In-vitro Anti-hyperglycemic Evaluation of Hydroalcoholic Extract of Delonix regia Bark

Anti-hyperglycemic agents is a substance that helps a person with diabetes control their level of glucose (sugar) in the blood. It includes insulin and oral anti-hyperglycemic agents. Diabetes is a metabolic disorder characterized by increased blood glucose levels leading to other major complications. Thus, obtaining these anti hyperglycemic agents through easily available flora is necessary. Delonix regia , a tree cultivated worldwide, has also been used as traditional medicine in various disorders. Aim of the project work was to evaluate the anti-hyperglycemic activity in the hydroalcoholic extract of D. regia bark for the treatment of hyperglycemia. The collected bark was dried, powdered and extracted through cold maceration method. The extract was further concentrated to obtain a gummy mass of the hydroalcoholic extract. The extract was subjected to phytochemical analysis through conventional chemical tests and GC-MS. After the identification of the phytoconstituents, they were studied for their clinically proven properties. In-vitro anti-hyperglycemic studies were carried out through assays like alpha-amylase inhibition assay and alpha-glucosidase inhibition assay. The results of the extract were compared with results of standard acarbose. The IC 50 standard values in alpha-amylase inhibition assay and ?-glucosidase inhibition assay were 98.77 and 84.33 ?g/mL, respectively. The IC 50 values of hydroalcoholic extract of D. regia bark in alpha-amylase and alpha-glucosidase inhibition assay were 167 and 116.31 ?g/mL, respectively. From the study, the hydroalcoholic extract of bark of D. regia exhibit anti-hyperglycemic activity compared to standard acarbose.

Roles of pancreatic stellate cells and pancreatic cancer cells in angiogenesis of pancreatic cancer: an in vitro study / 中华消化外科杂志

Objective:To investigate the role and mechanism of pancreatic stellate cells (PSCs) and pancreatic cancer cells (PCCs) in the angiogenesis of pancreatic cancer.Methods:The experimental study was conducted. The human PSCs and PCCs and human umbilical vein endothelial cells (HUVECs) were cultured in vitro. HUVECs was treated with PSCs/PCCs supernatants and matrix metalloproteinase (MMP) inhibitor of different types and concentrations. As controls, HUVECs treated with complete endoprime medium (C/E) and DMEM/Ham's F12 medium (D/F) were set as the C/E group and the D/F group, respectively. Observation indicators: (1) proliferation of HUVECs under different conditions; (2) tube formation of HUVECs under different conditions; (3) migration of HUVECs under different conditions; (4) expression of MMP-2 in the supernatants of PSCs and PCCs; (5) effect of MMP inhibitor GM6001 on migration of HUVECs. Measurement data with normal distribution were represented as Mean± SD, comparison among groups was conducted using the one way ANOVA and comparison between groups was conducted using the LSD- t test. Results:(1) Proliferation of HUVECs under different conditions. Results of HUVECs proliferation assay using 5-ethynyl-2′-deoxyuridine (EdU) labeling showed that the binding rate of EdU in the HUVECs of D/F group and HUVECs treated with supernatants of different concentration (25%, 50%, 75%, 95%) of PSCs was 12.4%±1.0%, 24.5%±2.9%, 25.3%±3.0%, 22.8%±2.0%, 22.9%±2.8%, respectively, showing a significant difference among them ( F=8.60, P<0.05). There were significant differences in the binding rate of EdU between HUVECs in the D/F group and HUVECs treated with supernatants of different concentration (25%, 50%, 75%, 95%) of PSCs, respectively ( P<0.05). The binding rate of EdU between HUVECs in the D/F group and HUVECs treated with supernatants of different concentration (25%, 50%, 75%, 95%) of PCCs was 12.4%±1.0%, 30.0%±3.2%, 32.1%±1.0%, 32.3%±3.5%, 26.2%±5.6%, respectively, showing a significant difference among them ( F=11.93, P<0.05). There were significant differences in the binding rate of EdU between HUVECs in the D/F group and HUVECs treated with supernatants of different concentration (25%, 50%, 75%, 95%) of PSCs, respectively ( P<0.05). (2) Tube formation of HUVECs under different conditions. Number of tube formation, length of tube in the HUVECs of D/F group and HUVECs treated with PSCs supernatants was 15.2±2.3, (12.1±1.5)mm and 49.7±3.2, (39.8±2.3)mm, respectively, showing significant differences between the two groups of HUVECs ( P<0.05). (3) Migration of HUVECs under different conditions. Results of single cell tracing experiment showed that the migration rate of HUVECs treated with supernatants of different ratio of PSCs and PCCs was faster than that of HUVECs in the D/F group, and the enhancement effect of supernatants of PSCs and PCCs was dose-dependent. The migration rate of HUVECs treated with mix supernatants of different concentration of PSCs and PCCs and supernatants of co-cultured PSCs and PCCs was faster than that of HUVECs in the D/F group. The migration rate of HUVECs treated supernatants of co-cultured PSCs and PCCs was faster than that of HUVECs treated with mix supernatants of different concentration of PSCs and PCCs, showing a synergistic effect in the HUVECs treated supernatants of co-cultured PSCs and PCCs. (4) Expression of MMP-2 in the supernatants of PSCs and PCCs. Results of gelatine zymography showed that the MMP-2 expression levels decreased sequentially in super-natants of co-cultured PSCs and PCCs, supernatants of PSCs, mix supernatants of PSCs and PCCs and supernatants PCCs. (5) Effect of MMP inhibitor GM6001 on migration of HUVECs. Results of single cell tracing experiment showed that the migration rate of HUVECs treated with PSCs supernatants combined with different concentration of GM6001 (0, 1, 10, 25 μmol/L) was (25.70±2.06)μm/h, (18.37±1.61)μm/h, (16.20±0.26)μm/h, (15.99±0.58)μm/h, respectively, showing a significant difference among them ( F=11.39, P<0.05). There were significant differences in the migration rate between HUVECs treated with PSCs supernatants combined with 1, 10, 25 μmol/L GM6001 and HUVECs treated with PSCs supernatants ( P<0.05). The migration rate of HUVECs treated with mix super-natants of PSCs and PCCs combined with different concentration of GM6001 (0, 1, 10, 25 μmol/L) was (30.06±3.70)μm/h, (22.76±1.56)μm/h, (23.87±2.84)μm/h, (22.10±2.35)μm/h, respectively, showing a significant difference among them ( F=4.06, P<0.05). There were significant differences in the migration rate between HUVECs treated with mix supernatants of PSCs and PCCs combined with 1, 10, 25 μmol/L GM6001 and HUVECs treated with mix supernatants of PSCs and PCCs ( P<0.05). Conclusions:Both PSCs and PCCs can promote the proliferation, migration and angiogenesis of HUVECs in vitro experiment. Releasing of MMP-2 by interaction between PSCs and PCCs is an important factor to stimulate endothelial cell migration, which increases the stimulating activity of angiogenesis, especially the migration ability of HUVECs.

