Estudio comparativo de la actividad anti-fúngica de extractos secuenciales de Fuchsia lycioides contra Candida sp / comparative study of the antifungal activity of sequencial extracts of Fuchsia lycioides against Candida sp

The genus Fuchsia is generally used in herbal preparations to treat conditions caused by microorganisms. Based on the popular use of this type of plants, the objective of this study was to obtain sequential extracts of increasing polarity from the branches of Fuchsia lycioides by maceration at room temperature and by the Soxhlet method at 60ºC, to later evaluate the antifungal capacity of the extracts against different clinical isolates of the Candida genus. The ethyl acetate extract exhibited strong anti-fungal activity, selectively inhibiting C. albicans strains with MIC and CMF values of 10 and 15 µg/mL, respectively; comparable with the drug itraconazole®. The analysis of the extract by GC-MS showed a high concentration of terpenoids (mainly phytol) and phenylpropanoids (mainly cinnamic acid), possibly responsible for the antifungal activity of the ethyl acetate extract of F. lycioides.

El género Fuchsia se usa generalmente en preparaciones de hierbas para tratar afecciones provocadas por microorganismos. En base al uso popular de este tipo de plantas, el objetivo de este estudio fue obtener los extractos secuenciales de polaridad creciente de las ramas de Fuchsia lycioides por maceración a temperatura ambiente y por el método Soxhlet a 60ºC, para luego evaluar la capacidad antifúngica de los extractos frente a diferentes aislados clínicos del genero Candida. El extracto de acetato de etilo exhibió una fuerte actividad antifúngica inhibiendo en forma selectiva las cepas de C. albicans con valores de CMI y de CMF de 10 y 15 µg/mL, respectivamente; comparables con el fármaco itraconazol®. El análisis del extracto por CG-EM mostró una alta concentración de terpenoides (principalmente fitol) y fenilpropanoides (principalmente ácido cinámico), posibles responsables de la actividad antifúngica del extracto de acetato de etilo de F. lycioides.

Gamma-oryzanol reduces renal inflammation and oxidative stress by modulating AGEs/RAGE axis in animals submitted to high sugar-fat diet / Gama-orizanol reduz a inflamação e o estresse oxidativo nos rins pela modulação do eixo RAGE/AGEs em animais submetidos a uma dieta rica em gordura e açúcar

Abstract Introduction: The receptor for AGEs (RAGE) is a multiligand member of the immunoglobulin superfamily of cell surface receptors expressed in many organs, among them, the kidneys. When activated, RAGE leads to a sequence of signaling that results in inflammation and oxidative stress, both involved in kidney disease pathogenesis. Gamma-oryzanol (γOz) comprises a mixture of ferulic acid (FA) esters and phytosterols (sterols and triterpene alcohols) mainly found in rice, with antioxidant and anti-inflammatory activities. Aim: To evaluate the effect of γOz to reduce renal inflammation and oxidative stress by modulating AGEs/RAGE axis in animals submitted to a high sugar-fat diet. Methods: Male Wistar rats (±187g) were randomly divided into two experimental groups: control (n = 7 animals) and high sugar-fat diet (HSF, n = 14 animals) for 20 weeks. After this period, when the presence of renal disease risk factors was detected in the HSF group (insulin resistance, dyslipidemia, increased systolic blood pressure and obesity), the HSF animals were divided to begin the treatment with γOz or continue receiving only HSF for 10 more weeks. Results: No effect of γOz on obesity and metabolic parameters was observed. However, kidney inflammation and oxidative stress decreased as soon as RAGE levels were reduced in HSF + γOz. Conclusion: It is possible to conclude that the gamma- oryzanol was effective in reducing inflammation and oxidative stress in the kidney by modulating the AGEs/RAGE axis.

Resumo Introdução: O receptor para AGEs (RAGE) é um membro multiligante da superfamília das imunoglobulinas dos receptores de superfície celular expresso em muitos órgãos, entre eles, os rins. Quando ativado, o RAGE leva a uma sequência de sinalização que resulta em inflamação e estresse oxidativo, ambos envolvidos na patogênese de doenças renais. O gama-orizanol (γOz) compreende uma mistura de ésteres de ácido ferúlico (AF) e fitoesteróis (esteróis e álcoois triterpenos) encontrados principalmente no arroz, com atividades antioxidantes e anti-inflamatórias. Objetivo: Avaliar o efeito do γOz para reduzir a inflamação renal e o estresse oxidativo pela modulação do eixo RAGE/AGEs em animais submetidos a uma dieta rica em gordura e açúcar. Métodos: Ratos Wistar machos (±187g) foram divididos aleatoriamente em dois grupos experimentais: controle (n = 7 animais) e dieta rica em gordura e açúcar (HSF, do inglês high sugar-fat diet, n = 14 animais) por 20 semanas. Após este período, quando foi detectada a presença de fatores de risco de doença renal no grupo HSF (resistência à insulina, dislipidemia, aumento da pressão arterial sistólica e obesidade), os animais HSF foram divididos para iniciar o tratamento com γOz ou continuar recebendo apenas HSF por mais 10 semanas. Resultados: Não foi observado nenhum efeito do γOz na obesidade e nos parâmetros metabólicos. No entanto, a inflamação e o estresse oxidativo renais diminuíram assim que os níveis de RAGE foram reduzidos em HSF + γOz. Conclusão: É possível concluir que o gama- orizanol foi eficaz em reduzir a inflamação e o estresse oxidativo no rim pela modulação do eixo RAGE/AGEs.

