A new oxoaporphine and liriodenine’s anti-neuroblastoma potential from the roots of Polyalthia bullata King

Polyalthia bullata King’s root yielded a new compound named 5-methylliridine (1) in addition to six previously identified compounds. These known compounds include liriodenine (2), 11-methoxyliriodenine (3), lysicamine (4), onychine (5), 5-hydroxy-6-methoxyonychine (6), and 8-methoxyeupolauridine (7). The structures of compounds 1-7 were determined through spectroscopic analysis. Liriodenine (2) exhibited a remarkable ability to decrease the cell viability of cancerous N2A cells to 22% within a 24 h timeframe, indicating its potential as an anti-neuroblastoma agent. Molecular docking results additionally suggested that oxoaporphines (1-4) have the potential to act as inhibitors of protein kinases. These findings highlight the therapeutic potential of P. bullata constituents in cancer treatment, particularly neuroblastoma, and contribute to understanding its medicinal properties

Chemical constituents and anti-neuroblastoma activity from Boesenbergia stenophylla

Three diarylheptanoids and one flavonoid, i.e. 7-(4-hydroxy-3-methoxyphenyl)-1-phenylhept-4-en-3-one (4), 5R-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenylheptan-3-one (5), 1,7-diphenylhept-4-en-3-one (6), and 3,5,7-trihydroxyflavone (7) were isolated and characterized from the rhizome of Boesenbergia stenophylla. Compounds 2 and 4 displayed excellent anti-neuroblastoma activity which reduces the cell viability to 30% and 20%, respectively. The results from the molecular docking experiments targeting the protein kinases regulating neuroblastoma cell survival (PI3K/AKT1 signalling pathway) are consistent with that of the in vitro results. Finally, the structures of 4-7 were elucidated using spectroscopic methods (UV, IR, NMR, and HRESIMS)

<i>Boesenbergia stenophylla</i>-Derived Stenophyllol B Exerts Antiproliferative and Oxidative Stress Responses in Triple-Negative Breast Cancer Cells with Few Side Effects in Normal Cells

Triple-negative breast cancer (TNBC) is insensitive to target therapy for non-TNBC and needs novel drug discovery. Extracts of the traditional herb Boesenbergia plant in Southern Asia exhibit anticancer effects and contain novel bioactive compounds but merely show cytotoxicity. We recently isolated a new compound from B. stenophylla, stenophyllol B (StenB), but the impact and mechanism of its proliferation-modulating function on TNBC cells remain uninvestigated. This study aimed to assess the antiproliferative responses of StenB in TNBC cells and examine the drug safety in normal cells. StenB effectively suppressed the proliferation of TNBC cells rather than normal cells in terms of an ATP assay. This preferential antiproliferative function was alleviated by pretreating inhibitors for oxidative stress (N-acetylcysteine (NAC)) and apoptosis (Z-VAD-FMK). Accordingly, the oxidative-stress-related mechanisms were further assessed. StenB caused subG1 and G2/M accumulation but reduced the G1 phase in TNBC cells, while normal cells remained unchanged between the control and StenB treatments. The apoptosis behavior of TNBC cells was suppressed by StenB, whereas that of normal cells was not suppressed according to an annexin V assay. StenB-modulated apoptosis signaling, such as for caspases 3, 8, and 9, was more significantly activated in TNBC than in normal cells. StenB also caused oxidative stress in TNBC cells but not in normal cells according to a flow cytometry assay monitoring reactive oxygen species, mitochondrial superoxide, and their membrane potential. StenB induced greater DNA damage responses (γH2AX and 8-hydroxy-2-deoxyguanosine) in TNBC than in normal cells. All these StenB responses were alleviated by NAC pretreatment. Collectively, StenB modulated oxidative stress responses, leading to the antiproliferation of TNBC cells with little cytotoxicity in normal cells