• Title/Summary/Keyword: inhibitory effects

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Inhibitory Effects of 12 Ginsenosides on the Activities of Seven Cytochromes P450 in Human Liver Microsomes

  • Jo, Jung Jae;Shrestha, Riya;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • v.7 no.4
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    • pp.106-110
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    • 2016
  • Ginseng, a traditional herbal drug, has been used in Eastern Asia for more than 2000 years. Various ginsenosides, which are the major bioactive components of ginseng products, have been shown to exert numerous beneficial effects on the human body when co-administered with drugs. However, this may give rise to ginsenoside-drug interactions, which is an important research consideration. In this study, acassette assay was performed the inhibitory effects of 12 ginsenosides on seven cytochrome P450 (CYP) isoforms in human liver microsomes (HLMs) using LC-MS/MS to predict the herb-drug interaction. After incubation of the 12 ginsenosides with seven cocktail CYP probes, the generated specific metabolites were quantified by LC-MS/MS to determine their activities. Ginsenoside Rb1 and F2 showed strong selective inhibitory effect on CYP2C9-catalyzed diclofenac 4'-hydroxylation and CYP2B6-catalyzed bupropion hydroxylation, respectively. Ginsenosides Rd showed weak inhibitory effect on the activities of CYP2B6, 2C9, 2C19, 2D6, 3A4, and compound K, while ginsenoside Rg3 showed weak inhibitory effects on CYP2B6. Other ginsenosides, Rc, Rf, Rg1, Rh1, Rf, and Re did not show significant inhibitory effects on the activities of the seven CYPs in HLM. Owing to the poor absorption of ginsenosides after oral administration in vivo, ginsenosides may not have significant side effects caused by interaction with other drugs.

Experimental Studies on the Antidiarrheal Effects of Anjang-san

  • Oh, Seung-Whan;Ryu, Bong-Ha
    • The Journal of Korean Medicine
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    • v.32 no.6
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    • pp.54-66
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    • 2011
  • Objectives: The purpose of the present study was to investigate the antidiarrheal effects of Anjang-san in mice and rats. Methods: We measured the content of condensed tannin in Anjang-san extract, and observed the effects of Anjang-san on the small intestinal and colonic transport of mice, as well as on mice models of diarrhea induced by castor oil and $MgSO_4$, and on rat models of castor oil-induced enteropooling. Results: Anjang-san showed significant inhibitory effects on abnormally increased small intestinal transit induced by pyridostigmine and neostigmine, and inhibitory effects on large intestinal transit. Anjang-san also exhibited antidiarrheal effects on diarrhea induced by $MgSO_4$, and inhibitory effects on castor oil-induced enteropooling. Anjang-san also improved castor oil-induced diarrhea based on simple numbers without statistical significance. Conclusion: These results demonstrate that Anjang-san has significant antidiarrheal properties and attests to its possible utility in functional diarrheas, irritable bowel syndrome and other gastrointestinal disorders based upon further studies.

A Study on Inhibitory Activities on Carbohydrase and Anti-Inflammatory Activities of Hot-Water and Ethanol Extracts from Immature Dried Bitter Melon (Momordica charantia L.) (미숙과 건여주(Momordica charantia L.) 열수 및 에탄올 추출물의 탄수화물 분해효소 저해 활성 및 항염증 활성에 대한 연구)

  • Nam, Seung-Woo;Kim, Meera
    • Journal of the East Asian Society of Dietary Life
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    • v.25 no.6
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    • pp.999-1006
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    • 2015
  • Bitter melon (Momordica charantia L.) has been used as a medicinal plant due to its biological activity. This study investigated the inhibitory effects on carbohydrase and anti-inflammatory effects of hot-water extract (WEM) and ethanol extract (EEM) from dried bitter melon cultivated in Korea. The inhibitory activities of EEM against ${\alpha}$-amylase and ${\alpha}$-glucosidase were over 70% at 4,000 ppm. The inhibitory activities of EEM were significantly higher than those of WEM at all concentrations. The anti-inflammatory effects were evaluated by measuring nitric oxide (NO) production in LPS-stimulated RAW264.7 cells. EEM did not show cytotoxicity on RAW264.7 cells at the test concentrations. Moreover, the inhibitory effect on NO production in LPS-stimulated RAW264.7 cells was significantly increased by the addition of EEM. These findings suggest that EEM has good inhibitory effect on carbohydrase and anti-inflammatory activity and it has potential as a source of natural functional material.