Uso de treprostinil sistémico en una paciente con hipertensión pulmonar grave, sin respuesta a la máxima terapia disponible / Use of treprostinil in a patient with a severe pulmonary arterial hypertension no responding to the maximal therapy available

En los pacientes con Hipertensión Arterial Pulmonar (HAP) de alto riesgo, en clase funcional (CF)IV, la terapia específica debe ser combinada y debe incluir una prostaciclina (PGI2) de uso sistémico en espera de trasplante bipulmonar (TBP). En el sistema público la única PGI2 disponible para asociar a Sildenafil y algún inhibidor de endotelina (Ambrisentan o Bosentan) es Iloprost nebulizado, que si bien es efectiva, no logra estabilizar los casos graves con severa disfunción del ventrículo derecho (VD). Se presenta el primer caso en el Instituto del Tórax, centro de referencia nacional de HAP, del uso de treprostinil en una paciente de 24 años con HAP grave e indicación de TBP. Treprostinil es un análogo sintético de PGI2 de uso subcutáneo en dosis desde 1 a 40 ng/kg/min. La paciente presentaba una situación de extrema gravedad: CF IV, distancia recorrida en el test de caminata de 6 min (DRTC 6 min) < 300 m,derrame pericárdico y severa disfunción del VD con TAPSE (índice de disfunción del VD) de 13 cm/s asociado a ProBNP >2.500 pg/ml. Luego de 6 meses de hospitalización en intermedio, terapia triple (Sildenafil, Ambrisentan e Iloprost nebulizado) asociado a O2,diuréticos y milrinona, logró ser dada de alta a las 3 semanas del inicio de treprostinil, regresando al trabajo a los 2 meses y estabilizando su condición en CF III, con DRTC 6 min > 440 m, mejoría de la función del VD(TAPSE 19). El ProBNP persistió elevado, 1.491 pg/ml, indicando que su enfermedad es grave y progresiva; sin embargo, ha logrado un nivel de estabilidad clínica que le permite una adecuada vida de relación familiar y laboral.

In high risk Pulmonary Arterial Hypertension (PAH) patients with functional class (FC) IV, specific therapy must be combined and must include systemic prostacyclin (PGI2), meanwhile they are enlisted for double lung transplant (DLT). In Chilean Public Health System, nebulized Iloprost is the only PGI2 available to combine with Sildenafil and either Ambrisentan or Bosentan as endothelin receptor antagonist. This association is not enough for severe cases with right ventricular (RV) dysfunction. The first case from the National Institute of Thorax as a referral center is presented now in a 24 years-old lady treated with treprostinil. She has severe PAH with DLT indication. Treprostinil is a PGI2 analog, for subcutaneous use in a dose from 1 to 40 ng/kg/min. She was extremely sick, with FC IV, she walked < 300 m at 6 min walking test (6 MWT), presented pericardial effusion and severe RV dysfunction, with TAPSE (echocardiography index for RV dysfunction)=13 cm/s, ProBNP > 2,500 pg/ml. Six months after being at intensive care unit with triple therapy (Sildenafil, ambrisentan and nebulized Iloprost) plus oxygen, diuretics and milrinone, she was finally discharged after receiving a 3 weeks treprostinil course. She came back to work two months later and her condition was more stable: FC III, she walked > 440 m at 6MWT, with a significant improvement in RV function with TAPSE = 19. Although ProBNP decreased to 1,491pg/ml, it was still high, pointing out the progressive nature of her disease. However, she met a better clinical condition which allows her to reach a much better quality of life from a personal, familial and social point of view.

Effects of artepillin C on model membranes displaying liquid immiscibility

It has been hypothesized that the therapeutic effects of artepillin C, a natural compound derived from Brazilian green propolis, are likely related to its partition in the lipid bilayer component of biological membranes. To test this hypothesis, we investigated the effects of the major compound of green propolis, artepillin C, on model membranes (small and giant unilamelar vesicles) composed of ternary lipid mixtures containing cholesterol, which display liquid-ordered (lo) and liquid-disordered (ld) phase coexistence. Specifically, we explored potential changes in relevant membrane parameters upon addition of artepillin C presenting both neutral and deprotonated states by means of small angle X-ray scattering (SAXS), differential scanning calorimetry (DSC), and confocal and multiphoton excitation fluorescence microscopy. Thermotropic analysis obtained from DSC experiments indicated a loss in the lipid cooperativity of lo phase at equilibrium conditions, while at similar conditions spontaneous formation of unilamellar vesicles from SAXS experiments showed that deprotonated artepillin C preferentially located at the surface of the membrane. Time-resolved experiments using fluorescence microscopy showed that at doses above 100 µM, artepillin C in its neutral state interacted with both liquid-ordered and liquid-disordered phases, inducing curvature stress and promoting dehydration at the membrane interface.