Study on the inhibition and remineralization of enamel demineralization by polydopamine in vitro / 口腔疾病防治

Objective@#To investigate the inhibitory effect of polydopamine (PDA) on enamel demineralization in isolated teeth and the induction of hydroxyapatite (HA) production on the surface of demineralized enamel to provide a novel protocol for the prevention and treatment of enamel demineralization. @*Methods@#Twenty isolated bovine teeth were cut into 20 enamel slices and randomly divided into an experimental group and a control group, with 10 slices in each group. The enamel slices in the experimental group were immersed in 2 mg/mL freshly prepared dopamine solution and incubated for 24 hours at room temperature in the dark to prepare the PDA coating, while the control group was left untreated. Then, the isolated bovine teeth, with and without PDA coating, were immersed in artificial demineralization solution at 37 °C for 3 days, followed by 7 days in simulated body fluid (SBF), and the immersion solution was changed daily. The surface morphology of enamel was observed by scanning electron microscopy (SEM), the calcium/phosphorus ratio of the enamel surface was analyzed by energy dispersive spectroscopy (EDS), and the characteristic functional groups in enamel deposits were analyzed by Fourier transform infrared spectroscopy (FTIR).@* Results@#Compared with the control group, the number of demineralized pores produced after 3 d of enamel demineralization with polydopamine coating was less, and the diameter was smaller. EDS elemental analysis showed that the Ca/P ratio after enamel demineralization was 2.37 in the experimental group, which was smaller than the 2.53 ratio in the control group. In the remineralization experiment, after 7 days of remineralization of PDA coated enamel in the experimental group, lamellar grains were produced on the enamel surface, and the growth showed obvious directionality, growth regularity and uniform arrangement. In the control group, the surface of enamel was flocculent mineral deposit, and the crystallinity was poor. The FTIR results proved that the enamel surface deposit of PDA-coated enamel was HA after 7 d of remineralization. @*Conclusion @#PDA can affect the nucleation process of HA and promote the production of HA on the surface of demineralized enamel.

The Positive Impact of Vitamin C (Ascorbic Acid) Utilisation in Cancer Treatment: A Scoping Review of Published Articles From the Perspective of the in Vitro Studies

@#Survival benefit of patients with advanced cancer was reported with intravenous vitamin C administration. Nevertheless, a recent systematic review failed to support the clinically use of vitamin C in cancer patients due to the diversity of interventions and cancer type. This study aimed to provide a scoping review of vitamin C utilisation and its impact on cancer treatment from the perspective of in vitro studies. The review was conducted using predefined search terms in three scientific databases. 44 articles were retrieved with a total of 15 cancer types being studied from 2015 to 2020. The findings were classified into primary and secondary outcome. The primary outcome refers to chief consequences of vitamin C treatment, while the secondary outcome denotes the additional advantages generated as a result of the primary outcome, which occurs both in monotherapy and combination therapy. This review discussed the major mechanism of vitamin C as anti-cancer and its relation with the outcomes.