EFFECT OF ZIZYPHI FRUCTUS EXTRACT ON THE BIOLOGICAL ACTIVITY OF GINGIVAL FIBROBLAST (대조 추출물분획이 치은 섬유아세포의 생물학적 활성화에 미치는 영향)

  • Yang, Chang-Ho;Lee, Yong-Moo;Cho, Ki-Yeong;Bae, Ki-Hwan;Chung, Chong-Pyoung
    • Journal of Periodontal and Implant Science
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    • v.24 no.1
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    • pp.144-154
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    • 1994
  • Final goal of periodontal treatment is to reconstruct the destructed periodontal tissue as well as to remove the necrotic pathologic elements. The purpose of this study is to investigate on the effect of Zizyphi extract to the inhibitory ability on collagenolytic activity of P gingivalis, biologic activity of gingival fibroblasts, and on the collagen and protein synthesis of gingival fibroblasts. Gingival fibroblast from giniva of first bicuspids from patient for orthodontic treatment were used and cultured. For the measurement of inhibitory ability of collagenolytic activity, crude enzyme was extracted and used on the basis of modified Ono's method. On the inhibition of collagenolytic enzyme from herbal extracts, collagenokit CLN-100 were used. The cellular activity of gingival fibroblast, were studied using MTT solution and measured optical density on 570mm by ELISA reader. To measure the effects on the ability of whole protein and collagen synthesis, cell membrane was destructed with ultrasonic grinder after culturing, centrifuged and counted by liquid scintilation counter. The inhibitory effects on producing of $IL-l{\beta}$ by monocyte, after promotion of producing $IL-l{\beta}$ by LPS, were compared with the mixture of herbal extracts and other drugs using thymocyte stimulation assay. About inhibitory effects of $PGF_2$. by gingival fibroblasts, herbal extract was compared with the addition of the other control groups using enzyme imunoassay. On the inhibition of collagenolytic activity by P. gingivalis, benzene extracts showed the most efficient inhibitory effects among the $19{\mu}g/ml$ of the compared extracts and 40.5% by Tetracycline. On the cellular activity promoting effects, compared extracts showed a bit of more effects than PDGF of $100{\mu}g/ml$ concentration and IGF of $20{\mu}g/ml$ concentration. All of the PDGF, IGF, Zizyphi Fructus extract should increase in collagen synthesis, but especially 70% ethylalcohol extracts of Zizyphi Fructus showed comparably high effects among the compared extracts. Effects on whole protein synthesis were slightly increased on every extract but especially 70% ethylalcohol extract showed significantly effective than any other estract. On the inhibitory effects of Zizyphi Fructus $IL-l{\beta}$ production by monocyte, compared extracts showed 70% of highly inhibitory effect than that of 60% inhibition effects on controlled group and each extracts showed no significant difference. In $PGF_2$ production inhibitroy effect of Zizyphi Fructus gingival fibroblasts, Herbal extracts showed 70% of inhibition comparing with tat of 90.2% of controlled group, but each extracts showed similar effects excluding the $H_2O$ extracts. These results suggested that Zizyphi Fructus might be useful medicine for inhibition of inflammatory mediator including $IL-l{\beta}$ and $PGF_2$.

