Flavonoid myricetin, usually found in tea and medicinal plants, has antioxidant and anti-inflammatory effects. Our objectives in this study were to verify the effects of myricetin on periodontal ligament fibroblasts (PDLFs) under inflammatory conditions and to observe its effects on osteoclast generation and on cytokine expression in RAW264.7 cells. To determine the effects of myricetin on PDLFs, we examined the expression and activity of proteolytic enzymes, including MMP-1, MMP-2, and MMP-8, which all play an important role in chronic periodontitis. We observed the effects of myricetin on intracellular signal transduction to verify the molecular mechanism involved. By measuring the formation of TRAP–positive multinucleated cells and the expression and activity of MMP-8, we were able to assess the effects of myricetin on osteoclast generation. In addition, by measuring the secretion of IL-6 and NO, we could evaluate the effects of myricetin on inflammatory mediators. We found that Myricetin had no effect on the viability of the PDLFs in the presence of inflammation, but it did decrease both the expression of MMP-1 and MMP-8 and the enzyme activity of MMP-2 and MMP-8 in these fibroblasts. Myricetin also decreased the lipopolysaccharide-stimulated phosphorylation of JNK, p38 signaling, IKKB, AKT, and p65RelA in the PDLFs. In the RAW264.7 cells, myricetin inhibited both the expression and the activity of MMP-8. Furthermore, Myricetin not only suppressed the generation of LPS-stimulated osteoclasts, but it also slightly inhibited LPS-stimulated degradation of IkB and decreased the release of LPS-induced IL-6 and NO. These findings suggest that myricetin alleviates the tissue-destructive processes that occur during periodontal inflammation.

We evaluated the larvicidal activity of 12 Apiaceae plant essential oils and their components against the Asian tiger mosquito, Aedes albopictus, and the inhibition of acetylcholine esterase with their components. Of the 12 plant essential oils tested, ajowan (Trachyspermum ammi), caraway seed (Carum carvi), carrot seed (Daucus carota), celery (Apium graveolens), cumin (Cuminum cyminum), dill (Anethum graveolens), and parsley (Petroselinum sativum) resulted in >90% larval mortality when used at 0.1 mg/mL. Of the compounds identified, α-phellandrene, α-terpinene, p-cymene, (-)-limonene, (+)-limonene, γ-terpinene, cuminaldehyde, neral, (S)-+-carvone, trans-anethole, thymol, carvacrol, myristicin, apiol, and carotol resulted in >80% larval mortality when used at 0.1 mg/mL.

Cystatins (CSTs) are reversible and competitive inhibitors of C1A cysteine proteases, corresponding to papain-like cathepsins in plants and animals. A viral CST (CpBV-CST1) was identified from a polydnavirus, Cotesia plutellae bracovirus. Our previous study indicated that overexpression of CpBV-CST1 interfered with immune response and development of Plutella xylostella larvae. This study produced a recombinant CpBV-CST1 protein (rCpBV-CST1) using bacterial expression system to analyze its inhibitory activity against cysteine protease and physiological role in the parasitism of an endoparsitoid wasp, Cotesia plutellae. The open reading frame (ORF) of CpBV-CST1 encodes a polypeptide of 138 amino acids (15 kDa). rCpBV-cystatin protein in BL21 STAR (DE3) competent cells containing a recombinant pGEX4T-3:CpBV-CST1 was overexpressed by 0.5 mM IPTG for 4 h. In biological activity assay, partially purified GST-fused rCpBV-CST1 showed inhibitory activity against papain. It also inhibited larval development of P. xylostella in a dose-dependent manner. These results suggest that CpBV-CST1 plays a role in retardation of larval development of P. xylostella during parasitism.

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.

본 연구에서는 기능성 식품 및 화장품 소재로써 갈색 느티만가닥버섯(Hypsizygus marmoreus)의 이용가능성을 조사하기 위해서 갈색 느티만가닥버섯 메탄올 추출물의 항산화 활성 및 tyrosinase 저해 효과를 갓(pileus)과 대(stipes)로 분리하여 부위별로 조사하였다. 메탄올 추출물 중 갓과 대의 총 폴리페놀 함량은 각각 8.7±3.27ug/mg과 5.6±2.85ug/mg이었고플라보노이드 함량은 각각 2.8±3.81ug/mg과 1.4±1.95ug/mg이었으며 총 폴리페놀과 플라보노이드 함량 모두 대보다 갓에서 높게 나타났다. Tyrosinase 저해 활성은 추출물의 농도에 따라 증가하는 경향을 나타내었으나 양성 대조구로 사용한 2% 알부틴(arbutin)과 비교했을 때 1200mg/ml의 고농도에서도 갓은66.9%, 대는 57.97%의 낮은 저해 활성을 나타내었다.항산화 활성은 DPPH에 의한 라디칼소거 활성을 측정하여 확인하였으며 갓과 대의 DPPH 라디칼 소거능은 20mg/ml의 농도에서도 각각 52.55%와 30.35%로 낮게 나타났다. 추출물이 B16BL6 mouse melanomacell에 미치는 영향을 알아보기 위해 WST-1 assay (4-[3-(4-iodophenyl)-2-(4-nitrophenyl)-2H-5-tetrazolio]-1,3-benzene disulphonate)를 이용하여 세포생존율을 조사하였으며 갓과 대 모두 200-2,000ug/ml의 농도로처리하였을 때 100% 이상의 생존율을 나타내었고추출물의 처리 농도가 증가함에 따라 세포생존율도증가하는 경향을 나타내었으며 양성대조군인 0.04%adenosine을 처리한 경우보다 높게 나타났다.

