The toxicity of cypress (Cupressus sempervirens) and howood (Cinnamomum camphora) essential oils, and its constituents to adult western flower thrips, Frankliniella occidentalis using leaf-dipping bioassay and vapour-phase toxicity bioassays. Both cypress and howood essential oils were toxic to western flower thrips. The most active principles were determined to be linalool, linalool oxide, cis-linalool oxide, trans-linalool oxide, camphor, and 1,8-cineole from cypress and howood essential oils. Linalool (24h LC50, 0.030 µg/cm2), linalool oxide (24h LC50, 0.036 µg/cm2), cis-linalool oxide (24h LC50, 0.043 µg/cm2), trans-linalool oxide (24h LC50, 0.045 µg/cm2), and camphor (24h LC50, 0.10 µg/cm2) were the most toxic. Potent toxicity was also observed with 1,8-cineole, a-pinene, d-limonene, a-terpinene, cinnamaldehyde, b-pinene, 3-carene a-terpineol, camphene, and terpineol (24h LC50, 0.33–0.65 µg/cm2). The spray bioassy of cypress and howood oil formulation (500 ppm) resulted in > 80% mortality toward western flower thrips population. Global efforts to reduce the level of toxic synthetic insecticides in the agricultural environment justify further studies on cypress and howood essential oil-derived materials as potential contact-action fumigants for the control of western flower thrips populations.

혈청 내 존재하는 효소 중 Glutamic pyruvic transaminase(GPT)는 근육이나 간세포의 손상에 대한 임상 화학적 지표로 사용 된다. 본 연구는 Landrace와 한국재래돼지의 F2 교잡 축군(N=1,105)에 대해 Porcine SNP 60K beadchip을 사용하여 유전자형 분석을 실시하고, GPT 형질과의 관련성을 검증하기 위해 Genome-Wide Association Study(GWAS)를 수행하였다. F2 교잡축군의 가계구조를 보정한 GWAS를 수행하기 위하여 혼합모형과 회귀분석을 조합한 GRAMMAR방법을 관련성 분석에 사용 하였다. 유의성 있는 SNP 표지들은 Sus scrofa chromosome(SSC) 6, 7, 그리고 13에서 동정되었다. 이들유의성 있는 SNP marker들에 가장 근접한 염색체상 위치의 유전자를 그 유전자의 기능을 고려하여 SSC7에서 2개의 위치후보유전자(BCL11B, AHNAK2)를 선정하였다. Pyrosequencing법을 통하여 이 들유전자 내에 존재하는 4개 SNP 표지들의 유전자형을 분석하여 GPT 형질간의 관련성 분석에 이용하였다. 관련성 분석결과, BCL11B g.267 T>C에서 nominal P=7.23×10-8 과 AHNAK2 g.1439 C>T에서 nominal P=5.64×10-6, g.1736 C>A에서 nominal P=3.51×10-6의 결과를 얻었다. 이 들 중 가장 유의한 결과를 얻은 BCL11B 유전자의 g.267 T>C SNP 표지는 추가 연구를 통하여 혈청 GPT 변이에 영향을 미치는 위치상 후보 유전자 표지로 사용 되어 질 수 있을 것이라 사료되어진다.

Alzheimer’s disease (AD) is the most common type of presenile and senile dementia. Human β-amyloid precursor cleavage enzyme (BACE-1) is a key enzyme responsible for amyloid plaque production. We assessed anti-BACE-1 and behavioral activities of curcuminoids from Curcuma longa, curcumin (CCN), demethoxycurcumin (DMCCN), and bisdemethoxycurcumin (BDMCCN) against AD fly models. Neuro-protective ability of curcuminoids was assessed using fly model system overexpressing BACE-1 and its substrate APP in compound eyes and entire neurons. BDMCCN has the strongest inhibitory activity toward BACE-1 with 17 μM IC50, which was 20 and 13 times lower than those of CCN and DMCCN respectively. Expression of APP/BACE-1 resulted in the progressive and measurable defects in morphology of eyes and locomotion. Supplementing diet with either 1 mM BDMCCN or CCN rescued APP/BACE1 expressing flies and kept them from developing both morphological and behavioral defects. Structural characteristics and hydrophobicity appear to play a role in determining inhibitory potency of curcuminoids on BACE-1.

