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1.
Ethnopharmacological relevance
Disturbed gastrointestinal (GI) motility can be associated with smooth muscle abnormalities and dysfunction. Exploring innovative approaches that can modulate the disturbed colonic motility are of great importance for clinical therapeutics. Naringenin, a flavonoid presented in many traditional Chinese herbal medicines, has been shown to have a relaxant effect on different smooth muscles. The aim of the present study was to investigate the effect of naringenin on regulation of GI motility.Material and methods
Mechanical recording was used to investigate the effect of naringenin on isolated rat colonic smooth muscle spontaneous contractions. Whole cell patch clamp, intracellular [Ca2+] concentration ([Ca2+]i) and membrane potential measurements were examined on primary cultures of colonic smooth muscle cells (SMCs). A neostigmine-stimulated rat model was utilized to investigate the effect of naringenin in vivo.Results
Naringenin induced a concentration-dependent inhibition (1–1000 μM) on rat colonic spontaneous contraction, which was reversible after wash out. The external Ca2+ influx induced contraction and [Ca2+]i increase were inhibited by naringenin (100 μM). In rat colonic SMCs, naringenin-induced membrane potential hyperpolarization was sensitive to TEA and selective large-conductance calcium-activated K+ (BKCa) channel inhibitor iberiotoxin. Under whole cell patch-clamp condition, naringenin stimulated an iberiotoxin-sensitive BKCa current, which was insensitive to changes in the [Ca2+]i concentration. Furthermore, naringenin significantly suppressed neostigmine-enhanced rat colon transit in vivo.Conclusion
Our results for the first time demonstrated the relaxant effect of flavonoid naringenin on colon smooth muscle both in vitro and in vivo. The relaxant effect of naringenin was attributed to direct activation of BKCa channels, which subsequently hyperpolarized the colonic SMCs and decreased Ca2+ influx through VDCC. Naringenin might be of therapeutic value in the treatment of GI motility disorders. 相似文献2.
Ethnopharmacological relevance
Ligusticum chuanxiong Hort. (Umbelliferae), a traditional Chinese medicinal herb, is often prescribed together with nitric oxide donors for treating coronary heart diseases such as angina in China; however, studies concerning their pharmacological interaction are scarce.Aim of the study
The objective of the present study was to examine the interaction between the Ligusticum chuanxiong major active constituent butylidenephthalide (BDPH) and the nitric oxide donor sodium nitroprusside (SNP) in vasorelaxation.Materials and methods
Vasorelaxation was examined in rat isolated aorta using an organ bath system.Results
BDPH and SNP interacted synergistically under 9,11-dideoxy-9α,11α-methanoepoxyprostaglandin H2 (U-46619)-induced tone. This synergism became greater with increasing U-46619 concentrations where Ca2+ sensitization contributed more significantly, and less when U-46619 was replaced with phenylephrine where participation of Ca2+ sensitization was minimal. BDPH-SNP synergism remained intact in the absence of external Ca2+, indicating that regulation of Ca2+ influx was not a requirement for the manifestation of this interaction.Conclusions
The present study demonstrated the synergistic relaxation between BDPH and SNP in rat isolated aorta. This interaction is related to an enhancement of the effectiveness of SNP in producing relaxation under tone induced mainly by Ca2+ sensitization. 相似文献3.
Ethnopharmacological relevance
Ginseng–Aconite Decoction (GAD), a traditional oriental medicine composed of Panax ginseng C.A. Mey. (Araliaceae) and Aconitum carmichaeli Debx. (Ranunculaceae) has been used as treatment for cardiovascular diseases from Song Dynasty of China. The purpose of the present study was to elucidate the possible mechanisms of GAD-induced positive inotropic effect.Material and methods
GAD-induced changes in atrial dynamics and cAMP efflux were determined in isolated perfused beating rabbit atria.Results
GAD significantly increased atrial dynamics such as stroke volume, pulse pressure and augmented cAMP efflux in beating rabbit atria. The inotropic effect was significantly attenuated by pre-treatment with KB-R7943, a reverse mode Na+/Ca2+ exchanger blocker. The GAD-induced increase in atrial dynamics was also markedly inhibited by staurosporine, a non-selective protein kinase inhibitor, and partly blocked by KT5720, a selective PKA inhibitor. The effect of GAD on atrial dynamics was not altered by pre-treatment with propranolol, a β-adrenergic receptor inhibitor, or diltiazem, an L-type Ca2+channel blocker. The phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine (IBMX) failed to modulate the GAD-induced increase in atrial dynamics, but markedly attenuated cAMP efflux in the beating atria.Conclusion
These results suggest that the GAD-induced positive inotropic effect in beating rabbit atria may be attributable to stimulation of the reverse mode Na+/Ca2+ exchanger, while PKA activity would, at least in part, be participated in the course. 相似文献4.