Inhibitory effect of baicalin on Streptococcus mutans UA159 in vitro / 口腔疾病防治

Objective @# To investigate the inhibitory effect of baicalin on Streptococcus mutans UA159 in vitro.@*Methods @#The minimum inhibitory concentration (MIC) of baicalin on Streptococcus mutans UA159 was determined by the liquid multiple dilution method combined with the OD600 value measured by microplate. The OD600 value of Streptococcus mutans UA159 in different concentrations of baicalin was measured by an enzyme mapping instrument. A growth curve was drawn, and the adhesion rate and adhesion inhibition rate were calculated. The effect of baicalin on the formation of Streptococcus mutans UA159 biofilms was observed by the crystal violet quantitative method and scanning electron microscopy. The effect of baicalin on the total number of Streptococcus mutans UA159 bacteria was observed by scanning electron microscopy.@*Results@#The MIC of baicalin on Streptococcus mutans UA159 was 12 mg/mL. With increasing baicalin concentration, the growth rate of Streptococcus mutans UA159 was slowed, the adhesion rate of Streptococcus mutans UA159 decreased and the adhesion inhibition rate increased（P < 0.05）. The results of crystal violet quantitative method showed that compared with the bacterial control group, the biofilm formation of Streptococcus mutans UA159 was significantly reduced after adding baicalin at 0 h, 6 h and 12 h (P < 0.001). Under a scanning electron microscope, the total number of bacteria decreased significantly after adding baicalin at 0 h, 6 h and 12 h.@*Conclusion@# baicalin ; natural medicine ; Streptococcus mutans UA159 ; caries ; minimum inhibitory concentration ; growth curve ; adhesion rate ; adhesion inhibition rate ; biofilm formation ; in vitro study

Staphylococcus aureus growth delay after exposure to low fluencies of blue light (470 nm) / Atraso no crescimento de Staphylococcus aureus após exposição à baixas fluências de luz azul (470 nm)

Antibiotic resistance is one of the greatest challenges to treat bacterial infections worldwide, leading to increase in medical expenses, prolonged hospital stay and increased mortality. The use of blue light has been suggested as an innovative alternative to overcome this problem. In this study we analyzed the antibacterial effect of blue light using low emission parameters on Staphylococcus aureus cultures. In vitro bacterial cultures were used in two experimental approaches. The first approach included single or fractionated blue light application provided by LED emitters (470 nm), with the following fluencies: 16.29, 27.16 and 54.32 J/cm2. For the second approach a power LED (470 nm) was used to deliver 54.32 J/cm2 fractionated in 3 applications. Our results demonstrated that bacterial cultures exposed to fractionated blue light radiation exhibited significantly smaller sizes colonies than the control group after 24 h incubation, however the affected bacteria were able to adapt and continue to proliferate after prolonged incubation time. We could conclude that the hypothetical clinical use of low fluencies of blue light as an antibacterial treatment is risky, since its action is not definitive and proves to be ineffective at least for the strain used in this study.

A resistência a antibióticos é um dos maiores desafios para o tratamento de infecções bacterianas em todo o mundo, levando ao aumento de despesas médicas, prolongamento da internação hospitalar e aumento da mortalidade. O uso da luz azul tem sido sugerido como uma alternativa inovadora para superar esse problema. Neste estudo, analisamos o efeito antibacteriano da luz azul usando parâmetros de baixa emissão em culturas de Staphylococcus aureus. Culturas bacterianas foram usadas em duas abordagens experimentais in vitro. A primeira abordagem incluiu o uso da aplicação única ou fracionada de luz azul fornecida por emissores de LED (470 nm), com as seguintes fluências: 16,29, 27,16 e 54,32 J/cm2. Para a segunda abordagem, um LED de potência (470 nm) foi usado para fornecer 54,32 J/cm2 fracionado em 3 aplicações. Nossos resultados demonstraram que as culturas bacterianas expostas à radiação de luz azul fracionada exibiram colônias de tamanhos significativamente menores do que o grupo controle após 24 h de incubação, no entanto, as bactérias afetadas foram capazes de se adaptar e continuar a proliferar após um tempo prolongado de incubação. Podemos concluir que o uso clínico hipotético de baixas fluências de luz azul como tratamento antibacteriano é arriscado, pois sua ação não é definitiva e mostra-se ineficaz, pelo menos para a cepa utilizada neste estudo.

Microbiological Efficacy Of Meropenem–Ethylenediaminetetraacetic Acid Combination As Compared To Meropenem In A Tertiary Care Intensive Care Unit

Background: With the global epidemic of sepsis on the rising trend and gram negative sepsis being one of the most commoncause of increasing morbidity and mortality in developing nations like India, it becomes imperative to understand the role ofcombination antibiotics in controlling this burden. Aim and Methodology: In this study, we recognized the potential therapeuticrole of Meropenem combined with EDTA against a clinical endemic isolate of multi-drug resistant extended spectrum betalactamases (ESBLs) producing pathogens was investigated. The E-test strips studied the antimicrobial susceptibility of thepathogens and were applied to check for in-vitro sensitivity to Meropenem and combination of Meropenem and Ca-EDTA. Result:The MIC value of Meropenem-EDTA (0.25) was less than 50% of that of Meropenem (2.45) in sensitive isolates. Conclusion:Meropenem in unification with EDTA can exhibit more potent antimicrobial activity against ESBL producing pathogens thanjust Meropenem or EDTA alone.