Preemptive analgesia with loxoprofen sodiumorally in extraction of impacted teeth / 北京大学学报(医学版)

OBJECTIVE@#To investigate the effectiveness of preemptive analgesia with loxoprofen sodium orally, which was a kind of non-steroid anti-inflammatory drugs, in extractions of mandibular impacted third teeth.@*METHODS@#There were questionnaires about postoperative pain for patients whose mandibular impacted third teeth were extracted from July 2017 to August 2017 in First Clinical Division of Peking University School and Hospital of Stomatology. All the patients did their routine clinical examinations and imaging examinations. After their mandibular impacted third teeth were extracted, the questionnaires were sent to them. The questionnaires were filled in by the patients on their own and returned one week later. There were 120 questionnaires that were sent and 105 questionnaires returned, of which 98 questionnaires were filled in completely. According to the inclusive criteria and exclusion criteria, 66 questionnaires were totally selected in this study. According to the time when the patients took their loxoprofen sodium orally firstly, the patients were divided into 3 groups. The first group was for patients who didn't take loxoprofen sodium during their extractions (non-medicine group). The second group was for patients who took 60 mg loxoprofen sodium 30 min before their extractions (preoperative group). The third group was for patients who took 60 mg loxoprofen sodium 30 min after their extractions (postoperative group). The operation time among the 3 groups was analyzed by Kruskal-Wallis method. The postoperative time points were 2, 4, 12,24 and 48 h after operation. The scores of visual analogue scales (VAS) for postoperative pain in each group at different postoperative time points were analyzed by Friedman method. At each postoperative time point, VAS scores in the different groups were analyzed by Kruskal-Wallis me-thod. The numbers of the patients taking loxoprofen sodium home and drug adverse reactions were also analyzed.@*RESULTS@#The operation time of the 3 groups was 15.0 (5.0,30.0) min and had no significant differences (P=0.848).VAS scores of non-medicine group 2,4, 12,24 and 48 h after operation were 1.75 (0.1,10.0), 6.25 (1.5,10.0), 2.00 (0.1,8.0), 2.00 (0.1,6.0) and 0.5 (0.1,5.5) separately and had significant differences (P<0.001).The VAS score at 4 h after operation was higher than the VAS scores at other time points after operation (P<0.005). Four hours after the operations, the VAS scores of preoperative group [2.0 (0.1,10.0)] and postoperative group [2.0 (0.1,5.0)] were lower significantly than those of non-medicine group [6.25 (1.5,10.0)] (P<0.001).The numbers of the patients taking loxoprofen sodium home were 9(40.9%) in non-medicine group,5(21.8%) in preoperative group and 7(33.3%) in postoperative group. The number of the patients who had drug adverse reactions in preoperative group (n=3,13.0%) and in postoperative group (n=4,19.0%) was less than the number of the patients who had drug adverse reactions in non-medicine group (n=8,36.4%).@*CONCLUSION@#There were two protocols of preemptive analgesia with loxoprofen sodium orally in extractions of mandibular impacted third teeth, which were taking 60 mg loxoprofen sodium orally 30 min before the extractions and taking 60 mg loxoprofen sodium orally 30 min after the extractions. Both of the two preemptive analgesia protocols could decrease the postoperative pain significantly.

HPPR encodes the hydroxyphenylpyruvate reductase required for the biosynthesis of hydrophilic phenolic acids in Salvia miltiorrhiza / 中国天然药物

Salvia miltiorrhiza is a medicinal plant widely used in the treatment of cardiovascular and cerebrovascular diseases. Hydrophilic phenolic acids, including rosmarinic acid (RA) and lithospermic acid B (LAB), are its primary medicinal ingredients. However, the biosynthetic pathway of RA and LAB in S. miltiorrhiza is still poorly understood. In the present study, we accomplished the isolation and characterization of a novel S. miltiorrhiza Hydroxyphenylpyruvate reductase (HPPR) gene, SmHPPR, which plays an important role in the biosynthesis of RA. SmHPPR contained a putative catalytic domain and a NAD(P)H-binding motif. The recombinant SmHPPR enzyme exhibited high HPPR activity, converting 4-hydroxyphenylpyruvic acid (pHPP) to 4-hydroxyphenyllactic acid (pHPL), and exhibited the highest affinity for substrate 4-hydroxyphenylpyruvate. SmHPPR expression could be induced by various treatments, including SA, GA, MeJA and Ag, and the changes in SmHPPR activity were correlated well with hydrophilic phenolic acid accumulation. SmHPPR was localized in cytoplasm, most likely close to the cytosolic NADPH-dependent hydroxypyruvate reductase active in photorespiration. In addition, the transgenic S. miltiorrhiza hairy roots overexpressing SmHPPR exhibited up to 10-fold increases in the products of hydrophilic phenolic acid pathway. In conclusion, our findings provide a new insight into the synthesis of active pharmaceutical compounds at molecular level.

