Puerarin, an isoflavonoid derived from Radix puerariae, potentiates endothelium-independent relaxation via the cyclic AMP pathway in porcine coronary artery

Yeung, Dennis K.Y.; Leung, Susan W.S.; Xu, Yan; Vanhoutte, Paul M.; Man, Ryk

doi:10.1016/j.ejphar.2006.08.078

Cited by 107 publications

(59 citation statements)

References 20 publications

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“…Ohwi, which is used in the treatment of cardiovascular diseases, such as coronary heart disease, cardiac infarction, arteriosclerosis and arrhythmia (Ren et al, 2006;Yeung et al, 2006). However, it was reported that oral bioavailability of PUE was just approximately 4%, the cumulative excretion rate of unchanged PUE in urine and feces was 45.33% in 24 h and most of it was mainly excreted by dejection (Gou et al, 2006;Luo et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

N-trimethyl chitosan (TMC)-modified microemulsions for improved oral bioavailability of puerarin: preparation and evaluation

et al. 2014

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The aim of this research was to increase the oral bioavailability of puerarin by N-trimethyl chitosan-modified microemulsions (TMC-MEs) loaded with puerarin. Different concentrations of TMC-modified microemulsions were prepared in our study, and then evaluated for particle size, zeta potential, morphological observation and changes of the microenvironment polarity of inner oil core. It was shown that the zeta potential of the microemulsion was increased with the increasing concentration of TMC, and the peak value was achieved when the concentration of TMC was 3.0 mg/mL. The enhancement of the ratio of I 1 /I 3 (the ratio between the first band and the third band of the emission fluorescence spectrum of pyrene, I 1 ¼ 373 nm, I 3 ¼ 384 nm) indicated that polarity of the inner core of TMC-MEs was increased with the addition of the modifier. Pharmacokinetic studies demonstrated that after oral administration of puerarin N-trimethyl chitosan (TMC)-modified microemulsions (PUE-TMEs) and puerarin microemulsions (PUE-MEs) to rats at a dose of 100 mg/kg, relative bioavailability was enhanced about 6.8-and 1.2-fold, respectively, compared to puerarin suspension (PUE-SUS) as control. It indicated that the TMC-MEs could be used as an effective formulation for enhancing the oral bioavailability of puerarin.

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Section: Introductionmentioning

confidence: 99%

N-trimethyl chitosan (TMC)-modified microemulsions for improved oral bioavailability of puerarin: preparation and evaluation

et al. 2014

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“…In summary, we have provided direct evidences for the activation of cloned BK Ca channels by puerarin, and shown that BK Ca channel activation contributes to puerarin-induced vasodilation, which is likely to be a mechanism by which puerarin exerts its action on rat thoracic aortas, in addition to its activation of endothelial nitric-oxide synthase and cAMP pathway, as demonstrated by other investigators (Ma et al, 2003;Yeung et al, 2006). The present findings are of interest for understanding the contribution of BK Ca openers to lowering blood pressure and improving other cardiovascular symptoms.…”

Section: Discussionmentioning

confidence: 54%

“…The vascular relaxing action of puerarin is one of the focuses of research on its pharmacology. It involves a variety of molecular mechanisms such as activation of endothelial nitric-oxide synthase (Ma et al, 2003) and the cAMP pathway (Yeung et al, 2006). Some researchers (Sun and Li, 2002;Dong et al, 2004) have shown that the potassium channel blocker tetraethylammonium can significantly block puerarin-induced vasodilation.…”

mentioning

confidence: 99%

Activation of Large-Conductance Calcium-Activated Potassium Channels by Puerarin: The Underlying Mechanism of Puerarin-Mediated Vasodilation

Sun¹,

Ding²,

Li³

et al. 2007

J Pharmacol Exp Ther

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Puerarin is the main isoflavone found in Pueraria lobata (Willd) Ohwi, which has been used in therapy for various cardiovascular diseases. The present study examined the effects of puerarin on the large-conductance voltage-and Ca 2ϩ -activated potassium (BK Ca ) channel and on rat thoracic aortas. BK Ca channels encoded with either ␣ (BK-␣) or ␣/␤ subunits (BK-␣ϩ␤1) were heterologously expressed in Xenopus oocytes or human embryonic kidney 293 cells. The activities of BK Ca channels were measured using excised patch-clamp recordings. Puerarin activated BK-␣ϩ␤1 currents with a half-maximal concentration (EC 50 ) of 0.8 nM and a Hill coefficient of 1.11 at 10 M Ca 2ϩ and with an EC 50 of 12.6 nM and a Hill coefficient of 1.08 at 0 M Ca 2ϩ . Puerarin (1 nM) induced a 16-mV leftward shift in the conductance-voltage curve for BK-␣ϩ␤1 currents at 10 M Ca 2ϩ and at 100 nM induced a 26-mV leftward shift at 0 M Ca 2ϩ . Puerarin mainly increased the BK-␣ϩ␤1 channel open probability without changing the unitary conductance. Activation was also detected in the absence of the ␤1 subunit. A deglycosylated analog of puerarin, daidzein, also activated BK Ca channels with weaker potency. In addition, puerarin (0.1 to 1000 M) caused concentration-dependent relaxations of rat thoracic aortic rings contracted with 1 M noradrenaline bitartrate (EC 50 ϭ 1.1 M). These were significantly inhibited by 50 nM iberiotoxin, a specific blocker of BK Ca channels. This is the first study demonstrating that puerarin activates BK Ca channels, especially BK-␣ϩ␤1 channels. The activation of the BK Ca channel probably contributes to the puerarin-mediated vasodilation action.

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“…Puerarin is an isoflavanone glycoside extracted from species in the family Leguminosae such as Radix puerariae and is currently used to treat ischemic cerebrovascular disease and other vascular dysfunctions in China (64). Studies found that puerarin had potent effects in improving learning and memory disorders induced by scopolamine or D-galactose in a mouse model (65).…”

Section: Puerarinmentioning

confidence: 99%

Research progresses on flavonoids isolated from traditional Chinese medicine in treatment of Alzheimer's disease

Gao

Inagaki

Liu

2013

Intractable Rare Dis Res

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Puerarin, an isoflavonoid derived from Radix puerariae, potentiates endothelium-independent relaxation via the cyclic AMP pathway in porcine coronary artery

Cited by 107 publications

References 20 publications

N-trimethyl chitosan (TMC)-modified microemulsions for improved oral bioavailability of puerarin: preparation and evaluation

N-trimethyl chitosan (TMC)-modified microemulsions for improved oral bioavailability of puerarin: preparation and evaluation

Activation of Large-Conductance Calcium-Activated Potassium Channels by Puerarin: The Underlying Mechanism of Puerarin-Mediated Vasodilation

Research progresses on flavonoids isolated from traditional Chinese medicine in treatment of Alzheimer's disease

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