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Fulltext Culture-proven bacterial keratitis in a Malaysian general hospital

Hooi SH, Hooi ST

Med J Malaysia, 2005 Dec;60(5):614-23.
PMID: 16515113

One hundred patients (101 eyes) with culture-proven bacterial keratitis were treated in the Department of Ophthalmology, Hospital Sultanah Aminah, Johor Bahru, over a 4-year period. The majority of patients was male (63%), Malay (60%), from the Johor Bahru district (62%) and aged between 41 to 50 years (20%). The ocular predisposing factors were ocular trauma (41 eyes), ocular surface disease (28 eyes) and contact lens wear (26 eyes). The corneal ulcers were mainly large (50.5%), central (59.4%) and colonized by Gram-negative bacteria (78.1%). The most frequently isolated microorganisms were Pseudomonas aeruginosa (67 eyes), Staphylococcus aureus (12 eyes), Acinetobacter baumanii (6 eyes), Klebsiella pneumoniae (5 eyes), Corynebacterium sp. (3 eyes:) and Streptococcus pneumonliae (3 eyes). Twelve eyes (11.8%) had polymicrobial infection. A good visual outcome occurred in 52.5% of eyes analysed. Prognostic factors for visual outcome include presenting Snellen visual acuity, time to presentation after onset of ocular symptoms, ocular predisposing factor, corneal ulcer location and corneal ulcer size.

Matched MeSH terms: Gram-Negative Bacteria/isolation & purification*
Antimicrobial activity of tiger's betel (Piper porphyrophyllum N.E. Br., Piperaceae)

Wiart C, Hannah NA, Yassim M, Hamimah H, Sulaiman M

Phytother Res, 2004 Sep;18(9):783-4.
PMID: 15478188

The ethanol extract of leaves of Piper porphyrophyllum N.E. Br. showed a broad spectrum of antibacterial activity. The activity was increased on fractionation (hexane, dichloromethane and aqueous), particularly in the aqueous fraction. No activity was shown against tested Candida albicans.

Matched MeSH terms: Gram-Negative Bacteria/drug effects
Antibacterial and antioxidant activity of naphthofuranquinones from the twigs of tropical mangrove Avicennia officinalis

Assaw S, Mohd Amir MIH, Khaw TT, Bakar K, Mohd Radzi SA, Mazlan NW

Nat Prod Res, 2020 Aug;34(16):2403-2406.
PMID: 30600710 DOI: 10.1080/14786419.2018.1538220

Mangrove plants are endowed with various biologically active compounds which have potent antibacterial and antioxidant properties. In present study, a bioactivity-guided fractionation for antibacterial and antioxidant active metabolites from the twigs of Avicennia officinalis collected from Kuala Selangor Nature Park, Selangor, Malaysia gave 13 major fractions. The antibacterial activity of A. officinalis fractions using well-diffusion showed strong selectivity on the Gram-positive bacteria (Staphylococcus epidermidis, S. aureus and Bacillus subtilis) with minimum inhibition concentration (MIC) values of 0.156-5.00 mg/mL. However, no antibacterial activities were observed on the Gram-negative bacteria (Vibrio cholera, Enterobacter cloacae and Escherichia coli). The active antibacterial fractions were further isolated using several chromatographic techniques to give two naphthofuranquinones, namely, avicenol C (1) and stenocarpoquinone B (2). Meanwhile, the antioxidant activity of A. officinalis fractions were evaluated using DPPH radical scavenging assay exhibited low antioxidant activities. Molecular structure of the naphthofuranquinones was elucidated using 1 D and 2 D NMR spectroscopy.