Variabilidad de la composición química del aceite esencial de nectandra megapotamica (spreng. ) mez (lauraceae) / Variability of chemical composition of essential oil from nectandra megapotamica (spreng. ) mez (lauraceae)

Este trabajo describe la variabilidad química del aceite esencial (AE) de N. megapotamica, utilizando análisis multivariado. Se colectaron hojas de tres individuos en una población en Santa Maria, Brasil, en cada estación durante un año y se clasificaron en hojas jóvenes y viejas. Los AE se obtuvieron por hidrodestilación y la composición química fue determinada por cromatografía de gases acoplada a espectrometría de masas. Se realizó un análisis de agrupamiento jerárquico para formación de grupos químicos (GQ) y análisis de componentes principales (ACP) para verificar cuáles constituyentes influenciaron la formación de grupos. Inicialmente se observaron dos agrupamientos en el dendrograma debido a concentraciones de α-pineno y biciclogermacreno, constituyentes mayoritarios. En el segundo corte se discriminaron cinco GQ, siendo este también el número de componentes principales con valores propios superiores a 1. Los isómeros de asarona se observaron solamente en el AE de dos individuos (GQ5), constituyendo los principales elementos de diferenciación.

This work describes the chemical variability of the essential oils (EO) of N. megapotamica using multivariate analysis. Leaves of three individuals of a population in Santa Maria-RS were collected per season for a year, and classified into young and old. The EO were obtained by hydrodistillation and the chemical composition was determined by gas chromatography coupled to mass spectrometry (GC/MS). Cluster analysis (HCA) were performed for formation of chemical groups (CG), and principal component analysis was done (PCA) to determine which constituents influenced the formation of groups. Initially, two clusters were observed in the dendrogram, due to the concentration of α-pinene and bicyclogermacrene, major constituents of the EO. The second section showed five different CG, which is also the number of principal components with eigenvalues greater than 1. The occurrence of isomers of asarone was observed only in EO of two individuals (CG5), containing the main elements of differentiation.

Senile insomnia treated with integrated acupuncture and medication therapy: a randomized controlled trial / 中国针灸

<p><b>OBJECTIVE</b>To compare the efficacy difference in the treatment of senile insomnia among western, medication, acupuncture and the integrated therapy of acupuncture and western medication.</p><p><b>METHODS</b>Ninety-eight patients of senile insomnia were randomized into a western medication group (30 cases), an acupuncture group (35 cases) and an integrated acupuncture and medication group (35 cases). In the western medication group, estazolam 1mg was prescribed, taken 30 min before going to bed, oryzanol 20 mg, oral administration, three times a day, for 4 weeks totally. In the acupuncture group, the simple acupuncture therapy was applied at Shenmen (HT 7), Sanyinjiao (SP 6), Anmian (Extra), Baihui (GV 20) and Sishencong (EX-HN 1), as well as the supplementary points selected according to the differentiation. The acupuncture treatment was given once a day, 5 treatments a week, for 4 weeks totally. In the integrated acupuncture and medication group, the western medication was combined with acupuncture. The dosage and usage of western medication were same as those in the western medication group; and acupoints in acupuncture treatment were same as those in the acupuncture group. The treatment lasted for 4 weeks in the three groups. Pittsburgh sleep quality index (PSQI) and clinical efficacy were observed before treatment, after 4 weeks' treatment and in 4 weeks after discontinuity of treatment in the three groups.</p><p><b>RESULTS</b>Four weeks after treatment, the clinical curative rates were 3. 3% (1/30), 21. 2% (7/33) and 25. 7% (9/35) in the western medication group, the acupuncture group and the integrated acupuncture and medicines group separately. The total effective rates were 70. 0%(21/30), 93. 9%(31/33) and 97. 1%(34/35) in the three groups separately. The curative rates and the total effective rates in the integrated acupuncture and medication group and the acupuncture group were higher than those in the western medication group separately (all, P<0. 01). PSQI scores after 4 Weeks' treatment were all improved as compared with those before treatment in the three groups (all P<0. 05). PSQI score in either the integrated acupuncture and medication group or the acupuncture group was lower than that in the western medication group, indicating the significant difference (both P< 0. 05). Four weeks after discontinuity of treatment, the efficacy was stable in the acupuncture group and the integrated acupuncture and medication group. PSQI score did not change as compared with that in the 4th week of treatment. The score in the western medication group ran back, close to that before treatment (P>0. 05). During the treatment, a few patients had dry mouth in the western medication group. The adverse reactions were not discovered in the other two groups.</p><p><b>CONCLUSION</b>The integrated therapy of acupuncture and medication achieves the quick efficacy on senile insomnia and rapidly relieves the symptoms, with quite high clinical curative rate and total effective rate obtained. The long-term efficacy is better than that of western medication. The integrated therapy is the first option among the three therapeutic programs.</p>

Study on HPLC specific chromatograms of Lu Dangshen / 中国中药杂志

In this paper, the RP-HPLC specific chromatography was adopted, with DIKMA-C18 (4.6 mm x 250 mm, 5 µm) as the chromatographic column, with a gradient elution compose of acetonitrile and 0.1% phosphoric acid at flow rate of 0.8 mL · min(-1), the detection wavelength was 220 nm. The difference of the HPLC specific chromatograms between the Lu Dangshen and other different base sources and different producing area of Codonopsis Radix was compared, involved in the similarities and differences of the number and the relative peak area of characteristic peaks in the HPLC specific chromatograms. The HPLC specific chromatograms of Lu Dangshen was established and the relative retention times of seven peaks was determined, and the peaks of codonopyrrolidium B, syringin, lobetyolin, tangshenoside I and atractylenoide III were identified; The HPLC specific chromatograms of Lu Dangshen provided a method for scientific evaluation and effective control the quality of Lu Dangshen from Shanxi famous-region.

