• 대한수의학회지
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• 제44권3호
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• pp.389-397
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• 2004

The therapeutic efficacy of xylamine in the field of psychological medicine has been recognized for years and the drug is used to treat depression and some other conditions, but little is known about its mechanism of action on vascular system. Therefore, the present study was designed to investigate the influence of xylamine on the contractile responses of isolated rat thoracic arteries to phenylephrine(PE) and potassium chloride(KCl). Xylamine produced a concentration-dependent relaxation in PE-precontracted endothelium intact(+E) rat aortic rings, but not in a KCl-precontracted aortic rings. Also, xylamine inhibited the PE-induced contraction in concentration-dependent manner, but not in the high KCl-induced contraction in +E rings. This concentration-dependent inhibition was suppressed by the removal of the endothelium (-E). The inhibitory effects of xylamine($0.3{\mu}M$) on the PE-induced contractions were suppressed by N(G)-nitro-L-arginine(L-NNA), N(omega)-nitro-L-arginine methyl ester(L-NAME), aminoguanidine, dexamethasone, methylene blue, 1H-[1,2,4]oxadiazolo [4,3-a]quinoxalin-1-one(ODQ), indomethacin, ryanodine, tetrabutylammonium(TBA), lidocaine, procaine and 0 mM extracellular $Na^+$, but not by 2-nitro-4-carboxyphenyl-n,n-diphenylcarbamate(NCDC), lithium, nifedipine, verapamil, 0 mM extracellular $Ca^{2+}$, glibenclamide and clotrimazole. These findings suggest that xylamine could act as a vasorelaxant and direct inhibitor of arterial contraction. This vasorelaxation involves an endothelial nitric oxide (NO)/cGMP (guanosine 3',5'-cyclic monophosphate) pathway or cyclooxygenase system, and an interference with $Ca^{2+}$ release, TBA-sensitive $Ca^{2+}$-activated $K^+$ channels and $Na^+$$ channels.

• The Korean Journal of Physiology and Pharmacology
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• 제21권6호
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• pp.687-694
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• 2017

Plumbagin, a hydroxy 1,4-naphthoquinone compound from plant metabolites, exhibits anticancer, antibacterial, and antifungal activities via modulating various signaling molecules. However, its effects on vascular functions are rarely studied except in pulmonary and coronary arteries where NADPH oxidase (NOX) inhibition was suggested as a mechanism. Here we investigate the effects of plumbagin on the contractility of skeletal artery (deep femoral artery, DFA), mesenteric artery (MA) and renal artery (RA) in rats. Although plumbagin alone had no effect on the isometric tone of DFA, $1{\mu}M$ phenylephrine (PhE)-induced partial contraction was largely augmented by plumbagin (${\Delta}T_{Plum}$, 125% of 80 mM KCl-induced contraction at $1{\mu}M$). With relatively higher concentrations (>$5{\mu}M$), plumbagin induced a transient contraction followed by tonic relaxation of DFA. Similar biphasic augmentation of the PhE-induced contraction was observed in MA and RA. VAS2870 and GKT137831, specific NOX4 inhibitors, neither mimicked nor inhibited ${\Delta}T_{Plum}$ in DFA. Also, pretreatment with tiron or catalase did not affect ${\Delta}T_{Plum}$ of DFA. Under the inhibition of PhE-contraction with L-type $Ca^{2+}$ channel blocker (nifedipine, $1{\mu}M$), plumbagin still induced tonic contraction, suggesting $Ca^{2+}$-sensitization mechanism of smooth muscle. Although ${\Delta}T_{Plum}$ was consistently observed under pretreatment with Rho A-kinase inhibitor (Y27632, $1{\mu}M$), a PKC inhibitor (GF 109203X, $10{\mu}M$) largely suppressed ${\Delta}T_{Plum}$. Taken together, it is suggested that plumbagin facilitates the PKC activation in the presence of vasoactive agonists in skeletal arteries. The biphasic contractile effects on the systemic arteries should be considered in the pharmacological studies of plumbagin and 1,4-naphthoquinones.