Matched MeSH terms: Gram-Negative Bacteria/drug effects
Gut bacteria of cockroaches are a potential source of antibacterial compound(s)

Akbar N, Siddiqui R, Iqbal M, Sagathevan K, Khan NA

Lett Appl Microbiol, 2018 May;66(5):416-426.
PMID: 29457249 DOI: 10.1111/lam.12867

Here, we hypothesized that the microbial gut flora of animals/pests living in polluted environments, produce substances to thwart bacterial infections. The overall aim of this study was to source microbes inhabiting unusual environmental niches for potential antimicrobial activity. Two cockroach species, Gromphadorhina portentosa (Madagascar) and Blaptica dubia (Dubia) were selected. The gut bacteria from these species were isolated and grown in RPMI 1640 and conditioned media were prepared. Conditioned media were tested against a panel of Gram-positive (Methicillin-resistant Staphylococcus aureus, Streptococcus pyogenes, Bacillus cereus) and Gram-negative (Escherichia coli K1, Salmonella enterica, Serratia marcescens, Pseudomonas aeruginosa, Klebsiella pneumoniae) bacteria, as well as the protist pathogen, Acanthamoeba castellanii. The results revealed that the gut bacteria of cockroaches produce active molecule(s) with potent antibacterial properties, as well as exhibit antiamoebic effects. However, heat-inactivation at 95°C for 10 min had no effect on conditioned media-mediated antibacterial and antiamoebic properties. These results suggest that bacteria from novel sources i.e. from the cockroach's gut produce molecules with bactericidal as well as amoebicidal properties that can ultimately lead to the development of therapeutic drugs.
SIGNIFICANCE AND IMPACT OF THE STUDY: The bacteria isolated from unusual dwellings such as the cockroaches' gut are a useful source of antibacterial and antiamoebal molecules. These are remarkable findings that will open several avenues in our search for novel antimicrobials from unique sources. Furthermore studies will lead to the identification of molecules to develop future antibacterials from insects.

Matched MeSH terms: Gram-Negative Bacteria/drug effects*
Synthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens

Hong W, Li J, Chang Z, Tan X, Yang H, Ouyang Y, et al.

J Antibiot (Tokyo), 2017 Jul;70(7):832-844.
PMID: 28465626 DOI: 10.1038/ja.2017.55

The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus. Four of these strains showed additional activity against Gram-negative bacteria, including extended-spectrum beta-lactamase producing Enterobacteriaceae, imipenem-resistant Klebsiella pneumoniae and multidrug-resistant Acinetobacter baumanii, and against Mycobacterium tuberculosis H37Ra. These four compounds are candidates for developing into broad-spectrum anti-infective agents.

Matched MeSH terms: Gram-Negative Bacteria/drug effects*
Are secondary forests second-rate? Comparing peatland greenhouse gas emissions, chemical and microbial community properties between primary and secondary forests in Peninsular Malaysia

Dhandapani S, Ritz K, Evers S, Yule CM, Sjögersten S

Sci Total Environ, 2019 Mar 10;655:220-231.
PMID: 30471590 DOI: 10.1016/j.scitotenv.2018.11.046

Tropical peatlands are globally important ecosystems with high C storage and are endangered by anthropogenic disturbances. Microbes in peatlands play an important role in sustaining the functions of peatlands as a C sink, yet their characteristics in these habitats are poorly understood. This research aimed to elucidate the responses of these complex ecosystems to disturbance by exploring greenhouse gas (GHG) emissions, nutrient contents, soil microbial communities and the functional interactions between these components in a primary and secondary peat swamp forest in Peninsular Malaysia. GHG measurements using closed chambers, and peat sampling were carried out in both wet and dry seasons. Microbial community phenotypes and nutrient content were determined using phospholipid fatty acid (PLFA) and inductively-coupled plasma mass spectrometry (ICP-MS) analyses respectively. CO2 emissions in the secondary peat swamp forest were > 50% higher than in the primary forest. CH4 emission rates were ca. 2 mg m-2 h-1 in the primary forest but the secondary forest was a CH4 sink, showing no seasonal variations in GHG emissions. Almost all the nutrient concentrations were significantly lower in the secondary forest, postulated to be due to nutrient leaching via drainage and higher rates of decomposition. Cu and Mo concentrations were negatively correlated with CO2 and CH4 emissions respectively. Microbial community structure was overwhelmingly dominated by bacteria in both forest types, however it was highly sensitive to land-use change and season. Gram-positive and Gram-negative relative abundance were positively correlated with CO2 and CH4 emissions respectively. Drainage related disturbances increased CO2 emissions, by reducing the nutrient content including some with known antimicrobial properties (Cu & Na) and by favouring Gram-positive bacteria over Gram-negative bacteria. These results suggest that the biogeochemistry of secondary peat swamp forest is fundamentally different from that of primary peat swamp forest, and these differences have significant functional impacts on their respective environments.

