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Acetylcholinesterase에 대한 (1,3-Dioxolan-2-yl 및 Dioxan-2-yl)methylaminium 유도체의 저해 작용
피택산(Taek San Phi),김윤배(Yun Bae Kim),김지천(Jee Cheon Kim),조영(Young Cho),석대은(Dai Eun Sok),차승희(Seung Hee Cha),서원준(Won Jun Seo) 대한약학회 1994 약학회지 Vol.38 No.5
We examined the inhibitory activity of (1,3-dioxolan-2-yl and 1,3-dioxan-2-yl)methylaminium derivatives(A; 1-8) against acetylcholinesterase. Derivatives of six-membered 1,3-dioxane exhibited more potent inhibitory effect than corresponding 5-membered 1,3-dioxolanes. The presence of methyl group at C4 position of dioxane ring was effective to increase the inhibitory potency of heterocyclic analogues. The activity of N-phenacyl-aminiums was greater than that of N,N,N-trimethyl-aminiums. In general, the terminal methyl group on 1,3-dioxane ring and the phenacyl group in ammonium compound A were assumed to be important factors to enhance the inhibitory action.
대두 lipoxygenase 에 의한 아라키돈산으로부터 lipoxins 으로서 전환
석대은,피택산,정창희,정윤수,강정부 ( Dai Eun Sok,Taek San Phi,Chang Hee Jung,Yun Su Chung,Jung Bu Kang ) 생화학분자생물학회 1988 BMB Reports Vol.21 No.2
The exposure of arachidonic acid to soybean lipoxygenase led to the formation of polar products showing intense absorption at 300-301 nm. These products were found to be lipoxin A and B isomers, based on UV spectrum, HPLC and GC/MS analyses. This method, convenient to prepare hundreds of micrograms of lipoxin A and B isomers, would be useful for the study on the biosynthesis and the biological activity of lipoxins.
Soybean Lipoxygenase-Catalyzed Conversion of Arachidonic Acid into Lipoxins
석대은,피택산,정창희,정윤수,강정부,Sok, Dai-Eun,Phi, Taek-San,Jung, Chang-Hee,Chung, Yun-Su,Kang, Jung-Bu 생화학분자생물학회 1988 한국생화학회지 Vol.21 No.2
아라키돈산에 대두 lipoxygenase를 작용시켰을때, 300-301 nm에서 강한 흡수를 나타내는 극성 물질들이 형성되었다. 이 물질들을 UV스펙트럼, HPLC, GC/MS에 의한 분석 결과, lipoxin A와 lipoxin B 이성체로 확인되었다. 이 방법은 수백 마이크로그람의 liposin A 및 B 이성체를 얻는데 편리한 것으로, lipoxins의 생합성과 생리적 활성을 연구하는데 유용할 것으로 사료된다. The exposure of arachidonic acid to soybean lipoxygenase led to the formation of polar products showing intense absorption at 300-301 nm. These products were found to be lipoxin A and B isomers, based on UV spectrum, HPLC and GC/MS analyses. This method, convenient to prepare hundreds of micrograms of lipoxin A and B isomers, would be useful for the study on the biosynthesis and the biological activity of lipoxins.
Physostigmine과 procyclidine으로 구성된 유기인제 중독 예방용 패취제의 약물농도에 따른 피부자극성 및 재결정화 경향 연구
김윤배(Yun-Bae Kim),피택산(Taek-San Phi),김왕수(Wang-Soo Kim),조영(Young Cho),서원준(Won-Jun Seo),최승주(Seung-Ju Choi),천기철(Ki-Cheol Cheon),허경행(Gyeung-Haeng Hur),연규백(Gyu-Baek Yeon) 한국실험동물학회 2004 한국실험동물학회 학술발표대회 논문집 Vol.2004 No.-
Skin irritation potencies of novel combinational transdermal patches, composed of various concentrations of physostigmine and procyclidine for the prophylaxis of organophosphate poisoning, were investigated in rabbits and human volunteers. In rabbits, procyclidine, but not 25% physostigmine, induced skin erythema in concentration- and attachment duration-dependent manners, in which moderate to severe redness was produced by attachment with patches containing 8% 01' higher concentrations of procyclidine over 3 days, although skin lesions including edema was not induced by patches containing procyclidine up to 10%. Interestingly, the erythemata caused by procyclidine were reduced by combination with physostigmine, and further by hydrocortisone, and the reactions were rapidly disappeared following detachment of the patches. The skin reactions induced by combinational patches in men were much similar to those in rabbits, although slight and transient edema, itching and pain were induced by patches containing 10% procyclidine, Whereas, patches containing pmcyclidine up to 6% in combination with physostigmine (15%) in the presence of hydrocortisone induced negligible redness, leading to scores lower than 1.0. Separately, only patches with a high concentration (10%) of procyclidine recrystallized from 3 weeks of storage at 4℃ and 23℃, but not at 37℃, reaching 96% after 25 weeks, although the recrystallization rate was greatly lowered by addition of hydrocortisone, Based on the skin irritation and recrystallization profiles, in addition to previous skin penetration and blood concentration analyses, we selected a combinational patch containing 1.5% physostigmine +6% procyclidine +0.5% hydrocortisone as a transient composition for the follow-up non-clinical toxicity studies.
