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Imidazo[1,2-a]pyridine Scaffold as Prospective Therapeutic Agents

Deep A, Bhatia RK, Kaur R, Kumar S, Jain UK, Singh H, et al.

Curr Top Med Chem, 2017;17(2):238-250.
PMID: 27237332

Imidazo[1,2-a]pyridine is one of the most potential bicyclic 5-6 heterocyclic rings that is recognized as a "drug prejudice" scaffold due to its broad range of applications in medicinal chemistry such as anticancer, antimycobacterial, antileishmanial, anticonvulsant, antimicrobial, antiviral, antidiabetic, proton pump inhibitor, insecticidal activities. This scaffold has also been represented in various marketed preparations such as zolimidine, zolpidem, alpidem. Therefore, several attempts were made to carry out the structural modifications of this scaffold to discover and develop novel therapeutic agents. This review provides a valuable insight into the research findings of wide range of derivatives of imidazo[1,2-a]pyridine scaffold leading to promising heterocyclic compounds which could be explored further for the synthesis of new derivatives as well as construction of potential drug-like chemical libraries for biological screening in search of new therapeutic agents.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Comparative effectiveness of interventions for the treatment of denture stomatitis: A systematic review with network meta-analysis

Xin YH, Ying TJ, Syeed MS, Veettil SK, Menon RK

J Prosthet Dent, 2025 Jan;133(1):108-123.
PMID: 36863936 DOI: 10.1016/j.prosdent.2023.01.007

STATEMENT OF PROBLEM: Symptomatic denture stomatitis (DS) is a painful oral mucosal disorder that can impair quality of life in denture wearers. A complete cure of DS is difficult to achieve, and the most efficacious regimen to treat DS has not yet been conclusively established.
PURPOSE: The purpose of this network meta-analysis was to assess the comparative efficacy of interventions used for the treatment of DS.
MATERIAL AND METHODS: A search was conducted for trials published in Medline, Scopus, PubMed, and Cochrane Central Register of Controlled Trials from inception until February 2022 (PROSPERO Reg no: CRD42021271366). Network meta-analysis was performed on data from randomized controlled trials that assessed the comparative efficacy of any form of intervention for the treatment of DS in denture wearers. Agents were ranked according to their effectiveness in the treatment of DS based on outcomes using surface under the cumulative ranking (SUCRA).
RESULTS: A total of 25 articles were included in the quantitative analysis. Topical antifungal agents (risk ratio [RR]=4.37[95% confidence interval [CI]: 2.15,8.90), topical antimicrobial agents used along with systemic antifungal agents (RR=4.25[95% CI: 1.79,10.33]), systemic antifungal agents (RR=4.25[95% CI: 1.79,10.10]), photodynamic therapy (RR=4.25[95% CI: 1.75,8.98]), and topical plant products (RR=3.40[95% CI: 1.59,7.26]) were found to effectively improve DS. Microwave disinfection concurrently administered with topical antifungal agents (RR=7.38(95% CI: 2.75,19.81), microwave disinfection 7.38[95% CI: 2.75,19.81]), topical antifungal agents (RR=4.88[95% CI: 1.92,12.42]), topical plant products (RR=4.49[95% CI: 1.70,11.82]), systemic antifungal agents together with topical antimicrobial agents (RR=3.85[95% CI: 1.33,11.10]), topical antimicrobial agents (RR=3.39[95% CI: 1.17,9.81]), systemic antifungal agents (RR=3.37[95% CI: 1.21,9.34]), and photodynamic therapy or photochemotherapy (PDT) (RR=2.93[95% CI: 1.01,8.47]) were found to effectively resolve mycological DS. Topical antifungals ranked highest in the SUCRA ranking for clinical improvement, whereas microwave disinfection concurrently administered with topical antifungal agents ranked highest for mycological resolution. None of the agents demonstrated significant side effects except for topical antimicrobial agents which demonstrated altered taste and staining of oral structures.
CONCLUSIONS: Available evidence suggests that topical antifungals, microwave, and systemic antifungals are effective in the treatment of DS, but confidence in these findings is low because of the limited number of studies and a high risk of bias. Additional clinical trials are needed on photodynamic therapy, topical plant products, and topical antimicrobials.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Fulltext Recent Updates on Treatment of Ocular Microbial Infections by Stem Cell Therapy: A Review

Teh SW, Mok PL, Abd Rashid M, Bastion MC, Ibrahim N, Higuchi A, et al.

