N,N′-Bis(2-chloro­benz­yl)-N′′-(2,2,2-trichloro­acet­yl)phospho­ric triamide

The P atom in the title compound, C16H15Cl5N3O2P, exhibits a tetra­hedral coordination geometry and the phosphoryl and carbonyl groups are anti with respect to one another. The dihedral angle between the benzene rings is 44.90 (15)°. One of the 2-chloro­benzyl­amido fragments is disordered over two sets of sites with occupancies of 0.8823 (17) and 0.1177 (17). In the crystal, adjacent mol­ecules are linked via N—H⋯O(P) and N—H⋯O(C) hydrogen bonds into an extended chain running parallel to the a axis

Cyclo­hex­yl(meth­yl)ammonium {bis­[cyclo­hex­yl(meth­yl)amino]­phosphor­yl}(4-methyl­phenyl­sulfon­yl)aza­nide

In the anion of the title salt, C7H16N+·C21H35N3O3PS−, the P and S atoms are both in distorted tetra­hedral environments and the angles at the tertiary N atoms confirm their sp 2 character. The two S=O groups are in syn and gauche conformations with respect to the phosphoryl group. In the crystal, N—H⋯O(=S) and N—H⋯O(=P) hydrogen bonds involving two anions and two cations form a centrosymmetric four-component cluster

Design and Development of Small-Molecule Arylaldoxime/5-Nitroimidazole Hybrids as Potent Inhibitors of MARK4: a Promising Approach for Target-Based Cancer Therapy

[Abstract] Microtubule affinity-regulating kinase 4 (MARK4), a member of the serine/threonine kinase family, is an emerging therapeutic target in anticancer drug discovery paradigm due to its involvement in regulation of microtubule dynamics, cell cycle regulation, and cancer progression. Therefore, to identify the novel chemical architecture for the design and development of novel MARK4 inhibitors with concomitant radical scavenging property, a series of small-molecule arylaldoxime/5-nitroimidazole conjugates were designed and synthesized via multistep chemical reactions following the pharmacophoric hybridization approach. Compound 4h was identified as a promising MARK4 inhibitor with high selectivity toward MARK4 inhibition as compared to the panel of screened 30 kinases pertaining to the serine/threonine family, which was validated by molecular docking and fluorescence binding studies. The comprehensive cell-based examination divulged the promising apoptotic, antiproliferative, and antioxidant potential for the chemotype 4h. The compound 4h was endowed with the Ka value of 3.6 × 103 M–1 for human serum albumin, which reflects its remarkable transportation and delivery properties to the target site via blood. The present study impedes that in the future, such compounds may stand as optimized pharmacological lead candidates in drug discovery for targeting cancer via MARK4 inhibition with a remarkable anticancer profile.Council of Scientific and Industrial Research (India); 09/466 (0220) 2K19 EMR-IGovernment of India; EMR/2015/002372Government of India; BT/PR12828/AAQ/1/622/2015Indian Council of Medical Research; 45/9/2019-PHA/BM

Synthesis and Antitumor Activity of Brominated-Ormeloxifene (Br-ORM) against Cervical Cancer

Aberrant regulation of β-catenin signaling is strongly linked with cancer proliferation, invasion, migration, and metastasis, thus, small molecules that can inhibit this pathway might have great clinical significance. Our molecular modeling studies suggest that ormeloxifene (ORM), a triphenylethylene molecule that docks with β-catenin, and its brominated analogue (Br-ORM) bind more effectively with relatively less energy (−7.6 kcal/mol) to the active site of β-catenin as compared to parent ORM. Herein, we report the synthesis and characterization of a Br-ORM by NMR and FTIR, as well as its anticancer activity in cervical cancer models. Br-ORM treatment effectively inhibited tumorigenic features (cell proliferation and colony-forming ability, etc.) and induced apoptotic death, as evident by pronounced PARP cleavage. Furthermore, Br-ORM treatment caused cell cycle arrest at the G1-S phase. Mechanistic investigation revealed that Br-ORM targets the key proteins involved in promoting epithelial–mesenchymal transition (EMT), as demonstrated by upregulation of E-cadherin and repression of N-cadherin, Vimentin, Snail, MMP-2, and MMP-9 expression. Br-ORM also represses the expression and nuclear subcellular localization of β-catenin. Consequently, Br-ORM treatment effectively inhibited tumor growth in an orthotopic cervical cancer xenograft mouse model along with EMT associated changes as compared to vehicle control-treated mice. Altogether, experimental findings suggest that Br-ORM is a novel, promising β-catenin inhibitor and therefore can be harnessed as a potent anticancer small molecule for cervical cancer treatment