Matched MeSH terms: Gram-Negative Bacteria/isolation & purification
Synergistic antibacterial actions of graphene oxide and antibiotics towards bacteria and the toxicological effects of graphene oxide on human epidermal keratinocytes

Pulingam T, Thong KL, Appaturi JN, Nordin NI, Dinshaw IJ, Lai CW, et al.

Eur J Pharm Sci, 2020 Jan 15;142:105087.
PMID: 31626968 DOI: 10.1016/j.ejps.2019.105087

Graphene oxide (GO) has displayed antibacterial activity that has been investigated in the past, however, information on synergistic activity of GO with conventional antibiotics is still lacking. The objectives of the study were to determine the combinatorial actions of GO and antibiotics against Gram-positive and Gram-negative bacteria and the toxicological effects of GO towards human epidermal keratinocytes (HaCaT). Interactions at molecular level between GO and antibiotics were analyzed using Attenuated Total Reflectance-Fourier-transform infrared spectroscopy (ATR-FTIR). Changes in the antibacterial activity of antibiotics towards bacteria through the addition of GO was investigated. Toxicity of GO towards HaCaT cells were examined as skin cells play a role as the first line of defense of the human body. The ATR-FTIR characterizations of GO and antibiotics showed adsorption of tested antibiotics onto GO. The combinatorial antibacterial activity of GO and antibiotics were found to increase when compared to GO or antibiotic alone. This was attributed to the ability of GO to disrupt bacterial membrane to allow for better adsorption of antibiotics. Cytotoxicity of GO was found to be dose-dependent towards HaCaT cell line, it is found to impose negligible toxic effects against the skin cells at concentration below 100 μg/mL.

Matched MeSH terms: Gram-Negative Bacteria/drug effects*
Antimicrobial Exploration Between Counterpart Endosymbiont and Host Plant (Tamarindus indica Linn.)

Chigurupati S, Vijayabalan S, Selvarajan KK, Aldubayan M, Alhowail A, Mani V, et al.

Curr Pharm Biotechnol, 2020;21(5):384-389.
PMID: 31657678 DOI: 10.2174/1389201020666191028105325

BACKGROUND: Endophytic bacteria produce various bioactive secondary metabolites, which benefit human health. Tamarindus indica L. is well known for its medicinal value in human health care. Several studies have reported on its biological effects from various parts of T. indica, but only a few studies have been devoted to examining the biological activity of endophytes of T. indica.
OBJECTIVES: In the present study, an endophyte was isolated from the leaves of T. indica and screened for its antimicrobial potential.
METHODS: The selected endophyte was identified by 16s rRNA partial genome sequencing and investigated for their antimicrobial potency. The preliminary phytochemical tests were conducted for the affirmation of phytoconstituents in the endophytic crude ethyl acetate extract of T. indica (TIM) and total phenolic content was performed. The antimicrobial potential of TIM was evaluated against human pathogenic ATCC gram-positive and gram-negative bacterial strains.
RESULTS: TIM exhibited an appreciable amount of gallic acid equivalent phenolic content (21.6 ± 0.04 mg GAE/g of crude extract). TIM showed the Minimum Inhibitory Concentration (MIC) at 250 μg/mL and Minimum Bactericidal Concentration (MBC) at 500 μg/mL among the selected human pathogenic ATCC strains. At MIC of 500 μg/mL, TIM displayed a significant zone of inhibition against P. aeruginosa and N. gonorrhoeae.
CONCLUSION: The results from our study highlighted for the first time the antimicrobial potential of endophytic bacterial strain Bacillus velezensis in T. indica leaves and it could be further explored as a source of natural antimicrobial agents.