Ethnopharmacological relevance
Radix Paeoniae Rubra (RPR) is an important traditional Chinese medicine (TCM) commonly used in clinic for a long history in China. RPR is the radix of either Paeonia lactiflora Pall. or Paeonia veitchii Lynch. RPR has a wide variety of pharmacological actions such as anti-thrombus, anti-coagulation, and anti-atherosclerotic properties, protecting heart and liver. However, the mechanisms involved are to be defined.Aim of the study
The aim of the present study was to define the effect of Paeonia lactiflora Pall. extracts on vascular tension and responsible mechanisms in rat thoracic aortic rings.Materials and methods
Ethanol extract of Paeonia lactiflora Pall. (EPL) was examined for their vascular relaxant effects in isolated phenylephrine-precontracted rat thoracic aorta.Results
EPL induced relaxation of the phenylephrine-precontracted aortic rings in a concentration-dependent manner. Vascular relaxation induced by EPL was significantly inhibited by removal of the endothelium or pretreatment of the rings with NG-nitro-l-arginine methylester (l-NAME) or 1H-[1,2,4]-oxadiazolo-[4,3-α]-quinoxalin-1-one (ODQ). Extracellular Ca2+ depletion or diltiazem significantly attenuated EPL-induced vasorelaxation. Modulators of the store-operated Ca2+ entry (SOCE), thapsigargin, 2-aminoethyl diphenylborinate and Gd3+, and an inhibitor of Akt, wortmannin, markedly attenuated the EPL-induced vasorelaxation. Further, the EPL-induced vasorelaxation was significantly attenuated by pretreatment with tetraethylammonium, a non-selective KCa channels blocker, or glibenclamide, an ATP-sensitive K+ channels inhibitor, respectively. Inhibition of cyclooxygenases with indomethacin, and adrenergic and muscarinic receptors blockade had no effects on the EPL-induced vasorelaxation.Conclusions
The present study suggests that EPL relaxes vascular smooth muscle via endothelium-dependent and Akt- and SOCE-eNOS-cGMP-mediated pathways through activation of both KCa and KATP channels and inhibition of L-type Ca2+ channels. 相似文献5.
Ethnopharmacological relevance
Danshen is a commonly used traditional Chinese medicine and has received considerable attention due to their beneficial effects on the health, including prevention of cardiovascular disease, and cancer. Tanshinone IIA, a major active constituent of Danshen, has been reported to have a neuroprotective profile.Aim of the study
An excessive release of glutamate is considered to be related to neuropathology of several neurological diseases. In this study, we investigated whether tanshinone IIA could affect endogenous glutamate release and explored the possible mechanism.Materials and methods
The experimental model was the isolated nerve terminals (synaptosomes) purified from the rat cerebral cortex. The release of glutamate was evoked by the K+ channel blocker 4-aminopyridine (4-AP) and measured by one-line enzyme-coupled fluorometric assay. We also used a membrane potential-sensitive dye to assay nerve terminal excitability and depolarization, and a Ca2+ indicator, Fura-2-acetoxymethyl ester, to monitor cytosolic Ca2+ concentrations ([Ca2+]C).Results
Tanshinone IIA inhibited the release of glutamate evoked by 4-AP in a concentration-dependent manner. Inhibition of glutamate release by tanshinone IIA was prevented by the chelating the extracellular Ca2+ ions, and by the vesicular transporter inhibitor bafilomycin A1. However, the glutamate transporter inhibitor DL-threo-beta-benzyl-oxyaspartate did not have any effect on the action of tanshinone IIA. Tanshinone IIA decreased the depolarization-induced increase in [Ca2+]C, whereas it did not alter the resting synaptosomal membrane potential or 4-AP-mediated depolarization. Furthermore, the effect of tanshinone IIA on evoked glutamate release was prevented by the Cav2.2 (N-type) and Cav2.1 (P/Q-type) channel blocker ω-conotoxin MVIIC, but not by the ryanodine receptor blocker dantrolene or the mitochondrial Na+/Ca2+ exchanger blocker CGP37157. Mitogen-activated protein kinase (MEK) inhibition also prevented the inhibitory effect of tanshinone IIA on evoked glutamate release.Conclusion
These results show that tanshinone IIA inhibits glutamate release from cortical synaptosomes in rats through the suppression of presynaptic voltage-dependent Ca2+ entry and MEK signaling cascade. 相似文献6.
