Daurinoline
Daurinoline is a non-competitive antagonist, it exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism, it would have a protective function on microcirculation of cerebral pia mater, which may be beneficial to relieve cerebral ischemic injury. Daurinoline could significantly reverse noradrenaline induced constriction of pial arterioles and venules, and increase the number of blood vessels which were decreased by noradrenaline.
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《Medical Journal of Wuhan University》 2011-01
Effects of Daurinoline on Microcirculation of Cerebral Pia Mater in Mice[Reference:
WebLink]
To investigate the effect of Daurinoline on cerebral pia mater microcirculation in mice.
METHODS AND RESULTS:
An open cranial window was performed and microcirculation disturbance state was established by means of administering noradrenaline on the cerebral pia mater. The effect of Daurinoline was observed from the changes of the diameters and numbers of the arterioles and venules. Daurinoline could significantly reverse noradrenaline induced constriction of pial arterioles and venules, and increase the number of blood vessels which were decreased by noradrenaline.
CONCLUSIONS:
It suggests that Daurinoline would have a protective function on microcirculation of cerebral pia mater, which may be beneficial to relieve cerebral ischemic injury.
Environ Toxicol Pharmacol . 2019 Feb;66:109-115.
Daurinoline suppressed the migration and invasion of chemo-resistant human non-small cell lung cancer cells by reversing EMT and Notch-1 and sensitized the cells to Taxol[Pubmed:
30641414]
Abstract
Non-small cell lung cancer (NSCLC) is one of the most common malignancies, and Taxol is a cornerstone in the treatment. However, taxol-resistance eventually limits the clinical effects and applications. Daurinoline could restore the sensitivity of resistant MCF-7/adr and KBv200 cells. Whereas, the effect of Daurinoline on the chemo-resistant NSCLC cells and the mechanism has not been elucidated. In this study, Daurinoline was firstly demonstrated that inhibited the proliferation, migration, invasion and EMT phenotype of chemo-resistant NSCLC cells. And these effects were associated with EMT and Notch-1 reversal. Moreover, Daurinoline could significantly enhance the anti-tumor effect of Taxol rather than epirubicin, adriamycin and cisplatin. And the reverse fold (RF) value of Daurinoline was greater than terfenadine reported before. There are little cytotoxic effects of Daurinoline and its derivatives reported by L.W. Fu, et al. (2001). Therefore, Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC patients.
Keywords: Chemosensitization; Daurinoline; EMT; Non-small cell lung cancer.
《Herald of Medicine》 2014-06
Relaxant Effect of Daurinoline on Vascular Smooth Muscle of Isolated Rabbit Basilar Artery[Reference:
WebLink]
To investigate the effect of Daurinoline on basilar artery vascular smooth muscle.
METHODS AND RESULTS:
The tension of isolated basilar artery ring of rabbit was measured. The effects of Daurinoline on the basilar artery contracted by methoxamine,5-hydroxytryptamine(5-HT),KCl and Histamine( His) were also examined. Dose-response curves of 5-HT and KCl were observed as well. Daurinoline exerted obvious relaxation effect on the basilar artery vascular ring contracted by methoxamine,5-HT,KCl and His in a concentration-dependent manner. IC50of Daurinoline in methoxamine,5-HT,KCl and His-treated rabbits was 8. 67 × 10- 5,1. 78 × 10- 6,6. 79 × 10- 7and 4. 98 × 10- 4mol · L- 1,respectively. The change of concentration-response curves of methoxamine,5-HT,KCl and His showed that Daurinoline was a non-competitive antagonist.
CONCLUSIONS:
Daurinoline exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism. The mechanism of relaxation action may be related to blockage of voltage-dependent or receptor-dependent calcium channels.