An assessment is made of the anti-proliferative activity of cicada slough-derived materials against 10 human cancer cell lines, including PC-3 and DU145 prostate cancer cell lines, using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results were compared with those of the commercially available anticancer agent with broad spectrum cisplatin. The ethanol extract of Cryptotympana spp. slough was proved to have anti-proliferative activity against A549 lung, AGS stomach, PC-3 and DU145 prostate, Hela cervix, HT-29 colon, MCF-7 breast, and SK-Hep-1 liver cancer cell lines except for Hep-2 larynx and SK-OV-3 ovary cancer cell lines. The biologically active constituent was characterized as the nonprotein α-amino acid theanine [2-amino-4-(ethylcarbamoyl)butyric acid] by spectroscopic analysis, including EI-MS and NMR. Theanine was isolated from the cicada slough as a new cytotoxic principle. Fifty percent inhibition concentration (IC50) values of the constituent against PC-3 was 6.52 μg/mL, respectively. The activity of theanine (IC50,6.52μg/mL) did not differ significantly from that of the anticancer agent cisplatin (IC50,7.39μg/mL) toward PC-3. In conclusion, further studies on the cicada slough-derived materials containing theanine as potential anticancer products or a lead molecule for the prevention or eradication from human prostate cancer.

Lung cancer caused by diverse changes in cells resulted by exposure to carcinogens found in tobacco smoke, the environment, or sequential accumulation of genetic changes to the normal epithelial cells of the lung. An assessment was made of the anti-proliferative activity of constituents from silkworm feces against 11 human cancer cell lines, including A549 and H727 lung cancer cell lines, using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. The ethanol extract of silkworm feces was proved to have anti-proliferative activity against all 11 species of human cancer cell lines. The biologically active constituent was characterized as vomifoliol (blumenol A) (1) and stigmasterol (2) by spectroscopic analysis ,including MS and NMR. In conclusion, global efforts to reduce the level of antitcancer agents justify further studies on the silkworm feces-derived materials containing vomifoliol and stigmasterol as potential anticancer products or lead compounds for the prevention or eradication from human lung cancer.

Antimicrobial peptides (AMPs) are an important component of innate defense mechanisms with broad-spectrum activities against various pathogenic microorganisms, including Gram-positive and Gram-negative bacteria, fungi, and viruses. Antibiotic resistance has become a pervasive and global health burden, resulting in the immediate need to develop a new class of antibiotic substances. We screened a 16-mer random peptide library using the yeast two-hybrid system with Beclin 1 as bait and found that two 16-mer peptides (named P4 and P30) appeared to interact with Beclin1 in the β-gal assay. The two candidate cDNAs were introduced into the yeast secretory system of Pichia pastoris and their expression induced in the presence of methanol. Spectrophotometric analysis and Disc clear zone assay using the supernatant of the yeast growth media showed that both of the two peptides had strong activities against Staphylococcus aureus, MRSA (methicillin resistance Staphylococcus aureus), MRSA2242, and MRSA-2250, but no effect on commensal Lactobacillus strains. PCR analysis of the genomic DNA of transformed Pichia pastoris using AOX1 primers revealed that the two cDNAs were integrated into the genome at the AOX1 locus. Our result suggests that these peptides could be developed as a useful alternative to classic chemical antibiotics.

