scholarly journals Phytochemical Evaluation of Lythrum Salicaria Extracts and Their Effects on Guinea-Pig Ileum

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Tímea Bencsik ◽  
Loránd Barthó ◽  
Viktor Sándor ◽  
Nóra Papp ◽  
Rita Benkó ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Guinea Pig ◽  
Ethyl Acetate ◽  
Water Extract ◽  
Lythrum Salicaria ◽  
Dependent Manner ◽  
Guinea Pig Ileum ◽  
Concentration Dependent Manner ◽  
Ethanol In Water

n-Hexane, chloroform, ethyl acetate and 50% ethanol in water extracts prepared from the air-dried flowering parts of Lythrum salicaria L. were tested for in vitro pharmacological properties on Guinea-pig ileum, which is suitable for detecting a whole range of neuronal and smooth muscle effects. UHPLC-MS was used to evaluate polyphenol components of the extracts. In the ileum, the most prominent response (46.4% related to 0.5 μM histamine) of the extracts causing smooth muscle contractions were triggered by the 50% ethanol in water extract in a concentration-dependent manner. Atropine, indomethacin and PPADS plus suramin significantly reduced the contractile response caused by this extract. The strongest inhibition was due to atropine. The results suggest that L. salicaria extracts have a moderate muscarinic receptor agonist effect in Guinea-pig ileum and that prostanoids and purinoceptor mechanisms are involved to some extent. Therefore diluted extracts of L. salicaria p.o. could be used as a mild stimulant of gastrointestinal motility. The 50% ethanol in water extract was rich in polyphenols. n-Hexane, chloroform and ethyl acetate extracts failed to contain catechin, caffeic acid, quercetin-3-D-galactoside and rutin, but they all showed spasmogenic effects, and, therefore we do not think that these compounds could be involved in the spasmogenic activity.

scholarly journals In Vitro Antiproliferative and Antioxidant Effects of Extracts from Rubus caesius Leaves and Their Quality Evaluation

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Daniel Mirosław Grochowski ◽  
Roman Paduch ◽  
Adrian Wiater ◽  
Adrianna Dudek ◽  
Małgorzata Pleszczyńska ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Water Extract ◽  
Ethyl Acetate Fraction ◽  
Human Colon ◽  
Dependent Manner ◽  
Human Colon Cancer ◽  
Concentration Dependent Manner ◽  
Two Stages

The present study was performed to evaluate the effect of different extracts and subfractions from Rubus caesius leaves on two human colon cancer cell lines obtained from two stages of the disease progression lines HT29 and SW948. Tested samples inhibited the viability of cells, both HT29 and SW948 lines, in a concentration-dependent manner. The most active was the ethyl acetate fraction which, applied at the highest concentration (250 μg/mL), decreased the viability of cells (HT29 and SW948) below 66%. The extracts and subfractions were also investigated for antioxidant activities on DPPH and FRAP assays. All extracts, with the exception of water extract at a dose of 250 μg/mL, almost totally reduced DPPH. The highest Fe3+ ion reduction was shown for the diethyl and ethyl acetate fractions. It was more than 6.5 times higher (at a dose 250 μg/mL) as compared to the control. The LC-MS studies of the analysed preparations showed that all samples contain a wide variety of polyphenolics, among which ellagitannins turned out to be the main constituents with dominant ellagic acid, sanguiin H-6, and flavonol derivatives.

scholarly journals In Vitro Pancreatic Lipase Inhibition by Marine Fungi Purpureocillium lilacinum Associated with Stylissa sp. Sponge as Anti-obesity Agent

2021 ◽  
Vol 29 (1) ◽  
pp. 76-86
Author(s):  
Wendi Nurul Fadillah ◽  
Nampiah Sukarno ◽  
Dyah Iswantini ◽  
Min Rahminiwati ◽  
Novriyandi Hanif ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Pancreatic Lipase ◽  
Metabolite Identification ◽  
Molecular Characteristics ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Purpureocillium Lilacinum ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