Adaptation and validation of the Inventory of Family Protective Factors for the Portuguese culture / Adaptação e Validação do Instrumento Inventory of Family Protective Factors para a cultura portuguesa / Adaptación y Validación del Instrumento Inventory of Family Protective Factors para la cultura portuguesa

OBJECTIVES: to adapt and validate the Inventory of Family Protective Factors (IFPF) for the Portuguese culture. This instrument assesses protective factors that contribute to family resilience. Studies addressing resilience are embedded within the salutogenic paradigm, i.e. it addresses protective factors of individuals or groups without underestimating risk factors or vulnerability. METHOD: in order to assess the IFPF's linguistic and conceptual equivalence, the instrument was translated, retro-translated and the think-aloud protocol was used. We then verified the instrument's sensitiveness, reliability and validity of results to assess its psychometric characteristics. A factor analysis was performed of the principal components with varimax rotation of the scale's items and Cronbach's alpha coefficient was calculated for each dimension. A total of 85 families with disabled children, selected through simple random sampling, self-administered the instrument. RESULTS: the IFPF presents psychometric characteristics that are appropriate for the Portuguese population (Cronbach's alpha = .90). CONCLUSION: the IFPF was adapted and validated for the Portuguese culture and is an instrument to be used in studies intended to assess protective factors of family resilience. .

OBJETIVOS: adaptar e validar o Inventory of Family Protective Factors para a cultura portuguesa. Esse instrumento avalia os fatores protetores que contribuem para a resiliência familiar. Os estudos sobre resiliência inserem-se no paradigma salutogênico, abordando os fatores protetores dos indivíduos, ou grupos, sem subestimar os fatores de risco ou vulnerabilidade. MÉTODO: para avaliar a equivalência linguística e conceitual do Inventory of Family Protective Factors realizou-se a tradução, retroversão e reflexão falada; para aferir as características psicométricas do instrumento, verificou-se a sensibilidade, confiabilidade e a validade dos resultados. Foi realizada uma análise fatorial de componentes principais com rotação Varimax dos itens da escala e calculou-se o coeficiente alfa de Cronbach para cada dimensão. Através de uma amostragem aleatória simples, aplicou-se esse instrumento a 85 famílias de crianças com necessidades especiais que o autopreencheram. RESULTADOS: o Inventory of Family Protective Factors apresenta características psicométricas adequadas para a população portuguesa (alfa de Cronbach de .90). CONCLUSÃO: o Inventory of Family Protective Factors foi adaptado e validado para a cultura portuguesa. Considera-se que se trata de um instrumento útil para estudos nos quais há a proposta de avaliar os fatores protetores da resiliência familiar. .

OBJETIVOS: adaptar y validar el Inventory of Family Protective Factors (IFPF) para la cultura portuguesa. Este instrumento evalúa los factores protectores que contribuyen para la resiliencia familiar. Los estudios sobre resiliencia se insieren en el paradigma salutogénico, abordando los factores protectores de los individuos o grupos, sin subestimar los factores de riesgo o vulnerabilidad. MÉTODO: para evaluar la equivalencia lingüística y conceptual del IFPF realizamos la traducción, retrotraducción y reflexión hablada; para evaluar las características psicométricas del instrumento verificamos la sensibilidad, confiabilidad y la validez de los resultados. Realizamos un análisis factorial de los componentes principales con rotación varimax de los ítems de la escala y calculamos el coeficiente Alpha de Cronbach para cada dimensión. A través de un muestreo aleatorio simple, aplicamos este instrumento a 85 familias de niños con necesidades especiales que lo autollenaron. RESULTADOS: el IFPF presenta características psicométricas adecuadas para la población portuguesa (alfa de Cronbach de 0,90). CONCLUSIÓN: el IFPF fue adaptado y validado para la cultura portuguesa. Consideramos que se trata de un instrumento útil para estudios que se propongan evaluar los factores protectores de la resiliencia familiar. .

Role of γ-oryzanol in drought-tolerant and susceptible cultivars of rice (Oryza sativa L.).

