• Title/Summary/Keyword: 5-HT1A

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Pharmacological Effect of Hawangyeonhaedoktang on Experimental Triglyceride Accumulated HepG2 Cells (실험적 중성지질 축적 HepG2세포에 미치는 황련해독탕의 약리적 효과)

  • 차재영;김대진;김석환;김영길;조영수
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.32 no.4
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    • pp.586-590
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    • 2003
  • The pharmacological effect of Korean-Chinese traditional herbal medicine, Hawangyeonhaedoktang (HT) on experimentally induced-triglyceride accumulation in cultured human hepatocyte HepG2 cells was studied. HePG2 cells were cultured in the Dulbecco's modified Eagle's (DME) medium without (Control medium) or with HT (0.5 mg/mL and 5.0 mg/mL) containing 1 mM oleate, 0.2% bovine serum albumin (BSA), and glucose 4.5 mg/mL for 6 and 24 hours in experiment I and 2 mM oleate, 0.5% BSA, and glucose 4.5 mg/mL for 6, 24 and in hours in Experiment II or 1 and 3 hours in Experiment III. Oleate [$^{14}$ C](0.5 $\mu$Ci/mL medium) added as a radioactive lipid precursor in the experiment I. In the experiment I, the intracellular triglyceride concentration was decreased remarkably during incubation for 6 and 24 hours, in a dose-dependent manner. At the same time, HT caused a decrease in the incorporation of [$^{14}$ C] oleate into intracellular triglyceride fraction and the secretion of triglyceride labeled with [$^{14}$ C] oleate into medium. In the experiment II and III compared to experiment I, the triglyceride accumulation in HepG2 cells was occurred, and HT prevented the accumulation of triglyceride during incubation for 24 and 48 hours. This result suggest that HT prevent the triglyceride accumulation in human hepatocytes by its inhibiting action on the intercellular triglyceride biosynthesis.

The Analgesic Effect of Bee Venom Acupuncture and Its Mechanism on the Type II Collagen-Induced Arthritis Rats

  • Seo, Byung-Kwan;Baek, Yong-Hyun;Choi, Do-Young;Park, Dong-Suk
    • Journal of Acupuncture Research
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    • v.22 no.2
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    • pp.19-32
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    • 2005
  • Objectives : to evaluate the analgesic effect of bee venom acupuncture on Choksamni (ST36) in the collagen-induced arthritis rats and investigate the role played by serotonergic receptor subtypes (5-HT1a, 5-HT2a) in the antinociceptive effect of bee venom acupuncture in a thermal hyperalgesia test Methods : Experiments were performed on 5 week-aged 60 male Sprague-Dawley rats according to National Institute of Health guidelines and the ethical guidelines of the International Association for the Study of Pain (IASP). Arthritis was induced with arthrogenic collagen emulsion (Bovine type II collagen ${\mu}g$ with incomplete Freund's adjuvant $100\;{\mu}g$). The onset of arthritis was considered to be present when erythema and swelling were detected in at least one joint. The thermal hyperalgesia was evaluated weekly with tail flick test in the rats of severity grade 3 without any injury at tail and foot (including inflammation, ulceration, snap). In the fourth week after first immunization, the analgesic effect of bee venom acupuncture (Choksamni, ST36) was measured with consecutive tail flick latency after intraperitoneal injection of spiroxatrine (1mg/kg) and spiperone (1mg/kg). Results : Chronic inflammatory pain was induced as time elapsed after the immunization of arthrogenic collagen and the maximum value was reached from third to fifth week. Chronic inflammatory pain induced by CIA was inhibited by bee venom acupuncture on the left ST36. The analgesic effect of bee venom acupuncture was inhibited by intraperitoneal injection of 5-HT1a antagonist spiroxatrine and 5-HT2a antagonist spiperone. Conclusions : Therefore, a conclusion. that the analgesic effect of bee venom acupuncture in the chronic inflammatory pain is partially mediated by 5-HT1a and 5-HT2a receptors can be made.