• The Korean Journal of Physiology and Pharmacology
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• 제20권5호
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• pp.477-485
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• 2016

CG200745 is a novel inhibitor of histone deacetylases (HDACs), initially developed for treatment of various hematological and solid cancers. Because it is water-soluble, it can be administered orally. We hypothesized that the HDAC inhibitor, CG200745, attenuates cardiac hypertrophy and fibrosis in deoxycorticosterone acetate (DOCA)-induced hypertensive rats. For establishment of hypertension, 40 mg/kg of DOCA was subcutaneously injected four times weekly into Sprague-Dawley rats. All the rats used in this study including those in the sham group had been unilaterally nephrectomized and allowed free access to drinking water containing 1% NaCl. Systolic blood pressure was measured by the tail-cuff method. Blood chemistry including sodium, potassium, glucose, triglyceride, and cholesterol levels was analyzed. Sections of the heart were visualized after trichrome and hematoxylin and eosin stain. The expression of hypertrophic genes such as atrial natriuretic peptide A (Nppa) and atrial natriuretic peptide B (Nppb) in addition to fibrotic genes such as Collagen-1, Collagen-3, connective tissue growth factor (Ctgf), and Fibronectin were measured by quantitative real-time PCR (qRT-PCR). Injection of DOCA increased systolic blood pressure, heart weight, and cardiac fibrosis, which was attenuated by CG200745. Neither DOCA nor CG200745 affected body weight, vascular contraction and relaxation responses, and blood chemistry. Injection of DOCA increased expression of both hypertrophic and fibrotic genes, which was abrogated by CG200745. These results indicate that CG200745 attenuates cardiac hypertrophy and fibrosis in DOCA-induced hypertensive rats.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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• pp.601-610
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• 2003

Biotin is a water-soluble vitamin used as a skin conditioning agent and promotes the formation of intercellular lipid layers through increased lipid synthesis, which improves the skin's natural barrier function. The anti-inflammatory effects of biotin have been investigated using in vitro assay models, such as MTT assay, measurements of concentrations of nitric oxide(NO), prostaglandin E2(PGE$_2$), and inhibition rate of 5-lipoxygenase(5-LOX). In comparison with biotin, other plant extracts were tested at the same time which were kudzu vine extract, sage extract, paeonia extract, and dipotassium glycyrrhetinate. Nitric oxide is a signal molecule with functions such as neurotransmission, local vascular relaxation, and anti-inflammation in many physiological and pathological processes. NO can cause apoptosis and necrosis of target cells such as keratinocytes and is generated from L-arginine by nitric oxide synthase (NOS). Prostanoids, including prostaglandins and thromboxanes, are generated by the phospholipase $A_2$/cyclooxygenase(COX) pathway, and leukotrienes are generated by the 5-lipoxygenase pathway from arachidonic acid. Prostaglandin E2 recently have been shown to be beneficial in the resolution of tissue injury and inflammation, also has been implicated as an immunosuppressive agent and plasma levels of PGE$_2$ are elevated in patients sustaining thermal injury. Lipoxygenase metabolites from arachidonic acid have been implicated in inflammation, anti-inflammatory activity of the raw materials was evaluated in vitro by the offered inhibition of lipoxygenase.

• 한국환경생태학회지
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• 제16권1호
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• pp.104-123
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• 2002

1998년 6월부터 2000년 4월까지 모두 총 6차례에 걸쳐 축령산과 서리산 일대의 관속식물조사를 수행한 결과 모두 112과 415속 688종 1아종 116변종 12품종으로 817종류의 식물이 조사되었다. 임상은 주로 신갈나무를 비롯한 참나무류가 우점한 가운데 다양한 낙엽활엽수종이 분포하고, 잣나무, 낙엽송 조림지가 일부지역을 대표한다. 산림청 지정 희귀식물은 모두 16종류가 분포했는데. 그 중 10종류가 새롭게 확인되었으며 특히, 북방계 식물로 너도바람꽃의 분포와 주요 약용식물인 백부자, 백작약, 미치광이풀, 가시오갈피 등과 남부지방에 주로 분포하는 것으로 알려진 개족도리의 출현은 이 지역이 식물분포학상으로 매우 중요한 지역임을 알 수 있다. 특산식물은 모두 35종류로 왕느릅나무, 점현호색, 토현삼, 고려엉겅퀴 등 22종류가 새롭게 추가 되었다. 귀화식물은 모두 39종류로 확인되었는데, 이 중 30종류가 새롭게 출현한 종류이며. 주변지역에 비해 낮은 귀화율(Nl)과 높은 자연파괴도(Ul)가 나타나는 것으로 산출되었다. 대상지역은 보존가치가 많은 식물자원이 분포하고 있으나 많은 탐방객의 출입과 주변 개발 등으로 자연파괴가 가속화될 우려가 있으므로 방문객 수 제한이나 자연휴식년제를 통한 생태계 보존이 필요하다고 하겠다.