In vitro fluoride release from five different fluoride varnishes / 대한구강보건학회지

OBJECTIVES: This study aims to compare the fluoride-release between different fluorine varnish under in vitro experimental conditions.METHODS: In this study, 5 fluoride varnish products distributed in Korea were selected. V-varnish™ (Vericom, Korea: VV), CavityShield™ (3M ESPE, USA: CS), Clinpro™ White varnish™ (3M ESPE, USA: CP), MI Varnish™ (GC, Japan: MI), and Fluor Protector (Ivoclar Vivadent, Liechtenstein: FP). For the in vitro study, 10 mg of each fluoride varnish was thinly applied to the same area of the specimen. The specimen was then immersed in 3 ml of distilled water at consistent intervals to confirm fluoride release. Nine specimens per group were used. Fluoride ion electrodes were used to measure the fluoride concentration of the solution. The Kruskal-Wallis nonparametric test was performed to compare between each experimental group, and the Wilcoxon signed-rank nonparametric test was performed to compare experimental groups over time. The significance level for a Type I error was set at 0.05. All statistical analyses were performed using SPSS 25.0 (IBM Co., Armonk, NY, USA).RESULTS: In vitro experiments showed that the amount of fluoride released from MI was higher than the other groups during the first 12 hours after application. However, the amount of fluoride released from CP and CS was higher than MI as the immersion time increased over 12 and 20 hours, respectively. The fluoride release from FP was the lowest at all measurement points.CONCLUSIONS: The results of this study showed that the remaining fluoride effect from rosin type fluoride varnishes was higher than liquid type fluoride varnishes. There were differences in the residual fluoride concentrations despite each fluoride varnish having the same fluoride content.

The role of carnosine on the oxidation reaction in vitro / 安徽医科大学学报

In this study, HRP or FeCl3were used as the catalysts in MTT, TMB and Mino reaction system, the effects of carnosine on the oxidation reaction were evaluated respectively. Indeed, carnosine was a pro-oxidant in luminol reaction, however an anti-oxidant in MTT assay. Once TMB was its substrate, carnosine was neutral in oxi-dation. Thus, it is supposed that the oxidative property of carnosine depends on the substrates.

Staphylococcus aureus growth delay after exposure to low fluencies of blue light (470 nm)

Abstract Antibiotic resistance is one of the greatest challenges to treat bacterial infections worldwide, leading to increase in medical expenses, prolonged hospital stay and increased mortality. The use of blue light has been suggested as an innovative alternative to overcome this problem. In this study we analyzed the antibacterial effect of blue light using low emission parameters on Staphylococcus aureus cultures. In vitro bacterial cultures were used in two experimental approaches. The first approach included single or fractionated blue light application provided by LED emitters (470 nm), with the following fluencies: 16.29, 27.16 and 54.32 J/cm2. For the second approach a power LED (470 nm) was used to deliver 54.32 J/cm2 fractionated in 3 applications. Our results demonstrated that bacterial cultures exposed to fractionated blue light radiation exhibited significantly smaller sizes colonies than the control group after 24 h incubation, however the affected bacteria were able to adapt and continue to proliferate after prolonged incubation time. We could conclude that the hypothetical clinical use of low fluencies of blue light as an antibacterial treatment is risky, since its action is not definitive and proves to be ineffective at least for the strain used in this study.

Resumo A resistência a antibióticos é um dos maiores desafios para o tratamento de infecções bacterianas em todo o mundo, levando ao aumento de despesas médicas, prolongamento da internação hospitalar e aumento da mortalidade. O uso da luz azul tem sido sugerido como uma alternativa inovadora para superar esse problema. Neste estudo, analisamos o efeito antibacteriano da luz azul usando parâmetros de baixa emissão em culturas de Staphylococcus aureus. Culturas bacterianas foram usadas em duas abordagens experimentais in vitro. A primeira abordagem incluiu o uso da aplicação única ou fracionada de luz azul fornecida por emissores de LED (470 nm), com as seguintes fluências: 16,29, 27,16 e 54,32 J/cm2. Para a segunda abordagem, um LED de potência (470 nm) foi usado para fornecer 54,32 J/cm2 fracionado em 3 aplicações. Nossos resultados demonstraram que as culturas bacterianas expostas à radiação de luz azul fracionada exibiram colônias de tamanhos significativamente menores do que o grupo controle após 24 h de incubação, no entanto, as bactérias afetadas foram capazes de se adaptar e continuar a proliferar após um tempo prolongado de incubação. Podemos concluir que o uso clínico hipotético de baixas fluências de luz azul como tratamento antibacteriano é arriscado, pois sua ação não é definitiva e mostra-se ineficaz, pelo menos para a cepa utilizada neste estudo.

