Displaying all 13 publications

Abstract:
Sort:
  1. Salman M, Khan AH, Syed Sulaiman SA, Khan JH, Hussain K, Shehzadi N
    Biomed Res Int, 2017;2017:4269875.
    PMID: 29124064 DOI: 10.1155/2017/4269875
    Background: Numerous medications are known to be associated with the development of lower urinary tract symptoms (LUTS). One such medication group is calcium channel blockers (CCB).

    Objective: To critically examine the literature regarding the involvement of CCB in manifestation of LUTS in humans.

    Methods: A systematic literature search was conducted on PubMed, SciELO, Scopus, and OpenGrey databases to find all potentially relevant research studies before August 2016.

    Results: Five studies met the inclusion criteria and were included in this review. Three out of five studies stated that CCB were involved in either precipitation or exacerbation of LUTS. As for the remaining two studies, one study found out that only the monotherapy of CCB was associated with increased prevalence of nocturia and voiding symptoms in young females, whereas the other study reported an inverse association of CCB with LUTS. The methodological quality of studies was considered high for four studies and low for one study.

    Conclusion: Healthcare providers should make efforts for an earlier identification of the individuals at risk of LUTS prior to the commencement of CCB therapy. Moreover, patients should be counselled to notify their healthcare provider if they notice urinary symptoms after the initiation of CCB.

    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  2. Xie CB, Shaikh LH, Garg S, Tanriver G, Teo AE, Zhou J, et al.
    Sci Rep, 2016 Apr 21;6:24697.
    PMID: 27098837 DOI: 10.1038/srep24697
    Aldosterone-producing adenomas (APAs) vary in phenotype and genotype. Zona glomerulosa (ZG)-like APAs frequently have mutations of an L-type calcium channel (LTCC) CaV1.3. Using a novel antagonist of CaV1.3, compound 8, we investigated the role of CaV1.3 on steroidogenesis in the human adrenocortical cell line, H295R, and in primary human adrenal cells. This investigational drug was compared with the common antihypertensive drug nifedipine, which has 4.5-fold selectivity for the vascular LTCC, CaV1.2, over CaV1.3. In H295R cells transfected with wild-type or mutant CaV1.3 channels, the latter produced more aldosterone than wild-type, which was ameliorated by 100 μM of compound 8. In primary adrenal and non-transfected H295R cells, compound 8 decreased aldosterone production similar to high concentration of nifedipine (100 μM). Selective CaV1.3 blockade may offer a novel way of treating primary hyperaldosteronism, which avoids the vascular side effects of CaV1.2-blockade, and provides targeted treatment for ZG-like APAs with mutations of CaV1.3.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  3. Abdullah HSTSH, Chia PW, Omar D, Chuah TS
    Sci Rep, 2021 07 09;11(1):14227.
    PMID: 34244589 DOI: 10.1038/s41598-021-93662-2
    Herbicide resistance is a worldwide problem in weed control. This prompts researchers to look for new modes of action to slow down the evolution of herbicide-resistant weeds. This research aims to determine the herbicidal action of thiazolo[3,2-a]pyrimidines derivatives, which are well known as antihypertensive drugs. The phytotoxic effects of ten compounds were investigated using leaf disc discoloration test and seed germination bioassay. At concentrations of 125 to 250 mg/L, the 5-(3-Fluoro-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid ethyl ester (c) was highly active against Oldenlandia verticillata and Eleusine indica. At application rates of 1.25 to 2.5 kg ai/ha, formulated c demonstrated selective post-emergence and pre-emergence herbicidal activity against O. verticillata, E. indica and Cyperus iria. In the crop tolerance test, formulated c outperformed the commercial herbicide diuron, with aerobic Oryza sativa being the most tolerant, followed by Zea mays, and Brassica rapa. The addition of calcium chloride partially nullified compound c's inhibitory effects on weed shoot growth, indicating that it has potential as a calcium channel blocker. Compound c acted by triggering electrolyte leakage without affecting photosystem II. These findings imply that c could be explored further as a template for developing new herbicides with novel modes of action.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology*
  4. Harun MSR, Marsh V, Elsaied NA, Webb KF, Elsheikha HM
    Brain Res, 2020 11 01;1746:147002.
    PMID: 32592740 DOI: 10.1016/j.brainres.2020.147002
    Toxoplasma gondii can cause parasitic encephalitis, a life-threatening infection that predominately occurs in immunocompromised individuals. T. gondii has the ability to invade the brain, but the mechanisms by which this parasite crosses the blood-brain-barrier (BBB) remain incompletely understood. The present study reports the changes associated with infection and replication of T. gondii within human brain microvascular endothelial cells (BMECs) in vitro. Our results indicated that exposure to T. gondii had an adverse impact on the function and integrity of the BMECs - through induction of cell cycle arrest, disruption of the BMEC barrier integrity, reduction of cellular viability and vitality, depolarization of the mitochondrial membrane potential, increase of the DNA fragmentation, and alteration of the expression of immune response and tight junction genes. The calcium channel/P-glycoprotein transporter inhibitor verapamil was effective in inhibiting T. gondii crossing the BMECs in a dose-dependent manner. The present study showed that T. gondii can compromise several functions of BMECs and demonstrated the ability of verapamil to inhibit T. gondii crossing of the BMECs in vitro.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology*
  5. Hoe SZ, Lee CN, Mok SL, Kamaruddin MY, Lam SK
    Clinics (Sao Paulo), 2011;66(1):143-50.
    PMID: 21437451
    INTRODUCTION: Gynura procumbens has been shown to decrease blood pressure via inhibition of the angiotensinconverting enzyme. However, other mechanisms that may contribute to the hypotensive effect have not been studied.

