• Title/Summary/Keyword: Active compounds

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Indigo Naturalis in Inflammatory Bowel Disease: mechanisms of action and insights from clinical trials

  • Hyeonjin Kim;Soohyun Jeong;Sung Wook Kim;Hyung-Jin Kim;Dae Yong Kim;Tae Han Yook;Gabsik Yang
    • Journal of Pharmacopuncture
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    • v.27 no.2
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    • pp.59-69
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    • 2024
  • This study investigates the therapeutic potential of Indigo Naturalis (IN) in treating a Inflammatory Bowel Disease (IBD). The objective is to comprehensively examine the effects and pharmacological mechanisms of IN on IBD, assessing its potential as an novel treatment for IBD. Analysis of 11 selected papers is conducted to understand the effects of IN, focusing on compounds like indirubin, isatin, indigo, and tryptanthrin. This study evaluates their impact on Disease Activity Index (DAI) score, colon length, mucosal damage, and macrophage infiltration in Dextran Sulfate Sodium (DSS)-induced colitis mice. Additionally, It investigate into the anti-inflammatory mechanisms, including Aryl hydrocarbon Receptor (AhR) pathway activation, Nuclear Factor kappa B (NF-κB)/nod-like receptor family pyrin domain containing 3 (NLRP3)/Interleukin 1 beta (IL-1β) inhibition, and modulation of Toll-like receptor 4 (TLR4)/myeloid differentiation primary response 88 (MYD88)/NF-κB and Mitogen Activated Protein Kinase (MAPK) pathways. Immunomodulatory effects on T helper 17 (Th17)/regulatory T cell (Treg cell) balance and Glycogen synthase kinase-3 beta (GSK3-β) expression are also explored. Furthermore, the study addresses the role of IN in restoring intestinal microbiota diversity, reducing pathogenic bacteria, and increasing beneficial bacteria. The findings reveal that IN, particularly indirubin and indigo, demonstrates significant improvements in DAI score, colon length, mucosal damage, and macrophage infiltration in DSS-induced colitis mice. The anti-inflammatory effects are attributed to the activation of the AhR pathway, inhibition of inflammatory pathways, and modulation of immune responses. These results exhibit the potential of IN in IBD treatment. Notably, the restoration of intestinal microbiota diversity and balance further supports its efficacy. IN emerges as a promising and effective treatment for IBD, demonstrating anti-inflammatory effects and positive outcomes in preclinical studies. However, potential side effects necessitate further investigation for safe therapeutic development. The study underscores the need for future research to explore a broader range of active ingredients in IN to enhance therapeutic efficacy and safety.

Nutritional compositions and antioxidative activities of two blueberry varieties cultivated in South Korea (국내산 두 품종 블루베리의 영양성분 및 항산화 활성 비교)

  • Song, Hyo-Nam;Park, Myoung-Su;Youn, Ho-Sik;Park, Sung-Jin;Hogstrand, Christer
    • Food Science and Preservation
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    • v.21 no.6
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    • pp.790-798
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    • 2014
  • The nutritional compositions and antioxidative activities of the Kimcheon lowbush and Pyungtaek highbush blueberries cultivated in South Korea were investigated. The approximate compositions, pH, and soluble-solid and mineral contents of P, Ca, Mg, Na, and Zn were determined. Both blueberry cultivars had mainly fructose and glucose as free sugars while disaccharides such as sucrose, maltose, and lactose were not detected in both. Oleic, linoleic, and linolenic fatty acids were the major fatty acids in both types of blueberries. The total of 16 free amino acids, including seven essential and nine non-essential amino acids, were higher in the Pyungtaek highbush blueberry. Among the amino acids, arginine was especially much higher in the Pyungtaek highbush blueberry. The anthocyanin, resveratrol, and polyphenol compounds, which are the important biologically active compounds in blueberries, were found. The anthocyanin contents of the Kimcheon lowbush and Pyungtaek highbush blueberries were 22.0 and 18.1 mg/100 g, respectively; the resveratrol contents by HPLC, 0.12 and 0.11 mg/100 g; and the total polyphenol contents, 141.3 and 138.4 mg/100 g. The electron-donating ability determined based on the DPPH radical scavenging activity was increased in a concentration-dependent manner, and it was higher than that of the Pyungtaek highbush blueberries, which implies that it is highly correlated with the higher amounts of total polyphenol, anthocyanin, and resveratrol in it. In conclusion, the two varieties of Korean blueberries can be suggested as potential sources of high-value-added functional foods.

