• 제목/요약/키워드: active agent

검색결과 779건 처리시간 0.03초

Taxol 유도체들의 생물학적 거동에 관한 연구 (Studies on the Biological Behaviors of Taxol Derivatives)

  • 오옥두;유대웅;임상무
    • 대한핵의학회지
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    • 제31권4호
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    • pp.440-451
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    • 1997
  • 본 연구에서는 항암제인 taxol의 $^{111}In$ 방사성표지화합물을 합성하여 암진단제로서의 이용 가능성을 보기 위한 기초 연구를 수행하였다. Taxol의 $^{111}In$ 표지화합물을 얻기 위해 taxol구조에서 C-13의 곁가지에 있는 C-2' 부분의 hydroxyl기를 DTPA anhydride 및 succinic anhydride와 반응시켜 taxol-DTPA와 2'-hemisuccinyltaxol을 합성하였다. 반응수율은 taxol-DTPA 접합체의 경우 34%이었으며, 2'-hemisuccinyltaxol은 80%이었다. MTT법을 사용하여 HT29, B16, P388, CT26 세포주에서 taxol-DTPA와 2'-hemisuccinyltaxol의 세포독성능실험에서는 taxol 보다는 못미치나 그 세포독성이 유지됨을 확인하였다. 합성된 taxol 유도체들을 리간드 교환법과 직접법을 사용하여 In-111을 표지하였다. Taxol-DTPA 접합체의 In-111 표지반응의 경우, 리간드교환법은 반응도중 침전이 생겨 반응이 어려워 직접법으로 In-111 표지화합물을 얻을 수 있었으며 그 표지수율은 100%이었다. 2'-hemisuccinyltaxol은 두 방법을 모두 시도하였으나 반응이 진행되지 않음을 확인하였다. In-111의 taxol-DTPA 접합체 및 2'-hemisuccinyltaxol에 대한 표지반응 수율은 HPLC, paper, instant thin-layer chromatography를 실시하여 결정하였다. Li-pophilicity의 실험에서는 친수성임이 확인되었으며, 세포결합능의 실험에서는 HT29, B16, P388, CT26 세포주와의 결합이 매우 낮음을 나타내었다. 혈청단백 질과의 결합능을 보기위하여 30% trichloroacetic acid 법을 수행하였으며, 약 30%정도만이 혈청단백질과 결합하여 그 값이 크지 않았다.

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목초액의 안정성 및 모발 성장 촉진 효과 (Evaluation of Stability in the Purified Wood Vinegar and Its Hair Growth Effect)

  • 조영호;이주연;이종화;조재수;이계원
    • 생명과학회지
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    • 제19권10호
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    • pp.1389-1395
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    • 2009
  • 천연물 신약으로 응용 가능성이 있는 목초액을 산화응집반응과 활성탄 등을 첨가하여 증류하는 방법으로 제조하였으며, 장기보존과 가속 저장 조건에서 목초액의 이화학적 변화(pH, 비중, 굴절률 및 용해 타르), 유해물질(카르보닐기, 벤조피렌 및 잔류용매) 그리고 유기산(개미산, 초산 및 프로피온산)의 변화를 검토하여 안정성을 평가하였다. 또한, 발모 모델로서 C57BL/6 마우스를 이용하여 모발 성장 효과를 살펴보았다. 보관 기간 중에 어떤 화학 결합이 일어나거나 또는 분해반응이 반복적으로 일어나지 않았다. 또한, 유해성분이나 주성분이 일정하게 유지되었고 특히 발암물질인 벤조피렌은 검출되지 않았다. 정제된 목초액 또는 미녹시딜을 2주 동안 등에 도포한 후, 어떤 임상 증상 없이 음성 대조군인 생리식염수보다 모발 성장을 촉진하였다. 따라서 화장품이나 천연물 신약으로 응용가능성이 높은 목초액을 함유한 제품 개발 시 일정한 양으로 유지되는 주성분을 함유하면서 페놀과 같은 유해물질을 줄일 수 있는 방법이 가능할 뿐만 아니라 모발 성장 촉진 효과가 있어 탈모환자에도 유용하게 사용될 것으로 기대되어진다.