Int J Mol Sci, 2018 Feb 13;19(2).
PMID: 29438279 DOI: 10.3390/ijms19020558

Ocular microbial infection has emerged as a major public health crisis during the past two decades. A variety of causative agents can cause ocular microbial infections; which are characterized by persistent and destructive inflammation of the ocular tissue; progressive visual disturbance; and may result in loss of visual function in patients if early and effective treatments are not received. The conventional therapeutic approaches to treat vision impairment and blindness resulting from microbial infections involve antimicrobial therapy to eliminate the offending pathogens or in severe cases; by surgical methods and retinal prosthesis replacing of the infected area. In cases where there is concurrent inflammation, once infection is controlled, anti-inflammatory agents are indicated to reduce ocular damage from inflammation which ensues. Despite advances in medical research; progress in the control of ocular microbial infections remains slow. The varying level of ocular tissue recovery in individuals and the incomplete visual functional restoration indicate the chief limitations of current strategies. The development of a more extensive therapy is needed to help in healing to regain vision in patients. Stem cells are multipotent stromal cells that can give rise to a vast variety of cell types following proper differentiation protocol. Stem cell therapy shows promise in reducing inflammation and repairing tissue damage on the eye caused by microbial infections by its ability to modulate immune response and promote tissue regeneration. This article reviews a selected list of common infectious agents affecting the eye; which include fungi; viruses; parasites and bacteria with the aim of discussing the current antimicrobial treatments and the associated therapeutic challenges. We also provide recent updates of the advances in stem cells studies on sepsis therapy as a suggestion of optimum treatment regime for ocular microbial infections.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Fulltext Investigating knowledge regarding antibiotics and antimicrobial resistance among pharmacy students in Sri Lankan universities

Sakeena MHF, Bennett AA, Jamshed S, Mohamed F, Herath DR, Gawarammana I, et al.

BMC Infect Dis, 2018 05 08;18(1):209.
PMID: 29739360 DOI: 10.1186/s12879-018-3107-8

BACKGROUND: Antimicrobial resistance (AMR) is a major challenge for global health care. Pharmacists play a key role in the health care setting to help support the quality use of medicines. The education, training, and experiences of pharmacy students have the potential to impact on patterns of antibiotic use in community and hospital settings. The aim of this study was to investigate antibiotic use, knowledge of antibiotics and AMR among undergraduate pharmacy students at Sri Lankan universities and to compare this between junior and senior pharmacy student groups.
METHODS: A cross-sectional study was conducted at the six universities in Sri Lanka that offer pharmacy undergraduate programmes. All pharmacy students in each university were invited to participate in this study using a self-administered questionnaire with ethics approval. The study instrument comprised five major sections: demographic information, self-reported antibiotic use, knowledge of antibiotic uses in human health, knowledge of AMR and antibiotic use in agriculture. Descriptive data analyses were conducted and Chi-squared analysis was used to explore associations between different variables and level of pharmacy education.
RESULTS: Four hundred sixty-six pharmacy students completed the questionnaire. A majority of participants (76%) reported antibiotic use in the past year. More than half (57%) of the junior pharmacy students incorrectly indicated that antibiotic use is appropriate for the management of cold and flu conditions. Senior pharmacy students (n = 206) reported significantly better antibiotic knowledge than junior students (n = 260), p

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
A repeated point prevalence survey of antimicrobial use in specialized cancer care hospital of Pakistan: findings and implications

Saleem Z, Hassali MA, Hashmi FK, Godman B, Bhutta OA

Hosp Pract (1995), 2019 Aug;47(3):149-154.
PMID: 31180791 DOI: 10.1080/21548331.2019.1628614

