• Title/Summary/Keyword: antibacterial compound

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Antibacterial and Antifungal Activities of a Naphthoquinone Derivative Isolated from the Fruits of Catalpa ovata G.$D_{ON}$

  • Kuk, Ju-Hee;Ma, Seung-Jin;Moon, Jae-Hak;Kim, Kil-Yong;Choi, Sang-Ho;Park, Keun-Hyung
    • Journal of Microbiology and Biotechnology
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    • v.12 no.5
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    • pp.858-863
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    • 2002
  • An antimicrobial compound was isolated from the MeOH extract of Catalpa ovata G.$D_{ON}$ fruits, and its structure was Identified as 4,9-dihydroxy-2,2-dimethyl-3,4-Uihydronaphtho[2,3-b]pyran-5,10-dione (HMNP). The antimicrobial activity of the Un was determined by measuring the dose-response inhibiton of microbial growth in liquid cultures and then compared with that of lapachol, a well known antimicrobial 1,4-naphthoquinone. The antimicrobial activity of the HMNP was more effective than that of lapachol over a wide range of test organisms. Gram-positive bacteria, yeast, and fungi ($IC_{50}$ $20-75\muM$) were found to be more sensitive to the HMNP than Cram-negative bacteria ($IC_{50}$ > $100\muM$). The HMNP also inhibited germination of spores of many fungi. The morphological defurmation of the fungal spores was induced by the treatment of HMNP, as illustrated by Scanning Electron Microscopy (SEM).

Biphasic augmentation of alpha-adrenergic contraction by plumbagin in rat systemic arteries

  • Kim, Hae Jin;Yoo, Hae Young;Zhang, Yin Hua;Kim, Woo Kyung;Kim, Sung Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.6
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    • pp.687-694
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    • 2017
  • Plumbagin, a hydroxy 1,4-naphthoquinone compound from plant metabolites, exhibits anticancer, antibacterial, and antifungal activities via modulating various signaling molecules. However, its effects on vascular functions are rarely studied except in pulmonary and coronary arteries where NADPH oxidase (NOX) inhibition was suggested as a mechanism. Here we investigate the effects of plumbagin on the contractility of skeletal artery (deep femoral artery, DFA), mesenteric artery (MA) and renal artery (RA) in rats. Although plumbagin alone had no effect on the isometric tone of DFA, $1{\mu}M$ phenylephrine (PhE)-induced partial contraction was largely augmented by plumbagin (${\Delta}T_{Plum}$, 125% of 80 mM KCl-induced contraction at $1{\mu}M$). With relatively higher concentrations (>$5{\mu}M$), plumbagin induced a transient contraction followed by tonic relaxation of DFA. Similar biphasic augmentation of the PhE-induced contraction was observed in MA and RA. VAS2870 and GKT137831, specific NOX4 inhibitors, neither mimicked nor inhibited ${\Delta}T_{Plum}$ in DFA. Also, pretreatment with tiron or catalase did not affect ${\Delta}T_{Plum}$ of DFA. Under the inhibition of PhE-contraction with L-type $Ca^{2+}$ channel blocker (nifedipine, $1{\mu}M$), plumbagin still induced tonic contraction, suggesting $Ca^{2+}$-sensitization mechanism of smooth muscle. Although ${\Delta}T_{Plum}$ was consistently observed under pretreatment with Rho A-kinase inhibitor (Y27632, $1{\mu}M$), a PKC inhibitor (GF 109203X, $10{\mu}M$) largely suppressed ${\Delta}T_{Plum}$. Taken together, it is suggested that plumbagin facilitates the PKC activation in the presence of vasoactive agonists in skeletal arteries. The biphasic contractile effects on the systemic arteries should be considered in the pharmacological studies of plumbagin and 1,4-naphthoquinones.

