Cancer Studies

Design, syntheses and biological evaluation of natural product aiphanol derivatives and analogues: Discovery of potent anticancer agents.

A recent study investigated the anticancer properties of aiphanol, a natural product found in traditional Chinese medicine. The researchers discovered that aiphanol can inhibit angiogenesis and tumor growth by blocking the VEGF/VEGFRs and COX2 signaling pathways. They designed and synthesized 40 derivatives and analogues of aiphanol, and two of them, 10j and 14c, showed the strongest inhibition of tumor cell growth across various cell lines. These analogues had 80 times greater potency than the original compound. The study also revealed that the presence of a specific substrate at the 7-position of benzo 1,4-dioxane is crucial for the anticancer activity. Molecular docking experiments showed that compound 14c binds tightly to both VEGFR2 and COX2. Overall, compounds 10j and 14c hold promise as potential candidates for future development of anticancer agents.

Yao L et al (2023).
Bioorg Med Chem Lett.
PubMed:
37182611

Exploring the therapeutic mechanisms of Gleditsiae Spina acting on pancreatic cancer via network pharmacology, molecular docking and molecular dynamics simulation.

The dried spines of Gleditsia sinensis Lam, known as "Gleditsiae Spina," contain various chemical components. This study used network pharmacology, molecular docking, and molecular dynamics simulations to investigate the potential of Gleditsiae Spina for treating pancreatic cancer. The study identified common targets such as AKT1, TP53, TNFα, IL6, and VEGFA. Critical pathways involved fisetin, eriodyctiol, kaempferol, and quercetin. The MD simulations showed that eriodyctiol and kaempferol had stable hydrogen bonds and high binding free energy for TP53. These findings can help explore leading compounds and potential drugs for pancreatic cancer.

Duan H et al (2023).
RSC Adv.
PubMed:
37181515

Therapeutic effects of Crataegus monogyna inhibitors against breast cancer.

A recent study combines data mining, network pharmacology, and docking analysis to potentially revolutionize breast cancer treatment. By exploring prestigious phytochemicals, the study identifies bioactive compounds in a particular plant that may alter target genes implicated in breast cancer. Docking analysis and simulation studies support these findings. The study proposes six key compounds that contribute to breast cancer development by affecting specific proteins. This integration of network pharmacology and bioinformatics provides convincing evidence for the potential of this plant to alleviate breast cancer and paves the way for further experimental research.

Basavarajappa GM et al (2023).
Front Pharmacol.
PubMed:
37180727

An In Vitro and In Vivo Assessment of Antitumor Activity of Extracts Derived from Three Well-Known Plant Species.

This study evaluated the antitumor activity of extracts from three plant species: L., L., and L. Using HPLC-MS analysis, the phytochemical profile of the extracts was determined. In vitro screening revealed that L. extracts had the strongest anticancer and antioxidant effects. In vivo assessment using a mouse model showed that administration of L. and green coffee bean extracts reduced ascites cell viability and oxidative stress in tumor samples. Combining chemotherapy with L. or L. extracts induced lipid peroxidation in tumor cells, decreasing tumor viability. These findings suggest that L. extract, especially, has potential as an anticancer agent when used in combination with chemotherapy.

Gligor O et al (2023).
Plants (Basel).
PubMed:
37176897

Cinnamaldehyde-Rich Cinnamon Extract Induces Cell Death in Colon Cancer Cell Lines HCT 116 and HT-29.

This study found that a cinnamon extract containing cinnamaldehyde has anti-cancer effects on colorectal cancer cells by inhibiting cell viability, proliferation, migration, inducing cell cycle arrest, causing mitochondrial stress, and activating apoptotic proteins.

Nile A et al (2023).
Int J Mol Sci.
PubMed:
37175897

Pulsatilla Saponins Inhibit Experimental Lung Metastasis of Melanoma via Targeting STAT6-Mediated M2 Macrophages Polarization.

Pulsatilla chinensis (Bge.) Regel, a traditional Chinese medicine, inhibits M2 macrophage polarization via the STAT6 pathway, reducing tumor progression and metastasis.

Yang X et al (2023).
Molecules.
PubMed:
37175092

Andrographolide induced ferroptosis in multiple myeloma cells by regulating the P38/Nrf2/HO-1 pathway.

Andrographis paniculata is a functional food used in Asia. Andrographolide (Andro), derived from it, has potent anticancer properties. This study shows that Andro induces ferroptosis (iron-dependent cell death) in multiple myeloma cells through the P38/Nrf2/HO-1 pathway, suggesting a potential treatment for the disease.

Li W et al (2023).
Arch Biochem Biophys.
PubMed:
37172672