    OBJECTIVES: To investigate the cardiovascular effects of a butanolic fraction of Gynura procumbens in rats.

    METHODS: Anaesthetized rats were given intravenous bolus injections of butanolic fraction at doses of 2.5-20 mg/kg in vivo. The effect of butanolic fraction on vascular reactivity was recorded in isolated rat aortic rings in vitro.

    RESULTS: Intravenous administrations of butanolic fraction elicited significant (p < 0.001) and dose-dependent decreases in the mean arterial pressure. However, a significant (p < 0.05) decrease in the heart rate was observed only at the higher doses (10 and 20 mg/kg). In isolated preparations of rat aortic rings, phenylephrine (1 × 10⁻⁶ M)- or potassium chloride (8 × 10⁻² M)-precontracted endothelium-intact and -denuded tissue; butanolic fraction (1 × 10⁻⁶ - 1 × 10⁻¹ g/ml) induced similar concentration-dependent relaxation of the vessels. In the presence of 2.5 × 10⁻³ and 5.0 × 10⁻³ g/ml butanolic fraction, the contractions induced by phenylephrine (1 × 10⁻⁹-3 × 10⁻⁵ M) and potassium chloride (1 × 10⁻² - 8 × 10⁻² M) were significantly antagonized. The calcium-induced vasocontractions (1 × 10⁻⁴-1 × 10⁻²M) were antagonized by butanolic fraction concentration-dependently in calcium-free and high potassium (6×10⁻² M) medium, as well as in calcium- and potassium-free medium containing 1×10⁻⁶ M phenylephrine. However, the contractions induced by noradrenaline (1 × 10⁻⁶ M) and caffeine (4.5 × 10⁻² M) were not affected by butanolic fraction.

    CONCLUSION: Butanolic fraction contains putative hypotensive compounds that appear to inhibit calcium influx via receptor-operated and/or voltage-dependent calcium channels to cause vasodilation and a consequent fall in blood pressure.

