• Title/Summary/Keyword: contractile activity

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Preliminary Mechanistic Study on the Trachea Smooth Muscle Relaxant Activity of Aqueous Leaf Extract of Tridax Procumbens in Male Wistar Rats

  • Salami, Shakiru Ademola;Salahdeen, Hussein Mofomosara;Anidu, Babatunde Shuaib;Murtala, Babatunde Adekunle;Alada, AbdulRasak Akinola
    • Journal of Pharmacopuncture
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    • v.25 no.3
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    • pp.209-215
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    • 2022
  • Objectives: Aqueous leaf extract of Tridax procumbens (ALETP) has potent relaxant activity. However, this relaxant activity in respiratory smooth muscle remains uninvestigated. This study investigates the effect of ALETP on the contractile activity of tracheal smooth muscle (TSM) in adult male Wistar rats. Methods: Twelve male Wistar rats divided into 2 groups and were treated with either 100 mg/kg of ALETP (ALETP treatment group) or vehicle (distilled water; control group) through oral gavage for 4 weeks. Dose responses of TSM from the 2 groups to acetylcholine (10-9 to 10-5 M), phenylephrine (10-9 to 10-5 M), and potassium chloride (KCl; 10-9 to 10-4 M) were determined cumulatively. Furthermore, cumulative dose responses to acetylcholine (10-9 to 10-5 M) after pre-incubation of TSM with atropine (10-5 M), L-NAME (10-4 M), indomethacin (10-4 M), and nifedipine (10-4 M), were determined. Results: Treatment with ALETP substantially inhibited TSM contraction stimulated by cumulative doses of acetylcholine, phenylephrine, and KCl. Furthermore, preincubation of TSM from the 2 groups in atropine significantly inhibited contractility in TSM. Incubation in L-NAME and indomethacin also significantly inhibited contractility in TSM of ALETP-treated rats compared to that of controls. Contractile activity of the TSM was also inhibited significantly with incubation in nifedipine in ALETP-treated rats. Conclusion: ALETP enhanced relaxant activity in rat TSM primarily by blocking the L-type calcium channel and promoting endothelial nitric oxide release. ALETP contains agents that may be useful in disorders of the respiratory tract.

Biological Activity of Extracts of the Starfish Asterias amurensis (아무르불가사리 추출물의 생리활성)

  • Go, Hye-Jin;Jo, Mi Jeong;Kim, Tae Young;Hong, Yong-Ki;Kim, Gun-Do;Lee, Byung-Woo;Park, Nam Gyu
    • Journal of Life Science
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    • v.24 no.5
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    • pp.491-497
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    • 2014
  • Nowadays, starfish is one of problems about interruption of marine ecosystem, so many researchers are focusing on application of the starfish (Asterias amurensis). In this study, we investigated the contractile and relaxant activity of the smooth muscles and the antimicrobial and antioxidant activity of six different tissues (muscle, gut, liver, tube feet, gonads, and body) of A. amurensis. Frozen samples were extracted with distilled water containing 1% acetic acid. Extracts from all the tissues, except the body tissue, showed potent antimicrobial activity against Escherichia coli D31. The dorsal retractor muscles (DRM) of muscle and gut extracts showed strong contraction responses. On the other hand, contractile activity on esophagus of squid Todarodes pacificus could be detected in all tissues tested. The contractile activity of the liver extract was higher than that of the other tissues. The body, tube feet, and liver extracts showed the contractile activity on the intestine of the panther puffer fish (Takifugu pardalis). Relaxation response on the DRM of starfish (A. pectinifera) was observed in all tissues tested. Increased antioxidant activity was observed in the gut, liver, and body extracts. The results suggest that the starfish (A. amurensis) is a potential source of novel bioactive compounds.

