzimáticas associadas com a resposta imunitária, hiperglicêmica e inflamatória no Diabetes mellitus.

Doseamento de flavonoides totais das partes aéreas de Thuja occidentalis Linn. (Cupressaceae) / Assay of total flavonoids from aerial parts of Thuja occidentalis Linn. (Cupressaceae)

Thuja occidentalis é largamente utilizada na forma de tinturas, sendo os flavonoides metabólitos de interesse da espécie, visto as distintas atividades farmacológicas citadas na literatura. Contudo, não há descrito método para a quantificação desses, sendo objetivo desse trabalho desenvolver um método colorimétrico direto utilizando cloreto de alumínio (AlCl3) por espectrofotometria UV, a fim de proporciona a quantificação de flavonoides totais, expresso em rutina. Para tal, avaliaram-se os seguintes parâmetros: concentração da solução hidroalcoólica (SH) (20, 40 e 70%); interferentes lipofílicos; volume da solução de AlCl3 2,5% (1, 2 e 3 mL) e proporção de droga vegetal (0,5, 1, 1,5 g). Adicionalmente, procedeuse a validação. A partir da avaliação dos interferentes lipofílicos, selecionou-se a SH 40% utilizando 1 g da droga vegetal. A cinética de complexação, demonstrou que a formação do complexo flavonoides-Al+3 é lenta, sendo o tempo de leitura ideal de 30 min no λ=403 nm, após a adição de 2 mL de AlCl3 2,5%. A rutina foi utilizada a conversão de absorvância em teor de flavonoides totais, uma vez que a espécie possui a presença majoritária de derivados quercetínicos do grupo flavonol na sua forma glicosilada. O método atendeu a todos os requisitos indicados para validação de uma matriz vegetal, consideração os fatores inerentes da espécie, possibilitando sua utilização na prática laboratorial.

Determinación de rutina y trigonelina en extractos de hojas de Bauhinia forficata subsp. pruinosa y evaluación del efecto hipoglicemiante en humanos / Determination of rutin and trigonelline in extracts of Bauhinia forficata subsp. pruinosa and hypoglycemic effect on diabetic and prediabetic patients humans

Diabetes mellitus type 2 is a metabolic disorder characterized by chronic hyperglycemia, and an important cardiovascular risk factor with a high morbidity and mortality worldwide. Phytotherapy can be an useful complement in the treatment of chronic diseases, so the hypoglycemic effect of Bauhinia forficata (L) subsp. pruinosa (Fabaceae) was evaluated, as used in Chilean traditional medicine. The content of rutin (R) and trigonelline (T) in aqueous extracts (0.15 and 1.0 percent infusions) and lyophilized extract from leaves of B. forficata were determined by HPLC. It was obtained 2.80 ugR/mL and 2.87 ugT/mL for 0.15 percent infusion, 12.48 ugR/mL and 16.24 ugT/mL for 1.0 percent infusion, and 5.70 ugR/mL and 8.14 ugT/mL for the lyophilized extract (0.1percent). Subsequently, a pilot clinical study in diabetic and prediabetic volunteers (n = 15) was performed, taking one dose of the 0.15 percent infusion, three times a day after meals, for 3 months. The results showed a significant statistically reduction in percent of HbA1c of 0.57 +/- 0.83 (p = 0.0179), suggesting that the 0.15 percent infusion of B. forficata could be useful in the prevention or complementary treatment of diabetes...