IgA 항체합성에 대한 초유함유 TGF-${\beta}$ 와 bifidobacteria의 영향 평가

  • 김평현;고준수
    • 한국축산식품학회:학술대회논문집
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    • 한국축산식품학회 2001년도 임시총회 및 제28차 추계학술발표회
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    • pp.43-56
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    • 2001
  • Colostrum contains various kinds of cytokines including TGF-${\beta}$ which is known to be multifunctional in immune response and act as an anti-inflammatory agent. First, we measured the amount of TGF-${\beta}$ in bovine and human colostrum. Expression pattern of TGF-${\beta}$ isotypes was dramatically different between human and bovine colostrial samples. Bovine colostrum collected on day 1 post-delivery retained $41.79{\pm}16.96ng/ml$ of TGF-${\beta}$ 1 and $108.4{\pm}78.65ng/ml$ of TGF-${\beta}$ 2 while in human, $284{\pm}124.75ng/ml$ of TGF-${\beta}$ 1 and $29.75{\pm}6.73ng/ml$ of TGF-${\beta}$ 2. Thus, TGF-${\beta}$ is the predominant TGF-${\beta}$ isotype in bovine colostrum and vice versa in human colostrum. Both TGF-${\beta}$ isotypes diminished significantly in human and bovine colostrum with time. Next, biological activity of colostrial samples was examined in vitro. Both human and bovine colostrum increased IgA synthesis by LPS-activated mouse spleen B cells, which is a typical effect of TGF-${\beta}$ on the mouse B cell differentiation. Futhermore, we found that anti-proliferative activity in MV1LU cells by colostrum samples disappeared by addition of anti-TGF-${\beta}$ 1 and anti-TGF-${\beta}$ 2 antibody. In conclusion, there are substantial amounts of biologically active TGF-${\beta}$ 1 and TGF-${\beta}$ 2 in bovine and human colostrum. The results that the colostrum can increase IgA expression has important implications since IgA is the major Ig class produced in the gastrointestinal tract. We have previously shown that the stimulatory effect of Bifidobacteria bifidum on spllen B cells was quite similar to that of LPS which is a well-known polyclonal activator for murine B cells. In the present study, we further asked whether B. bifidum regulate the synthesis of IgA by mucosal lymphoid cells present in Peyers patches (PP) and mesenteric lymph nodes (MLN). B. bifidum alone, but not C. perfringens, significantly induced overall IgA and IgM synthesis by both MLN and PP cells. This observation indicates that B. bifidum possesses a modulatory effect on the mucosal antibody production in vivo. We, therefore, investigated the mucosal antibody prodduction following peroral administration of B. bifidum to mice. Ingested B. bifidum significantly increased the numbers of Ig (IgM, IgG, and IgA) secreting cells in the culture of both MLN and spleen cells, indicating that peroally introduced B. bifidum enhances mucosal and systemic antibody response. Importantly, however, B. bifidum itself does not induce the own specific antibody responses, implying that B. bifidum do not incite any unwanted immune reaction. Subsequently, it was found that excapsulation of B. bifidum further augments the total IgA production by increasing the number of IgA-secreting cells in the culture of both MLN and spleen cells. Finally, we found that the immuno-stimulating activity of B. bifidum is due to its cell wall components but not due to any actively secreting component(s) from bacteria. Thus our data reveal that peroral administration of B. bifidum can enhance intestinal IgA production and that encapsulation of B. bifidum further reinforces the IgA production.

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비타민 A 및 피리딘으로 유발된 사염화탄소 유발성 간독성에 대한 2-(알릴티오)피라진의 보호효과: ${\Phi}$x-174 DNA 손상에 미치는 효과 (Protective Effects of 2-(Allylthio)pyrazine on Retinoyl Palmitate- and Pyridine-Potentiated Carbon tetrachloride- induced Hepatotoxicity: Effect on ${\Phi}x$-174 DNA Strand Breakage)