This study aimed to evaluate the potential of marine fungus Purpureocillium lilacinum isolated from an Indonesian marine sponge Stylissa sp. as an anti-obesity agent through pancreatic lipase inhibition assay. The fungus was identified as P. lilacinum through morphological and molecular characteristics. The fungal extract’s inhibition activity and kinetics were evaluated using spectrophotometry and Lineweaver-Burk plots. Ethyl acetate and butanol were used for extraction. Both extracts showed pancreatic lipase inhibition in a concentration-dependent manner. Both crude extracts were then fractionated once. All fractionated extracts showed inhibitory activity above 50%, with the highest activity found in fraction 5 of ethyl acetate at 93.41% inhibition. The best fractionated extract had an IC50value of 220.60 µg.mL-1. The most active fraction of P. lilacinum had a competitive-type inhibitor behavior as shown by the value of Vmax not significantly changing from 388.80 to 382.62 mM pNP.min-1, and the Michaelis-Menten constant (KM) increased from 2.02 to 5.47 mM in the presence of 500 µg.mL-1 fractionated extract. Metabolite identification with LC-MS/MS QTOF suggested that galangin, kaempferol, and quercetin were responsible for the observed lipase inhibition.

Guinea pig visceral C-fiber neurons are diverse with respect to the K+ currents involved in action-potential repolarization

1994 ◽  
Vol 71 (2) ◽  
pp. 561-574 ◽  
Author(s):  
E. P. Christian ◽  
J. Togo ◽  
K. E. Naper
Keyword(s):  
Guinea Pig ◽  
Action Potential ◽  
Outward Current ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Whole Cell ◽  
C Fiber ◽  
K Current ◽  
Action Potential Repolarization

1. Intracellular recordings were made from C-fiber neurons identified by antidromic conduction velocity in intact guinea pig nodose ganglia maintained in vitro, and whole-cell patch clamp recordings were made from dissociated guinea pig nodose neurons to investigate the contribution of various K+ conductances to action-potential repolarization. 2. The repolarizing phase of the intracellularly recorded action potential was prolonged in a concentration-dependent manner by charybdotoxin (Chtx; EC50 = 39 nM) or iberiatoxin (Ibtx; EC50 = 48 nM) in a subpopulation of 16/36 C-fiber neurons. In a subset of these experiments, removal of extracellular Ca2+ reversibly prolonged action-potential duration (APD) in the same 4/9 intracellularly recorded C-fiber neurons affected by Chtx (> or = 100 nM). These convergent results support that a Ca(2+)-activated K+ current (IC) contributes to action-potential repolarization in a restricted subpopulation of C-fiber neurons. 3. Tetraethylammonium (TEA; 1-10 mM) increased APD considerably further in the presence of 100-250 nM Chtx or Ibtx, or in nominally Ca(2+)-free superfusate in 14/14 intracellularly recorded C-fiber neurons. TEA affected APD similarly in subpopulations of neurons with and without IC, suggesting that a voltage-dependent K+ current (IK) contributes significantly to action-potential repolarization in most nodose C-fiber neurons. 4. Substitution of Mn2+ for Ca2+ reduced outward whole-cell currents elicited by voltage command steps positive to -30 mV (2-25 ms) in a subpopulation of 21/36 dissociated nodose neurons, supporting the heterogeneous expression of IC. The kinetics of outward tail current relaxations (tau s of 1.5-2 ms) measured at the return of 2-3 ms depolarizing steps to -40 mV were indistinguishable in neurons with and without IC, precluding a separation of the nodose IC and IK by a difference in deactivation rates. 5. Chtx (10-250 nM) reduced in a subpopulation of 3/8 C-fiber neurons the total outward current elicited by voltage steps depolarized to -30 mV in single microelectrode voltage-clamp recordings. TEA (5-10 mM) further reduced outward current in the presence of 100-250 nM Chtx in all eight experiments. The Chtx-sensitive current was taken to represent IC, and the TEA-sensitive current, the IK component contributing to action-potential repolarization. 6. Rapidly inactivating current (IA) was implicated in action-potential repolarization in a subpopulation of intracellularly recorded C-fiber neurons. In 4/7 neurons, incremented hyperpolarizing prepulses negative to -50 mV progressively shortened APD.(ABSTRACT TRUNCATED AT 400 WORDS)

scholarly journals In Vitro Antioxidant Capacity and Neuronal Cell Toxicity of Roots of Ostericum koreanum Maximowicz