Occluding Effect of the Application of Fluoride Compounds and Desensitizers on Dentinal Tubules (불소도포 및 지각과민처치제 적용 후 상아세관 폐쇄효과와 지속력 평가)

  • Lee, Ye-Jin;Jeong, Moon-Jin;Ahn, Yong-Soon;Cheun, Su-Kyung;Jeong, Soon-Jeong;Lim, Do-Seon
    • Journal of dental hygiene science
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    • v.16 no.4
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    • pp.272-283
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    • 2016
  • This study compared and analyzed the occluding effects of fluoride compounds and desensitizers, which are commonly used in dental clinics, on dentinal tubules. This study also evaluated the persistence of the active ingredients over time by performing toothbrushing with an electric toothbrush. Thirty-five molar teeth, which had been extracted within the past 3 months from healthy people without tooth decays, amalgam fillings, or dental crowns, were divided into 4 pieces each. Of these, 135 teeth pieces were used as study specimens. These specimens were divided into a control group, an untreated group, and 5 experimental groups (acidulated fluoride gel, fluoride varnish, Gluma, Super Seal, and SE-Bond). The specimens were then subjected to toothbrushing equivalent to 1 week (140 times), 2 weeks (280 times), and 4 weeks (560 times), and the occluding effects on dentinal tubules in 3 regions of each specimen were examined under a scanning electron microscope. The fluoride varnish treated group showed the highest degree of dentinal tubule occlusion effects during the first, second, and fourth weeks of toothbrushing, with the SE-Bond treated group showing the second highest degree and the Gluma treated group showing the lowest degree. After 4 weeks of toothbrushing, the Gluma treated group and the Super Seal treated group showed the lowest degrees of dentinal tubule occlusion effects. In summary, the fluoride varnish treated group and the SE-Bond treated group displayed higher occlusion effects even after 4 weeks of treatment than did the other experimental groups. Therefore, it is the authors' belief that fluoride varnish and SE-Bond are effective for treating dentinal hyperesthesia.

Biological Control of Fusarium Head Blight on Wheat by Polyacetylenes Derived from Cirsium japonicum Roots (대계근에서 분리한 Polyacetylene계 화합물을 이용한 밀 이삭마름병 방제)

  • Kim, Ji-In;Kim, Kihyun;Park, Ae Ran;Choi, Gyung Ja;Park, Hae Woong;Kim, In Seon;Kim, Jin-Cheol
    • Research in Plant Disease
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    • v.22 no.3
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    • pp.145-151
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    • 2016
  • Chemical fungicides have reduced Fusarium head blight (FHB) severity. However, by the effects of fungicide residues, they can only be used up to 30 days before time of harvest. Therefore, the development of new biofungicides that are applicable until harvest is required. In order to select plant extracts having antifungal activity against Fusarium graminearum for the control of FHB, we investigated the inhibitory effects of 225 medicinal plant extracts on spore germination of F. graminearum. Of these plant extracts, the methanol extract of Cirsium japonicum (CJ) roots showed the strongest antifungal activity. Through solvent partitioning, repeated column chromatography, and spore germination bioassay, two chemicals were purified and then their chemical structures were identified as ciryneol C (CC) and 1-heptadecene-11,13-diyne-8,9,10-triol (HD-ol) which are polyacetylene substances. Two active compounds effectively inhibited the germination of F. graminearum macroconidia; HD-ol ($IC_{50}$ of $3.17{\mu}g/ml$) showed stronger spore germination inhibitory activity than that of CC ($IC_{50}$ of $28.14{\mu}g/ml$). In addition, the wettable powder type formulation of ethyl acetate extract of CJ roots suppressed the development of FHB in dose-dependent manner, with control values of 78.92% and 31.56% at 250- and 500-fold dilutions, respectively. Combining these findings suggest that the crude extract of CJ roots containing polyacetylene compounds could be used as botanical fungicide for the control of FHB.