Background: The extensive use of broad-spectrum antimicrobials in immunocompromised patients is inevitable in situations where culture and sensitivity testing is challenging. However, their overuse leads to an increase in antimicrobial resistance (AMR), which is a growing concern. Method: A repeated point prevalence survey (PPS) was conducted to assess the pattern of antimicrobial prescribing in a specialized cancer care hospital in Pakistan using the methodology employed by the European Centre of Disease Prevention and Control. Results: Out of 313 hospitalized patients, 156 (49.8%) were prescribed one or more antimicrobials, 82 (50.9) in 2017 and 74 (48.7) in 2018. The average bed occupancy in the hospital was 80.3%. Fever in neutropenic patients (20.2%), lower respiratory tract infections (17.8%), and sepsis (14.9%) were the three most common clinical indications. The total number of prescribed antimicrobials was 242, of whom, 41 (16.9%) were given orally and 201 (83.1%) were given parenterally. The most commonly used antimicrobials were piperacillin plus enzyme inhibitor (31.8%), meropenem (7.9%), ceftriaxone (6.2%) and vancomycin (6.2%). Of the total prescribed antimicrobials, 42 (17.3%) antimicrobials were used in surgical departments, 89 (36.8) in adult medical departments, 73 (30.1%) in pediatric medical departments and 38 (15.7) in the intensive care unit (ICU). In addition to these antibacterials, there was relatively high use of antivirals (acyclovir; 4.1%) and antifungals (fluconazole; 3.7%, amphotericin B; 2.9%). Conclusion: The study concluded that broad-spectrum antimicrobial usage in cancer hospitals in Pakistan is high, which can be a risk factor for the emergence of AMR. Repeated PPS is a fruitful way to maintain a focus on inappropriate antimicrobial use and develop pertinent intervention programs targeteing specific issues to improve future use.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Review: antimicrobial properties of allicin used alone or in combination with other medications

Choo S, Chin VK, Wong EH, Madhavan P, Tay ST, Yong PVC, et al.

Folia Microbiol (Praha), 2020 Jun;65(3):451-465.
PMID: 32207097 DOI: 10.1007/s12223-020-00786-5

Garlic (Allium sativum L.) is a well-known spice widely utilised for its medicinal properties. There is an extensive record of the many beneficial health effects of garlic which can be traced back to as early as the ancient Egyptian era. One of the most studied properties of garlic is its ability to cure certain ailments caused by infections. In the 1940s, the antimicrobial activities exhibited by garlic were first reported to be due to allicin, a volatile compound extracted from raw garlic. Since then, allicin has been widely investigated for its putative inhibitory activities against a wide range of microorganisms. Allicin has demonstrated a preference for targeting the thiol-containing proteins and/or enzymes in microorganisms. It has also demonstrated the ability to regulate several genes essential for the virulence of microorganisms. Recently, it was reported that allicin may function better in combination with other antimicrobials compared to when used alone. When used in combination with antibiotics or antifungals, allicin enhanced the antimicrobial activities of these substances and improved the antimicrobial efficacy. Hence, it is likely that combination therapy of allicin with additional antimicrobial drug(s) could serve as a viable alternative for combating rising antimicrobial resistance. This review focuses on the antimicrobial activities exhibited by allicin alone as well as in combination with other substances. The mechanisms of action of allicin elucidated by some of the studies are also highlighted in the present review in order to provide a comprehensive overview of this versatile bioactive compound and the mechanistic evidence supporting its potential use in antimicrobial therapy.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Causative organisms in acute exacerbation of chronic airways disease and response to ofloxacin therapy

Sufarlan AW, Zainudin BM, Pit S, Ishak I

Drugs, 1995;49 Suppl 2:442-5.
PMID: 8549394
Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Ofloxacin, a new quinolone for the treatment of gonorrhea

Rajakumar MK, Ngeow YF, Khor BS, Lim KF

Sex Transm Dis, 1988 1 1;15(1):25-6.
PMID: 3162781

Forty-three patients with uncomplicated gonorrhea were treated with 400 mg of ofloxacin. All had cultures negative for Neisseria gonorrhoeae at follow-up within two weeks of treatment. Minimal side effects were reported. Ofloxacin appears to be satisfactory as a single-dose oral drug for the treatment of gonococcal urethritis, including those cases caused by penicillinase-producing strains of N. gonorrhoeae.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Fulltext Calcium sensing receptor hyperactivation through viral envelop protein E of SARS CoV2: A novel target for cardio-renal damage in COVID-19 infection

Singh Y, Ali H, Alharbi KS, Almalki WH, Kazmi I, Al-Abbasi FA, et al.

