Isoflavonoids에 의한 혈관이완효과에 있어 Rho-kinase의 역할

제현동,Je, Hyun-Dong 대한약학회 2006 약학회지 Vol.50 No.4

The aim of present study was to investigate the possible influence of Rho-kinase inhibition on the plant-derived estrogen-like compounds-induced arterial relaxation. Agonist- or depolarization-induced vascular smooth muscle contractions involve the activation of Rho-kinase pathway. However there are no reports addressing the question whether this pathway is involved in genistein-or daidzein-induced vascular relaxation in rat aortae precontracted with phenylephrine or thromboxane $A_2$ mimetic U-46619. We hypothesized that Rho-kinase inhibition plays a role in vascular relaxation evoked by genistein or daidzein in rat aortae. Endothelium-intact and denuded arterial rings from male Sprague-Dawley rats were used and isometric contractions were recorded using a computerized data acquisition system. Genistein concentration-dependently inhibited phenylephrine or thromboxane $A_2-induced$ contraction regardless of endothelial function. Surprisingly, in the agonists-induced contraction, similar results were also observed in aortae treated with daidzein, the inactive congener for protein tyrosine kinase inhibition, suggesting that Rho-kinase might act upstream of tyrosine kinases in phenylephrine-induced contraction. In conclusion, in the agonists-precontracted rat aortae, genistein and daidzein showed similar relaxant response regardless of tyrosine kinase inhibition or endothelial function.

위장관 수축성에 대한 Histamine과 Atropine의 융합성 조절 효과

제현동,민영실,Je, Hyun Dong,Min, Young Sil 중소기업융합학회 2021 융합정보논문지 Vol.11 No.10

본 연구에서 진단, 과민반응 검사에 사용되며 의약품에 불순물로 포함되어 규제되는 histamine의 단독 및 병용 투여에서 조직/근육 선택적 장관 수축성 조절에 대한 실험을 하고자 하였다. Histamine은 muscarinic receptor 작용 외에 histamine H1 receptor에 대한 직접 작용으로 수축성을 증가시켰고 회장/결장 윤주근에서 수축성을 거의 증가시키지 않았다. 또한 M3 수용체에 선택적으로 작용하는 atropine의 병용 효과를 관찰하였는데 histamine과 병용된 atropine은 장관 중 회장의 종주근의 수축성을 거의 감소시키지 않았고 회장/결장의 윤주근의 수축성을 감소시키지 않았다. 따라서 적어도 회장의 종주근에서 histamine은 M3 수용체를 거의 경유하지 않고 작용하고 atropine은 항무스카린 효과 외에 histamine에 의한 조직 선택적 위장관 운동성을 거의 조절하지 않는 것으로 생각된다. 그리고 이러한 단순한 검색은 의약품 불순물 검사로 선호될 것으로 생각된다. The aim of the study was to observe the influence and related mechanism of histamine and its analogues used for hypersensitivity tests and used as an indicator of impurities in drugs on the tissue-specific intestinal contraction. Intestinal contraction includes the activation of thick or thin filament regulation. However, there are few reports addressing the question whether this regulation is involved in histamine-induced regulation. We hypothesized that histamine plays a role in tissue-dependent regulation of intestinal contractility. Denuded ileal/colonic longitudinal and circular muscles of male rats were used and isometric contractions were recorded using a data acquisition system. Interestingly, histamine alone didn't increase the contraction of the circular muscle but increased the contraction of the longitudinal muscle. Histamine together with atropine (M3 receptor antagonist) didn't inhibit the contraction of the longitudinal and circular muscle. Therefore, histamine alone and together with atropine increases the ileal longitudinal muscle contraction suggesting that additional mechanisms (decreased receptor density, postreceptor signaling or distribution of agonists) might be involved in the regulation of ileal muscle contractility. In conclusion, histamine and/or atropine has some effect on the regulation of the longitudinal contractility regardless of M3 receptor and the simpler test would be preferred as the drug impurity test compared to more complicated tests.

Carbachol에 의한 위장관 수축에 대한 rebamipide의 조절 효과

제현동 ( Hyun Dong Je ) 대구가톨릭대학교 자연과학연구소 2013 자연과학연구논문집 Vol.11 No.1

The aim of present study was to investigate the possible influence and related mechanism of rebamipide on the intestinal smooth muscle contraction. Intestinal contraction involves the activation of thick or thin filament pathway. However, there are no reports addressing the question whether this pathway is involved in rebamipide-induced regulation. We hypothesized that rebamipide plays a role in intestinal contraction evoked by carbachol in rat intestine. Denuded ileal and colonic muscles from male rats were used and isometric contractions were recorded using a computerized data acquisition system. Interestingly, rebamipide alone didn``t inhibit and rather slightly increased the contraction in the denuded muscle. Therefore, rebamipide alone and together with indomethacin increases the ileal contraction suggesting that additional pathways might be involved in the regulation of ileal contractility. In conclusion, rebamipide has some effect on the regulation of intestinal contractility.