The toxicity of bay leaf (Pimenta racemosa) and palmorasa (Cymbopogon martini) essential oils, and its constituents, and structurally related compounds to adult American house dust mites, Dermatophagoides farinae was examined. Both bay leaf (24 h LC50, 131.95 μg/cm2) and palmorosa (24 h LC50, 116.10 μg/cm2) essential oils were toxic to mites. The most active principles were determined to be citral, methyleugenol, eugenol, and geranyl acetate from both bay leaf and palmorosa oils. Citral (24 h LC50, 1.13 μg/cm2), methyl eugenol (5.78 μg/cm2), eugenol (24 h LC50, 12.52 μg/cm2) and geranyl acetate (24 h LC50, 18.79 μg/cm2) were the most toxic. The toxicity of these compounds was more toxic than that of commercially available acaricides such as, benzylbenzoate (LC50,8.41μg/cm2) and deet (37.67 μg/cm2). Potent toxicity was also observed with nerol, linalool and geraniol (LC50, 21.44–54.61 μg/cm2). These compounds were consistently more toxic in closed versus open containers, indicating that their mode of delivery was largely a result of vapour action. Both bay leaf and palmorosa oil, and their constituents shown their potentials as effective alternatives for harmful synthetic acaricides for the control of Dermatophagoides populations as fumigants in contact and therefore illustrated the need for further study of these essential oils.

Medicinal plant extracts from 27 plant species in 20 families were tested for their larvicidal activity against house fly, Musca domestica (L.). Responses varied with plant material and concentration. Among plant species tested, Phryma leptostachya var. asiatica showed 100% larvicidal activity against M. domestica at 10 mg/g concentration. Larvicidal activities of Atractylodes japonica, Saussurea lappa, Asiasarum sieboldi, and Gleditsia japonica var. koraiensis were 89.3, 85.3, 93.3 and 96.6% at 10 mg/g concentration, respectively. Extracts of Prunus persica, Curcuma longa and Paeonia moutan produced moderate activity. Larvicidal activity of other plant extracts was less than 50%. Among test plant species, Phryma leptostachya var. asiatica showed the most potent larvicidal activity. The active constituent of P. leptostachya var. asiatica roots was identified as the leptostachyol acetate by spectroscopic analysis. The LC50valuesofleptostachyolacetateagainstM. domestica larvae was 0.039 mg/g. Naturally occurring medicinal plant extracts and Phryma leptostachya var. asiatica root–derived compounds merit further study as potential house fly larval control agents or lead compounds.

An assessment was made of beta-site amyloid precursor protein (APP) cleaving enzyme (BACE1) inhibitory, feeding, climbing activities and lifespan of the diarylalkyls curcumin (CCN), demethoxycurcumin (DCCN) and bisdemethoxycurcumin (BDCCN) identified in the rhizomes of Curcuma longa. Based on IC50 values, BDCCN (0.024 mM) was the most inhibitory constituent, followed by DCCN (0.31 mM) and CCN (0.59 mM). Overall the three curcuminoids were significantly less inhibitory than BACE1 inhibitor IV isophthalamide (8.5 × 10-5 mM). The expression of human APP and BACE1 in compound eye of Drosophila melangaster presented rough abnormal ommatidial lattice. Co-expression of APP and BACE1 within the developing nervous system of drosophila showed climbing defects. These transgenic flies kept on media containing 1 mM of CCN and BDCCN were observed to ameliorate eye degeneration, significantly suppress locomotive dysfunctions, and increase media life time, as well as isophthalamide. CCN and BDCCN as human BACE1 inhibitory constituents may be used as potential therapeutics or lead molecules to develop Alzheimer's disease treatment drugs.

In order to develop an efficient microbial source of cellulase enzyme system, cellulolytic fungal strain was newly isolated from traditional Korean nuruk samples in the present study. The crude enzyme extract of this fungal strain, avicelase, CMCase and β-glucosidase activities reached the maximal points of 6.73, 3.22, and 5.64 units/mL, respectively and was used for the subsequent enzymatic saccharification on pretreated deproteinised and lipid-extracted rice bran. This strain was identified as Penicillium sp. determined by cellular fatty acid composition analysis. Three different pretreatment conditions were evaluated on the deproteinised and lipid-extracted rice bran at 121oC/1.5 psi for 5 different residence times: one with 0.1 N sulfuric acid, another with 0.1 N sodium hydroxide, and the last with distilled water. The greatest enzymatic saccharification yield increased up to 75.2% from acid-catalyzed autoclaving pretreatment for 30 min. The acid-catalyzed autoclaving pretreatment enhanced the saccharifying ability of the newly isolated cellulolytic fungal strain on the deproteinised and lipid-extracted rice bran.

