Ca2+ channel blocking effect of iso-S-petasin in rat aortic smooth muscle cells

Wang, Guei-Jane; Wu, Xi-Chen; Lin, Yun‐Lian; Ren, Jun; Shum, Andrew Yau‐Chik; Wu, Yu‐Yuan; Chen, Chieh-Fu

doi:10.1016/s0014-2999(02)01764-8

Cited by 28 publications

(21 citation statements)

References 8 publications

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“…S-Petasin (Wang et al, 2001) and iso-S-petasin (Wang et al, 2002) were found recently to inhibit smooth and cardiac muscle contraction by inhibiting L-type VGCCs (presumably of the Ca v 1.2 isoform, which is predominant in these tissues; Sinnegger-Brauns et al, 2004) within a concentration range similar to the Ca v 2.1 inhibition reported here. This indicates that these petasins are not isoform-selective blockers of VGCCs.…”

Section: Discussionsupporting

confidence: 78%

“…Petasins comprise at least 20% of the constituents in the preparations of P. hybridus used in clinical trials, suggesting that these sesquiterpenes represent the active principle. Low micromolar concentrations of petasins have been shown to inhibit L-type VGCCs in smooth and cardiac muscle (Wang et al, 2001(Wang et al, , 2002(Wang et al, , 2004Esberg et al, 2003). Therefore, it is possible that they are also inhibitors of neuronal Ca v 2.1 channels.…”

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confidence: 99%

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Use-Dependent Block of Voltage-Gated Ca_v2.1 Ca²⁺Channels by Petasins and Eudesmol Isomers

Horak¹,

Koschak²,

Stuppner³

et al. 2009

J Pharmacol Exp Ther

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Migraine is a frequent and often disabling disease. Treatment is unsatisfactory in many patients. A disturbed dynamic balance between excitatory and inhibitory signal processing with enhanced cortical activity probably underlies common forms of migraine. Presynaptic voltage-gated Ca 2ϩ channels are critical determinants of neurotransmitter release and also contribute to trigeminovascular signal transduction. Because clinical evidence exists for migraine-prophylactic actions of Petasites hybridus extracts, we investigated whether petasins comprising the main constituents of the extract inhibit currents through presynaptic Ca v 2.1 channels expressed in Xenopus laevis oocytes. P. hybridus extract (0.02 mg/ml), petasin, neopetasin, isopetasin, S-petasin, and iso-S-petasin (50 M) were weak tonic blockers of Ca v 2

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Section: Discussionsupporting

confidence: 78%

mentioning

confidence: 99%

Use-Dependent Block of Voltage-Gated Ca_v2.1 Ca²⁺Channels by Petasins and Eudesmol Isomers

Horak¹,

Koschak²,

Stuppner³

et al. 2009

J Pharmacol Exp Ther

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“…Some pharmacological studies have suggested that petasin and s-petasin were active ingredients in this plant [1,5,16,17], furthermore, we found that bakkenolide B (Fig. 1), a major component in the leaves of Petasites japonicus, showed significant effects in an ovalbumin-induced asthma model in our previous studies [11].…”

Section: Introductionsupporting

confidence: 63%

Optimization of Extraction Conditions for Bakkenolide B from the Leaves of Petasites japonicus by Using Response Surface Methodology

Kim¹,

Kim²,

Chung³

et al. 2014

Journal of Life Science

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Optimal conditions for extraction of bakkenolide B from Petasites japonicus leaves were determined by using response surface methodology. A second-order Box-Behnken design representing three extraction temperatures (80, 100, 120℃), three extraction times (30, 45, 60 min), and three solvent pH's (5, 7, 9) was executed. The efficiency of the extraction conditions was defined using the β-hexosamidase assay by comparing both the bakkenolide B content and its anti-allergic activity expressed as extract inhibition on degranulation. The response surface plot described for the bakkenolide B content showed that the maximum content was predicted as 121.6 µg/g with extraction conditions of 127.1℃, 46.6 min, and pH 7.7. Extraction temperature and time were important factors in determining bakkenolide B content. Using regression analysis, correlation between the inhibition effect of mast cell degranulation and bakkenolide B content was found to be low.

