Exploring the antimicrobial and cytotoxic potential of novel chloroquine analogues.

Aim: To synthesize novel chloroquine analogues and evaluate them for antimicrobial and cytotoxic potential. Methods: Novel analogues were synthesized from chloroquine by nucleophilic substitution reaction at the 4-amino position. Results: Analogue CS1 showed maximum antimicrobial potential (30.3 ± 0.15 mm zone) against Pseudomonas aeruginosa and produced a 19.2 ± 0.21 mm zone against Candida albicans, while CS0 produced no zone at the same concentration. Analogue CS9 has excellent cytotoxic potential (HeLa cell line), showing 100% inhibition (IC50 = 8.9 ± 1.2 µg/ml), compared with CS0 (61.9% inhibition at 30 µg/ml). Conclusion: These synthesized chloroquine analogues have excellent activity against different microbial strains and cervical cancer cell lines (HeLa) compared with their parent molecule.

Novel amodiaquine analogues to treat cervical cancer and microbial infection in the future.

Aim: To synthesize and explore the therapeutic potential of amodiaquine analogues. Methodology: New promising analogues were synthesized by nucleophilic substitution at the 4-amino position and were characterized using 1H NMR, 13C NMR and FT-IR spectroscopic techniques. Results: Antibacterial and cytotoxic screening revealed the high potency of these compounds; analogue AS1 had an 34.3 ± 0.18 mm zone of inhibition against Pseudomonas aeruginosa. Excellent activity against fungal strains, that is, Candida albicans (39.6 ± 0.23 mm) was shown by analogue AS2. Analogue AS1 had an IC50 = 4.2 µg/ml against the HeLa cell line (cervical cancer) and binding energy against 5GWK (-8.32688 kcal/mol), 1PFK (-6.4780 kcal/mol) and 1TUP (-6.5279 kcal/mol) in the docking study. Conclusion: The obtained results reveal that these analogues exhibit potent antimicrobial and cytotoxic potential.

A Mature Cystic Teratoma of the Urinary Bladder.

We report a case of a mature cystic teratoma of urinary bladder in a 17-year female, which is extremely rare. The patient presented with pain in suprapubic region for one year. On computerized tomography (CT) of abdomen and pelvis, a welldefined, enhancing heterogeneous soft tissue density lesion measuring 2.5x2.3x3 cm with mean density of 48 Hounsfield unit was found originating from the superior wall of the urinary bladder and projecting into the lumen. Cystoscopy showed a 2X2 cm growth containing concretions. Resection of the lesion was done with wide margin by transurethral resection of bladder tumor (TURBT). Histopathological examination showed fragments of skin, sebaceous glands, fat and muscle cells, confirming mature cystic teratoma.

Lymphocytic esophagitis: An Australian (Queensland) case series of a newly recognized mimic of eosinophilic esophagitis.

BACKGROUND AND AIM: Lymphocytic esophagitis (LoE) is a recently described upper gastrointestinal tract "disorder" diagnosis of which hinges on histology and is characterized by the excessive infiltration of lymphocytes in the peripapillary fields of the esophageal epithelium, with clinical manifestations similar to those of eosinophilic esophagitis (EoE). In this article, we aim to describe for the first time the clinico-pathological characteristics of a large cohort of Australian (Queensland) cases of LoE. METHODS: Histological data that fulfilled the criteria (predominant lymphocytic infiltration in the peripapillary fields, none or minimal neutrophils or eosinophils, and no infection) were collected between January 2014 and May 2016 from a number of major Queensland Public Hospital anatomical pathology laboratories. Patient presentations were subsequently examined to compile clinical and endoscopic correlates. RESULTS: A total of 62 cases of LoE were identified. The median age was 55 years, with 59.6% of subjects being male. Major clinical manifestations included dysphagia (32), epigastric or abdominal pain (8), gastro-esophageal reflux (8), association with Crohn's disease (8), and vomiting or diarrhea (6). Endoscopy was normal in 47% of cases; 47% had appearances similar to those of EoE. There were three cases with associated mild monilial esophagitis (6%). CONCLUSION: LoE is a relatively recently recognized condition of the esophagus with variable clinical and endoscopic findings. Diagnosis is based on characteristic histological features. Further investigation is needed to ascertain the etiopathology and natural history of the condition and to establish a safe and effective treatment regimen.