La diabetes mellitus tipo 2 es una alteración metabólica caracterizada por hiperglicemia crónica, y un importante factor de riesgo cardiovascular con elevada morbimortalidad a nivel mundial. La Fitoterapia puede ser un complemento útil en el tratamiento de enfermedades crónicas, por lo que se evaluó el efecto hipoglicemiante de Bauhinia forficata (L) subsp. pruinosa (Fabaceae), según su uso en medicina tradicional Chilena. Se determinó mediante HPLC el contenido de rutina (R) y trigonelina (T) en infusos (0.15 por ciento y 1.0 por ciento) y extracto acuoso liofilizado de las hojas de B. forficata. Se obtuvo para el infuso 0.15 por ciento = 2.80 ugR/mL y 2.87 ugT/mL, infuso 1.0 por ciento = 12.48 ugR/mL y 16.24 ugT/mL, y en el extracto liofilizado 0.1 por ciento = 5.70 ugR/mL y 8.14 ugT/mL. Posteriormente, se realizó un estudio clínico piloto en voluntarios diabéticos y prediabéticos (n = 15), tomando una dosis del infuso al 0.15 por ciento, tres veces al día después de las comidas, durante 3 meses. Los resultados mostraron una reducción estadísticamente significativa del por ciento de HbA1c de 0.57 +/- 0.83 (p = 0.0179), sugiriendo que el infuso de hojas de B. forficata (0.15 por ciento) podría ser útil en la prevención o tratamiento complementario de la diabetes...

Relaxant effects of a hydroalcoholic extract of Ruta graveolens on isolated rat tracheal rings

BACKGROUND: Ruta graveolens L. (R. graveolens) is a medicinal plant employed in non-traditional medicines that has various therapeutic properties, including anthelmintic, and vasodilatory actions, among others. We evaluated the trachea-relaxant effects of hydroalcoholic extract of R. graveolens against potassium chloride (KCl)- and carbachol-induced contraction of rat tracheal rings in an isolated organ bath. RESULTS: The results showed that the airway smooth muscle contraction induced by the depolarizing agent (KCl) and cholinergic agonist (carbachol) was markedly reduced by R. graveolens in a concentration-dependent manner, with maximum values of 109 ± 7.9 % and 118 ± 2.6 %, respectively (changes in tension expressed as positive percentages of change in proportion to maximum contraction), at the concentration of 45 µg/mL (half-maximal inhibitory concentration IC50: 35.5 µg/mL and 27.8 µg/mL for KCl- and carbachol-induced contraction, respectively). Additionally, the presence of R. graveolens produced rightward parallel displacement of carbachol dose-response curves and reduced over 35 % of the maximum smooth muscle contraction. CONCLUSIONS: The hydroalcoholic extract of R. graveolens exhibited relaxant activity on rat tracheal rings. The results suggest that the trachea-relaxant effect is mediated by a non-competitive antagonistic mechanism. More detailed studies are needed to identify the target of the inhibition, and to determine more precisely the pharmacological mechanisms involved in the observed biological effects.

Influência da rutina na fotoestabilização da avobenzona (filtro UVA) e do ρ-metoxicinamato de octila (filtro UVB) / Influence of rutin in photostabilization of avobenzone (UVA filter) and octyl methoxycinnamate (UVB filter)

Com o intuito de promover proteção de amplo espectro, na maioria dos protetores solares estão associados pelo menos dois filtros orgânicos (UVA e UVB). A combinação da avobenzona (BMBM), filtro UVA, e do p--metoxicinamato de octila (EHMC), filtro UVB, é conhecida e muito utilizada em formulações manipulas e industrializadas, porém apresenta alteração na absorção espectral após exposição à radiação UV. A estratégia empregada com maior frequência para reduzir a instabilidade da combinação é baseada na adição de agentes fotoestabilizadores. A adição de substâncias naturais em formulações fotoprotetoras vem sendo explorada, especialmente o grupo dos flavonoides, como a rutina, que apresenta resultados positivos em relação à eficácia fotoprotetora. O objetivo principal desta pesquisa foi avaliar o potencial da rutina como substância fotoestabilizadora dos filtros EHMC e BMBM. Foram desenvolvidas formulações contendo os dois filtros associados ou não com rutina de acordo planejamento fatorial em três níveis. As formulações foram avaliadas quanto a eficácia fotoprotetora in vitro aplicadas em placas de PMMA e analisadas por espectrofotometria de refletância com esfera de integração antes e após a exposição à radiação UV. As interações moleculares dos filtros com a rutina foram avaliadas por 1H RMN, DSC, TG e análise qualitativa da supressão do estado energético singleto. A adição de rutina nas formulações contendo 5,0% (p/p) de BMBM e 10,0% (p/p) de EHMC promoveu elevação na conservação do FPS in vitro de 53,9% para 65,8 (0,1% de rutina) e 70,8% (1,0% de rutina). As curvas DSC e TG da rutina apresentaram alterações promovidas pela presença dos filtros BMBM e EHMC, indicando interação entre o flavonoide e os filtros. Após dose de 5760 J cm-2 de radiação UV o valor da razão trans/cis para o filtro EHMC em solução adicionado do filtro BMBM foi elevado de 5,5±0,1, sem adição de rutina, para 12,6±0,4, com adição da rutina. A análise qualitativa da supressão do estado singleto indicou que um dos mecanismos envolvidos na fotoestabilização dos filtros BMBM e EHMC é a supressão do estado energético singleto. Os resultados reportados neste estudo indicaram que a adição da rutina em formulações fotoprotetoras representa um caminho simples e efetivo para elevar a fotoestabilidade da combinação dos filtros BMBM e EHMC. A adição da rutina em formulações fotoprotetoras representa uma estratégia promissora, pois aliada a ação fotoestabilizadora, verificada nesse estudo, esse flavonoide possui propriedades antioxidante e quelante de metais que podem colaborar para o desenvolvimento de formulações fotoprotetoras de amplo espectro com aumento da segurança e eficácia