• The Korean Journal of Physiology and Pharmacology
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• 제1권6호
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• pp.769-774
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• 1997

Non-neuronal high affinity binding sites for benzodiazepines have been found in many peripheral tissues including cardiac muscle and vascular smooth muscle, and have been designated as 'peripheral benzodiazepine receptor'. Benzodiazepines have been shown to induce relaxation of the ileal, vesical, and uterine smooth muscles. However, it is still unclear about possible involvement of peripheral benzodiazepine receptor on the contractility of trachealis muscle. This study was performed to investigate the role of the peripheral benzodiazepine receptor on the contractility of canine trachealis muscle. Canine trachealis muscle strips of 15 mm long were suspended in an isolated organ bath containing 1 ml of physiological salt solution maintained at $37^{\circ}C$, and aerated with $95%\;O_2/5%\;CO_2$. Isometric myography was performed, and the results of the experiments were as follows: Ro5-4684, FGIN-1-27 and clonazepam reduced a basal tone of isolated canine trachealis muscle strip concentration dependently, relaxant actions of RoS-4684 and FGIN-1-27 were antagonized by PK11195, a peripheral benzodiazepine receptor antagonist. Flumazenil, a central type antagonist, did not antagonize the relaxant action of Peripheral type agonists. Saturation binding assay of [3H]Ro5-4864 showed a high affinity$(Kd=5.33{\pm}1.27nM,\;Bmax=\;867.3{\pm}147.2\;fmol/mg\;protein)$ binding site on the canine trachealis muscle. Ro 5-4684 suppressed the bethanechol-, 5-hydroxyoyptamine- and histamine- induced contractions. Platelet activating factor (PAF) exerted strong and prolonged contraction in trachealis muscle strip. Strong tonic contraction by PAE was attenuated by Ro 5-4684, but not by WEB 2086, a PAF antagonist. Based on these results, it is concluded that the peripheral benzodiazepine receptor mediates the inhibitory regulation of contractilty of canine trachealis muscle.

• Journal of Preventive Medicine and Public Health
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• 제32권2호
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• pp.162-169
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• 1999

Objectives: The aim of this study was to investigate the attitudes toward complementary and alternative medicine among 1,490 residents(339 households) in Suwon city. Methods: All respondents were asked about types, frequency, effects, side-effects, views, and cost of complementary or alternative medicine through a questionnaire from July 24th to 27th. Six therapies were investigated: diet; acupuncture/ massage/ chiropractic etc., mind control such as Ki/ Yoga/ spiritual therapy/ relaxation therapy etc.; nutritional supplements, cultural remedies; and Herb medications Results: The results of this survey were as follows: 35.6% of respondents had experiences with at least one or more types of complementary and alternative medicine. The average number of different types of therapies used was 3.4. More experience with various types of therapies were found among those respondents of higher education, older age group, higher income, married group, religious group than among the opposite groups of respondents. Herb medications were used most frequently(39.8%), followed by minor grains(37.9%), Ginseng(23.8%), Boshintang(21.5%), acupuncture(20.3%), Gaesojou(15.3%) Gingko nut(12.0%), mushroom(11.5%), Cupping therapy(10.2%), and black goat(0.0%). Acupuncture and Herb medications were used for treatment of hypertension the most frequently; minor grains or silkworm for treatment of diabetic mellitus; vegetables for treatment of obesity; acupuncture, Cupping Therapy, Herb medications for treatment of rheumatism; and acupuncture, Herb medications, or exercises for treatment of Cerebro Vascular Accident(CVA). The average costs of treatment were 108,000 Won for hypertension, 87,200 Won for diabetic mellitus, 16,800 Won for obesity, 68,800 Won for rheumatism, and 87,500 Won for CVA. Among 10.9% of respondents, there were 13 cases of side-effects with acupuncture, Herb medications, and Gaesojou. Among the cases of side-effects, majority was due to Herb medications. Respondents reported that Cupping Therapy was the most effective, followed by acupuncture, Ginseng, Gingko nut, Boshintang, black goat, minor grains, Gaesojou, Herb medications, vegetables, and mushroom. In response to the views of complementary and alternative medicine which they had used, they recommended minor grains first, followed by Ginseng, acupuncture, Gingko nut, Cupping Therapy, vegetables, Boshintang, black goat, mushroom and Herb medications. In contrast, they did not recommend Herb medications, acupuncture, nor Gaesojou. Conclusions: These findings indicate that many people use various complementary and alternative medicine without any guidelines for treatment of serious chronic diseases not even to invigorate themselves. It is, therefore, suggested that medical doctors or scientists verify the true effects or side-effects from the most common complementary or alternative therapies through experiments. Also medical doctors should provide a comfortable atmosphere for discussion among doctors and patients who would like to try these therapies.

