scholarly journals Antispasmodic effect of hydroalcoholic and flavonoids extracts of Dracocephalum kotschyi on rabbit bladder

2020 ◽  
Vol 9 (2) ◽  
pp. 145-152
Author(s):  
Hassan Sadraei ◽  
Seyed Ebrahim Sajjadi ◽  
Arefe Tarafdar
Keyword(s):  
Smooth Muscle ◽  
The Other ◽  
Organ Bath ◽  
Dependent Manner ◽  
Bladder Smooth Muscle ◽  
Concentration Dependent Manner ◽  
Standard Drug ◽  
Other Hand ◽  
Dracocephalum Kotschyi ◽  
Rabbit Bladder

Introduction: Dracocephalum kotschyi extract has antispasmodic activities on smooth muscle including ileum, uterus and trachea. The objective of this research was to investigate antispasmodic activity of hydroalcoholic and flavonoids extracts of D. kotschyi on rabbit bladder contractions. Methods: Rabbits were euthanized by carbon dioxide asphyxiation and the whole bladder was dissected out and immersed in the Tyrode’s solution. Longitudinal bladder strips were mounted vertically in an organ bath at 37°C and gassed continuously with O2 . Bladder strips were contracted with acetylcholine (ACh), KCl, or electrical field stimulation (EFS). Isotonic tension of the tissue was recorded before and after addition of hydroalcoholic or flavonoids rich extracts of D. kotschyi. Nifedipine and propantheline were used as standard drugs. Results: Standard drug propantheline, prevented bladder phasic contraction induced by ACh (1µM) without affecting KCl response. On the other hand, cumulative addition of nifedipine attenuated the tonic contractions induced by KCl (20mM) on bladder smooth muscle. Hydroalcoholic and flavonoids extracts of D. kotschyiat concentration ranges of 10-320 µg/ mL in a concentration dependent way inhibited bladder tonic contraction induced by KCl (n=6). Both extracts also in a concentration-dependent manner relaxed EFS and ACh-induced contractions (range, 20–1280 µg/mL) of bladder smooth muscle in vitro. Complete inhibition was achieved with the highest used concentrations of the extracts. The inhibitory effect of the extract was reversible following washing the tissues with fresh Tyrode’s solution. Conclusion: This study clearly demonstrated that D. kotschyi extracts were able to prevent contractions induced by ACh, KCl or EFS in isolated rabbit bladder. This means that people consuming this medicinal plant may face urinary retention which could be a problem for patients with prostate hypertrophy. On the other hand, this plant might be useful in patients with urinary incontinence. However, its usefulness must be assessed in the controlled clinical trials.

scholarly journals Bronchodilator effect of apigenin and luteolin, two components of Dracocephalum kotschyi on isolated rabbit trachea

2019 ◽  
Vol 8 (4) ◽  
pp. 281-286 ◽  
Author(s):  
Hassan Sadraei ◽  
Seyed Mostapha Ghanadian ◽  
Gholamreza Asghari ◽  
Aminreza Gavahian
Keyword(s):  
Smooth Muscle ◽  
Tracheal Ring ◽  
Tracheal Smooth Muscle ◽  
Organ Bath ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Standard Drug ◽  
Solvent Fractionation ◽  
Dracocephalum Kotschyi

Introduction: Dracocephalum kotschyi is a native Iranian plant with antispasmodic activities on smooth muscles such as ileum and uterus. However, so far antispasmodic effect of D. kotschyi on tracheal smooth muscle has not been reported. Therefore, the objective of this research was to investigate antispasmodic activity of D. kotschyi extract and two of its components luteolin and apigenin on rabbit tracheal contraction in vitro. Methods: Rabbits were euthanized by carbon dioxide and the trachea was dissected and immersed in a Tyrode’s solution. Tracheal rings were prepared and mounted vertically in an organ bath at 37°C and gassed continuously with O2. The tracheal ring preparations were contracted with acetylcholine (ACh) and KCl. The isotonic tension was recorded before and after addition of aminophylline, apigenin, luteolin or flavonoids rich extract of D. kotschyi. Flavonoids rich extract were prepared from D. kotschyi using solvent-solvent fractionation technique. Results: Standard drug aminophylline, prevented tracheal ring preparation contracted with ACh. Cumulative addition of aminophylline also attenuated tonic contraction induced by KCl on tracheal smooth muscle. D. kotschyi extract at concentration ranges of 32-512 μg/mL in a concentration dependent manner inhibited KCl and ACh induced tracheal contraction. Apigenin and luteolin (range 16–512 μg/mL) relaxed KCl and ACh-induced contraction of tracheal smooth muscle in vitro in a concentration-dependent manner. Conclusion: This study demonstrated that D. kotschyi extract is a relaxant of tracheal smooth muscle. The relaxant effect of D. kotschyi extract could be due to its flavonoids component such as apigenin and luteolin.

