scholarly journals Chemical Analysis and Calcium Channel Blocking Activity of the Essential Oil of Perovskia abrotanoides

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Abdul Jabbar Shah ◽  
Munawwer Rasheed ◽  
Qaiser Jabeen ◽  
Amir Ahmed ◽  
Rasool Bakhsh Tareen ◽  
...  
Keyword(s):  
Essential Oil ◽  
Calcium Channel ◽  
Response Curves ◽  
Spasmolytic Activity ◽  
Medicinal Use ◽  
Voltage Dependent ◽  
Rabbit Jejunum ◽  
Voltage Dependent Calcium Channels ◽  
Pre Treatment ◽  
Perovskia Abrotanoides

The aim of this study was to investigate the chemical composition and provide a pharmacological base for the medicinal use of the essential oil of Perovskia abrotanoides (Pa. Oil) in gastrointestinal disorders, such as colic. The chemical investigation resulted in the identification of 26 compounds, of which tricyclene, β- trans-ocimene, terpinene-4-acetate, terpinen-4-ol, caran-3β-ol, linalyl acetate, β-caryophyllene oxide and α-elemene had not previously been reported from P. abrotanoides. Major constituents were 1,8-cineol and δ–3-carene, which constituting 50% of the oil. In the isolated rabbit jejunum preparation Pa.Oil caused inhibition of spontaneous and high K+ (80 mM)-induced contractions, with respective EC50 values of 0.13 (0.08-0.20; n=4) and 0.90 mg/mL (0.50–1.60; n=5), thus showing that spasmolytic activity is mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pre-treatment of the tissue with Pa. Oil (0.03-0.1 mg/mL) caused a rightward shift in the Ca++ concentration-response curves, similar to that caused by verapamil, a standard calcium channel blocker. These data indicate that the essential oil of P. abrotanoides possesses spasmolytic activity mediated possibly through inhibition of voltage-dependent calcium channels, which may explain its medicinal use in colic and possibly diarrhea.

scholarly journals Voltage-Dependent Calcium Channel CaV1.3 Subunits Regulate the Light Peak of the Electroretinogram

2007 ◽  
Vol 97 (5) ◽  
pp. 3731-3735 ◽  
Author(s):  
Jiang Wu ◽  
Alan D. Marmorstein ◽  
Jörg Striessnig ◽  
Neal S. Peachey
Keyword(s):  
Calcium Channel ◽  
Pigment Epithelium ◽  
Retinal Pigment ◽  
Rod Photoreceptor ◽  
Wild Type ◽  
Fast Oscillation ◽  
Light Peak ◽  
Voltage Dependent Calcium Channel ◽  
Voltage Dependent ◽  
Voltage Dependent Calcium Channels

In response to light, the mouse retinal pigment epithelium (RPE) generates a series of slow changes in potential that are referred to as the c-wave, fast oscillation (FO), and light peak (LP) of the electroretinogram (ERG). The LP is generated by a depolarization of the basolateral RPE plasma membrane by the activation of a calcium-sensitive chloride conductance. We have previously shown that the LP is reduced in both mice and rats by nimodipine, which blocks voltage-dependent calcium channels (VDCCs) and is abnormal in lethargic mice, carrying a null mutation in the calcium channel β4 subunit. To define the α1 subunit involved in this process, we examined mice lacking CaV1.3. In comparison with wild-type (WT) control littermates, LPs were reduced in CaV1.3−/− mice. This pattern matched closely with that previously noted in lethargic mice, confirming a role for VDCCs in regulating the signaling pathway that culminates in LP generation. These abnormalities do not reflect a defect in rod photoreceptor activity, which provides the input to the RPE to generate the c-wave, FO, and LP, because ERG a-waves were comparable in WT and CaV1.3−/− littermates. Our results identify CaV1.3 as the principal pore-forming subunit of VDCCs involved in stimulating the ERG LP.

scholarly journals Comparison of the effects of L-type calcium channel antagonist Amlodipine with L/N-type calcium channel antagonist Cilnidipine on blood pressure, heart rate, proteinuria and lipid profile in hypertensive patients

