RESUMO Objetivo: Características clínico-patológicas e moleculares distintas foram observadas em tumores de cólon no lado direito ou esquerdo. O presente estudo teve como objetivo caracterizar o câncer de cólon e sua lateralidade em uma população rural norte-paquistanesa diagnosticada com câncer de cólon nesta instituição. Métodos: O estudo incluiu 70 pacientes que foram submetidos a quimioterapia adjuvante no Instituto Bannu de Medicina Nuclear Radioterapia Oncológica (BINOR), Bannu, Paquistão, entre janeiro de 2014 e dezembro de 2017. O teste qui-quadrado foi utilizado para mensurar a significância das variáveis categóricas. Valores de p menores que 0,05 foram considerados significativos. Resultados: A média de idade ao diagnóstico entre pacientes com câncer de cólon no lado direito foi de 43,94 anos e entre aqueles com câncer de cólon no lado esquerdo, 49,83, sem diferença significativa. Os pacientes do sexo masculino apresentaram mais tumores no lado direito (77% vs. 54%, p = 0,044) e as pacientes do sexo feminino apresentaram mais tumores no lado esquerdo (46% vs. 23%, p = 0,044). Tumores mal diferenciados foram mais comumente observados no lado direito (20% vs. 0%, p = 0,020). Adenocarcinoma mucinoso foi observado principalmente em casos de tumores no lado direito (37% vs. 3%, p ≤ 0,001). A apresentação local estava mais avançada em tumores de cólon no lado direito, com mais linfonodos positivos (83% vs. 60%, p = 0,025) e invasão linfovascular (51% vs. 37%, p = 0,016). O cólon sigmoide foi o sublocal mais comum. Conclusão: O presente estudo é o primeiro relato de câncer de cólon em uma população rural no norte do Paquistão. Em comparação com dados globais, observou-se um surgimento mais precoce dos tumores (44-50 anos).

ABSTRACT Objectives: Different clinicopathological and molecular features have been demonstrated between right and left sided colon cancers. We aimed to characterize colon cancer and sidedness among a North-Pakistani rural population diagnosed with colon cancer in our institution. Methods: Seventy patients were included in the study that received adjuvant chemotherapy at Bannu Institute of Nuclear Medicine Oncology and Radiotherapy) Bannu, Pakistan from January 2014 to December 2017. Chi-square test was used for significance of categorical variables. p-Values less than 0.05 were considered significant. Results: Mean age at diagnosis for right side colon cancer patients was 43.94 years and for left side colon cancer, it was 49.83 with no significant difference. Male patients were presented more with right (77% vs. 54%, p = 0.044) and females with predominantly left sided tumours i.e. (46% vs. 23%, p = 0.044). Right sided cancer tended to be more poorly differentiated (20% vs. 0%, p = 0.020). Mucinous adenocarcinoma was seen mostly in right sided colon cancer (37% vs. 3%, p ≤ 0.001). There were more locally advanced presentation of right side colon cancer with more node positive (83% vs. 60%, p = 0.025) and lymphovascular invasion (51% vs. 37%, p = 0.016). Sigmoid colon was the most common tumour subsite involved. Conclusion: Our study is the first report of colon cancer in a rural population in North-Pakistan. An earlier onset of tumours (44-50 years) was observed in comparison with global data.

Some novel derivatives of 2-(9H-Purin-6-ylsulfanyl) acetohydrazide were synthesized by reacting it with respective aldehydes in ethanol. The antithyroid effect of these compounds was ascertained in vitro by studying their complexation with iodine spectrophotometrically. In vivo, the hormonal as well as histological variations in male Wistar rats demonstrated significant antithyroid potential (p ≤ 0.05) of these compounds.

Algunos nuevos derivados de la 2-(9H-purin-6-ilsulfanil) acetohidrazida fueron sintetizados mediante la reacción con los respectivos aldehídos en etanol. El efecto antitiroideo de estos compuestos se determinó in vitro mediante el estudio espectrofotométrico de sus complejos con yodo. In vivo, las variaciones hormonales e histológicas en ratas macho Wistar demostraron de manera significativa (p ≤ 0,05) el potencial antitiroideo de estos compuestos.