 ,  , The larvicidal activities of Piper nigrum fruit methanol extracts and its constituents against larvae of the diamondback moth, Plutella xylostella, were investigated using the leaf dipping method. Administering the P. nigrum methanol extract resulted in 100 and 97% mortality against diamondback moth larvae at 5.0 and 2.5 mg/mL concentrations, respectively. Larvicidal activities of the P. nigrum fruit-derived piperidine alkaloids, piperine, and N-isobutylamide, as well as pellitorine, guineensine, pipercide, and retrofractamide A against P. xylostella varied according to test compound. Based on the 48 h LC50 values, the most toxic compound to diamondback moth larvae was guineensine (0.013 mg/mL) followed by retrofractamide A (0.020mg/mL), pipercide (0.033mg/mL), and pellitorine (0.046 mg/mL). The LC50 value of piperine was >, 0.5 mg/mL.

The toxicity of materials derived from the seed of Pongamia pinnata to third instars of insecticide-susceptible Culex pipiens pallens and Aedes aegypti and wild Aedes albopictus was examined using a direct contact bioassay. Results were compared with those of the currently used insecticides fenthion and temephos. The active principles of Pongamia pinnata were identified as the karanjin (1), karanjachromene (2), pongamol (3), pongarotene (4), oleic acid (5), and palmitic acid (6) by spectroscopic analysis. Based on 24 h LC50 values, karanjin (14.61 and 16.13 mg/L) was the most toxic compound, followed by oleic acid (18.07 and 18.45 mg/L) and karanjachromene (18.74 and 20.57 mg/L). These constituents were less toxic than either fenthion (LC50, 0.0031 and 0.0048 mg/L) or temephos (0.021 and 0.050 mg/L) against Ae. aegypti and Cx. p. pallens. Low toxicity was produced by pongamol (LC50, 23.95 and 25.76 mg/L), pongarotene (25.52 and 37.61 mg/L), and palmitic acid (34.50 and 42.96 mg/L). Against A. alpopictus instars, oleic acid (LC50, 18.79 mg/L) was most toxic. Low toxicity was observed with the other five constituents (LC50, 35.26- 85.61 mg/L). P. pinnata seed-derived active principles, particularly karanjin, karanjachromene, and oleic acid, merits further study as potential mosquito larvicides for the control of mosquito populations in light of global efforts to reduce the level of highly toxic synthetic larvicides in the aquatic environment.

Antimicrobial peptides are widely found in living organisms and are known to play a critical role in innate immunity. Numerous antimicrobial peptides from diverse species appear to be effective against pathogenic microorganisms of bacteria, fungi, protozoa, and viruses. Because antibiotic resistance is a global health issue in the fight against pathogenic microorganisms, there has been an urgent need for development of new antibiotic substances. In the current study, we performed yeast two hybrid screening using Beclin1 bait in order to find new peptide antibiotics from a random peptide library. Two candidate peptides from the screening were expressed in a yeast secretory system of Pichia pastoris and tested for any antimicrobial activity against Staphylococcus aureus, MRSA, MRSA2242, MRSA2250, Lactobacillus casei, and Lactobacillus acidophilus. Disc clear zone assay and spectrophotometric analysis revealed that the two peptides exert a decent activity against the pathogenic bacteria, in contrast to minimal effect on the commensal Lactobacillus strains. Taken together, this study presents novel peptides with antibacterial activity against the pathogenic forms of Staphylococcus aureus and suggests the possibility that these peptides, upon further characterization, may be developed as clinically useful antibiotics.