저농도 및 고농도의 알코올의 투여와 혈관수축성의 조절

제현동(Hyun Dong Je) 대한약학회 2012 약학회지 Vol.56 No.3

The aim of present study was to investigate the possible influence and related mechanism of alcohol on the arterial contraction. Vascular contraction involves the activation of thick or thin filament pathway. However, there are no reports addressing the question whether this pathway is involved in alcohol-induced regulation. We hypothesized that alcohol plays a role in vascular contraction evoked by a vasoconstrictor in rat aortae regardless of endothelial function. Denuded arterial rings from male rats were used and isometric contractions were recorded using a computerized data acquisition system. Interestingly, alcohol at a low concentration (3% v/v) inhibited thromboxane A2 or phorbol ester-induced contraction with endothelial function but at a high concentration (10%) didn't inhibit and rather increased the contraction in the denuded muscle. Therefore, alcohol at a low concentration decreases the contraction and alcohol at a high concentration increases the contraction suggesting that additional pathways different from endothelial nitric oxide synthesis might be involved in the regulation of contractility. In conclusion, alcohol has some effect on the regulation of contractility regardless of endothelial function.

Passiflora caerulea 유래 dihydroxyflavone의 투여와 항염증 및 진통효과의 평가

제현동 ( Hyun Dong Je ) 대구가톨릭대학교 자연과학연구소 2016 자연과학연구논문집 Vol.14 No.1

The aim of present study was to investigate the possible influence and related mechanism of Passiflora caerulea derived-dihydroxyflavone (chrysin) on the inflammation or nociception. Passiflora caerulea is a species of flowering plant native to South America (Argentina, Chile, Paraguay, Uruguay and Brazil). However, there are no reports on the antinociceptive or anti-inflammatory properties of dihydroxyflavone, the primary ingredient of Passiflora caerulea. We hypothesized that dihydroxyflavone plays a role in the modulation of inflammation or nociception evoked by carrageenan, acetic acid or heat. Male Institute of Cancer Research mice were used and the size of edema, frequency of writhing and latency of abnormal behaviors such as licking, flicking, shaking or jumping were measured and recorded. The present study was carried out to evaluate the anti-inflammatory and antinociceptive effects of dihydroxyflavone. The administration of dihydroxyflavone (30 and 100 mg/kg) inhibited carrageenan-induced paw edema only at the final phase suggesting the blockade of synthesis or release of prostaglandins. It also reduced the frequency of the acetic acid-induced writhing reflex in mice. In addition, the administration of dihydroxyflavone prolonged the latency for extraordinary reaction at the hot plate in mice. In conclusion, dihydroxyflavone has anti-inflammatory and analgesic properties and is a potential therapeutic for inflammation and nociception.

전처치된 지치 유래 naphthoquinone의 혈관 수축성 조절 효과

제현동 ( Hyun Dong Je ) 대구가톨릭대학교 자연과학연구소 2015 자연과학연구논문집 Vol.13 No.1

The present study was undertaken to investigate the influence of naphthoquinone (shikonin) on vascular smooth muscle contractility and to determine the mechanism involved. We hypothesized that naphthoquinone, the primary ingredient of Lithospermum erythrorhizon, plays a role in vascular relaxation through inhibition of Rho-kinase in rat aortae. Intact or denuded arterial rings from male Sprague-Dawley rats were used and isometric tensions were recorded using a computerized data acquisition system. Interestingly, naphthoquinone significantly inhibited fluoride, phorbol ester or thromboxane A2 mimetic-induced contraction in denuded muscles suggesting that additional pathways different from endothelial nitric oxide synthesis such as inhibition of Rho-kinase or MEK might be involved in the vasorelaxation. Furthermore, naphthoquinone nonspecifically inhibited fluoride- or phorbol ester-induced contraction suggesting the mechanism including inhibition of fluoride- or phorbol ester-induced increases in MYPT1 or ERK1/2 phosphorylation. This study provides evidence that naphthoquinone induces vascular relaxation through inhibition of Rho-kinase or MEK in rat aortae.

