Synthesis and biological evaluation of some hybrid 2-quinolinone derivatives containing cinnamic acid as anti-breast cancer drugs

ABSTRACT. A new series of hybrid 2-quinolinone derivatives were synthesized by using 7-hydroxy-4-methyl-1-amino-quinolin-2-one (2) and cinnamic acid. Hybrid halogenated 2-quinolinone derivatives (3-(7-hydroxy-4-methyl-3,6,8-tribromo-2-oxo-2H-quinolin-1-ylamino)-3-phenyl acrylic acid (4) and 3-(7-acetoxy-4-methyl-3,6,8-tribromo-2-oxo-1H-quinolin-1-ylamino)-3-phenyl acrylic acid (7)) were prepared via the halogenation of 3-(7-hydroxy-4-methyl-2-oxo-2H-quinolin-1-ylamino)-3-phenyl acrylic acid (3) with bromine to give compound 4 with acetic anhydride led to the formation of hydride halogenated 2-quinolinone derivative (7). All the synthesized hybrid 2-quinolinone and hybrid halogenated 2-quinolinone derivatives were tested for their cytotoxicity against MCF-7 cell line. DNA flow cytometric analysis of compounds 3 showed cell cycle arrest at G2/M phase with concomitant increase of cells in apoptotic phase. Dual annexin-V/propidium iodide staining assay of compound 3 revealed that, the selected molecule increases the apoptosis of MCF-7 cells more than control.                     KEY WORDS: Quinolinone, Hybrid, Cinnamic acid, Apoptosis, MCF-7 cells   Bull. Chem. Soc. Ethiop. 2021, 35(3), 551-564. DOI: https://dx.doi.org/10.4314/bcse.v35i3.

Synthesis of novel nitrogen heterocycles bearing biological active carboxamide moiety as potential antitumor agents

ABSTRACT. In the present study, synthesis of a simple series of nitrogen heterocycles containing N-(p-bromophenyl) carboxamide moiety, such as benzimidazole, benzoxazine, oxadiazole and triazole compounds, by using 4-bromo aniline and diethyl oxalate as a key starting material has been described. Five nitrogen heterocycles compounds moiety were evaluated for their anticancer activity against MCF-7 cell line. The results revealed that compound 8 (N-(4-bromophenyl)-5-thioxo-1,3,4-oxadiazole-2-carboxamide) was the most potent cytotoxic activity. Cell cycle analysis demonstrated that compound 8 induce cell cycle arrest at G1 phase with apoptosis inducing activity marked by increase in G0 phase.                     KEY WORDS: Synthesis, Nitrogen heterocycles, Carboxamide, Antitumor agents   Bull. Chem. Soc. Ethiop. 2021, 35(2), 449-459. DOI: https://dx.doi.org/10.4314/bcse.v35i2.1

A Laser-Guided Spinal Cord Displacement Injury in Adult Mice

Mouse models are unique for studying molecular mechanisms of neurotrauma because of the availability of various genetic modified mouse lines. For spinal cord injury (SCI) research, producing an accurate injury is essential, but it is challenging because of the small size of the mouse cord and the inconsistency of injury production. The Louisville Injury System Apparatus (LISA) impactor has been shown to produce precise contusive SCI in adult rats. Here, we examined whether the LISA impactor could be used to create accurate and graded contusive SCIs in mice. Adult C57BL/6 mice received a T10 laminectomy followed by 0.2, 0.5, and 0.8 mm displacement injuries, guided by a laser, from the dorsal surface of the spinal cord using the LISA impactor. Basso Mouse Scale (BMS), grid-walking, TreadScan, and Hargreaves analyses were performed for up to 6 weeks post-injury. All mice were euthanized at the 7th week, and the spinal cords were collected for histological analysis. Our results showed that the LISA impactor produced accurate and consistent contusive SCIs corresponding to mild, moderate, and severe injuries to the cord. The degree of injury severities could be readily determined by the BMS locomotor, grid-walking, and TreadScan gait assessments. The cutaneous hyperalgesia threshold was also significantly increased as the injury severity increased. The terminal lesion area and the spared white matter of the injury epicenter were strongly correlated with the injury severities. We conclude that the LISA device, guided by a laser, can produce reliable graded contusive SCIs in mice, resulting in severity-dependent behavioral and histopathological deficits

Ethanol production from lignocellulosic materials by fermentation process using yeast

