Antimicrobial Activity of Artemisinin and Precursor Derived fromIn VitroPlantlets ofArtemisia annuaL.

Artemisia annuaL., a medicinal herb, produces secondary metabolites with antimicrobial property. In Malaysia due to the tropical hot climate,A. annuacould not be planted for production of artemisinin, the main bioactive compound. In this study, the leaves of threein vitro A. annuaL. clones were, extracted and two bioactive compounds, artemisinin and a precursor, were isolated by thin layer chromatography. These compounds were found to be effective in inhibiting the growth of Gram-positive and Gram-negative bacteria but notCandida albicans. Their antimicrobial activity was similar to that of antibactericidal antibiotic streptomycin. They were found to inhibit the growth of the tested microbes at the minimum inhibition concentration of 0.09 mg/mL, and toxicity test using brine shrimp showed that even the low concentration of 0.09 mg/mL was very lethal towards the brine shrimps with 100% mortality rate. This study hence indicated thatin vitrocultured plantlets ofA. annuacan be used as the alternative method for production of artemisinin and its precursor with antimicrobial activities.

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Isolation, Screening and Antimicrobial Activity of Aeromonas hydrophila from Spoiled Vegetables and Biochemical Analysis of Estuarine Microbial Sediments

Current Biotechnology ◽

10.2174/2211550109666200302121552 ◽

2020 ◽

Vol 9 (3) ◽

pp. 192-197

Author(s):

Kumar Swathi ◽

Duraisamy Ramachandhiran ◽

Raju Murali ◽

Veerasamy Vinothkumar

Keyword(s):

Antimicrobial Activity ◽

Aeromonas Hydrophila ◽

Biochemical Analysis ◽

Bioactive Compound ◽

Antimicrobial Activities ◽

Gram Negative ◽

Enzyme Screening ◽

Pseudomonas Species ◽

Layer Chromatography ◽

Spore Forming Bacteria

Background: Aeromonas hydrophila is a heterotrophic, Gram-negative, rod-shaped, facultative anaerobic, non-spore forming bacteria that are autochthonous and widely dispersed in marine environments. The study aims at investigating the screening of Aeromonas hydrophila from spoiled vegetables and the sediment sample collected from three different estuaries located in the Bay of Bengal (Vedharanyam, Parangipettai and Pichavaram, Tamilnadu, India) for the presence of enzymes and antimicrobial activities. Objective: Isolation, enzyme screening, antimicrobial activity of Aeromonas hydrophila from spoiled vegetables and three different estuarine microbial sediment samples for the purpose of biochemical and enzymatic analysis. Methods: The bioactive compound produced by this strain was purified by using thin-layer chromatography. Results: The purified isolate of Aeromonas hydrophila strain produces good antimicrobial activity against Aspergillus niger, Candida albicans, Staphylococcus, Klebsiella and pseudomonas species. Conclusion: These isolates producing amylase, protease, lipase, and gelatinase enzymes, which are commercially very important and used in many industries and other biochemical sectors.

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Synthesis, lipophilicity and antimicrobial activity evaluation of some new thiazolyl-oxadiazolines

Medicine and Pharmacy Reports ◽

10.15386/cjmed-473 ◽

2015 ◽

Vol 88 (4) ◽

pp. 521-529 ◽

Cited By ~ 1

Author(s):

Cristina Ioana Stoica ◽

Ioana Ionuț ◽

Adrian Pîrnău ◽

Carmen Pop ◽

Ancuța Rotar ◽

...

Keyword(s):

Antimicrobial Activity ◽

Antimicrobial Agents ◽

Chemical Characterization ◽

Principal Component ◽

Antimicrobial Activities ◽

Bacterial Strains ◽

Pca Method ◽

Physical And Chemical ◽

Layer Chromatography

Background and aims. Synthesis of new potential antimicrobial agents and evaluation of their lipophilicity.Methods. Ten new thiazolyl-oxadiazoline derivatives were synthesized and their structures were validated by 1H-NMR and mass spectrometry. The lipophilicity of the compounds was evaluated using the principal component analysis (PCA) method. The necessary data for applying this method were obtained by reverse-phase thin-layer chromatography (RP-TLC). The antimicrobial activities were tested in vitro against four bacterial strains and one fungal strain.Results. The lipophilicity varied with the structure but could not be correlated with the antimicrobial activity, since this was modest.Conclusions. We have synthesized ten new heterocyclic compounds. After their physical and chemical characterization, we determined their lipophilicity and screened their antimicrobial activity.