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.

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.

Considering the dearth of information regarding the medicinal properties of Luffa cylindrica, we assessed the antioxidative, antimutagenic and hyperplasia inhibitory activity of cancer cells from Luffa cylindrica extracts by employing biological and biochemical assays. Ethanol extracts of Luffa cylindrica inhibited MDA-BSA (malondialdehyde-bovine serum albumin) conjugation reaction (66.38±2.65), DPPH (1, 1-diphenyl-2-picryl-hydrazyl) radical production (60.13±0.42) and lipid peroxidation (56.04±3.24). In this study, Luffa cylindrica is believed to exert possible antioxidative effects. The direct and indirect antimutagenic effects of the ethanol extracts of Luffa cylindrica were examined by the Ames test using Salmonella typimurium TA98 and TA100. The inhibitory effects on indirect and direct mutagenicity shows an weak tendency, particularly in direct mutagenicity mediated by 2-nitrofluorene in Salmonella typimurium TA98 (5.82±5.74) and in indirect mutagenicity mediated by 2-anthramine in Salmonella typimurium TA100 (5.76±2.15). The ethanol extracts of Luffa cylindrica on cancer cell hyperplasia inhibitory activity via MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5 diphenyltetrazolium bromide) assay exerted cytotoxic effects on Hela cells (55.83±3.83) and MCF-7 cells (33.03±2.09), which were used in this study. Based on these results, it believed that the ethanol extracts of Luffa cylindrica have antioxidative capacities as well as hyperplasia inhibitory activity of cancer cells. Furthemore, Luffa cylindrica is a candidate for the prevention and dietetic treatment of chronic diseases and for the development of functional food.

The mushrooms have been used as traditional medicines and food resources in many countries. The objective of this study was to determine antioxidant compounds and to evoluate tyrosinase inhibitory activity of extracts from Hypsizigus marmoreus. The pileus and stipe of Hypsizigus marmoreus were extracted with methanol and water, separately. The methanol extract of Hypsizigus marmoreus were fractioned by hexane, chloroform, ethylacetate and buthanol. The concentrations of total polyphenolics and flavonoids in methanol extracts were investigated by colorimetric methods. The concentrations of total polyphenolics and flavonoids in methanol extract of the pileus was higher than methanol extract of the stipe. The DPPH redical scavenging activity of the pileus extract was also higher than stipe extract in methanol extract. The IC50 of DPPH redical scavenging activity of the pileus and stipe in methanol extract were 18 mg/ml and 1 10 mg/ml, respectively. The IC50 of tyrosinase inhibitory activity of the pileus and stipe in methanol extract were 500 mg/ml and 1,000 mg/ml in methanol extract. These results suggest that Hypsizigus marmoreus can be potentially used as a source of natural antioxidant agent in the cosmetic industry as well as the food, pharmaceutical and medicinal industry.

We examined the effects of biological activity Phellinus linteus mycelium culture with cassiae semen extract. Firstly, the optimal temperature, initial pH and culture period for mycelial growth in a liquid culture of P. linteus were determined, and they were 30℃, pH 5.0 and 8 days respectively. The five herbal materials were examined against several health functional efficacies, and, as a result, Cassiae semen was chosen, with its superior inhibitory effects in β-glucuronidase inhibitory activity, electron donating activity, ACE inhibitory, and α-glucosidase inhibitory activities(95.3%, 80.9%, 96.1 and 24.2%, respectively). P. linteus fruit body was investigated on β-glucuronidase inhibitory activity, electron donating activity, ACE inhibitory, and α-glucosidase inhibitory activities, and they were 54.7%, 81.9%, 30.0% and 20.1%, respectively. Accordingly, C. semen was used in the following experiment, to give an additive functional effect on the P. linteus. As the amount of C. semen in the cultural media increased, mycelial weight and β-glucan contents also increased, but final pH was not influenced. In addition, the β-glucuronidase inhibitory activity, electron donating activity, and α- glucosidase inhibitory activity increased. P. linteus mycelium culture showed higher activities in the other three tests above, except for electron donating activity, when C. semen was added to the medium before cultivation.

A series of novel diaryl ether analogs possessing gallate moiety were synthesized and NF-κB inhibitory activity and cytotoxicity were evaluated. NF-κB luciferase activities in prostate LNCaP and colon cancer HCT116 cells showed that 2a, 2c, 2d, 2g, and 2i had potent to moderate inhibitory activities. In addition, 2a exerted more potent cytotoxicity than the reference compound, obovatol, against prostate (LNCaP and PC-3) and colon cancer (HCT116 and SW620) cells.

An endoparasitoid wasp, Cotesia plutellae parasitized young larvae of diamondback moth, Plutella xylostella. Parasitized larvae exhibit sign ificant immunosuppression and fail to metamorphose to pupal stage. Especially, during last instar of parasitized P.xylostella, massive nutrients divert from host to wasp development. CpBV15α ,a host translation inhibitory factors encoded in C. Plutella bracovirus(CpBV), plays a crucial role in suppressing host usage of amino acids. Its promoter analysis shows that CpBV15α specifically inhibit host development in late larval period. To understand its inhibitory target, its specific expression was performed in non-parasitized P. xylostella by in vivo transient expression technique. Total plasma proteins were analyzed by 2D gel electrophoresis and determined target genes inhibited by CpBV15α. Immunoprecipation of cellular extract with CpBV15α antibody captured eIF2B. CpBV15α shares sequence homology with eIF5, especially at its eIF2B-binding region. Our results suggest that CpBV15α may sequester eIF2B, which result in malfunctioning of eIF2 cycling to form a translation initiation complex.