Isolation and Identification of a Photosensitizer from Pueraria thunbergiana Leaves that Induces Apoptosis in SK-HEP-1 Cells (P. thunbergiana 잎으로부터 SK-HEP-1세포에 대한 apoptosis를 유도하는 광과민성물질의 분리 및 구조동정)

  • Lee, Jun Young;Kim, Mi Kyeong;Ha, Jun Young;Kim, Yong Gyun;Hong, Chang Oh;Kim, So Young;Kim, Chung-Hwan;Kim, Keun Ki
    • Journal of Life Science
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    • v.24 no.3
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    • pp.242-251
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    • 2014
  • The objective of this study was to isolate a photosensitizer from Pueraria thunbergiana leaves that induces apoptosis in SK-HEP-1 cells. Column chromatography and thin layer chromatography were used to isolate active compounds from extracts of P. thunbergiana leaves. The structures of the isolated compounds were determined by 1D-NMR, 2D-NMR, and FAB-mass spectroscopy. A substance, named M4-3, was purified from the leaves of P. thunbergiana using various chromatography methods, and the absorbance of the substance was measured. The absorbance was highest at 410 nm, suggesting that the M4-3 substance was a different compound from chlorophyll a and b, which absorb at 410, 502, 533, and 607 nm. Further analyses revealed that the M4-3 compound was a $13^2$-hydoxy pheophorbide, a methyl ester with a molecular weight of 662. M4-3 was identified as a derivative compound of pheophorbide, with a structure that magnesium comes away from the porphyrin ring. The results of the analysis of the cytotoxicity of the M4-3 substance against the SK-HEP-1 cells revealed that it inhibited rates of cell growth by 40% and 80% at a concentration of 0.04 ${\mu}M$ and 0.08 ${\mu}M$, respectively. The M4-3 compound was found to be a photosensitizer for cytotoxicity because it was appeared only in light condition as examining activity in different irradiation conditions (light condition and nonlight condition) under the same concentration. Analysis of morphological changes in the cells following cell death induced by exposure to the M4-3 substance reveled representative phenomena of apoptosis (nuclear condensation, vesicle formation, and fragmentation of DNA). The induction of apoptosis was attributed to the compound's photodynamic activity.

Identification of Allelopathic Substances from Polygonum hydropiper and Polygonum aviculare (여뀌.마디풀로부터 상호대립억제작용물질(相互對立抑制作用物質)의 분리(分離).동정(同定))

  • Woo, S.W.;Kim, K.U.
    • Korean Journal of Weed Science
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    • v.7 no.2
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    • pp.144-155
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    • 1987
  • Water extracts of polygonum hydropiper and Polygonum aviculare completely inhibited the germination of lettuce seeds. Methanol extracts from these two species also inhibited the seed germination of lettuce (Lactuca sativa) and Oenothera odorata. Fifteen phenolic acids in total were identified by GLC from P. hydropiper and eighteen from P. aviculare. The most common phenolic acids identified from P. hydropiper were sinapic, salicylic+vanillic and ferulic acid presented in all the fractions. In addition, salicylic+vanillic, tannic+gallic, sinapic, ferulic and p-coumaric acid seemed to be important phenolic compounds in terms of quantity. However, salicylic+vanillic acids were the unique phenolic acids occurred in all the fractions of P. aviculare. The others such as tannic+gallic, sinapic, ferulic, p-coumaric acid, p-cresol and catechol present in large amount appeared also the important phenolic substances influencing allelopathic effects of P. aviculare. Linolenic acid and oxalic acid were the major fatty and organic acids in both plant species, presented in 2.38mg/g and 20.588mg/g in P. hydropiper, 3.70mg/g and 14.288mg/g in P. aviculare, respectively, which seem to be exhibiting allelopathic effects of these plants. Total alkaloids were presented in low amount such as 0.20% in P. hydropiper arid 0.22% in P. aviculare which may not be important elements. Pet. ether extracts were 2.42% in P. hydropiper and 1.65% in P. aviculare, which exhibit another potential for allelopathic effects that need further investigation. Various authentic phenolic compounds at different concentrations inhibited the germination of lettuce seed, indicating that the phenolic substances identified here may be directly related to biologically active substance.

