Steaming is a method that has traditionally been used for medicinal plant extraction. This study investigated nitrite oxide production, ferrous ion chelating activity, α-glucosidase, xanthine oxidase, and acetylcholinesterase inhibitory activities of ethanol, acetone and hot-water extracts of Codonopsis lanceolata prepared by steaming seven times. MTT assay showed that each extract was non-toxic up to a concentration of 700 μg/mL confirming that there was no cytotoxicity in all extracts. The α-glucosidase, xanthine oxidase, and acetylcholinesterase inhibitory activities exhibited by the hot-water extract obtained from steaming seven times were higher (83.1%) than the other extracts. Higher production of nitrite oxide and better ferrous chelating activity was recorded with hot-water extract compared to ethanol and acetone extracts. These results indicated that more steaming of Codonopsis lanceolata extracts would be required to validate the possibility of developing antioxidants. Also, further study is needed to determine if the components present in the tested extracts might be useful in the prevention of Alzheimer's disease. These results showed that hot-water extracts may be useful for their antioxidant and the production inhibitory activity of nitrite oxide. It will be helpful in the investigation of the constituent analysis of the steam-processed product of Codonopsis lanceolata.

이산화염소는 병원미생물에 대한 소독제로 사용되고 있다. 최근 저곡해충에 대한 이산화염소의 산화적 스트레스에 의한 살충력이 확인되 었다. 그러나 이산화염소의 산화적 스트레스에 의한 대상 곤충의 체내 분자 종말점에 대해서는 알려지지 않았다. 본 연구는 화랑곡나방(Plodia interpunctella)의 아세틸콜린에스터레이즈가 이산화염소의 분자표적으로 가정하고 노출에 따른 이 효소의 활성을 분석하였다. 아세틸콜린에스 터레이즈 활성은 화랑곡나방 발육 시기에 따라 상이했다. 화랑곡나방 5령 유충에서 치사를 일으킬 수 있는 이산화염소 농도 처리는 아세틸콜린에 스터레이즈 활성을 뚜렷하게 증가시켰다. 또한 훈증제 형태의 이산화염소 처리에서도 아세틸콜린에스터레이즈 활성 증가가 유발되었다. 화랑곡 나방 5령 유충은 음성주광성을 보이는 데, 이산화염소 처리는 이 선천성 행동을 교란하였다. 이러한 결과는 아세틸콜린에스터레이즈가 이산화염 소 처리에 따른 산화적 스트레스의 분자표적 가운데 하나라는 것을 제시하고 있다.

Fumigant and contact toxicities of 11 Myrtaceae plant essential oils and their constituents against adult male and female Blattella germanica were evaluated. Of 11 Myrtaceae plant essential oils, Eucalyptus polybractea, E. smithii, E. radiata, E. dives, E. globulus, and Melaleuca uncinata, showed 100% fumigant toxicity against adult male German cockroaches at a concentration of 7.5 mg/liter air concentration. In contact toxicity tests, E. polybractea, E. smithii, E. radiata, E. dives, E. globulus, M. dissitiflora, and M. uncinata produced strong insecticidal activity against adult male and female German cockroaches. Of the essential oil constituents, terpinolene, α-terpinene, and terpinen-4-ol demonstrated strong fumigant toxicity against adult male and female B. germanica. Eugenol, isoeugenol, methyl eugenol, and terpinen-4-ol showed strong contact toxicity against adult male B. germanica. The toxicity of the constituent blends identified from M. dissitiflora essential oils indicated that terpinen-4-ol were major contributor to the fumigant activity or contact toxicity of the artificial blend. Only isoeugenol exhibited inhibition activity against male acetylcholinesterase. IC50values of isoeugenol were 0.22 mg/mL against male acetylcholinesterase.