Rapid industrialization and growing population result to high demand for energy. Depletion and rise in price of petroleum as well as environmental pollution necessitates the need for alternative source of fuel, hence bioethanol production. Rice bran (Oryza sativa), Corn bran (Zea mays) and Sorghum bran (Sorghum guinense) and saw dusts of Khaya senegalensis (Red wood), Terminalia superba (Black wood), Gmelina arborea (White wood), were used for the study. The yeasts used for the study were isolated from fermented beverages (Sorghum beer, Millet beverage and Palm wine). The results of the lignocellulosic biomass of white saw dust, red saw dust, black saw dust, rice bran, corn bran and sorghum bran revealed cellulose components as 77.78%, 75.55%, 68.59%, 64.83%, 54.82% and 55.14% respectively. A total of 25 yeasts were isolates and identified using API 20C AUX strip. The yeast isolates, K2, B5, B7 and P1 had the highest ethanol tolerance value of 14%. The results showed that the ethanol-producing ability of the yeast isolates ranged from 4.1% to 10.3%. Fourier Transform Infrared Spectrophotometer (FTIR) and Gas Chromatography and Mass Spectrometry (GC-MS) analyses showed that ethanol is the main compound produced by yeasts from the lignocellulosic materials. This study revealed that Saccharomyces cerevisiae isolated from palm wine (P1) is best in ethanol production and tolerance, and this high prolific strain can be exploited or engineered for ethanol production. Therefore, Lignocellulosic biomasses are recommended as raw materials for producing ethanol, which is a promising alternative energy source as against the depleting petroleum.Keywords: Ethanol, Lignocellulose, Yeasts, Beverages and Saccharomyces cerevisiae

Outcomes and challenges in the management of gestational trophoblastic disease in a tertiary institution in Nigeria

Context: Gestational Trophoblastic Diseases are a spectrum of interrelated diseases disorders that arise from abnormal pregnancy and are characterized by excessive elevation of Human Chorionic Gonadotrophins. They include both benign and malignant forms; hydatidiform mole, Invasive mole, Placental Site Trophoblastic (PSTT) tumour and Choriocarcinoma.Objective: The objective of this study was to present the outcomes and challenges encountered in the management of GTDs in a tertiary centre in South-western part of Nigeria.Study Design, Setting and Subjects: This was a retrospective study of the cases of gestational trophoblastic disease managed at Obafemi Awolowo University Teaching hospitals complex, Ile Ife between 2009 and 2013. Data were retrieved from the case records and telephone calls were put across the patients to enquire about the state of health of the patients. Data was analysed using SPSS version 20.Main Outcome Measures: The main outcome measures were the incidence of GTDs, outcomes and challenges encountered in the management of patients with gestational trophoblastic disease.Results: A total of 27 women were managed for GTDs; 22 had hydatidiform moles and 5 were managed for choriocarcinoma. The mean age of the patients was 31.9 years SD 6.94, mean parity 2 SD 1.53; mean duration of amenorrhoea was 15.7 weeks SD 4.92. The most common presenting symptom was vaginal bleeding in 81.5% of cases. Non-adherence to prescribed treatment was high as over half of the patients with molar pregnancy was lost to follow up after molar evacuation. Mortality was also high among patients with GTDs as 60% of the patients with choriocarcinoma died during treatment

PRODUCTION AND SOME QUALITY ATTRIBUTES OF RICE-BAMBARA NUT FLOUR EXTRUDED FLAKES

The proximate, functional and sensory properties of Rice-Bambara flakes were investigated. The flour was mixed at different proportions (100% Rice flour, 90:10, 80:20, 70:30, 60:40, 50:50 Rice-Bambara flour). The proximate composition, functional properties and sensory acceptability of the flakes were determined using standard laboratory procedures. The water absorption capacity ranged from 1.90 to 2.50. The swelling power and solubility index ranged from 3.51-4.37 and 13.35-20.50, respectively. The fat, protein, ash, crude fiber, moisture and carbohydrate contents ranged from 1.33-3.13%, 5.30-18.37%, 0.37-1.34%, 0.26-1.38%, 4.99-6.79%, and 69.35-85.18% respectively. Sensory panelists«¤?? scores for color, taste, aroma, texture and overall acceptability ranged from 4.46-7.23, 4.11-6.70, 5.00-7.09, 4.32-6.14, and 4.73-6.91 respectively. There were significant differences (P<0.05) between the sensory, functional and proximate properties of the flakes. The study showed that 90:10 Rice-Bambara flour extruded flakes had better functional properties and sensory acceptability

An audit of uterovaginal prolapse in Ogbomoso, south-west Nigeria

Objective: Uterovaginal prolapse (UVP) as a gynaecological problem is very common especially in multipara. This condition is important to gynaecologists practicing in Sub-Saharan Africa because of its strong link with multiparity, poor conduct of labour, and most importantly, its role as a cause of chronic morbidity in many post-menopausal women necessitating major gynaecological surgeries.Methods: A retrospective study of utero-vaginal prolapse to determine the prevalence, presentation , management patterns and complications of UVP at the Bowen University Teaching Hospital , Ogbomosho, Oyo State, Nigeria between January 1, 2010 and December 31, 2014. Relevant data were obtained from the case notes, which included age, parity, presenting symptoms, number of living children, types of delivery, types of surgical management and associated operative morbidity and mortality. The data were presented as simple percentages.Results: The prevalence of uterovaginal prolapse was 5.4%. The mean age at presentation was 51.4± 3.3 years. The mean parity was 4.2± 1.6. Fifty-six (90.3%) of them were at least 40 years old . Majority of the patients( 80.6%) were grand-multiparous. The commonest symptom was 'something coming down the vagina' in 96% of the study subjects. Difficult labour was found to be the most common associated factor in 47 (76.2%) of the patients Second degree prolapse was the commonest type of presentation (74.2%). The most common form of treatment offered was vaginal hysterectomy with pelvic floor repair, 46 (74.2%) of the patients. Twenty -four (38.7%) patients had vaginal pessaries inserted for various degrees of UVP.Conclusion: Uterovaginal prolapse is a common gynaecological condition of the parous and elderly postmenopausal women associated with a decreased body image and quality of life. Supervised hospital deliveries and limiting the family size by efficient contraception deserve priority attention to prevent this social malady.Keywords: Difficult labour, uterovaginal prolapse, hysterectomy, multiparit

