A Progressive Philippine School for Children: Proposal and Presentation for Prospective Parents

Presents a philosophical framework for a proposed elementary school in the Philippines, the Philippine School for Children (PSC). It summarizes the major contributions of a family of theorists: Piaget, Dewey, and Vygotsky and applies their theories to the development of PSC. The study also includes a description of several features of a progressive classroom for kindergarten and grade one. The content of the study serves as a basis for the presentation of a progressive approach to education to prospective parents. Possible questions from prospective parents are raised and addressed at the conclusion of the study

Antiulcerogenic and antioxidant activities of Baccharis trimera (Less) DC (Asteraceae)

A "carqueja", Baccharis trimera (Less) DC (Asteraceae), é uma espécie vegetal característica de regiões tropicais, muito utilizada na medicina popular como antiinflamatória, hipoglicemiante e em tratamento de problemas digestivos. A avaliação da atividade antiúlcera do extrato bruto liofilizado e do extrato liofilizado da "resina" (porção que durante a concentração dos extratos ficava depositada no fundo do recipiente com aspecto viscoso e pegajoso) foi realizada através de indução aguda por etanol acidificado. O extrato bruto liofilizado, na dose de 400 mg/ kg, reduziu a área de lesão em 90%, 200 mg/kg, 87%, 100 mg/kg, 66% e o fármaco controle (lansoprazol), 66%. O extrato liofilizado da "resina", administrado na dose de 400 mg/kg, reduziu a área de lesão em 82%, 200 mg/kg, 82%, 100 mg/kg, 53% e o fármaco controle (lansoprazol), 70%. A atividade antioxidante foi ensaiada com extrato bruto liofilizado, extrato liofilizado da "resina", pó da droga e frações clorofórmica, acetato de etila, etanol e etanol 50% através do método que reduz o radical 2,2'-difenil-1-picril-hidrazil (DPPH), permitindo após o equilíbrio da reação, calcular a quantidade de antioxidante gasta para reduzir 50% do DPPH, apresentando resultado evidente, comparado à vitamina E. Não foram verificados sinais de alteração aparente no ensaio de toxicidade na dose única de 5g/kg, em camundongos.Baccharis trimera (Less) DC (Asteraceae) is a medicinal Brazilian plant well-known by "carqueja". Natural from tropical regions, used as home-made medicine as anti-inflammatory, hypoglycemiant and for the treatment of digestive problems. The evaluation of the antiulcer activity of the extract and the "resin" (portion which during the extracts concentration was settled at the bottom of the recipient, showing a viscous and clammy aspect), was accomplished through the acute induction by acidified ethanol. The lyophilized extract, at a dose of 400 mg/kg, reduced the lesion area at 90%; 200 mg/kg, at 87%; 100 mg/kg, at 66%; and the control (lansoprazol) at 66%. The "resin" administered at the 400 mg/kg dose reduced the lesion area at 82%; 200 mg/kg, at 82%, 100 mg/kg, at 53% and the control (lansoprazol), at 70%. The antioxidant activity of the lyophilized extract, of the "resin" of the powdered drug, of the chloroform, ethyl acetate, ethanol and 50% ethanol fractions was tested following the method which reduces the 2,2-dipheny l-1 -picrylhydrazyl (DPPH) radical, permitting after the reaction balance, to calculate the amount of antioxidant spent to reduce 50% of the DPPH. The result was meaningful, when compared with the vitamin E result. The acute toxicity test performed in mice showed no apparent alteration

Синтез, протимікробна активність та докінгові дослідження 6-(1H-бензімідазол-2- іл)-5-метилтієно[2,3-d]піримідин-4(3H)-онів з ацетамідними та 1,2,4-оксадіазол-5- ілметильними замісниками