Inhibition of acetylcholinesterase (AChE) is one of the important modes of action available for the control of insects. An assessment was made of the electric eel AChE inhibitory activity of 55 endophytic fungi isolated from the leaves of Huperzia serrata collected in Eunshi, Hubei Province, China. Of 55 mycelial extracts and 55 ethyl acetate-soluble fractions from liquid culture of the fungi, the ethyl acetate-soluble fraction of strain ES056 exhibited strong AChE inhibitory activity (88%) at a concentration of 100 μg/mL. Based on morphological characteristics and nuclear ribosomal DNA ITS sequence analysis, this fungus showed greatest similarity to members of the order Eurotiales and was shown to be most closely related to members of the Aspergillus aculeatus group. It was designated Aspergillus sp. MY056. This strain merits further study as a potential anti-AChE product.

I conducted experiments in Drosophila to investigate the consequences of altered acetylcholinesterase (AChE) activity in the nervous system. In ace hypomorphic mutant larvae, the amount of ace mRNA and the activity of AChE both in vivo and in vitro were significantly reduced compared with those of controls. Reduced Ace in Drosophila larvae resulted in significant down-regulation of branch length and the number of boutons in Type 1 glutamatergic neuromuscular junctions (NMJs). These defects in ace hypomorphic mutant larvae were suppressed when Musca domestica AChE was transgenically expressed. Because AChE inhibitors are utilized for medications for Alzheimer’s disease, we investigated whether pharmacological inhibition of AChE activity induced any synaptic defects. I found that controls exposed to a sublethal dose of DDVP phenocopied the synaptic structural defects of the ace hypomorphic mutant. These results suggest that down-regulation of AChE activity, regardless of whether it is due to genetic or pharmacological manipulations, results in altered synaptic architecture. This study suggests that exposure to AChE inhibitors for 6-12 months may induce altered synaptic architectures in human brains with Alzheimer’s diseases, similar to those reported here. These changes may underlie or contribute to the loss of efficacy of AChE inhibitors after prolonged treatment.

Western blot analysis using acetylcholinesterase (AChE)-specific antibody was conducted to determine whether AChE gene (Tuace) duplication actually results in overproduction of AChE in Tetranychus urticae (TuAChE). The protein quantities of TuAChE in seven field-collected mite populations were precisely correlated with the copy numbers. To investigate the effects of each mutation on AChE insensitivity and possible fitness cost, eight variants of TuAChE were in vitro expressed using the baculovirus expression system. Kinetic analysis revealed that the Ala391Thr mutation did not change kinetic properties of AChE, whereas the Gly228Ser and Phe439Trp mutations significantly increased the insensitivity to monocrotophos. Moreover, when the Gly228Ser and Phe439Trp mutations are present together, insensitivity increased over a thousand-fold, showing that both mutations confer resistance in a synergistic manner. Presence of the mutations, however, reduced catalytic efficiency of AChE considerably, suggesting an apparent fitness cost in monocrotophosresistant mites. Reconstitution of the multiple copies of AChE having different compositions of mutations revealed that the catalytic efficiencies of the six-copy and two-copy AChEs (resembling the AD and PyriF strains of mite, respectively) were still lower but comparable to that of wildtype AChE. These finding clearly suggested that multiple rounds of Tuace duplication was needed to compensate the reduced catalytic activity of AChE caused by mutations.

초 록 벼멸구의 살충제 저항성 기구를 구명하고자 fenobucarb, carbofuran 및 diazinon으로 벼멸구를 14~18세대 누대 도태하여 얻어진 벼멸구를 대상으로 저항성 기구를 조사하였으며, 얻어진 결과중 acetylcholinesterase(AChE)와 esterase의 활성 변화에 대하여 보고하고자 한다. AChE활성은 fenobucarb선발 계통에서 1.6배 증가하였으나 타 계통에서는 차이가 없었고, 세포내 분포도 mitochondrial fraction에서 70% 이상으로 계통간 차이가 없었다. 반면, AChE감수성은 fenobucarb와 carbofuran선발 계통에서 각각의 공시 살충제에 대하여 12.2배, 5.6배 감소하였으나 diazinon선발 계통에서는 diazoxon에 대하여 1.7배 감소에 그쳤다. Esterase활성은 fenobucarb선발계통에서 5.6~6.8배, carbofuran선발계통에서 6.4~7.8배, diazinon선발계통에서 4.0~4.4배 증가하였다. 벼멸구의 저항성 증가에 다른 요인이 관련됨을 배제할 수 없으나, 본 실험 결과 esterase 활성증가와 AChE감수성 저하라는 두 요인이 상승적으로 작용하여 벼멸구 저항성을 유발하였음을 확인하였다.