    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  6. Ghayur MN, Gilani AH, Khan A, Amor EC, Villaseñor IM, Choudhary MI
    Phytother Res, 2006 Jan;20(1):49-52.
    PMID: 16397921
    Syzygium samarangense (Family; Myrtaceae) or 'makopa', as it is commonly known, is native to Malaysia, some islands of Indonesia and to Far East in general. This study was undertaken to rationalize the use of this plant in hypermotility states of the gut. The hexane extract of S. samarangense (Ss.Hex) was found to dose-dependently (10-3000 microg/mL) relax the spontaneously contracting isolated rabbit jejunum. When tested for a possible calcium channel blocking (CCB) activity, the extract (10-1000 microg/mL) relaxed the high K+-induced contractions and also decreased the Ca++ dose-response curves in a dose-dependent manner (30-100 microg/mL), confirming the CCB activity. Four flavonoids isolated from the hexane extract were tested for a possible spasmolytic activity. All flavonoids, identified as: 2'-hydroxy-4',6'-dimethoxy-3'-methylchalcone (SS1), 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone (SS2), 2',4'-dihydroxy-6'-methoxy-3'-methylchalcone (SS3) and 7-hydroxy-5-methoxy-6,8-dimethylflavanone (SS4), showed dose-dependent (10-1000 microg/mL) spasmolytic activity with SS2 being the most potent. These results indicate that the presence of compounds with spasmolytic and calcium antagonist activity may be responsible for the medicinal use of the plant in diarrhoea.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  7. Khan AU, Ullah R, Khan A, Mustafa MR, Hussain J, Murugan DD, et al.
    Clin Exp Hypertens, 2012;34(2):132-9.
    PMID: 21967029 DOI: 10.3109/10641963.2011.601383
    This study describes the vasorelaxant potential of some pure compounds isolated from Phlomis bracteosa L. marrubiin, phlomeoic acid, and two new constituents labeled as RA and RB. In rat thoracic aortic rings denuded of endothelium, marrubiin, phlomeoic acid, RA, and RB caused relaxation of high K(+) (80 mM) and phenylephrine (1 μM)-induced contractions at the concentration range of 1.0-1000 μg/mL. Marrubiin, phlomeoic acid, RA, and RB concentration dependently (3.0-10 μg/mL) shifted the Ca(++) curves to the right obtained in Ca(++)-free medium. The vasodilator effect of marrubiin, phlomeoic acid, RA, and RB was partially blocked by N(ω)-nitro-L-arginine methyl ester in endothelium-intact aorta preparations. These results reveal that P. bracteosa constituents: marrubiin, phlomeoic acid, RA, and RB exhibit vasodilator action occurred via a combination of endothelium-independent Ca(++) antagonism and endothelium-dependent N(ω)-nitro-L-arginine methyl ester-sensitive nitric oxide-modulating mechanism.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  8. Tan CS, Loh YC, Ng CH, Ch'ng YS, Asmawi MZ, Ahmad M, et al.
    Biomed Pharmacother, 2018 Jan;97:985-994.
    PMID: 29136777 DOI: 10.1016/j.biopha.2017.11.021
    Although Banxia Baizhu Tianma Tang (BBT) has been long administered for hypertensive treatment in Traditional Chinese Medicine (TCM), the ratio of the herbal components that makes up the formulation has not been optimized with respect to the anti-hypertensive effect that it inherently possesses. A newly amended BBT (ABBT) formulation was developed using the evidence-based approach of orthogonal stimulus-response compatibility model. The ABBT showed enhanced therapeutic effect while maintaining its traditional theoretical approach rooted in TCM. This study was designed to investigate the possible mechanism of actions involved in the vasodilatory activity of ABBT-50 by evaluating its vasodilative effect on isolated Sprague Dawley rats in the presence of absence of various antagonists. When pre-contracted with phenylephrine, relaxation was observed in endothelium intact (EC50=0.027±0.003mg/ml, Rmax=109.8±2.12%) and denuded aortic rings (EC50=0.409±0.073mg/ml, Rmax=63.15±1.78%), as well as in endothelium intact aortic rings pre-contracted with potassium chloride (EC50=32.7±12.16mg/ml, Rmax=34.02±3.82%). Significant decrease in the vasodilative effect of ABBT-50 was observed in the presence of Nω-nitro-l-arginine methyl ester (EC50=0.12±0.021mg/ml, Rmax=75.33±3.28%), 1H-[1,2,4] Oxadiazolo[4,3-a]quinoxalin-1-one (EC50=0.463±0.18mg/ml, Rmax=54.48±2.02%), methylene blue (EC50=0.19±0.037mg/ml, Rmax=83.69±3.19%), indomethacin (EC50=0.313±0.046mg/ml, Rmax=71.33±4.12%), atropine (EC50=0.146±0.013mg/ml, Rmax=77.2±3.41%), and 4-aminopyridine (EC50=0.045±0.008mg/ml, Rmax=95.55±2.36%). ABBT-50 was also suppressing Ca2+ release from sarcoplasmic reticulum and inhibiting calcium channels. Vasodilatory effects of ABBT-50 are mediated through NO/sGC/cGMP cascade and PGI2, followed by muscarinic pathways and calcium channels.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  9. Bhaskar HN, Udupa SL, Udupa AL
    Indian J Exp Biol, 2005 Mar;43(3):294-6.
    PMID: 15816421
    Effect of two calcium channel blockers (CCBs) nifedipine and amlodipine, was studied on normal and steroid depressed wound healing in albino rats, using the dead space wound model. The drugs enhanced normal healing as evidenced by increase in tensile strength of 10 days old granulation tissue. There was neither a significant change in the hydroxyproline level (or collagen) nor a change in the glycosaminoglycan content in granulation tissue. However, lysyloxidase level was increased significantly. The increase in tensile strength could thus be attributed to better cross-linking and maturation of collagen rather than collagen synthesis per se. The drugs were also able to overcome steroid depressed wound healing. It is likely that the prohealing effects may be related to the improved antioxidant status too, since superoxide dismutase levels were observed to be higher in the CCB- treated animals.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  10. Salleh N, Ahmad VN
    BMC Complement Altern Med, 2013 Dec 14;13:359.
    PMID: 24330515 DOI: 10.1186/1472-6882-13-359
    BACKGROUND: Ficus deltoidea, is a perennial herb that is used to assist labor, firm the uterus post-delivery and to prevent postpartum bleeding. In view of its claimed uterotonic action, the mechanisms underlying plant's effect on uterine contraction were investigated.