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In vitro antimicrobial activities of several extracts endophytic Pseudomonas azotoformans UICC B-91

IOP Conference Series Earth and Environmental Science ◽

10.1088/1755-1315/948/1/012068 ◽

2021 ◽

Vol 948 (1) ◽

pp. 012068

Author(s):

E Oktarina ◽

R H Pratiwi ◽

W Mangunwardoyo ◽

I Hidayat ◽

E Saepudin

Keyword(s):

Staphylococcus Aureus ◽

Crude Extract ◽

Pathogenic Bacteria ◽

Bioactive Compound ◽

Antimicrobial Activities ◽

Inhibitory Effect ◽

Diffusion Method ◽

Minimum Concentration ◽

Layer Chromatography

Abstract Pseudomonas azotoformans known for the benefit on agriculture area as soil fertility enhancer. Pseudomonas azotoformans UICC B-91 was successfully isolated from tissues of N. altissima which traditionally known for treating infectious diseases. Therefore, endophytic P. azotoformans might contain antimicrobial compound. This research aims on exploring the antimicrobial activities of several extracts P. azotoformans UICC B-91 against pathogenic microbes. Isolates were extracted with dichloromethane, chloroform, and ethyl acetate. Each crude extract was observed for its potential antimicrobial activity with disc diffusion method against several pathogen microbes. Bioactive compound was assayed by thin layer chromatography (TLC) and screened by bioautography. Results indicated that all crude extract have inhibitory effect on Escherichia coli ATCC 8739, Bacillus cereus ATCC 10876, Staphylococcus aureus ATCC 6583, Staphylococcus aureus ATCC 25923, Salmonella typhimurium ATCC 25241, Pseudomonas aeruginosa ATCC 15442, Bacillus subtilis ATCC 19659 and Candida albicans ATCC 10231. Highest clear zone was on dichloromethane extract. TLC fraction of dichloromethane extract was able to inhibit growth on pathogenic bacteria (except for B. subtilis ATCC 19659 and S. aureus ATCC 6583) and fungi at minimum concentration in the range 125-1,000 μg/mL and 125 μg/mL, respectively. Bioactive compound from endophytic P. azotoformans extracted with dichloromethane have antibacterial and anticandidal effect.

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Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

Current Bioactive Compounds ◽

10.2174/1573407214666180226130957 ◽

2019 ◽

Vol 15 (1) ◽

pp. 63-70

Author(s):

Shiv Dev Singh ◽

Arvind Kumar ◽

Firoz Babar ◽

Neetu Sachan ◽

Arun Kumar Sharma

Keyword(s):

Antimicrobial Activity ◽

Potassium Hydroxide ◽

Antimicrobial Agents ◽

Pyrimidine Ring ◽

Antimicrobial Activities ◽

Screening Methods ◽

Chlorpheniramine Maleate ◽

In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

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In Vitro Antimicrobial Activity of Essential Oil Extracted from Leaves of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le in Vietnam

Plants ◽

10.3390/plants9040453 ◽

2020 ◽

Vol 9 (4) ◽

pp. 453 ◽

Cited By ~ 8

Author(s):

Nhan Trong Le ◽

Duc Viet Ho ◽

Tuan Quoc Doan ◽

Anh Tuan Le ◽

Ain Raal ◽

...

Keyword(s):