In Vitro Activity of Methyl Gallate Isolated from Galla Rhois Alone and in Combination with Ciprofloxacin Against Clinical Isolates of Salmonella

  • Choi, Jang-Gi;Kang, Ok-Hwa;Lee, Young-Seob;Oh, You-Chang;Chae, Hee-Sung;Jang, Hye-Jin;Kim, Jong-Hak;Sohn, Dong-Hwan;Shin, Dong-Won;Park, Hyun;Kwon, Dong-Yeul
    • Journal of Microbiology and Biotechnology
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    • v.18 no.11
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    • pp.1848-1852
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    • 2008
  • Salmonella remains a primary cause of food poisoning worldwide, and massive outbreaks have been witnessed in recent years. Therefore, this study investigated the antimicrobial activity of methyl gallate (MG), which exhibited good antibacterial activity ($MIC=3.9-125{\mu}g/ml$) against all the bacterial strains tested. In a checkerboard dilution test, MG markedly lowered the MICs of ciprofloxacin (CPFX) against Salmonella. The combined activity of CPFX and MG against Salmonella resulted in fractional inhibitory concentrations (FICs) ranging from 0.0037 to 0.015 and from 0.24 to $7.8{\mu}g/ml$, respectively. Meanwhile, the FIC index ranged from 0.31-0.37, indicating a marked synergistic relationship between CPFX and MG against Salmonella. Time-kill assays also showed a decrease in the CFU/ml between the combination and the more active compound. Therefore, this study demonstrated that MG and CPFX can act synergistically in inhibiting Salmonella in vitro.

Physicochemical Properties, Stabilities and Pharmacokinetics of Cephalosporin 3'-Quinolone Dithiocarbamate (세팔로스포린 3'-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태)

  • 나성범;공재양;김완주;지웅길
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.638-646
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    • 1993
  • A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

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Synthesis and Biological Activities of Some New 3,6-Disubstituted 1,2,4-Triazolo[3,4-b]1,3,4-thiadiazole Derivatives

  • Rafiq, Muhammad;Saleem, Muhammad;Hanif, Muhammad;Maqsood, Muhammad Rizwan;Rama, Nasim Hasan;Lee, Ki-Hwan;Seo, Sung-Yum
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.3943-3949
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    • 2012
  • A series of aromatic hydrazides 3a-j were prepared by refluxing esters 2a-j with hydrazine hydrate in methanol, which were prepared by the esterification of 1a-j. Acetohydrazides 3a-j upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazate salts 4a-j, which on refluxing with hydrazine hydrate yielded substituted 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-j. The target compounds 6a-j were synthesized by condensing furan-3-carboxylic acid in the presence of polyphosphoric acid under reflux. The structures of newly synthesized compounds were characterized by IR, $^1H$ NMR, $^{13}C$ NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their urease, acetylcholine esterase inhibition, antioxidant and alkaline phosphatase inhibition activity. Almost all of the compounds 6a-j showed good to excellent activities against urease and acetylcholine esterase more than the reference drugs. Compounds 6f and 6g were more potent scavenger of free radicals than the reference n-propyl gallate. Compound 6b and 6h showed excellent activities of alkaline phosphatase as compare to the reference $KH_2PO_4$.

Studies on Physiological Activity of Bacillus subtilis JM-3 Isolated from Anchovy Sauce (멸치액젓으로부터 분리한 Bacillus subtilis JM-3의 생리활성기능에 관한 연구)

  • Lee, Sang-Soo;Kim, Sang-Moo;Shin, Il-Shik
    • Korean Journal of Food Science and Technology
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    • v.35 no.4
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    • pp.684-689
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    • 2003
  • In previous paper, we isolated the bacteria, Bacillus subtilis JM-3, with proteolytic and fibrinolytic activity for candidate microorganisms that have rapid fermenting and physiological functions from anchovy sauce. This study was carried out to search physiological functions of Bacillus subtilis JM-3, such as antimicrobial, antioxidative, antimutagenic, angiotensin-converting enzyme inhibition, and anticarcinogenic activity in vitro. The cell free culture of Bacillus subtilis JM-3 showed strong antibacterial activity against Listeria monocytogenes, antioxidative activity with 87% of inhibition rate against linoleic acid, 50% of antimutagenic activity against N-nitrosodimethylamine and N-nitrosomorpholine, and 88.9% of growth inhibition rate against SNU-1 cell line (stomach cancer cell of human). However, Bacillus subtilis JM-3 did not show angiotensin-converting enzyme inhibition activity.

