Search

[Display omitted] • Six C-3′-C-6″ type of biflavonoids were isolated from S. trichoclada. • RF-A showed the strongest activity against MCF-7 cells among all isolated compounds. • RF-A induced the accumulation of ROS and Lipid peroxidation in MCF-7 cells. • RF-A induced ferroptosis in MCF-7 cells via the upregulation of VDAC2 protein. Breast cancer is one of the major malignant tumors in females, and currently, recurrence and metastasis are the main obstacles preventing effective breast cancer treatment. Biflavonoids of secondary metabolites from plants are excellent anticancer agents to fight sensitive and resistant breast cancer cell lines. In this study, six C-3′-C-6″ biflavonoids, including one new robustaflavone A (1 , RF-A) and five known robustaflavone derivatives (2 – 6) , were isolated from Selaginella trichoclada for the first time. We aimed to evaluate the inhibitory effects of compounds 1 – 6 against human breast cancer MCF-7 cells. Among the six compounds, RF-A showed the strongest activity, decreasing cell viability with an IC 50 value of 11.89 μΜ. Furthermore, RF-A strikingly induced MCF-7 nonapoptotic cell death through ferroptosis by enhancing the expression of VDAC2 channels and reducing the expression of Nedd4 E3 ubiquitin ligase, leading to lipid peroxidation and ROS production. The results suggested that RF-A has potential as a novel breast cancer treatment through its regulation of the mitochondrial VDAC2 and Nedd4 pathways. [ABSTRACT FROM AUTHOR]

• The structure of polyhydroxy serratene triterpenoids is quite novel. • All compounds revealed selective cytotoxicities against MCF-7 cells. • Biosynthetic pathways of compounds were proposed. • UV spectrums provide some references for the structure of serratene triterpenoids. Phytochemical investigation of the 70% aqueous EtOH extract of Lycopodium complanatum led to six new polyhydroxy serratene triterpenoids (serrat A-F, 1 – 6), along with a known analogue (7). Their structures and configurations were elucidated by data analysis of HRESIMS, 1D and 2D NMR, in combination with comparisons of reported experimental spectroscopic data. All the isolates were evaluated cytotoxic activities against HepG2 cells, MCF-7 cells and series human lung cancer cell lines A549, Calu-6, NCI-H441, NCI-H226 and NCI-H1975. The results indicated that certain compounds inhibited proliferation of human cancer cells. Moreover, all compounds possessed selective cytotoxic activities on MCF-7 cells. Further, possible biosynthesis pathways of these compounds were proposed. [ABSTRACT FROM AUTHOR]

• Eight new serratane triterpenoids were isolated from Lycopodium complanatum. • The absolute configurations of 6 – 8 were determined by DFT GIAO 13C NMR calculations. • The cytotoxic activities were assessed on seven different human cancer cell lines. • All compounds could inhibit the NO release of RAW 264.7 cells induced by LPS. Phytochemical investigation of the ethyl acetate fraction of Lycopodium complanatum led to eight new serratane triterpenoids (lycomplanatums A-H, 1 – 8), along with five known analogues (9 – 13). Their structures were elucidated by extensive spectroscopic methods, including 1D/2D NMR, HRESIMS, and DFT GIAO 13C NMR calculation. Among them, compounds 2 and 13 showed moderate antiproliferative effects against seven human cancer cell lines, especially for MCF-7 with IC 50 values of 13.8–44.7 μM. Additionally, the compounds were screened for anti-inflammatory effects based on their inhibitory activities of nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 cells, and compounds 2 and 13 diminished NO production more potently than others in a concentration-dependent manner. [ABSTRACT FROM AUTHOR]

• Chalcone analogues containing a thieno[2,3- d ]pyrimidin-2-yl group were synthesized and evaluated as anti-tumor agents. • Compound 8d was the most potent analogue, with IC 50 values ranging between 2.65 and 11.44 μM in seven cancer cell lines. • Compound 8d induced an accumulation of HCT-116 cells in the sub-G1 phase. • 8d -induced apoptosis was confirmed by Annexin-V, JC-1, H2DCFDA and MitoSox™ Red staining assays. • The mitochondrial death pathway might be involved in 8d -induced apoptosis in HCT-116 cells. Many natural or synthetic chalcones have potential anti-tumor activity. Here, we synthesized two series of chalcone analogues containing a thieno[2,3- d ]pyrimidin-2-yl group and evaluated for their cytotoxic activity towards cultured human lung cancer A549 and colorectal HCT-116 cells. Among them, compound 8d was the most cytotoxic against HCT-116 cells, with an IC 50 value of 2.65 μM. Analyses of the phenotypic changes induced by this compound found a dose-dependent accumulation of HCT-116 cells in sub-G1 phase, indicating that compound 8d might induce apoptosis. Furthermore, we found that 8d triggered mitochondrial membrane potential depolarization, promoted reactive oxygen species formation in HCT-116 cells, and increased the percentage of early and late apoptotic cells. Finally, immunoblotting indicated that 8d increased PARP-1 and caspases 3, 7 and 9 cleavage. These data suggest that compound 8d induces apoptosis via the mitochondrial death pathway. [ABSTRACT FROM AUTHOR]