• Bulletin of the Korean Chemical Society
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• 제33권8호
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• pp.2597-2602
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• 2012

Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.

• 약학회지
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• 제31권1호
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• pp.19-24
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• 1987

In order to find out the pharmacologically active but less toxic compounds than piperine, the actions of several amide derivatives of 5-phenyl-2, 4-pentadienoic acid on the CNS depressant activities were examined. The nine amide derivatives were investigated by using ICR mice as an experimental amimals on acute toxicities, anticonvulsant, sedative, analgesic and antipyretic effects. In the case of acute toxicities, all derivatives were weaker than piperine except compound III. Compound I showed strong anticonvulsant activity. On the other hand, compound I, III and IV significantly prolonged the sleeping time induced by hexobarbital in mice. Compound I, III and IV exhibited better analgesic effect than aspirin while compound II, V, VII and IX showed similar antipyretic activity to aspirin.

• Advances in Traditional Medicine
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• 제8권3호
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• pp.215-221
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• 2008

In this present study Indian traditional Ayurvedic herbal formulation Amritaristo has been studied to assess the general pharmacological effect on mice. The drug showed no significant activity on the neuropharmacological test models experimented. The increased pentobarbital sleeping time was considered related with hepatic metabolism of pentobarbital. The formulation exhibited a non-significant reduction of gastrointestinal motility, and devoid of any acute diuretic activity. The tested drug revealed antidiarrhoeal activity on castor oil-induced model, whereas on magnesium sulphate-induced model no effect was observed.

• Advances in Traditional Medicine
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• 제8권4호
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• pp.448-451
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• 2008

Picrorhiza kurrooa Royle. is a well known medicinal plant among the indigenous medical practitioners of India. Present study is the first time to report the activity on the central nervous system. Preliminary study of the hot water extract showed significant depressant activity on the hole board test as evidenced from the ambulation and head dipping scores. The extract showed better activity compared to diazepam on the duration of pentobarbital induced sleeping time.

• Archives of Pharmacal Research
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• 제11권4호
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• pp.301-307
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• 1988

Relationship between the maintenance of hypertension and central serotonergic nervous system activity in opontaneously hypertensive rats (SHR) was studied. Serotonin turnover-rates were measured in 5 brain areas as an index of serotonergic neuronal activity and compared at the ages of 14 weeks in two types of animals; (1) spontaneously hypertensive rats (SHR) (2) normotensive wistar kyoto rats (WKY). In 14-week old SHR, central serotonin turnover rate was significantly lower in telencephalon, hypothalamus/thalamus and midbrain than normotensive rat, but significantly higher in cerebellum. There were no significant differences between serotonin turnover rate in pons/medulla of SHR and that of normotensive rat. THese data suggest that the abnormally lower turnover rates of serotonin in telencephalon, hypothalamus/thalamus and midbrain may be one of the underlying neuronal factors for manifestation of hypertension in SHR.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.73-73
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• 1995

We investigated the effect of derivatized phospholipid, P-pyridoxyl dipalmiuylphosphatidylethanolamine (P-pyr-DPPE), on the catalytic activity of purified porcine brain glutamate decarboxylase(GAD) which catalyzes the synthesis of GABA known as major inhibitory neurotransmitter in CNS. When the P-pyr-DPPE was incorporated into dipalmitdylphosphatidylcholine(DPPC) or phosphatidylserine(PS) vesicles, these vesicles enhanced the catalytic activity of GAD. P-pyr-DPPE also interacted with apoglutamate decarboxylase(apoGAD) and produced the free pyridoxal-5-phosphate(PLP) which is the natural cofactor of GAD. This result indicated that apoGAD catalyzed the cleavage reaction of the P-pyridoxyl moiety of the derivatized phopholipid to generate free PLP, and then free PLP bound to the apoGAD resulting in restroration of the catalytic activity of the enzyme.