In order to promote broad-spectrum protection, most sunscreens are associated with at least two organic filters (UVA and UVB). The combination of avobenzone (BMBM), UVA filter, and octyl methoxycinnamate (EHMC), UVB filter, is well known and widely used in industrial formulations and pharmaceutical compounding, but shows alteration in spectral absorption after UV radiation exposure. The most commonly used strategy to reduce the instability of the combination is based on the addition of photostabilizer agents. The addition of natural substances in sunscreen formulations has been explored, especially the group of flavonoids such as rutin, which shows positive results regarding photoprotective efficacy. The main objective of this research was to evaluate the potential of rutin as a photostabilizer substance of EHMC and BMBM. Formulations were developed containing the two filters associated or not with rutin, according to factorial design at three levels. The formulations were evaluated for in vitro photoprotective efficacy applied on PMMA plates and analyzed by spectrophotometer with integrating sphere reflectance before and after exposure to UV radiation. Molecular interactions of filters with rutin were evaluated by 1H NMR, DSC, TG and qualitative analysis of the suppression of singlet energy state. The addition of rutin in the formulations containing 5.0 % (w/w) BMBM and 10.0 % (w/w) EHMC promoted an increase in the preservation of in vitro SPF of 53.9% to 65.8 (0.1 % rutin) and 70.8 % (1.0% rutin). The DSC and TG curves of rutin showed changes promoted by the presence of BMBM and EHMC filters, indicating interaction between the flavonoid and filters. After 5760 J cm-2 of UV radiation the value of the trans/cis ratio for the EHMC filter added from the BMBM filter was increased from 5.5 ± 0.1 without addition of rutin, to 12.6 ± 0 4,with the addition of rutin. Qualitative analysis of the suppression of the singlet state indicated that one of the mechanisms involved in the photostabilization BMBM and EHMC filters is suppression of singlet excited state.The results reported in this study indicate that the addition of rutin in sunscreen formulations is a simple and effective way to increase the photostability of the combination of BMBM and EHMC. The addition of rutin in sunscreen formulations represents a promising strategy, for allied with the photostabilization action, observed in this study, this flavonoid has antioxidant and chelating properties of metals that can contribute to the development of broad-spectrum sunscreens formulations with increased safety and efficacy

Determination of rutin in Erythroxylum suberosum extract by liquid chromatography: applicability in standardization of herbs and stability studies / Determinación de rutina en el extracto Erythroxylum suberosum por cromatografía líquida: aplicación de la normalización de las hierbas y los estudios de estabilidad

In this study, a reverse phase-high performance liquid chromatography (RP-HPLC) technique for determination of rutin in Erythroxylum suberosum extract was developed and validated. A regression analysis was performed, with the observation of good linearity (r = 0.9997). The values obtained for precision and accuracy determination are in agreement with ICH guidelines. The detection and the quantitation limits of rutin were 0.19 ug/mL and 0.60 ug/mL, respectively. The results demonstrated that the developed method is a reliable HPLC technique for determination of rutin in E. suberosum extract. In addition, the applicability of this method in stability studies and standardization of herbs was investigated.

