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The seasonal shift in the homogeneity of the periphytic protozoan fauna was studied based on a four-season baseline survey in the coastal waters of the Yellow Sea, northern China. Samples were collected using glass microscope slides as an artificial substratum at a depth of 2 m after the immersion time of 14 days during each of the four seasons (winter, spring, summer, and autumn, 2017). The protozoan fauna showed a clear seasonal shift in species composition and a significant variation in homogeneity in terms of both compositional and community structure during four seasons. The dispersion measures and β-diversity index represented an increase in the trend from spring to winter. These findings suggest that the homogeneity of the periphytic protozoan fauna was subject to a significant variability shaped mainly by species composition during a four-season cycle in marine ecosystems.The present study aims to formulate the characterization and distribution of microplastic in the estuarine surface sediments of Kayamkulam estuary, southwest coast of India. The sediments were dominated by fibre and film shaped microplastic substances. The surface sediments were dominated by polyethylene. The distribution of microplastics was significantly higher than that observed in the other study regions, except for Pearl river estuary and Guanabara Bay. The distribution of microplastics was chiefly controlled by estuarine inundating water and the distance of the sampling site from the open sea.During the Covid-19 pandemic, personal protection equipment (PPE) was widely used to control the virus further spared. In this study, the presence of PPE wastes along the coastline of Bushehr port, the Persian Gulf from nine stations was investigated (4 times during 40 days), and their potential for microplastics (MPs) creation was preliminarily assessed. In total, more than 2380 PPE were collected in the study area. No significant differences were found between various beaches regarding their types and common activities. In addition, the estimated disposal rate of PPE per day and year is 350 and 127,750 items, respectively. More than 10% of the collected PPE from Bushehr's coastal areas on each sampling day were damaged. Based on the microscopic analysis, the left surgical masks and torn plastic gloves in the coastal regions are emerging sources of secondary microfibers and MP particles (mostly fragments and films) in the marine environments, respectively.The development of new molecules for the treatment of leishmaniasis is, a neglected parasitic disease, is urgent as current anti-leishmanial therapeutics are hampered by drug toxicity and resistance. The pyrrolo[1,2-b]isoquinoline core was selected as starting point, and palladium-catalyzed Heck-initiated cascade reactions were developed for the synthesis of a series of C-10 substituted derivatives. Their in vitro leishmanicidal activity against visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis was evaluated. The best activity was found, in general, for the 10-arylmethyl substituted pyrroloisoquinolines. In particular, 2ad (IC50 = 3.30 μM, SI > 77.01) and 2bb (IC50 = 3.93 μM, SI > 58.77) were approximately 10-fold more potent and selective than the drug of reference (miltefosine), against L. amazonensis on in vitro promastigote assays, while 2ae was the more active compound in the in vitro amastigote assays (IC50 = 33.59 μM, SI > 8.93). Notably, almost all compounds showed low cytotoxicity, CC50 > 100 μg/mL in J774 cells, highest tested dose. In addition, we have developed the first Perturbation Theory Machine Learning (PTML) algorithm able to predict simultaneously multiple biological activity parameters (IC50, Ki, etc.) vs. any Leishmania species and target protein, with high values of specificity (>98%) and sensitivity (>90%) in both training and validation series. Therefore, this model may be useful to reduce time and assay costs (material and human resources) in the drug discovery process.Artemisinin-based combination therapies (ACTs) have been able to reduce the clinical and pathological malaria cases in endemic areas around the globe. However, recent reports have shown a progressive decline in malaria parasite clearance in South-east Asia after ACT treatment, thus envisaging a need for new artemisinin (ART) derivatives and combinations. To address the emergence of drug resistance to current antimalarials, here we report the synthesis of artemisinin-peptidyl vinyl phosphonate hybrid molecules that show superior efficacy than artemisinin alone against chloroquine-resistant as well as multidrug-resistant Plasmodium falciparum strains with EC50 in pico-molar ranges. Chroman 1 concentration Further, the compounds effectively inhibited the survival of ring-stage parasite for laboratory-adapted artemisinin-resistant parasite lines as compared to artemisinin. These hybrid molecules showed complete parasite clearance in vivo using P. berghei mouse malaria model in comparison to artemisinin alone. Studies on the mode of action of hybrid molecules suggested that these artemisinin-peptidyl vinyl phosphonate hybrid molecules possessed dual activities inhibited falcipain-2 (FP-2) activity, a P. falciparum cysteine protease involved in hemoglobin degradation, and also blocked the hemozoin formation in the food-vacuole, a step earlier shown to be blocked by artemisinin. Since these hybrid molecules blocked multiple steps of a pathway and showed synergistic efficacies, we believe that these lead compounds can be developed as effective antimalarials to prevent the spread of resistance to current antimalarials.Hymenialdisine an alkaloid of oroidin class has drawn the attention of researchers owing to its unique structural features and interesting biological properties. Hymenialdisine exhibited promising inhibitory activity against a number of therapeutically important kinases viz., CDKs, GSK-3β etc., and showed anti-cancer, anti-inflammatory, anti-HIV, neuroprotective, anti-fouling, anti-plasmodium properties. Hymenialdisine and other structurally related oroidin alkaloids such as dibromo-hymenialdisine, stevensine, hymenin, axinohydantoin, spongicidines A-D, latonduines and callyspongisines contain pyrrolo[2,3-c] azepin-8-one core in common. Keeping in view of the interesting structural and therapeutic features of HMD, several structural modifications were carried around the fused-azepinone core which resulted in a number of diverse structural motifs like indolo-azepinones, paullones, aza-paullones, darpones and 5,7-dihydro-6H-benzo[b]pyrimido[4,5-d] azepin-6-one. In this review, an attempt is made to collate and review the structures of diverse hymenialdisine and related fused-azepinones of synthetic/natural origin and their biological properties.
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