Tsai CC Huang SC Liu JK Wang HC Tsai TR Tsai PJ Liu CW Chang LC 《Journal of ethnopharmacology》2012,142(3):694-699
Ethnopharmacological relevance
Danshen, root of Salvia miltiorrhiza (SM), has been traditionally used in Chinese medicine for the treatment of heart, abdomen, gurgling in the intestines, and relieving fullness. However, the effects of SM on intestine have rarely been done to date.Aim of the study
To investigate the contraction effect of SM on isolated rat ileum and its mechanisms involved.Materials and methods
The isometric contractions of ileum segments were investigated in organ baths for spontaneous activity and response to ethanolic extracts of SM. To determine the contraction mechanism caused by SM extracts, atropine (a muscarinic receptor antagonist), tetrodotoxin (TTX, a sodium channel blocker), nifedipine (a calcium channel blocker), Ca2+ free Krebs solution with EGTA, or trifluoperazine (TFP, a calmodulin blocker) was administered and its response to cumulative dosages of SM extracts were examined. The effect of SM extracts on Ca2+ signaling in the intestinal epithelial cell-6 (IEC-6) was examined using fura-2 as a Ca2+ indicator.Results
SM extracts caused dose-dependent tonic contraction on rat ileum in ex vivo organ bath studies. The contraction induced by SM extracts was not inhibited by atropine, TTX, nifedipine, or in Ca2+ free solution. However, the ileal contractions induced by SM extracts were significantly inhibited by TFP in a dose-dependent manner. In IEC-6 cells, the SM extracts induced extracellular Ca2+ entry and massive intracellular Ca2+ release in Ca2+-contained medium, and induced intracellular Ca2+ release in Ca2+-free medium.Conclusion
These results demonstrate that SM extracts cause ileal contraction through the Ca2+-calmodulin pathway. 相似文献7.
Aim of the study
The present study deals with the anti-spasmodic activity of the aqueous and the methanolic extracts of the leaves and the root barks of Zizyphus lotus (L.) Desf. on male rats.Materials and methods
This activity was assessed on contractions of isolated rat duodenum, induced by acetylcholine, KCl, and BaCl2 and compared with the effect of atropine and papaverine.Results
Both extracts of leaves and root barks caused significant relaxation of spontaneous contractions and produced a concentration-dependent inhibition (P < 0.01–0.001) of contraction induced by spasmogenic agents.Conclusion
These results indicate that Zizyphus lotus extracts contain anti-spasmodic constituents mediating their effect through cholinergic receptors and blockade Ca2+ influx. This could explain the traditional use of Zizyphus lotus in the treatment of the intestinal diseases. 相似文献8.
Ethnopharmacological relevance
Korean red ginseng (KRG), one of heat-processed Korean ginseng (Panax ginseng C.A. Meyer), has a long history as herbal remedy for antidiabetic effect.Aim of the study
The effect and mechanism of KRG on stimulation of insulin release were investigated in isolated rat pancreatic islets.Material and methods
Pancreatic islets isolated from rats were used to evaluate the insulinotropic action of KRG. The effect of Ca on the insulinotropic action of KRG was investigated.Results
The aqueous ethanolic extract of KRG (AEE-KRG) (0.1–1.0 mg/ml) significantly evoked a stimulation of insulin release at 3.3 mM glucose compared to the control. Experiments at different glucose concentrations (8.4 and 16.7 mM) showed that AEE-KRG significantly stimulated on its own whereas it did not potentiate insulin secretion induced by glucose. The extracellular Ca2+-free condition, a L-type Ca2+ channel blocker and an ATP-sensitive K+ channel opener significantly inhibited insulin secretion evoked by AEE-KRG.Conclusion
These findings suggest that KRG displays beneficial effects in the treatment of diabetes at least in part via the stimulation of insulin release in a glucose-independent manner. 相似文献9.