2016 ◽  
Vol 15 (3) ◽  
pp. 460-465
Author(s):  
Kiran Kumar Singal ◽  
Neerja Singal ◽  
Abhinav Gupta ◽  
Akash Garg ◽  
Ravi Kumar
Keyword(s):  
Blood Pressure ◽  
Calcium Channel ◽  
Calcium Channel Antagonist ◽  
Total Cholesterol Level ◽  
Medical Science ◽  
Reflex Tachycardia ◽  
Before And After ◽  
Voltage Dependent ◽  
Amlodipine Group ◽  
Voltage Dependent Calcium Channels

Background: Cilnidipine is a novel and unique 1,4-dydropyridine derivative calcium antagonist that exerts potent inhibitory actions not only on L-type but also on N-type voltage dependent calcium channels. Blockade of the neural N-type calcium channel inhibits the secretion of norepinephrine from peripheral neural terminals and depresses sympathetic nervous system activity.Objective and methods: The purpose of this study was to assess the effect of Cilnidipine and Amlodipine on blood pressure (BP) levels. We did BP monitoring before and after once-daily use of Cilnidipine and Amlodipine in 100 hypertensive patients.Results: Both drugs significantly reduced systolic BP (SBP) and diastolic BP (DBP). However, the reductions in pulse rate (PR) were significantly greater in the Cilnidipine group than the Amlodipine group. N-type calcium channel blockade by Cilnidipine may not cause reflex tachycardia, and may be useful for hypertensive treatment.Conclusion: There was significant reduction in proteinuria with Clindipine as compared to Amlodipine. However, there were no significant change in total cholesterol level in diabetes and non-diabetics in both the group.Bangladesh Journal of Medical Science Vol.15(3) 2016 p.460-465

scholarly journals Ethnopharmacological basis for antispasmodic, antidiarrheal and antiemetic activities of Ceratonia siliqua pods

2017 ◽  
Vol 12 (4) ◽  
pp. 384
Author(s):  
Irfan Hamid ◽  
Khalid Hussain Janbaz
Keyword(s):  
Crude Extract ◽  
Video Clip ◽  
Dependent Manner ◽  
Ceratonia Siliqua ◽  
Spasmolytic Activity ◽  
Rabbit Jejunum ◽  
Pre Treatment ◽  
Dose Dependent

<p class="Abstract">The study was conducted to provide the ethnopharmacological bases of the crude extract of seed pods of <em>Ceratonia siliqua</em> in the gastrointestinal spasm, diarrhea and emesis. In segregated rabbit jejunum, it showed dose-dependent (0.01-10 mg/mL) relaxation of spontaneous as well as carbachol (1 µM)-induced contraction. Pre-treatment of segregated rat ileum with <em>C. siliqua</em>, significantly (p&lt;0.0001) suppressed the carbachol (1 µM)-induced contraction similar to atropine (1 µM). These results indicated that <em>C. siliqua</em> possesses spasmolytic activity through possible blockage of muscarinic receptor in jejunum preparations. Furthermore, the crude extract inhibited the castor oil-induced diarrhea, charcoal meal propulsion in mice and copper sulfate-induced retches in chicks in a dose-dependent manner (100, 200, 300 mg/kg). These in vitro and in vivo results indicate that <em>C. siliqua</em> possesses the spasmolytic and antidiarrheal activities mediated possibly through blockage of muscarinic receptors. Thus, this study provides a rationale for its folkloric use.</p><p><strong>Video Clip of Methodology</strong>:</p><p>12 min 42 sec   <a href="https://www.youtube.com/v/BQGWdIZqpsY">Full Screen</a>   <a href="https://www.youtube.com/watch?v=BQGWdIZqpsY">Alternate</a></p>

Calcium channels contribute to the decrease in blood pressure of pregnant rats

2002 ◽  
Vol 282 (2) ◽  
pp. H665-H671 ◽  
Author(s):  
May Simaan ◽  
Chanterelle Cadorette ◽  
Matthieu Poterek ◽  
Jean St-Louis ◽  
Michèle Brochu
Keyword(s):  
Blood Pressure ◽  
Calcium Channels ◽  
Calcium Channel ◽  
Plasma Renin ◽  
Late Pregnancy ◽  
Pregnant Rats ◽  
Affect Body Weight ◽  
Voltage Dependent ◽  
Voltage Dependent Calcium Channels ◽  
Calcium Channel Activator

