In the present study, three new aconitine-type diterpenoid alkaloids brochyponines A–C(1–3) were isolated from the roots of Aconitum brevicalcaratum. Their structures were established on the basis of extensive spect...In the present study, three new aconitine-type diterpenoid alkaloids brochyponines A–C(1–3) were isolated from the roots of Aconitum brevicalcaratum. Their structures were established on the basis of extensive spectroscopic analyses(IR, HR-ESI-MS, and 1D and 2D NMR). The NMR data of salt form for compound 1 in CDCl_3 were also measured.展开更多
Objective: To explore the proliferation inhibitory effect of quinones from Blaps rynchopetera defense secretion on colorectal tumor cell lines. Methods: Human colorectal cancer cell HT-29, human colorectal adenocarcin...Objective: To explore the proliferation inhibitory effect of quinones from Blaps rynchopetera defense secretion on colorectal tumor cell lines. Methods: Human colorectal cancer cell HT-29, human colorectal adenocarcinoma cell Caco-2 and normal human colon epithelial cell CCD841 were chosen for the evaluation of inhibitory activity of the main quinones of B. rynchopetera defense secretion, including methyl p-benzoquinone(MBQ), ethyl p-benzoquinone(EBQ), and methyl hydroquinone(MHQ), through methyl thiazolyl tetrazolium assay. The tumor-related factors, cell cycles, related gene expressions and protein levels were detected by enzyme-linked immunosorbent assy, flow cytometry, RT-polymerase chain reaction and Western blot, respectively. Results: MBQ, EBQ, and MHQ could significantly inhibit the proliferation of Caco-2, with half maximal inhibitory concentration(IC50) values of 7.04±0.88, 10.92±0.32, 9.35±0.83, HT-29, with IC50values of 14.90±2.71, 20.50±6.37, 13.90±1.30, and CCD841, with IC50values of 11.40±0.68, 7.02±0.44 and 7.83±0.05 μg/mL, respectively. Tested quinones can reduce the expression of tumor-related factors tumor necrosis factor α, interleukin(IL)-10, and IL-6 in HT-29 cells, selectively promote apoptosis, and regulate the cell cycle which can reduce the proportion of cells in the G1phase and increase the proportion of the S phase.Meanwhile, tested quinones could up-regulate mRNA and protein expression of GSK-3β and APC, while down-regulate that of β-catenin, Frizzled1, c-Myc, and CyclinD1 in the Wnt/β-catenin pathway of HT-29 cells.Conclusion: Quinones from B. rynchopetera defense secretion could inhibit the proliferation of colorectal tumor cells and reduce the expression of related factors, which would be functioned by regulating cell cycle, selectively promoting apoptosis, and affecting Wnt/β-catenin pathway-related mRNA and protein expressions.展开更多
基金financially supported by the National Natural Science Foundation of China(No.81460648)Guizhou Science and Technology Foundation of China(No.QKHJC[2018]1193)Yunling Scholars of Yunnan province,and Program for Excellent Young Talents,Yunnan University
文摘In the present study, three new aconitine-type diterpenoid alkaloids brochyponines A–C(1–3) were isolated from the roots of Aconitum brevicalcaratum. Their structures were established on the basis of extensive spectroscopic analyses(IR, HR-ESI-MS, and 1D and 2D NMR). The NMR data of salt form for compound 1 in CDCl_3 were also measured.
基金National Natural Science Foundation of China(No.81960755)Bio-pharmaceutical Major Project of Yunnan Province(No.202002AA100007)+1 种基金Yunnan Fundamental Research Project(No.202001AU070022)Program for Innovative Research Team of Yunnan Province(No.202305AS350001)。
文摘Objective: To explore the proliferation inhibitory effect of quinones from Blaps rynchopetera defense secretion on colorectal tumor cell lines. Methods: Human colorectal cancer cell HT-29, human colorectal adenocarcinoma cell Caco-2 and normal human colon epithelial cell CCD841 were chosen for the evaluation of inhibitory activity of the main quinones of B. rynchopetera defense secretion, including methyl p-benzoquinone(MBQ), ethyl p-benzoquinone(EBQ), and methyl hydroquinone(MHQ), through methyl thiazolyl tetrazolium assay. The tumor-related factors, cell cycles, related gene expressions and protein levels were detected by enzyme-linked immunosorbent assy, flow cytometry, RT-polymerase chain reaction and Western blot, respectively. Results: MBQ, EBQ, and MHQ could significantly inhibit the proliferation of Caco-2, with half maximal inhibitory concentration(IC50) values of 7.04±0.88, 10.92±0.32, 9.35±0.83, HT-29, with IC50values of 14.90±2.71, 20.50±6.37, 13.90±1.30, and CCD841, with IC50values of 11.40±0.68, 7.02±0.44 and 7.83±0.05 μg/mL, respectively. Tested quinones can reduce the expression of tumor-related factors tumor necrosis factor α, interleukin(IL)-10, and IL-6 in HT-29 cells, selectively promote apoptosis, and regulate the cell cycle which can reduce the proportion of cells in the G1phase and increase the proportion of the S phase.Meanwhile, tested quinones could up-regulate mRNA and protein expression of GSK-3β and APC, while down-regulate that of β-catenin, Frizzled1, c-Myc, and CyclinD1 in the Wnt/β-catenin pathway of HT-29 cells.Conclusion: Quinones from B. rynchopetera defense secretion could inhibit the proliferation of colorectal tumor cells and reduce the expression of related factors, which would be functioned by regulating cell cycle, selectively promoting apoptosis, and affecting Wnt/β-catenin pathway-related mRNA and protein expressions.