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Indol-3-Carbinol Regulated Tight Junction Permeability and Associated-Protein Level and Suppressed Cell Invasion in Human Colon Cancer Cell Line, HT-29 (인돌 (Indol-3-Carbinol)이 인체대장암세포 HT-29 세포의 투과성 밀착결합조절과 세포 침윤성 억제에 미치는 영향)

  • Kim, Sung-Ok;Choi, Yung-Hyun;Choe, Won-Kyung
    • Journal of Nutrition and Health
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    • v.41 no.1
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    • pp.13-21
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    • 2008
  • To determine whether indol-3-carbinol (BC, $C_9H_9NO$), an autolysis product of a glucosinolate and a glucobrassicin in vegetables, regulated tight junction proteins (TJ) and suppressed cell invasion in colon cancer cells, this experiment was performed. Our results indicate that I3C inhibit cell growth of HT-29 cells in a dose (0, 50, $100{\mu}M$) and time (0, 24 and 48h) dependent manner. Using the wound healing and matrigel invasion study, respectively, BC inhibits the cell motility and invasion of the ovarian cancer cell line. The TEER values were increased in HT-29 cells grown in transwells treated with BC, reversely, paracellular permeability was decreased in those of condition. Claudin-1, claudin-5, ZO-1 and occuldin have been shown to be positively expressed in HT-29 coloncancer cells. I3C occurs concurrently with a significant decrease in the levels of those of proteins in HT-29 cells. But E-cadherin level in the HT-29 was increased by I3C. The reduction of claudin-1 and claudin-5 protein levels occurred post-transcriptionaly since their mRNA levels are no difference by I3C. Therefore, our results suggest that I3C may be expected to inhibit cancer metastasis and invasion by tighten the cell junction and restoring tight junction in colon cancer cell line, HT-29.

A Study on the Acupoint and Utilization of HT1 (극천(HT1)의 취혈과 활용에 대한 연구)

  • Kang, Tae-Ri;Lee, Sang-Ryong
    • Korean Journal of Acupuncture
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    • v.34 no.4
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    • pp.185-190
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    • 2017
  • Objectives : The research was conducted for the use of HT1 in the shoulder disease through correct acupuncture. Methods : (1) The contents were compared through reviewing literature. (2) The literature was studied in conjunction with the shoulder pathology and anatomical structures. Results : (1) The location of HT1 is described as 'in the axilla, over the axillary artery' in many literature, and the depth of HT1 is as shallow as 1 cm. The WHO standard also follows this. (2) There were many references to 'in the axilla, between the big muscles' in later generations, but there were mixed opinions about the exact muscle names. Based on the acupunctural review and the musculoskeletal study, the big muscles are considered to be 'Pectoralis major' and 'Latissimus dorsi'. (3) Among the muscles constituting the rotator cuff, applying acupuncture on HT1 is essential for 'Subscapularis m.'. Therefore, it is effective to stimulate 'Subscapularis m.' to a depth of 1.5 to 4 cm. Conclusions : The accurate acupoint of HT1 enables various uses of flank, armpit, shoulder and arm diseases as well as cardiopathy. Especially, it helps to treat the muscles through safe and effective acupuncture in shoulder rotator cuff disorder.

Imbalance in the spinal serotonergic pathway induces aggravation of mechanical allodynia and microglial activation in carrageenan inflammation

  • Junxiu Jin;Dong Ho Kang;Jin Jeon;Hyung Gon Lee;Woong Mo Kim;Myung Ha Yoon;Jeong Il Choi
    • The Korean Journal of Pain
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    • v.36 no.1
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    • pp.51-59
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    • 2023
  • Background: This study investigated the effect of an excess and a deficit of spinal 5-hydroxytryptamine (5-HT) on the mechanical allodynia and neuroglia activation in a rodent pain model of carrageenan inflammation. Methods: Male Sprague-Dawley rats were implanted with an intrathecal (i.t.) catheter to administer the drug. To induce an excess or deficit of 5-HT in the spinal cord, animals were given either three i.t. 5-HT injections at 24-hour intervals or a single i.t. injection of 5,7-dihydroxytryptamine (5,7-DHT) before carrageenan inflammation. Mechanical allodynia was measured using the von Frey test for 0-4 hours (early phase) and 24-28 hours (late phase) after carrageenan injection. The changes in the activation of microglia and astrocyte were examined using immunofluorescence of the dorsal horn of the lumbar spinal cord. Results: Both an excess and a deficit of spinal 5-HT had no or a minimal effect on the intensity of mechanical allodynia during the early phase but prevented the attenuation of mechanical allodynia during the late phase, which was observed in animals not treated with i.t. 5-HT or 5,7-DHT. Animals with an excess or deficit of 5-HT showed stronger activation of microglia, but not astrocyte, during the early and late phases, than did normal animals. Conclusions: Imbalance in the descending 5-HT pathway in the spinal cord could aggravate the mechanical allodynia and enhance the activation of microglia, suggesting that the spinal 5-HT pathway plays an essential role in maintaining the nociceptive processing in balance between facilitation and inhibition in inflammatory pain caused by carrageenan inflammation.

