RESUMO
Alzheimer's disease (AD) is a neurological condition currently with 47 million people suffering from it globally. AD might have many reasons such as genetic issues, environmental factors, and Aß accumulation, which is the biomarker of the disease. Since the primary reason is unknown, there is no targeted treatment at the moment, but ongoing research aims to slow its progression by managing amyloid-beta peptide production rather than symptomatic improvement. Since phytochemicals have been demonstrated to possess antioxidant, anti-inflammatory, and neuroprotective properties, they may target multiple pathological factors and can reduce the risk of the disease. Curcumin, as a phytochemical found in turmeric known for its antioxidant, free radical scavenging properties, and as an antiamyloid in treating AD, has come under investigation. Although its low bioavailability limits its efficacy, a prominent drug delivery system (DDS) is desired to overcome it. Hence, the potency of lipid-based nanoparticles encapsulating curcumin (LNPs-CUR) is considered in this study as a promising DDS. In vivo studies in animal models indicate LNPs-CUR effectively slow amyloid plaque formation, leading to cognitive enhancement and reduced toxicity compared to free CUR. However, a deeper understanding of CUR's pharmacokinetics and safety profile is crucial before LNPs-CUR can be considered as a medicine. Future investigations may explore the combination of NPs with other therapeutic agents to increase their efficacy in AD cases. This review provides the current position of CUR in the AD therapy paradigm, the DDS suggestions for CUR, and the previous research from the point of analytical view focused on the advantages and challenges.
RESUMO
C-N cross-coupling bond formation reactions have become valuable approaches to synthesizing anilines and their derivatives, known as important chemical compounds. Recent developments in this field have focused on versatile catalysts, simple operation methods, and green reaction conditions. This review article presents an overview of C-N cross-coupling reactions in pharmaceutical compound synthesis reports. Selected examples of N-arylation reactions of various nitrogen-based compounds and aryl halides are defined for preparing pharmaceutical molecules.
RESUMO
Recombinant human erythropoietin (rHuEPO) as a glycoprotein growth factor has been considered a biological drug for treatment of anemic patients with chronic renal failure or who receive cancer chemotherapy. Biological activity and circulation time are 2 parameters that are important to achieve EPO's efficacy. Previous efforts for increasing EPO's efficacy have focused on glycosylation modification via adding more sialic acid antenna and generates more negative charged protein. Evidences cleared that EPO's activity increased by numbers of N-glycan moieties with presence of sialic acids at their terminus. Correlation between bioactivity and glycosylation with terminal sialylation is theoretically achieved using the calculation of the amount of charge profile of the EPO variants called "I-number." Here, we studied and compared the relationship between bioactivities of different EPOs that contained various I-numbers and the effect of their secondary and tertiary protein structures on measured in vivo efficacy. Eight recombinant EPOs batches were produced under the same condition. I-numbers found out by EPO's charge profiles determination using capillary electrophoresis and activities were studied upon erythroid precursor cell stimulation in mice. Analyzing the bioactivity, I-number, and structural studies revealed that in spite of I-number, conformational changes in protein structure and presence of aggregated species impact bioactivity substantially.
