Neferine exerts its antithrombotic effect by inhibiting platelet aggregation and promoting dissociation of platelet aggregates

Zhou, Yajun; Xiang, Jizhou; Yuan, Hongjin; Liu, Hui; Tang, Qiang; Hao, Hong-Zhen; Yin, Zhang; Wang, Jialing; Ming, Zhang-Yin

doi:10.1016/j.thromres.2013.05.018

Cited by 57 publications

(32 citation statements)

References 32 publications

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“…There is an abundance of evidence showing that this alkaloid has sedative, anti‐pyretic, (Sugimoto et al ., ), anti‐arrhythmic (Narayana Moorthy et al ., ), anti‐depressant (Sugimoto et al ., ) and autophagy‐inducible effects (Poornima et al ., ). Moreover, Nef also has effects related to cardiovascular diseases and neurological disorders, such as anti‐thrombotic (Zhou et al ., ) and inhibitory effects on the β‐site amyloid precursor protein‐cleaving enzyme 1 (Jung et al ., ). However, as yet, the effects of Nef on cerebral ischaemia have not been explored.…”

Section: Introductionmentioning

confidence: 99%

Mitochondrial protective effect of neferine through the modulation of nuclear factor erythroid 2‐related factor 2 signalling in ischaemic stroke

Chen

Yang

et al. 2018

British J Pharmacology

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Background and Purpose Ischaemic stroke is a leading cause of death and long‐term disability. Promising neuroprotective compounds are urgently needed to overcome clinical therapeutic limitations. Neuroprotective agents are limited to single‐target agents, which further limit their clinical effectiveness. Due to the brain's particular energy requirements, the energy micro‐environment, centred in mitochondria, is a new research hotspot in the complex pathology of ischaemic stroke. Here, we studied the effects of neferine (Nef), a bis‐benzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera Gaertn, on ischaemic stroke and its underlying mitochondrial protective mechanisms. Experimental Approach Rats with permanent middle cerebral artery occlusion (pMCAO)‐induced focal cerebral ischaemia and tert‐butyl hydroperoxide (t‐BHP)‐injured PC12 cells were used to investigate the neuroprotective effects of Nef, particularly with regard to energy micro‐environment regulation by mitochondria and its mechanism in vivo and in vitro. Key Results Nef protected t‐BHP‐injured PC12 cells in vitro and ameliorated neurological score, infarct volume, regional cerebral blood flow, cerebral microstructure and oxidant‐related enzyme deficits in pMCAO rats in vivo. Nef also prevented mitochondrial dysfunction both in vivo and in vitro. The underlying mechanism of the mitochondrial protective effect of Nef might be attributed to the increased translocation of Nrf2 to the nucleus. Furthermore, the translocation of Nrf2 to nucleus was also decreased by sequestosome 1 (p62) knockdown. Conclusions and Implications Our results demonstrated that Nef might have therapeutic potential for ischaemic stroke and may exert its protective role through mitochondrial protection. This protection might be attributed to the modulation of Nrf2 signalling.

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Section: Introductionmentioning

confidence: 99%

Mitochondrial protective effect of neferine through the modulation of nuclear factor erythroid 2‐related factor 2 signalling in ischaemic stroke

Chen

Yang

et al. 2018

British J Pharmacology

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“…The inhibitory effects of neferine on platelet activation might be relevant in cases involving aberrant platelet activation where neferine could be used as an antiplatelet and antithrombotic agent 15 .…”

Section: Antithrombotic Effectmentioning

confidence: 99%

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2016

IJPSR

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objectives: Nelumbo nucifera Gaertn (Nelumbonaceae) known by numerous common names including Indian lotus, sacred lotus, bean of India, or simply lotus is one of the most important medicinal plants. In this review there is discussion about therapeutic potential of the different parts of the plant (leaves, seeds, flower, and rhizome) which can be used in traditional system of medicine. This review also describes various compounds isolated from different parts of the plant and therapeutic benefits derived from those phytocontituents. The aim of this review is to summarize the pharmacological, phytochemical and therapeutical knowledge of Nelumbo nucifera Gaertn. Key findings: The pharmacological studies have shown that N. nucifera possesses various pharmacological activities like anti-ischemic, antioxidant, anticancer, antiviral, antiobesity, lipolytic, hypocholestemic, antipyretic, hepatoprotective, hypoglycemic, antidiarrhoeal, antifungal, antibacterial, anti-inflammatory and diuretic activities. Several different types of compounds have been derived from this plant belonging to different chemical groups, including alkaloids, flavonoids, glycosides triterpenoid, etc., with own therapeutic impact. So the pharmacological effects and various active ingredients of different parts of N. nucifera are well understood. Summary: This review will facilitate to gain all about the past scientific research and will provide the necessary information about the enormous pharmacological activities of Nelumbo nucifera Gaertn which will insist the researchers for future research to protect human beings from various types of diseases and may serves as a natural gold for the promotion of mankind.

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“…It attenuated pulmonary fibrosis in in vitro and in vivo studies [11]. Moreover, it showed an antiplatelet and antithrombotic effect [12]. The potential anticancer effect of neferine has been studied as well.…”

Section: Introductionmentioning

confidence: 99%

Vasorelaxant and Antihypertensive Effects of Neferine in Rats: An In Vitro and In Vivo Study

et al. 2020

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The present study was performed to examine the antihypertensive effect of neferine in hypertensive rats and its relaxant mechanisms in isolated rat thoracic aorta. The antihypertensive effect was evaluated by tail-cuff methods on NG-nitro-L-arginine methyl ester (L-NAME) (40 mg/kg BW) 4-week hypertensive-induced hypertensive rats. The vasorelaxant effect and its mechanisms were studied by the organ bath technique in the thoracic aorta isolated from normotensive rats. The results indicated that the treatment of neferine (1 mg/kg and 10 mg/kg) markedly decreased the systolic blood pressure (SBP) when compared with the hypertension group (137.75 ± 10.14 mmHg and 132.23 ± 9.5 mmHg, respectively, p < 0.001), without affecting the heart rate. Moreover, neferine (10−12 − 10−4 M) exhibited concentration-dependent vasorelaxation in endothelium-intact rings (Emax values = 98.95 ± 0.66% and pD2 = 7.93 ± 0.28) and endothelium-denuded rings (Emax values = 90.61 ± 1.91% and pD2 = 6.85 ± 0.36). The effects of neferine were reduced by pre-incubation with L-NAME and 1H-[1,2,4]oxadiazolo[4,3-a] quinoxalin-1-one (ODQ) but not with pre-incubation with indomethacin and K+channel blockers. Neferine attenuated the contractions induced by phenylephrine and caffeine in a Ca2+-free solution and also inhibited in CaCl2- and phenylephrine-induced contracted rings. Our study suggests that neferine exhibited hypertensive potential, induced vasorelaxation through the endothelium nitric oxide synthase (eNOS)/nitric oxide (NO)/soluble guanylyl cyclase (sGC) pathway and involved the modulation of Ca2+ influx through Ca2+ channels and intracellular Ca2+ release from the sarcoplasmic reticulum.

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Neferine exerts its antithrombotic effect by inhibiting platelet aggregation and promoting dissociation of platelet aggregates

Cited by 57 publications

References 32 publications

Mitochondrial protective effect of neferine through the modulation of nuclear factor erythroid 2‐related factor 2 signalling in ischaemic stroke

Mitochondrial protective effect of neferine through the modulation of nuclear factor erythroid 2‐related factor 2 signalling in ischaemic stroke

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Vasorelaxant and Antihypertensive Effects of Neferine in Rats: An In Vitro and In Vivo Study

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