En este estudio, la técnica de cromatografía líquida de alta resolución en fase reversa para la determinación de la rutina en el extracto Erythroxylum suberosum fue desarrollada y validada. Se realizó un análisis de regresión, con la observación de una buena linealidad (r = 0,9997). Los valores obtenidos para la precisión y la determinación de la precisión están de acuerdo con las directrices ICH. La detección y cuantificación de los límites de la rutina fueron 0,19 ug / mL y 0,60 ug / mL, respectivamente. Los resultados demostraron que el método desarrollado es una técnica fiable de HPLC para la determinación de la rutina en el extracto de E. suberosum. Además, se investigó la aplicabilidad de este método en los estudios de estabilidad y la estandarización de hierbas.

Síntese e avaliação da segurança in vitro da rutina e do succinato de rutina visando sua incorporação em formulações fotoprotetoras eficazes associados a filtros químicos e físico / Synthesis and in vitro safety evaluation of rutin and rutin succinate aiming their incorporation into effective sunscreens associated with chemical and physical filters

A tendência atual do mercado cosmético é desenvolver produtos que contenham insumos de origem vegetal. O objetivo deste trabalho foi a aplicação da Tecnologia da Química Verde na síntese da rutina visando o aumento da estabilidade dessa em formulações cosméticas com sua eficácia antioxidante e fotoprotetora. Realizou-se a síntese química por meio da introdução de grupos carboxilatos às hidroxilas do dissacarídeo na molécula de rutina, gerando como produto final o succinato de rutina. Este derivado e/ou a rutina foram incorporados em 74 formulações-teste e, selecionadas 12 (sistemas emulsionados O/A), após serem submetidas à Avaliação Preliminar de Estabilidade (APE) e ao Teste de Estabilidade Acelerada (TEA), sob variações de temperatura e umidade. Utilizou-se agentes emolientes e silicones para facilitar a solubilização e/ou dispersão dos filtros químicos e físicos. A segunda etapa deste trabalho foi a avaliação da segurança do succinato de rutina, tendo como padrão a rutina, por meio do método alternativo de toxicidade in vitro, o XTT. Após o screening das concentrações ensaiadas, as que apresentaram menor nível de morte celular foram respectivamente, 0,1% ou 1 mg/mL (rutina) e 0,4% ou 4 mg/mL (succinato de rutina). Segundo os resultados do TEA, as formulações contendo succinato de rutina associada ou não aos filtros solares em ambas as bases cosméticas (A - Crodafos®CES + Uniox®C e B - Hostacerin®SAF) foram selecionadas para a continuidade do Teste de Estabilidade Normal (TEN). Neste teste, as emulsões fotoprotetoras foram avaliadas frente aos parâmetros: propriedades organolépticas (aspecto, cor e odor), aspectos físico-químicos (medição de pH e de viscosidade) e funcionais (atividade antirradicalar e eficácia fotoprotetora in vitro). Os resultados apresentados pela formulação MS (succinato de rutina associado aos filtros químicos e físico) foram: homogeneidade, a não modificação de cor e odor em temperatura ambiente, a não alterações significativas...

The current cosmetic market trend is to develop products containing vegetables raw materials. This work proposed to use the Technology of Green Chemical to increase the rutin stability in cosmetic formulas as regards of its antioxidant and photoprotective properties. The chemical synthesis was realized by the introduction of carboxylate groups on sugar moiety of rutin producing in rutin succinate. This derivative and/or rutin were incorporated into 74 test formulas. After the undergoing to preliminary and accelerated stabilities under different temperature and humidity conditions were selected 12 formulas (O/W emulsions). Emollient agents and silicones were used to improve the solubility and/or dispersion of the chemical and physical filters. The second stage of this work was to evaluate the safety of rutin succinate, rutin used as an internal standard, using the alternative method of in vitro toxicity, the XTT. After the screening of tested concentrations, the concentrations of the samples with the lowest level of cell death were 0.1% or 1 mg/mL (rutin) and 0.4% or 4 mg/mL (rutin succinate), respectively. According to results obtained in accelerated stability testing, the formulations containing rutin succinate in combination or not with UV filters in both O/W emulsions (A - Crodafos®CES + Uniox®C and B - Hostacerin®SAF) were selected for the long term stability test. In this test the sunscreens were evaluated in the following parameters: the organoleptic properties (appearance, color and odor), physico-chemical aspects (pH value and viscosity) and functional (antiradicalar activity and in vitro photoprotection efficacy). The results presented by the MS formula (rutin succinate associated with physical filter and chemical filters) were: uniformity, stability of color and odor at room temperature and showed no significant difference, as well stability in: pH and SPF (Sun Protection Factor) values, hysteresis area, antiradicalar activity. These results were...