Chi-Man Koon Subiyanto Fong Elaine Wat Yan-Ping Wang David Wing-Shing Cheung Clara Bik-San Lau Ping-Chung Leung Han-Dong Sun Qin-Shi Zhao Kwok-Pui Fung 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
Erigerontis Herba is widely used as a traditional Chinese medicine and is commonly used for neuroprotection and vascular protection.Aim of study
In this study, the vasodilator effects of Erigerontis Herba (DZXX) were investigated using rat isolated aorta rings.Material and method
The involvement of endothelium in the vasorelaxation was studied by comparing response of endothelium-intact and endothelium-denuded aorta rings which precontracted with U46619. The involvement of K+ channels was studied by pretreatment of the aorta rings with various K+ channel inhibitors. The involvement of Ca2+ channel was studied by incubating aorta rings with Ca2+-free solution, primed with U46619 prior to elicit contraction by addition of Ca2+ solution.Results
DZXX (0.2–2 mg/ml) induced a concentration-dependent relaxation on U44619-precontracted aorta rings with EC50 of 0.354±0.036 mg/ml. Removal of endothelium or pretreatment with a BKCa inhibitor iberiotoxin, KIR inhibitor barium chloride or Kv inhibitor 4-aminopyridine produced no effect on the DZXX-induced vasorelaxation. However, pretreatment with a KATP inhibitor glibenclamide or a non-selective K+ channel inhibitor tetraethylammonium produced significant inhibition on the DZXX-induced vasorelaxation by 29.9% and 21.3%, respectively. Pretreatment with DZXX (0.4, 1.2 and 2 mg/ml) produced a concentration-dependent inhibition on Ca2+-induced vasoconstriction.Conclusions
These results suggest that the vasodilator effect of DZXX was endothelium-independent, mediated by decreasing the influx of Ca2+ by calcium channel inhibition and increasing the influx of K+ by opening of a KATP channel. 相似文献10.
Aim of this study
Aralia cordata has been used to alleviate symptoms of osteoarthritis (OA) in traditional medicine. However, there is no in vivo study related with the therapeutic effects and mechanisms of Aralia cordata. On the basis of this background, our study was designed to examine the cartilage protective and proliferative effects of Aralia cordata by using a collagenase-induced osteoarthritis (CIA) rabbit model.Materials and methods
The right knees of rabbits were injected intra-articularly with collagenase, and rabbits were orally administered with distilled water (vehicle), Aralia cordata (200 mg/kg) and celecoxib (100 mg/kg) once a day for 28 days after the initiation of the CIA.Results
In histopathologic studying by using H&;E and Safranin O staining, Aralia cordata showed a cartilage protective effect in CIA rabbit femoral condyle. However, celecoxib had no effect on cartilage protection in CIA. The inflammatory mediators involved in cartilage destruction, such as COX-2 and PGE2, were inhibited in the Aralia cordata-treated group. Aralia cordata also showed an anti-apoptotic effect through suppression of caspase-3 activity and chondrocyte proliferation induction in both in vivo and in vitro.Conclusion
These results indicate that Aralia cordata showed cartilage protective effects through the down-regulations of COX-2 expression, PGE2 production, caspase-3 activity, and chondrocyte proliferation in the CIA rabbit model. 相似文献11.
Jinhuan Wang Feng Sun Weizheng Sun Haitao Shi Yanli Yong Sijia Liu Limei Liu 《Journal of traditional Chinese medicine》2014
Objective
To observe the clinical efficacy of Busuishengxue granules on non-severe aplastic anemia (NSAA) and investigate its effect on the mitogen-activated protein kinase/extracellular signal-regulated kinase (MAPK/ERK) pathway.Methods
Sixty NSAA patients were divided equally into two groups. Subjects in the experimental group were treated with Busuishengxue granules, and the control group with Zaizaoshengxue tablets. The treatment course was 6 months and curative efficacy was compared between the two groups as well as with 10 healthy individuals. Flow cytometry (FCM) was used to detect the intracellular concentration of Ca2 + ([Ca2 +]i). Western blotting was employed to detect the expression of enzymes in the MAPK/ERK pathway.Results
The efficacy of Busuishengxue granules was significantly better than that of Zaizaoshengxue tablets (P<0.05). Before treatment, expression of JNK, phospho-ERK 1/2 and p-JNK was higher, and [Ca2 +]i higher, than that of the control group (P< 0.05). After treatment with Busuishengxue granules, expression of all enzymes related to signal transduction pathways in the blood cells of NSSA patients were altered to different degrees.Conclusion
Busuishengxue granules had a better effect with regard to improving symptom scores, increasing the number of blood leukocytes, and increasing hemoglobin levels than Zaizaoshengxue tablets, and they differed slightly in terms of increasing the number of platelets. 相似文献12.
