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Tyrosinase Inhibitory Effect of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one Derivatives ((E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one 유도체들의 tyrosinase 활성억제 효과)

  • Lee, Eun Kyeong;Kim, Ju Hyun;Moon, Kyoung Mi;Ha, Sugyeong;Noh, Sang-Gyun;Kim, Dae Hyun;Lee, Bonggi;Kim, Do Hyun;Kim, Su Jeong;Ullah, Sultan;Moon, Hyung Ryong;Chung, Hae Young
    • Journal of Life Science
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    • v.27 no.2
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    • pp.139-148
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    • 2017
  • The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 ($IC_{50}=0.1456{\mu}M$) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid ($IC_{50}=17.2{\mu}M$), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.

Effects of Dietary Supplementation of Coffee Meal on Growth Performance, Blood Biochemical Profiles and Antioxidant Defense System in Broiler Chickens (사료 내 항산화원으로서 커피박 첨가가 닭의 사양성적, 혈액생화학성상 및 항산화 작용에 미치는 영향)

  • Ko, Young-Hyun;Kang, Sun-Young;Jang, In-Surk
    • Korean Journal of Poultry Science
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    • v.39 no.3
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    • pp.223-232
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    • 2012
  • The effects of dietary supplementation of dried coffee meal (CM) on growth performance, blood biochemical profiles, the weights of immune-related organs, and the antioxidant defense system in broiler chicks were examined. A total of 162, 3-day-old male broiler chickens were assigned to three dietary groups: control group (CON), control diet added with 0.5% CM (CM0.5), and control diet added with 1.0% CM (CM1.0). In vitro antioxidant activity test, coffee extracts showed concentration-dependent increase in radical scavenging activity. Dietary addition of 0.5 and 1.0% of CM did not have negative effects on growth performance and feed conversion during the experimental periods, whereas dietary CM significantly (P<0.05) increased the relative weight of thymus without changes in the other organ weights. In addition, birds fed the diet supplemented with CM (0.5 and 1.0%) significantly increased blood albumin without affecting other components including glucose, triglyceride and cholesterol compared with those fed control diet. In antioxidant defense system, the specific activities of superoxide dismutase, glutathione peroxidase and glutathione S-transferase and the level of glutathione in the small intestine and liver were not affected by dietary supplementation of CM. However, hepatic lipid peroxidation in birds fed the diet supplemented with 0.5% CM was significantly (P<0.05) decreased compared with that in control birds. In conclusion, dietary supplementation of CM(0.5~1.0%) has potential for use as a natural antioxidant source without negative effect on growth performance in broiler chickens.

Impact of Environmental Factors on in vitro Interactions and Niche Overlap between Aspergillus ochraceus and other Storage Fungi (Aspergillus ochraceus와 다른 저장균간의 in vitro 상호작용 및 Niche Overlap에 미치는 환경요인의 영향)

  • Lee, Hyang-Burm;Magan, Naresh;Yu, Seung-Hun
    • The Korean Journal of Mycology
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    • v.27 no.4 s.91
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    • pp.283-288
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    • 1999
  • The effect of water activity ($a_w,\;0.9{\sim}0.995$) and temperature ($18{\sim}30^{\circ}$C) on in vitro growth and interactions between ochratoxin-producing Aspergillus ochraceus and six other fungi (Alternaria alternata, Aspergillus candidus, A. flavus, A. niger, Eurotium amstelodami, E. rubrum) isolated from maize grain were investigated. A. ochraceus and each six other species were paired and their interactions given a numerical score to obtain an index of dominance ($I_D$) for each species. Generally A. ochraceus was very competitive and dominant against other fungi. It was, however, dominanted by Alternaria alternata and A. niger at high $a_w\;(0.995\;a_w)$, and mutually antagonistic when paired with E. amstelodami and E. rubrum at low $a_w\;(0.9\;a_w)$. The growth rates of each species were also calculated under the same range of environmental conditions. They were markedly influenced by aw and temperature. At high temperature ($30^{\circ}C$), A. ochraceus grew most rapidly under slightly drier conditions ($0.95\;a_w$), while A. alternata, A. flavus and A. niger did at high water availability level ($0.995\;a_w$). At $18^{\circ}C\;and\;25^{\circ}C$, and high $a_w$ level ($0.995\;a_w$), A. alternata grew fastest, while A. candidus, E. amstelodami and E. rubrum grew very slowly. Using Biolog plates the effect of $a_w$ and temperature on utilization patterns of carbon sources in maize was evaluated. The niche overlap index (NOI) relative to A. ochraceus was determined and compared with that of each interacting species. Under high water available condition ($0.995\;a_w$). the NOI of A. ochraceus was often >0.9, indicative of the coexistence with other interacting species. However, against E. amstelodami and E. rubrum at $18^{\circ}C$, the species had NOI <0.8, indicative of occupation of different niches. At low $a_w\;(0.95\;a_w)$, NOI for A. ochraceus was <0.8 when paired with A. alternata and A. niger also suggested the occupation of different niches.