Influences of Testosterone and Estrogen on the Contractile Sensitivity to Oxytocics, the Cholinesterase activity and Electrolytes of the Uterine Muscle of Rabbits (Testosterone 및 Estrogen 투여(投與)가 자궁수축약(子宮收縮藥)의 적출자궁(摘出子宮) 수축성(收縮性)에 미치는 영향(影響)과 자궁근내(子宮筋內) Cholinesterase 활성도(活性度) 및 전해질(電解質)에 미치는 효과(?果))

  • Koo, Hee-Soo;Kong, Wha-Soon;Kim, Soon-Yeung;Song, Hyun-Sub;Lee, Jeung-Ja
    • The Korean Journal of Pharmacology
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    • v.6 no.1
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    • pp.45-55
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    • 1970
  • It is well known that the uterine contractility is affected by sexual hormone. In this experiment, the authors attempted to study the influences of testosterone and estrogen or the uterine contractility to oxytocics. The contractile sensitivity of the excised uterine muscle of non-castrated and castrated rabbits with testosterone and estrogen 24 hours before experiment is observed respectively. And the cholinesterase activity and electrolytes (Na, K, Ca and Mg) in the uterine muscle are measured in order to study the relationship with contractile sensitivity and those changes. The results obtained were summarized as follows: 1. The contractile effect of spareng on the excised uterine muscle of non-castrated rabbits pretreated with estrogen was markedly increased in small dose, but that of rabbits pretreated with testosterone was significantly increased in large dose, comparing with that of the control group. In castrated rabbits, the contractile sensitivity of the uterine muscle to spareng was significantly increased by pretreatment with estrogen in large dose but it was markedly decreased by pretreatment with testosterone in small dose. 2. The contractile effect of quinine on the excised uterine muscle of non-castrated rabbits pretreated with estrogen was significantly decreased but that of castrated rabbits pretreated with both estrogen and testosterone were markedly increased comparing with that of the control group. 3. The cholinesterase activity in the uterine muscle of non-castrated rabbits was significantly increased by pretreatment with small dose of estrogen or large dose of testosterone, but that of castrated rabbits was markedly decreased by pretreatment with large dose of estrogen. 4. Na and K contents in the uterine muscle of non-castrated rabbits were markedly increased by pretreatment with both estrogen and testosterone, but that of castrated rabbits was significantly increased by pretreatment with small dose of estrogen. 5. Ca content in uterine muscle of non-castrated rabbits was significantly decreased by pretreatment with both large dose of estrogen and testosterone but increased by pretreatment of testosterone. In castrated rabbits, Ca content was significantly decreased by pretreatment with both estrogen and testosterone. 6. Mg content in the uterine muscle of non-castrated rabbits was markedly increased by pretreatment with estrogen and small dose of testosterone, but that of castrated rabbits was significantly decreased by pretreatment with both large dose of estrogen and testosterone.

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Isolation of a Novel Neuropeptide with Contractile Activity on the Smooth Muscle from the Snakehead Channa argus (가물치(Channa argus)로부터 평활근 수축활성 펩타이드의 정제)

  • Go, Hye-Jin;Park, Nam-Gyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.45 no.2
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    • pp.114-121
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    • 2012
  • A novel neuropeptide was isolated from the skin of the snakehead Channa argus using the dorsal retractor muscle (DRM) of a starfish Asterina pectinifera as a bioassay system. The amino acid sequence of the purified peptide was analyzed using automated sequencing and MALDI-TOF mass spectrophotometry. The primary structure of the purified peptide was determined to be Pro-Ala-Leu-Ala-Leu. To investigate the complete primary structure of this peptide, Pro- Ala-Leu-Ala-Leu-OH and Pro-Ala-Leu-Ala-Leu-NH2 were synthesized. The chemical and pharmacological properties of the synthetic peptides were compared with those of the native peptide. Both the native peptide and synthetic Pro-Ala- Leu-Ala-Leu-OH had identical behaviors on the reverse-phase and cation-exchange HPLC chromatograms. Synthetic Pro-Ala-Leu-Ala-Leu-OH showed contractile activity on the DRM, and the threshold concentration of this peptide was approximately $10^{-8}$ M. The maximal contractile effect ($E_{max}$) of this peptide was $294{\pm}45.4$% at $10^{-5}$ M.

