Current Medicinal Chemistry - Volume 32, Issue 20, 2025

The beneficial effects of curcumin against various chronic disorders have been shown in the last few decades. However, due to its low bioavailability, therapeutic effects are less than expected. Piperine has been used in scientific evaluations as an effective compound to increase the bioavailability of curcumin. The present review investigated the impact of curcumin plus piperine intake on oxidative stress and inflammatory markers of Randomized Clinical Trials (RCTs).

Using relevant keywords, we searched Cochrane Library, Scopus, PubMed, and Web of Science between January 1^st, 1970, and September 30^th, 2022. A comprehensive search for RCTs was performed. Continuous data were pooled by Standard Mean Difference (SMD) and 95% confidence interval. All related statistical analyses were performed using Comprehensive Meta-Analysis (CMA) software.

A total of 13 articles were incorporated into the final meta-analysis. According to the current meta-analysis, curcumin plus piperine administration showed a significantly increased SOD activity and GSH levels while significantly decreased MDA concentrations. In addition, our study revealed that curcumin plus piperine significantly decreased TNF-α and IL-6 concentrations.

These results indicated that curcumin plus piperine administration could effectively reduce oxidative stress and inflammation.

Organoselenium (OSe) agents and Schiff bases have demonstrated immense potential in the pharmaceutical field due to their broad spectrum of medicinal activities.

We herein report the antitumor activities of bis diselenide-based Schiff bases (3a-3c) derived from bis(4-aminophenyl)diselenide 2 and organoselenide-based Schiff bases (5a-c) derived from p-(methylselanyl)phenyl amine (4). The antitumor activity was estimated against fifteen cancer cell lines. Also, the growth inhibition percentage (GI%) of the Schiff bases tethered OSe compounds was evaluated against two normal cell lines, namely, human skin fibroblasts (HSF) and olfactory ensheathing cell line (OEC), to estimate the potential safety and selectivity. Furthermore, the cytotoxic inhibitory concentration 50 (IC50) was assessed against the cancer cell lines with the most outstanding GI% using the SRB assay.

Compounds 3a, 3b, 3c, and 5a showed the lowest IC50 values compared to those of doxorubicin (DOX) against HCT116, HEPG2, A549, MDA-MB-468, and FaDu cancer cell lines, respectively, especially against the HCT116 subtype, assuring their potential anticancer activity. On the other side, the apoptotic potentials of the most active compounds (3a, 3b, 3c, and 5a) were also evaluated for apoptosis-related genes (P53, BAX, caspases 3, 6, 8, and 9, MMP2, MMP9, and BCL-2). Interestingly, compounds 3a, 3b, 3c, and 5a upregulated P53, BAX, and caspases 3, 6, 8, and 9 by (2.66, 2.26, 2.44, and 2.57)-, (1.62, 1.52, 1.37, and 1.47)-, (1.87, 1.75, 2.02, and 1.75)-, (1.96, 1.74, 2.06, and 2.30)-, (4.25, 3.78, 3.53, and 3.96)-, and (2.04, 1.72, 1.90, and 1.63)-fold change, respectively. Furthermore, MMP2, MMP9, and BCL-2 were downregulated by (0.39, 0.51, 0.33, and 0.28)-, (0.29, 0.32, 0.37, and 0.41)-, and (0.42, 0.35, 0.29, and 0.38)-fold-change, upon treatment with compounds 3a, 3b, 3c, and 5a, respectively, assuring the apoptotic potentials. Finally, molecular docking also greatly recommends the potential activity of the examined candidates (especially 3a and 3c) against the GSTP1 receptor as a recommended mechanism for their antitumor activity.

Our findings point to significant anticancer activities of Schiff bases tethered OSe agents, suggesting their promising potential for development as effective anticancer drugs.

Aptamers are increasingly applied in cancer research. Here, we have performed the first bibliometric analysis to demonstrate the evolution of aptamers in cancer research over the past decade and to reveal future trends.

Original articles and reviews on aptamers in cancer research published from 2013 to 2022 were retrieved from the Web of Science Core Collection database. VOSviewer, CiteSpace, and R software were used for bibliometric analysis of the literature and visualization of the results.

A total of 1627 eligible publications were analyzed. Annual and cumulative publications have been found to be steadily increased. China was the most productive country (884 publications) and Hunan University was the most productive institution (97 publications). The United States had the highest level of international collaboration (betweenness centrality = 0.55). Wei-Hong Tan was the most productive author (68 publications) and Craig Tuerk was the most cited author (387 citations). Analytical Chemistry and Biosensors and Bioelectronics were the most influential journals in this field. Three major themes were identified: aptamer selection techniques, aptamer-targeted drug delivery, and aptasensors for cancer detection. The research hotspots have shifted from aptamer selection, targeted drug delivery, molecular imaging, and biomarker detection to electrochemical aptasensors and therapeutic applications. The future may focus on high specificity and affinity in aptamer selection, aptasensor fabrication, aptamer-targeted drug delivery, and therapeutic aptamer development.

The field of aptamers in cancer research has been steadily developing over the past decade, and future research may focus on aptamer application in cancer detection and therapy and the improvement of aptamer selection.

This study was designed to develop a ferroptosis-related gene signature for guiding the prognostic prediction in colorectal cancer (CRC) and to explore the potential in the molecular functions of the gene signature.

Ferroptosis is mainly characterized by lipid peroxide accumulation on the cell membranes in an iron-dependent manner, resulting in cellular oxidative stress, metabolic disorders, and, ultimately, cell death. This study aimed to develop a prognostic ferroptosis signature in CRC and explore its potential molecular function.

The present work was designed to devise a ferroptosis signature for CRC prognosis and explore its potential molecular function.

Single-cell RNA sequencing data GSE161277 and transcriptome sequencing data GSE17537 and TCGA-CRC from the Gene Expression Omnibus (GEO) and the Cancer Genome Atlas (TCGA) databases were downloaded, respectively. Quality control, dimension reduction, clustering, and clustering of single-cell RNA sequencing (scRNA-seq) data were performed using the Seurat package. A total of 259 ferroptosis-correlated genes from the FerrDb database were acquired. The single sample gene set enrichment analysis (ssGSEA) was performed to calculate the scores of genes related to ferroptosis. ESTIMATE was used to calculate immune infiltration. Independent prognostic factors were determined by performing Weighted Gene Co-Expression Network Analysis (WGCNA), univariate and Cox analyses, and Lasso analyses were used to search for independent prognostic factors.

From the scRNA-seq (GSE161277) dataset, 22 cell clusters were initially identified, and according to immune cell markers, only 8 types of cells (Follicular B, central memory T cell, Epithelial, Natural killer T cell, Plasma B, M1 macrophage, Fibroblasts, and Mast cell) were finally determined to be related to CRC prognosis. The results of the scRNA-seq analysis showed that the score of ferroptosis-related genes was higher in tumour tissues and in 8 types of cells in tumour samples. In the TCGA dataset, CRC samples were divided into ferroptosis-related high scores, ferroptosis-related median scores, and ferroptosis-related low scores. Immune cell analysis revealed that ferroptosis-related high scores had the highest abundance of immune cells. An 11-gene signature was developed by WGCNA, univariate Cox, and Lasso Cox regression. The prediction ability of the signature was successfully validated in the GSE17537 dataset. A comprehensive nomogram combining the 11 signature genes and clinical parameters could effectively predict the overall survival of CRC patients.

The present molecular signature established based on the 11 ferroptosis-related genes performed well in assessing CRC prognosis. The present discoveries could inspire further research on ferroptosis, providing a new direction for CRC management.