Square-wave voltammetric determination of rutin in pharmaceutical formulations using a carbon composite electrode modified with copper (II) phosphate immobilized in polyester resin

A carbon composite electrode modified with copper (II) phosphate immobilized in a polyester resin (Cu3(PO4)2-Poly) for the determination of rutin in pharmaceutical samples by square-wave voltammetry is described herein. The modified electrode allows the determination of rutin at a potential (0.20 V vs. Ag/AgCl (3.0 mol L-1 KCl)) lower than that observed at an unmodified electrode. The peak current was found to be linear to the rutin concentration in the range from 9.9 × 10-8 to 2.5 × 10-6 mol L-1, with a detection limit of 1.2×10-8 mol L-1. The response of the electrode was stable, with no variation in baseline levels within several hours of continuous operation. The surface morphology of the modified electrode was characterized by scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) system. The results obtained are precise and accurate. In addition, these results are in agreement with those obtained by the chromatographic method at a 95% confidence level.

Descreve-se um eletrodo de carbono modificado com fosfato de cobre (II) imobilizado em uma resina de poliéster (Cu3(PO4)2-Poly) para a determinação de rutina em amostras farmacêuticas por voltametria de onda quadrada. O eletrodo modificado permite a determinação de rutina em potencial (0.20 V vs Ag / AgCl (3,0 mol L-1 KCl)) menor que o observado em um eletrodo não modificado. Verificou-se que a corrente de pico foi linear com a concentração de rutina na faixa de 9,9 × 10-8 a 2,5 × 10-6 mol L-1, com um limite de detecção de 1,2 × 10-8 mol L¹. A resposta do eletrodo foi estável, sem variação significativa dentro de várias horas de operação contínua. A morfologia da superfície do eletrodo modificado foi caracterizada por microscopia eletrônica de varredura (MEV) e pelo sistema de energia dispersiva de raios-X (EDX). Os resultados obtidos foram precisos e exatos. Ademais, estes resultados estão de acordo com aqueles obtidos pelo método cromatográfico a um nível de confiança de 95%.

Antifungal activity of five species of Polygala

Crude extracts and fractions of five species of Polygala - P. campestris, P. cyparissias, P. paniculata, P. pulchella and P. sabulosa - were investigated for their in vitro antifungal activity against opportunistic Candida species, Cryptococcus gattii and Sporothrix schenckii with bioautographic and microdilution assays. In the bioautographic assays, the major extracts were active against the fungi tested. In the minimal concentration inhibitory (MIC) assay, the hexane extract of P. paniculata and EtOAc fraction of P. sabulosa showed the best antifungal activity, with MIC values of 60 and 30 µg/mL, respectively, against C. tropicalis, C. gattii and S. schenckii. The compounds isolated from P. sabulosa prenyloxycoumarin and 1,2,3,4,5,6-hexanehexol displayed antifungal activity against S. schenckii (with MICs of 125 µg/mL and 250 µg/mL, respectively) and C. gattii (both with MICs of 250 µg/mL). Rutin and aurapten isolated from P. paniculata showed antifungal activity against C. gattii with MIC values of 60 and 250 µg/mL, respectively. In the antifungal screening, few of the isolated compounds showed good antifungal inhibition. The compound á-spinasterol showed broad activity against the species tested, while rutin had the best activity with the lowest MIC values for the microorganisms tested. These two compounds may be chemically modified by the introduction of a substitute group that would alter several physico-chemical properties of the molecule, such as hydrophobicity, electronic density and steric strain.