Propolis 유래 trihydroxyflavone의 투여와 통증 조절 및 항염증 효과의 평가

제현동 ( Je Hyun Dong ) 대구가톨릭대학교 자연과학연구소 2017 자연과학연구논문집 Vol.15 No.1

In this study, we investigated the possible influence and related mechanism of propolis derived-trihydroxyflavone on the nociception or inflammation. Propolis is a resinous mixture that honey bees produce by mixing saliva and beewax with exudate gathered from tree buds, sap flows or other botanical sources. However, there are no reports on the antinociceptive or anti-inflammatory properties of trihydroxyflavone, the primary ingredient of propolis. We hypothesized that trihydroxyflavone plays a role in the modulation of inflammation or nociception evoked by carrageenan, acetic acid or heat. Male Institute of Cancer Research mice were used and the size of edema, frequency of writhing and latency of abnormal behaviors such as licking, flicking, shaking or jumping were measured and recorded. The present study was carried out to evaluate the anti-inflammatory and antinociceptive effects of trihydroxyflavone. The administration of trihydroxyflavone (30 and 100 mg/kg) inhibited carrageenan-induced paw edema only at the final phase suggesting the blockade of synthesis or release of prostaglandins. It also reduced the frequency of the acetic acid-induced writhing reflex in mice. In addition, the administration of trihydroxyflavone prolonged the latency for extraordinary reaction at the hot plate in mice. In conclusion, trihydroxyflavone has anti-inflammatory and analgesic properties and is a potential therapeutic for nociception and inflammation.

쑥 유래 eupatilin의 투여와 통증 조절 및 수면 유도 효과의 평가

제현동 ( Je Hyun Dong ) 대구가톨릭대학교 자연과학연구소 2018 자연과학연구논문집 Vol.16 No.1

In this study, we investigated the possible influence and related mechanism of Artemisia asiatica derived-eupatilin on the nociception or anesthesia. Eupatilin (5,7-Dihydroxy-3',4',6-trimethoxyflavone) is an O-methylated flavone, a type of flavonoids found in Artemisia asiatica (Asteraceae). However, there are no reports on the antinociceptive or hypnotic properties of eupatilin, the primary ingredient of Artemisia asiatica. We hypothesized that eupatilin plays a role in the modulation of insomnia or nociception evoked by acetic acid or heat. Male Institute of Cancer Research mice were used and the duration of sleep, frequency of writhing and latency of abnormal behaviors such as licking, flicking, shaking or jumping were measured and recorded. The present study was carried out to evaluate the hypnotic and antinociceptive effects of eupatilin. The administration of eupatilin (30 and 100 mg/kg) increased barbiturate-induced sleep suggesting the activation of GABA_A receptor. It also reduced the frequency of the acetic acid-induced writhing reflex in mice. In addition, the administration of eupatilin prolonged the latency for extraordinary reaction at the hot plate in mice. In conclusion, eupatilin has hypnotic and analgesic properties and is a potential therapeutic for nociception and insomnia.

대두 유래 genistein의 투여와 불안 조절 및 수면 유도 효과의 평가

제현동 ( Je Hyun Dong ) 대구가톨릭대학교 자연과학연구소 2019 자연과학연구논문집 Vol.17 No.1

In this study, we investigated the possible influence and related mechanisms that have yet to be clearly demonstrated of Glycine max derived-genistein on the antianxiety or anesthesia. Genistein (5,7- Dihydroxy - 3 - (4 - hydroxy phenyl) chromen - 4 - one) which exert protective effects on the cardiovascular system through mechanisms that have yet to be clearly demonstrated, is a hydroxylated isoflavone, a type of flavonoids found in Glycine max (Fabaceae). However, there are no reports on the antianxiety or hypnotic properties of genistein, the primary ingredient of Glycine max. We hypothesized that genistein plays a role in the modulation of insomnia or anxiery evoked by elevated plus maze. Male Institute of Cancer Research mice were used and the duration of sleep, duration and entry frequency into open arms were measured and recorded. The present study was carried out to evaluate the antianxiety and hypnotic effects of genistein. The administration of genistein (30 and 100 mg/kg) increased b arbitur ate - induced sleep suggesting the activation of GABAA receptor. It also increased the duration and entry frequency into open arms in the maze. In conclusion, genistein has hypnotic and antianxiety properties and is a potential therapeutic for anxiety and insomnia.

참마 유래 diosgenin의 투여와 불안 조절 및 통증 억제 효과의 평가

제현동 ( Je Hyun Dong ) 대구가톨릭대학교 자연과학연구소 2020 자연과학연구논문집 Vol.18 No.1

The study was undertaken to investigate the influence and related mechanisms that have yet to be explicitly demonstrated of Dioscorea villosa (Dioscoreaceae) derived-diosgenin on the antianxiety or antinociception. However, there are no reports on the antianxiety or antinociceptive properties of diosgenin, the primary ingredient of Dioscorea villosa. We hypothesized that diosgenin plays a role in the modulation of nociception or anxiety evoked by elevated plus maze. Institute of Cancer Research male mice were used and the frequency of writhing, the duration of sleep, and entry frequency and duration into open arms were measured and recorded. The administration of diosgenin (30 and 100 mg/kg) decreased the frequency of writhing reflex suggesting the inhibition of prostaglandin synthesis. It also increased the duration and entry frequency into open arms in the maze. In conclusion, diosgenin has antinociceptive and antianxiety properties and is a potential therapeutic for anxiety and insomnia.