Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives

A series of 4-aryl methylidene-2-phenyl/methyl-5-(4H)-oxazolone derivatives (2-7) have been synthesized using the reported method by condensation of aldehydes with N-benzoyl / N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. The compounds (2-6) are new derivatives. The structures of compounds were evaluated on the basis of 1H-NMR, 13C-NMR, EIMS, FT-IR and elemental analysis. All the compounds were screened for their antibacterial and urease inhibition activity. Antibacterial activity was tested by agar well diffusion method using Mueller Hinton Agar medium. Compound (2) showed excellent activity against S. aureus which has 16 mm (80%) inhibition and above 24 mm (70%) against S. typhi. The most active compound against E. coli was compound (6) having 20 mm (80%) inhibition followed by compound (5) having above 18 mm (70%) inhibition. Urease inhibition activity of all the compounds was determined by indophenol method. Compounds (3, 6) and (7) showed significant inhibition against Jacks bean urease

Relationship of Age, BMI, Serum Calcium and Estradiol with BMD in Postmenopausal Osteoporotic Females

Introduction: The current study was designed to investigate the relationship of age, body mass index (BMI), serum calcium and estradiol with bone mineral density (BMD) in postmenopausal females with and without osteoporosis. Subjects & Methods: One hundred females were included in this study and were divided into two groups (fifty in each group): postmenopausal females without osteoporosis (age: 54.36 ± 0.51 yrs) and postmenopausal females with osteoporosis (age: 59.92 ± 0.68 yrs). BMD assessment was done on calcaneous by peripheral ultrasound bone densitometry and T scores were calculated. Serum estradiol was measured by ELIZA and calcium levels were determined by using spectrophotometric kit. Results: BMD was significantly lower in postmenopausal osteoporotic females as compared to postmenopausal non-osteoporotic females which indicated increased bone loss in osteoporotic group. Serum calcium levels were significantly lower in postmenopausal females with osteoporosis (8.73 ± 0.08) as compared to postmenopausal females without osteoporosis (9.04 ± 0.09). BMD was correlated with body weight ( r= 0.50, p<0.05; r= 0.45, p<0.05) and BMI (r=0.61, p<0.01; r= 0.31, p<0.05) in both groups. Negative correlation of BMD was found with age (r= -0.67, p<0.01r= -0.57, p<0.05) and calcium (r= -0.44, p<0.05; r= -0.38, p<0.05) in postmenopausal females with and without osteoporosis respectively. Osteopenia was detected in postmenopausal females without osteoporosis. Conclusion: It is concluded that increasing age, low body weight, low BMI, and low BMD are few of the contributing factors to osteoporosi

Evaluation of some biological activities of Abelia triflora R Br (Caprifoliaceae) constituents

Purpose: To investigate the antioxidant, anti-inflammatory, antidiabetic,  cardiovascular and cytotoxic activities of the leaf extract and major compounds isolated from Abelia triflora R. Br. (Caprifoliaceae)Methods: The chloroform soluble fraction of A. triflora leaves was subjected to several column chromatographic separations to isolate its constituents.  Anti-inflammatory and antioxidant activities were determined in terms of the ability to inhibit NF-kB, iNOS activity and lipoxygenase enzyme, and to decrease oxidative stress in HepG2 cells. Antidiabetic and cardiovascular activities were determined by screening for peroxisome proliferator-activated receptor alpha (PPARα) and PPARɣ agonistic activities. In vitro cytotoxic activity was determined against a set of four human cancer cell lines (SK-MEL, KB, BT-549, SK-OV-3) and two  non-cancerous kidney cell lines (LLC-PK1 and VERO). Cell viability was measured by neutral red assay.Results: Three triterpene acids were isolated from the chloroform fraction namely; ursolic acid (4), 2, 3-dihydroxy ursolic acid (5) and 2, 3, 21-trihydroxy ursolic acid (6). The results showed that ursolic acid exhibited potent inhibition of lipoxygenase enzyme and iNOS (inducible nitric oxide synthase) activity with IC50 (half-maximal inhibitory concentration) value of 13.0 μg/mL, compared to parthenolide positive standard (IC50, 0.3μg/mL); furthermore, it inhibited NF-kB (nuclear factor-kappa B) with IC50 of 25.0 μg/mL, compared to parthenolide (positive standard, (IC50, 0.5 μg/mL). Also, ursolic acid possessed the highest cytotoxic effect against the three cell lines, SK-MEL (IC50, 14.5 μg/mL), BT-549 (IC50, 16.0 μg/mL) and SK-OV-3 (IC50, 12.5 μg/mL). Only 2,3-dihydroxy ursolic acid activated PPARɣ (1.5-fold at 25 μM), compared to rosiglitazone (positive standard, 3.7 fold at 10 μM)Conclusion: Among the investigated compounds, ursolic acid exhibited the highest anti-inflammatory and cytotoxic activities, while 2,3-dihydroxy ursolic acid demonstrated antidiabetic activity via activation of PPARɣ.Keywords: Abelia triflora, Anti-inflammatory, Antidiabetic, Cardiovascular activity, Antioxidant, Cytotoxi