Antimicrobial Activity ◽

Chemical Composition ◽

Essential Oil ◽

Inhibitory Concentration ◽

Antimicrobial Activities ◽

Antiviral Effects ◽

Scientific Report ◽

Main Components ◽

Hiv 1

The present study aimed to determine the antimicrobial activity and chemical composition of leaves-extracted essential oil of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le (L. domatiophorus), including antibacterial, antimycotic, antitrichomonas and antiviral effects. The essential oil was obtained using hydrodistillation, with an average yield of 0.34 ± 0.01% (v/w, dry leaves). There were 52 constituents as identified by GC/MS with available authentic standards, representing 96.74% of the entire leaves oil. The essential oil was comprised of three main components, namely viridiflorene (16.47%), (-)-δ-cadinene (15.58%) and γ-muurolene (8.00%). The oil showed good antimicrobial activities against several species: Gram-positive strains: Staphylococcus aureus (two strains) and Enterococcus faecalis, with Minimum Inhibitory Concentration (MIC) and Minimum Lethal Concentration (MLC) values from 0.25 to 1% (v/v); Gram-negative strains such as Escherichia coli (two strains), Pseudomonas aeruginosa (two strains) and Klebsiella pneumoniae, with MIC and MLC values between 2% and 8% (v/v); and finally Candida species, having MIC and MLC between 0.12 and 4% (v/v).Antitrichomonas activity of the oil was also undertaken, showing IC50, IC90 and MLC values of 0.008%, 0.016% and 0.03% (v/v), respectively, after 48h of incubation. The essential oil resultedin being completely ineffective against tested viruses, ssRNA+ (HIV-1, YFV, BVDV, Sb-1, CV-B4), ssRNA- (hRSVA2, VSV), dsRNA (Reo-1), and dsDNA (HSV-1, VV) viruses with EC50 values over 100 µg/mL. This is the first, yet comprehensive, scientific report about the chemical composition and pharmacological properties of the essential oil in L. domatiophorus.

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Screening of Antimicrobial Activity and Cytotoxic Effects of Two Cladonia Species

Zeitschrift für Naturforschung C ◽

10.1515/znc-2013-5-604 ◽

2013 ◽

Vol 68 (5-6) ◽

pp. 191-197 ◽

Cited By ~ 2

Author(s):

Birkan Açıkgöz ◽

İskender Karaltı ◽

Melike Ersöz ◽

Zeynep M. Coşkun ◽

Gülşah Çobanoğlu ◽

...

Keyword(s):

Antimicrobial Activity ◽

Antimicrobial Activities ◽

Chloroform Extract ◽

Cytotoxic Effects ◽

Minimal Inhibitory Concentrations ◽

E Coli ◽

Methanol Extracts ◽

Gram Positive Bacteria

The present study explores the antimicrobial activity and cytotoxic effects in culture assays of two fruticose soil lichens, Cladonia rangiformis Hoffm. and Cladonia convoluta (Lamkey) Cout., to contribute to possible pharmacological uses of lichens. In vitro antimicrobial activities of methanol and chloroform extracts against two Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), two Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus), and the yeast Candida albicans were examined using the paper disc method and through determination of minimal inhibitory concentrations (MICs). The data showed the presence of antibiotic substances in the chloroform and the methanol extracts of the lichen species. The chloroform extracts exhibited more signifi cant antimicrobial activity than the methanol extracts. However, a higher antifungal activity was noted in the methanol extract of C. rangiformis. The maximum antimicrobial activity was recorded for the chloroform extract of C. convoluta against E. coli. The cytotoxic effects of the lichen extracts on human breast cancer MCF-7 cells were evaluated by the trypan blue assay yielding IC50 values of ca. 173 and 167 μg/ml for the extracts from C. rangiformis and C. convoluta, respectively.

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Screening of antimicrobial activity of essential oil and methanol extract of Satureja hortensis on foodborne bacteria and fungi

Czech Journal of Food Sciences ◽

10.17221/753-cjfs ◽

2008 ◽

Vol 25 (No. 2) ◽

pp. 81-89 ◽

Cited By ~ 43

Author(s):

A. Adiguzel ◽

H. Ozer ◽

H. Kilic ◽

B. Cetin

Keyword(s):

Antimicrobial Activity ◽

Chemical Composition ◽

Minimum Inhibitory Concentration ◽

Essential Oil ◽

Inhibitory Concentration ◽

Methanol Extract ◽

Antimicrobial Activities ◽

Satureja Hortensis ◽

Bacteria And Fungi

The present work reports the in vitro antimicrobial activities of the essential oil and methanol extract from Satureja hortensis as well as the content of its essential oil. The chemical composition of hydrodistilled essential oil of Satureja hortensis was analysed by means of GC-MS. Thirty constituents were identified. The main constituents of the oil were thymol (40.54%), γ-terpinene (18.56%), carvacrol (13.98%), and p-cymene (8.97). The essential oil of Satureja hortensis exhibited the activity against 25 bacteria, 8 fungi, and a yeast, C. albicans; exerting the Minimum Inhibitory Concentration values (MIC) ranging from 15.62 to 250 µl/ml. Similarly, methanol extract of the plant also showed antimicrobial activity.