Hydrolyzed collagen interferes with in vitro photoprotective effectiveness of sunscreens

ABSTRACT The chronological skin aging is a progressive and natural process with genetic and physiological changes. However, ultraviolet (UV) radiation may accelerate the oxidative stress, generating carcinogenesis and photoaging. Natural compounds and their applications are considered a trend in the cosmetic market. The protein-based film-forming compounds play an important role, once it collaborates for the better distribution of sunscreens on the skin. Here we investigated the in vitro photoprotective effectiveness of sunscreens containing the hydrolyzed collagen associated with UVA, UVB and/or inorganic filters. Sunscreens were developed with octocrylene (7.5%), butyl methoxydibenzoylmethane (avobenzone) (3.0%) and/or titanium dioxide (5.0%), associated or not with the hydrolyzed collagen (3.0%). In vitro photoprotective effectiveness was determined in a Labsphere(r) UV2000S by the establishment of the sun protection factor (SPF) and critical wavelength (nm) values. Physicochemical and organoleptic characteristics were also assayed. The hydrolyzed collagen subjectively improved the formulation sensory characteristics. However, this bioactive compound led to a decrease of the SPF values of the photoprotective formulations containing octocrylene alone and octocrylene + butyl methoxydibenzoylmethane + TiO2. This inadequate interaction may be considered during the development of new sunscreens intended to contain protein-based components.

Development of a new HPLC method for in vitro and in vivo studies of haloperidol in solid lipid nanoparticles

ABSTRACT A simple and sensitive HPLC method was developed and validated for the quantification of haloperidol in solid lipid nanoparticles (SLNs). The developed method was used for detection of shelf life of haloperidol in SLNs. Calibration curve of haloperidol was also constructed in rat plasma using loratidine as internal standard. In vivo studies were performed on rats and concentration of haloperidol in brain and blood was measured for the determination of various pharmacokinetic and hence brain targeting parameters. Chromatogram separation was achieved using C18 column as stationary phase. The mobile phase consisted of 100 mM/L potassium dihydrogen phosphate-acetonitrile-TEA (10:90:0.1, v/v/v) and the pH was adjusted with o-phosphoric acid to 3.5. Flow rate of mobile phase was 2 mL/minute and eluents were monitored at 230 nm using UV/VIS detector. The method was validated for linearity, precision, accuracy, reproducibility, limit of detection (LOD) and limit of quantification (LOQ). Linearity for haloperidol was in the range of 1-16 µg/mL. The value of LOD and LOQ was found to be 0.045 and 0.135 μg/mL respectively. The shelf life of SLNs formulation was found to be 2.31 years at 4 oC. Various parameters like drug targeting index (DTI), drug targeting efficiency (DTE) and nose-to-brain direct transport (DTP) were determined for HP-SLNs & HP-Sol administered intranasally to evaluate the extent of nose-to-brain delivery. The value of DTI, DTE and DTP for HP-SLNs was found to be 23.62, 2362.43 % and 95.77% while for HP-Sol, values were 11.28, 1128.61 % and 91.14 % respectively.

In vitro study of the effect of an essential oil and a delmopinol mouth rinse on dental plaque bacteria.

Context: Mouthrinses are used, by many of our patients, as a complement to daily dental hygiene routine. The use of a toothbrush and an interproximal cleaning method may not be enough to control dental plaque. Essential oils and delmopinol mouth rinses are effective for the prevention of dental caries and gingivitis. To study the effect of an essential oil and a delmopinol mouth rinse on dental plaque bacteria, an in vitro study was developed. Aims: The objective of this study was to determine the antibacterial activity of an essential oil and a delmopinol mouth rinse on Streptococcus mutans, Lactobacilli, and aerobic and anaerobic dental plaque nonspecific bacteria. Design: Samples of human dental plaque were collected from consenting participants and bacteria isolated. Disk‑diffusion tests were performed to obtain the minimum concentration of the mouth rinses necessary to inhibit bacterial growth. The ability of the commercial mouth rinses to inhibit bacterial growth was studied in comparison to a positive control (0.2% chlorhexidine) and a negative laboratorial control (sterilized water). Results: The minimum inhibitory concentration was found to be inferior to the commercial essential oils and delmopinol mouth rinses concentrations. Delmopinol and essential oils have significant antibacterial properties shown in vitro only for aerobic bacteria, and for S. mutans, Lactobacillus, and anaerobic bacteria, the results were not statistically significant. Conclusions: Essential oils and chlorhexidine are statistically similar and better than delmopinol for aerobic bacteria growth inhibition. For the other bacteria, essential oils and delmopinol are not statistically promising. Results show that essential oils only may help patients to maintain good oral health as a complement to daily brushing and interproximal cleaning.

Comparative antioxidant and bioavailability studies of Vitamin C in Phyllanthus emblica Linn. and its combinations with Piper nigrum Linn. and Zingiber officinale Roscoe

ABSTRACT Phyllanthus emblica Linn. (amla) is used in Ayurveda, the ancient Indian system of medicine and its major constituent is vitamin C which has effective free radical scavenging property. The purpose of this study was to evaluate the in vitro antioxidant activity and the bioavailability profile of vitamin C in amla and its combinations with piperine and ginger in comparison to synthetic vitamin C using New Zealand rabbits. In vitro antioxidant activity studies of synthetic vitamin C, amla, amla with piperine and amla with ginger were carried out using different models such as 2,2-Diphenyl-1-picrylhydrazyl, Nitric Oxide, Hydrogen peroxide scavenging methods, Total reductive capability and Oxygen Radical Absorbance Capacity estimation. The study results showed that synthetic vitamin C, amla, amla with piperine and amla with ginger possess significant in vitro antioxidant activity. For bioavailability studies, synthetic vitamin C, amla, amla with piperine and amla with ginger 100 mg/kg, were administered orally and the serum samples were analyzed by HPLC at 0, 1, 2, 3, 4, 6, 8, 10, 12 and 24 hours. Bioavailability studies revealed that amla with piperine combination has higher concentration of vitamin C when compared to synthetic vitamin C. This is probably due to presence of piperine, which is a bioavailability enhancer. The present study supports the fact that amla with piperine combination can be an alternative to synthetic vitamin C.