Food Security Challenges Emanating from COVID-19

Food security is a multidimensional notion and it can be achieved at individual, domestic, regional, countrywide and global levels. This is achieved when all individuals, at all times, have physical and economic access to adequate, safe, and nutritious food to fulfill their intake needs and food choices for an active and healthy life. As a result of COVID-19, global activity has witnessed an exceptional decline. The physical distance, school closures, trade restrictions, and country lockdowns for controlling the COVID-19 pandemic have led to escalated nutritional challenges globally. Food insecurity is defined as the persistent concern about access to sufficient and affordable food at all times. Food insecurity causes stress in people. This review aimed to evaluate the extent of disruption and break in the chain of continuity of food security as a result of the COVID- 19 pandemic. The review perused peculiar causes of food insecurity in the context of the COVID-19 pandemic along with measures to counter them for the attainment of sufficient food security. This review article methodology was inclusive of the utilization of three search engines. These included PubMed, Google as well as Google Scholar. The keywords included food security, food chain, challenges as well as COVID-19, and health outcomes. Articles were included based on being published from the year 2008-2023. Out of 66 articles, 50 were included (75%). The food availability having deteriorated due to the COVID-19 pandemic has affected food security globally leading to various adverse health outcomes. Also, this has added to the burden of hunger and malnutrition across the globe. A special focus on agriculture can aid in dealing with the shortage of food. The COVID-19 pandemic has culminated in tremendous detrimental repercussions on food security. Food chain improvement and efficiency can be of pivotal importance in connection with the food security challenges having ensued following the COVID-19 pandemic. How to cite this: Junejo S, Javaid Q, Lateef M. Food Security Challenges Emanating from COVID-19. Life and Science. 2024; 5(4): 573-. doi: http://doi.org/10.37185/LnS.1.1.57

Novel Crown Ether-Functionalized Fusidic Acid Butyl Ester: Synthesis, Biological Evaluation, In Silico ADMET, and Molecular Docking Studies

Crown ethers have gained importance in the field of medicine because of their resemblance to natural ionophores like valinomycin. With the goal of developing new pharmacologically important crown ethers, a novel series of crown ethers linked with Fusidic acid butyl ester 10a–d were synthesized and characterized by means of their 1H NMR, 13C NMR DEPT-135, FT-IR, and mass spectrometry. In vitro antioxidant and α-glucosidase inhibition activities of all crown ethers along with the precursor Fusidic acid butyl ester were examined and compared to the standard butylated hydroxyanisole and acarbose, respectively. Compounds (FABE-16-crown-4) 10b and (FABE-19-crown-5) 10c showed high antioxidant potential with the IC50 = 22.5 ± 0.2 μM and 32.1 ± 0.3 μM, respectively, when compared to the standard BHA (IC50 = 44.2 ± 0.34 μM). To understand the binding mode of the compounds, molecular docking investigations were performed using human antioxidant protein, peroxiredoxin 5. Molecular docking studies revealed higher docking scores (−6.5 and −6.7 kcal/mol) for the highly active compounds 10c and 10b, respectively, than standard BHA (−5.3 kcal/mol). Synthesized crown ethers exhibited moderate α-glucosidase inhibition with (IC50 = 23.5 ± 0.2 to 76.5 ± 0.1 μM) when compared to acarbose as standard (IC50 = 5.2 ± 0.8 μM). The in silico ADMET predictions indicated that the prepared compounds obeyed (bRO5) and Veber’s rule for the acceptance as orally administered drugs and indicated that all the prepared crown ethers exhibited calculated values of drug likeness parameters in acceptable ranges that showed good potential of these molecules for further drug development investigations

Evaluation of c-reactive protein in breast cancer by enzyme linked immunoassay technique

Abstract&#x0D; Objective: To explore the serum levels of C-reactive protein in breast cancer patients, and to investigate the relationship between  inflammation and progression of breast cancer.&#x0D; Methods: The  case-control study  was conducted at Bahria University Medical and Dental College, Karachi, from September 2015 to December 2018, and comprised breast cancer patients in group A and and an equal number of age-matched healthy women in control group B. C-reactive protein levels were evaluated in serum samples using enzyme-linked immunosorbent assay in both the groups and micro ribonucleic acid levels in serum were quantified using real time polymerase chain reaction. Data was analysed using SPSS 16.&#x0D; Results: Of the 170 subjects, 85(50%) were in each of the two groups. C-reactive protein and micro ribonucleic acid expression were significantly different in group A (p&lt;0.001). There was no correlation (r = 0.162, p&gt;0.01) between the tumour  markers in  group B (p&gt;0.05).&#x0D; Conclusion: Significantly raised C-reactive protein levels showed there was a link between inflammation and breast cancer.&#x0D; Key Words: Breast cancer, C-reactive protein, MicroRNA 16. Continuous....</jats:p

Immune System Enriching Micronutrients: Essential Ingredient for Wellbeing in COVID-19

&#x0D; &#x0D; &#x0D; The World Health Organization (WHO) on March 11, 2020, has declared the novel coronavirus (COVID-19) onset a global pandemic. Consequently, there has been noticeable economic adversity globally and a significant loss of life. A strong functioning immune system is crucial for adequate defense against pathogenic organisms. The intricacy of the interplay between nutrition and immunology is wide ranging. In the context of novel corona virus disease, competent immune system requires adequate supply of essential nutrients including vitamin C, D, E, A, B6, B12, folateandtraceelements,includingzinc,iron,selenium,magnesium,copper to support innate and adaptive immune systems. Other nutrients such as omega-3 fatty acids also support immune system effectively, specifically by helping to resolve the inflammatory response. Deficiencies or suboptimal status in micronutrients negatively affects immune function and can decrease resistance to infections. AlthoughmuchremainstobeknownaboutCOVID-19,itisimportantthat,toavertthelikelihoodof being infected with COVID-19, nutrition intake targeted towards boosting immune system is indispensable.&#x0D; &#x0D; &#x0D; </jats:p