• Asian Pacific Journal of Cancer Prevention
• /
• 제13권5호
• /
• pp.2009-2014
• /
• 2012

Objective: Taspine, isolated from Radix et Rhizoma Leonticis has demosntrated potential proctiective effects against cancer. Tas13D, a novel taspine derivative synthetized by structure-based drug design, have been shown to possess interesting biological and pharmacological activities. The current study was designed to evaluate its antiproliferative activity and underlying mechanisms. Methods: Antiproliferative activity of tas13D was evaluated by xenograft in athymic mice in vivo, and by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) and cell migration assays with human liver cancer (SMMC-7721) cell lines in vitro. Docking between tas13D and VEGFR and EGFR was studied by with a Sybyl/Surflex module. VEGF and EGF and their receptor expression was determined by ELISA and real-time PCR methods, respectively. Results: Our present study showed that tas13D inhibited SMMC-7721 xenograft tumor growth, bound tightly with the active site of kinase domains of EGFR and VEGFR, and reduced SMMC-7721 cell proliferation (IC=34.7 ${\mu}mol/L$) and migration compared to negative controls. VEGF and EGF mRNAs were significantly reduced by tas13D treatment in a dose-dependent manner, along with VEGF and EGF production. Conclusion: The obtained results suggest that tas13D inhibits tumor growth and cell proliferation by inhibiting cell migration, downregulating mRNA expression of VEGF and EGF, and decreasing angiogenic factor production. Tas13D deserves further consideration as a chemotherapeutic agent.

• 한국작물학회:학술대회논문집
• /
• 한국작물학회 2022년도 추계학술대회
• /
• pp.284-284
• /
• 2022

The overall effects of gibberellic acid (GA3) with NaCl on different rice genotypes are inadequately understood. The present study determines the effect of different GA3 concentrations on the morphophysiological, molecular and biochemical effects of 120 mM NaCl salt stress in rice seedlings. Salt stress reduced germination percentages and seedling growth and decreased bioactive GA content. It also downregulated the relative expression of a-amylase-related genes - OsAmy1A, OsAmy1C, and OsAmy3C in the salt-sensitive IR28 cultivar. Salt stress differentially regulated the expression of GA biosynthetic genes. Salt stress increased antioxidant activity in all rice genotypes tested, except in IR28. GA3 (50 and 100 µM) mitigates the effect of salt stress, rescuing seed germination and growth attributes. GA3 significantly increased bioactive GA content in Nagdong and pokkali (50 µM) and Cheongcheong and IR28 (100 µM) cultivars. The a-amylase genes were also significantly upregulated by GA3. Similarly, GA3 upregulated OsGA2oxl and OsGA2ox9 expression in the Cheongcheong and salt-sensitive IR28 cultivars. The present study demonstrated that salt stress inactivates bioactive GA - inhibiting germination and seedlings growth - and decreases bioactive GA content and GSH activity in IR28 and Pokkali cultivars. Further, GA3 significantly reversed the effects of 120 mM NaCl salt stress in different rice genotypes. The current study also suggests if we know the coastal area water NaCl concentration we can apply the exogenous GA3 accordingly. Thus, we would be able to grow rice cultivars near the coastal area and reduce the rice damage by salinity.

• The Plant Pathology Journal
• /
• 제25권4호
• /
• pp.352-360
• /
• 2009

The potential of three plants extracts, to protect potato plants against bacterial wilt caused by Ralstonia solanacearum was determined under greenhouse and field conditions. All soil drenching treatments of aqueous plant extracts of Hibsicus sabdariffa, Punica granatum and Eucalyptus globulus significantly reduced the disease severity compared with inoculated control. Although the applications of all three plant extracts resulted in similar reductions of disease severity in field up 63.23 to 68.39%, treatment of E. globulus leaf extract was found greater in restricting the symptom development than other the two plant extracts in the greenhouse. More than 94% reduction in the bacterial wilt symptom was observed in potato plants. All tested plant extracts were effective in inhibiting the growth of bacterial pathogen, not only in vitro, but also in stem of potato plants as compared with the inoculated control Potato plants treated with extract of H. sabdariffa reduced bacterial growth more effectively than treatment with P. granatum and E. globulus. Activity of defence-related enzymes, including peroxidase, polyphenoloxidase and phenylalanine ammonia lyase, were significantly increased in plants treated with the plant extracts compared to the control during the experimental period. In general, the higher enzymes activities were determined in both inoculated and non-inoculated treated potato plants after 8 days from plant extracts treatment. These results suggested that these plant extracts may be play an important role in controlling the potato bacterial wilt disease, through they have antimicrobial activity and induction of systemic resistance in potato plants.