Neuroprotective Effect of 8-OH-DPAT on Long-term Sequelae from Prenatal Ischemia in Rats

  • Lee, Se-Oul;Zhang, Tie-Yuan;Kim, Gun-Tae;Kim, Hee-Soo;Lee, Jong-Doo;Jahng, Jeong-Won;Kim, Dong-Goo
    • The Korean Journal of Physiology and Pharmacology
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    • v.6 no.6
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    • pp.293-297
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    • 2002
  • The role of 5-hydroxytryptamine $(5-HT)_1A$ receptor activity in prenatal ischemia was studied, by injecting 8-hydroxy-dipropylaminotetraline (8-OH-DPAT; $50{\mu}g/kg,$ s.c.), a $5-HT_1A$ agonist on gestation day 17, and 30 min later inducing transient ischemia by ligating the uterine vessels for 30 min. On postnatal day 95, rats that had experienced prenatal ischemia showed impaired motor coordination and reduced concentration of 5-HT in the cerebellum compared with Sham-operated controls. In addition, they showed increased $5-HT_1A$ receptor densities in the cerebral cortex. Pretreatment with 8-OH-DPAT ameliorated the behavioral and neurochemical sequelae measured in the present study. The results suggest that $5-HT_1A$ receptors protect the brain from ischemic insult and/or facilitate recovery after prenatally experienced ischemia.

Synthesis and Small Animal Brain PET Study of a Serotonin Receptor Radiotracer, 18F-Mefway (세로토닌 5-HT1A수용체 방사성 추적자 18F-Mefway의 합성과 소동물 뇌 PET 연구)

  • Ahn, Sung-Min;Hong, Tae-Kee;Ryu, Young-Hoon;Choi, Jae-Yong;Kim, Sung-Chul
    • The Journal of the Korea Contents Association
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    • v.9 no.11
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    • pp.262-270
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    • 2009
  • $^{18}F$-mefway has been developed as radioligand for serotonin receptor 5-$HT_{1A}$. The object of this study was to obtain the mefway precursor with the higher yield than previous method and to identify whether $^{18}F$-mefway can bind to 5-$HT_{1A}$ or not. from microPET imaging of small animal brain. Precursor was prepared by a modification of the reported procedure then [$^{18}F$] labeling was performed by adding $^{18}F$ ion at $130^{\circ}C$ in the hot cell for 30min. After purification of reaction mixture using alumina Sep-pak and HPLC, microPET images of small animal brain were determined. The chemical yield of precursor was increased from 9% to 34% using oxalyl chloride and LAH/diethylether. We synthesized a precursor which was successfully labeled with no-carrier-added $^{18}F$-by new synthetic route. This research suggest that $^{18}F$-mefway will be used a radiopharmaceutical for evaluation of central nerve system disorder as imaging a gent for 5-$HT_{1A}$ receptor.

Review of Sexual Dysfunction in Male Schizophrenics (남자 정신분열병 환자에서 성기능장애에 대한 검토)

