• Applied Biological Chemistry
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• 제25권3호
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• pp.155-160
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• 1982

Claviceps spp.는 tryptophan함유배지에서 적갈색 색소를 형성한다. D.L.-tryptophan$[side\;chain-3^{14}C]$를 배지에 첨가하였을 때 $^{14}C-labeled$ pigment와 constant specific radioactivity를 갖는 5-hydroxytryptophan을 재결정 분리하였다. 동시에 $^{14}C-labeled$ 5-hydroxytryptophan으로 같은 실험을 행한 결과, tryptophan 보다 4배 이상, 색소물질로 주입되는 것을 관찰할 수 있었다. 한편, UV-spectrum 및 fluorometric analysis등에 의하여 배지중 5-hydroxytryptophan이 생합성되는 것을 확인할 수 있었다. tryptophan에서 출발하는 또 하나의 ergot pigment 생합성경로는 곰팡이 생육배지중에서 40pmde/mg protein 농도의 cytochrome p-450을 분리 정제할 수 있어 tryptophan이 hydroxylation되어 5-hydroytryptophan으로 전환하는 효소학적 반응으로 검정되어 hydroxylation반응이 우선하는 기작에 의한 것임을 알 수 있다.

• 생약학회지
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• 제26권4호
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• pp.355-359
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• 1995

To find serotonin(5-hydroxytryptamine, 5-HT)-antagonizing activities in traditional herbal drugs, crude extracts from 66 kinds of traditional herbal drugs were randomly screened for inhibitory effects on 5-hydroxytryptophan(HTP)-induced diarrhea in mice. Intraperitoneal injection of 5-HTP(2.5 mg/kg) induced diarrhea in 92% of mice, when observed from 10 to 15 min after injection. Crude extracts(2 g/kg) from 66 kinds of traditional herbal drugs were orally pretreated for 1 h before 5-HTP injection. Of the 66 herbal drugs screened, Ephedrae Herba(麻黃), Cimicifugae Rhizoma(升麻), Anisi stellati Fructus(八角茴香), Aurantii Fructus(枳實), Polygalae Radix(遠志) showed the most potent inhibiting activities against 5-HTP(2.5 mg/kg)-induced diarrhea in mice. There are at least 3 possible mechanisms that would be responsible for the inhibitory effect of crude extracts on 5-HTP-induced diarrhea; 1) crude extract-induced inhibition of the activity of aromatic aminoacid decarboxylase catalyzing the conversion of 5-HTP to 5-HT, 2) crude extract-induced blockade of 5-HT receptor(s) in the gastrointestinal tract responsible for 5-HTP-induced diarrhea, 3) crude extract-induced inhibition of gastrointestinal activity, irrespective of 5-HT system. The exact mechanisms and molecules, responsible for the inhibitory effect of crude extracts on 5-HTP-induced diarrhea remain to be clarified.

• 한국축산식품학회지
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• 제37권5호
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• pp.646-653
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• 2017

Alcalase hydrolysis of liquid egg white was used to produce 5-hydroxytryptophan (HTP) under various conditions and investigate the sleep-potentiating activity of liquid egg white hydrolysate (LEH) on pentobarbital-induced sleep. Alcalase hydrolysis yielded the highest content of 5-HTP ($13.50{\mu}g/mL$), while neutrase hydrolysis showed the lowest 5-HTP content ($5.23{\mu}g/mL$). The liquid egg white to water ratio (1:1) was optimal for the production of 5-HTP with high amino-nitrogen (A-N) content and degree of hydrolysis. The 5-HTP, amino-nitrogen, and degree of hydrolysis increased until 24 h of hydrolysis and slightly increased thereafter during hydrolysis with 2% and 5% enzyme addition. 5-HTP administration at doses of 6 and 9 mg/kg significantly increased sleep duration and decreased sleep latency time compared to that in the control (p<0.05). LEH (150 mg/mouse), which was equivalent to 5-HTP at 6 mg/kg, significantly decreased sleep latency time and increased sleep duration time compared to that in the control (p<0.05). Oral administration of LEH showed sleep-potentiating effects because of 5-HTP. The sleep-potentiating activity of LEH may have occurred through 5-HTP in our pentobarbital-induced sleep model. LEH may be a valuable alternative to sleep enhancement and may be used as a sleep-potentiating agent.