  • 김상건;조주연;최성희;김낙두
    • 약학회지
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    • 제40권6호
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    • pp.727-733
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    • 1996
  • 2-(Allylthio)pyrazine is effective in selectively suppressing constitutive and inducible expression of cytochrome P450 2E1. The effect of 2-(allylthio)pyrazine against potentiat ed chemical injury was studied in rats. Vitamin-A pretreatment of rats substantially increased carbon tetrachloride hepatotoxicity, as supported by an ~4-fold increase in serum alanine aminotransferase (ALT) activity. Concomitant pretreatment of rats with 2-(allylthio)pyrazine at the daily dose of 200mg/kg resulted in a 76% decrease in vitamin-A-potentiated hepatotoxicity, which supported the possibility that 2-(allylthio)pyrazine protects the liver against chemical-induced hepatic injury by the mechanism associated with Kupffer cell inactivation. Pyridine pretreatment caused substantial enhancement in carbon tetrachloride hepatotoxicity. 2-(Allylthio)pyrazine treatment of rats reduced the pyridine-potentiated toxicity in a dose-dependent manner. Animals treated with both pyridine and 2-(allylthio)pyrazine prior to intoxicating dose of CCl$_4$ resulted in 85% and 47% decreases in pyridine-increased triglycerides and cholesterol levels in the liver. The protective effect of 2-(allylthio)pyrazine on the DNA strand breakage induced by benzenetriol was assessed by measuring the conversion of supercoiled ${\Phi}x$-174 DNA to the open relaxed form. 2-(Allylthio)pyrazine blocked the benzenetriol-induced conversion of supercoiled DNA to open circular form in a dose-dependent manner. The presence of 2-(allylthio)pyrazine at the doses from I to 10mM in the incubation mixture containing 5 ${\mu}$M benzenetriol completely protected benzenetriol-induced DNA strand breakage with the EC50 for the 2-(allylthio)pyrazine blocking being noted as ~220 ${\mu}$M, whereas allyl disulfide exerted protecting effect at relatively high concentrations (i.e. ~850 ${\mu}$M), suggesting that 2-(allylthio)pyrazine effectively scavenges the reactive oxygen species. These results provide evidence that 2-(allylthio)pyrazine blocks vitamin A- or pyridine-potentiated CCl$_4$ hepatotoxicity and that the agent is active in protecting DNA by scavenging the reactive oxygen species.

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밀폐공간 종류별 유해가스 발생 농도 평가 (Exposure Assessment of Hazardous gases in Confined Spaces)

  • 박현희;유계묵;함승헌;정광재;신민아;이구용;장경조;윤충식
    • 한국산업보건학회지
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    • 제19권4호
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    • pp.381-389
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    • 2009
  • Confined spaces are inherently dangerous workplace and many fatal and nonfatal accidents have been reported. Even though these accidents occur in various kinds of confined spaces, there has rarely been reported on the health hazard agent, i.e., the types of gases and their concentration ranges. Therefore in this study, we evaluated several toxic and asphyxiating gas concentrations in various confined spaces. We surveyed 57 manholes, 3 sewage treatment plants, 2 yellow radish manufacturing companies and 7 barges to measure the concentrations of oxygen($O_2$), hydrogen sulfide($H_2S$), carbon monoxide(CO), ammonia($NH_3$). Lower Explosion Limits(LEL) and Volatile Organic Compounds (VOCs). Those four types of confined spaces occupies 56% of accidents during last 9 years in Korea. In 57 manholes, the concentration varied according to the types of manholes; rainfall and sewage, and by location; residential and industrial areas. Sewage manhole in industrial area was evaluated as the most hazardous than other types of manhole like rainfall manholes, residential sewage manholes. The highest $H_2S$ concentration and the lowest $O_2$ concentration at sewage manhole in industrial area were 300 ppm, 8.7% respectively. In 3 sewage treatment plants, $H_2S$ and $NH_3$ concentrations were reached up to the 500 ppm and 200 ppm respectively. Two yellow radish manufacturing companies showed the concentrations of 316 ppm, 505.2 ppm, 90 ppm and 15.7% for $H_2S$, CO, VOCs and $O_2$, respectively. Seven barges showed 15.9%~20.9% oxygen concentration. Gas species and concentration ranges varied by the types and location of confined spaces; CO, $H_2S$, $O_2$ could be hazardous in manhole, especially manhole connected to sewage plants. CO, $H_2S$, LEL, $O_2$, $NH_3$ should be controlled in sludge silo and sluge pumping confined spaces in sewage treatment plant. The activity of lifting out radish from the storage tank was evaluated more hazardous rather than the other activities in yellow radish manufacturing industry. The employers must conduct the survey to identify all possible confined spaces in their local workplace prior to performing the tasks. At the national level to reduce the accidents in the confined spaces, we suggest that systemic approach and active education program including possible hazards, standard operation procedures, ventilation plan, and personal protective equipment in confined spaces should be implemented.