RESUMO Phyllanthus emblica Linn. (amla) é utilizada na medicina Ayurveda, medicina da Índia antiga e seu principal constituinte é a vitamina C, que possui propriedade sequestrante de radicais livres. O propósito deste estudo foi avaliar a atividade antioxidante in vitro e o perfil de biodisponibilidade da vitamina C na amla e suas combinações com piperina e gengibre em comparação com a vitamina C sintética, utilizando coelhos da Nova Zelândia. Os estudos de atividade antioxidante in vitro de vitamina C sintética, amla, amla com piperina e amla com gengibre foram realizados utilizando-se diferentes modelos para sequestrantes, como 2,2-difenil-1-picrilidrazil, óxido nítrico, peróxido de hidrogênio, capacidade redutiva total e a estimativa da capacidade de absorvância do radical oxigênio. Os resultados do estudo mostraram que vitamina C sintética, amla, amla com piperina e amla com gengibre possuem atividade antioxidante in vitro significativa. Para os estudos de biodisponibilidade, administraram-se oralmente vitamina C sintética, amla, amla com piperina e amla com gengibre 100 mg/kg e as amostras de soro foram analisadas por CLAE em 0, 1, 2, 3, 4, 6, 8, 10, 12 e 24 horas. Os estudos de biodisponibilidade revelaram que a associação de amla com piperina tem maior concentração de vitamina C, quando comparada com a vitamina C sintética. Este efeito é provavelmente devido à presença de piperina, que é intensificador de biodisponibilidade. O presente estudo apoia o fato de que a associação de amla e piperina pode ser uma alternativa para a vitamina C sintética.

Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

ABSTRACT Transdermal nicotine patches have been used in smoking cessation therapy, suggested for the treatment of skin disorders with eosinophilic infiltration and have been found to improve attention performance in patients with Alzheimer's disease and age-associated memory impairment. However, skin irritation with extended patch use is still a problem. The aim of this work was to develop a simple to prepare liquid crystalline system containing vitamin E TPGS that would be able to control nicotine delivery and reduce irritation and sensitization problems. The liquid crystalline phases were macroscopically characterized by visual analysis and examined microscopically under a polarized light microscope. Topical and transdermal delivery of nicotine were investigated in vitro using porcine ear skin mounted on a Franz diffusion cell. Nicotine skin permeation from the developed cubic phase followed zero-order kinetics (r = 0.993) and was significantly enhanced after 12 h when compared to the control formulation (nicotine solution) (p < 0.05) (138.86 ± 20.44 and 64.91 ± 4.06 μg/cm2, respectively). Cubic phase was also able to target viable skin layers in comparison to control solution (8.18 ± 1.89 and 2.63 ± 2.51 μg/cm2, respectively). Further studies to evaluate skin sensitization and irritation are now necessary.

RESUMO Adesivos transdérmicos de nicotina são utilizados para cessação de fumar, tratamento de problemas de pele com infiltração de eosinófilos e para melhorar a atenção em pacientes com doença de Alzheimer e enfraquecimento da memória associada à idade. No entanto, a irritação da pele com o uso prolongado dos adesivos ainda é um problema. O objetivo deste trabalho foi desenvolver sistema líquido cristalino (SLC) de preparo simples contendo vitamina E TPGS capaz de controlar a liberação de nicotina e reduzir os problemas de irritação cutânea. Os SLCs foram caracterizados por análise visual e microscopia de luz polarizada. As administrações tópica e transdérmica de nicotina foram investigadas in vitro utilizando pele de orelha de porco em célula de difusão de Franz. A permeação da nicotina veiculada pela fase cúbica desenvolvida seguiu cinética de ordem zero (r = 0,993) e foi significativamente maior do que o controle (solução de nicotina) após 12 h (p < 0,05) (138,86 ± 20,44 e 64,91 ± 4,06 µg/cm2, respectivamente). A fase cúbica também promoveu aumento da penetração de nicotina nas camadas viáveis da pele quando comparado ao controle (8,18 ± 1,89 e 2,63 ± 2,51 µg/cm2, respectivamente). Estudos futuros para avaliar a sensibilização e irritação da pele são necessários.