Aim. To synthesize, study the antimicrobial activity and suggest antimicrobial activity mechanism for the novel derivatives of 6-(1H-benzimidazol-2-yl)-5-methylthieno[2,3-d]pyrimidin-4(3H)-one. Results and discussion. As the result of the targeted modification of 6-(1H-benzimidazol-2-yl)-5-methylthieno[2,3-d]-pyrimidin-4(3H)-one in position 3 with acetamide and 1,2,4-oxadiazol-5-ylmethyl substituents, the compounds, which demonstrated better antimicrobial activity in the agar well diffusion assay than the reference drug Streptomycin, were obtained. To elucidate the mechanism of action of the novel compounds, the docking studies were con-ducted to the active site of the 16S subunit of ribosomal RNA, the proven target for aminoglycoside antibiotics, as well as tRNA (Guanine37-N1)-methyltransferase (TrmD), which inhibitors were considered as a new potential class of antibiotics. Experimental part. By the interaction of 6-(1H-benzimidazol-2-yl)-5-methylthieno[2,3-d]pyrimidin-4(3H)-one with a series of N-arylchloroacetamides and 3-aryl-5-(chloromethyl)-1,2,4-oxadiazoles in DMF in the presence of K2CO3 the target compounds were obtained. The antimicrobial activity was assessed by the agar well diffusion method. The concentration of microbial cells was determined by the McFarland standard; the value was 107 cells in 1 mL of the media. The 18 – 24 hour culture of microorganisms was used for tests. For the bacteria cultivation, Müller-Hinton agar was used, Sabouraud agar was applied for C. albicans cultivation. The compounds were tested as the DMSO solution with the concentration of 100 µg/mL; the volume of the solution was 0.3 mL, the same volume was used for Streptomycin (the concentration 30 µg/mL). The docking studies were performed using Autodock Vina. Crystallographic data for the complexes of Streptomycin with the 16S subunit of ribosomal RNA (1NTB) and its active site, as well as for tRNA (Guanine37-N1)-methyltransferase (EC 2.1.1.228; TrmD) (5ZHN) and its active site were obtained from the Protein Data Bank.Conclusions. It has been determined that 2-[6-(1H-benzimidazol-2-yl)-5-methyl-4-oxothieno[2,3-d]pyrimidin-3(4H)-yl]-N-[4-(ethoxy)phenyl]acetamide, which is the most active as an antimicrobial agent among the compounds tested, also shows the best binding activity towards the active site of tRNA (guanine37-N1)-methyltransferase.Мета. Синтезувати й дослідити протимікробну активність нових похідних 6-(1H-бензімідазол-2-іл)-5-метилтієно[2,3-d]піримідин-4(3H)-онів та запропонувати механізм протимікробної активності.Результати та їх обговорення. У результаті цілеспрямованої модифікації положення 3 6-(1H-бензімідазол-2-іл)-5-метилтієно[2,3-d]піримідин-4(3H)-ону ацетамідним та 1,2,4-оксадіазол-5-ілметильним замісниками було одержано сполуки з визначеною методом дифузії в агар протимікробною активністю, що є більшою за активність препарату порівняння Стрептоміцину. З метою з’ясування механізму дії синтезованих сполук було проведено докінгові дослідження щодо активного сайту субодиниці 16S рибосомальної РНК, яка є підтвердженою мішенню для аміноглікозидних антибіотиків, а також тРНК (Гуанін-37-N1)-метилтрансферази (TrmD), інгібітори якої розглядаються як новий потенційний клас антибіотиків. Експериментальна частина. Шляхом взаємодії 6-(1H-бензімідазол-2-іл)-5-метилтієно[2,3-d]піримідин-4(3H)-ону з рядом N-арилхлороацетамідів та 3-арил-5-(хлорометил)-1,2,4-оксадіазолів в умовах ДМФА-K2CO3 було одержано цільові сполуки. Антимікробну активність визначали методом дифузії в агар. Концентрацію мікробних клітин визначали за МакФарландом; мікробне навантаження склало 107 мікробних одиниць в 1 мл середовища. Для тестів використовували 18 – 24 годинну культуру мікроорганізмів. Для культивування бактерій використовували агар Мюллера-Гінтона; для культивування C. albicans використовували агар Сабуро. Сполуки вводили методом дифузії в агар (лунками) у вигляді розчину у ДМСО в концентрації 100 мкг/мл в об’ємі 0,3 мл; аналогічний об’єм використовували для Стрептоміцину (конц. 30 мкг/мл). Докінгові дослідження проводили за допомогою програми Autodock Vina. Кристалографічні дані для комплексів стрептоміцину з 16S субодиницею рибосомальної РНК (1NTB) та її активного сайту і для тРНК (Гуанін-37-N1)-метилтрансферази (EC 2.1.1.228; TrmD) (5ZHN) та її активного сайту було отримано з Protein Data Bank.Висновки. Виявлено, що сполука 2-[6-(1H-бензімідазол-2-іл)-5-метил-4-оксотієно[2,3-d]піримідин-3(4H)-іл]-N-[4-(етокси)феніл]ацетамід, яка характеризується найбільшою протимікробною активністю, у докінгових розрахунках є також найбільш ефективним інгібітором тРНК (Гуанін-37-N1)-метилтрансферази

The role of advanced glycation end products in patogenesis of diabetic nephropathy

Diabetes mellitus (DM) and chronic kidney disease are the diseases that have exceeded epidemic thresholds in terms of prevalence all over the world. That made it possible to classify them as non-communicable epidemics of the XXI century. Diabetic nephropathy (DN) is implicated with high levels of disablement and mortality. Advanced glycation end products (AGE) play a key role in the progression of DN. Increased formation of AGE occurs due to hyperglycemia under the conditions of diabetes. Moreover, there are additional factors in DN that increase the elaboration of AGE, such as high levels of oxidative stress and decreased renal clearance which slows down the AGE excretion. Both immediate effects of AGE and interaction of AGE with its cell-bound receptor (RAGE) result in a сascade of events that lead to further progression of DN. Thus, the research of the new therapeutic approaches targeted on the AGE-RAGE system is of great interest to slow progression of DN and improve the prognosis

Improving PLS-SEM use for business marketing research

A review of studies published in Industrial Marketing Management over the past two decades and more shows that these studies not only used partial least squares structural equation modeling (PLS-SEM) widely to estimate and empirically substantiate theoretically established models with constructs, but did so increasingly. In line with their study goals, researchers provided reasons for using PLS-SEM (e.g., model complexity, limited sample size, and prediction). These reasons are frequently not fully convincing, requiring further clarification. Additionally, our review reveals that researchers' assessment and reporting of their measurement and structural models are insufficient. Certain tests and thresholds that they use are also inappropriate. Finally, researchers seldom apply more advanced PLS-SEM analytic techniques, although these can support the results' robustness and may create new insights. This paper addresses the issues by reviewing business marketing studies to clarify PLS-SEM's appropriate use. Furthermore, the paper provides researchers and practitioners in the business marketing field with a best practice orientation and describes new opportunities for using PLS-SEM. To this end, the paper offers guidelines and checklists to support future PLS-SEM applications