    METHODS: Adult female SD rats were injected with 2 mg/kg 17β-oestradiol (E2) to synchronize their oestrous cycle. A day after injection, uteri were removed for in-vitro contraction studies. The dose dependent effect of Ficus deltoidea aqeous extract (FDA) on the tension produced by the isolated rat's uteri was determined. The effects of atropine (2×10(-8) M), atosiban (0.5 IU), THG113.31 (10 μM), oxodipine (0.25 mM), EDTA (1 mM), 2-amino-ethoxy-diphenylborate (2-APB) (40 mM) and thapsigargin (1 mM) on the maximum force of contraction (Emax) achieved following 2 mg/ml FDA administration were also investigated.

    RESULTS: FDA induced in-vitro contraction of the isolated rat's uteri in a dose-dependent manner. Administration of atropine, atosiban and THG113.31 reduced the Emax with atosiban having the greatest effect. The Emax was also reduced following oxodipine and EDTA administration. There was no significant change observed following 2-APB administration. Thapsigargin, however, augmented Emax.

    CONCLUSIONS: FDA-induced contraction of the isolated rat's uteri is mediated via multiple uterotonin receptors (muscarinic, oxytocin and prostaglandin F2α) and was dependent on the extracellular Ca2+. Contraction, however, was not dependent on the Ca2+ release from the internal stores. This in-vitro study provides the first scientific evidence on the claimed effect of Ficus Deltoidea on uterine contraction.

