Synthesis and biological evaluation of chromanone-based derivatives as potential anti-neuroinflammatory agents.

As a privileged scaffold, chromanone has been extensively introduced in the design of drug leads with diverse pharmacological features, particularly in the area of inflammatory diseases. Herein, the preparation of chromanone-based derivatives (4a-4i) was smoothly achieved, and their structures were characterized using H NMR, C NMR, and ESI-HRMS spectroscopy techniques. Out of them, analogue 4e exhibited the most potent inhibitory capacity against the NO release and iNOS expression, without apparent cytotoxicity.

The NDUFV2 gene silencing inhibits the proliferation of two drug-resistant cancer cell lines.

Background: Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. It is unlikely that there will ever be a single cure for cancer, but the development of molecular biology and cell biology has brought new options for cancer treatment. Our research group found in the preliminary experiments that AAs exhibited significant anti-tumor activity.

Three new antitumor annonaceous acetogenins from the seeds of Annona squamosa.

Two new annonaceous acetogenins squamocin P (2) and annosquatin III (3) and one new ACG precursor dieporeticenin B (1) along with five known precursors (4-8) were isolated from the seeds of Annona squamosa. Their structures were ascertained by chemical methods and various spectral evidences. These compounds showed inhibitory effects against three multidrug-resistant (MDR) cancer cell lines.

Antitumor activity of Annona squamosa seed oil.

Context: Custard apple (Annona squamosa Linn.) is an edible tropical fruit, and its seeds have been used to treat "malignant sore" (cancer) and other usage as insecticide. A comparison of extraction processes, chemical composition analysis and antitumor activity of A.

[Structure activity relationship of annonaceous acetogenins against multidrug resistant human lung cancer cell line A549/Taxol in vitro].

10 kinds of annonaceous acetogenins were selected for antitumor activity testing against human lung cancer cell line A549/Taxol and the structure activity relationship was analyzed.MTT assay was used to detect the inhibitory activities of 10 kinds of annonaceous acetogenins and positive drugs against A549/Taxol cells, respectively uvariamicin-Ⅲ(1), uvariamicin-Ⅱ(2), annosquacin D(3), desacetyluvaricin(4), annosquatin A(5), squamostatin D(6), bullatacin(7), squamocin(8), motrilin(9), annosquatin B(10), verapamil and cisplatin. Annonaceous acetogenins showed significant inhibitory activities against A549/Taxol cells, and were more potent than the positive drug verapamil and cisplatin.

Metabolomics study on the toxicity of Annona squamosa by ultraperformance liquid-chromatography high-definition mass spectrometry coupled with pattern recognition approach and metabolic pathways analysis.

Ethnopharmacological Relevance: Annona squamosa Linn (Annonaceae) is a commonly used and effective traditional Chinese medicine (TCM) especially in the South China. The seeds of Annona squamosa Linn (SAS) have been used as a folk remedy to treat "malignant sores" (cancer) in South of China, but they also have high toxicity on human body.

Aim Of The Study: To discover the potential biomarkers in the mice caused by SAS.