Detection of flavonoids in Alpinia purpurata (Vieill. ) K. Schum. leaves using high-performance liquid chromatography / Detecção de flavonóides em folhas de Alpinia purpurata (Vieill. ) K. Schum. por cromatografia líquida de alta eficiência

The species Alpinia purpurata is scarcely cited as to ethnopharmacology and phytochemistry. This study aimed to analyze bioactive compounds through high-performance liquid chromatography (HPLC). Hydroalcoholic crude extract was obtained from A. purpurata dried leaves. Folin-Ciocalteau method was used to quantify total phenols, using gallic acid as standard. The obtained result was 15.6 mg GAE g-1. The crude extract was partitioned with the solvents ethyl acetate and butanol, followed by thin-layer chromatography (TLC) and HPLC. The flavonoids kaempferol-3-O-glucuronide and rutin were detected at a higher concentration in ethyl acetate and butanolic extracts. The butanolic extract contains the highest flavonoid percentage (94.3 percent). A. purpurata presents important flavonoids of therapeutic use, already verified for A. zerumbet. This is the first study verifying the presence of flavonoids in A. purpurata extracts.

A espécie Alpinia purpurata apresenta poucas citações referentes a etnofarmacologia e fitoquímica. Este estudo propõe a análise de substâncias bioativas através da técnica de cromatografia líquida de alta eficiência (CLAE). O extrato bruto hidroalcóolico foi obtido a partir de folhas secas de A. purpurata. A quantificação de fenóis totais foi realizada pelo método de Folin-Ciocalteau, usando ácido gálico como padrão. Como resultado, foi verificado 15,6 mg EAG g-1. O extrato bruto foi particionado com os solventes acetato de etila e butanol e depois analisado por cromatografia em camada delgada e CLAE. Nos extratos acetato de etila e butanólico foi detectada a presença dos flavonóides kaempferol-3-O-glicuronídeo e rutina, em maior concentração. O extrato butanólico contém a maior porcentagem de flavonóides (94,3 por cento). Esta espécie possui flavonóides importantes no uso terapêutico, já antes verificados para a espécie A. zerumbet. Este é o primeiro trabalho que verifica a presença de flavonóides em extratos de A. purpurata.

Quantitative estimation of betasitosterol, lupeol, quercetin and quercetin glycosides from leaflets of Soymida febrifuga using HPTLC technique

Soymida febrifuga [Meliaceae] dried leaflets [10 gm] were extracted with petroleum ether. Unsaponifiable matter quantitatively used for sample preparation, labeled as SF-U. Another 10 gm leaflet powder was extracted with methanol and quantitatively used for sample preparation labeled as SF-A. Sample and standard solution were dosage on three different plates and developed in its respective mobile phase plates were scanned using TLC scanner III and estimated using integration software CATs 4.05. Calculations for percentage were done considering standard and sample Rf, AUC and dilution factor. Estimation of b Sitosterol, Lupeol, Quercetin, Quercetin-3-O-galactoside, Quercetin-3-O-xyloside and Quercetin-3-O-rutinoside were determined as 0.02146% w/w, 0.0377% w/w, 0.4079% w/w, 0.6197% w/w, 2.974% w/w and 3.235% w/w respectively with the help of HPLC techniques

major constituent of the acetone fraction of ethiopian moringa stenopetala leaves

Phytochemical investigation of the leaves of Moringa stenopetala [Moringaceae], a plant widely used in Ethiopian traditional medicine for the control of diabetes and hypertension, afforded the medicinally useful glycoside rutin. The structure was assigned on the basis of spectroscopic methods [UV, MS, 1H-NMR, 13C-NMR] and hydrolytic studies. The rutin content in the dried leaves was found to be about 1%. Although rutin has been isolated from many plant families, this is the first report of its occurrence in the family Moringaceae

Identificaçäo cromatográfica de flavonóides contidos em drágeas / Chromatographic identification of flavonoids in coated tablets

Os flavonóides Rutina e Hesperidina foram isolados e identificados em drágeas que os continham por cromatografia em camada delgada