Drought-tolerant cultivars and their phytochemical composition, which has a role in providing drought tolerance are gaining importance. In this study, rice bran oil and semi-purified oryzanol (SPO) obtained from five rice (Oryza sativa L.) cultivars, namely P1401 and PB1 (drought-susceptible) and N22, PNR381 and APO (drought-tolerant) were analyzed for the γ-oryzanol content, an antioxidant present in considerable amount in the rice bran. The higher level of γ-oryzanol and its antioxidant activity was observed in drought-tolerant cultivars (N22, PNR381 and APO) as compared to drought-susceptible (PB1 and P1401), suggesting the role of γ-oryzanol in drought tolerance, as antioxidants are known to play an important role by scavenging free radicals. The total antioxidant activity of γ-oryzanol might be attributed to 24-methylene cycloartanyl ferulate, a major component of γ-oryzanol. By enhancing the level of active oryzanol components identified in this study by genetic and molecular means could impart increased drought tolerance.

Long-term effects with ambrisentan monotherapy in patients with pulmonary arterial hypertension / 中华心血管病杂志

<p><b>OBJECTIVE</b>To investigate long-term efficacy and safety of ambrisentan monotherapy in patients with pulmonary arterial hypertension (PAH).</p><p><b>METHODS</b>Patients with PAH who received 2.5 mg or 5 mg of ambrisentan once daily between July 10, 2011 and August 30, 2012 for at least 6 months were enrolled. The efficacy endpoints were change in exercise capacity, World Health Organization (WHO) functional class and N-terminal pro-brain natriuretic peptide (NT-proBNP) level, echocardiographic parameters. The safety endpoint was the safety of long-term ambrisentan administration, as defined by the incidence and severity of adverse events.</p><p><b>RESULTS</b>A total of 18 patients with PAH were enrolled. Mean age was (39 ± 17) years, 8 (55.6%) were female, and 11 (61.1%) patients were in WHO functional class III. The median duration of treatment was 17 months (range: 6-26 months). After treatment, the 6MWD was significantly increased[ (495 ± 97) m vs. (400 ± 91) m, P < 0.001], NT-proBNP was significantly reduced [308 (53-1 645) ng/L vs. 80(22-454) ng/L, P = 0.005], the systolic pulmonary artery was significantly decreased [(62 ± 30) mmHg vs. (82 ± 41) mmHg, P = 0.001] and left ventricular end diastolic diameter was significantly increased [(44 ± 6) mm vs. (40 ± 6) mm, P < 0.004] compared to pre-treatment. WHO functional class was improved compared with baseline in 11(61.1%) patients, stable in 7(38.9%) patients. No patient died during the treatment period. No patient was withdrawn from this study for safety reasons.</p><p><b>CONCLUSIONS</b>Long-term treatment of ambrisentan can effectively improve the exercise capacity, reduce systolic pulmonary artery pressure and NT-proBNP in PAH patients. Ambrisentan is safe and well tolerated in Chinese PAH patients.</p>

Comparative pharmacokinetics of syringin, eleutheroside E and isofraxidin in rat plasma after intravenous administration of each monomer and Ciwujia injection / 中国中药杂志

To compare the pharmacokinetics of syringin, eleutheroside E and isofraxidin after intravenous administration of each monomer and Ciwujia injection. Twenty-four Sprague-Dawley rats were randomly divided into four groups and intravenously administrated with syringin, eleutheroside E, isofraxidin, and Ciwujia injection, respectively. The concentrations of the three components in rat plasma were determined by LC-MS/MS. DAS 2.0 software was applied to calculate the pharmacokinetic parameters while the SPSS 17.0 software was used for statistical analysis. Significant difference (P < 0.05) was found between each monomer and the injection on the main pharmacokinetic parameters such as AUC, CL and t1,/2. Compared with the injection, the group treated with the syringin has obvious decrease in AUC, and increase in CL while the group treated with eleutheroside E has obvious increase in AUC, and decrease in CL The t1/2 of isofraxidin was prolonged in Ciwujia injection. Pharmacokinetic characters of the ingredients in the injection varied greatly from the monomer. Other constituents in the injection may have an impact on the pharmacokinetic profiles of these three components.

Regulation of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid biosynthesis in cell suspension cultures of Saussurea involucrata / 中国中药杂志

Syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid are three main bioactive ingredients in herbs of Saussurea involucrata with various pharmacological properties, while their contents are very low. In this study, the biosynthesis of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid in the cell suspension cultures of S. involucrata were regulated by feeding carbon sources and precursors, which resulted in a great increase of the contents and yields of the above three bioactive ingredients. After 16 days of fermentation, the yields of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid reached 339.0, 225.3, 512.7 mg x L(-1), respectively. Meanwhile, their contents increased up to 67.9, 1.9, 10.6 times of wild medicinal material, respectively. The results provided a solid basis for further studies on application of cell suspension cultures of S. involucrata for large-scale production of bioactive compounds syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid.

Two new phenylpropanoids from Micromelum integerrimum / 中国天然药物

AIM@#To investigate the chemical and bioactive constituents from the stems and leaves of Micromelum integerrimum.@*METHOD@#The chemical constituents were isolated and purified by silica gel, Sephadex LH-20, and HPLC. Their structures were mainly elucidated on the basis of extensive 1D- and 2D-NMR spectroscopy and mass spectrometry. Their cytotoxicity and antimicrobial activities were tested by the SRB and turbidimetric methods, respectively.@*RESULTS@#Two new phenylpropanoids and two known coumarins were obtained, and their structures were identified as microintegerrin A (1), microintegerrin B (2), scopoletin (3), and scopolin (4). All of the compounds were tested for their cytotoxicity against three cancer cell lines (HeLa, A549, and BGC-823) and for antimicrobial activity against the fungus Candida albicans and the bacterium Staphylococcus aureus.@*CONCLUSION@#Two new phenylpropanoids 1 and 2 were isolated and identified from the stems and leaves of M. intgerrimum. None of the compounds showed cytotoxic or antimicrobial activity at the tested concentration of 20 μg·mL(-1).