Biological Activities of Extracts from Crucian Carp (붕어 고음추출물의 생리활성)

  • KIM Chan-Hee;SEO Jung-Kil;GO Hye-Jin;PARK Nam Gyu;CHUNG Joon-Ki;HWANG Eun-Young;Ryu Hong-Soo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.32 no.4
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    • pp.507-511
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    • 1999
  • The pharmacological effects of hydrocooked extracts of crucian carp have been investigated. All of the hydrocooked extracts showed the contractile effect on the isolated rat duodenum and decreased to a certain extent the normal blood pressure in anesthetized rat. The hydrocooked extracts also exhibited a dose-dependent relaxation on the isolated rat aorta precontracted with 50 mM KCl. All of these except for RM 60 fraction haying cytotoxic effect against MCF-7 human breast cancer cell showed neither antibacterial activity nor antitumor activity. In addition, we found that although body weight gain in the hydrocooked extracts treated group were all reduced significantly compared to control group, there were no significant changes in the hematological parameters, except that the levels of high-density lipoprotein was significantly increased. These results suggest that the hydrocooked extracts of crucian carp may contain a variety of bioactive materials.

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The Study on the Change of EGG and HRV through Respiratory Control (호흡조절에 따른 위전도와 심박변이도 변화 연구)

  • Haa, Song-Yong;Park, Young-Bae;Yang, Dong-Hoon;Park, Young-Jae;Kim, Min-Yong
    • The Journal of the Society of Korean Medicine Diagnostics
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    • v.11 no.1
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    • pp.157-166
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    • 2007
  • Background: The change in the respiratory pattern has an influence on the change in the autonomic nervous system, which in turn has an influence on the EGG to measure a gastric activity. However, the study on the influence on the EGG parameters by respiratory control and on the correlation between the HRV and EGG through respiratory control has not been perform yet. Objective: It is to perform a series of experiments to find out how the EGG parameters are influenced by the controlled respiration and what correlation there may exist between the EGG and HRV to measure the change in the autonomic nervous system after controlled respiration. Methods: 1st Experiment: During a 15minutes' voluntary respiration, HRV was measured, and it was measured again during another 15 minutes' controlled respiration. 2nd Experiment: After an eight hours' fast, EGG was measured for a period of 30 minutes, and then after another 15 minutes' voluntary respiration, a test-meal was offered for 10 minutes and again EGG was measured. The next day, after an 8 hour's fast, EGG was measured for 30 minutes, and after a 15 minutes' controlled respiration and offered with a test-meal for 10 minutes and then EGG was measured again for 30 minutes. Results: 1. It was observed in all the channels that the power ratio increased more after controlled respiration than after voluntary respiration. No statistical significance, however, could be observed. 2. Through controlled respiration, the HF of HRV and the power ratio of EGG Channel 4 was negatively correlated, while the LF/HF of HRV and the power ratio of EGG channel 1 & 4 was positive correlated. Such correlations as mentioned above, however, could not be observed in HRV & EGG through voluntary respiration. Conclusions: 1. It was concluded that the increase in the power of gastric contractile after controlled respiration is bigger than the increase in the power of gastric contractile after voluntary respiration. 2. It was concluded that the gastric contractile power and sympathetic activity through controlled respiration was negatively correlated, while the gastric contractile power and parasympathetic activity through controlled respiration was positively correlated.

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Conformation and Biological Activity of the Neuropeptide $\gamma$ (Neuropeptide $\gamma$의 구조 및 생리활성)

  • Ku Hee-Jung;SEO Jung-Kil;KIM Eun-Hi;HUH Min-Do;CHUNG Joon-Ki;PARK Jang-Su;KANG Shin-Won;PARK Nam Gyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.30 no.2
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    • pp.244-251
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    • 1997
  • The relationship between structure and biological activity was studied on the three neuropeptides (mammalian, trout- and goldfish-neuropeptide $\gamma$) that were syntheized by the solid-phase method. Circular dichroism spectra showed that mammalian, trout- and goldfish-neuropeptide $\gamma$ adopted an unordered structure in buffer solution. In the-presence of neutral and acidic liposomes, mammalian and trout-neuropeptioe $\gamma$ also took a random structure. However, goldfish-neuropeptide $\gamma$ took an $\alpha-helical$ structure in acidic liposomes. The intestinal motility response was investigated with carp intestines, guinea-pig ileums and rat duodenums. In case of carp intestine, contractile activity was as follows : goldfish-neuropeptide $\gamma\simeq$ trout-neuropeptide $\gamma>$ mammalian-neuropeptide $\gamma$, On the other hand, the contractile activity of mammalian-neuropeptide $\gamma$ was more potent than trout- and goldfish-neuropeptide $\gamma$ in the guinea-pig ileums and rat duodenums. These results suggest that neuropeptide $\gamma$ show the species-specific activity.