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Protective Effect of the Ethyl Acetate-fraction of Methanol Extract of Ophiophogon japonicus on Amyloid beta Peptide-induced Cytotoxicity in PC12 Cells (소엽맥문동-에틸아세테이트 분획물의 아밀로이드 베타단백질-유발 세포독성에 대한 억제 효능)

  • Moon, Ja-Young;Kim, Eun-Sook;Choi, Soo-Jin;Kim, Jin-Ik;Choi, Nack-Shik;Lee, Kyoung;Park, Woo-Jin;Choi, Young-Whan
    • Journal of Life Science
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    • v.29 no.2
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    • pp.173-180
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    • 2019
  • Amyloid ${\beta}$-protein ($A{\beta}$) is the principal component of senile plaques characteristic of Alzheimer's disease (AD) and elicits a toxic effect on neurons in vitro and in vivo. Many environmental factors, including antioxidants and proteoglycans, modify $A{\beta}$ toxicity. It is worthwhile to isolate novel natural compounds that could prove therapeutic for patients with AD without causing detrimental side effects. In this study, we investigated the in vitro neuroprotective effects of the ethyl acetate fraction of methanol extract of Ophiophogon japonicas (OJEA fraction). We used an MTT reduction assay to detect protective effects of the OJEA fraction on $A{\beta}_{25-35}$-induced cytotoxicity to PC12 cells. We also used a cell-based ${\beta}$-secretase assay system to investigate the inhibitory effect of the OJEA fraction on ${\beta}$-secretase activity. In addition, we performed an in vitro lipid peroxidation assay to evaluate the protective effect of the OJEA fraction against oxidative stress induced by $A{\beta}_{25-35}$ in PC12 cells. The OJEA fraction had strong protective effects against $A{\beta}_{25-35}$-induced cytotoxicity to PC12 cells and was strongly inhibitory to ${\beta}$-secretase activity, which resulted in the attenuation of $A{\beta}$ generation. In addition, the OJEA fraction significantly decreased malondialdehyde (MDA) content, which is induced by the exposure of PC12 cells to $A{\beta}_{25-35}$. Our results suggested that the OJEA fraction contained active compounds exhibiting a neuroprotective effect on $A{\beta}$ toxicity.

Comparison of the Efficacy of Disinfectants to Control Caseous Lymphadenitis in Korean Black Goat Farms (흑염소의 건락성 림프절염 제어를 위한 소독제 효능 비교)

  • Cho, Hyeunwoo;Kim, Yeona;Jang, Beomsoon;Kim, Chan-Lan;Park, Kun Taek
    • Journal of Food Hygiene and Safety
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    • v.37 no.5
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    • pp.317-322
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    • 2022
  • Corynebacterium pseudotuberculosis is the causative agent of caseous lymphadenitis (CLA), a chronic contagious disease in small ruminants. The prevalence of CLA has been reported to be >50% in Korean black goats. CLA is difficult to control due to a lack of efficient vaccines and treatment methods. Effective disinfection of the farm environment may be an alternative strategy for reducing the spread of C. pseudotuberculosis. The objective of this study was to evaluate the efficacy of commercial disinfectants against CLA. The six commercial disinfectants, largely composed of sodium dichloroisocyanurate, sodium hypochlorite, potassium monopersulfate triple salt, quaternary ammonium, citric acid, and copper sulfate, were tested against five different genotypes of C. pseudotuberculosis isolated from goat farms in Korea. Efficacy tests were performed in accordance with the disinfectant efficacy test guidelines recommended by the Animal and Plant Quarantine Agency of Korea with slight modifications. All disinfectants except for copper sulfate exhibited >99.99% killing efficacy under hard water conditions following 30 min of incubation, which is the recommended standard treatment time according to guidelines. The minimum bactericidal treatment time was evaluated by employing treatments for durations of 1, 5, and 15 min. The most effective compounds under hard water conditions were sodium dichloroisocyanurate, potassium monopersulfate triple salt, and sodium hypochlorite, exhibiting >99.99% killing efficacy after 1 min of treatment. In the aqueous solution forms, citric acid and the quaternary ammonium compound were the most effective, but required at least 5 min to kill >99.99% of the bacteria. The current study characterizes the killing efficacy of six commercial disinfectant active compounds against C. pseudotuberculosis. Thus, this study provides essential information regarding the efficacy of the disinfectants used to control CLA in goat farms.