Matched MeSH terms: Gram-Negative Bacteria/drug effects
Antibiotic resistance and sensitivity pattern of Metallo-β-Lactamase Producing Gram-Negative Bacilli in ventilator-associated pneumonia in the intensive care unit of a public medical school hospital in Bangladesh

Nusrat T, Akter N, Rahman NAA, Godman B, D Rozario DT, Haque M

Hosp Pract (1995), 2020 Aug;48(3):128-136.
PMID: 32271642 DOI: 10.1080/21548331.2020.1754687

BACKGROUND: Ventilator-associated pneumonia (VAP) is the most common nosocomial infection in intensive care units (ICU), accounting for 25% of all ICU infections. Antimicrobial resistance is increasing and becoming a significant health problem worldwide, increasing hospital length of stay, mortality and costs. Identifying antibiotic resistance patterns in VAP is important as this can cause outbreaks in ICUs. To date, there have been limited studies assessing this in Bangladesh. Consequently, the primary objective of this research was to study the species of bacterial growth and to determine the antibiotic resistance patterns of Metallo-β-Lactamase (MBL) producing gram-negative bacilli among ICU patients with VAP in a public medical school hospital, Bangladesh. In addition, identify the factors associated with a positive culture to provide future guidance.
METHOD: Cross-sectional study performed in the Chattogram Medical College Hospital, Bangladesh. Mueller Hinton agar plates were used for antibiotic sensitivity testing by the Kirby-Buer disc diffusion test.
RESULTS: Among 105 clinically suspected VAP cases, qualitative cultures were positive in 95 (90%) of them. The most common bacteria identified were Acinetobacter spp. (43.2%), Klebsiella spp. (20%) and Pseudomonas spp. (18.9%). A positive culture was not associated with patients' age or gender. Among 41 isolated Acinetobacter spp., 38 (92.7%) were resistant to gentamicin followed by 36 (87.8%) to ceftriaxone. Among 24 isolated Klebsiella spp., 22 (83.3%) were resistant to ceftriaxone. Among 18 isolated Pseudomonas spp., 16 (88.8%) were resistant to ciprofloxacin, and 13 (72.2%) were resistant to ceftriaxone. Among nine isolated E.coli, all were resistant to ceftriaxone and ciprofloxacin. All four Proteus spp. (100%) isolated were resistant to ciprofloxacin. Additionally, phenotype MBL producing was 65.22% and genotype was 45.65% among imipenem resistant pathogens. Imipenem resistant pathogens were sensitive to amoxyclav, amikacin¸ azithromycin, ceftazidime, ceftriaxone, colistin and gentamycin.
CONCLUSION: A positive culture was detected in 90% of VAP patients, but it was not associated with the patients' age and gender. The most common bacteria identified were Acinetobacter spp., Klebsiella spp. and Pseudomonas spp., where the majority of these were resistant to ceftriaxone. The results are being used to provide future guidance on the empiric management of VAP in this hospital.

Matched MeSH terms: Gram-Negative Bacteria/isolation & purification*
Fulltext Free radical scavenging, antimicrobial and immunomodulatory activities of Orthosiphon stamineus

Alshawsh MA, Abdulla MA, Ismail S, Amin ZA, Qader SW, Hadi HA, et al.

Molecules, 2012;17(5):5385-95.
PMID: 22569417 DOI: 10.3390/molecules17055385

Orthosiphon stamineus is considered an important traditional folk medicine. In this study ethanol and aqueous extracts of O. stamineus were evaluated in vitro for their antioxidant, antimicrobial as well as for their immunomodulatory properties on human peripheral blood mononuclear cells (PBMCs). The DPPH radical scavenging method was used for the determination of antioxidant activity, while the antibacterial efficacy was investigated by both disc diffusion method and Minimum Inhibitory Concentration (MIC) against four bacterial strains (Gram-positive and Gram-negative). Furthermore, the immunomodulatory potential of the extracts was investigated through the MTT assay. Aqueous extract of O. stamineus exhibited significant free radical scavenging activity with IC₅₀ 50 9.6 µg/mL, whereas the IC₅₀ for the ethanol extract was 21.4 µg/mL. The best antimicrobial activity was shown by the aqueous extract of O. stamineus against Staphylococcus aureus, with inhibition zone of 10.5 mm and MIC value 1.56 mg/mL. Moreover, the results observed from the MTT assay showed that both plant extracts stimulated the PBMCs proliferation in vitro in a concentration-dependent manner, but the aqueous extract has remarkable activity against PBMCs. These findings indicate that O. stamineus showed high antioxidant activity and may be considered as an immunomodulatory agent.

Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/growth & development
Fulltext Sustainable drug release from polycaprolactone coated chitin-lignin gel fibrous scaffolds

Abudula T, Gauthaman K, Mostafavi A, Alshahrie A, Salah N, Morganti P, et al.

Sci Rep, 2020 11 24;10(1):20428.
PMID: 33235239 DOI: 10.1038/s41598-020-76971-w

Non-healing wounds have placed an enormous stress on both patients and healthcare systems worldwide. Severe complications induced by these wounds can lead to limb amputation or even death and urgently require more effective treatments. Electrospun scaffolds have great potential for improving wound healing treatments by providing controlled drug delivery. Previously, we developed fibrous scaffolds from complex carbohydrate polymers [i.e. chitin-lignin (CL) gels]. However, their application was limited by solubility and undesirable burst drug release. Here, a coaxial electrospinning is applied to encapsulate the CL gels with polycaprolactone (PCL). Presence of a PCL shell layer thus provides longer shelf-life for the CL gels in a wet environment and sustainable drug release. Antibiotics loaded into core-shell fibrous platform effectively inhibit both gram-positive and -negative bacteria without inducting observable cytotoxicity. Therefore, PCL coated CL fibrous gel platforms appear to be good candidates for controlled drug release based wound dressing applications.

Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/growth & development
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases

Narender M, Jaswanth S B, Umasankar K, Malathi J, Raghuram Reddy A, Umadevi KR, et al.

Bioorg Med Chem Lett, 2016 Feb 01;26(3):836-840.
PMID: 26755393 DOI: 10.1016/j.bmcl.2015.12.083

Development of multidrug resistant (MDR) and extensively drug resistant (XDR) tuberculosis (TB) has been considered as major health burden, globally. In order to develop novel, potential molecules against drug resistant TB, twenty two (22) new 3-substituted-7-benzyl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one (6a-k) and 3-substituted-7-benzyl-2-methyl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one (7a-k) derivatives were designed and synthesized by using appropriate synthetic protocols. Pantothenate synthetase (PS) was considered as the target for the molecular docking studies and evaluated the binding pattern at active site, as PS plays a significant role in the biosynthesis of pantothenate in Mycobacterium tuberculosis (MTB). The preliminary in vitro antibacterial screening of test compounds was carried out against two strains of Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli and Klebsiella pneumoniae) bacteria. The antimycobacterial screening was performed against MTB H37Rv and an isoniazid-resistant clinical isolate of MTB. The compounds 6b, 6c, 6d, 6k, 7b, 7c, 7d and 7k exhibited promising antibacterial activity MIC in the range of 15-73 μM against all bacterial strains used and compounds 6d and 7b showed antimycobacterial activity (IC50 <340 μM in LRP assay) and (MIC <9 μM in broth microdilution method).

Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/metabolism
Intestinal carriage of multidrug-resistant gram-negative bacteria in preterm-infants during hospitalization in neonatal intensive care unit (NICU)

Yap PS, Ahmad Kamar A, Chong CW, Yap IK, Thong KL, Choo YM, et al.

Pathog Glob Health, 2016 Sep;110(6):238-246.
PMID: 27650884

The prevalence and antibiotic susceptibility of intestinal carriage of Gram-negative bacteria among preterm infants admitted to the neonatal intensive care unit (NICU) in a tertiary teaching hospital in Malaysia were determined. A total of 34 stool specimens were obtained from preterm infants upon admission and once weekly up to two weeks during hospitalization. The presumptive colonies of Escherichia coli and Klebsiella pneumoniae were selected for identification, antibiotic susceptibility testing, and subtyping by using pulsed-field gel electrophoresis (PFGE). Out of 76 Gram-negative isolates, highest resistance was detected for amoxicillin/clavulanate (30.8%, n = 16), ceftriaxone (42.3%, n = 22), ceftazidime (28.8%, n = 15), cefoxitin (28.8%, n = 15), aztreonam (36.5%, n = 19), and polymyxin B (23.1%, n = 12). Three colistin resistant K. pneumoniae have also been detected based on E-test analysis. Thirty-nine isolates of K. pneumoniae and 20 isolates of E. coli were resistant to more than three antimicrobial classes and were categorized as multidrug resistant (MDR). PFGE analysis revealed a higher diversity in pulsotypes for K. pneumoniae (18 pulsotypes) in comparison to E. coli (four pulsotypes). In addition, a total of fifteen pulsotypes was observed from 39 MDR K. pneumoniae. The risk factors for antibiotic resistance were assessed using random forest analysis. Gender was found to be the most important predictor for colistin resistant while length, OFC, and delivery mode were showing greater predictive power in the polymyxin B resistance. This study revealed worrying prevalence rates of intestinal carriage of multidrug-resistant K. pneumoniae and E. coli of hospitalized preterm infants in Malaysia, particularly high resistance to polymyxins.

Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/isolation & purification*
Fulltext Antimicrobial activities of Bacillus velezensis strains isolated from stingless bee products against methicillin-resistant Staphylococcus aureus

Baharudin MMA, Ngalimat MS, Mohd Shariff F, Balia Yusof ZN, Karim M, Baharum SN, et al.

PLoS One, 2021;16(5):e0251514.
PMID: 33974665 DOI: 10.1371/journal.pone.0251514

Infections caused by methicillin-resistant Staphylococcus aureus (MRSA) have reached epidemic proportions globally. Therefore, there is an urgent need for a continuous supply of antibiotics to combat the problem. In this study, bacteria initially identified as species belonging to the Bacillus amyloliquefaciens operational group were re-identified based on the housekeeping gene, gyrB. Cell-free supernatants (CFS) from the strains were used for antimicrobial tests using the agar well diffusion assay against MRSA and various types of pathogenic bacteria. The minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and physicochemical characteristics of the CFS were determined. Based on gyrB sequence analysis, five strains (PD9, B7, PU1, BP1 and L9) were identified as Bacillus velezensis. The CFS of all B. velezensis strains showed broad inhibitory activities against Gram-negative and -positive as well as MRSA strains. Strain PD9 against MRSA ATCC 33742 was chosen for further analysis as it showed the biggest zone of inhibition (21.0 ± 0.4 mm). The MIC and MBC values obtained were 125 μl/ml. The crude antimicrobial extract showed bactericidal activity and was stable at various temperatures (40-80°C), pH (4-12), surfactants (Tween 20, Tween 80, SDS and Triton X-100) and metal ions (MgCI2, NaCI2, ZnNO3 and CuSO4) when tested. However, the crude extract was not stable when treated with proteinase K. All these properties resembled the characteristics of peptides. The antimicrobial compound from the selected strain was purified by using solvent extraction method and silica gel column chromatography. The purified compound was subjected to High Performance Liquid Chromatography which resulted in a single peak of the anti-MRSA compound being detected. The molecular weight of the anti-MRSA compound was determined by using SDS-PAGE and zymogram. The size of the purified antimicrobial peptide was approximately ~ 5 kDa. The antimicrobial peptide produced from B. velezensis strain PD9 is a promising alternative to combat the spread of MRSA infections in the future.

Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/growth & development
Fulltext The Antimicrobial efficacy of Elaeis guineensis: characterization, in vitro and in vivo studies

Vijayarathna S, Zakaria Z, Chen Y, Latha LY, Kanwar JR, Sasidharan S

Molecules, 2012 Apr 26;17(5):4860-77.
PMID: 22538489 DOI: 10.3390/molecules17054860

The urgent need to treat multi-drug resistant pathogenic microorganisms in chronically infected patients has given rise to the development of new antimicrobials from natural resources. We have tested Elaeis guineensis Jacq (Arecaceae) methanol extract against a variety of bacterial, fungal and yeast strains associated with infections. Our studies have demonstrated that E. guineensis exhibits excellent antimicrobial activity in vitro and in vivo against the bacterial and fungal strains tested. A marked inhibitory effect of the E. guineensis extracts was observed against C. albicans whereby E. guineensis extract at ½, 1, or 2 times the MIC significantly inhibited C. albicans growth with a noticeable drop in optical density (OD) of the bacterial culture. This finding confirmed the anticandidal activity of the extract on C. albicans. Imaging using scanning (SEM) and transmission (TEM) electron microscopy was done to determine the major alterations in the microstructure of the extract-treated C. albicans. The main abnormalities noted via SEM and TEM studies were the alteration in morphology of the yeast cells. In vivo antimicrobial activity was studies in mice that had been inoculated with C. albicans and exhibited good anticandidal activity. The authors conclude that the extract may be used as a candidate for the development of anticandidal agent.

Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/growth & development
Fulltext Antimycobacterial, antimicrobial, and biocompatibility properties of para-aminosalicylic acid with zinc layered hydroxide and Zn/Al layered double hydroxide nanocomposites

Saifullah B, El Zowalaty ME, Arulselvan P, Fakurazi S, Webster TJ, Geilich BM, et al.

Drug Des Devel Ther, 2014;8:1029-36.
PMID: 25114509 DOI: 10.2147/DDDT.S63753

The treatment of tuberculosis by chemotherapy is complicated due to multiple drug prescriptions, long treatment duration, and adverse side effects. We report here for the first time an in vitro therapeutic effect of nanocomposites based on para-aminosalicylic acid with zinc layered hydroxide (PAS-ZLH) and zinc-aluminum layered double hydroxides (PAS-Zn/Al LDH), against mycobacteria, Gram-positive bacteria, and Gram-negative bacteria. The nanocomposites demonstrated good antimycobacterial activity and were found to be effective in killing Gram-positive and Gram-negative bacteria. A biocompatibility study revealed good biocompatibility of the PAS-ZLH nanocomposites against normal human MRC-5 lung cells. The para-aminosalicylic acid loading was quantified with high-performance liquid chromatography analysis. In summary, the present preliminary in vitro studies are highly encouraging for further in vivo studies of PAS-ZLH and PAS-Zn/Al LDH nanocomposites to treat tuberculosis.

Matched MeSH terms: Gram-Negative Bacteria/drug effects
Fulltext Synthesis of novel bisindolylmethane Schiff bases and their antibacterial activity

Imran S, Taha M, Ismail NH, Khan KM, Naz F, Hussain M, et al.

Molecules, 2014;19(8):11722-40.
PMID: 25102118 DOI: 10.3390/molecules190811722

In an effort to develop new antibacterial drugs, some novel bisindolylmethane derivatives containing Schiff base moieties were prepared and screened for their antibacterial activity. The synthesis of the bisindolylmethane Schiff base derivatives 3-26 was carried out in three steps. First, the nitro group of 3,3'-((4-nitrophenyl)-methylene)bis(1H-indole) (1) was reduced to give the amino substituted bisindolylmethane 2 without affecting the unsaturation of the bisindolylmethane moiety using nickel boride in situ generated. Reduction of compound 1 using various catalysts showed that combination of sodium borohydride and nickel acetate provides the highest yield for compound 2. Bisindolylmethane Schiff base derivatives were synthesized by coupling various benzaldehydes with amino substituted bisindolylmethane 2. All synthesized compounds were characterized by various spectroscopic methods. The bisindolylmethane Schiff base derivatives were evaluated against selected Gram-positive and Gram-negative bacterial strains. Derivatives having halogen and nitro substituent display weak to moderate antibacterial activity against Salmonella typhi, S. paratyphi A and S. paratyphi B.

Matched MeSH terms: Gram-Negative Bacteria/drug effects*
Fulltext Heteroaryl chalcones: design, synthesis, X-ray crystal structures and biological evaluation

Kumar CS, Loh WS, Ooi CW, Quah CK, Fun HK

Molecules, 2013 Oct 15;18(10):12707-24.
PMID: 24132195 DOI: 10.3390/molecules181012707

Chalcone derivatives have attracted increasing attention due to their numerous pharmacological activities. Changes in their structures have displayed high degree of diversity that has proven to result in a broad spectrum of biological activities. The present study highlights the synthesis of some halogen substituted chalcones 3(a-i) containing the 5-chlorothiophene moiety, their X-ray crystal structures and the evaluation of possible biological activities such as antibacterial, antifungal and reducing power abilities. The results indicate the tested compounds show a varied range of inhibition values against all the tested microbial strains. Compound 3c with a p-fluoro substituent on the phenyl ring exhibits elevated antimicrobial activity, whereas the compounds 3e and 3f displayed the least antimicrobial activities. The compounds 3d, 3e, 3f and 3i showed good ferric and cupric reducing abilities, and the compounds 3b and 3c showed the weakest reducing power in the series.