학생과학탐구 올림픽 행사를 통해 본 혁신 지향 교사의 특징 (The Characteristics of Science Teachers Participating in the Student Science Inquiry Olympic)

  • 명전옥;서정아;박승재
    • 한국과학교육학회지
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    • 제18권2호
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    • pp.137-148
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    • 1998
  • 본 연구는 제 1회 학생과학탐구올림픽에 참여한 과학 교사의 혁신 지향적인 특성을 비참여 교사와 비교하였다. 연구 대상은 세 집단의 교사였는데, (1) 탐구 올림픽에 참가한 학생의 지도 교사 집단, (2) 탐구 올림픽을 관람한 교사 집단, (3) 다단계 유충 군집 표집에 의해 추출된 비참여 교사 집단이었다. 연구도구는 설문지였는데 우편으로 우송되었고, 236명으로부터 회수되었고, 총 회수율은 45%였다. 대체적으로 탐구 올림픽에 참여한 교사들(학생 지도 교사 및 관람 교사)은 비참여 교사들에 비해 다음 4가지 범주에서 다른 특성을 보였다. 첫째, 탐구 올림픽 참여 교사는 비참여 교사보다 자아 실현, 즉 과학교육에 대한 관심, 변화 시도 욕구, 내적 성취동기가 더 높았다. 둘째, 탐구 올림픽 참여 교사는 과거 과학행사 참여 정도와 진급 욕구가 비참여 교사보다 높았다. 셋째, 탐구 올림픽 참여 교사는 비참여 교사에 비해 의사소통 행태면에서 더 높은 여론 선도력, 변화 주체측과의 더 많은 접촉, 자신이 속한 사회를 좀 더 근대적으로 인식하였다. 넷째, 탐구올림픽 참여 교사들은 비참여 교사보다 사회적 지위가 더 높았다. 본 연구 결과는 과학교사의 혁신성을 측정하는 도구 개발에 기초 자료를 제공할 것이며, 이는 혁신 초기에 보다 효과적인 혁신 대상, 보급 시기와 설득 전략을 파악하여 혁신 추진력을 중대시키는데 도움을 줄 것이다.

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토양미생물제제에 의한 음식물폐기물의 퇴비화 검토 (Food Waste Composting by Soil Microbial Inoculators)

  • 배일상;정권;전은미;김광진;이동훈
    • 유기물자원화
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    • 제8권4호
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    • pp.160-167
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    • 2000
  • 음식물 퇴비화를 위한 토양미생물제재의 퇴비화 효율을 평가하며, 토양미생물제재의 미생물수와 퇴비화과정에서 식종의 효과를 조사하였다. 분석대상 음식물은 본 연구원 구내식당에서 수거한 후 물리화학적특성을 분석하였다. 대상시료는 Bulking Agent로서 톱밥을 사용하여 함수율을 65%로 조정 후 반응기 B에 10%의 토양미생물제를 식종하였다. 토양미생물제제의 미생물은 호기성세균수가 $2.98{\times}10^9/g$이상, 방선균이 $3.93{\times}10^7/g$이상, 효모가 $1.21{\times} 10^5/g$, 균류가 $5.79{\times}10^7/g$ 이상이었다. 퇴비화 기간동안 최고온도는 Reactor A가 반응 10일후에 개시후 바로 급격한 변화를 보였으며, 반응이 종료된 후 두 Reactor 공히 pH8.9를 나타내었다. Reactor B의 경우 최대온도인 4일후에 $CO_2$농도도 역시 최대인 10.8%를 나타냈으며, Reactor A는 최대온도인 10일후에 6.1%를 나타내었다. 한편 Reactor A는 $r_{d}$(유기물질의 분해율)치가 0.35에서 0.41로 17.1%상승하였으며, Reactor B의 경우 0.31에서 0.51로 64.5%상승하였다.

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Protective effects of PEP-1-Catalase on stress-induced cellular toxicity and MPTP-induced Parkinson's disease

  • Eom, Seon Ae;Kim, Dae Won;Shin, Min Jea;Ahn, Eun Hee;Chung, Seok Young;Sohn, Eun Jeong;Jo, Hyo Sang;Jeon, Su-Jeong;Kim, Duk-Soo;Kwon, Hyeok Yil;Cho, Sung-Woo;Han, Kyu Hyung;Park, Jinseu;Eum, Won Sik;Choi, Soo Young
    • BMB Reports
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    • 제48권7호
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    • pp.395-400
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    • 2015
  • Parkinson's disease (PD) is a neurodegenerative disability caused by a decrease of dopaminergic neurons in the substantia nigra (SN). Although the etiology of PD is not clear, oxidative stress is believed to lead to PD. Catalase is antioxidant enzyme which plays an active role in cells as a reactive oxygen species (ROS) scavenger. Thus, we investigated whether PEP-1-Catalase protects against 1-methyl-4-phenylpyridinium (MPP+) induced SH-SY5Y neuronal cell death and in a 1-methyl-4-phenyl-1,2,3,6-trtrahydropyridine (MPTP) induced PD animal model. PEP-1-Catalase transduced into SH-SY5Y cells significantly protecting them against MPP+-induced death by decreasing ROS and regulating cellular survival signals including Akt, Bax, Bcl-2, and p38. Immunohistochemical analysis showed that transduced PEP-1-Catalase markedly protected against neuronal cell death in the SN in the PD animal model. Our results indicate that PEP-1-Catalase may have potential as a therapeutic agent for PD and other oxidative stress related diseases. [BMB Reports 2015; 48(7): 395-400]