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Toxicity of lectin extracted from Korean mistletoe (Viscum album coloratum) in piglets and its effects on the immunogenicity of Aujeszky's disease virus vaccines (한국산 겨우살이(Viscum album coloratum)로부터 추출된 lectin의 돼지에 대한 독성 및 오제스키병 백신의 면역원성에 미치는 영향)

  • Yeo, Sang-Geon
    • Korean Journal of Veterinary Research
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    • v.46 no.3
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    • pp.225-234
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    • 2006
  • In the present study toxicity and immunostimulating activity of the lectin(KML-C), which was extracted from Korean mistletoe(Viscum album coloratum) were investigated in swine. To determine the toxicity, lectin was injected into thigh or cervical muscles of 4-week-old piglets(Landrace) and observed clinically and pathologically. For determination of the immnunostimulating activity, lectin($0.7{\mu}g/kg$ of body weight)-adjuvanted vaccine of Aujeszky's disease virus(ADV)(NYJ1-87) which was inactivated by 0.2% formalin was injected into the cervical muscle of antibody-negative piglets in the same age group. Subpopulation of the immune cells and serum neutralizing(SN) antibodies in the piglets were examined after vaccination, and resistance of the piglets against challenge by virulent NYJ1-87 was further examined. The results were also compared with those from piglets injected with aluminum hydroxide [$Al(OH)_3$]-adjuvanted vaccine of inactivated NYJ1-87 and NYJ1-87 vaccine without adjuvant, and the results are as follows. By injection of lectin with $30{\mu}g/kg$ of body weight to the thigh muscle, all of 12 piglets died after signs such as dyspnea, fever, systemic erythema and subcutaneous hemorrhages, and lesions pertaining to poisonous hepatitis and dysfunction of kidney were observed. By injection of lectin with $7{\mu}g/kg$ of body weight to the thigh muscle, all of 12 piglets showed signs such as edema and cutaneous hemorrhage in the injected area, lameness and depression, and lesions pertaining to poisonous hepatitis and dysfunction of kidney were observed. By injection of lectin with 1, 3 and $5{\mu}g/kg$ of body weight to the thigh muscle of each one piglet, signs such as congestion, induration and grayish coloration in the injected area, depression and inappetence were observed in all piglets. Toxic changes were also observed in the liver and kidney of piglets by lectin of 3 and $5{\mu}g$. By injection of lectin with 0.5 and $0.7{\mu}g/kg$ of body weight to the cervical muscle of each 9 piglets, all piglets were clinically normal and there were no significant changes in blood counts and chemistry values. Whereas, epithelial swelling and vacuolation of convoluted tubules were observed from one piglet injected with lectin of $0.7{\mu}g$, and necrosis and fibrosis of muscular fiber were observed in the muscle of one piglet injected with lectin of $0.5{\mu}g$. Only population of sIgM+ B lymphocytes increased among immune cells in all of 15 piglets immunized with lectin($0.7{\mu}g/kg$ of body weight)-adjuvanted vaccine, while compared to those in $Al(OH)_3$-adjuvanted vaccine and vaccine without adjuvant. No additional stimulation to the immune cells was recognized when lectin was added to $Al(OH)_3$-adjuvanted vaccine. In piglets immunized with lectin-adjuvanted vaccine, SN titers in reciprocal values for loge were 1.3-4.0 at 1-4 weeks after vaccination, which was similar to those with 1.0-3.3 by vaccine without adjuvant but lower than those with 2.0-5.7 by $Al(OH)_3$-adjuvanted vaccine. Also, no additional increase in the SN titers was recognized when lectin was added to $Al(OH)_3$-adjuvanted vaccine. Piglets immunized with lectin-adjuvanted vaccine were resistant to challenge by the virulent NYJ1-87 at 4 weeks after vaccination, and the SN titers reached to 5.0 one week after challenge, which was higher than those with 4.0 by vaccine without adjuvant but somewhat lower than those with 7.7 by $Al(OH)_3$-adjuvanted vaccine.