Evaluation of Sensory Profile of Milk Analogs Containing Clove Oil: A Preliminary Study

  • Tae-Jin Kim;Kun-Ho Seo;Jung-Whan Chon;Hye-Young Youn;Hyeon-Jin Kim;Hajeong Jeong;Seok-Hyeong Kang;Won-Uk Hwang;Dongkwan Jeong;Kwang-Young Song
    • Journal of Dairy Science and Biotechnology
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    • v.41 no.1
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    • pp.26-33
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    • 2023
  • Eugenol, which can be extracted from clove oil, is a phenolic aromatic compound and has been found to have antibacterial, antiviral, antifungal, anticancer, anti-inflammatory, and antioxidant functions. Consequently, clove oil has long been used in several fields (food, medicine, skincare). Hence, in this study, the sensory profile of clove oil contained in milk analogs (almond, oat, and soy milks) was evaluated at different amounts (added at 0.25%-0.5% increments from 0% to 1.5%). Because of the strong scent of clove oil, the value of the evaluation for sensory profile determined in this study tended to be low. However, compared with the control group, good values in the evaluation for the sensory profile were found in all samples containing 0.25% of clove oil. We evaluated clove oil contained in milk analogs to help increase their sales through products with improved functionality.

Characterization of Vancomycin Resistant Enterococci and Drug Ligand Interaction between vanA of E. faecalis with the Bio-Compounds from Aegles marmelos

  • Jayavarsha V;Smiline Girija A.S;Shoba Gunasekaran;Vijayashree Priyadharsini J
    • Journal of Pharmacopuncture
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    • v.26 no.3
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    • pp.247-256
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    • 2023
  • Objectives: Enterococcus faecalis is a gram positive diplococci, highly versatile and a normal commensal of the gut microbiome. Resistance to vancomycin is a serious issue in various health-care setting exhibited by vancomycin resistant Enterococci (VRE) due to the alteration in the peptidoglycan synthesis pathway. This study is thus aimed to detect the VRE from the patients with root caries from the clinical isolates of E. faecalis and to evaluate the in-silico interactions between vanA and the Aegles marmelos bio-compounds. Methods: E. faecalis was phenotypically characterized from 20 root caries samples and the frequency of vanA and vanB genes was detected by polymerase chain reaction (PCR). Further crude methanolic extracts from the dried leaves of A. marmelos was assessed for its antimicrobial activity. This is followed by the selection of five A. marmelos bio-compounds for the computational approach towards the drug ligand interactions. Results: 12 strains (60%) of E. faecalis was identified from the root caries samples and vanA was detected from two strains (16%). Both the stains showed the presence of vanA and none of the strains possessed vanB. Crude extract of A. marmelos showed promising antibacterial activity against the VRE strains. In-silico analysis of the A. marmelos biocompounds revealed Imperatonin as the best compound with high docking energy (-8.11) and hydrogen bonds with < 140 TPSA (Topological polar surface area) and zero violations. Conclusion: The present study records the VRE strains among the root caries with imperatorin from A. marmelos as a promising drug candidate. However the study requires further experimentation and validation.