Phytoconstituents from Sidastrum micranthum (A. St.-Hil.) Fryxell (Malvaceae) and antimicrobial activity of pheophytin a

abstract Sidastrum micranthum (A. St.-Hil.) Fryxell, a member of the Malvaceae family, is called malva preta in Brazil. As this species is commonly used to treat bronchitis, cough, and asthma, better knowledge of its chemical compounds is important. The phytochemical study of its hexane extract, using chromatographic techniques, led to isolation of six compounds: the triterpene isoarborinol, a mixture of sitosterol and stigmasterol, sitosterol-3-O-β-D-glucopyranoside, pheophytin a, and 132-hydroxy-(132-S)-pheophytin a. Structural identification of these compounds was carried out using spectroscopic methods such as IR and 1D and 2D NMR (HOMOCOSY, HMQC, HMBC, and NOESY). Compounds isolated from S. micranthum were screened for their in vitro antifungal and antibacterial activity against twenty fungal and bacterial standard strains. Pheophytin a exhibited antimicrobial action against all microorganisms tested.

resumo Sidastrum micranthum (A. St.-Hil.) Fryxell, pertencente à família Malvaceae, é conhecida no Brasil como "malva preta". A espécie é popularmente usada contra bronquite, tosse e asma, mostrando a relevância de conhecer melhor sua composição química. O estudo fitoquímico do extrato hexânico da espécie, utilizando técnicas cromatográficas, conduziu ao isolamento de seis compostos: o triterpeno isoarborinol, mistura de sitosterol e estigmasterol, sitosterol-3-O-β-D-glicopiranosídeo, feofitina a e de 132-hidroxi-(132-S)-feofitina a. A identificação estrutural destes compostos foi realizada com base em métodos espectroscópicos, tais como IV, RMN 1D e 2D (HOMOCOSY, HMQC, HMBC e NOESY). As substâncias isoladas de Sidastrum micranthum foram avaliadas quanto às suas atividades antimicrobianas in vitro, contra vinte cepas fúngicas e bacterianas. A feofitina a mostrou ação antimicrobiana contra todos os microrganismos testados.

Formulation of gastroresistant tablets containing sodium alendronate-loaded blend microparticles / Formulação de comprimidos gastro-resistentes que contêm na mistura micropartículas carregadas de alendronato de sódio

Sodium alendronate is an antiresorptive drug used for the treatment of postmenopausal osteoporosis. However, its oral administration is associated with low bioavailability and gastroesophageal irritation. This work aimed at developing tablets containing sodium alendronate-loaded microparticles by direct compression to achieve a safe and effective form. The parameters evaluated were average weight, hardness, thickness and drug content. In vitro release tests were carried out using simulated gastric and intestinal fluids, and the profiles were analyzed through the Korsmeyer-Peppas mono- or biexponential dependent approaches. Tablets presented adequate average weight, thickness, good mechanical properties and drug content close to 100%. Moreover, the formulation released less than 11% of sodium alendronate in gastric fluid, exhibiting a good gastroresistance. At pH 6.8, almost 100% of the drug was released in 12h, showing a prolonged profile. The mathematical modeling indicated that the experimental data was better fitted to the biexponential equation. Furthermore, a good correlation coefficient was obtained for the Korsmeyer-Peppas model and the release exponent suggested that the drug dissolution was driven by anomalous transport. In conclusion, the microparticulated tablets can be considered a promising alternative for oral delivery of sodium alendronate...

O alendronato de sódio é um fármaco da classe dos bisfosfonatos, comumente utilizado no tratamento da osteoporose pós-menopausa. Entretanto, sua administração oral está associada à baixa biodisponibilidade e irritação gastroesofágica. Este trabalho objetivou o desenvolvimento de comprimidos contendo micropartículas de alendronato de sódio por compressão direta, a fim de obter uma forma segura e eficaz. Os parâmetros avaliados foram peso médio, dureza, espessura e teor de fármaco. Estudos de liberação in vitro foram realizados utilizando fluído gástrico e intestinal simulado e o perfil de liberação foi analisado pelos modelos matemáticos de Korsmeyer-Peppas, mono- e biexponencial. Os comprimidos apresentaram peso médio adequado, espessura, dureza e teor próximo a 100%. Além disso, a formulação liberou menos de 11% do fármaco em fluído gástrico, mostrando uma boa gastrorresistência. Em pH 6,8, em torno de 100% do fármaco foram liberados em 12 h, apresentando liberação prolongada. A modelagem matemática indica que os resultados seguem a equação biexponencial. Pela análise do expoente de liberação obtido no modelo de Korsmeyer-Peppas sugere-se que a dissolução do fármaco ocorre por transporte anômalo. Concluindo, a preparação dos comprimidos microparticulados pode ser considerada uma alternativa promissora para a liberação oral do alendronato de sódio...