Growth Performance, Immune Response and Carcass Characteristics of Finishing Pigs by Feeding Stevia and Charcoal (스테비아와 숯이 급여된 비육돈의 사양성적, 면역력 및 도체특성)

  • Choi, Jung-Soek;Jung, Dong-Soon;Lee, Ju-Ho;Choi, Yang-Il;Lee, Jae-Joon
    • Food Science of Animal Resources
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    • v.32 no.2
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    • pp.228-233
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    • 2012
  • This study was conducted to determine the effects of stevia (Stevia rebaudiana bertoni) and charcoal supplementation on growth performance, immune response and carcass characteristics of finishing pigs. A total of 420 pigs (LYD) were randomly allocated into 7 treatments with 3 replications. Dietary treatments were 1) T1 (basal diet), 2) T2 (basal diet+0.3% stevia), 3) T3 (basal diet+0.6% stevia), 4) T4 (basal diet+0.3% charcoal), 5) T5 (basal diet+0.6% charcoal), 6) T6 (basal diet+0.3% stevia+0.3% charcoal) and 7) T7 (basal diet+0.6% stevia+0.6% charcoal). During the experimental period, average daily gain (ADG) was higher in T2 and T6 groups than the other treatments (p<0.05). Feed conversion ratio (FCR) was higher in T6 group compared to the others (p<0.05). There were no significant differences in total cholesterol level and glutamic pyruvic transaminase (GPT) activity of blood among treatments. In glutamic oxaloacetic transaminase (GOT) activity, T3, T5, T6 and T7 groups showed lower values (p<0.05) compared to T1. Insulin-like growth factor-1 concentration was higher in T2 and T6 groups than the others (p<0.05), but there were no significant differences in immunoglobulin G, lymphocyte, eosinophil, basophil and atypical lymph levels among treatments. In neutrophil, T6 showed higher level compared to the others (p<0.05). In the carcass characteristics, T6 showed higher level of a carcass grade compared to the other treatments. However, carcass length did not show any significant difference among treatments. As a result, dietary supplementation of 0.3% stevia and 0.3% charcoal showed higher ADG, higher FCR and better immune response resulting in better growth performance and carcass characteristics of finishing pigs.

Quercetin suppress CCL20 by reducing IκBα/STAT3 phosphorylation in TNF-α/IL-17A induced HaCaT cells (TNF-α/IL-17A 유도된 HaCaT 세포주에서 Quercetin의 IκBα/STAT3 인산화 조절에 의한 CCL20 발현 억제)

  • Kim, Mi Ran;Kim, Min Young;Hwang, Hyung Seo
    • Journal of Applied Biological Chemistry
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    • v.63 no.3
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    • pp.211-219
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    • 2020
  • Quercetin is a polyphenol compound with excellent antioxidant and anti-inflammatory activity. However, little has been reported about the efficacy of quercetin to control psoriasis. Thus, we aimed to investigate the effect of quercetin to regulate psoriatic dermatitis with HaCaT cell lines activated by TNF-α and IL-17A, which are in vitro psoriasis skin models. When quercetin was treated with TNF-α-activated HaCaT cell line, inflammatory cytokine expressions such as IL-1α, IL-1β and IL-6 were reduced by 49.1±7.14, 42.8±8.16, and 34.5±2.52%, respectively. In addition, mRNA expression levels of IL-8 and CCL20 the chemokines that attract immune cells such as Th17 cells and dendritic cells to the inflammatory reaction site, were also reduced by 38.4±5.83 and 52.9±4.59% compared to the TNF-α treatment group. The expression of proteins KRT6A and KRT16, which was nonspecifically increased in psoriatic skin was also significantly suppressed. Moreover, phosphorylation of IκBα and STAT3 proteins activated by TNF-α was also significantly inhibited. After stimulating the HaCaT with IL-17A, known as another psoriasis-inducing cytokine, it was observed that IκBα mRNA expression decreased by 55.8±5.28%, and STAT3 phosphorylation was downregulated by 36.3±6.81%. Finally, after co-activation by TNF-α/IL-17A, quercetin inhibited all of IL-1α, IL-1β, IL-6, TNF-α and CCL20 gene expression. The above results strongly suggest that quercetin is a material that has not only anti-oxidant and anti-inflammatory activities, but also has an activity in improving psoriasis.