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Purification of Neuropeptide with the Contractile Activity on the Smooth Muscle from the Skin of Conger Eel Conger myriaster (붕장어(Conger myriaster)의 피부로부터 평활근 수축작용을 지닌 신경성 펩타이드의 정제)

  • Go, Hye-Jin;Park, Nam-Gyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.45 no.4
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    • pp.358-366
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    • 2012
  • A novel neuropeptide was isolated from the skin of the conger eel Conger myriaster using hagfish Eptatretus burgeri intestine as a bioassay system. The sequence of the purified peptide was analyzed using automated amino acid sequencing and MALDI-TOF mass spectrophotometry. The molecular ion peak in the MALDI-TOF mass spectrum of the peptide was at m/z 962.89 $(M+H)^+$. The sequence of the peptide was determined to be L-P-M-L-E-T-Q-M, and was tentatively named comyrin. To investigate the complete primary structure of comyrin, comyrin-OH and comyrin-$NH_2$ were synthesized and the chemical and pharmacological properties of the synthetic peptides were compared with those of the native peptide. However, the elution time of synthetic peptides did not match that of the native peptide on the reverse-phase HPLC chromatogram. In addition, the synthetic peptides did not cause contractile activity in the intestinal smooth muscle of the hagfish. Based on these results, one possible reason for this disagreement may be the presence of a D-amino acid in comyrin.

Isolation and Purification of Neuropeptides from the Tube Feet of the Starfish Asterias amurensis (아무르 불가사리(Asterias amurensis)의 관족으로부터 신경성 펩타이드의 분리 및 정제)

  • Jo, Mi Jeong;Go, Hye-Jin;Kim, Gun-Do;Park, Nam Gyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.47 no.2
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    • pp.129-134
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    • 2014
  • Two neuropeptides were purified from the acidified tube feet extract of the starfish Asterias amurensis by C18 reversed phase and size-exclusion high-performance liquid chromatography (HPLC). The tube feet extract and the purified peptides (AST-I and AST-II) showed potent contractile activity on dorsal retractor muscle (DRM) of the starfish Asterina pectinifera and intestine (smooth muscle) of the panther puffer Takifugu pardalis. Treatment of the purified peptides with dithiothreitol (DTT) for 60 min at $37^{\circ}C$ significantly altered their retention times, suggesting that these compounds contained disulfide bonds. The molecular weights of AST-I and AST-II were determined to be 2064.2 Da and 6137.2 Da, respectively, by MALDI-TOF mass spectrometry.

Effects of age on angiotensin II response and antagonistic activity of losartan in rat aorta and liver

  • Jung, Yi-Sook;Lee, Sung-Hou;Shin, Hwa-Sup
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.462-468
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    • 1996
  • The present study was undertaken to investigate the effects of age on angiotensin II (AII) response and antagonistic activity of losartan using aortic rings and liver homogenates from rats ranging in age from 0.7 to 20 months. Whether the endothelium was present or not, the maximum contractile response to AII decreased with age. Removal of the endothelium enhanced AII-induced maximum contraction and these endothelial effects seemed to be due to endothelium-derived relaxing factor (EDRF) in all ages. Equilibrium binding studies demonstrated an age-related decrease in maximum binding $(B_{max})$ with little change in binding affinity $(K_d)$. In rat aorta, the extent of losartan-induced parallel shifts $(K_B)$ in AII concentration-response curves was not significantly different between ages. In addition, $IC_{50}$ value of losartan in competition binding was not changed with age in rat liver homogenates. These results suggest that the potency of losartan is not altered with age in rat aorta and liver, although AII-induced contractile response and the maximum AII binding decreased significantly with age.

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