Drug Dev Res, 2021 09;82(6):784-788.
PMID: 33687087 DOI: 10.1002/ddr.21810

Over the recent decades, a number of new pathogens have emerged within specific and diverse populations across the globe, namely, the Nipah virus, the Ebola virus, the Zika virus, and coronaviruses (CoVs) to name a few. Recently, a new form of coronavirus was identified in the city of Wuhan, China. Interestingly, the genomic architecture of the virus did not match with any of the existing genomic sequencing data of previously sequenced CoVs. This had led scientists to confirm the emergence of a new CoV strain. Originally, named as 2019-nCoV, the strain is now called as SARS-CoV-2. High serum levels of proinflammatory mediators, namely, interleukin-12 (IL-12), IL-1β, IL-6, interferon-gamma (IFNγ), chemoattractant protein-1, and IFN-inducible protein, have been repeatedly observed in subjects who were infected with this virus. In addition, the virus demonstrated strong coagulation activation properties, leading to further the understanding on the SARS-CoV2. To our understanding, these findings are unique to the published literature. Numerous studies have reported anomalies, namely, decline in the number of lymphocytes, platelets and albumins; and a rise in neutrophil count, aspartate transaminase, alanine aminotransaminase, lactate dehydrogenase, troponins, creatinine, complete bilirubin, D-dimers, and procalcitonin. Supplementation of calcium during the SARS CoV-2 associated hyperactive stage of calcium-sensing receptors (CaSR) may be harmful to the cardio-renal system. Thus, pharmacological inhibition of CaSR may prevent the increase in the levels of intracellular calcium, oxidative, inflammatory stress, and cardio-renal cellular apoptosis induced by high cytokines level in COVID-19 infection.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
The role of artificial intelligence in the battle against antimicrobial-resistant bacteria

Lau HJ, Lim CH, Foo SC, Tan HS

Curr Genet, 2021 Jun;67(3):421-429.
PMID: 33585980 DOI: 10.1007/s00294-021-01156-5

Antimicrobial resistance (AMR) in bacteria is a global health crisis due to the rapid emergence of multidrug-resistant bacteria and the lengthy development of new antimicrobials. In light of this, artificial intelligence in the form of machine learning has been viewed as a potential counter to delay the spread of AMR. With the aid of AI, there are possibilities to predict and identify AMR in bacteria efficiently. Furthermore, a combination of machine learning algorithms and lab testing can help to accelerate the process of discovering new antimicrobials. To date, many machine learning algorithms for antimicrobial-resistance discovery had been created and vigorously validated. Most of these algorithms produced accurate results and outperformed the traditional methods which relied on sequence comparison within a database. This mini-review will provide an updated overview of antimicrobial design workflow using the latest machine-learning antimicrobial discovery algorithms in the last 5 years. With this review, we hope to improve upon the current AMR identification and antimicrobial development techniques by introducing the use of AI into the mix, including how the algorithms could be made more effective.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Fulltext Typology of interventions for antimicrobial use and antimicrobial resistance in aquaculture systems in low- and middle-income countries

Garza M, Mohan CV, Brunton L, Wieland B, Häsler B

Int J Antimicrob Agents, 2022 Jan;59(1):106495.
PMID: 34896577 DOI: 10.1016/j.ijantimicag.2021.106495

Indiscriminate antimicrobial use (AMU) in aquaculture to treat and prevent diseases is common and can lead to the emergence of antimicrobial-resistant micro-organisms, potentially impacting public health and connected ecosystems. This study aimed to develop a typology to classify and characterise interventions to reduce AMU in aquaculture and identify points of action. Seventeen aquaculture and animal health professionals in Asian and African countries were interviewed to gather information on characteristics of interventions in different contexts to develop a typology. Seven types of interventions were defined: (i) legislation and regulations; (ii) industry rules and standards; (iii) voluntary instruments; (iv) commercial technology and alternatives to antimicrobials; (v) on-farm management; (vi) learning and awareness-raising; and (vii) activities with co-benefits. Types were based on intervention function, scope of implementation, implementer, compulsion, strength of the intervention, AMU/antimicrobial resistance (AMR) objective and stakeholder to influence. For each type, examples were described and discussed. The most common interventions to address AMU and AMR were legislative and regulatory frameworks and voluntary instruments, including National Action Plans. Interventions addressing AMU/AMR specifically were scarce. Other interventions focused on indirect effect pathways to AMU and AMR reduction aiming to improve good aquaculture practices, disease prevention and improved management. Monitoring and evaluation of these interventions were found to be rare, only present for interventions driven by development projects and international agencies. The presented typology of existing strategies and interventions addressing AMU/AMR in aquaculture systems can guide evaluation of AMR-sensitive interventions that promote responsible AMU, and informs the design and implementation of future interventions.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Evaluation of polycaprolactone matrices for the intravaginal delivery of metronidazole in the treatment of bacterial vaginosis