• Animal cells and systems
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• 제9권2호
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• pp.101-105
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• 2005

[ ${\beta}ig-h3$ ] is a secretory protein that is induced by $TGF-{\beta}$ and implicated in various disease conditions including fibrosis. We have previously reported that ${\beta}ig-h3$ expression is implicated in astrocyte response to brain injury. In this study, we further investigated potential roles of ${\beta}ig-h3$ protein in the injured central nervous system (CNS). We specifically assessed whether the treatment of microglial cells with ${\beta}ig-h3$ can regulate microglial activity. Microglial cells are the prime effector cells in CNS immune and inflammatory responses. When activated, they produce a number of inflammatory mediators, which can promote neuronal injury. We prepared conditioned medium from the stable CHO cell line transfected with human ${\beta}ig-h3$ cDNA. We then examined the effects of the conditioned medium on the LPS- or $IFN-{\gamma}-mediated$ induction of proinflammatory molecules in microglial cells. Preincubation with the conditioned medium significantly attenuated LPS-mediated upregulation of $TNF-{\alpha},\;IL-1{\beta}$, iNOS and COX-2 mRNA expression in BV2 murine microglial cells. It also reduced $IFN-{\gamma}-mediated$ upregulation of $TNF-{\alpha}$ and COX-2 mRNA expression but not iNOS mRNA expression. Assays of nitric oxide release correlated with the mRNA data, which showed selective inhibition of LPS-mediated nitric oxide production. Although the regulatory mechanisms need to be further investigated, these results suggest that astrocyte-derived ${\beta}ig-h3$ may contribute to protection of the CNS from immune-mediated damage via controlling microglial inflammatory responses.

• 대한핵의학회지
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• 제38권2호
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• pp.161-170
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• 2004

분자영상은 살아있는 개체의 몸 속에서 일어나는 생물학적 반응이나 특정한 표적분자를 비관혈적이며 반복적으로 영상화하는 기술이다. 이를 위해서는 두 가지 기본 요소가 요구되는 바 하나는 관심 생물현상에 의해 농도나 분광특성이 변하는 분자영상용 추적자이며 다른 하나는 이런 추적자를 모니터링하는 장비이다. 분자 핵의학 영상기술은 이제 신경과학분야에서도 활발히 적용되고 있으며 신경관련 기초연구나 뇌질환 관련 신약개발에 이미 중요한 역할을 하고 있다. 최근에는 살아있는 개체에서 약제 투여가 뇌에 미치는 약물학적, 생리적 영향을 조사하는 데에도 이용되고 있다. 다가오는 미래에는 각종 뇌질환에서 특이적 표적을 공략하는 새로운 분자치료가 개발되어 뇌질환 치료에 혁명적인 변화를 가져올 것으로 예상되고 있다. 그 예로, 파킨슨씨 병과 같은 퇴행성 신경질환에 줄기세포를 이용한 자가수선, 신경보호, 약물분비 치료, 성장인자와의 병행치료 등이 개발되고, 유전자 치료도 이용될 것으로 보인다. 신경 분자 핵의학 영상은 이와 같은 새로운 뇌질환 치료기술의 개발에 있어서 뇌 안에서 일어나는 분자수준의 변화를 실시간으로 모니터링함으로써 관련연구에 크게 기여할 것으로 기대된다.

• Applied Biological Chemistry
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• 제41권4호
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• pp.246-250
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• 1998

The cytotoxic activity of methanol extracts of 25 leguminous seeds in vitro was evaluated by sulforhodamine B assay, using the five human solid A549 lung, SK-OV-2 ovarian, SK-MEL-2 melanoma, XF-498 CNS and HCT-15 colon tumor cell lines. The responses varied with both cell line arid leguminous seed used. Extracts of Canavalia lineata and Glycine soja revealed potent cytotoxic activity against A549 arid SK-MEL-2 cell lines. Moderate activity was observed in the extracts of Cassia obtusifolia and Glyeine max var. chungtae, and C. lineata and Vigna angulasis against SK-MEL-2 and HCT-15 cell lines, respectively. The other seed extracts were ineffective against model tumor cell lines. Because of their potent cytotoxic activities, the activity of each solvent fraction from C. lineata and G. soja was determined and the potent activity was produced from their chloroform fractions. As a naturally occurring therapeutic agent, leguminous seeds described could be useful for developing new types of anti-tumor agents.

• 한국생물물리학회:학술대회논문집
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• 한국생물물리학회 1998년도 학술발표회
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• pp.14-14
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• 1998

Mammalian brian contains substantial amounts of chelatable zinc in presynaptic vesicles of certain glutamatergic terminals. The synaptic zinc is released with intense neuronal activity, suggesting its role in synaptic transmission. However, in pathological conditions, zinc may get released too excessively, which may contribute to neuronal death as shown in cortical cultures.(omitted)