Effects of ambrisentan in treatment of pulmonary arterial hypertension: a pilot study with 15 patients / 中华心血管病杂志

<p><b>OBJECTIVE</b>To investigate the preliminary efficacy and safety of ambrisentan, a selective endothelin receptor antagonist, in patients with pulmonary arterial hypertension (PAH).</p><p><b>METHODS</b>A total of 15 patients with PAH, including 10 patients with idiopathic PAH and 5 patients with associated connective-tissue disease, received 2.5 mg or 5 mg of ambrisentan once daily for 12 weeks. Before and after 12 weeks treatment, 6-minute walk test (6-MWD), WHO functional classification (WHO FC) and N-terminal pro-brain natriuretic peptide (NT-proBNP) were measured.</p><p><b>RESULTS</b>After 12 weeks treatment, the 6-MWD was significantly increased [(376.5 ± 108.2) m vs.(460.3 ± 95.7) m, P = 0.021] and the systolic pulmonary artery was significantly decreased [(85.0 ± 33.3) mm Hg (1 mm Hg = 0.133 kPa)vs. (70.5 ± 30.5) mm Hg,P = 0.015] and NT-proBNP was significantly reduced [892.0 (99.0-2245.0) ng/L vs. 205.0 (56.0-534.0) ng/L, P = 0.026] than before treatment. WHO FC was improved in 4 patients after 12 weeks treatment. No patient was withdrawn from this study for safety reasons.</p><p><b>CONCLUSIONS</b>Ambrisentan treatment can effectively improve the exercise capacity, and reduce systolic pulmonary artery pressure and NT-proBNP in PAH patients. Ambrisentan use is safe and could be well tolerated in Chinese PAH patients.</p>

Peroxisome proliferator-activated receptor α/γ agonist tesaglitazar stabilizes atherosclerotic plaque in diabetic low density lipoprotein receptor knockout mice / 中华心血管病杂志

<p><b>OBJECTIVE</b>To investigate the effects of peroxisome proliferator-activated receptor (PPAR) α/γ agonist on atherosclerotic plaque stabilization in diabetic LDL receptor knockout (LDLr-/-) mice.</p><p><b>METHODS</b>Female 4-week-old LDLr-/- mice fed with high-glucose and high-fat diet for 4 weeks were randomly divided into three groups (n = 15 each): control group (only fed with high-glucose and high-fat diet), diabetic group [induced by high-glucose and high-fat diet combined with a low-dose of streptozotocin (STZ)] without tesaglitazar and with tesaglitazar (20 µg/kg oral treatment). After 6 weeks, the mice were sacrificed, body weight, fasting blood glucose (Glu), total cholesterol (TC), triglyceride (TG) levels were measured. The expression of ICAM-1, VCAM-1, MCP-1 in the brachiocephalic atherosclerotic lesions were determined by Western blot and immunohistochemistry, respectively. Brachiocephalic artery was prepared for morphologic study (HE, oil red O, Sirius red staining) and immunohistochemical analysis (macrophage surface molecule-3, α-smooth muscle actin), respectively.</p><p><b>RESULTS</b>Serum TC [(32.34 ± 3.26) mmol/L vs. (16.17 ± 1.91) mmol/L], TG [(3.57 ± 0.99) mmol/L vs. (2.21 ± 0.11) mmol/L] and Glu [(15.21 ± 4.67) mmol/L vs. (6.89 ± 0.83) mmol/L] levels were significantly higher in diabetic group than in the control group (all P < 0.01). The expression of ICAM-1 (2.31 ± 0.35 vs.1.34 ± 0.21), VCAM-1 (1.65 ± 0.14 vs.0.82 ± 0.26), MCP-1 (2.27 ± 0.16 vs.1.56 ± 0.23) were significantly upregulated in diabetic group compared with control group (all P < 0.01). Brachiocephalic atherosclerotic plaque area [(4.597 ± 1.260)×10(3) µm(2) vs. (0.075 ± 0.030)×10(3) µm(2)], lipid deposition [(47.23 ± 2.64)% vs. (9.67 ± 1.75)%], Mac-3 positive area [(19.15 ± 3.51)% vs. (1.72 ± 0.16)%], α-smooth muscle actin [(5.54 ± 1.17)% vs. (2.13 ± 0.41)%] and collagen content [(4.27 ± 0.74)% vs. (0.43 ± 0.09)%] were all significantly larger/higher in diabetic LDLr-/- mice than in the control group (all P < 0.01). While tesaglitazar treatment significantly reduced serum TC [(30.47 ± 3.18) mmol/L], TG [(3.14 ± 0.71) mmol/L] and Glu [(7.92 ± 1.28) mmol/L] levels (all P < 0.01). Similarly, the expression of ICAM-1 [(1.84 ± 0.22)], VCAM-1 [(1.27 ± 0.11)], MCP-1 [(1.83 ± 0.24)], brachiocephalic atherosclerotic lesion area[(1.283 ± 0.410)×10(3) µm(2)], lipid deposition[(23.52 ± 1.39)%] were also significantly reduced by tesaglitazar (all P < 0.05). Moreover, tesaglitazar increased α-smooth muscle actin [(9.46 ± 1.47)%] and collagen content [(6.32 ± 1.15)%] in diabetic LDLr-/- mice (all P < 0.05). In addition, lipid deposition and Mac-3 positive areas [(10.67 ± 0.88)% vs. (15.83 ± 1.01)%] in the aortic root were also reduced in tesaglitazar treated diabetic LDLr-/- mice (P < 0.01).</p><p><b>CONCLUSIONS</b>Tesaglitazar has anti-inflammatory effects in the diabetic LDLr-/- mice. Tesaglitazar could reduce lipid deposition, increase collagen and α-SMA content in the brachiocephalic atherosclerotic lesions, thus, stabilize atherosclerotic plaque in this model.</p>

