Radiation‐induced lung injury (RILI), divided into early radiation pneumonia (RP) and late radiation‐induced pulmonary fibrosis (RIPF), is a common serious disease after clinical chest radiotherapy or nuclear accident, which seriously threatens the life safety of patients. There has been no effective prevention or treatment strategy till now. Epithelial‐mesenchymal transition (EMT) is a key step in the occurrence and development of RILI. In this study, we demonstrated that emetine dihydrochloride (EDD) alleviated RILI through inhibiting EMT. We found that EDD significantly attenuated EMT‐related markers, reduced Smad3 phosphorylation expression after radiation. Then, for the first time, we observed EDD alleviated lung hyperaemia and reduced collagen deposit induced by irradiation, providing protection against RILI. Finally, it was found that EDD inhibited radiation‐induced EMT in lung tissues. Our study suggested that EDD alleviated RILI through inhibiting EMT by blocking Smad3 signalling pathways. In summary, our results indicated that EDD is a novel potential radioprotector for RILI.

2021-11-01·Physiology & behavior3区 · 医学

Effects of area postrema lesions and bilateral subdiaphragmatic afferent vagotomy on emetine-induced conditioned taste avoidance in rats.

3区 · 医学

Article

作者: Wei, Zimo ; Fujita, Mayu ; Yoshizawa, Tomohiko ; Funahashi, Makoto ; Huang, Helai ; Inui, Tadashi ; Su, Shaoyi

We investigated the effect of area postrema lesions and selective vagotomy of afferent fibers on emetine-induced nausea in rats. We evaluated the acquisition of the conditioned taste avoidance (CTA) to 0.1% saccharin solution after conditioning with emetine dihydrochloride (5.54 mg/kg, i.p., 1% BW). The CTA was measured in three groups of rats: a bilateral subdiaphragmatic afferent vagotomy group, an area postrema lesion group, and a sham lesion group. The bilateral vagotomy and sham groups of rats showed acquisition of CTA within 2 days of the test date. Taste avoidance was never conditioned in the area postrema lesion group. These results indicate that the area postrema plays a crucial role in the induction of emetine-induced nausea.

2020-03-24·Antimicrobial agents and chemotherapy2区 · 医学

Lead Optimization of Dehydroemetine for Repositioned Use in Malaria

2区 · 医学

Article

作者: Burusco, Kepa K. ; Fernández-Álvaro, Elena ; Wilkinson, James ; Panwar, Priyanka ; Gutnov, Andrey ; Matthews, Holly ; Bryce, Richard A. ; Abubaker, Muna ; Nirmalan, Niroshini

Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel antimalarial treatments. The antiamoebic compound emetine dihydrochloride has been identified as a potent in vitro inhibitor of the multidrug-resistant strain K1 of Plasmodium falciparum (50% inhibitory concentration [IC 50 ], 47 nM ± 2.1 nM [mean ± standard deviation]). Dehydroemetine, a synthetic analogue of emetine dihydrochloride, has been reported to have less-cardiotoxic effects than emetine.

100 项与 Emeriamine dihydrochloride 相关的药物交易

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