scholarly journals Antiausterity Activity of Arctigenin Enantiomers: Importance of (2R,3R)-Absolute Configuration

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Suresh Awale ◽  
Mamoru Kato ◽  
Dya Fita Dibwe ◽  
Feng Li ◽  
Chika Miyoshi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Absolute Configuration ◽  
The Other ◽  
Dependent Manner ◽  
Meoh Extract ◽  
Concentration Dependent Manner ◽  
Akt Activation ◽  
Other Hand

From a MeOH extract of powdered roots of Wikstroema indica, six dibenzyl-γ-butyrolactone-type lignans with (2 S,3 S)-absolute configuration [(+)-arctigenin (1), (+)-matairesinol (2), (+)-trachelogenin (3), (+)-nortrachelogenin (4), (+)-hinokinin (5), and (+)-kusunokinin (6)] were isolated, whereas three dibenzyl-γ-butyrolactone-type lignans with (2 R,3 R)-absolute configuration [(-)-arctigenin (1), (-)-matairesinol (2), (-)-trachelogenin (3)] were isolated from Trachelospermum asiaticum. The in vitro preferential cytotoxic activity of the nine compounds was evaluated against human pancreatic PANC-1 cancer cells in nutrient-deprived medium (NDM), but none of the six lignans (1–6) with (2 S,3 S)-absolute configuration showed preferential cytotoxicity. On the other hand, three lignans (1*–3*) with (2 R,3 R)-absolute configuration exhibited preferential cytotoxicity in a concentration-dependent manner with PC50 values of 0.54, 6.82, and 5.85 μM, respectively. Furthermore, the effect of (-)- and (+)-arctigenin was evaluated against the activation of Akt, which is a key process in the tolerance to nutrition starvation. Interestingly, only (-)-arctigenin (1*) strongly suppressed the activation of Akt. These results indicate that the (2 R,3 R)-absolute configuration of (-)-enantiomers should be required for the preferential cytotoxicity through the inhibition of Akt activation.

scholarly journals Suppression of progesterone-enhanced hyperactivation in hamster spermatozoa by estrogen

Reproduction ◽  
2010 ◽  
Vol 140 (3) ◽  
pp. 453-464 ◽  
Author(s):  
Masakatsu Fujinoki
Keyword(s):  
Steroid Hormones ◽  
Sperm Head ◽  
The Other ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Other Hand ◽  
Sperm Proteins ◽  
17Β Estradiol

In this study, I examined whether sperm hyperactivation in hamster is regulated by steroid hormones such as estrogen (estradiol, E2) and progesterone. Although sperm hyperactivation was enhanced by progesterone, 17β-estradiol (17βE2) itself did not affect sperm hyperactivation. However, 17βE2 suppressed progesterone-enhanced hyperactivation in a concentration-dependent manner through non-genomic pathways when spermatozoa were exposed to 17βE2 at the same time or before exposure to progesterone. When spermatozoa were exposed to 17βE2 after exposure to progesterone, 17βE2 did not suppress progesterone-enhanced hyperactivation. Moreover, 17α-estradiol, an inactive isomer of E2, did not suppress progesterone-enhanced hyperactivation. Observations using a FITC-conjugated 17βE2 showed that it binds to the acrosome region of the sperm head. Binding of 17βE2 to spermatozoa was not inhibited by progesterone, although 17βE2 did not suppress progesterone-enhanced hyperactivation when spermatozoa were exposed to 17βE2 after exposure to progesterone. On the other hand, binding of progesterone to spermatozoa was also not inhibited by 17βE2 even if progesterone-enhanced hyperactivation was suppressed by 17βE2. Although tyrosine phosphorylations of sperm proteins were enhanced by progesterone, enhancement of tyrosine phosphorylations by progesterone was suppressed by 17βE2. Moreover, tyrosine phosphorylations were inhibited by 17βE2 when only 17βE2 was added to the medium. From these results, it is likely that 17βE2 competitively suppresses progesterone-enhanced hyperactivation through the inhibition of tyrosine phosphorylations via non-genomic pathways.