Effect of Recombinant Lactobacillus Expressing Canine GM-CSF on Immune Function in Dogs

  • Chung, Jin-Young;Sung, Eui-Jae;Cho, Chun-Gyu;Seo, Kyoung-Won;Lee, Jong-Soo;Bhang, Dong-Ha;Lee, Hee-Woo;Hwang, Cheol-Yong;Lee, Wan-Kyu;Youn, Hwa-Young;Kim, Chul-Joong
    • Journal of Microbiology and Biotechnology
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    • 제19권11호
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    • pp.1401-1407
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    • 2009
  • Many Lactobacillus strains have been promoted as good probiotics for the prevention and treatment of diseases. We engineered recombinant Lactobacillus casei, producing biologically active canine granulocyte macrophage colony stimulating factor (cGM-CSF), and investigated its possibility as a good probiotic agent for dogs. Expression of the cGM-CSF protein in the recombinant Lactobacillus was confirmed by SDS-PAGE and Western blotting methods. For the in vivo study, 18 Beagle puppies of 7 weeks of age were divided into three groups; the control group was fed only on a regular diet and the two treatment groups were fed on a diet supplemented with either $1\times10^9$ colony forming units (CFU)/day of L. casei or L. casei expressing cGM-CSF protein for 7 weeks. Body weight was measured, and fecal and blood samples were collected from the dogs during the experiment for the measurement of hematology, fecal immunoglobulin (Ig)A and IgG, circulating IgA and IgG, and canine corona virus (CCV)-specific IgG. There were no differences in body weights among the groups, but monocyte counts in hematology and serum IgA were higher in the group receiving L. casei expressing cGM-CSF than in the other two groups. After the administration of CCV vaccine, CCV-specific IgG in serum increased more in the group supplemented with L. casei expressing cGM-CSF than the other two groups. This study shows that a dietary L. casei expressing cGM-CSF enhances specific immune functions at both the mucosal and systemic levels in puppies.

화학적, 대사적 산화반응 중 생성되는 S-oxide를 이용한 O-ethyl S-methyl ethylphosphonothioate (1) 의 독성 기작에 관한 연구 (Study of the possible mode of action of O-ethyl S-methyl ethylphosphonothioate via the formation of S-oxide in chemical and metabolic oxidation systems)

  • 허장현;;한대성
    • 한국환경농학회지
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    • 제10권2호
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    • pp.167-177
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    • 1991
  • O,S-dialkyl alkylphosphonothioates 계열 유기인제 농약의 체내 작용기작을 이해하기 위하여 model 화합물 (1), O-ethyl S-methyl ethylphosphonothioate [$LD_{50}$(rat, oral) 4.6mg/kg ; $K_i$(bovine erythrocyte acetylcholinesterase) 303 $M^{-1}min^{-1}$]이 선정되었다. 이 유기인계 화합물들은 체내에서 활성화(活性化) 과정을 겪으면서 독성(毒性)을 발현하는 것으로 가설(假說)되어져 왔다. 생체 내 mixed function oxidases에 의한 산화 활성화 과정을 화학적(化學的)으로 재현하기 위하여 두 종류의 유기산화제 즉, meta-chloroperoxybenzoic acid와 monoperoxyphthalic acid가 사용되었고, 대사적(代謝的) 산화를 재현하기 위하여 쥐 간(肝)에서 추출한 microsomal oxidation system을 이용한 in vitro 산화반응이 시도되었다. 산화반응 중간생성물인 S-oxide의 존재가 전구물질(1)의 가설적 산화 반응경로를 통해서 간접적으로나마 충분히 확인 되어질 수 있었다. 더욱이 ethanol을 이용한 trapping 실험에서 불안정한 산화중간물질인 S-oxide가 강한 phosphorylating agent라는 것이 확인되어, 전구물질 (1)로부터 산화반응을 거치면서 생성된 이 중간물질이 체내 신경전달에 중요한 역할을 하는 acetylcholinesterase를 phosphorylation하게 되고, 결국 이런 활성화 과정을 통해 이 계열의 화합물들이 독성을 발휘하는 것으로 이해될 수 있었다.

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