Pathak M, Turner M, Palmer C, Coombes AG

J Biomater Appl, 2014 Sep;29(3):354-63.
PMID: 24682036 DOI: 10.1177/0885328214528256

Microporous, poly (ɛ-caprolactone) (PCL) matrices loaded with the antibacterial, metronidazole were produced by rapidly cooling suspensions of drug powder in PCL solutions in acetone. Drug incorporation in the matrices increased from 2.0% to 10.6% w/w on raising the drug loading of the PCL solution from 5% to 20% w/w measured with respect to the PCL content. Drug loading efficiencies of 40-53% were obtained. Rapid 'burst release' of 35-55% of the metronidazole content was recorded over 24 h when matrices were immersed in simulated vaginal fluid (SVF), due to the presence of large amounts of drug on matrix surface as revealed by Raman microscopy. Gradual release of around 80% of the drug content occurred over the following 12 days. Metronidazole released from PCL matrices in SVF retained antimicrobial activity against Gardnerella vaginalis in vitro at levels up to 97% compared to the free drug. Basic modelling predicted that the concentrations of metronidazole released into vaginal fluid in vivo from a PCL matrix in the form of an intravaginal ring would exceed the minimum inhibitory concentration of metronidazole against G. vaginalis. These findings recommend further investigation of PCL matrices as intravaginal devices for controlled delivery of metronidazole in the treatment and prevention of bacterial vaginosis.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Melioidosis imported into Nepal

Shrestha N, Sharma S, Khanal B, Bhatta N, Dhakal S

Scand. J. Infect. Dis., 2005;37(1):64-6.
PMID: 15764193

This is a report of the first recognized case of melioidosis in Nepal. Illness began 1 month after returning from Malaysia after a 1 y stay. The case highlights the importance of ascertaining the travel history in any patient with a suspected infectious disease in this age of global travel.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Fulltext Perceptions and Practices of Community Pharmacists towards Antimicrobial Stewardship in the State of Selangor, Malaysia

Khan MU, Hassali MA, Ahmad A, Elkalmi RM, Zaidi ST, Dhingra S

PLoS One, 2016;11(2):e0149623.
PMID: 26901404 DOI: 10.1371/journal.pone.0149623

BACKGROUND: Increasing antimicrobial resistance is one of the pressing concerns globally. Injudicious use of antibiotics is one of the modifiable factors responsible for antimicrobial resistance. Given the widespread use of antimicrobials in community settings, pharmacists have an important role in ensuring appropriate use of antibiotics. The objective of this study was to assess the perception and self-reported practices of community pharmacists towards antimicrobial stewardship.
METHODS: A cross-sectional study was conducted among community pharmacists between March-April, 2015, using a self-administered, pre-tested questionnaire in the State of Selangor, Malaysia. A simple random sampling approach was used to select pharmacy sites. Descriptive and inferential statistical methods were used to analyse the data.
RESULTS: A total of 188 pharmacists responded to the survey, giving a response rate of 83.5%. The majority of participants (n = 182, 96.8%) believed that antimicrobial stewardship program helps healthcare professionals to improve the quality of patient care. However, more than half of pharmacists were neutral in their opinion about the incorporation of antimicrobial stewardship programs in community pharmacies (n = 102, 54.2%). Though collaboration was often done by pharmacists with other health professionals over the use of antibiotics (n = 104, 55.3%), a significant proportion of participants (n = 102, 54.2%) rarely/occasionally participate in antimicrobial awareness campaigns. Pharmacists having postgraduate qualification were more likely to held positive perceptions of, and were engaged in, antimicrobial stewardship than their non-postgraduate counterpart (p<0.05). Similarly, more experienced pharmacists (> 10 years) held positive perceptions towards antimicrobial stewardship (p<0.05).
CONCLUSION: The study highlighted some gaps in the perception and practices of community pharmacist towards antimicrobial stewardship. Development of customized interventions would be critical to bridging these gaps and improve their perception and practices towards antimicrobial stewardship.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Sepsis in tropical regions: Report from the task force on tropical diseases by the World Federation of Societies of Intensive and Critical Care Medicine