    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  11. Bello I, Usman NS, Mahmud R, Asmawi MZ
    J Ethnopharmacol, 2015 Dec 4;175:422-31.
    PMID: 26429073 DOI: 10.1016/j.jep.2015.09.031
    Alstonia scholaris has a long history of use in the Ayurveda traditional treatment of various ailments including hypertension. We have reported the blood pressure lowering activity of the extract of A. scholaris. The following research aim to delineate the pharmacological mechanism involve in the antihypertensive action.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology*
  12. Ch'ng YS, Loh YC, Tan CS, Ahmad M, Asmawi MZ, Wan Omar WM, et al.
    J Med Food, 2018 Mar;21(3):289-301.
    PMID: 29420109 DOI: 10.1089/jmf.2017.4008
    The seeds of Swietenia macrophylla King (SM) (Meliaceae) are used as a folk medicine for the treatment of hypertension in Malaysia. However, the antihypertensive and vasorelaxant effects of SM seeds are still not widely studied. Thus, this study was designed to investigate the in vivo antihypertensive effects and in vitro mechanism of vasorelaxation of a 50% ethanolic SM seed extract (SM50) and the fingerprint of SM50 was developed through tri-step Fourier transform infrared (FTIR) spectroscopy. The vasorelaxant activity and the underlying mechanisms of SM50 were evaluated on thoracic aortic rings isolated from Sprague-Dawley rats in the presence of antagonists. The pharmacological effect of SM50 was investigated by oral administration of spontaneously hypertensive rats (SHRs) with three different doses of SM50 (1000, 500, and 250 mg/kg/day) for 4 weeks and their systolic blood pressure (SBP) and diastolic blood pressure (DBP) values were measured weekly using tail-cuff method. The tri-step FTIR macro-fingerprint of SM50 showed that SM50 contains stachyose, flavonoids, limonoids, and ester, which may contribute to its vasorelaxant effect. The results showed that the vasorelaxant activity of SM50 was mostly attributed to channel-linked receptors pathways through the blockage of voltage-operated calcium channels (VOCC). SM50 also acts as both potassium channels opener and inositol triphosphate receptor (IP3R) inhibitor, followed by β2-adrenergic pathway, and ultimately mediated through the nitric oxide/soluble guanylyl cyclase/cyclic 3',5'-guanosine monophosphate (NO/sGC/cGMP) signaling pathways. The treatment of SM50 also significantly decreased the SBP and DBP in SHRs. In conclusion, the antihypertensive mechanism of SM50 was mediated by VOCC, K+ channels, IP3R, G-protein-coupled β2-adrenergic receptor, and followed by NO/sGC/cGMP signaling mechanism pathways in descending order. The data suggested that SM50 has the potential to be used as a herbal medicament to treat hypertension.
    Matched MeSH terms: Calcium Channel Blockers/pharmacology
  13. Janbaz KH, Arif J, Saqib F, Imran I, Ashraf M, Zia-Ul-Haq M, et al.
    BMC Complement Altern Med, 2014 Feb 22;14:71.
    PMID: 24559094 DOI: 10.1186/1472-6882-14-71
    BACKGROUND: Isodon rugosus is used in folk Pakistan traditional practices to cure ailments related to gastrointestinal, respiratory and cardiovascular problems. Present study was undertaken to validate these folkloric uses.

    METHODS: A crude methanol extract of the aerial parts of Isodon rugosus (Ir.Cr.) was used for both in vitro and in vivo experiments. The plant extract was tested on isolated rabbit jejunum preparations for possible presence of spasmolytic activity. Moreover, isolated rabbit tracheal and aorta preparations were used to ascertain the relaxant effects of the extract. Acetylcholinesterase and butyrylcholinesterase inhibitory activities of Ir.Cr were also determined as well as its antioxidant activity. The in vivo antiemetic activity of the extract was evaluated by using the chick emesis model, while the analgesic and antipyretic activities were conducted on albino mice.

    RESULTS: The application of the crude extract of I. rugosus to isolated rabbit jejunum preparations exhibited relaxant effect (0.01-0.3 mg/ml). The Ir.Cr also relaxed K+(80 m M)-induced spastic contractions in isolated rabbit jejunum preparations and shifted the Ca+2 concentration response curves towards right (0.01-0.3 mg/ml). Similarly, the extract, when applied to the isolated rabbit tracheal preparations relaxed the carbachol (1 μM)--as well as K+ (80 mM)-induced contractions in a concentration range of 0.01-1.0 mg/ml. Moreover, it also relaxed (0.01-3.0 mg/ml) the phenylephrine (1 μM)- and K+ (80 mM)-induced contractions in isolated rabbit aorta preparations. The Ir.Cr (80 mg/kg) demonstrated antipyretic activity on pyrogen-induced pyrexia in rabbits as compared to aspirin as standard drug. The Ir.Cr also exhibited anti-oxidant as well as inhibitory effect on acetyl- and butyryl-cholinesterase and lipoxygenase (0.5 mg/ml).

    CONCLUSIONS: The observed relaxant effect on isolated rabbit jejunum, trachea and aorta preparations caused by Ir.Cr is possibly to be mediated through Ca+2 channel blockade and therefore may provided scientific basis to validate the folkloric uses of the plant in the management of gastrointestinal, respiratory and cardiovascular ailments. The observed antioxidant activity as well as the lipoxygenase inhibitory activity may validate its traditional use in pain and inflammations.

    Matched MeSH terms: Calcium Channel Blockers/pharmacology
Filters
Contact Us

Please provide feedback to Administrator ([email protected])

External Links