Amyloid-β Inspired Short Peptide Amphiphile Facilitates Synthesis of Silver Nanoparticles as Potential Antibacterial Agents

An amyloid-β inspired biocompatible short peptide amphiphile (sPA) molecule was used for controlled and targeted delivery of bioactive silver nanoparticles via transforming sPA nanostructures. Such sPA-AgNPs hybrid structures can be further used to develop antibacterial materials to combat emerging bacterial resistance. Due to the excellent antibacterial activity of silver, the growth of clinically relevant bacteria was inhibited in the presence of AgNPs-sPA hybrids. Bacterial tests demonstrated that the high biocompatibility and low cytotoxicity of the designed sPA allow it to work as a model drug delivery agent. It therefore shows great potential in locally addressing bacterial infections. The results of our study suggest that these nanodevices have the potential to trap and then engage in the facile delivery of their chemical payload at the target site, thereby working as potential delivery materials. This system has potential therapeutic value for the treatment of microbiota triggered progression of neurodegenerative diseases.     

1-[2-(1-Cyclobutylpiperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]propan-1-one: a Histamine H3 Receptor Inverse Agonist with Efficacy in Animal Models of Cognition

A series of chemical optimizations, which was guided by in vitro affinity at histamine H₃ receptor (H₃R), modulation of lipophilicity, ADME properties and preclinical efficacy resulted in the identification of 1-[2-(1-cyclobutylpiperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]propan-1-one ( 45 e ) as a potent and selective (K_i=4.0 nM) H₃R inverse agonist. Dipsogenia induced by (R)-α-methylhistamine was dose dependently antagonized by 45 e , confirming its functional antagonism at H₃R. It is devoid of hERG and phospholipidosis issues. Compound 45 e has adequate oral exposures and favorable half-life in both rats and dogs. It has demonstrated high receptor occupancy (ED₈₀=0.22 mg/kg) and robust efficacy in object recognition task and, dose dependently increased acetylcholine levels in brain. The sub-therapeutic doses of 45 e in combination with donepezil significantly increased acetylcholine levels. The potent affinity, selectivity, in vivo efficacy and drug like properties together with safety, warrant for further development of this molecule for potential treatment of cognitive disorders associated with Alzheimer's disease.     

Sonodynamic Therapy with Metal Complexes: A New Promise in Cancer Therapy

In recent years, to overcome the problem of low tissue penetration power of light in photodynamic therapy (PDT), sonodynamic therapy (SDT) with ultrasound (US) as the drug stimulus has emerged as a potential alternative to PDT. The significantly higher tissue penetration capacity of US is reported to allow the treatment of deep-seated tumours. In general, organic molecules and nanomaterials dominate as the sonosensitizers in this area of research, and the potential of metal complexes in SDT is not yet well explored. In this highlight, we have summarized two recent literature reports in which researchers have explored the efficiency of metal complexes as sonosensitizers for the first time. These reports indicate the high potential of metal complexes in SDT.     

AI-enabled farm-friendly automatic machine for washing,image-based sorting,and weight grading of citrus fruits: Design optimization,performance evaluation,and ergonomic assessment

The modernization of postharvest operations and penetration of emerging technologies in horticultural processing have provided intelligent solutions for reducing postharvest losses. Work environmental and occupational health issues require immediate attention as the awkward posture and continuous drudgery-prone on-farm sorting and grading activities may lead to musculoskeletal disorders. The main objective of this study was to develop an automatic farm-friendly machine for real-time citrus fruit washing, image-based sorting, and weight grading; designed optimally and equipped with an embedded system comprising a lightweight convolutional neural network (CNN) model. Also included in this study was a thorough ergonomic assessment of the developed machine in a real work environment. The parametric choice of the fruit washing and singulation system was performed by employing computational fluid dynamics modeling and response surface methodology designed optimization. It was observed that under steady-state conditions, the water jet would arrive at a velocity of 11.36 m/s which would eventually suit a singulation conveyor with a slope of 25°. A noninvasive grading and sorting approach for citrus fruits is presented in this paper that leverages deep learning to classify the fruits into “accept” and “reject” classes. The custom lightweight CNN model “SortNet” has shown excellent classification results with an overall accuracy of 97.6%. The ergonomic evaluation shows that the average body part discomfort score in case of operating an automatic fruit grading machine was much lower (12.3 ± 2.0) than the traditional method (30.9 ± 3.3). Further, in the case of machine operation, the percentage load on the muscles ranged from 28.67 to 34.31 reflecting that subjects can work for longer duration on the machine without fatigue as compared with the traditional manual operation.     

Mutagens in commercial food processing and its microbial transformation

Food Science and Biotechnology - Mutagens are chemical molecules that have the ability to damage DNA. Mutagens can enter into our body upon consumption of improperly cooked or processed food...