Vasorelaxant effect of harman

Shi, Chuen-Chao; Chen, Suying; Wang, Guei-Jane; Liao, Jyh‐Fei; Chen, Chieh-Fu

doi:10.1016/s0014-2999(99)00928-0

Cited by 51 publications

(29 citation statements)

References 17 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Ca 2+ is also released from intracellular stores upon activation [12] . KCl depolarizes and opens VOC, leading to Ca 2+ influx, whilst PHE is able to open ROC to induce calcium influx in aorta without producing membrane depolarization [11,[13][14][15] . Calycosin significantly inhibited KCl-induced vasocontraction, and antagonized Ca 2+ -induced contraction in aortic rings exposed to KCl, suggesting that calycosin decreased extracellular Ca 2+ influx through VOC.…”

Section: Discussionmentioning

confidence: 99%

Calcium channel blocking activity of calycosin, a major active component of Astragali Radix, on rat aorta1

Wang

Cheng

et al. 2006

Acta Pharmacologica Sinica

View full text Add to dashboard Cite

Aim: To investigate the vasoactivity of calycosin, a major active component of Astragali Radix. Methods: Experiments were performed on isolated rat thoracic aortic rings pre-contracted with phenylephrine (PHE) or KCl. Results: Calycosin produced a concentration-dependent relaxation on the tissue pre-contracted using PHE with 4.46±0.13 of pD 2 and 95.85%±2.67% of E max ; or using KCl with 4.27±0.05 of pD 2 and 99.06%±2.15% of E max , and displaced downwards the concentration-response curves of aortic rings to PHE or KCl. The relaxant effect of calycosin on denuded endothelium aortic rings was the same as on intact endothelium aortic rings, and its vasorelaxant effect was not influenced by L-NAME or indomethacin. In Ca 2+ -free solution, calycosin (30 µmol/L) did not have an effect on PHE (1×10 -6 mol/L)-induced aortic ring contraction. The effects of calycosin and nifedipine where somewhat different; calycosin decreased aortic ring contractions induced by the two agonists, but nifedipine displayed a more potent inhibitory effect on KCl-induced contractions than on PHE-induced contractions, and the vascular relaxing effects of calycosin and nifidipine were additive on PHEinduced contraction but not KCl-induced. Conclusion: Calycosin is a vasorelaxant. Its action is endothelium-independent and is unrelated to intracellular Ca 2+ release. It is a noncompetitive Ca 2+ channel blocker. The effect of calycosin on Ca 2+ channel blockade may be different from that of dihydropyridines. This study demonstrated a novel pharmacological activity of calycosin, and supplied a theoretic foundation for Astragali Radix application.

show abstract

Section: Discussionmentioning

confidence: 99%

Calcium channel blocking activity of calycosin, a major active component of Astragali Radix, on rat aorta1

Wang

Cheng

et al. 2006

Acta Pharmacologica Sinica

View full text Add to dashboard Cite

show abstract

“…Recently, we reported the in vivo cardiovascular effect and in vitro vasorelaxant effect of harman ( Fig. 1), another harmala alkaloid (19). Our results suggested that the vasorelaxant effect of harman may be involved in its hypotensive effect, and the vasorelaxant effect is attributed to its actions on the endothelial cells to release nitric oxide (NO) and on the vascular smooth muscles to inhibit the contractions induced by the activation of receptor-linked and voltagedependent Ca 2+ channels.…”

mentioning

confidence: 71%

“…To evaluate the vasorelaxant and endothelium-dependent effects of test compounds, endothelium-intact and -denuded preparations were pretreated with phenylephrine (PE, 0.3 mM) or KCl (60 mM) to produce sustained contractions (19). Lack of functional vascular endothelium was confirmed by the loss of relaxant response to 3 mM acetylcholine before the experiment began.…”

Section: Vasorelaxant Effectsmentioning

confidence: 99%

“…Because the chemical structures of these 4 compounds are very similar, the present study was carried out to compare harmine, harmaline and harmalol in terms of vasorelaxant effects on the isolated rat thoracic aorta preparations and stimulating effects on NO release from cultured rat aortic endothelial cells. To compare with harman (19), their affinities for cardiac a1-adrenoceptors and the 1,4-dihydropyridine (DHP) binding site of L-type Ca 2+ channels were also studied with receptor binding assays.…”

mentioning

confidence: 99%

See 1 more Smart Citation

Comparative Study on the Vasorelaxant Effects of Three Harmala Alkaloids In Vitro

Shi¹,

Liao²,

Chen

2001

Japanese Journal of Pharmacology

Self Cite

View full text Add to dashboard Cite

ABSTRACT-Three psychological active principles from the seeds of Peganum harmala L., harmine, harmaline and harmalol, showed vasorelaxant activities in isolated rat thoracic aorta preparations precontracted by phenylephrine or KCl with rank order of relaxation potency of harmine > harmaline > harmalol. The vasorelaxant effects of harmine and harmaline (but not harmalol) were attenuated by endothelium removal or pretreatment with a nitric oxide (NO) synthase N M -nitro-L-arginine methyl ester. In cultured rat aortic endothelial cells, harmine and harmaline (but not harmalol) increased NO release, which was dependent on the presence of external Ca 2+. In endothelium-denuded preparations, pretreatment of harmine, harmaline or harmalol (3 -30 mM) inhibited phenylephrine-induced contractions in a non-competitive manner. Receptor binding assays indicated that all 3 compounds interacted with cardiac a1-adrenoceptors with comparable affinities (Ki value around 31 -36 mM), but only harmine weakly interacted with the cardiac 1,4-dihydropyridine binding site of L-type Ca 2+ channels (Ki value of 408 mM). Therefore, the present results suggested that the vasorelaxant effects of harmine and harmaline are attributed to their actions on the endothelial cells to release NO and on the vascular smooth muscles to inhibit the contractions induced by the activation of receptor-linked and voltage-dependent Ca 2+ channels. The vasorelaxant effect of harmalol was not endothelium-dependent.

show abstract

“…Harmaline (C 13 H 14 N 2 O) is reported to be used as an abortifacient, narcotics, aphrodisiac, stimulant and sedative, emmenagogue, emetic, vermifuge, and soporific [5]. There were also some reports concerning the cardiovascular actions of harmala alkaloids [6].…”

mentioning

confidence: 99%

A framework for harmla alkaloid extraction process development using fuzzy-rough sets feature selection and J48 classification

Badria¹,

Habib²,

Shoaip³

et al. 2017

IJACR

View full text Add to dashboard Cite

Vasorelaxant effect of harman

Cited by 51 publications

References 17 publications

Calcium channel blocking activity of calycosin, a major active component of Astragali Radix, on rat aorta1

Calcium channel blocking activity of calycosin, a major active component of Astragali Radix, on rat aorta1

Comparative Study on the Vasorelaxant Effects of Three Harmala Alkaloids In Vitro

A framework for harmla alkaloid extraction process development using fuzzy-rough sets feature selection and J48 classification

Contact Info

Product

Resources

About