2011 ◽  
Vol 8 (3) ◽  
pp. 1451-1455
Author(s):  
Ramalingam Mahesh ◽  
Hyo Won Jung ◽  
Jun Hong Park ◽  
Yong-Ki Park
Keyword(s):  
Cell Viability ◽  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Neuronal Cell ◽  
Ethyl Acetate Fraction ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ostericum Koreanum

Ostericum koreanummaximowicz (Umbelliferae), a medicinal herb in Korean Oriental Medicine, has been applied to treat cold, headache, neuralgia and arthralgia. The ethyl acetate fraction ofO. koreanumroot was subjected toin vitroantioxidant activity with different methods for free radical scavenging activities. In addition, the cell viability and nitric oxide release assays were performed here for the first time in neuroblastoma (Neuro-2a) cell cultures. Among all the tested methods, the ethyl acetate fraction was expressed very active, exhibiting a good Trolox equivalent values and IC50, comparable to that of the commercial antioxidants, Trolox and ascorbic acid, respectively. The results showed that there was a reduction of cell viability by the fraction in a concentration dependent manner. These results suggest thatO. koreanumshows good antioxidant activitiesin vitroby inhibiting free radicals. These findings provide a rationale for thein vivotesting. Also, the major constituents behind the antioxidant mechanisms of this fraction warrant further study.

scholarly journals Triterpenoids, Including One with Smooth Muscle Relaxant Activity, from Rubus idaeus (Raspberry) Leaves

2006 ◽  
Vol 1 (8) ◽  
pp. 1934578X0600100
Author(s):  
Janne Rojas Vera ◽  
Christopher G. Dacke ◽  
Asmita V. Patel ◽  
Gerald Blunden
Keyword(s):  
Smooth Muscle ◽  
Guinea Pig ◽  
Column Chromatography ◽  
Muscle Relaxant ◽  
Methanol Extract ◽  
Rubus Idaeus ◽  
Guinea Pig Ileum ◽  
Muscle Relaxant Activity ◽  
Smooth Muscle Relaxant

A methanol extract of Rubus idaeus leaves was fractionated by column chromatography and the eluted samples were tested for their ability to relax transmurally stimulated Guinea pig ileum preparations in vitro. Two distinct bands of activity were detected. From band one sitosterol and eight triterpenoids were characterized, but only olean-18-ene-1β, 2α, 3α-triol demonstrated smooth muscle relaxant activity. This compound is, to the best of our knowledge, novel, as are olean-12-ene-3β, 29-diol and urs-12-ene-3β, 30-diol.

Serotonin reuptake inhibitors fluoxetine and citalopram relax intestinal smooth muscle

2001 ◽  
Vol 79 (7) ◽  
pp. 580-584 ◽  
Author(s):  
Pal Pacher ◽  
Zoltan Ungvari ◽  
Valéria Kecskeméti ◽  
Tamás Friedmann ◽  
Susanna Furst
Keyword(s):  
Smooth Muscle ◽  
Serotonin Reuptake ◽  
Longitudinal Muscle ◽  
Contractile Activity ◽  
Electrical Field Stimulation ◽  
Intestinal Smooth Muscle ◽  
Dependent Manner ◽  
Guinea Pig Ileum ◽  
Electrical Field ◽  
Concentration Dependent Manner