Pregnancy is associated with hemodynamic changes such as reduced vascular resistance and blood pressure. We reported that, during late pregnancy, the activity of voltage-dependent calcium channels (VDCC) is altered in the adrenal cortex and vascular smooth muscle. These observations suggested that the late pregnancy-induced decrease in blood pressure is linked to diminished VDCC function. We attempted to prevent pregnancy-induced reduced blood pressure with a calcium channel activator (CGP 28392) in pregnant rats and to mimic it by administration of a calcium channel blocker (nifedipine) to nonpregnant rats. Treatment was given from the 15th day of gestation for 7 days. The systolic blood pressure of CGP 28392-treated pregnant rats rose transiently for 2 days and then declined toward values of nontreated pregnant controls, although remaining higher. However, nonpregnant rats maintained their high arterial pressure throughout CGP 28392 treatment. Nifedipine lowered the blood pressure in nonpregnant rats to values of nontreated term-pregnant controls. Both agents did not affect body weight, water or food intake, plasma renin activity, and plasma aldosterone or corticosterone levels. Nifedipine and CGP 28392 treatment of nonpregnant and pregnant animals, respectively, did not modify the response of aortic rings to KCl. These results show that VDCC activation caused hypertension, which modified the extent of the decrease in blood pressure at the end of pregnancy.

Studies on antihypertensive and antispasmodic activities of Andropogon muricatus Retz.This article is one of a selection of papers published in this special issue (part 1 of 2) on the Safety and Efficacy of Natural Health Products.

2007 ◽  
Vol 85 (9) ◽  
pp. 911-917 ◽  
Author(s):  
Anwar H. Gilani ◽  
Abdul J. Shah ◽  
Khalid H. Janbaz ◽  
Shahida P. Ahmed ◽  
Muhammad N. Ghayur
Keyword(s):  
Calcium Channel ◽  
Rabbit Aorta ◽  
Natural Health Products ◽  
Response Curves ◽  
Medicinal Uses ◽  
Health Products ◽  
Rabbit Jejunum ◽  
The Right

The aqueous-methanolic crude extract of Andropogon muricatus (Am.Cr) was investigated pharmacologically to determine some of its medicinal uses in cardiovascular and gastrointestinal disorders. A series of in vivo and in vitro studies were conducted to evaluate dose-dependent effects of Am.Cr on mean arterial pressure (MAP), cardiac and vascular contractions, and to further investigate the potential mechanism of action. Intravenous administration of Am.Cr (10–50 mg/kg) caused a fall (18%–56%) in MAP in normotensive rats under anesthesia. When tested in isolated guinea pig atria, Am.Cr (0.03–5.0 mg/mL) exhibited a cardiodepressant effect on the rate and force of spontaneous contractions. In isolated rabbit aorta, Am.Cr caused inhibition of K+ (80 mmol/L)-induced contractions at a lower concentration than of phenylephrine. In isolated rabbit jejunum preparations, Am.Cr (0.01–0.10 mg/mL) caused relaxation of spontaneous and high K+ (80 mmol/L)-induced contractions, suggesting that the spasmolytic effect is mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pretreatment of the tissue with Am.Cr (0.03–0.1 mg/mL) shifted the Ca2+ dose–response curves to the right, similar to that caused by verapamil. These data indicate that the blood pressure-lowering and spasmolytic effects of Am.Cr are mediated possibly through a calcium channel blocking activity. Phytochemical screening of Am.Cr revealed the presence of phenols, saponins, tannins, and terpenes, which may be responsible for the observed vasodilator, cardiodepressant, and antispasmodic activities. This study shows potential with respect to its medicinal use in cardiovascular and gut disorders.