  • Choi, Yeong Tae;Cheon, Jin Sook;Oh, Byoung Hoon
    • Korean Journal of Biological Psychiatry
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    • v.7 no.1
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    • pp.85-98
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    • 2000
  • Objective : There are four possible explanations for the sexual dysfunction of schizophrenics. The first is the possibility of a real structural aspect. The second possibility is that sexual function changes secondary to the illness. The third possibility is that there are medical and sociocultural barriers to sexual expression for chronic schizophrenics. The fourth possibility is that sexual dysfunction due to antipsychotic medication. However, we didn't know the precise cause of sexual dysfunction in schizophrenics. Therefore, the purpose of this study was to explore the mechanism of illness itself and antipsychotics on sexual dysfunction in male schizophrenics. Methods : The serum prolactin(PRL), testosterone(TST), and the plasma serotonin(5-HT) concentrations were measured by radioimmunoassay and high performance liquid chromatography method for 100 healthy male schizophrenics according to the DSM-IV. Concomitantly, the severity of psychotic symptoms using Clinical Global Impression(CGI), Brief Psychiatric Rating Scale(BPRS), Positive and Negative Syndrome Scale(PANSS), and the severity of side effects for antipsychotics using Extrapyramidal Side Effects Scale(EPSE), Anticholinergic Side Effects Scale(ACSE), the cognitive function using PANSS-Cognitive Function(PANSS-CF), Mini Mental State Exam-Korean(MMSE-K), and the sexual dysfunction using Sexual Functioning Questionnaire(SFQ), Questionnaire for Sexual Dysfunction in Men were assessed. The PRL, TST, and 5-HT levels of 50 healthy male controls who had no medical, neurological, and psychiatric illnesses were evaluated. The sexual function using SFQ(items FGa, FNa) were also assessed. Furthermore, the correlation with age, education, religion, economic status, age at onset, duration of illnesses, duration of admission, levels of PRL, TST, 5-HT, antipsychotic dosages, potency, benztropine, total duration of medication, EPSE, ACSE, CGI, BPRS, PANSS, PANSS-CF, MMSE-K and sexual dysfunctions were identified in male schizophrenics. Results : 1) The frequencies of sexual dysfunctions for schizophrenics(80%) were significantly(p<0.001) higher than those for controls(42%). The sexual dysfunctions according to sexual response cycle were 'low sexual desire' 76%, 'impairment of achieving erection' 75%, 'impairment of maintaining erection' 75%, 'impairment of obtaining orgasm' 32%, 'impairment in the quality of orgasm' 61%, 'impairment in quantity of ejaculate' 44%, 'premature ejaculation' 15%, and 'delayed ejaculation' 50%. 2) The PRL, 5-HT levels of schizophrenics($28.5{\pm}20.6ng/ml$, $298.5{\pm}89.1ng/ml$) were significantly(p<0.001) higher than those of controls($10{\pm}5.6ng/ml$, $169.2{\pm}37.8ng/ml$), while the TST levels of schizophrenics($4.3{\pm}1.5ng/ml$) and controls($4.5{\pm}1.2ng/ml$) were not significantly different. The sexual dysfunctions of schizophrenics who had abnormal 5-HT levels($4.7{\pm}1.3$ scores) were significantly(p<0.05) higher than those of who had normal 5-HT levels($3.8{\pm}1.6$ scores) on item D7. 3) The sexual dysfunctions of unmarried schizophrenics were significantly(p<0.01 : p<0.05) higher than those of married schizophrenics($6.1{\pm}2.8$ scores, $4.7{\pm}1.3$ scores on item FGa : ${\beta}$=-0.211 on item FNa). The sexual dysfunctions were positively correlated with the rise of 5-HT levels(r=0.209, p<0.05 on item D4 and r=0.241, p<0.05 on item D7), the higher age at onset(r=0.275, p<0.01 on item FNa : r=-0.202, p<0.05 on item FDa), the longer duration of illnesses(r=0.237, p<0.05 on item D6), the longer duration of admission(r=0.234, p<0.05 on item D4 : r=0.328, p<0.05 on item D6), the longer total duration of medication(r=0.237, p<0.05 on item D6). However, age, education, religion, economic status, PRL, TST levels, antipsychotics dosage, potency, benztropine, ACSE, CGI, BPRS, PANSS, PANSS-CF, MMSE-K scores were not correlated with increased sexual dysfunctions. Conclusions : Male schizophrenics have significantly more sexual dysfunction to compare with controls. The higher frequencies of sexual dysfunctions were low sexual desire and erectile disorder. The unmarried, higher age at onset, and longer duration of diseases were positively correlated with increased sexual dysfunctions. Also high 5-HT levels were positively correlated with increased sexual dysfunctions. This means that studies of plasma 5-HT levels, albeit questionable indicators of central 5-HT function, offer some additional support for the association of sexual dysfunction with excess 5-HT activity as primary pathology of schizophrenia. Our findings suggest that excess 5-HT activity seems to affect the patient's sexual function.