Antifungal and Antioxidant Activities of Extracts from Leaves and Flowers of Camellia japonica L. (동백나무 잎과 꽃 추출물의 항미생물 활성 및 항산화 효과)

  • Lee, Sook-Young;Hwang, Eun-Ju;Kim, Gi-Hae;Choi, Young-Bok;Lim, Chae-Young;Kim, Sun-Min
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.3
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    • pp.93-100
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    • 2005
  • This research was performed to investigate the possibilities of industrial usage of camellia (Camellia japonica L.) by examining the antioxidant and antimicrobial effects of methanol extract with different sections. Content of total phenolics, DPPH radical scavenging activities and antibacterial activity of young leaf, mature leaf, flower bud, flower, bark, and seed of camellia were compared in vitro experimental models. Total phenolics was contained the higher in young leaf (74.62 mg), flower bud (65.02 mg) and flower (62.42 mg) but less than 20.95 mg per 100 g of dry weight in other parts of Camellia japonica L. And effects of antioxidant measured by DPPH radical scavenger activity ($RC_{50}$, reduce concentration 50%), was shown higher $7.16{\sim}18.14\;{\mu}g/m{\ell}$ in methanol extract of young leaf, flower bud and flower than $61.23\;{\mu}g/m{\ell}$ of BHT as a chemical oxidant. Also, the antimicrobial activity of Camellia japonica L. extracts determined using a paper disc method against food-borne pathogen and food spoilage bacteria, the young leaves extracts showed the most active antimicrobial activity against 7 kinds of harmful microorganisms. Flower bud extracts showed the highest antibacterial activity against P. aeruginosa and Enterobacter spp. C1036. In addition, the minimum inhibitory concentration (MIC) of young leaf extract against B. subtillis,S. fradiae,S. aureus,E. coli,P. aeruginosa, Enterobacter spp. C1036, and S. typhimurium were revealed 1 to 15 ${\mu}g/m{\ell}$. As a result, antimicrobial activity of camellia extracts was shown higher gram positive bacteria than gram negative bacteria.

Antibacterial Effects of Natural Essential Oils from Various Spices against Vibrio Species and Their Volatile Constituents (몇 가지 천연 향신료 정유의 Vibrio속 균주들에 대한 항균효과 및 그 휘발성 성분)

  • Yoo, Mi-Ji;Kim, Yong-Suk;Shin, Dong-Hwa
    • Korean Journal of Food Science and Technology
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    • v.38 no.3
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    • pp.438-443
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    • 2006
  • Antibacterial effects of six volatile essential oils against Vibrio sp. were evaluated. Volatile components of essential oil were analyzed by gas chromatography and gas chromatography mass spectrometry. Ginger oil treatment inhibited growth of V. parahaemolyticus by 22.5-85.7%. Main volatile compounds of ginger oil were ${\beta}-bisabolene$ (35.19%, peak area) and ${\beta}-sesquiphellandrene$ (12.22%). V. parahaemolyticus was completely inhibited at 1,000 ppm by treatment with mustard oil. Tolerances of V. vulnificus 01 and 02 were twice higher than that of V. parahaemolyticus. Main volatile compound of mustard oil was allyl isothiocyanate (92.55%). Garlic oil treatment of 1,000 ppm inhibited growths of V. parahaemolyticus, V. vulnificus 01, and V. vulnificus 02 by 22.8, 14.6, and 32.9%, respectively. Main volatile compounds of garlic oil were dimethyl sulfide (49.39%) and methyl 2-propenyl disulfide (10.09%). Growth of V. vulnificus 02 was inhibited by 60.6-80.3% via treatment with bud, leaf, and whole oil of clove. Antibacterial activity of whole clove oil on V. vulnificus 02 was stronger than those of ginger, mustard, and garlic oil. Main volatile compounds were eugenol (83.33%) and ${\beta}-caryophyllene$ (7.47%) in clove bud, eugenol (87.46%) and ${\beta}-caryophyllene$ (10.03%) in clove leaf, and eugenol (86.04%) and ${\beta}-caryophyllene$ (9.71%) in whole clove. These results revealed essential oils from spices could be used as potential agents to inhibit Vibrio sp.