Selective serotonin reuptake inhibitor antidepressants (SSRIs) exert depressant effects on cardiac myocytes and vascular smooth muscle cells by inhibiting Ca2+ channels. We hypothesized that the SSRIs fluoxetine and citalopram affect the contractile activity of intestinal smooth muscle by interfering with Ca2+ entry and (or) signaling pathways. The effects of fluoxetine and citalopram on contractions of guinea-pig ileum longitudinal muscle-myenteric plexus preparations (LMMP) were compared with the effects of the voltage-operated Ca2+ channel inhibitors nifedipine and diltiazem. In a concentration-dependent manner, nifedipine, diltiazem, fluoxetine, and citalopram elicited relaxation of LMMPs contracted by electrical field stimulation (EC50 values of 4 × 10–7 M, 1.4 × 10–6 M, 1.4 × 10–5, and 6.8 × 10–6 M, respectively). Nifedipine, diltiazem, fluoxetine, and citalopram also relaxed LMMPs contracted with a depolarizing concentration of KCl (48 mM; EC50 values of 1.8 × 10–8 M, 1.4 × 10–7 M, 3.7 × 10–6 M, and 6.3 × 10–6, respectively), a response that could be reversed by increasing the extracellular Ca2+ concentration (2.5–30 mM). These data suggest that fluoxetine and citalopram elicit relaxation of intestinal smooth muscle, likely by inhibiting Ca2+ channel(s). This effect may be of clinical importance.Key words: fluoxetine (Prozac(r)), citalopram (Seropram(r)), nifedipine, diltiazem, L-type Ca2+ channels, intestinal smooth muscle.

scholarly journals Antioxidant Activities of Extracts from Sarcocarp of Cotoneaster multiflorus

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Xiangping Liu ◽  
Jia Jia ◽  
Xuemin Jing ◽  
Guoliang Li
Keyword(s):  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Water Extract ◽  
Reducing Power ◽  
Ethyl Acetate Fraction ◽  
Dependent Manner ◽  
Antioxidant Power ◽  
Water Fraction

The ethanol-water (7 : 3, v/v) extract of Cotoneaster multiflorus sarcocarp was sequentially fractionated by liquid-liquid partition using n-hexane, diethyl ether, methylene dichloride, and ethyl acetate. The contents of total polyphenols, total flavones, and oligomeric proanthocyanidins in the five parts (including the ethanol-water extract) were determined. In addition, 2,2-diphenyl-1-picrylhydrazyl free radical-scavenging, 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radical cation decolorization, reducing power, ferric reducing antioxidant power, and lipid peroxidation inhibition assays were conducted to test the antioxidant activities of Sample 1 (the ethanol-water fraction) and Sample 2 (the ethyl acetate fraction) in vitro. In the above five assays, Sample 2 showed greater antioxidant capacities than Sample 1. Furthermore, Sample 2 was better able to protect low-density lipoproteins from oxidation in a dose-dependent manner. The test results show that C. multiflorus sarcocarp, especially the ethyl acetate-soluble fraction, may be a potential source of natural antioxidants.

Neural and myogenic effects of leukotrienes C4, D4, and E4 on canine bronchial smooth muscle

1994 ◽  
Vol 266 (4) ◽  
pp. L414-L425 ◽  
Author(s):  
A. Abela ◽  
E. E. Daniel
Keyword(s):  
Smooth Muscle ◽  
Receptor Antagonist ◽  
Contractile Activity ◽  
Neuromuscular Control ◽  
Dependent Manner ◽  
Gamma Glutamyl Transpeptidase ◽  
Response Curves ◽  
Bronchial Smooth Muscle ◽  
Concentration Dependent Manner