• Biomolecules & Therapeutics
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• 제31권4호
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• pp.402-410
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• 2023

Long-term administration of levodopa (L-DOPA) to patients with Parkinson's disease (PD) commonly results in involuntary dyskinetic movements, as is known for L-DOPA-induced dyskinesia (LID). 5-Hydroxytryptophan (5-HTP) has recently been shown to alleviate LID; however, no biochemical alterations to aberrant excitatory conditions have been revealed yet. In the present study, we aimed to confirm its anti-dyskinetic effect and to discover the unknown molecular mechanisms of action of 5-HTP in LID. We made an LID-induced mouse model through chronic L-DOPA treatment to 6-hydroxydopamine-induced hemi-parkinsonian mice and then administered 5-HTP 60 mg/kg for 15 days orally to LID-induced mice. In addition, we performed behavioral tests and analyzed the histological alterations in the lesioned part of the striatum (ST). Our results showed that 5-HTP significantly suppressed all types of dyskinetic movements (axial, limb, orolingual and locomotive) and its effects were similar to those of amantadine, the only approved drug by Food and Drug Administration. Moreover, 5-HTP did not affect the efficacy of L-DOPA on PD motor manifestations. From a molecular perspective, 5-HTP treatment significantly decreased phosphorylated CREB and ΔFosB expression, commonly known as downstream factors, increased in LID conditions. Furthermore, we found that the effects of 5-HTP were not mediated by dopamine1 receptor (D1)/DARPP32/ERK signaling, but regulated by AKT/mTOR/S6K signaling, which showed different mechanisms with amantadine in the denervated ST. Taken together, 5-HTP alleviates LID by regulating the hyperactivated striatal AKT/mTOR/S6K and CREB/ΔFosB signaling.

• Journal of Pharmaceutical Investigation
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• 제16권4호
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• pp.135-138
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• 1986

Ginseng total saponins(GS), protopanaxadiol saponins(PD) and protopanaxadiol saponins(PT) antagonized the analgesia in mice induced by morphine. The administrations of 2,4-dihydroxyphenylalanine, and 5-hydroxytryptophan reduced the GS, PD and PT antagonisms of morphine analgesia. Possible mechanisms involved in the antagonistic actions of GS, PD and PT on morphine analgesia were described.

• Journal of Ginseng Research
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• 제11권2호
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• pp.123-129
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• 1987

Antagonisms of the analgesic effect of morphine in mice by ginsenoside Rbl, Rb2, Rgl and Re were investigated in these experiments. These ginsenosides antagonized the analgesic effect induced by morphine in mice and the administration of 2,4-dihy-droxyphenylalanine or 5-hydroxytryptophan reduced the antagonisms of morphine analgesia by the ginsenosides. Possible mechanisms involved in the antagonistic actions of the ginsenosides on morphine analgesia were described.

• Bulletin of the Korean Chemical Society
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• 제13권3호
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• pp.290-296
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• 1992

Four plausible precursors (21, 22, 24, and 25), just prior to formation of the oxathiazepine ring in eudistomin, were synthesized by the Pictet-Spengler condensation of N-hydroxytryptamine (15) or N-hydroxytryptophan ester (19) with cysteinal derivatives (5 and 10). In the case of the parent compound (21), one of these four precursors, treatment with dihalomethane in the presence of a phase transfer catalyst gave an eudistomin analogue (26) having the oxathiazepine ring in 35-50% yield.

• Journal of Genetic Medicine
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• 제6권2호
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• pp.170-174
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• 2009

저자들은 생후 3개월에 전형적인 페닐케톤뇨증으로 진단받고 식사요법을 유지하였으나 지연된 발달 소견 및 지능 저하를 보이고 경련 증상이 있었던 9세 남자 환아에서 효소 검사와 유전자분석으로 dihydropterine reductase (DHPR) 결핍증을 진단하였다. 그리고 $BH_4$, 신경전달물질 전구체 투여 및 엽산 보충으로 DHPR 결핍증을 치료한 1례를 경험하였기에 문헌고찰과 함께 보고한다.

• 약학회지
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• 제38권6호
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• pp.791-794
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• 1994

Sixteen kinds of naturally occurring phenolic compounds including 5 stilbenes, 7 flavonoids and 4 anthraquinones were examined in the inhibitory activity against rat liver AADC(aromatic L-amino acid decarboxylase) in vitro, using 5-hydroxytryptophan as a substrate. Three hydroxystilbenes, resveratrol 1, rhapontigenin 3 and piceatanol 5, which were known to be monoamine oxidase A inhibitors, exhibited a significant inhibition against AADC($IC_{50}$=20, 8 and $5\;{\mu}M$, respectively). By the comparison of the activity of each phenolic compound, it was suggested that the 3',4'-dihydroxyphenyl group of stilbenes or flavones was the best pharmacophore for the AADC inhibitory activity.

• 한국동물학회지
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• 제8권2호
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• pp.85-88
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• 1965

There are few papers on the biosynthesis of serotonin in the enterochromaffin cell in the pancrease. The present studies were performed to clarify this problem by use of autoradiography in the auinea pig injected of 5-HTP-H3 in dose of 1 vc/g. body weight, The appearance of the above mentioned cells in the pancreas of the rabbit was also studied morphologically. The results are as follows ; 1. Enterochromaffin cells were found in the epithelia of all the pancreating ducts and a few acini of normal male rabbit and most numerous in the intramural pancreatic ducts. 2. The redioautographic silver grains overling the enterochormaffin cells in the guinea pig pancreas are considered to be due to the newly synthesized radioactive serotonin in the cells from injected 5-HTP-H3.