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“…Two of these compounds, namely S ‐petasin and iso‐ S ‐petasin, have been studied extensively and were found to have cardiovascular regulatory (especially vasodilatory) effects 1–4 . In rat isolated aortic rings, both S ‐petasin and iso‐ S ‐petasin inhibit vasoconstriction by blocking the influx of extracellular Ca 2+ through L‐type voltage‐dependent Ca 2+ channels (VDCC) in vascular smooth muscle cells (VSMCs) and cardiomyocytes 1–4 . Furthermore, intracellular Ca 2+ and L‐type Ca 2+ channel recordings reveal the involvement of Ca 2+ channels in the cardiovascular responses to the sesquiterpenes 1,2,4 .…”

Section: Introductionmentioning

confidence: 99%

Cellular calcium regulatory machinery of vasorelaxation elicited by petasin

Wang

Lin

Chen³

et al. 2010

Clin Exp Pharma Physio

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1. The present study examined the cytosolic Ca(2+) regulatory machinery involved in the vasorelaxation produced by petasin, a sesquiterpene isolated from Petasites formosanus. 2. Aortic rings isolated from Sprague-Dawley rats were exposed to petasin (0.01-100 micromol/L) to elucidate its vascular effects on isometric contraction elicited by vasoconstrictors, as well as the contribution of the endothelium and Ca(2+) to the responses observed. In addition, L-type voltage-dependent Ca(2+) channel (VDCC) activity and [Ca(2+)](i) were determined in cultured vascular smooth muscle cells (VSMCs) from Sprague-Dawley rats in the presence of 1-100 micromol/L petasin using whole-cell patch-clamp recording and the fluorescent probe fura-2/AM. The effects of petasin on vascular responses were compared between aortic rings from spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto (WKY) rats. 3. Petasin reduced isometric contraction elicited by KCl or the L-type Ca(2+) channel opener BayK 8644 (IC(50) 3.0 +/- 0.4 and 4.1 +/- 1.1 micromol/L, respectively) in aortic rings isolated from Sprague-Dawley rats, independent of the endothelium. In addition, petasin triggered a rightward shift in the concentration-response curve to KCl while reducing the maximal response by 82%. In Ca(2+)-depleted and high K(+)-depolarized aortic rings, 1-100 micromol/L petasin pretreatment attenuated the Ca(2+)-induced contraction in a concentration-dependent manner. 4. In cultured VSMCs, whole-cell patch-clamp recording revealed that petasin inhibited VDCC activity. Measurement of [Ca(2+)](i) using fura-2/AM fluorescence indicated that petasin suppressed the KCl-induced increase in [Ca(2+)](i). However, receptor binding assays failed to identify any significant interaction between petasin and the dihydropyridine binding sites of the L-type VDCC. 5. In aortic rings from SHR and WKY rats, petasin inhibited Ca(2+)-induced contractions in Ca(2+)-depleted and high K(+)-depolarized solution with a more pronounced effect in rings from SHR. 6. Together, the results suggest that direct Ca(2+) antagonism of L-type VDCC in vascular smooth muscle may account, at least in part, for petasin-induced vasorelaxation. The more pronounced effect of the sesquiterpene in blood vessels from SHR suggests its possible therapeutic potential in the mangement of hypertension.

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Ca2+ channel blocking effect of iso-S-petasin in rat aortic smooth muscle cells

Cited by 28 publications

References 8 publications

Use-Dependent Block of Voltage-Gated Ca_v2.1 Ca²⁺Channels by Petasins and Eudesmol Isomers

Use-Dependent Block of Voltage-Gated Ca_v2.1 Ca²⁺Channels by Petasins and Eudesmol Isomers

Optimization of Extraction Conditions for Bakkenolide B from the Leaves of Petasites japonicus by Using Response Surface Methodology

Cellular calcium regulatory machinery of vasorelaxation elicited by petasin

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Ca2+ channel blocking effect of iso-S-petasin in rat aortic smooth muscle cells

Cited by 28 publications

References 8 publications

Use-Dependent Block of Voltage-Gated Cav2.1 Ca2+Channels by Petasins and Eudesmol Isomers

Use-Dependent Block of Voltage-Gated Cav2.1 Ca2+Channels by Petasins and Eudesmol Isomers

Optimization of Extraction Conditions for Bakkenolide B from the Leaves of Petasites japonicus by Using Response Surface Methodology

Cellular calcium regulatory machinery of vasorelaxation elicited by petasin

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Product

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Use-Dependent Block of Voltage-Gated Ca_v2.1 Ca²⁺Channels by Petasins and Eudesmol Isomers

Use-Dependent Block of Voltage-Gated Ca_v2.1 Ca²⁺Channels by Petasins and Eudesmol Isomers