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Facilitation of serotonin-induced contraction of rat mesenteric artery by ketamine

  • Park, Sang Woong;Noh, Hyun Ju;Kim, Jung Min;Kim, Bokyung;Cho, Sung-Il;Kim, Yoon Soo;Woo, Nam Sik;Kim, Sung Hun;Bae, Young Min
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.6
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    • pp.605-611
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    • 2016
  • Ketamine is an anesthetic with hypertensive effects, which make it useful for patients at risk of shock. However, previous ex vivo studies reported vasodilatory actions of ketamine in isolated arteries. In this study, we reexamined the effects of ketamine on arterial tones in the presence and absence of physiological concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) by measuring the isometric tension of endothelium-denuded rat mesenteric arterial rings. Ketamine little affected the resting tone of control mesenteric arterial rings, but, in the presence of 5-HT (100~200 nM), ketamine ($10{\sim}100{\mu}M$) markedly contracted the arterial rings. Ketamine did not contract arterial rings in the presence of NE (10 nM), indicating that the vasoconstrictive action of ketamine is 5-HT-dependent. The concentration-response curves (CRCs) of 5-HT were clearly shifted to the left in the presence of ketamine ($30{\mu}M$), whereas the CRCs of NE were little affected by ketamine. The left shift of the 5-HT CRCs caused by ketamine was reversed with ketanserin, a competitive 5-$HT_{2A}$ receptor inhibitor, indicating that ketamine facilitated the activation of 5-$HT_{2A}$ receptors. Anpirtoline and BW723C86, selective agonists of 5-$HT_{1B}$ and 5-$HT_{2B}$ receptors, respectively, did not contract arterial rings in the absence or presence of ketamine. These results indicate that ketamine specifically enhances 5-$HT_{2A}$ receptor-mediated vasoconstriction and that it is vasoconstrictive in a clinical setting. The facilitative action of ketamine on 5-$HT_{2A}$ receptors should be considered in ketamine-induced hypertension as well as in the pathogenesis of diseases such as schizophrenia, wherein experimental animal models are frequently generated using ketamine.

Effects of Xingjian(LR2),Shaofu(HT8) by Reinforcing and Reducing on the Regional Cerebral Blood Flow and Mean Arterial Blood Pressure in Normal Rats (행간(行間)·소부(少府) 보사침법(補瀉鍼法)이 국소뇌혈류량(局所腦血流量) 및 평균혈압(平均血壓)에 미치는 영향(影響))

  • Shin, Jeong-cheol;Ryu, Chung-ryul;Cho, Myeng-rae
    • Journal of Acupuncture Research
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    • v.20 no.6
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    • pp.190-200
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    • 2003
  • Objective: The purpose of this study is to examine influences by the order, Reduction and Reinforcement in Acupuncture on cerebral hemodynamics [regional cerebral blood flow(rCBF) and mean arterial blood pressure(MABP)] in normal rats. Methods: This experiments was to to investigate eath other changes of rCBF and MABP at Xingjian(LR2)(1st) Shaofu(HT8)(2nd) Reduction, Xingjian(LR2)(1st) Shaofu(HT8)(2nd) Reinforcement, Shaofu(HT8)(1st) Xingjian(LR2)(2st) Reduction and Shaofu(HT8)(1st) Xingjian(LR2)(2st) Reduction in Acupuncture. Results: 1. LR2(1st) HT8(2nd) Reduction in Acupuncture was decreased rCBF and MABP in compared with normal condition. 2. LR2(1st) HT8(2nd) Reinforcement in Acupuncture was significantly decreased rCBF, and was decreased MABP in compared with normal condition. 3. HT8(1st) LR2(2st) Reduction in Acupuncture was decreased rCBF during acupuncture but was recovered rCBF after with-drawing of the neddle. 4. HT8(1st) LR2(2st) Reduction in Acupuncture was decreased MABP during acupuncture and after withdrawing of the neddle. 5. HT8(1st) LR2(2st) Reinforcement in Acupuncture was significantly increased rCBF during acupuncture and 30min after withdrawing of the neddle. 6. HT8(1st) LR2(2st) Reinforcement in Acupuncture was decreased MABP during acupuncture, but was recovered MABP after withdrawing of the neddle. Conclusions: I suggested that LR2 HT8 Reduction in Acupuncture and LR2 HT8 Reinforcement in Acupuncture cause a diverse response of cerebral hemodynas.

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