A number of quinolone-3-acetic acids were synthesized by cyclocondensation of substituted anilines with diethyl acetylsuccinate in the presence of phosphorous pentoxide and followed by base hydrolysis of the resultant esters to form respective acids. All synthesized compounds were found to exhibit antibacterial activities against a range of gram-positive (Bacillus subtilis, Staphylococcus aureus) and gram-negative bacteria (Shigella sonnei, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhi) by broth dilution method. All the compounds exhibited antibacterial activities comparable to fluoroquinolones and in some cases even better activity was found. These findings suggest a great potential of these compounds for screening and use as antibacterial compounds for further studies with a battery of bacteria.

Some novel as well as known derivatives of 8-sulfanyl-3,9-dihydro-1H-purine-2,6-dione were synthesized and their antithyroid activity was measured in rats after administration of a daily dose of 20mg/kg via i.p. injection for 15 days. Free thyroxine and triiodothyronine concentrations were determined using radioimmunoassay technique. The assay results showed decrease in the hormonal concentrations for the animals treated with these compounds as compared to the control animals. Similarly, thyroid stimulating hormone level was measured with ELISA method and the results demonstrated a comparative increase of this hormone for the treated animals. The hormonal variations indicated significant (α<0.05) activity of the compounds. Histological study of thyroid tissues from the test animals showed cellular modifications in the treated animals like cylindrical shape of follicular epithelium, depletion of colloid and high values of thyroid body indices. All these factors further confirmed the antithyroid effects of the compounds under study.

Se sintetizaron algunos derivados nuevos y ya conocidos de la 8-sulfanil-3,9-dihidro-1H-purin-2,6-diona, y se determinó su actividad antitiroidea en ratas, tras la administración de una dosis diaria de 20 mg/kg a través de inyección intraperitoneal durante 15 días. Las concentraciones de tiroxina y triyodotironina libres se determinaron utilizando la técnica de radioinmunoensayo. Los resultados de los ensayos mostraron una disminución en las concentraciones hormonales de los animales tratados con estos compuestos en comparación con los animales control. Del mismo modo, el nivel de la hormona estimulante de la tiroides se midió con el método ELISA y los resultados demostraron un aumento comparativo de esta hormona en los animales tratados. Las variaciones hormonales indicaron actividad significativa (α < 0.05) de los compuestos. El estudio histológico de los tejidos de la tiroides de los animales de laboratorio mostró cambios celulares en los animales tratados, tales como la forma cilíndrica del epitelio folicular, la reducción en los valores de coloide y elevación de los índices del cuerpo tiroideo. Todos estos factores confirman también los efectos antitiroideos de los compuestos en estudio.

A atividade antitireóidea do 6-cloropurina, in vitro, foi determinada espectrofotometricamente por estudos de formação de seu complexo com iodo. O complexo mostrou estequiometria de 1:1. A constante de formação do complexo encontrada foi 7,652 × 10³ L mol-1, o que indicou um bom potencial de 6-cloropurina, como agente antitireóideo. Posteriores verificações mostraram mudanças nos níveis hormonais tireóideos em coelhos machos, in vivo, após administração da dose via intraperitoneal (i.p.) durante 14 dias e medindo os níveis de triiodotironina (T3) e tetraiodotironina (T4) livres, na circulação sanguínea, usando-se a técnica de radioimunoensaio. As análises de sangue mostraram decréscimo nos níveis de T3 e T4 livres em animais tratados, quando comparados com os controles. Desta maneira, confirmou-se uma boa atividade antitireóidea do 6-cloropurina.

Antithyroid activity of 6-chloropurine was determined, in vitro, by studying its complex formation with iodine spectrophotometrically. The complex exhibited a 1:1 stoichiometry. Formation constant (Kc) of the complex was found to be 7.652 × 10³ L mol-1, which indicated good antithyroid potential of 6-chloropurine. For further verification, changes in the thyroid hormone levels of the male rabbits were observed, in vivo, after administering the dose through intra peritoneal (i.p.) injections for 14 days and measuring free triiodothyronine (T3) and tetraiodothyronine (T4) levels in the blood serum using radioimmunoassay technique. The blood assays showed decrease in free T3 and T4 levels in the treated animals as compared to the control ones thus confirming fairly good antithyroid activity of 6-choloropurine.