Aim of the study
The effect of thymoquinone (TQ), the main constituent of the volatile oil of black seed (Nigella sativa L. family Ranunculaceae), on the isolated rat pulmonary arterial rings was investigated.Materials and methods
Isolated rat pulmonary arterial rings were precontracted with phenylephrine and concentration–response curves to TQ were constructed. The effects of different receptors antagonists or enzyme inhibitors were examined.Results
TQ caused a concentration-dependent decrease in the tension of the pulmonary arterial rings precontracted by phenylephrine. The effects of TQ were not influenced by pretreatment of the rings with propranolol (a non-selective β-blocker), atropine (a non-selective blocker for muscarinic receptors), theophylline (an adenosine receptor antagonist), indomethacin (a cyclooxygenase inhibitor), L-NAME (a NO synthase inhibitor), methylene blue (an inhibitor of soluble guanylyl cyclase) and nifedipine (a Ca2+ channel blocker). The effects of TQ were significantly potentiated by bosentan (an ETA/ETB receptor antagonist). The effects of TQ were slightly abolished by pretreatment of the rings with glibenclamide (a non-selective blocker of ATP-sensitive K+ channels). TQ totally abolished the pressor effects of serotonin and phenylephrine on the isolated rat pulmonary arterial rings.Conclusion
The results of the present study suggest that TQ-induced relaxation of the precontracted pulmonary artery is probably mediated, at least in part, by activation of ATP-sensitive potassium channels and possibly by non-competitive blocking of serotonin, α1 and endothelin receptors. 相似文献13.
Shih-Hurng Loh Yi-Ting Tsai Chung-Yi Lee Chung-Yi Chang Chien-Sung Tsai Tzu-Hurng Cheng Cheng-I Lin 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
Dehydroevodiamine alkaloid (DeHE), a bioactive component of the Chinese herbal medicine Wu-Chu-Yu (Evodiae frutus), exerted antiarrhythmic effect in guinea-pig ventricular myocytes. We further characterize the electromechanical effects of DeHE in the human atrial and ventricular tissues obtained from hearts of patients undergoing corrective cardiac surgery or heart transplantation.Materials and methods
The transmembrane potentials of human myocardia were recorded with a traditional microelectrode technique while sarcolemmal Na+ and Ca2+ currents in single human cardiomyocytes were measured by a whole-cell patch-clamp technique. The intracellular pH (pHi) and Na+–H+ exchanger (NHE) activity were determined using BCECF-fluorescence in human atria.Results
In human atria, DeHE (0.1–0.3 μM) depressed upstroke velocity, amplitude of action potential, and contractile force, both in slow and fast response action potential. Moreover, the similar depressant effects of DeHE were found in human ventricular myocardium. Both in isolated human atrial and ventricular myocytes, DeHE (0.1–1 μM) reversibly, concentration-dependently decreased the Na+ and Ca2+currents. Moreover, DeHE (0.1 and 0.3 μM) suppressed delayed afterdepolarizations and aftercontractions, induced by epinephrine and high [Ca2+]o in atria. In human ventricular myocardium, the strophanthidin-induced triggered activities were attenuated by pretreating DeHE (0.3 μM). The resting pHi and NHE activity were also significantly increased by DeHE (0.1–0.3 μM).Conclusions
We concluded for the first time that, in the human hearts, DeHE could antagonize triggered arrhythmias induced by cardiotonic agents through a general reduction of the Na+ and Ca2+ inward currents, while increase of resting pHi and NHE activity. 相似文献14.