Matched MeSH terms: Gram-Negative Bacteria/drug effects
Fulltext Acute toxicity evaluation, antibacterial, antioxidant and immunomodulatory effects of Melastoma malabathricum

Alnajar ZA, Abdulla MA, Ali HM, Alshawsh MA, Hadi AH

Molecules, 2012;17(3):3547-59.
PMID: 22433579 DOI: 10.3390/molecules17033547

Melastoma malabathricum (MM) is a well-known plant in Malaysian traditional medicine, locally known as senduduk. Its ethanol and aqueous extracts have been used in the present investigation to study the immunomodulatory role on human peripheral blood mononuclear cell (PBMC), and the DPPH, ABTS and FRAP free radical scavenging activities were also measured. Total flavonoids and total phenolic contents were assayed and the antibacterial effect was tested against four species of bacteria; two Gram-positive (Staphylococcus aureus and Streptococcus agalactiae) and two Gram-negative (Escherichia coli and Klebsilla pneumonia). The tests were carried out using the disc diffusion, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) methods. Moreover, the acute toxicity was evaluated in vivo on the ethanol extract of MM to establish its safety when administered orally. In our results, both extracts of MM showed abilities to scavenge DPPH and ABTS free radicals, IC(50) values: (11.599 ± 0.84, 10.573 ± 0.58 µmol/L) and (62.657 ± 0.78, 63.939 ± 0.48 µmol/L) for ethanol and aqueous extracts respectively. Indeed the ethanol extract evidenced high phenolic content (384.33 ± 0.005 mg/g), flavonoids contents (85.8 ± 0.009 mg/g) and ferric reducing antioxidant power (33,590 ± 0.038 mmol/g), with high activity against S. aureus and S. agalactiae (11 ± 0.3 and 12 ± 0.6 mm inhibition zones). Likewise, the percentage of peripheral blood mononuclear cells (PBMC) viability was increased in response to MM, IC(50) values (1.781 ± 1.2 and 6.545 ± 0.93 µg/mL) for ethanol and aqueous extracts, respectively. In addition, our results showed that the MM extract is safe even at a high dose of 5,000 mg/kg and has no oral toxicity. These findings suggest the excellent medicinal bioactivity of MM and explain the popularity of this plant in the folk medicine as a remedy for different illnesses.

Matched MeSH terms: Gram-Negative Bacteria/drug effects
Fulltext Flavonoid analyses and antimicrobial activity of various parts of Phaleria macrocarpa (Scheff.) Boerl fruit

Hendra R, Ahmad S, Sukari A, Shukor MY, Oskoueian E

Int J Mol Sci, 2011;12(6):3422-31.
PMID: 21747685 DOI: 10.3390/ijms12063422

Phaleria macrocarpa (Scheff.) Boerl (Thymelaceae) is commonly known as 'Crown of God', 'Mahkota Dewa', and 'Pau'. It originates from Papua Island, Indonesia and it grows in tropical areas. Empirically, it is potent in treating the hypertensive, diabetic, cancer and diuretic patients. It has a long history of ethnopharmacological usage, and the lack of information about its biological activities led us to investigate the possible biological activities by characterisation of flavonoids and antimicrobial activity of various part of P. macrocarpa against pathogenic bacteria and fungi. The results showed that kaempferol, myricetin, naringin, and rutin were the major flavonoids present in the pericarp while naringin and quercetin were found in the mesocarp and seed. Furthermore, the antibacterial activity of different parts of P. macrocarpa fruit showed a weak ability to moderate antibacterial activity against pathogenic tested bacteria (inhibition range: 0.93-2.17 cm) at concentration of 0.3 mg/disc. The anti fungi activity was only found in seed extract against Aspergillus niger (1.87 cm) at concentration of 0.3 mg/well. From the results obtained, P. macrocarpa fruit could be considered as a natural antimicrobial source due to the presence of flavonoid compounds.

Matched MeSH terms: Gram-Negative Bacteria/drug effects

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