McGloughlin S, Richards GA, Nor MBM, Prayag S, Baker T, Amin P

J Crit Care, 2018 08;46:115-118.
PMID: 29310974 DOI: 10.1016/j.jcrc.2017.12.018

Sepsis and septic shock in the tropics are caused by a wide array of organisms. These infections are encountered mainly in low and middle-income countries (LMIC) where a lack of infrastructure and medical facilities contribute to the high morbidity and mortality. Published sepsis guidelines are based on studies primarily performed in high income countries and as such recommendations may or may not be relevant to practice in the tropics. Failure to adhere to guidelines, particularly among non-intensive care specialists even in high-income countries, is an area of concern for sepsis management. Additionally, inappropriate use of antimicrobials has led to significant antimicrobial resistance. Access to rapid, low-cost, and accurate diagnostic tests is critical in countries where tropical diseases are prevalent to facilitate early diagnosis and treatment. Implementation of performance improvement programs may improve outcomes for patients with sepsis and the addition of resuscitation and treatment bundles may further reduce mortality. Associated co-morbidities such as malnutrition and HIV influence outcomes and must be considered.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Fulltext Naïve Human Antibody Libraries for Infectious Diseases

Chan SK, Rahumatullah A, Lai JY, Lim TS

Adv Exp Med Biol, 2017;1053:35-59.
PMID: 29549634 DOI: 10.1007/978-3-319-72077-7_3

Many countries are facing an uphill battle in combating the spread of infectious diseases. The constant evolution of microorganisms magnifies the problem as it facilitates the re-emergence of old infectious diseases as well as promote the introduction of new and more deadly variants. Evidently, infectious diseases have contributed to an alarming rate of mortality worldwide making it a growing concern. Historically, antibodies have been used successfully to prevent and treat infectious diseases since the nineteenth century using antisera collected from immunized animals. The inherent ability of antibodies to trigger effector mechanisms aids the immune system to fight off pathogens that invades the host. Immune libraries have always been an important source of antibodies for infectious diseases due to the skewed repertoire generated post infection. Even so, the role and ability of naïve antibody libraries should not be underestimated. The naïve repertoire has its own unique advantages in generating antibodies against target antigens. This chapter will highlight the concept, advantages and application of human naïve libraries as a source to isolate antibodies against infectious disease target antigens.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
The Role of Nanoparticles in the Inhibition of Multidrug-Resistant Bacteria and Biofilms

AlMatar M, Makky EA, Var I, Koksal F

Curr Drug Deliv, 2018;15(4):470-484.
PMID: 29219055 DOI: 10.2174/1567201815666171207163504

BACKGROUND: Until recently, one of the main reasons for mortality has been infectious diseases, and bacteria that are drug-resistant have emerged as a result of the wide application, as well as the misuse of antibacterial medications. Having multidrug-resistance, bacteria present a great problem for the efficient management of bacterial infections and this challenge has resulted in the creation of other means of dealing with bacterial diseases. Of late, metallic nanoparticles (NPs), employed as antibacterial agents, have the potential for use against resistance to bacterial drugs.
OBJECTIVE: The mechanisms of bacterial resistance are described in this review and this is followed by an outline of the features and uses of metallic NPs as antibiotic agents to address bacteria that are antibiotic- sensitive and resistant. Additionally, a general impression of metallic NPs as antibiofilm bactericidal agents is presented.
CONCLUSION: Biofilms and bacterial strains that are resistant to antibiotics present a grave public health challenge and this has enhanced the need to develop new bactericidal agents. Therefore, nanomaterials are considered as a potential platform for managing bacterial infections.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Fulltext Extraction and Characterization of Organ Components of the Malaysian Sea Cucumber Holothuria leucospilota Yielded Bioactives Exhibiting Diverse Properties

Ceesay A, Nor Shamsudin M, Aliyu-Paiko M, Ismail IS, Nazarudin MF, Mohamed Alipiah N