Serotonin relaxes porcine pial veins

1994 ◽  
Vol 266 (3) ◽  
pp. H1000-H1006 ◽  
Author(s):  
T. J. Lee ◽  
M. Ueno ◽  
N. Sunagane ◽  
M. H. Sun
Keyword(s):  
Muscle Tone ◽  
The Other ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Pial Arteries ◽  
Concentration Dependent Manner ◽  
Vasoactive Substances ◽  
Other Hand ◽  
Mechanical Stretching ◽  
Or Applications

The effect of serotonin [5-hydroxytryptamine (5-HT)] on pial venous tone of the pig was examined using in vitro tissue bath techniques. Isolated pial venous rings exhibited spontaneous rhythmic contractions (SRC) on mechanical stretching and/or applications of several vasoactive substances, including norepinephrine. On the other hand, KCl induced sustained active muscle tone (SAT) without SRC. The SRC induced by mechanical stretching were not affected by tetrodotoxin, nitro-L-arginine, alpha- and beta-adrenergic, histaminergic, and muscarinic receptor antagonists, indicating that the SRC in porcine pial veins are of myogenic origin. The SRC induced by stretching or applications of vasoactive substances and SAT induced by KCl were inhibited by 5-HT in a concentration-dependent manner. The inhibition was prevented by methysergide and methiothepin but not by ketanserin, propranolol, 3 alpha-tropanyl-1H-indole-3-carboxylic acid ester, hemoglobin, or nitro-L-arginine. The SRC and SAT were inhibited by 5-carboxamidotryptamine (5-CT), 8-hydroxy-2-di-N-propylaminotetralin HBr (8-OHDPAT), 1-[3-(trifluoromethyl)phenyl]piperazine (TFMPP), and 5-methoxytryptamine (5-MT), but not by sumatriptan, alpha-methylserotonin, or 2-methylserotonin. On the other hand, 5-CT, 8-OHDPAT, TFMPP, 5-MT, and sumatriptan constricted the porcine pial arteries exclusively. In 15% of pial venous preparations examined, 5-HT at low concentrations induced ketanserin-sensitive constrictions. These results indicate that the porcine pial venous smooth muscle contains multiple subtypes of 5-HT receptors. The 5-HT inhibition of SRC and SAT is predominant and is mediated by 5-HT1-like receptors, which, however, do not seem to correspond to 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, 5-HT1E, or 5-HT1F receptor subtypes.(ABSTRACT TRUNCATED AT 250 WORDS)

scholarly journals β-Adrenergic relaxation of mouse urinary bladder smooth muscle in the absence of large-conductance Ca2+-activated K+ channel

2008 ◽  
Vol 295 (4) ◽  
pp. F1149-F1157 ◽  
Author(s):  
Sean M. Brown ◽  
Lilia M. Bentcheva-Petkova ◽  
Lei Liu ◽  
Kiril L. Hristov ◽  
Muyan Chen ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Urinary Bladder ◽  
Bk Channel ◽  
K Channel ◽  
Dependent Manner ◽  
Bladder Smooth Muscle ◽  
Response Curves ◽  
Concentration Dependent Manner ◽  
Leftward Shift ◽  
Urinary Bladder Smooth Muscle

In urinary bladder smooth muscle (UBSM), stimulation of β-adrenergic receptors (β-ARs) leads to activation of the large-conductance Ca2+-activated K+ (BK) channel currents (Petkov GV and Nelson MT. Am J Physiol Cell Physiol 288: C1255–C1263, 2005). In this study we tested the hypothesis that the BK channel mediates UBSM relaxation in response to β-AR stimulation using the highly specific BK channel inhibitor iberiotoxin (IBTX) and a BK channel knockout (BK-KO) mouse model in which the gene for the pore-forming subunit was deleted. UBSM strips isolated from wild-type (WT) and BK-KO mice were stimulated with 20 mM K+ or 1 μM carbachol to induce phasic and tonic contractions. BK-KO and WT UBSM strips pretreated with IBTX had increased overall contractility, and UBSM BK-KO cells were depolarized with ∼12 mV. Isoproterenol, a nonspecific β-AR agonist, and forskolin, an adenylate cyclase activator, decreased phasic and tonic contractions of WT UBSM strips in a concentration-dependent manner. In the presence of IBTX, the concentration-response curves to isoproterenol and forskolin were shifted to the right in WT UBSM strips. Isoproterenol- and forskolin-mediated relaxations were enhanced in BK-KO UBSM strips, and a leftward shift in the concentration-response curves was observed. The leftward shift was eliminated upon PKA inhibition with H-89, suggesting upregulation of the β-AR-cAMP pathway in BK-KO mice. These results indicate that the BK channel is a key modulator in β-AR-mediated relaxation of UBSM and further suggest that alterations in BK channel expression or function could contribute to some pathophysiological conditions such as overactive bladder and urinary incontinence.