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Dissociating antibacterial from ototoxic effects of gentamicin C-subtypes

Proceedings of the National Academy of Sciences ◽

10.1073/pnas.2013065117 ◽

2020 ◽

Vol 117 (51) ◽

pp. 32423-32432

Author(s):

Mary E. O’Sullivan ◽

Yohan Song ◽

Robert Greenhouse ◽

Randy Lin ◽

Adela Perez ◽

...

Keyword(s):

Antimicrobial Activity ◽

Side Effects ◽

Hair Cell ◽

Aminoglycoside Antibiotic ◽

Antimicrobial Activities ◽

Proof Of Concept ◽

Cell Toxicity ◽

Structure Activity ◽

Future Drug

Gentamicin is a potent broad-spectrum aminoglycoside antibiotic whose use is hampered by ototoxic side-effects. Hospital gentamicin is a mixture of five gentamicin C-subtypes and several impurities of various ranges of nonexact concentrations. We developed a purification strategy enabling assaying of individual C-subtypes and impurities for ototoxicity and antimicrobial activity. We found that C-subtypes displayed broad and potent in vitro antimicrobial activities comparable to the hospital gentamicin mixture. In contrast, they showed different degrees of ototoxicity in cochlear explants, with gentamicin C2b being the least and gentamicin C2 the most ototoxic. Structure–activity relationships identified sites in the C4′-C6′ region on ring I that reduced ototoxicity while preserving antimicrobial activity, thus identifying targets for future drug design and mechanisms for hair cell toxicity. Structure–activity relationship data suggested and electrophysiological data showed that the C-subtypes both bind and permeate the hair cell mechanotransducer channel, with the stronger the binding the less ototoxic the compound. Finally, both individual and reformulated mixtures of C-subtypes demonstrated decreased ototoxicity while maintaining antimicrobial activity, thereby serving as a proof-of-concept of drug reformulation to minimizing ototoxicity of gentamicin in patients.

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DESIGN AND SYNTHESIS OF NOVEL 1-((DIMETHYLAMINO)METHYL)-3-(4-(3-(SUBSTITUTE DPHENYL)-4-OXOTHIAZOLIDIN-2-YL)PHENYLIMINO)-5-NITROINDOLIN-2-ONES AS POTENT ANTITUBERCULAR AGENTS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i5.31965 ◽

2019 ◽

pp. 200-207

Author(s):

KOSARAJU LAHARI ◽

RAJA SUNDARARAJAN

Keyword(s):

Antimicrobial Activity ◽

Antimicrobial Agents ◽

Biological Activities ◽

Antimicrobial Activities ◽

Mannich Bases ◽

Proton Nuclear Magnetic Resonance ◽

Design And Synthesis ◽

Group Variation

Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results. Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi. Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed. Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.

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In VitroAntimicrobial Activity of Essential Oil ofThymus schimperi,Matricaria chamomilla,Eucalyptus globulus, andRosmarinus officinalis

International Journal of Microbiology ◽

10.1155/2016/9545693 ◽

2016 ◽

Vol 2016 ◽

pp. 1-8 ◽

Cited By ~ 30

Author(s):

Awol Mekonnen ◽

Berhanu Yitayew ◽

Alemnesh Tesema ◽

Solomon Taddese

Keyword(s):

Antimicrobial Activity ◽

Minimum Inhibitory Concentration ◽

Essential Oil ◽

Essential Oils ◽

Inhibitory Concentration ◽

Antimicrobial Activities ◽

Diffusion Method ◽

Drug Preparation ◽

Bacteria And Fungi

In this study, thein vitroantimicrobial activities of four plant essential oils (T. schimperi,E. globulus,R. officinalis, andM. Chamomilla) were evaluated against bacteria and fungi. The studies were carried out using agar diffusion method for screening the most effective essential oils and agar dilution to determine minimum inhibitory concentration of the essential oils. Results of this study revealed that essential oils ofT. schimperi,E. globulus, andR. officinaliswere active against bacteria and some fungi. The antimicrobial effect ofM. chamomillawas found to be weaker and did not show any antimicrobial activity. The minimum inhibitory concentration values ofT. schimperiwere<15.75 mg/mL for most of the bacteria and fungi used in this study. The minimum inhibitory concentration values of the other essential oils were in the range of 15.75–36.33 mg/mL against tested bacteria. This study highlighted the antimicrobial activity of the essential oil ofE. globulus,M. chamomilla,T. Schimperi, andR. officinalis. The results indicated thatT. schimperihave shown strong antimicrobial activity which could be potential candidates for preparation of antimicrobial drug preparation.

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