The leukotrienes (LTs), referred to as the slow-reacting substance of anaphylaxis (SRS-A), are reported to have little or no activity in the canine airway. The objective of this study was to determine whether LTC4, LTD4, and LTE4 (10(-10)-10(-7) M) play a role in neuromuscular control of third- to fifth-order canine bronchi. In the presence of 1 microM indomethacin (Indo), canine bronchial smooth muscle contracted and was depolarized in a concentration-dependent manner by LTC4 or LTD4 but not by LTE4. LTC4 and LTD4 concentration-response curves were not significantly affected when conducted in the presence of any of the following: 10(-7) M propranolol (beta-adrenoceptor antagonist), 10(-6) M chlorpheniramine (H1-receptor antagonist), 10(-6) M ketanserin (nonselective 5-hydroxytryptamine receptor antagonist), 10(-7) M atropine (muscarinic receptor antagonist), and 10(-6) M tetrodotoxin (sodium channel blocker). LTC4 and LTD4 also potentiated electrical field-stimulated (EFS) excitatory junction potentials (EJPs), suggesting a possible prejunctional enhancement of acetylcholine release. In the absence of Indo, no postjunctional responses to LTC4 and LTD4 occurred. Endogenous prostaglandin E2 (PGE2) and 6-keto-PGF1 alpha (a stable metabolite of PGI2) levels from canine bronchi were significantly reduced by Indo. In the presence of Indo, addition of > or = 10(-8) M of PGE2 suppressed contractions to LTC4 and LTD4. These data suggest that the decrease in PGE2 and PGI2 production by Indo is sufficient to unmask the excitatory postjunctional actions of LTC4 and LTD4 on bronchial smooth muscle. Serine borate (45 mM; an inhibitor of gamma-glutamyl transpeptidase, which prevents the conversion of LTC4 to LTD4) increased selectively the contractile activity of LTC4. L-Cysteine (3 mM; an inhibitor of an aminopeptidase, which prevents the conversion of LTD4 to LTE4) enhanced the contractile responses to LTD4. Serine borate increased the amplitude and duration of EFS contractions and potentiated the amplitude of EFS EJPs; the last effects were prevented by nordihydroguaiaretic acid. These and other studies suggest that LTs are synthesized by canine bronchi and have receptors on canine bronchial smooth muscle but that contractions to LTC4 and LTD4 in the canine airway are usually not observed because of the presence of inhibitory prostanoids (PGE2 and PGI2). We suggest that decreases in PGE2 and PGI2 in models of airway disease in combination with increases in LTC4, LTD4, and thromboxane A2 may contribute to airway hyperresponsiveness in vitro.

Differential sensitivities of the sphincter of Oddi and gallbladder to cholecystokinin in the guinea pig: their role in transsphincteric bile flow

1992 ◽  
Vol 70 (10) ◽  
pp. 1336-1341 ◽  
Author(s):  
Karen Harrington ◽  
Arieh Bomzon ◽  
Keith A. Sharkey ◽  
Joseph S. Davison ◽  
Eldon A. Shaffer
Keyword(s):  
Guinea Pig ◽  
Circular Muscle ◽  
Sphincter Of Oddi ◽  
Dependent Manner ◽  
Field Stimulation ◽  
Response Curves ◽  
Gallbladder Contraction ◽  
Concentration Dependent Manner ◽  
Cholinergic Mechanism

Cholecystokinin (CCK) is considered to simply contract the gallbladder and relax the sphincter of Oddi with meals. In this study, we examined this hypothesis by investigating the action of CCK on the sphincter of Oddi and gallbladder of the guinea pig. The experimental design used an in vitro preparation of the sphincter of Oddi to measure contraction of the circular muscle. CCK increased tone in both the gallbladder and the sphincter of Oddi in a concentration-dependent manner. The normalized concentration–response curves for CCK, however, revealed that the gallbladder had a greater sensitivity to CCK (ED50 7 nM) than the sphincter of Oddi (ED50 22 nM; p < 0.01). Conversely, the sphincter was more sensitive to bethanechol than was the gallbladder. When the sphincter of Oddi was stimulated maximally with CCK in the presence of atropine (10−6 M) or tetrodotoxin (10−6 M), the contractile response was significantly reduced (p < 0.05) although not abolished. Conversely, atropine completely abolished the responses to bethanechol (10−3 M) and transmural field stimulation (70 V, 10 Hz, 1 ms, for 20 s). Transmural field stimulation of the sphincter that had been precontracted with CCK (26 nM) caused a transient, initial relaxation followed by contraction. Pretreatment with atropine augmented the duration of this relaxation, which could be completely abolished by tetrodotoxin. Thus, CCK contracts the sphincter of Oddi in the guinea pig by a direct (myogenic) and a neural (likely cholinergic) mechanism. Relaxation of the sphincter of Oddi also occurs in the guinea pig via noncholinergic inhibitory nerves. Duodenal delivery of bile is expedited by CCK, which induces gallbladder contraction at low, near-physiological levels without stimulating the sphincter. Under other conditions, sphincter of Oddi relaxation may facilitate transsphincteric flow. In contrast, increased cholinergic tone may help prevent duodenal reflux into the biliary system.Key words: cholecystokinin, bethanechol, enteric nervous system, gallbladder function, sphincter of Oddi.

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