Physostigmine 과 Procyclidine 으로 구성된 복합예방제의 유기인제 해독효능
허경행(Gyeung Haeng Hur),천기철(Ki Cheol Cheon),피택산(Taek San Phi),김지천(Jee Cheon Kim),홍대식(Dea Sik Hong),박훈(Hoon Park),정창희(Chang Hee Jung),이용한(Yong Han Lee),김윤배(Yun Bae Kim) 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.1
N/A Antidotal efficacy of combinational prophylactics composed of physostigmine plus procyclidine, alone or in combination with antidotes such as atropine plus 2-pralidoxime or atropine plus HI-6, was evaluated in rats. Physostigmine (0.1 mg/kg) plus procyclidine (3 mg/kg), pretreated subcutaneously 30 min prior to subcutaneous exposure to organophosphates of militarily importance, exerted protection ratios of 7.2, 6.5, 4.0, 2.9 and 8.0 fold for tabun, sarin, soman, cyclosarin and V-agent, respectively. In comparison, low effects (1.7 fold for soman and 1.3 fold for cyclosarin) were achieved with the traditional antidotes atropine (17.4 mg/ kg) plus 2-pralidoxime (30 mg/kg) administered intramuscularly immediately after organophosphate, in contrast to high effects (5.5 fold for soman and 160.0 fold for cyclosarin) with atropine (17.4 mg/kg) plus HI-6 (125 mg/kg), although the protection ratio markedly decreased when treatment of antidotes was delayed. Noteworthy, the combinational prophylactics markedly potentiated the effects of antidotes to higher than 5.0 fold in all cases. In addition, the combinational prophylactics fully prevented the seizures and excitotoxic brain injuries induced by a high dose (100 mg/kg, 1.3 LD_(50)) of soman. Taken together, it is suggested that the prophylactics composed of physostigmine and procyclidine, in combination with posttreatment antidotes, could be a promising regimen for the prevention of lethality, seizures and brain injuries induced by organophosphates possessing diverse properties.
Physostigmine과 procyclidine으로 구성된 유기인제 중독 복합예방제에 대한 4주 반복투여 독성평가
이종성(Jong-Sung Lee),황재식(Zai-Zhi Huang),강현구(Hyun-Gu Kang),박선희(Sun-Hee Park),박철범(Cheol-Beom Park),박종일(Jong-Il Park),김왕수(Wang-Soo Kim),피택산(Taek-San Phi),최은경(Ehn-Kyoung Choi),황석연(Seock-Yeon Hwang),강종구(Jong 한국실험동물학회 2003 Laboratory Animal Research Vol.19 No.4
Physostigmine과 procyclidine으로 구성된 유기인제 중독 복합예방제에 대한 2주 반복투여 용량설정시험
황재식(Zai-Zhi Huang),강현구(Hyun-Gu Kang),박선희(Sun-Hee Park),강성귀(Seong-kwi Kang),이종성(Jong-Sung Lee),박종일(Jong-Il Park),김왕수(Wang-Soo Kim),피택산(Taek-San Phi),황석연(Seok-Yeon Hwang),강종구(Jong-Koo Kang),김윤배(Yun-Bae 한국실험동물학회 2003 Laboratory Animal Research Vol.19 No.4
피리도스티그민 정제의 함량 측정을 위한 HPLC 분석법
피택산,조영,석대은,차승희,정윤수 한국약제학회 1991 Journal of Pharmaceutical Investigation Vol.21 No.3
A reverse-phase, ion-pair high performance liquid chromatographic (HPLC) method for the simultaneous quantative determination of pyridostigmine and its hydrolytic product, 3-hydroxy-N-methyl-pyridinium (HMP), is described. The assay of pyridostigmine and HMP was linear in the range of amount from 24 to 60 ㎎/tablet and from 2.4 to 12.0 ㎎/tablet, respectively, with coefficient of variation (C.V.) of 0.05-0.12% (n=7) and 0.25-0.52% (n=5), respectively, and applicable conveniently even in the case of the mixture of pyridostigmine and HMP. Meanwhile, the conventional UV method gave inaccurate results for the aged pyridostigmine tablets. In the extraction of pyridostigmine from tablets prior to be assayed by HPLC, methanol was found to be more effective than ethanol or distilled water. Multiple extraction (four times) with methanol resulted in the full recovery of pyridostigmine, whereas ethanol gave 95% recovery even after four times extraction. Based on these results, the present method would be very useful for the accurate determination of pyridostigmine in the aged pyridostigmine tablets.