Since the acetylcholinesterase (AChE) inhibitor is used to treat Alzheimer’s disease, the present study aimed to analyze the component with anti-AChE activity from the essential oil of Artemisia iwayomogi (Compositae). The four major components of the essential oil were identified to be camphor (29.8%), borneol (28.0%), eucalyptol (5.81%) and coumarin (5.49%) from a gas chromatography-mass spectrometry (GC-MS). The essential oil and its three components, camphor, borneol, and coumarin, were subjected to anti-AChE assay. The IC50 values of the essential oil and coumarin were shown to be 0.298 ㎎/㎖ and 0.236 ㎎/㎖, though those of other two components, camphor and borneol, were more than 0.250 ㎎/㎖. These results suggest that coumarin is an active substance of this essential oil with anti-AChE activity.

본 연구에서는 20종 생약 열수추출물의 AChE 활성, 산화 스트레스로 인한 지질 과산화물 생성 억제능 및 뇌신경 세포 사멸에 대한 보호효과를 비교하였다. AChE의 억제활 성은 산수유, 감초, 당귀 열수추출물에서 우수하였으며, 그 중 산수유가 가장 높은 억제율을 나타내었다. 또한 H2O2/ FeSO4로 산화 스트레스를 유발시켜 생약 열수추출물의 지 질과산화물 생성 억제 활성을 조사한 결과 소엽, 하수오, 계피 및 감초 열수추출물에서 높은 항산화 활성을 보였다. L-Glutamate에 의해 유도된 신경세포 독성에 대한 보호효 과는 감초, 계피, 길경, 박하 열수추출물의 100 μg/mL 농도 에서 관찰되었다. 본 연구를 종합적으로 살펴보았을 때, 감초 열수추출물이 치매 예방 및 개선제로써의 활용가능성 이 가장 뛰어난 것으로 판단된다. 향후 치매예방 효능을 가지는 새로운 화합물 발굴을 위한 기초자료로 활용될 것으 로 사료된다.

본 연구에서는 국내에서 시판되고 있는 4종류의 차 즉, 녹차, 보이차, 우롱차 및 홍차 열수추출물의 페놀성 화합물, 항산화 및 퇴행성 뇌신경질환 저해활성에 대하여 조사하였다. 시판 차 열수추출물의 총 페놀성 화합물 함량은 이었으며, 녹차, 보이차, 우롱차 및 홍차 열수추출물의 총 플라보놀 함량은 각각 350.96, 254.17, 334.48 및 240.23 mg/100 g이었다. 녹차, 보이차, 우롱차 및 홍차 열수추출물의 총 카테킨 함량은 각각

The effects of organophosphorus and carbamate pesticides were examined inhibition of the acetylcholinesterase activity in the chicken brain with enzyme - inhibition methods. The acetylcholinesterase activity in chicken brain determined by the Ellman method was 167 μmol/min/g protein. The optimum pH of acetycholinesterase was 8.2. pI_50 of acetycholinesterase by some organophosphorus were 3.80M of phosphorodithioate, 4.04M of phosphorothioate, 6.33M of phosphate, and 6.60M of phosphrothiolate. pI_50 of acetycholinesterase by some carbamates were 5.10M of XMC, 5. 90M of carbofuran, 6.16M of isoprocarb, 6.30M of carbaryl, 6.47M of BPMC, and 6.77M of propoxur. pI_50 of carbamates selected was similar to that of phosphorothioate and phosphate organophosphates