Dihydropyridine-sensitive single calcium channels in airway smooth muscle cells

1990 ◽  
Vol 259 (6) ◽  
pp. L468-L480 ◽  
Author(s):  
J. F. Worley ◽  
M. I. Kotlikoff
Keyword(s):  
Smooth Muscle ◽  
Calcium Channels ◽  
Smooth Muscle Cells ◽  
Calcium Channel ◽  
Airway Smooth Muscle ◽  
Muscle Cells ◽  
Membrane Depolarization ◽  
Airway Smooth Muscle Cells ◽  
Voltage Dependent ◽  
Voltage Dependent Calcium Channels

We have identified and characterized single voltage-dependent calcium channels in both acutely dissociated rat bronchial and cultured human tracheobronchial smooth muscle cells using the patch-clamp technique. In both cell types, on-cell membrane patches displayed unitary currents selective for barium ions and exhibited one conductance level (21–26 pS), and the open state probability was increased by membrane depolarization. Unitary barium currents were enhanced by the calcium channel selective agonist, BAY R 5417, and inhibited by the dihydropyridine calcium channel antagonist, nisoldipine (apparent inhibition constant less than 100 nM). Moreover, the degree of nisoldipine inhibition of the rat bronchial smooth muscle channels was increased with membrane depolarization in a manner consistent with the drug interacting with highest affinity to the inactivated channel state. In addition, the sensitivity to BAY R 5417 augmentation and nisoldipine inhibition of depolarization-induced tonic force of intact rat bronchial ring segments was in close agreement to the single channel results. Thus these data suggest that activation of voltage-dependent calcium channels can influence airway contraction and that dihydropyridines may be effective modulators of depolarization-induced increases in bronchial tone. We conclude that both rat and human airway smooth muscle cells have high-conductance voltage-dependent calcium channels that interact in a predictable manner with dihydropyridines and are similar to voltage-dependent calcium channels observed in other smooth muscle cells.

scholarly journals Calcium entry blocking activity of the Elaeagnus umbellata fruit extract explains its use in diarrhea and gut spasm

2016 ◽  
Vol 11 (3) ◽  
pp. 585 ◽  
Author(s):  
Nayyab Rafique ◽  
Taous Khan ◽  
Abdul Jabbar Shah
Keyword(s):  
Ethyl Acetate ◽  
Crude Extract ◽  
Video Clip ◽  
Ethyl Acetate Fraction ◽  
Response Curves ◽  
Aqueous Fraction ◽  
Elaeagnus Umbellata ◽  
High K ◽  
Medicinal Use ◽  
Rabbit Jejunum

<p class="Abstract">This study was aimed to explore the pharmacological basis of potential medicinal use of <em>Elaeagnus umbellata</em> in gut disorders. Crude extract of <em>E. umbellata</em>, which was found positive for flavonoids, terpenoids and tannins, provided 9.9-71.9% protection in castor oil-induced diarrhea in mice, like verapamil. In isolated rabbit jejunum preparations, crude extract caused inhibition of spontaneous and high K<sup>+</sup>-induced contractions, with respective EC<sub>50</sub> values of  0.3 (0.1-0.5) and 0.5 mg/mL, suggesting Ca<sup>++</sup> channel blockade (CCB). Pretreatment of tissue with crude extract (0.1–1 mg/mL) caused a rightward shift in Ca<sup>++</sup> concentration-response curves. With the exception of aqueous fraction, <em>n</em>-hexane, chloroform and ethyl acetate inhibited spontaneous and high K<sup>+</sup>-induced contractions and displaced rightward Ca<sup>++</sup> concentration-response curves. Extract was found safe up to 10 mg/kg in mice. Our data shows that anti-diarrheal effect of crude extract of <em>E. umbellate</em> is due to CCB-mediated spasmolytic effect, concentrated in the ethyl acetate fraction and suggests its medicinal importance in diarrhea and spasm.</p><p><strong>Video Clip</strong></p><p><a href="https://youtube.com/v/Qo_y3ULC4E0">Isolation of rat jejunum</a>:  2 min 32 sec </p>

scholarly journals Pharmacological basis for medicinal use of Ziziphyus nummularia (Rhamnaceae) leaves in gastrointestinal disorders