Inhibitory effect of recombinant human interferon α-2b on influenza virus / 中华临床感染病杂志

Objective To investigate the effect of recombinant human interferon α-2b on influenza virus in vitro.Methods Influenza A virus subtype H1N1 and influenza B/Y virus were inoculated into Vero cells and different concentrations of interferon α-2b and oseltamivir were added.Numbers of virus plaques were observed and calculated,and quantitative RT-PCR were used to assess the inhibitory effect of interferon α-2b and oseltamivir in vitro.The nuclear export of viral ribonucleoprotein (RNP) complexes were monitored under fluorescence microscope.Results Virus plaque test showed that influenza A viruses subtype H1N1 were significantly inhibited when 10 μg/μL interferon α-2b and 10 μg/μL oseltamivir were added,and the numbers of plaques were 7.5 × 108 and 15 × 108 PFU/mL,respectively;the inhibitory effect of oseltamivir was better than that of interferon α-2b.Influenza B/Y viruses were also inhibited when 10 μg/μL interferon α-2b and 10 μg/μL oseltamivir were added,and the numbers of plaques were 1.1 × 108 and 1.5 × 108 PFU/mL,respectively.Quantitative RT-PCR results showed that the cycle threshold (CT) values of influenza A virus subtype H1N1 and influenza B/Y virus were much higher when 10 μmol/L interferon α-2b and 10 μmol/L oseltamivir were added.CT values of influenza A virus subtype H1N1 were 16,26 and 35 before and after inferferon α-2b and oseltamivir were added.CT values of influenza B/Y virus were 18,27 and 31 before and after interferon α-2b and oseltamivir were added.Reduction in the nuclear export of viral RNP in influenza A virus subtype H1N1-infected Vero cells was also observed when 10 μmol/L interferon α-2b were added.Conclusion Interferon α-2b has significantly inhibitory effect on both influenza A virus subtype H1N1 and influenza B/Y virus in vitro.

Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

Tretinoin is used in the management of acne and it is part of a gold standard treatment for photoaging. It has also been reported as an agent for superficial chemical peeling in highly concentrated formulations with few considerations about skin penetration. The aim of this study was to evaluate the influence of drug concentration and vehicles currently used on skin penetration of tretinoin. In vitro permeation tests were carried out using Franz diffusion cells fitted with porcine ear skin and 10% aqueous methanol in the receptor compartment. Formulations studied, cream or hydroalcoholic dispersion, containing 0.25%, 1% and 5% of tretinoin were placed in the donor compartment for six hours. Tretinoin concentration in skin layers was measured by high performance liquid chromatography. The largest amount of tretinoin from both vehicles was detected in stratum corneum with significant differences among the three concentrations. The hydroalcoholic dispersion was the best vehicle. Significant amounts of tretinoin were found even in deep layers of epidermis. The formulation with 0.25% tretinoin showed better results when considered the amount of tretinoin on skin in terms of percentage. Finally, skin penetration of tretinoin was influenced by vehicle and concentration of this drug used in formulation.

A tretinoína é usada no tratamento de acne e é considerada como padrão de ouro para o tratamento do fotoenvelhecimento. Em altas concentrações, é relatada como um agente para peeling químico superficial, com poucas considerações sobre a penetração na pele. O objetivo deste estudo foi avaliar a influência da concentração do fármaco e os veículos comumente usados na penetração cutânea da tretinoína. Testes in vitro de penetração foram realizados com células de difusão de Franz equipados com pele da orelha de porco e 10% de solução aquosa de metanol no compartimento receptor. As formulações estudadas, creme ou dispersão hidroalcoólica, contendo 0,25%, 1% e 5% de tretinoína foram colocadas no compartimento doador, durante seis horas. A concentração da tretinoína foi medida por cromatografia líquida de alta eficiência. A maior quantidade de tretinoína foi detectada no estrato córneo com diferenças significativas entre as três concentrações. A dispersão hidroalcoólica foi o melhor veículo. Quantidades significativas de tretinoína foram encontradas nas camadas profundas da epiderme. A formulação com 0,25% de tretinoína mostrou melhores resultados em termos de porcentagem penetrada na pele. Por fim, a penetração de tretinoína na pele foi influenciada pelo veículo e pela concentração desta utilizada na formulação.

Benzydamine Oral Spray Inhibiting Parasympathetic Function of Tracheal Smooth Muscle

OBJECTIVES: Benzydamine is a nonsteroidal anti-inflammatory agents agent with anti-inflammatory and local anesthesia properties that is available in the entire world as an oral spray for oral mucositis patients who are suffering from radiation effects. The effect of benzydamine on oral mucositis in vivo is well known; however, the effect of the drug on tracheal smooth muscle has rarely been explored. During administration of the benzydamine for oral symptoms, it might affect the trachea via oral intake or inhalation. METHODS: We examined the effectiveness of benzydamine on isolated rat tracheal smooth muscle. The following assessments of benzydamine were performed: effect on tracheal smooth muscle resting tension; effect on contraction caused by 10(-6)M methacholine as a parasympathetic mimetic; and effect of the drug on electrically induced tracheal smooth muscle contractions. RESULTS: Addition of methacholine to the incubation medium caused the trachea to contract in a dose-dependent manner. Addition of benzydamine at doses of 10(-5)M or above elicited a significant relaxation response to 10(-6)M methacholine-induced contraction. Benzydamine could inhibit electrical field stimulation-induced spike contraction. It alone had a minimal effect on the basal tension of trachea as the concentration increased. CONCLUSION: This study indicated that high concentrations of benzydamine might actually inhibit parasympathetic function of the trachea. Benzydamine might reduce asthma attacks in oral mucositis patients because it could inhibit parasympathetic function and reduce methacholine-induced contraction of tracheal smooth muscle.