Ocular manifestations of dengue fever in Bangladesh during its out break

Dengue fever, borne by Aedes aegypti mosquito, is one of the most common and most prevalent forms of flavivirus infections in humans, endemic in tropics and warm temperate regions of the world. We report a spectrum of ocular manifestations of dengue fever along with its associated laboratory findings. To study the ocular manifestations associated with dengue fever. This study was conducted in 600 patients hospitalized with diagnosis of dengue fever over a period of 3 months from March 2019 to May 2019. All patients underwent complete evaluation with respect to systemic and ophthalmic examination in different institutions of Bangladesh. A total of 600 patients were diagnosed with dengue fever; of which, 375 (62.5%) were men and 225 (37.5%) were women. Mean age was 32 years (20–60 years). Only 195 patients (32.7%) had complaints of retrobulbar pain in the eyes. 10 patients (1.67%) had blurring of vision. Ocular findings were present in 340 patients (56.7%). Most common anterior segment findings were subconjunctival haemorrhage in 275 patients (45.8%). Posterior segment findings were present in 80 patients (13.3%); of which, 70 (87.5%) had retinal haemorrhages. Ocular changes had resolved in all the cases, which came for follow-up in 8–10 weeks. It was mostly attributed to the improving platelet count. The incidence of ocular complications in dengue fever is increasing, hence all patients with dengue should be referred to an ophthalmologist to prevent any sight-threatening BSMMU J 2022; 15(1): 16-1

Determinants of Arsenicosis Patients’ Perception and Social Implications of Arsenic Poisoning through Groundwater in Bangladesh

Adverse human health effects ranging from skin lesions to internal cancers as well as widespread social and psychological problems caused by arsenic contaminated drinking water in Bangladesh may be the biggest arsenic calamity in the world. From an arsenicosis patients survey, this paper empirically analyzes the determinants of arsenicosis patients’ perception about chronic arsenic poisoning and social and psychological implications of arsenicosis. In this study, cross-sectional data were collected from the Matlab and Hajiganj Upzillas of Chandpur district which are known to be highly contaminated with arsenic in their underground water. Respondents informed that arsenic poisoning causes a wide range of social and psychological problems. Female respondents were less vulnerable in the case of social problems (p < 0.01) and more vulnerable for the psychological problems (p < 0.001) of arsenicosis than male respondents. The results based on logit analysis showed that education (p < 0.01) and household income (p < 0.05) were significantly correlated to respondents’ perception about arsenicosis. The arsenicosis related special program (s) needs a clear understanding of people’s perception about arsenic exposure for abating the health burden as well as social and psychological problems

An overview of the Leucospidae (Hymenoptera, Chalcidoidea) of the Arabian Peninsula with description of a new species

An overview of the family Leucospidae (Hymenoptera, Chalcidoidea) is provided for the leucospid fauna of the Arabian Peninsula. Two genera containing four species are identified based on morphometrics and colour patterns. One species, Leucospis ayezae Usman, Anwar &amp;amp; Ahmad, sp. nov., is described. Leucospis elegans Klug had been previously recorded from Arabia Felix (= Yemen) and is recorded here for the first time from Saudi Arabia. The status of Leucospis aff. namibica from Yemen has been clarified, and this species is placed here in the genus Micrapion Kriechbaumer as M. clavaforme Steffan. An updated key and a map showing the distribution of the family Leucospidae in the Arabian Peninsula is provided. The occurrence and color morphs of all leucospid species that have been recorded so far from the region are briefly discussed

