With the adjustment of human diet and lifestyle changes, the prevalence of obesity is increasing year by year. Obesity is closely related to the excessive accumulation of white adipose tissue (WAT), which can synthesize and secrete a variety of adipokines. Apelin is a biologically active peptide in the adipokines family. Past studies have shown that apelin plays an important regulatory role in the pathogenesis and pathophysiology of diseases such as the cardiovascular system, respiratory system, digestive system, nervous system, and endocrine system. Apelin is also closely related to diabetes and obesity. Therefore, we anticipate that apelin-13 has an effect on lipometabolism and intend to explore the effect of apelin-13 on lipometabolism at the cellular and animal levels. In in vitro experiments, amidation-modified apelin-13 can significantly reduce the lipid content; TG content; and the expression of PPARγ, perilipin mRNA, and protein in adipocytes. Animal experiments also show that amidation modification apelin-13 can improve the abnormal biochemical indicators of diet-induced obesity (DOI) rats and can reduce the average diameter of adipocytes in adipose tissue, the concentration of glycerol, and the expression of PPARγ and perilipin mRNA and protein. Our results show that apelin-13 can affect the metabolism of adipose tissue, inhibit adipogenic differentiation of adipocytes, promote lipolysis, and thereby improve obesity. The mechanism may be regulating the expression of PPARγ to inhibit adipogenic differentiation and regulating the expression of perilipin to promote lipolysis. This study helps us understand the role of apelin-13 in adipose tissue and provide a basis for the elucidation of the regulation mechanism of lipometabolism and the development of antiobesity drugs.
Objective. The effects of apelin-13 on the expression of Bcl-2 and caspase-3 factors and the apoptosis of adipocytes were studied at the cellular and animal levels. Methods. 3T3-L1 preadipocytes were cultured and grouped. The third-generation cells were added to the control DMSO solvent and amidation-modified apelin-13. The expression of Bcl-2 and caspase-3 were detected. The cell growth viability and cell apoptosis were detected. DOI model rats were established. The effects of apelin-13 on DOI rat biochemical indicators, the expression of Bcl-2, caspase-3, and cell apoptosis were investigated by injecting amidation-modified apelin-13 through the tail vein. Result. In in vitro experiments, amidation-modified apelin-13 can significantly reduce the growth viability of adipocytes and the expression of Bcl-2, increase the expression of caspase-3, and promote the apoptosis of adipocytes. Animal experiments also show that apelin-13 modified by amidation can adjust the abnormal biochemical indicators of DOI rats, decrease the expression of Bcl-2 in adipose tissue, increase the expression of caspase-3, and promote the apoptosis of adipocytes. Conclusion. Amidation of apelin-13 can promote fat cell apoptosis and reduce the incidence of obesity. The mechanism may be accomplished by inhibiting Bcl-2 and caspase-3 factors. This study helps us understand the effect of apelin-13 on fat cell apoptosis and hopes to provide a basis for the development of antiobesity drugs.
Aptamers are artificial single-stranded DNA or RNA sequences, usually 20-60 bases long, that fold into secondary and tertiary structures, which enables their binding to a wide range of targets, including amino acids, drugs, proteins or even entire cells, with high affinity and specificity. Generally synthesized through an in vitro selection and amplification process known as the SELEX (systematic evolution of ligands by exponential enrichment), selected aptamers have dissociation constants ranging from nanomolar to picomolar level. Nanotechnology is the manipulation of matter on an atomic and molecular scale, generally in the 1-100 nm dimension range. The many unique physicochemical properties of nanoparticles include their ultra-small size, large surface area-to-mass ratio, and high reactivity, making them different from bulk materials and overcoming some of the limitations found in traditional therapeutic and diagnostic agents. By combining both technologies, aptamer-conjugated nanoparticles offer new opportunities for applications in biomedicine, including early diagnosis and drug delivery. This review summarizes the recent developments in aptamer-mediated drug delivery for therapeutics based on aptamer conjugation with a variety of nanoparticles.
Colorectal cancer (CRC) has become one of the top ten malignant tumors with a high incidence rate and mortality. Due to the lack of a good CRC screening program, most of the CRC patients are being transferred at the time of treatment. The conventional treatment cannot effectively improve the prognosis of CRC patients, and the target drugs can significantly prolong the overall survival of patients in the advanced stage. However, the use of single drug may lead to acquired drug resistance and various serious complications. Therefore, combined targeted drug therapy is the main alternative treatment with poor effect of single targeted drug therapy, which has important research significance for the treatment of CRC. Therefore, this study intends to culture CRC cell lines in vitro at the cell level and intervene with the GLP-1 receptor agonist liraglutide. The effects of liraglutide on the PI3K/Akt/mTOR signal pathway and CRC cell proliferation, cycle, migration, invasion, and apoptosis are explored by detecting cell proliferation, cycle, migration, invasion, and apoptosis and the expression of related mRNA and protein. The results showed that liraglutide, a GLP-1 receptor agonist, could block the CRC cell cycle, reduce cell proliferation, migration, and invasion and promote apoptosis by inhibiting the PI3K/Akt/mTOR signal pathway.
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