Intrapartum prediction of birth weight using maternal anthropometric measurements and ultrasound scan

This prospective study was conducted at Federal Medical Centre, Owo, Nigeria, between April 1st and 31st of July, 2013 to predict birth weight in labour using four clinical methods and ultrasound scan independently and comparatively to determine which is closest to the actual birth weight. The four clinical methods are Ojwang's formula, Johnson's formula, 5% of maternal weight and 10% of maternal body mass index. A total of 100 women who fulfilled the inclusion criteria had their foetal weight estimated using the methods. Accuracy of the prediction was determined by mean weight difference, percentage error and proportion of estimates within 10% of actual birth weight.Tests of significant difference were done and the level of significance was set at 0.05.Correlation and regression analyses were carried out.Of the five methods used, ultrasound scan estimation had the highest correlation coefficient of 0.681(P<0.001) followed by Ojwang's rule with correlation coefficient of 0.675(P<0.001). The prediction using Johnson's method performed next to Ojwang's rule with correlation coefficient of 0.629(P<0.001).The methods using 5% maternal weight and 10% maternal BMI had correlation coefficients of 0.312(P<0.001) and 0.220(P<0.001) respectively. It was then concluded that there is positive significant correlation between the methods used and actual birth weight. The method using 10% maternal BMI is the least reliable while the ultrasound scan estimate was the most reliable. Ojwang's rule estimation performed next to ultrasound and should be considered first in settings where ultrasound machine or the expertise to use the machine is lacking.Keywords: Birth weight, Foetal weight, Ultrasonography, Pregnancy, Delivery, Prospective studie

Prevalence, predictors, and perceived susceptibility to placental malaria parasitemia among pregnant women in a tertiary hospital in South-Western Nigeria

Objective: Is to determine the prevalence and predictors of placental malaria among pregnant women.Methodology: The study was cross-sectional in design. It was carried out over six months. We administered Pretested questionnaire to 300 eligible subjects. The researchers took maternal peripheral blood for malaria parasites while cord and placental blood sample at delivery for neonatal packed cell volume (PCV) and Malaria parasite. Data were analyzed using STATA 10.Result: One hundred and forty-four (48%) participants had placental malaria parasitemia, while 173 (57.7%) had peripheral malaria parasitemia. Maternal age less than 20 years (P=0.008), low parity, and hemoglobin type AA (P=0.002) were significantly associated with a higher prevalence of placental parasitemia. Maternal secondary and tertiary education (P=0.013), perceived susceptibility to placental malaria and IPT use (p=0.014) were significantly associated with lower prevalence.Conclusion: This study has shown that placental parasitemia is a significant problem in pregnancy as it is strongly associated with certain maternal factors. There is the need to intensify control efforts aimed at reducing malaria in pregnancy in Nigeria, and mothers with increased risk factors should receive more focused attention. Keywords: Prevalence, risk factors, placental malaria, pregnanc

Premature rupture of membranes at term: immediate induction of labor versus expectant management

Objective: To compare the maternal outcomes of immediate induction of labor with expectant management in women presenting with premature rupture of membranes (PROM) at term.Methods: One hundred and fifty two women with PROM at term were randomized into either immediate induction of labor with oxytocin or expectant management for a period of 12 hours. The primary outcome measure was the incidence of clinical endometritis in each group. Secondary outcomes were the mode of delivery, the neonatal outcome and the proportion of women in the expectant management group that progressed to spontaneous labor.Results: The immediate induction arm had a lower caesarean section rate, (7.9% vs 28.9%, P=0.001), higher spontaneous vaginal delivery rate (92.1% vs 71.1%; P=0.001) and lower incidence of clinical endometritis (0% vs 5.3%, P=0.006), when compared with the expectant management arm. The estimated duration of labor was shorter in the expectant management arm (8.9±2.17hours vs 10.6±2.35hours; P=<0.001). Neonatal morbidity rates were comparable in both groups.Conclusion: Immediate induction of labor in women with PROM at term resulted in significantly lower rate of infectious morbidity without increasing the risk of operative delivery. It is therefore recommended as the management option of choice.Keywords: Premature rupture of membranes, induction of labor, endometriti