• Journal of Ginseng Research
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• 제26권1호
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• pp.1-5
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• 2002

고려홍삼은 혈압강하효과가 있음이 잘 알려져 있다. 이에 백서장간막이 동맥의 저항혈관에서 고려홍삼 사포닌 성분의 혈관 이완기전을 규명하고자 내경이 150$\mu\textrm{m}$이하의 작은 혈관을 이요하여 여러 실험 조건에서 장력의 변화를 측정하여 다음과 같은 결과를 얻었다. 고려홍삼 사포닌 성분은 농도 의존적으로 (0.01mg/$m\ell$~1mg/$m\ell$) 혈관 평활근을 이완시켰으며 내피세포를 제거한 상태에서도 혈관의 이완효과는 지속되었다. A23187 이나 phorbol 12, 13-dibutyrate 에 의한 수축에서는 고려홍삼 사포닌에 의한 혈관의 이완효과가 나타나지 않았다. 고려홍삼 사포닌에 의한 혈관이완효과는 실험용액의 $K^{+}$ 농도를 증가시키면 감소되었으며 각종 $K^{+}$이 온통로 억제제인 tetaethylammonium, glybenclamide, 4-aminopyridine 및 BaCl$_2$를 전처치한 결과 BaCl$_2$에 의해서만 농도에 의존적으로 고려홍삼 사포닌에 의한 혈관이완작용이 억제되었다. 이상의 실험결과로부터 고려홍삼 사포닌은 장간막 동맥의 저항혈관에서 $K^{+}$의 유출을 증가시켜 혈관평활근을 이완시키며 $Ba^{2+}$에 의하여 차단되는 $K^{+}$ 이온통로가 고려홍삼 사포닌에 의한 혈관이완작용에 관여함을 알 수 있었다.

• 약학회지
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• 제41권6호
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• pp.802-816
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• 1997

In order to investigate the pharmacological properties of New Woohwangehungsimwon Pill (NWCH). Effects of Woohwangehungsimwon Pill (WCH) and NWCH were compared using various experimental models. In isolated rat aorta, NWCH and WCH showed the relaxation of blood vessels in maximum contractile response to phenylephrine ($10^{-6}$M) without regard to endothelium containing or denuded rings of the rat aorta. Furthermore, the presence of the inhibitors of NO synthase and guanylate cyclase did not affect significantly the relaxative effects of NWCH and WCH. NWCH and WCH inhibited the vascular contractions induced by acethylcholine, prostaglandin endoperoxide or peroxide in a dose-dependent manner. In conscious spontaneously hypertensive rats(SHRs), NWCH and WCH decreased significantly heart rate. These, at high doses, had a negative inotropic effect that was a decrease of LVDP and (-dp/dt)/(+dp/dt) in the isolated perfused rat hearts, and also decreased the contractile force and heart rate in the isolated rat right atria. In excised guinea-pig papillary muscle, these had no effects on parameters of action potential at low doses, whereas inhibited the cardiac, contractility at high doses. Furthermore, these had a significant inhibitory effects on heart acceleration in normotensive rats and SHRs. These results suggested that NWCH and WCH have weak cardiovascular effects, and that there is no significant differences between two preparations.

• The Korean Journal of Physiology and Pharmacology
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• 제2권3호
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• pp.323-330
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• 1998

Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ?${\alpha}$-adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$, $5.99{\pm}1.16$ and $5.57{\pm}0.34$, respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$, respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ?${\beta}-adrenoceptors$. YS 49, YS 51, and higenamine showed ?${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$, respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$. Thus, these chemicals may be useful in the treatment of congestive heart failure.