Sustainable and eco-friendly dyeing of traditional grass cloth with a reactive dye in palm oil medium

Traditional grass cloth has been used in China for a long time for the manufacturing of various household furnishing textiles and ladieswear. However, traditionally the grass cloth is dyed with reactive dyes in an aqueous medium, but the dyeing process is not sustainable because of high energy and water usage and the production of coloured effluent. In this work, the possibility of palm oil/water dual-phase dyeing of traditional grass cloth with a reactive dye, C.I. Reactive Blue 194 (Reactive Blue 194), was explored. The grass cloth soaked in an alkaline solution with 80–140% pick-up was dyed in a palm oil dyebath containing dye powder dispersed in a palm oil medium. The initial study confirmed that the pre-treatment of the fabric with an alkaline solution with 140% pick-up was beneficial for the uniform distribution of the dye in the fibres. The dyeing process parameters (e.g., fixation temperature, solution pH, and fixation time) for the grass cloth dyeing with the Reactive Blue 194 were optimised by using the Taguchi method. The pH of the alkali pre-treatment solution was found to be the most influential factor, as confirmed by the analysis of variance in terms of the percentage of contribution (94.41%), which was statistically significant (P < 0.05). The confirmation tests were carried out under optimal settings, and a higher K/S (24.06) was found compared with the initial condition (21.51). X-ray diffraction analysis indicated that the dyeing process did not affect the crystallinity of the grass cloth fibres. Furthermore, the recovery of palm oil from the spent dyebath was around 99%, and up to five times recycling and reuse of palm oil were studied for the dyeing of grass cloth. The colour strength of the grass cloths dyed in the palm oil recycled up to five times was similar to the cloth dyed in fresh palm oil. The results show that palm oil can be used as a dyeing medium for the sustainable dyeing of grass cloth with effluent reduction, which can be extended to the dyeing of other textile fibres

Models Analyses for Allelopathic Effects of Chicory at Equivalent Coupling of Nitrogen Supply and pH Level on F. arundinacea, T. repens and M. sativa

Alllelopathic potential of chicory was investigated by evaluating its effect on seed germination, soluble sugar, malondialdehyde (MDA) and the chlorophyll content of three target plants species (Festuca arundinacea, Trifolium repens and Medicago sativa). The secretion of allelochemicals was regulated by keeping the donor plant (chicory) separate from the three target plant species and using different pH and nitrogen levels. Leachates from donor pots with different pH levels and nitrogen concentrations continuously irrigated the target pots containing the seedlings. The allelopathic effects of the chicory at equivalent coupling of nitrogen supply and pH level on the three target plants species were explored via models analyses. The results suggested a positive effect of nitrogen supply and pH level on allelochemical secretion from chicory plants. The nitrogen supply and pH level were located at a rectangular area defined by 149 to 168 mg/l nitrogen supply combining 4.95 to 7.0 pH value and point located at nitrogen supply 177 mg/l, pH 6.33 when they were in equivalent coupling effects; whereas the inhibitory effects of equivalent coupling nitrogen supply and pH level were located at rectangular area defined by 125 to 131 mg/l nitrogen supply combining 6.71 to 6.88 pH value and two points respectively located at nitrogen supply 180 mg/l with pH 6.38 and nitrogen supply 166 mg/l with pH 7.59. Aqueous extracts of chicory fleshy roots and leaves accompanied by treatment at different sand pH values and nitrogen concentrations influenced germination, seedling growth, soluble sugar, MDA and chlorophyll of F. arundinacea, T. repens and M. sativa. Additionally, we determined the phenolics contents of root and leaf aqueous extracts, which were 0.104% and 0.044% on average, respectively