scholarly journals Effect of an Ethanol Extract ofScutellaria baicalensison Relaxation in Corpus Cavernosum Smooth Muscle

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Xiang Li ◽  
Hyun Cheol Oh ◽  
Su Bin Son ◽  
Yun Jung Lee ◽  
Dae Gill Kang ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Corpus Cavernosum ◽  
Ethanol Extract ◽  
Organ Bath ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Perfusion Model ◽  
Rabbit Corpus Cavernosum ◽  
Dose Dependent ◽  
Cavernous Smooth Muscle

Aims of study. The aim of the present study was to investigate whether an ethanol extract ofScutellaria baicalensis(ESB) relaxes penile corpus cavernosum muscle in organ bath experiments.Materials and methods. Changes in tension of cavernous smooth muscle strips were determined by penile strip chamber model and in penile perfusion model. Isolated endothelium-intact rabbit corpus cavernosum was precontracted with phenylephrine (PE) and then treated with ESB.Results. ESB relaxed penile smooth muscle in a dose-dependent manner, and this was inhibited by pre-treatment with NG-nitro-l-arginine methyl ester (l-NAME), a nitric oxide (NO) synthase inhibitor, and 1H-[1, 2, 4]-oxadiazolo-[4,3-α]-quinoxalin-1-one (ODQ), a soluble guanylyl cyclase (sGC) inhibitor. ESB-induced relaxation was significantly attenuated by pretreatment with tetraethylammonium (TEA), a nonselective K+channel blocker, and charybdotoxin, a selective Ca2+-dependent K+channel inhibitor. ESB increased the cGMP levels of rabbit corpus cavernosum in a concentration-dependent manner without changes in cAMP levels. In a perfusion model of penile tissue, ESB also relaxed penile corpus cavernosum smooth muscle in a dose-dependent manner.Conclusion. Taken together, these results suggest that ESB relaxed rabbit cavernous smooth muscle via the NO/cGMP system and Ca2+-sensitive K+channels in the corpus cavernosum.

scholarly journals Antioxidant and Prooxidant Effects of Metal Dafonates on the NADPH-Dependent Lipid Peroxidation in the Murine Hepatic Microsomal System

1999 ◽  
Vol 6 (3) ◽  
pp. 169-175 ◽  
Author(s):  
M. Gupta ◽  
R. K. Kale ◽  
P. P. Kulkarni ◽  
S. B. Padhye
Keyword(s):  
Lipid Peroxidation ◽  
Metal Ions ◽  
The Other ◽  
Inhibition Constant ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Other Hand ◽  
Significant Reversal

Dafone inhibits the lipid peroxidation significantly in a concentration dependent manner. The inhibition was found to be an uncompetitive type with the inhibition constant (Ki) of 62.5 μM On the other hand complexation with metal ions results in a significant reversal from antioxidant to pro-oxidant properties for the resulting complexes which are cationic and with associated halometallate anions. The nature of the potentiation in case of the ferric compound was of competitive type with activation constant (Ka) having the value 32.5 μM . The neutral copper-dafonate complex, however, inhibits lipid peroxidation with increase in concentration.

Distinct pathways to refill ACh-sensitive internal Ca2+ stores in canine airway smooth muscle

1993 ◽  
Vol 265 (1) ◽  
pp. C28-C35 ◽  
Author(s):  
J. P. Bourreau ◽  
C. Y. Kwan ◽  
E. E. Daniel
Keyword(s):  
Smooth Muscle ◽  
Channel Blocker ◽  
Cyclopiazonic Acid ◽  
Inhibitory Effect ◽  
Tonic Contraction ◽  
The Other ◽  
K Channel ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
K Channel Opener

The ability of extracellular Ca2+ to refill internal Ca2+ stores of canine tracheal smooth muscle after a prior depletion by acetylcholine (ACh) was assessed using a novel sarcoplasmic reticulum (SR) Ca2+ pump inhibitor, cyclopiazonic acid (CPA). The transient contraction induced by ACh in a medium free of Ca2+ was used as an index for the content of agonist-sensitive intracellular Ca2+ stores. CPA inhibited in a concentration-dependent manner the refilling of the stores occurring during high KCl stimulation, and this inhibitory effect was independent of the external Ca2+ concentration. On the other hand, CPA was less effective in inhibiting the refilling occurring during prolonged ACh stimulation, especially when external Ca2+ concentration was raised. At 5.0 mM external Ca2+ or when 0.1 microM BAY 8644 was present in the medium, CPA was ineffective in inhibiting the refilling occurring during prolonged ACh stimulation. The maximum ACh-induced contraction in Ca(2+)-containing medium was independent of the extent of internal store Ca2+ load in the absence of L-type Ca2+ channel blocker but was highly dependent on the extent of internal Ca2+ load in the presence of the Ca2+ channel blocker. Hyperpolarization of the plasma membrane with the K+ channel opener cromakalim reduced the amplitude of ACh tonic contraction. Subsequent addition of nifedipine further reduced ACh tonic contraction. It is concluded that two different pathways for external Ca2+ are used to refill ACh-sensitive internal stores. One involves active Ca2+ uptake via a CPA-sensitive Ca2+ pump, and the other involves a CPA-insensitive pathway whose nature remains to be determined.

