Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 25, Issue 12, 2025

The prevalent disease known as breast cancer has a significant impact on both men's and women's health and quality of life.

The aim of this study was to explore the potential roles of Lecaniodiscus cupanioides (planch.) extract and triterpenoid-derived gold nanoparticles (AuNPs) in cancer therapy, specifically targeting MCF-7 breast cancer cell lines.

Gold nanoparticles were synthesized utilizing triterpenoid (ZJ-AuNPs) and leaf extract from Lecaniodiscus cupanioides (LC-AuNPs). Fourier transform infrared spectroscopy (FTIR), Dynamic light scattering (DLS), High-resolution transmission electron microscopy (HRTEM), and UV-vis spectroscopy were employed to characterize the nanoparticles. Additionally, the MTT assay was used to assess the impact of AuNPs on cancer cell viability using MCF-7 breast cancer cell lines.

Analysis of ZJ-AuNPs and LC-AuNPs revealed DLS zeta potentials of -31.8 and -35.8 mV, respectively, and a corresponding UV-vis absorption maxima at 540 and 550 nm. Also, the ZJ-AuNPs and LC-AuNPs had respective zeta-sizes that ranged from 25.84 to 35.98 nm and polydispersive index values between 0.2360 and 0.773. Furthermore, the presence of the chemical groups -OH and -NH was shown to be necessary for the green method of capping and reducing the gold nanoparticles. Nevertheless, a significant decrease in cell viability percentages was noted in the MTT experiment, accompanied by an increase in the quantity or concentration of the nanoparticles for both ZJ-AuNPs and LC-AuNPs.

Given the data obtained in this study, the biosynthesized ZJ-AuNPs and LC-AuNPs were shown to possess potent cytotoxic effects on breast cancer cells. Hence, they may be valuable tools in the development of new cancer chemotherapy drugs.

Anlotinib has demonstrated durable clinical benefits in patients with unresectable or metastatic bone and soft-tissue sarcomas.

92 patients treated with chemotherapy combined with or without anlotinib were collected and analyzed. The objective response rate (ORR) and disease control rate (DCR) were analyzed. Long-term survival was assessed using the Kaplan-Meier method, including median progression-free survival (mPFS) and overall survival (mOS).

Liposarcoma, synovial sarcoma, and rhabdomyosarcoma were the primary pathological subtypes of the 92 patients. The median age was 46 (range, 11-75) years. The ORR and DCR of the anlotinib-chemotherapy combination used as first-line therapy were 31.9% and 85.1%, respectively. However, the ORR and DCR were only 6.7% and 57.8% in the chemotherapy alone, respectively. Compared with the chemotherapy group, improvements were observed in the mPFS and mOS with anlotinib-based regimen (mPFS, 8.3 vs. 3.0 months; mOS, 59.0 vs. 22.0 months). Anlotinib-associated adverse events were well tolerated and mainly occurred in grades I and II. New anlotinib-related adverse reactions were not noted.

Anlotinib-based regimen as a first-line therapy showed a positive effect on the treatment of unresectable or metastatic BSTSs. The anlotinib-associated adverse events were minor and well tolerated.

This study aims to enhance the delivery of polyphenols using nanotechnology.

To develop and evaluate liposomal formulations for improved delivery and stability of polyphenols, specifically focusing on Rutin.

Liposomal formulations were meticulously prepared via the Thin-Film Hydration method. Comprehensive physical characterization was conducted, including stability assessments using Dynamic Light Scattering (DLS) and Thermogravimetric Analysis (TGA). The free radical scavenging activity was measured using the DPPH• assay, and MTT cell viability assays were performed to assess anti-proliferative effects.

The results demonstrated a significant reduction in nanoparticle size from 123 nm to 116 nm and an increase in charge from -14 to -22 with rising Rutin concentrations. The formulation achieved enhanced homogeneity at a Rutin concentration of 2.0 mg/mL and showed higher stability. Incorporating Rutin improved the formulation's stability over 30 days, as evidenced by a decrease in the Differential Scanning Calorimetry peak temperature from 58.65°C to 54.42°C. Rutin-loaded and co-loaded nanoliposomes exhibited remarkable selectivity against PANC1 and MCF7 cell lines, with IC50 values of 2.13±0.35 μg/mL and 4.75±0.19 μg/mL, respectively.

PEGylated Rutin-loaded nanoliposomes offer a promising platform for biodegradable and biocompatible drug delivery systems, enhancing the bioavailability, solubility, and stability of the polyphenols.

In this study, 25 synthetic cyclic lipopeptides (CLPs) were investigated for their anticancer potential against mouse melanoma (B16F10) cells, human prostate cancer (PC-3), human colorectal adenocarcinoma (HT-29) and mouse embryonic fibroblast (NIH3T3) cells.

The cytotoxic activity of investigated compounds was evaluated using MTT and CV assays. In order to examine the mechanism of action of the most potent compound cell cycle analysis, apoptosis assay, caspase activity, CFSE and DHR staining, DAF-FM, autophagy and immunocytochemistry caspase-3 assays were performed.

During the fast screening, compound 9, was identified as prospective active CLP against B16F10 cell line at 10 µM concentration. MTT and CV assays exhibited at least four times higher cytotoxic potential of 9 (IC50 = 8.4±1.3 µM, MTT; 10.6±1.1 µM, CV) in comparison to control drug natural occurring CLP surfactin (IC50 = 50.3±0.6 µM, MTT; 40.4±0.3 µM, CV). The use of flow cytometry analysis confirmed that apoptosis was involved in the death of B16F10 cells after treatment with 9, as demonstrated also by DAPI staining. Caspase activity could be detected during cell death (ApoStat assay, immunocytochemistry caspase-3 assay). Compound 9 provokes enhancement of nitric oxide (NO) production in B16F10 cells but does not trigger ROS/RNS generation or autophagy.

The study highlights that synthetic macrocycle 9 has superior tumor-specificity and potential as an anticancer agent compared to surfactin and cisplatin. These findings could guide the development of more selective and less harmful macrocyclic lipopeptides for cancer therapy.