Ethnopharmacological relevance
Aralia nudicaulis, or wild sarsaparilla, is used as a traditional medicinal plant for the treatment of various illnesses by many of the Canadian First Nations. Iroquois and Algonquin First Nations of Eastern Canada use a tea prepared from dried Aralia nudicaulis rhizome as a cough medicine and for the treatment of tuberculosis. Previous investigations of aqueous extracts of Aralia nudicaulis rhizomes have shown it to possess antimycobacterial activity.Aim of the study
To isolate and identify antimycobacterial constituents from Aralia nudicaulis rhizomes.Materials and methods
Methanolic extracts of Aralia nudicaulis rhizomes were subjected to bioassay guided fractionation using the microplate resazurin assay (MRA) to assess inhibitory activity against Mycobacterium tuberculosis strain H37Ra. The antimycobacterial constituents were identified by NMR, MS and polarimetry.Results
Two C17 polyacetylenes with significant antimycobacterial activity were isolated from the Aralia nudicaulis rhizome extract. The polyacetylenes were identified as (3R)-falcarinol and (3R, 9R, 10S)-panaxydol. Falcarinol and panaxydol displayed MICs of 25.6 μM and 36.0 μM and IC50s of 15.3 μM and 23.5 μM against Mycobacterium tuberculosis H37Ra.Conclusions
Falcarinol and panaxydol were identified as the principal constituents responsible for the antimycobacterial activity of Aralia nudicaulis rhizomes validating an ethnopharmacological use of this plant by the Canadian First Nations. 相似文献15.
16.
Gabrieli Penha Bezerra Roberto Wagner da Silva Góis Teresinha Silva de Brito Francisco José Batista de Lima Mary Anne Medeiros Bandeira Nirla Rodrigues Romero Pedro Jorge Caldas Magalhães Gilvandete Maria Pinheiro Santiago 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Hymenaea courbaril L. (Caesalpinoideae) is used in Brazilian folk medicine to treat anemia, kidney problems, sore throat and other dysfunctions of the respiratory system, such as bronchitis and asthma, although such properties are yet to be scientifically validated.Aim of the study
In order to give a scientific basis to support the traditional use of Hymenaea courbaril, this study was designed to evaluate antioxidant, myorelaxant and anti-inflammatory properties of the ethanol extract from stem bark and its fractions. The myorelaxant effect of astilbin, a flavonoid isolated from the bioactive ethyl acetate fraction (EAF), has also been evaluated.Material and methods
In the present study ethanol extract from stem bark (EEHC) and fractions were analyzed using bioassay-guided fractionation. The following activities were investigated: antioxidant by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, myorelaxant on rat tracheal smooth muscle, and anti-inflammatory using ovalbumin-induced leukocytosis and airway hyperresponsiveness in rats.Results
The results of the present investigation show that the whole extract of Hymenaea courbaril and some of its fractions strongly scavenged DPPH radical. The extract showed myorelaxant activity on rat trachea, being EAF its highest efficient fraction. Bio-guided study allowed the isolation of astilbin, a well-known flavonoid. The activity induced by this compound indicates that it may be partly responsible for the myorelaxant effect of EAF. EAF reduced contractions that depended on divalent cation inflow through voltage-operated Ca2+ channels (VOCCs) or receptor-operated Ca2+ channels (ROCCs), but it was more potent to inhibit VOCC- than ROCC-dependent contraction induced by Ca2+ addition in ACh-enriched Ca2+-free medium. Oral pretreatment of antigen-challenged animals with EAF prevented airway hyperresponsiveness on KCl-induced contraction and reduced the number of total white cells, particularly eosinophils and neutrophils in bronchoalveolar lavage.Conclusions
This study provided scientific basis that Hymenaea courbaril presents potential antioxidant, myorelaxant and anti-inflammatory actions, which support its use in folk medicine to treat inflammatory airway diseases. 相似文献17.