Initiation of distension-induced descending peristaltic reflex in opossum esophagus: role of muscle contractility

2001 ◽  
Vol 280 (3) ◽  
pp. G431-G438 ◽  
Author(s):  
A. Muinuddin ◽  
W. G. Paterson
Keyword(s):  
Smooth Muscle ◽  
Muscle Tension ◽  
Organ Bath ◽  
Dependent Manner ◽  
Krebs Solution ◽  
Muscle Contractility ◽  
Concentration Dependent Manner ◽  
Peristaltic Reflex ◽  
Over The Top

The balloon distension (BD)-induced descending peristaltic reflex in the opossum smooth muscle esophagus is abolished in vitro when a Ca2+-free Krebs solution is placed at the site of distension, suggesting that either synaptic transmission occurs at the origin of the reflex or initiation of the reflex requires the development of muscle tension in response to BD. To test the latter possibility, an 8- to 10-cm length of smooth muscle esophagus was placed in a dual-chamber organ bath, isolating the stimulating (orad) from the recording site (aborad). Nifedipine addition to the orad chamber (i.e., site of distension) inhibited the BD-induced “off” contractions in both chambers in a concentration-dependent manner. However, the aborad response to electrical field stimulation (EFS) was unaffected. Atropine addition to the orad chamber had no effect on BD or EFS responses in either chamber. To examine the effects of these agents on tonic contractility, an isobaric barostat was employed. Pressure-volume curves were not altered by Ca2+-free Krebs solution, nifedipine, or TTX, suggesting that resting esophageal tone is not dependent on neural factors or muscle contractility. However, both Ca2+-free Krebs solution and nifedipine markedly decreased phasic contractions over the top of the distending bag. These observations suggest that local, stretch-induced phasic muscle contraction is required for initiation of the BD-induced descending peristaltic reflex.

scholarly journals Beneficial effects of methanolic extract of Indigofera linnaei Ali. on the inflammatory and nociceptive responses in rodent models

2016 ◽  
Vol 52 (1) ◽  
pp. 113-123
Author(s):  
Raju Senthil Kumar ◽  
Balasubramanian Rajkapoor ◽  
Perumal Perumal ◽  
Sekar Vinoth Kumar ◽  
Arunachalam Suba Geetha
Keyword(s):  
Methanol Extract ◽  
Latency Period ◽  
Dependent Manner ◽  
Rodent Models ◽  
Hot Plate ◽  
Concentration Dependent Manner ◽  
Standard Drug ◽  
Beneficial Effects ◽  
Nociceptive Responses

ABSTRACT Indigofera linnaei Ali. (Tamil Name: Cheppu Nerinjil) belongs to the family Fabaceae, used for the treatment of various ailments in the traditional system of medicine. In the present study, the beneficial effects of methanol extract of whole plant of I. linnaei (MEIL) were evaluated on inflammation and nociception responses in rodent models. In vitro nitric oxide (NO), lipoxygenase (LOX) and cyclooxygense (COX) inhibitory activities were also performed to understand the mode of action. MEIL at the dose of 200 & 400 mg/kg, p.o. significantly inhibited carrageenan induced rat paw volume and reduced the weight of granuloma in cotton pellet granuloma model. The results obtained were comparable with the standard drug aceclofenac. The anti-nociceptive effect of MEIL in mice was evaluated in hot plate and acetic acid induced writhing model. The plant extract significantly reduced the number of writhes and the analgesic effect was higher than that of the standard drug aspirin. However, the extract fails to increase the latency period in hot plate method suggesting that the extract produce nociception by peripheral activity. The extract produced inhibitory effect on NO, LOX and COX in concentration dependent manner. The extract exhibited pronounced and selective COX-2 inhibition. Altogether, these results suggested that the methanol extract of Indigofera linnaei could be considered as a potential anti-inflammatory and analgesic agent.

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