Efficacy of Alfuzosin After Shock Wave Lithotripsy for the Treatment of Ureteral Calculi

PURPOSE: We evaluated the efficacy of alfuzosin for the treatment of ureteral calculi less than 10 mm in diameter after extracorporeal shock wave lithotripsy (ESWL). MATERIALS AND METHODS: A randomized, single-blind clinical trial was performed prospectively by one physician between June 2010 and August 2011. A total of 84 patients with ureteral calculi 5 to 10 mm in diameter were divided into two groups. Alfuzosin 10 mg (once daily) and loxoprofen sodium 68.1 mg (as needed) were prescribed to group 1 (n=41), and loxoprofen sodium 68.1 mg (as needed) only was prescribed to group 2 (n=44). The drug administration began immediately after ESWL and continued until stone expulsion was confirmed up to a maximum of 42 days after the procedure. RESULTS: Thirty-nine of 41 (95.1%) patients in group 1 and 40 of 43 (93.0%) patients in group 2 ultimately passed stones (p=0.96). The number of ESWL sessions was 1.34+/-0.65 and 1.41+/-0.85 in groups 1 and 2, respectively (p=0.33). The patients who required analgesics after ESWL were 8 (19.5%) in group 1 and 13 (30.2%) in group 2 (p=0.31). Visual analogue scale pain severity scores were 5.33+/-1.22 and 6.43+/-1.36 in groups 1 and 2, respectively (p=0.056). The time to stone expulsion in groups 1 and 2 was 9.5+/-4.8 days and 14.7+/-9.8 days, respectively (p=0.005). No significant adverse effects occurred. CONCLUSIONS: The use of alfuzosin in combination with ESWL seems to facilitate stone passage and to reduce the time of stone expulsion but does not affect the stone-free rate.

Surgical Management of Bisphosphonate Related Osteonecrosis of the Jaw Using Pedicled Buccal Fat Pad Flap

Comparison The Safety and The Efficacy between the Group of using Pelubiprofen Tab. and the Group of using Aceclofenac Tab. on Back Pain Patients: Multi Institution, Double Blind, Random Sample

STUDY DESIGN: Multi institution, double blind, random sample. OBJECTIVES: We conducted a comparative study with Aceclofenac Tab, which is widely used in the clinical field in order to observe the Pelubiprofen Tab's clinical efficiency in patients with back pain. SUMMARY OF LITERATURE REVIEW: Among the numerous literatures regarding the chronic back pain, there is are few studies with Pelubiprofen Tab's clinical efficiency. MATERIALS AND METHODS: We computed an experimental model through a case control study, practiced from January, 2010 to January, 2011, and thereby, 298 back pain patients were selected. This study was conducted through a multi institution, double blind, and random sample. We compared the experimental and control groups' clinical efficiency that was estimated by VAS after 28 days of medication. Also, we compared the treatment efficiency of both drugs by using a variation of Oswestry Disability Index (ODI) and Physician's Global assessment, with a total usage of relief medicine. Also, the side effect and clinical pathologic result were tested. Statistical analysis was done with three different methods, Safety method, ITT (Intent-To-Treat), and PP (Per Protocol). Logistic regression model was used, and this result was compared by a Chi-square or Fisher's Exact test. RESULTS: Comparing the VAS of both groups, VAS decreased with statistical significance. Both groups didn't show a significant difference in VAS (p=0.6764). As the decrement of the total dosage of relief medicine, the decrease in the control group was rather higher, but the difference didn't show any statistical significance (p=0.9955). The experimental group was not inferior than that of the control group in ODI and PGA variation. Analyzing the side effect, both groups didn't show any significant difference (p=0.9843). CONCLUSIONS: As a result of the clinical trial, Pelubiprofen Tab. applied to back pain patients was not inferior to that of aceclofenac Tab., in terms of efficiency, and didn't show any significant difference in safety.