Haoping Mao Han Zhang Hong Wang Yuefei Wang Fenrong Zhao Limin Hu Nobuyuki Yanagihara Xiumei Gao 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Salvia miltiorrhiza (Danshen) is a well known traditional Chinese herb, which has been used widely in China for the treatment of cardiovascular diseases in clinic.Aim of this study
The aim of the present study is to clarify the effects of lipophilic extract of Salvia miltiorrhiza (LESM) on catecholamine (CA) secretion, a traditional Chinese medicine used widely for the treatment of cardiovascular diseases in China.Materials and methods
LESM was evaluated for its effects on CA secretion using HPLC-ECD method. The effects of LESM on 22Na+ influx and intracellular calcium ([Ca2+]i) were also investigated.Results
Our results showed that LEMS directly stimulated basal CA secretion in an extracellular Ca2+-dependent manner. And the stimulation was not affected by combination of hexamethonium (Hex), an inhibitor of nAChR. LESM also directly elevated [Ca2+]i. In addition, using selective blockers of voltage-dependent Ca2+ channels, such as nitrendipine (for L-type), ω-agatoxin-IVA (for P-type) and ω-conotoxin-GVIA (for N-type), it was found that nitrendipine suppressed the elevation of [Ca2+]i induced by LESM, but not ω-agatoxin-IVA or ω-conotoxin-GVIA. Compared with acetylcholine (ACh) only, however, combination of LESM with ACh inhibited the raise of CA secretion, 22Na+ influx and [Ca2+]i in a concentration-dependent manner. Furthermore, LESM also inhibited CA secretion induced by veratridine (Ver), and 56 mM K+ at concentrations similar to those for [Ca2+]i rise. One of the lipophilic active compounds, cryptotanshione (Cryp), also had the same effects on CA secretion with LESM.Conclusions
All these findings suggest that LESM exerts dual effects on CA secretion in cultured bovine adrenal medullary cells. LESM exerts antagonistic effects on nAChR, voltage-dependent Na+ and Ca2+ channels, whereas it is an agonist of L-type Ca2+ channel when it used alone. 相似文献18.
Francesca Borrelli Nicola Borbone Raffaele Capasso Domenico Montesano Simona De Marino Gabriella Aviello Giovanni Aprea Stefania Masone Angelo A. Izzo 《Journal of ethnopharmacology》2009
Ethnopharmacological importance
Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.Aim of the study
To investigate the mode of the relaxing action of a methanolic extract prepared from the seeds of Celastrus paniculatus (CPE, 0.0001–10 μg/mL) in the rat ileum and to try to confirm on human tissues the intestinal pharmacological activity of the extract.Materials and methods
The relaxant effect of CPE was studied in vitro by evaluating its effect on the spontaneous contractions of the isolated ileum.Results
CPE exerted a tetrodotoxin- and ω-conotoxin-resistant inhibitory effect on rat ileum motility (IC50: 0.24 ± 0.02 μg/mL; Emax: 99.0 ± 0.60%). The inhibitory effect was reduced by nifedipine but not by cyclopiazonic acid. Experiments with specific antagonists enabled us to exclude the involvement of the main endogenous spasmogenic (i.e. acetylcholine and tachykinins) and relaxing (noradrenaline, nitric oxide, ATP) compounds. CPE also relaxed the isolated human ileum (IC50: 0.26 ± 0.02 μg/mL; Emax: 99.1 ± 0.46%).Conclusion
It is concluded that (i) CPE exerted a powerful myogenic and L-type Ca2+-dependent relaxing effect in the isolated rat ileum and that (ii) the human ileum is sensitive to the inhibitory effect of CPE. If confirmed in vivo, our data could explain the traditional use of this herb in the treatment of intestinal spasms. 相似文献19.
François Senejoux Céline Demougeot Magdalena Cuciureanu Anca Miron Rodica Cuciureanu Alain Berthelot Corine Girard-Thernier 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Aerial parts of Heracleum sphondylium L. (HS) are used in traditional medicine to treat hypertension. To provide pharmacological basis for this use, we investigated the vasorelaxant effects of a dichloromethane extract of HS (HSDE) and the mechanisms involved.Materials and methods
Activity of HSDE was evaluated on rat isolated thoracic aortic rings.Results
HSDE induced vasorelaxation in phenylephrine (PE, 10−6 mol/L) and high KCl—(6×10−2 mol/L) pre-contracted aortic rings that was independent on the presence of endothelium. HSDE markedly decreased extracellular Ca2+-induced contraction in high-KCl and PE pre-challenged rings. It also inhibited the intracellular Ca2+ release sensitive to PE (10−6 M). The relaxant effect of HSDE were blunted by 4-amino-pyridine (4-AP, 10−3 mol/L), an inhibitor of voltage-dependent K+ channels.Conclusion
Our results provide the first evidence that a dichloromethane extract of Heracleum sphondylium L. exhibits vasorelaxant properties through endothelium-independent mechanisms involving the inhibition of Ca2+ mobilization and changes in Kv channel conductances. These data argue for its use as antihypertensive therapy in traditional medicine. 相似文献20.
Qiyang Shou Shuizhen Pan Jue Tu Jianping Jiang Yun Ling Yueqin Cai Minli Chen Dejun Wang 《Journal of ethnopharmacology》2013