In Vitro Sortase A Inhibitory and Antimicrobial Activity of Flavonoids Isolated from the Roots of Sophora flavescens

Ikhoon Oh,신종헌,Woo-Young Yang,Soon-Chun Chung,김태윤,오기봉 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.2

A series of flavonoids (1-14) was isolated from the roots of Sophora flavescens. We evaluated their ability to inhibit both microbial growth and sortase A, an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus. Most prenylated flavonoids (7-13) displayed potent inhibitory activity against gram-positive and gram-negative bacteria except E. coli, with minimum inhibitory concentrations values ranging from 4.40 to 27.7 μM, and weak or no activity against fungal strains tested. Kurarinol (6) was a potent inhibitor of sortase A, with an IC_50 value of 107.7 ± 6.6 μM. A preliminary structure-activity relationship, including essential structural requirements, is described.

In Vitro Na^+/K^+-ATPase Inhibitory Activity and Antimicrobial Activity of Sesquiterpenes Isolated from Thujopsis dolabrata

Ikhoon Oh,신종헌,Woo-Young Yang,Jiyoung Park,Sooryun Lee,마응천,오기봉 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.12

A series of sesquiterpenes and hinokitiol-related compounds (1-15) was isolated from the essential oil of Thujopsis dolabrata Sieb. et Zucc. var. hondai Makino, and their structures were determined by combined spectroscopic analyses. The inhibitory effects of these compounds on microbial cell growth and Na^+/K^+-ATPase were evaluated in vitro. It was found that (-)-elema-1,3,11(13)-trien-12-ol (5), α,β,γ-costol (8), and chamigrenol (11) inhibit the activities of Na^+/K^+-ATPase, with IC_50 values of 11.2 ± 0.11, 12.2 ± 0.09, and 15.9 ± 0.54 μg/mL, respectively. Thujopsene (1), cedrol (9), γ-cuparenol (10), and chamigrenol (11) showed potent antibacterial activity, with MIC values in the range of 25-50 μg/mL, and β-thujaplicin (12) exhibited a broad spectrum of antibacterial and antifungal activity. These results indicate that these isolated compounds are promising candidates for the development of potent Na^+/K^+ ATPase inhibitors and antimicrobial agents.

Anti-inflammatory activity of compounds isolated from <i>Astragalus sinicus</i> L. in cytokine-induced keratinocytes and skin

Kim, Byung-Hak,Oh, Ikhoon,Kim, Jung-Ho,Jeon, Ju-eun,Jeon, Byeongwook,Shin, Jongheon,Kim, Tae-Yoon Nature Publishing Group 2014 Experimental and molecular medicine Vol.46 No.3

<P>Inflammation is a part of the complex biological responses of a tissue to injury that protect the organ by removing injurious stimuli and initiating the healing process, and is considered as a mechanism of innate immunity. To identify biologically active compounds against pathogenic inflammatory and immune responses, we fractionated water, aqueous methanol and <I>n</I>-hexane layers from nine kinds of leguminosae and examined anti-inflammatory activity of the fractions in human keratinocytes and mouse skin. Among the fractions, rf3 and rf4, isolated from the aqueous methanol layer of <I>Astragalus sinicus</I> L., exhibited the strongest reactive oxygen species (ROS)-scavenging and anti-inflammatory activities as measured by inhibition of the intracellular ROS production, nuclear factor-kappaB (NF-κB), janus kinase (JAK)/signal transducer and activator of transcription (STAT), and phosphatidylinositol 3-kinase/Akt signaling in cytokine-stimulated human keratinocytes, as well as by effects on T-cell differentiation in mouse CD4<SUP>+</SUP> T cells. In addition, topical application of rf3 and rf4 suppressed the progression of psoriasis-like dermatitis and expression of pro-inflammatory mediators in interleukin (IL)-23-injected mouse ears. Our results suggest that <I>Astragalus sinicus</I> L. may ameliorate chronic inflammatory skin diseases due to its antioxidant and anti-inflammatory activities via regulation of the intracellular ROS production, NF-κB, JAK/STAT and PI3/Akt signaling cascades as well as immune responses, and these results are the first report that <I>Astragalus sinicus</I> L. exhibits pharmacological activity.</P>

Acylated Kaempferol Glycosides from <i>Laurus nobilis</i> Leaves and Their Inhibitory Effects on Na⁺/K⁺-Adenosine Triphosphatase

Lee, Sooryun,Chung, Soon-Chun,Lee, So-Hyoung,Park, Wanki,Oh, Ikhoon,Mar, Woongchon,Shin, Jongheon,Oh, Ki-Bong Pharmaceutical Society of Japan 2012 Biological & pharmaceutical bulletin Vol.35 No.3