목적: 콘택트렌즈 착용자들이 느끼는 건성안과 관련된 안구증상을 알아보고자 한다. 방법: 하루 평균 8시간 이상, 주 3일 이상 콘택트렌즈를 착용하는 대학생들에게 콘택트렌즈 착용과 관련된 건성안설문지(CLDEQ)를 작성하도록 하여 성별, 착용렌즈에 따른 안구증상의 정도를 0점에서 5점 척도로 하여, 건조감과 기타 안구증상들과의 상관성을 알아보았으며 콘택트렌즈로 인해 유발되는 안구증상을 관리하는 방법과 비용 등에 대해 알아보았다. 결과: 콘택트렌즈 착용과 관련된 안구증상의 정도를 점수화한 결과, 안구건조감(dryness) 2.53±0.86점, 안구불편감(discomfort) 2.35±0.81점, 흐려보임(blurry vision)이 2.27±0.86점으로 높게 나왔고 눈부심(light sensitivity) 1.49±0.79점, 작열감(burning/stinging)이 1.43±0.78점으로 낮게 나왔다. 착용시간이 길어질수록 증상이 심해져 건조감은 렌즈착용 2시간 동안 1.81±0.93점에서 렌즈를 제거하기 전에는 3.63±1.13점(t=-27.755, p=0.000)으로 증가하였고 안구불편감은 1.84±1.10점에서 3.28±1.33점(t= -17.897, p=0.000)으로 증가하였다. 안구건조감과 다른 안구증상들 사이에서도 상관성이 있었다. 남자보다 여자에서, 정기교체렌즈나 일회용 렌즈보다는 연속착용렌즈에서 안구증상과 관련된 점수가 높았다. 결론: 건조감이나 안구불편감과 같은 증상이 콘택트렌즈 착용자들에게 흔하게 발생하는 것으로 보여지며 저녁이 될수록 그 증상이 심해지는 것으로 나타났다.

The toxicity of materials derived from seed of Pongamia pinnata Pierre toward to third instar larvae of Aedes aegypti and Culex pipiens pallens was examined using direct contact bioassay. Results were compared with those of the currently used insecticides: fenthion and temephos. The active principles of Pongamia pinnata were identified as the karanjin (1), pongamone (2), palmitic acid (3) and karanjachromene (4), by spectroscopic analysis. Based on 24h LC50 values, karanjin (14.61 and 16.13 ppm) was the most toxic compound but less effective than fenthion (0.0031 and 0.068 ppm) and temephos (0.016 and 0.056 ppm) against Ae. aegypti and Cx p. pallens. Moderate toxicity was produced by pongamone (34.50 and 39.53 ppm), palmitic acid (36.93 and 42.96 ppm), and karanjachromene (43.05 and 48.95 ppm). P. pinnata seed derived materials, particularly karanjin, merit further study as potential mosquito larvicides for the control of mosquito populations in light of global efforts to reduce the level of highly toxic synthetic larvicides in the aquatic environment

The toxicity of materials derived from rhizome of Cnidium officinale Makino to adults from B and Q biotype of Bemisia tabaci was examined using a leaf-dipping bioassay. Results were compared with those of two currently used insecticides: acetamiprid and thiamethoxam. The active principles of C. officinale rhizome were identified as butylidenephthalide (1), ligustilide (2), and 3-butylphthalide (3) by spectroscopic analysis. These compounds exhibited 100% mortality against both B and Q biotype adults at 2.5 mg/ml. At a concentration of 1.25 mg/ml, butylidenephthalide produced 88 and 92% mortality against B and Q biotype adults, respectively. 3-butylphthalide showed 100 and 89% mortality against B and Q type adults, respectively. Ligustilide exhibited 97 and 100% mortality against B and Q type adults, respectively. The toxicity of these compounds to B type adults was almost equal to that of thiamethoxam and acetamiprid, whereas two insecticides exhibited 40% mortality to Q biotype. C. officinale rhizome-derived materials merit further study as potential insecticides for the control of B. tabaci populations due to global efforts to reduce the level of highly toxic synthetic pesticides.