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The Inhibitory Effects of Maekmundongcheongpye-eum and Liriopis Tuber on the IL-6, IL-16 and GM-CSF mRNA Levels in Human Epithelial Cells (맥문동청폐음과 맥문동이 인간기관지 상피세포의 IL-6, IL-16, GM-CSF mRNA level에 미치는 영향)

  • 정해준;정희재;정승기;이형구
    • The Journal of Korean Medicine
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    • v.23 no.1
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    • pp.11-23
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    • 2002
  • Objectives: We aimed to identify the dose-dependent inhibitory effects of Maekmundongcheongpye-eum and Liriopis Tuber on the mRNA expression of IL-6, IL-16, GM-CSF involved in the asthma model. Methods: In the study BEAS-2B cell lines, human epithelial cells were used. These cells were stimulated with tumor necrosis factor $(TNF)-{\alpha}$ for artificial inflammatory expression. ${\beta}-actin$ messenger RNA (mRNA) was used by internal standard. After 24 hours of Maekmundongcheongpye-eum, Liriopis Tuber-treatment, total cellular RNAs were collected, treating RNAzol directly on the alive cells. Then the transcriptional activities of IL-6, 16, GM-CSF were measured by RT-PCR with electrophoresis. Results: In the Maekmundongcheongpye-eum study, the mRNA expression of IL-6 showed 48% transcriptional inhibitory effect compared to the control group in the $100{\;}{\mu}l/ml$ category (P<0.001). In the IL-16, there was 53% and 57% transcriptional inhibitory effect compared to the control group in the $20{\;}{\mu}l/ml$ and $100{\;}{\mu}l/ml$ categories (P<0.001). In the GM-CSF, there was no inhibitory effect. In the Liriopis Tuber study, the mRNA expression of IL-6 showed 43% transcriptional inhibitory effect compared to the control group in the $100{\;}{\mu}l/ml$ category (p<0.005). In the IL-16, 34% and 26% of transcriptional inhibitory effect was shown compared to the control group in the $20{\;}{\mu}l/ml$ and $100{\;}{\mu}l/ml$ categories, respectively (P<0.05). In the GM-CSF, there was no inhibitory effect. Conclusions: This study shows that Maekmundongcheongpye-eum and Liriopis Tuber have dose-dependent inhibitory effects on the mRNA expression of IL-6 and IL-16 in BEAS-2B cell lines, human epithelial cells. Advanced studies are required to investigate the mechanisms of inhibition by herbal medicine in the asthma model.

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The Study on Depigmentation of Kamikwibi-Tang (가미귀비탕의 미백효과에 관한 연구)

  • Park, Ho-Soon;Kim,Hye-Jung;Kim, Yoon-Bum
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.17 no.2
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    • pp.48-58
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    • 2004
  • Objective: This study was performed to investigate the depigmentation effects of the extracts of Kamikwibi-Tang. Methods Inhibition of tyrosinase activity, melanin production & cell viability in cultured B16 melanoma cells, UV screen and cytoprotective effects on PC12 cells injured by hydrogen peroxide were measured. Results: The extracts of Kamikwibi-Tang did not have any inhibitory effects on tyrosinase activity and did not show any inhibitory effects on melanin production in melanoma cells and also did not have any inhibitory effects on UV screen. But the extracts showed high cytoprotective effects on PC12 cells injured by hydrogen peroxide. Conclusion : These results suggest that Kamikwibi-Tang indrectly inhibits melanin biosynthesis which is involved in hyperpigmentation and could be used as a whitening agent for the skin.

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Inhibitory Effect of Doenjang(fermented Korean soy paste) Extracts and Linoleic Acid on the Growth of Human Cancer Cell Lines

  • Park, Kun-Young;Lee, Jeong-Min;Moon, Suk-Hee;Jung, Keun-Ok
    • Preventive Nutrition and Food Science
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    • v.5 no.2
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    • pp.114-118
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    • 2000
  • The inhibitory effects of doenjang extracts and linoleic acid(LA) which was identified as one of the active compounds in doenjang on the growth of human cancer cells were studied, comparing to the actions on normal cells. Methanol extract and hexane fraction from doenjang exhibited the strong growth inhibitory effect on HT-29 human colon carcinoma cells. Inhibitory effects of chloroform, ethyl acetate, butanol and aqueous fractions on the cancer cells were observed, moderately or weakly. When cell counts of SNU-C$_1$human colon carcinoma cells were determined daily for 6 days, the inhibitory effect of hexane fraction on this cell line was higher than that of the methanol extract from doenjang. LA completely suppressed the growth of SNU-C$_1$cells after 4 days, while conjugated linoleic acid(CLA) resulted in 98% inhibition after 6 days. With the addition of LA and other free fatty acids such as stearic acid, oleic acid, linolenic acid and ${\gamma}$-linolenic acid (${\gamma}$-LnA) to the culture system, the growth of HT-29 cells and SNU-C$_1$cells was greatly suppressed after 6 days. Inhibitory effects of LA ${\gamma}$-LnA on the growth of these cells were stronger than other fatty acids. On the growth of AZ-521 human gastric carcinoma cells, LA and CLA completely cuppressed the growth of the cells after 4 days and 3 days, respectively. At the level of 0.001%~0.01% of LA, there was no cytotoxic effect on normal rat kidney cells and normal intestine human cells. These results showed that LA, a major active compound of doenjang, had strong inhibitory effects on the growth of human cancer cells without damaging normal cells.