Angiotensin Converting Enzyme Inhibition and Antihypertensive Effects of Phyllostachys pubescens Culm Extracts in Spontaneously Hypertensive Rats (맹종죽 줄기 추출물을 투여한 본태성 고혈압 쥐(SHR)의 ACE 저해 활성 및 혈압 강하 효과)

  • Kim, Jung-Suk;Kim, Mi-Jeong;Park, Min-Hee;Ryu, Bog-Mi;Moon, Gap-Soon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.1
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    • pp.27-34
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    • 2008
  • This study investigated the anti-hypertensive effect of Phyllostachys pubescens culm extract (PCE) by examining its effects on renal angiotensin-converting enzyme (ACE) inhibition and blood pressure using the spontaneously hypertensive rat (SHR) system. Systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured weekly for 8 weeks. Also, total antioxidant capacity and protein oxidation of tissues were examined by plasma Trolox Equivalent Antioxidant Capacity assay (TEAC) and hepatic protein carbonyl values, respectively. Twenty male SHR were randomly divided into four groups: PCE50, PCE100, and PCE500 (50, 100, and 500 mg of PCE per kilogram bodyweight daily, respectively), and control group. At week 2, the SBP in all PCE groups appeared to be significantly lower than the control (p<0.05), whereas the DBP were not different until week 4 (p<0.05). At week 8, SBP in the PCE500 was lower by 20% than the control. PCE groups considerably suppressed ACE dose-dependently compared with the control. Plasma TEAC and hepatic protein carbonyl values indicated increased antioxidative activity due to the PCE feed. No adverse effect was observed on the liver of SHR as there was no difference for the GOT and GPT values among the groups. Results of this study suggest that ACE inhibition may be one possible mechanism for the blood pressure lowering effect of PCE; thus, long term consumption of PCE may be beneficial in preventing high blood pressure along with the increased antioxidative status.

The effect of Ca-P coatings of anodized implant surface on response of osteoblast-like cells in vitro (임플란트 표면의 Ca-P 코팅 방법이 MG63 골모유사세포 반응에 미치는 영향에 대한 in vitro 연구)

  • Kim, Il-Yeon;Jung, Sung-Min;Hwang, Soon-Jung;Shin, Sang-Wan
    • The Journal of Korean Academy of Prosthodontics
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    • v.47 no.4
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    • pp.376-384
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    • 2009
  • Purpose: The purpose of this study was to evaluate the response of osteoblast-like cells to Ca-P coated surface obtained via Ion beam-assisted deposition (IBAD) method and Sol-Gel process on anodized surface by cellular proliferation and differentiation. Material and methods: The surface of a commercially pure titanium (Grade IV) discs with dimension of 10mm diameter and 2 mm thickness was modified by anodic oxidation under a constant voltage of 300 V. The experimental groups were coated with Ca-P by the IBAD method and Sol-Gel process on anodized surface. The surface roughness (Ra) of specimens was measured by optical interferometer and each surface was examined by SEM. To evaluate cell response, MG63 cells were cultured and cell proliferation, ALP activity and the ability of cell differentiation were examined. Also, cell morphology was examined by SEM. The significant of each group was verified by Kruskal-Wallis Test ($\alpha$=.05). Results: The Ra value of Ca-P coated surface by IBAD method was significantly higher than Ca-P coated surface by Sol-gel process (P < .05). The level of cell proliferation and ALP activity was higher in Ca-P coated surface by IBAD method (P<.05). The expression of ALP showed higher level expression in Ca-P coated surface by IBAD method. Cells grown on Ca-P coated surface by IBAD method were uniformly distributed and developed a very close layer. Conclusion: These experiments showed better performances of Ca-P coated surface by IBAD method with respect to Ca-P coated surface by Sol-gel process. Ca-P coated surface by IBAD method appear to give rise more mature osteoblast characteristics and might result in increased bone growth and bone-implant contact.