Numerical investigation of vortex shedding mechanism for staggered rows of cylinders.

This numerical investigation deals with study of flow past seven square cylinders arranged in staggered configuration. Simulations to the underlying problem are carried out by using the single relaxation time lattice Boltzmann method. The gap spacing between the staggered rows is varied in streamwise direction from 0.25 to 2 and for three transverse spacing i.e. T* = 1, 1.5 and 2. The complex vortex shedding mechanism is visualized for different streamwise and transverse gap spacings. Furthermore, the vortex shedding mechanisms in the wake of downstream row of cylinders are debated by using vorticity snapshots, time-trace plots of drag and lift coefficients and power spectra visualization of lift coefficient. It is also observed that the secondary cylinder interaction frequency contributes significantly to the hydrodynamic forces experienced by the cylinders. The physical parameters, such as Strouhal number, the drag and lift coefficients and their root-mean-square values have also been discussed in detail.

Anticancer, antimicrobial and antioxidant potential of sterically tuned bis-N-heterocyclic salts.

The current study was conducted to evaluate the antimicrobial, antioxidant, antileishmanial and cytotoxic potential of designed derivatives of 1,1'-(1,3-phenylenebis(methylene))bis(3-alkyl/aryl-1H-benzimidazol-3-ium) salts. The antibacterial potential of the test compounds was investigated against Staphylococcus aureus, Pseudomonas aeruginosa and two methicillin-resistant S. aureus (MRSA) strains (MRSA10, MRSA11), where compound 6 showed the best results. For brine shrimp lethality bioassay (BSLB), compound 6 again showed up to 100% mortality at 200 µg/mL and 56.7% mortality at 6.25 µg/mL. Antileishmanial assay was performed against Leishmania tropica at 20 µg/mL dosage, where 6 showed the most promising activity with 16.26% survival (83.74% mortality; IC50=14.63 µg/mL). The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. Compound 6 was found to be the most effective cytotoxic compound with 75% inhibition of HCT-116 proliferation at 1 mg/mL concentration. Succinctly, 6 exhibited impressive pharmacological potential that might be attributed to its higher lipophilic character owing to the longer N-substituted alkyl chains when compared to the other test compounds.

Transitions in the flow patterns and aerodynamic characteristics of the flow around staggered rows of cylinders.

A two-dimensional numerical study of flow across rows of identical square cylinders arranged in staggered fashion is carried out. This study will unreveal complex flow physics depending upon the Reynolds number (Re) and gap spacing (g) between the cylinders. The combined effect of Reynolds number and gap spacing on the flow physics around staggered rows of cylinders are numerically studied for 20 ≤ Re ≤ 140 and 1 ≤ g ≤ 6. We use the lattice Boltzmann method for numerical computations. It is found that with increase in gap spacing between the cylinders the critical Reynolds number for the onset of vortex shedding also increases. We observed a strong effect of Reynolds number at g = 2 and 4. Secondary cylinder interaction frequency disappears for large Reynolds number at g = 6 and 5 and the flow around cylinders are fully dominated by the primary vortex shedding frequency. This ensures that at large gap spacing with an increase in the Reynolds number the wakes interaction between and behind the cylinders is weaken. Furthermore, it also ensures that the wake interaction behind the cylinders is strongly influenced by the jets in the gap spacing between the cylinders. We also found that g = 2 is the critical gap spacing for flow across rows of staggered square cylinders for the considered range of Reynolds number. Depending on the Reynolds number we observed; synchronous, quasi-periodic-I, quasi-periodic-II, and chaotic flow patterns. In synchronous flow pattern, an in-phase and anti-phase characteristics of consecutive cylinders has been observed. The important physical parameters are also analyzed and discussed in detail.