• 생약학회지
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• 제29권3호
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• pp.187-192
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• 1998

The ethyl acetate fraction of Uncariae Ramulus et Uncus, which showed anticonvulsant effects against pentylenetetrazole (PTZ) treated mice, were subjected to column chromatography to isolate ursolic acid and hyperin from active eluate. Hyperin decreased the elevated activities of GABA-T and xanthine oxidase and lipid peroxide level dose-dependently in PTZ treated mice brain tissue in vitro, but no effect on superoxide dismutase activity. The effects on such enzyme and component seemed to be related with biosynthesis or metabolism of neurotransmitters.

• 약학회지
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• 제54권1호
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• pp.1-7
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• 2010

Valerian (Valeriana officinalis L.) is a perennial that has been used for medicinal purposes from the ancient times and valerian preparations including root and rhizome extracts are known to possess a variety of biological activities such as anticonvulsant, antidepressant, sleep aid, tranquilizer, and anti-HIV activities. Main components of the extracts were classified according to the structural features. Importantly, one of the main components, isovaleramide, has drawn our attention due to the concise structure, broad spectrum, and low toxicities. The general aspects including generation of this interesting molecule, a variety of activities, pharmacokinetic properties, derivatization, and fusion with other known drugs were described. Isovaleramide has been isolated from valerian probably as an isolation artifact after treatment of ammonia to prepare ammoniated tincture, and is known to exhibit anticonvulsant, anxiolytic, sedative, and sleep aid activities without distinct side effects such as excessive sedation and decreasing muscle tone. It was also found to be well absorbed into the circulation system without specific cytotoxicity and genotoxicity. The derivatives of isovaleramide, valpromide, valrocemide and valnoctamide were also briefly discussed.

• Biomolecules & Therapeutics
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• 제28권2호
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• pp.137-144
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• 2020

Epilepsy is a brain disorder that affects millions of people worldwide and is usually managed using currently available antiepileptic drugs, which result in adverse effects and are ineffective in approximately 20-25% of patients. Thus, there is growing interest in the development of new antiepileptic drugs with fewer side effects. In a previous study, we showed that a Rehmannia glutinosa (RG) water extract has protective effects against electroshock- and pentylenetetrazol (PTZ)-induced seizures, with fewer side effects. In this study, the objective was to identify the RG components that are responsible for its anticonvulsant effects. Initially, a number of RG components (aucubin, acteoside, catalpol, and mannitol) were screened, and the anticonvulsant effects of different doses of catalpol, mannitol, and their combination on electroshock- and chemically (PTZ or strychnine)-induced seizures in mice, were further assessed. Gamma-aminobutyric acid (GABA) receptor binding assay and electroencephalography (EEG) analysis were conducted to identify the potential underlying drug mechanism. Additionally, treated mice were tested using open-field and rotarod tests. Catalpol, mannitol, and their combination increased threshold against electroshock-induced seizures, and decreased the percentage of seizure responses induced by PTZ, a GABA antagonist. GABA receptor binding assay results revealed that catalpol and mannitol are associated with GABA receptor activity, and EEG analysis provided evidence that catalpol and mannitol have anticonvulsant effects against PTZ-induced seizures. In summary, our results indicate that catalpol and mannitol have anticonvulsant properties, and may mediate the protective effects of RG against seizures.

• 대한화학회지
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• 제54권1호
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• pp.158-164
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• 2010

• Archives of Pharmacal Research
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• 제23권4호
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• pp.344-348
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• 2000

80% Aqueous MeOH extracts from the wood of Caesalpinia sappan, which showed remarkable anticonvulsant activity, were fractionated using EtOAc, n-BuOH, and $H_2$O. Among them, the EtOAc fraction significantly inhibited the activities of two GABA degradative enzymes, succinic semialdehyde dehydrogenase (SSADH) and succinic semialdehyde reductase (SSAR). Repeated column chromatographies for the fraction guided by activity test led to the isolation of the two active principal components. Their chemical structures were determined to be sappanchalcone and brazilin based on spectral data. The pure compounds, sappanchalcone (1) and brazilin (2), inactivated the SSAR activities in a dose dependent manner, whereas SSADH was inhibited partially by sappanchalcone and not by brazilin.

• Journal of Hospice and Palliative Care
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• 제1권1호
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• pp.65-68
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• 1998

The neuropathic pains are not well controlled by common analgesics and opioid drugs in terminal cancer patients. The types of these pains are divided within the two cages, one is due to continuous central sensitization and the other is due to paroxymal peripheral sensitization. The mechanism of continuous central sensitization is the activity of dorsal horn neurones that are activated by C-fiber input. The tricyclic antidepressants, non-tricyclic antidepressants, and oral local anaesthesia probably produce analgesic effects in neuropathic pains through suppression of this activity. The mechanism of paroxymal peripheral sensitization is the hyper-excitability of peripheral neurones. The neuropathic pains due to peripheral sensitization respond relatively the anticonvulsants and baclofen that stabilize membranes and suppress paroxymal electrical discharge. The patients was a 38-year-old female who complained of hyperthemia on upper right extremity. The symptom of this patient was improved with anticonvulsant(dilantin 600mg).

• 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.

• The Korean Journal of Pain
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• 제13권1호
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• pp.101-104
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• 2000

Since conventional analgesics have showed limited therapertic value in the treatment of painful neuropathy, the new anticonvulsant gabapentin, has been tried and turned out to be effective and safe in the treatment for various forms of neuropathic pain. The basic pathophysiology of neuropathic pains is abnormal neuronal hyperactivity similar to epileptic seizures. Therefore, we could expect that neuropathic pain would be suppressed by anticonvulsants which inhibit abnormal excessive neuronal output and nerve conduction. This report include effective pain relief in four cases of neuropathic pain with gabapentin without any significant complications.

• Journal of Applied Biological Chemistry
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• 제48권1호
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• pp.32-34
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• 2005

Arils of Euporia longana L. was extracted with 80% aqueous MeOH and partitioned successively with EtOAc, n-BuOH and $H_2O$. From the n-BuOH fraction, furan compound was isolated through silica gel column chromatography. The results of physico-chemical data including NMR, MS and IR revealed the compound to be 5-(hydroxymethyl)-2-furfuraldehyde. This compound stimulated GDH I activity by $19.2{\pm}0.6$, $41.2{\pm}0.9$, $68.4{\pm}1.1$, $80.3{\pm}0.9$ and $85.9{\pm}1.6%$ at in vitro concentrations of 0.005, 0.008, 0.02 and 0.03 %, respectively.

• Pediatric Gastroenterology, Hepatology & Nutrition
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• 제10권2호
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• pp.202-205
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• 2007

저자들은 6세 된 남아에서 4년간의 반복적이고, 발작적인 복통의 원인을 규명하던 중 만성 복통의 타 기질적 질환들이 배제되고, 뇌파 검사의 이상 소견과 함께 항경련제의 사용에 증상의 극적인 소실을 보여 복성 간질로 진단된 1예를 경험하고 문헌 고찰과 함께 보고하는 바이다.