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Inhibitory Effects of Chinese Medicinal Plants on the Platelet-Activating Factor (PAF) Receptor Binding (중국 약용식물의 혈소판 활성화인자 수용체 결합 억제활성)

  • Kang, Young-Hwa
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.4
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    • pp.178-181
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    • 2005
  • Methanolic extracts of fifteen Chinese medicinal plants were screened for platelet-activating factor (PAF) receptor binding inhibitory activity using rabbit platelet. Campsis grandiflora, Dalbergia odorifera, Vaccaria segetalis and Zanthoxylum nitidum showed significant inhibitory effects on the platelet-activating factor (PAF) receptor binding. Campsis grandiflora, Dalbergia odorifera, Vaccaria segetalis and Zanthoxylum nitidum inhibited 52%, 56%, 70%, and 66% respectively at the concentration of 0.2 mg/ml.

Inhibitory Effects of Cysteine on Growth and Protease Production of Preudomonas sp. RP-222 and its Mutant MR-3966 (Pseudomonas sp. RP-222와 변이주 MR-3966 의 생육 및 Protease 생산에 Cysteine이 미치는 저해효과)

  • Lee, Kwang-Soo;Kang, Shin-Kwon;Son, Bong-Soo;Roh, Jong-Soo;Kim, Gyeong-Sook;Chun, Sung-Sik;Sung, Nack-Kie
    • Microbiology and Biotechnology Letters
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    • v.22 no.6
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    • pp.621-626
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    • 1994
  • Cysteine showed strong inhibitory effect on growth and protease production of Pseudo- monas sp. RP-222 and its mutant, MR-3966. Mid- to late-log phase cells were most sensitive to the presence of 10 mM cysteine. The inhibition caused by cysteine was almost completely overcome by addition of isoleucine, leucine and valine mixture to the medium, and inclusion of iso#leucine alone could greatly reduce the inhibitory effects of cysteine. Homocysteine and #cysteine, sulfur compounds having similar structure as cysteine, inhibited to varying degrees the growth of both strains. Cysteine and homocysteine were strong inhibitors of threonine deaminase but not transa#- minase B. These results suggest a relationship between the growth-inhibitory effects of cysteine and other sulfur compounds and the inhibition of isoleucine synthesis at the level of threonine deaminase.

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Antioxidative and Antimutagenic Effects and Hyperplasia Inhibitory Activity of Cancer Cells from Luffa cylindrica Extracts (수세미오이(Sponge-gourd: Luffa cylindrica L.) 추출물의 항산화, 항돌연변이 및 암세포 증식 억제 효과)

  • Oh, Se-In;Lee, Mee-Sook
    • The Korean Journal of Food And Nutrition
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    • v.25 no.4
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    • pp.888-896
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    • 2012
  • 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 ($66.38{\pm}2.65$), DPPH (1,1-diphenyl-2-picryl-hydrazyl) radical production ($60.13{\pm}0.42$) and lipid peroxidation ($56.04{\pm}3.24$). 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 ($5.82{\pm}5.74$) and in indirect mutagenicity mediated by 2-anthramine in Salmonella typimurium TA100 ($5.76{\pm}2.15$). 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 ($55.83{\pm}3.83$) and MCF-7 cells ($33.03{\pm}2.09$), 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.