The combretastatins (cis-stilbenoid molecules) have received significant interest because of their simple chemical structures, excellent antiproliferative activity, and novel anti-tubulin molecular mechanism of action. Significant efforts have been carried out aiming at stabilizing the active cis-isomers. A new series of cis-vinylamide derivatives containing trimethoxyphenyl moiety were synthesized and characterized. Their anticancer activities were evaluated in vitro against MCF-7 breast cancer cell line. Compounds 2f, 3, and 5 displayed potent cytotoxic activity against the breast cancer cell line compared with CA-4 as the reference compound. The microtubule polymerization assay and flow cytometry analysis confirmed that the cytotoxic activity of compound 3 was related to inhibitory activity against tubulin polymerization. Compound 3 showed pro-apoptotic activity by inducting a significant increase in the percentage of pre-G1 phase in DNA flow cytometry compared to untreated control. The pro-apoptotic activity of compound 3 was inferred by a significant increase in the percentage of fluorescent annexin V/PI positive apoptotic cells. It also increased the level of caspase 3 compared to the untreated control.

Few researches have explored the production of pharmaceuticals from aquatic plants. Therefore, this study explored, for the first time, the phytochemical composition and bioactivities of ten aquatic plants. Aquatic plant shoots from various Nile River canals were collected, dried, and ground for aqueous extract preparation. Phytochemical composition and antioxidant capacity were assessed using DPPH assays. Extracts were tested for antiparasitic, antibacterial, anti-biofilm, and anticancer activities through standard in vitro assays, measuring IC₅₀ values, and evaluating mechanisms of action, including cell viability and high-content screening assays. The results showed that the aquatic plants were rich in pharmaceutical compounds. The antioxidant capacity of these extracts exceeded that of vitamin C. The extracts showed promising antiparasitic activity against pathogens like Opisthorchis viverrini and Plasmodium falciparum, with IC₅₀ values between 0.7 and 2.5 µg/mL. They also demonstrated low MICs against various pathogenic bacteria, causing DNA damage, increased plasma membrane permeability, and 90% biofilm inhibition. In terms of anticancer activity, extracts were effective against a panel of cancer cell lines, with Ludwigia stolonifera exhibiting the highest efficacy. Its IC₅₀ ranged from 0.5 µg/mL for pancreatic, esophageal, and colon cancer cells to 1.5 µg/mL for gastric cancer cells. Overall, IC₅₀ values for all extracts were below 6 µg/mL, showing significant apoptotic activity, increased nuclear intensity, plasma membrane permeability, mitochondrial membrane permeability, and cytochrome c release, and outperforming doxorubicin. This study highlights the potential of aquatic plants as sources for new, safe, and effective drugs with strong antiparasitic, antibacterial, and anticancer properties.

There is a shortage in the experimental research directly comparing the effectiveness of different nanoparticles in boosting asparaginase (ASNase) activity. This study assessed the impact of various nanoparticles on enhancing ASNase activity, stability, and anticancer effects through immobilization. Escherichia coli ASNase was immobilized on different nanoparticles, and its efficiency was measured. The research included analyzing the enzyme’s secondary structure, stability, activity at different temperatures, kinetic parameters, shelf life, and activity in blood serum. The anticancer efficacy was determined by measuring the IC₅₀. The study also investigated the anticancer mechanisms by examining the enzyme’s toxicity on cancer cells, focusing on apoptosis indicators like nuclear intensity, membrane permeability, mitochondrial membrane permeability, and cytochrome c release. Among the tested nanoparticles, nano chitosan yielded the best improvements. ASNase immobilized on nano chitosan reached 90% immobilization efficiency fastest among the studied nanoparticles, achieving this within 72 h, whereas other nanoparticles took 120 h. Immobilization modified ASNase’s secondary structure by increasing alpha helices and reducing random coils, with nanochitosan and magnetic iron oxide showing the most pronounced effects. Immobilized ASNase exhibited enhanced activity, stability across temperature (widest with nanochitosan, 25–65 °C), and a broader optimal pH range compared to the free enzyme, with a K_m of 1.227 mM and a V_max of 454.54 U/mg protein. Notably, the nano-chitosan-immobilized ASNase retained over 85% of its activity after 9 months of storage and maintained high activity in blood serum. This improved stability and activity translated into the highest anticancer activity (Lowest IC₅₀) and was more effective than doxorubicin in disrupting cancer cell structures.