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  • 1
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    Identification of 16,25-O-diacetyl-cucurbitane F and 25-O-acetyl-23,24-dihydrocucurbitacin F as novel anti-cancer chemicals (2018)
    Royal Society
    Details
    Publication Date: 2018-08-16
    Description: Seven new cucurbitane glucosides, hemslepensides J-P ( 1 – 7 ), and two known compounds, 16,25- O -diacetyl-cucurbitane F ( 8 ) and 25- O -acetyl-23,24-dihydrocucurbitacin F ( 9 ), were isolated from the tubers of Hemsleya pengxianensis var. jinfushanensis . The structures of 1 – 7 were elucidated using infrared absorption spectroscopy, nuclear magnetic resonance spectroscopy and high-resolution electrospray ionization mass spectrometry. The treatment of HT29 cells, human colon cancer cells, with compounds 8 and 9 inhibited cell proliferation. Further study demonstrated that compounds 8 and 9 induced F-actin aggregation, G 2 /M phase cell cycle arrest and cell apoptosis in HT29 cells. In summary, the present study enriched the chemical composition research of H. pengxianensis , and suggested that the compounds 8 / 9 treatment may be a potentially useful therapeutic option for colon cancer.
    Keywords: medicinal chemistry, plant science
    Electronic ISSN: 2054-5703
    Topics: Natural Sciences in General
    Published by Royal Society
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  • 2
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    Synthesis of gypsogenin derivatives with capabilities to arrest cell cycle and induce apoptosis in human cancer cells (2018)
    Royal Society
    Details
    Publication Date: 2018-01-25
    Description: Thirty-two gypsogenin derivatives were synthesized and screened for their cytotoxic activities. Their structures were established using IR, 1 H NMR, 13 C NMR, and LC-MS spectroscopic data. In MTT assays nearly all the compounds displayed good cytotoxicity in the low μM range for several human tumour cell lines (A549, LOVO, SKOV3 and HepG2). Low IC 50 values were obtained especially for the carboxamides 7a – 7j , for an oxime derivative 3 and a (2,4-dinitrophenyl)hydrazono derivative 4 . In particular, the IC 50 values of compounds 4 (IC 50 = 2.97 ± 1.13 µM) and 7 g (IC 50 = 3.59 ± 2.04 µM) against LOVO cells were found to be much lower than those of the other derivatives and parent compound. These compounds were submitted to an extensive biological testing and proved compounds 4 and 7 g to act mainly by an arrest of the tumour cells in the S phase of the cell cycle. In addition, compounds 4 and 7 g triggered the apoptotic pathway in cancer cells, showing high apoptosis ratios.
    Keywords: medicinal chemistry
    Electronic ISSN: 2054-5703
    Topics: Natural Sciences in General
    Published by Royal Society
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