• International Journal of Oral Biology
• /
• 제44권4호
• /
• pp.152-159
• /
• 2019

The oral care probiotic strain Weissella cibaria CMU (oraCMU) inhibits volatile sulphur compounds associated with halitosis, presumably by inhibiting the growth of associated oral pathogens. In the present study, we investigated whether oraCMU inhibits the production of these compounds by suppressing the expression of mgl. This gene encodes L-methionine-α-deamino-γ-mercaptomethane-lyase (METase) and is involved in the production of methyl mercaptan (CH₃SH) by Porphyromonas gingivalis. Therefore, we specifically investigated the effects of oraCMU on the growth, CH₃SH production, METase activity, and mgl expression of P. gingivalis. The minimum inhibitory concentrations of cell-free supernatant and secreted proteins from oraCMU were 125 mg/mL and 800 ㎍/mL, respectively. At sub-minimum inhibitory concentration levels, these metabolites inhibited CH₃SH production, but they also reduced P. gingivalis viability. Only heat-killed oraCMU decreased CH₃SH production without affecting P. gingivalis viability. Heat-killed oraCMU also inhibited METase activity toward L-methionine and mgl mRNA expression (p < 0.05). In summary, we demonstrated the inhibition of volatile sulphur compounds via the antimicrobial action of oraCMU and, for the first time, the inhibition of such compounds by heat-killed oraCMU, which occurred at the molecular level.

• 미생물학회지
• /
• 제51권2호
• /
• pp.177-180
• /
• 2015

Bordetella bronchiseptica에 의한 돼지위축성비염과 Salmonella gallinarum에 의한 가금티푸스 방지 방법을 찾기 위해서 두 세균병원체에 항균활성을 갖는 세균 균주를 축산농가의 여러 시료로부터 분리하였다. 분리균주 372개 중 TK3 균주가 두 병원체에 대해 가장 우수한 항균활성을 나타내었으며, 16S rRNA 염기서열 분석 결과 Bacillus amyloliquefaciens로 동정되었다. B. amyloliquefaciens TK3는 siderophore, rhamnolipid와 antimicrobial peptide 같은 항균물질을 분비하여 두 병원체의 생장을 저해할 수 있었다. TK3 균주는 Chrome azurol S 한천 평판에서 siderophore 생성반지름이 14일 배양 후 0.53 cm이었으며, King's B 배지에서 1.06 mmol/ml의 siderophore를 생성하였다. 또한 82.4 mg/L의 rhamnolipid를 분비하였으며, LB배지에 $30{\mu}l/ml$ 농도의 추출된 antimicrobial peptide 첨가 시 두 병원체의 생장을 완전히 저해하였다.

• 한국식품과학회지
• /
• 제5권1호
• /
• pp.33-35
• /
• 1973

대두(大豆)를 침지(浸漬)후 $100^{\circ}C$에서 2분간 가열하면 불쾌한 풋 냄새의 발생을 충분히 억제할 수 있다. 건조한 대두(大豆)의 경우는 $100^{\circ}C$에서 3분간 가열하면 같은 효과를 나타낸다. 이와 같은 간단한 열처리(熱處理)는 병아리 사육시험의 결과 발육조해인자(發育阻害因子)를 불활성화(不活性化)시키기에는 불충분하다. 이취(異臭)의 조해(阻害)는 lipoxygenase 활성(活性)의 상실과 일치하며 이것이 그 원인인 것으로 생각된다.

• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2003년도 춘계학술대회 논문집
• /
• pp.95.2-95
• /
• 2003

Ketoconazole is a well-studied drug that blocks fungal growth and testosterone synthesis in humans and rodents by inhibiting the activity of cytochrome P-450 enzymes. But there were no reports that ketoconazole affects on enzymes related to degradation of testosterone. Aromatase converts testosterone to estradiol. Change of aromatase protein level may destroy hormone homeostasis. (omitted)

• 약학회지
• /
• 제46권3호
• /
• pp.203-207
• /
• 2002

The antifungal activities of the essential oils from Anthemis nobilis, Ciderus atlantica, Juniperus communis, Lavandula angustifolia, Pelargonium graveolens, Pogestemon patchouli, Rosmarinus officinalis, and Styrax tonkinensis which are recommended for the treatment of microbial infections in aromatherapy and complementary medicines were tested against Candida spp. The activities were measured by broth dilution method and disk diffusion assay. Most of the test oils inhibited growth of Candida albicans, C. utilis and C. tropicalis. Especially, the essential oil from Pelargonium graveolens and its main component, citronellol showed the strongest activity among the herbs except benzoic acid from Styrax tonkinensis which is well-known antimicrobial compound. As a result of checkerboard microtiter test. synergistic effect of citronellol, was shown when the component was combinated with ketoconazole, displaying a fractional inhibiting concentration (FIC) index of 0.37 against C. albicans.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.359.2-359.2
• /
• 2002

In the previous study, we reported that 2'-hydroxy-4'-methxoychalcone, synthetic chalcone inhibited PGE2 production in TPA- stimulated rat peritoneal macrophages by inhibiting the induction of COX-2 protein. The present study was carried out to clarify whether 2'-hydroxy-4'-methoxychalcone inhibit angiogenesis by the experimental methods in vitro and in vivo. 2'-Hydroxy-4'-methoxychalcone decreased angiogenesis of both chick embryos in the chorioallantoic membrane assay and basic fibroblast growth factor-induced vessel formation inthe mouse Martigel plug assay. (omitted)

• 한국식품영양과학회지
• /
• 제41권2호
• /
• pp.261-269
• /
• 2012

본 연구에서 18종의 한약재추출물을 제조하여 병원성세균에 대한 한약재의 항균활성을 측정하였다. 오배자, 오미자 및 소목 메탄올 추출물은 대부분 균주에 대해 5 mg/mL 수준에서 항균활성을 나타냈으나 15여 종의 한약재추출물들은 30 mg/mL 수준에서 항균활성을 나타냈다. 오배자의 S. epidermidis와 Bor. bronchiseptica에 대한 최소저해농도는 0.6 mg/mL로 나타났다. 우수한 항균활성이 확인된 오배자, 소목, 오미자, 황금을 대상으로 극성이 다른 5가지 용매로 순차 분획하여 항균활성을 검토한 결과 대부분의 균주에서 EtOAc층이 다른 분획층에 비해 성장억제효과가 높게 나타났다. 항균력이 우수한 한약재추출물의 미생물 증식억제 효과를 조사하기 위해 증식배지에 0, 100, 300 및 500 ppm의 메탄올 추출물을 첨가하였다. 한약재 추출물을 첨가하지 않은 대조구에서는 12시간 이후 급격한 균의 성장을 나타내고 있으나 오배자와 소목추출물의 첨가 농도가 높을수록 그람 양성균인 S. aureus, S. epidermidis 및 L. monocytogenes는 뚜렷한 억제효과를 나타냈다. 오배자추출물은 그람음성균인 Sal. Pullorum과 Sal. Choleraesuis의 성장을 저해하였고 Bor. bronchiseptica, E. coli serotype $O_8$은 오배자와 소목추출물은 낮은 농도에서 성장이 다소 저해되었음을 보여주었고, 추출물의 농도가 높을수록 균의 성장이 강하게 억제되었다.