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Calyx wooden spoon anthraquinone compounds in vitro anti- tumor activity

Author: ZhouQiYin
Tutor: DingLan
School: Northwest Normal University
Course: Cell Biology
Keywords: Calyx wooden spoon Anthraquinone Cytotoxic activity QSAR Indicus aldehyde DNA damage Apoptosis Cell migration Cytoskeleton
CLC: R285
Type: Master's thesis
Year: 2009
Downloads: 161
Quote: 1
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Abstract

Anthraquinone compounds have antioxidant, anti-inflammatory, antibacterial, inhibition of tumor cell growth and induce apoptosis of tumor cells and other biological characteristics. Calyx wooden spoon (Xanthophytum Attopvensis Pierre) was Rubiaceae (Rubiaceae) spoon calyx Hirmer (Paedicalyx) plants produced in Guangdong, Hainan, Yunnan and other places, for medicinal folk, mainly for the treatment of jaundice and hepatitis, containing eight kinds of anthraquinone compounds. In this study, from the SRB assay wooden spoon isolated calyx 6 kinds of anthraquinone compound of four kinds of human tumor cell lines (HepG2, SGC-7901, Glc-82, HL-60) in vitro cytotoxic activity, and the Their structure-activity relationships were analyzed; exploit growth curve, Comet assay, flow cytometry and AO / EB double staining, anthraquinone compounds were detected indicus aldehyde human promyelocytic leukemia cells HL-60 growth inhibition, DNA damage ability, the role of cell cycle arrest and induction of apoptosis; detected indicus aldehyde on HepG2 cells growth inhibition, cell migration and cell cytoskeleton. The results were as follows: (1) No sugar-substituted 1,3 - dihydroxy - anthraquinone aldehyde (compound 1) and 1 - methoxy-2 - formyl -3 - hydroxy-anthraquinone (compound 2 ) four kinds of cell lines showed a strong cytotoxic activity, having a sugar group than anthraquinones high cytotoxic activity of about 4.7-12.7 times, which may be due to a large sugar substituent such steric compound with cells caused by weakening the interaction between the target molecule; only substituent at C-1 of different compounds 1 (-OH) and Compound 2 (-OCH3) have similar cytotoxic activity, indicates that the substituent loci - OH and-OCH3 contribution of cytotoxicity similar to the compound; and compared to the other three cell lines, HL-60 cells than the other three adherent cells anthraquinone compound has a higher sensitivity of the former than the latter IC50 values by 1.2-2.5 times lower. (2) Tiger thorn aldehyde on human promyelocytic HL-60 cells in a time-and concentration-dependent growth inhibition and DNA damage induced effect, compared with the control group, the drug treatment group (5-12.5μg · mL-1 ) have caused a highly significant (P lt; 0.01) comet rate. 5,10,12.5 and 15μg mL-1 Tiger thorn in 12-60 hours aldehyde induced HL-60 cell cycle arrest in G1 phase, 30μg mL-1 Tiger thorn in 12-60 hours aldehyde induced HL-60 cells in S phase block, 40μg mL-1 Tiger thorn in 12-60 hours aldehyde HL-60 cells induced G2 / M phase arrest; drug-induced apoptosis in HL-60 cells there is a time and concentration-dependent manner, and 2.5-12.5μg · mL-1 of the drug within 72 hours induced apoptosis rate reached a significant level (P lt; 0.05) or very significant level (P lt; 0.01). (3) Tiger thorn aldehyde on the growth of HepG2 cells has a strong inhibitory effect was time-and concentration-dependent manner; indicus aldehyde inhibition of HepG2 cell migration also presents time and concentration-dependent manner. Treated cells become shorter stress fibers disappear, adherent cells weakened and turned round, and apoptosis. 4-20μg · mL-1 indicus aldehyde-induced apoptosis in 24h, 48h and 72h compared with the control group were highly significant differences (P lt; 0.01). Experimental results are as follows: (1) According to NCI guidelines, 6 anthraquinone compound of compound 1 and compound 2 with further research value. Further, since the test compounds 3-6 are C-3 substituted sugar, as to whether all the sugar-substituted cytotoxic activity were decreased, need to be further confirmed. (2) indicus aldehyde on HL-60 cells showed a strong inhibitory effect and the induction of apoptosis and can therefore be considered as a potential anti-leukemia. (3) Tiger thorn aldehyde-induced cytoskeletal changes that weakened adherent HepG2 cells became round and inhibit cell migration and further induce apoptosis, but its exact mechanism behind the need to further study the tiger as a thorn aldehyde potential anti-HCC drugs to provide more credible evidence.

Calyx wooden spoon anthraquinone compounds in vitro anti- tumor activity

Abstract

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