<P>Na<SUP>+</SUP>/K<SUP>+</SUP>-adenosine triphosphatase (ATPase) inhibitors have considerable therapeutic potential against some heart diseases like congestive heart failure and cardiac arrhythmias. Through bioassay-guided separation of the leaf extract of <I>Laurus nobilis</I>, six acylated kaempferol glycosides (compounds <B>1</B>—<B>6</B>) were isolated. Their structures were determined on the basis of spectroscopic analysis and comparison with reported data. All the isolates were subjected to <I>in vitro</I> bioassays to evaluate their inhibitory activities against Na<SUP>+</SUP>/K<SUP>+</SUP>-ATPase from porcine cerebral cortex and bacterial growth. These studies led to the identification of compounds <B>1</B>—<B>6</B> as potent Na<SUP>+</SUP>/K<SUP>+</SUP>-ATPase inhibitors, with IC<SUB>50</SUB> values in the range of 4.0±0.1—10.4±0.6 μ<SMALL>M</SMALL>. These compounds also exhibited a broad spectrum of antibacterial activity. In particular, compounds 4 and 6 showed potent inhibitory activities against several bacterial strains, except <I>Escherichia coli</I>, with minimum inhibitory concentration (MIC) values in the range of 0.65—2.08 μg/mL. Thus, <I>L. nobilis</I>-derived acylated kaempferol glycosides may have a potential to be leads for the development of Na<SUP>+</SUP>/K<SUP>+</SUP> ATPase inhibitors (<B>1</B>—<B>6</B>) and antibacterial agents (<B>4</B>, <B>6</B>).</P>

Effect of by BIOVITA 3 (a Blend of Three Probiotics) on Dextran Sulfate Sodium-Induced Colitis in Mice

Han Sol Choi,Dayoung Kim,Ye-Ji Jang,Jin Seok Moon,Ikhoon Oh 건강기능식품미래포럼 2024 건강기능식품미래포럼 학술지 Vol.4 No.1

Probiotics play an important role in maintaining gut health by modulating the composition of the gut microbiota. BIOVITA 3 is a blend of freeze-dried powders of three probiotics including Clostridium butyricum IDCC 1301, Weizmannia coagulans IDCC 1201, and Bacillus subtilis IDCC 1101. Previous research has shown that this probiotic blend can relieve constipation in mice by rebalancing gut microbes, suggesting its potential benefits for conditions like inflammatory bowel disease (IBD). To explore this possibility, we conducted an experiment examining BIOVITA 3's effect on colitis induced by dextran sulfate sodium (DSS) in mice. For this purpose, mice were orally administered BIOVITA 3 (1 × 106 CFU) or starch (38 mg/mL)once daily for three weeks, followed by replacing a drinking water with 3% DSS in water with unrestricted access for seven days. The onset of colitis was evident through significant increases in the scores of disease activity index (DAI), levels of pro-inflammatory proteins in colon tissues, and damage scores of colon tissues observed through histology. Among these markers of inflammation, the DAI scores and levels of pro-inflammatory proteins (interleukin [IL]-6, interferon-γ, IL-17, leukotriene B4, and myeloperoxidase) were significantly reduced in the group treated with BIOVITA 3 compared to the starch-treated group. These findings support that BIOVITA 3 mitigates symptoms associated with DSS-induced colitis in mice, suggesting its potential therapeutic benefits for IBD.

BIOVITA 3, a Mixture of Three Probiotics, Ameliorates the Loperamide-Induced Constipation in Rats

Jin Seok Moon,Dayoung Kim,Ji Eun Kim,Ye-Ji Jang,Han Sol Choi,Ikhoon Oh 건강기능식품미래포럼 2023 건강기능식품미래포럼 학술지 Vol.3 No.3

BIOVITA 3, a probiotic blend powder that includes Bacillus subtilis IDCC 1101, Weizmannia coagulans IDCC1201, and Clostridium butyricum IDCC1301, has been used for various intestinal disorders. However, its effectiveness on constipation has not been investigated. This study aimed to assess how BIOVITA 3 alleviates constipation induced by loperamide. Sprague-Dawley rats were orally administered three different doses of BIOVITA 3 (1.0 × 107, 1.0 × 108, or 1.0 × 109 CFU) for 7 days and then loperamide (5 mg/kg, orally) to induce constipation. Compared to the control rats (starch for 7 days followed by loperamide), the BIOVITA 3-treated rats showed dose-dependent increases in the number of fecal pellets, fecal water content, and gastrointestinal transit time (an index of bowel movement). Additionally, the BIOVITA 3-treated rats showed higher levels of short-chain fatty acids (SCFAs) in the feces than the control rats. Furthermore, there were decreases in harmful bacteria such as Prevotella and Turicibacter in the BIOVITA 3-treated rats while the control rats showed the increases of these bacteria. These results suggest that BIOVITA 3 has the capacity to relieve constipation by enhancing the bowel movement, regulating the levels of SCFAs, and improving the gut's microbial balance.