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1.
Acta Pharm Sin B ; 13(8): 3400-3413, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37655314

ABSTRACT

Colorectal cancer (CRC) is a type of malignant tumor that seriously threatens human health and life, and its treatment has always been a difficulty and hotspot in research. Herein, this study for the first time reports that antipsychotic aripiprazole (Ari) against the proliferation of CRC cells both in vitro and in vivo, but with less damage in normal colon cells. Mechanistically, the results showed that 5-hydroxytryptamine 2B receptor (HTR2B) and its coupling protein G protein subunit alpha q (Gαq) were highly distributed in CRC cells. Ari had a strong affinity with HTR2B and inhibited HTR2B downstream signaling. Blockade of HTR2B signaling suppressed the growth of CRC cells, but HTR2B was not found to have independent anticancer activity. Interestingly, the binding of Gαq to HTR2B was decreased after Ari treatment. Knockdown of Gαq not only restricted CRC cell growth, but also directly affected the anti-CRC efficacy of Ari. Moreover, an interaction between Ari and Gαq was found in that the mutation at amino acid 190 of Gαq reduced the efficacy of Ari. Thus, these results confirm that Gαq coupled to HTR2B was a potential target of Ari in mediating CRC proliferation. Collectively, this study provides a novel effective strategy for CRC therapy and favorable evidence for promoting Ari as an anticancer agent.

2.
Huan Jing Ke Xue ; 27(1): 47-50, 2006 Jan.
Article in Chinese | MEDLINE | ID: mdl-16599119

ABSTRACT

Oxidant strengthening the degradation of DMF aqueous solution was investigated when TiO2 fiber is used as the photocatalyst. When the UV light was absent, ozone per se could not make DMF degrade, which proves that DMF is a stable substance. But ozone could increase obviously photocatalytic degradation rate of DMF in O3/TiO2 (F). Under the same reaction condition, photocatalytic degradation rate and speed of DMF in O3/TiO2 (F) was almost 1.5 times and 2 times higher than that in air/ TiO2 (F) and H2O2/TiO2 (F) respectively. COD analysis showed DMF was almost mineralized completely when the reaction was carried out for 120 min. Through Hinsberg test secondary amine was proved as one of intermediates in the process of DMF photocatalytic degradation. Rise of pH value of reaction solution also showed that amine was produced in the photocatalytic reaction process. Degradation speed of DMA in O3/TiO2 (F) was higher than that in air/TiO2 (F). The increasing degradation rate and speed of DMF was mainly caused by fast degradation of secondary amine in the process of DMF photocatalytic degradation in O3/TiO2 (F).


Subject(s)
Dimethylformamide/chemistry , Oxidants/chemistry , Photochemistry/methods , Titanium/chemistry , Waste Disposal, Fluid/methods , Biodegradation, Environmental , Catalysis , Oxidation-Reduction , Ozone/chemistry
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