2017 ◽  
Vol 16 (10) ◽  
pp. 2379-2385
Author(s):  
Sayed Muzahir Hussain ◽  
Aslam Khan ◽  
Arif-ullah Khan ◽  
Neelum Gul Qazi ◽  
Fawad Ali
Keyword(s):  
Castor Oil ◽  
Saline Group ◽  
Antagonistic Effect ◽  
Fluid Accumulation ◽  
Response Curves ◽  
Medicinal Use ◽  
Gastrointestinal Ulcer ◽  
Rabbit Jejunum ◽  
Ziziphus Nummularia ◽  
Pharmacological Basis

Purpose: To explore the pharmacological basis for the folkloric use of Ziziphus nummularia for treating diarrhea and gastrointestinal spasm.Methods: Ziziphus nummularia crude extract (Zn.Cr) was investigated for  antidiarrheal activity (50, 100 and 300 mg/kg) in terms of reduction diarrhea  droppings as well as for antisecretory activity (300 and 1000 mg/kg) in castor-oil induced model in mice. The effect of the extract on potassium chloride (KCl, 80 mM)-induced contractions in isolated rabbit jejunum tissues were was also  examined. Furthermore, the antiulcer properties of the extract was assessed in an ethanol-induced gastrointestinal ulcer model.Results: Zn.Cr (50 – 1000 mg/kg) exhibited protective effect against castor  oil-induced diarrhea (p <0.05, p < 0.01 vs saline group) and intestinal fluid  accumulation (p < 0.001 vs. castor oil group) in mice. In isolated rabbit jejunum model, Zn.Cr concentration-dependently (0.01, 0.1, 0.3, 0.5, 1 and 3 mg/mL) caused relaxation of spontaneous and KCl-induced contractions, similar to  verapamil. Calcium antagonistic effect was indicated, as pretreatment of intestinal tissues with Zn.Cr (0.3, 0.5 and 1.0 mg/mL) produced a rightward shift in Ca2+ concentration-response curves, with suppression of maximum contraction. In ethanol-induced gastric ulceration assay, Zn.Cr (300 and 1000 mg/kg) caused52.5 and 93.6 % inhibition, respectively (p < 0.001 vs. saline group).Conclusion: These results reveal that Ziziphus nummularia possesses anti-diarrheal, anti-secretory, anti-spasmodic and anti-ulcer actions, mediated possibly through voltage-gated Ca2+channel blockade.Keywords: Ziziphus nummularia, Anti-diarrheal, Anti-secretory, Anti-spasmodic, Anti-ulcer

Dissection of the Calcium Channel Domains Responsible for Modulation of Neuronal Voltage-Dependent Calcium Channels by G Proteins

1999 ◽  
Vol 868 (1 MOLECULAR AND) ◽  
pp. 160-174 ◽  
Author(s):  
ANNETTE C. DOLPHIN ◽  
KAREN M. PAGE ◽  
NICHOLAS S. BERROW ◽  
GARY J. STEPHENS ◽  
CARLES CANTI
Keyword(s):  
Calcium Channels ◽  
Calcium Channel ◽  
G Proteins ◽  
Voltage Dependent ◽  
Voltage Dependent Calcium Channels

scholarly journals Partners in Crime: Towards New Ways of Targeting Calcium Channels

2019 ◽  
Vol 20 (24) ◽  
pp. 6344 ◽  
Author(s):  
Lucile Noyer ◽  
Loic Lemonnier ◽  
Pascal Mariot ◽  
Dimitra Gkika
Keyword(s):  
Calcium Channels ◽  
Calcium Channel ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Interaction Domain ◽  
Domain Structures ◽  
Voltage Dependent ◽  
Voltage Dependent Calcium Channels ◽  
Transient Receptor ◽  
Partner Proteins

The characterization of calcium channel interactome in the last decades opened a new way of perceiving ion channel function and regulation. Partner proteins of ion channels can now be considered as major components of the calcium homeostatic mechanisms, while the reinforcement or disruption of their interaction with the channel units now represents an attractive target in research and therapeutics. In this review we will focus on the targeting of calcium channel partner proteins in order to act on the channel activity, and on its consequences for cell and organism physiology. Given the recent advances in the partner proteins’ identification, characterization, as well as in the resolution of their interaction domain structures, we will develop the latest findings on the interacting proteins of the following channels: voltage-dependent calcium channels, transient receptor potential and ORAI channels, and inositol 1,4,5-trisphosphate receptor.

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