Peptide Properties of Rapid Salted and Fermented Anchovy Sauce Using Various Pretenses 1. Hydrolysis of Anchovy Sauce and Actomyosin by Various Pretenses (단백질 분해효소를 이용하여 제조한 속성 멸치 액젓의 펩티드 특성 1. 단백질 분해효소에 의한 멸치 액젓 및 Actomyosin의 가수분해)

  • KIM In-Soo;CHOI Young-Joon;HEU Min-Soo;CHO Young-Je;IM Yeong-Sun;GU Yeun-Suk;YEO Saeng-Gyu;PARK Jae-Woon
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.32 no.4
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    • pp.481-487
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    • 1999
  • The optimal conditions of enzymatic hydrolysis for preparation of rapid salted and fermented anchovy sauce (SFAS) using various pretenses such as trypsin, chymotrypsin, crude enzyme from squid liver and viscera, Alcalase, Neutrase and Protamex were studied. SFAS prepared with squid viscera had higher level of VBN (173.6 mg/100 g) when stored for 70 days than other samples, and peroxide values were almost equal among all samples during fermentation period. Total amino acids and nonprotein nitrogenous compounds remarkably increased as SFAS treated with Alcalase or Protamex which exhibited higher the hydrolysis rate of $57\%$ at 60 day than others. The optimal pHs of trypsin, chymotryosin, Alcalase, Neutrase and Protamex on anchovy actomyosin were 7.5, 6.5, 6.5, 7.0 and 5.0, respectively. Optimal temperatures of trypsin, chymotryosin, Alcalase and Neutrase were 55, 45, 60 and $55^{\circ}C$, respectively. Otherwise, Protamex activity increased as temperature increased from 20 to $70^{\circ}C$. Protamex had higher $K_m$ (3.545) and $V_{max}$ value (2.688) than others. Protamex affected less by NaCl had $52.5\%$ activity at the fermentation condition of $20^{\circ}C$ and $25\%$ NaCl. Protamex appeared to be very effective for the hydrolysis of crude actomyosin from ancnovy.

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Antibacterial Effect of Hiscus cannabinus L. Methanol Extract against Pathogenic Bacteria in Domestic Animals (Kenaf methanol 추출물의 가축 주요 병원성 균에 대한 항균효과)

  • Lim, Jeong-Ju;Kim, Dong-Hyeok;Lee, Jin-Ju;Kim, Dae-Geun;Lee, Hu-Jang;Min, Won-Gi;Park, Dong-Jin;Huh, Moo-Ryong;Chang, Hong-Hee;Rhee, Man-Hee;Kim, Suk
    • Journal of agriculture & life science
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    • v.45 no.2
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    • pp.43-50
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    • 2011
  • Hibiscus cannabinus L. is a plant in the Malvaceae family, that was seeded at June 1st in 2010 and harvested at November 18th. The present study was designated to investigate the safety for host cells, antibacterial effects of Hibiscus cannabinus L. of flower (HCME-F) or leaf (HMEF-L) methanol extract for typical Gram's positive bacteria (St. aureus and Str. epidermidis) or Gram's negative bacteria (S. typhimurium and E. coli). In treatment of different concentrations of HCME-F or HMEF-L (1, 50 and $100{\mu}g/ml$), cytotoxic effects were not shown to RAW 264.7 cells until 24 h incubation. In determination of antibacterial activity of HCME-F or HMEF-L, the antibacterial activities for St. aureus and Str. epidermidis were markedly increased compared to that of untreated control group, but antibacterial activity of HCME-F or HMEF-L for S. typhimurium and E. coli were not changed. Taken together, we demonstrated that methanol extract of HCME-F or HMEF-L showed the safety for RAW 264.7 cells and antibacterial activities for Gram's positive pathogenic bacteria St. aureus and Str. epidermidis. These findings suggest that a methanol extract of Kenaf flower or leaf may be useful alternatives of conventional chemotherapies for dermatitis and mastitis causing Gram's positive pathogens such as Stapylococcus spp. and Streptococcus spp. in domestic animals and humans.