Changes in physiologically active ingredients and anti-inflammatory properties of underutilized wild vegetables by complex fermentation using beneficial microorganisms (유용미생물에 의한 저이용 산채류의 복합발효 중 생리활성 성분 및 항염증 변화)

  • Sang-Hyeob Sim;Ha KyoungChoi;Da Eun Lee;Soo Chang Na;Dae Il Hwang;Hyo Bin Oh;Yi Teak Lim;Tae-Young Kim;Dae-Woon Kim
    • Food Science and Preservation
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    • v.31 no.2
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    • pp.287-297
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    • 2024
  • It was confirmed that complex fermentation (CF) was more efficient than single-strain fermentations in inducing changes in the contents of phenolic compounds of Maclura tricuspidate and Pyrus Montana Nakai. A mixture of Maclura tricuspidata, Pyrus montana Nakai, Platycodon grandiflorum and Codonopsis lanceolata were fermented in CF using Aspergillus shirousamii (koji), yeast, and lactic acid bacteria (LAB) for 24 days, and the pH, °Brix, total acidity, anti-oxidant activity, polyphenol content, nitric oxide (NO), and Western blotting of inducible nitric oxide synthase (iNOS), cyclo-oxygenase-2 (COX-2), and tumor necrosis factor-𝛼 (TNF-𝛼) of the sample were determined. There was no significant change in pH and total acidity. °Brix significantly decreased from day 6 onwards. HPLC confirmed that the concentrations of chlorogenic acid, 4-hydrobenzoic acid, vanillic acid, and caffeic acid significantly increased from day 18 during the fermentation. Additionally, DPPH, ABTS radical scavenging activity, total phenol, and total flavonoid were confirmed to be increased until 18 days. NO was significantly inhibited from day 6, along with significant inhibition of iNOS, COX-2, and TNF-a. In conclusion, this study confirmed that CF of low-use (or underutilized) wild vegetables enhances phenolic compounds. It effectively suppresses NO, iNOS, COX-2, and TNF-𝛼, markers of inflammation-related pathogenesis. Altogether, our results suggest that CF of the above plants has a potential anti-inflammatory effect.

Identification of Active Agents for Reductive Dechlorination Reactions in Cement/Fe (II) Systems by Using Cement Components (시멘트 구성성분을 이용한 시멘트/Fe(II)의 TCE 환원성 탈염소화 반응의 유효반응 성분 규명)

  • Jeong, Yu-Yeon;Kim, Hong-Seok;Hwang, In-Seong
    • Journal of Soil and Groundwater Environment
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    • v.13 no.1
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    • pp.92-100
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    • 2008
  • Experimental studies were conducted to identify the active agents for reductive dechlorination of TCE in cement/Fe(II) systems focusing on cement components such as CaO, $Fe_2O_3$, and $Al_2O_3$. A hematite that was used to simulate an $Fe_2O_3$ component in cement was found to have degradation efficiencies (k = 0.641 $day^{-1}$) equivalent to that of cement/Fe(II) systems in the presence of CaO/Fe(II), only when it contained an aluminum impurity$(Al_2O_3)$. When the effect of $Al_2O_3$ content of hematite/CaO/$Al_2O_3$/Fe(II) system was tested, the mole ratio of $Al_2O_3$ to CaO affected the rate of TCE degradation with an optimum ratio around 1 : 10 that resulted in a rate constant of 0.895 $day^{-1}$. In the SEM images of hematite/CaO/$Al_2O_3$/Fe(II) systems, acicular crystals were also found that were also observed in cement/Fe(II) systems. Thus it was suspected that these crystals were reactive reductants and that they might be goethite or ettringite that are known to have acicular structures. An EDS element map analysis revealed that these crystals were not goethite crystals. A subsequent experiment that tested reactivities of compounds formed during the ettringite synthesis showed that ettringite and minerals associated with ettringite formation are not reactive reductants. These observations conclude that a mineral containing CaO and $Al_2O_3$ with a acicular structure could be a major reactive reductant of cement/Fe(II) systems.