Biomed Res Int, 2019;2019:2640684.
PMID: 31119160 DOI: 10.1155/2019/2640684

The aim of the present study was to extract and characterize bioactive components from separate body organs of Holothuria leucospilota. Preliminary qualitative assessment of the crude extracts was positive for phenols, terpenoids, carbohydrates, flavonoids, saponins, glycosides, cardiac glycosides, steroids, phlobatannins, and tannins in all body organs evaluated. Phenolics were the most abundant group of bioactives accounting for approximately 80%. The extraction solvent mixtures that yielded most compounds evaluated were methanol/acetone (3:1, v:v) and methanol/distilled water (3:1, v:v). In other analyses, GC-MS data revealed diverse metabolic and biologically active compounds, where those in high concentrations included 2-Pentanone, 4-hydroxy-4-methyl- among the ketones; phenol- 2,4-bis(1,1-dimethylethyl)-, a phenol group; and 2-Chlorooctane, a hydrocarbon. Among FA and their methyl/ethyl esters, n-hexadecanoic acid, 5,8,11,14-eicosatetraenoic acid ethyl ester (arachidonic acid), and 5,8,11,14,17-eicosapentaenoic acid methyl ester (EPA) were among the most abundant FAMEs accounting for approximately 50% of the subgroups measured. Data from GC-FID analysis revealed methyl laurate (C12:0), methyl myristate (C14:0), methyl palmitate (C16:0), and methyl stearate (18:0) methyl esters as the most abundant saturated FA, whereas cis-9-oleic methyl ester (C18:1) and methyl linoleate (C18:2) were found as the major monounsaturated FA and PUFA FAMEs, respectively, in the body wall of the species. Taken together, the extraction and characterization of different categories of metabolically and biologically active compounds in various organ extracts of H. leucospilota suggest that the species is potentially a rich source of cholesterol-lowering, antioxidant, antimicrobial, and anticancer agents. These substances are known to benefit human health and assist in disease prevention. These findings justify the use of sea cucumbers in traditional folklore medication and the current interest and attention focused on the species to mine for bioactives in new drugs research.

Matched MeSH terms: Anti-Infective Agents/therapeutic use
Antimicrobial prescribing and determinants of antimicrobial resistance: a qualitative study among physicians in Pakistan

Saleem Z, Hassali MA, Godman B, Hashmi FK, Saleem F

Int J Clin Pharm, 2019 Oct;41(5):1348-1358.
PMID: 31273588 DOI: 10.1007/s11096-019-00875-7

Background Understanding physicians' perception about antimicrobial use and resistance is essential to ensure that the objectives of the Pakistan national action plan on antimicrobial resistance are met. Little is currently known about physicians' perceptions in Pakistan. Objective Assess physicians' perception surrounding antibiotic use and resistance, factors influencing antibiotic prescribing and potential interventions to improve future antibiotic prescribing. Settings The study was conducted in Lahore, the capital of the province of Punjab, which is the second largest and most populous city of Pakistan. Method Qualitative study was conducted with a semi-structured interview guide involving in-depth face-to-face interviews with purposively selected physicians. Audiorecorded interviews were transcribed verbatim and transcripts analyzed by thematic content analysis. Main outcome measures Themes surrounding the perspectives of physicians on issues of antimicrobial use and resistance. Results Five major themes emerged: (1) knowledge and perception of physicians about antimicrobials, (2) antimicrobial prescribing behaviors of physicians, (3) factors influencing prescribing, (4) determinants of antimicrobial resistance, (5) and potential interventions to reduce antimicrobial resistance. The main challenges and issues associated with antibiotic prescribing were the improvement of knowledge, implementation of hygienic measures, access to and clarity of treatment recommendations and minimizing external factors influencing prescribing including pharmaceutical company activities. Suggestions for the future included stricter regulations for prescribing, improved diagnosis, availability of local guidelines and monitoring of prescribing and resistance patterns. Conclusion Identification of concerns regarding inappropriate antimicrobial prescribing will enable specific initiatives and approaches to improve future antimicrobial use and reduce antimicrobial resistance in Pakistan.

Matched MeSH terms: Anti-Infective Agents/therapeutic use*
Exploring Antimicrobials from the Flora and Fauna of Marine: Opportunities and Limitations

Venkateskumar K, Parasuraman S, Chuen LY, Ravichandran V, Balamurgan S

Curr Drug Discov Technol, 2020;17(4):507-514.
PMID: 31424372 DOI: 10.2174/1570163816666190819141344

About 95% of earth living space lies deep below the ocean's surface and it harbors extraordinary diversity of marine organisms. Marine biodiversity is an exceptional reservoir of natural products, bioactive compounds, nutraceuticals and other potential compounds of commercial value. Timeline for the development of the drug from a plant, synthetic and other alternative sources is too lengthy. Exploration of the marine environment for potential bioactive compounds has gained focus and huge opportunity lies ahead for the exploration of such vast resources in the ocean. Further, the evolution of superbugs with increasing resistance to the currently available drugs is alarming and it needs coordinated efforts to resolve them. World Health Organization recommends the need and necessity to develop effective bioactive compounds to combat problems associated with antimicrobial resistance. Based on these factors, it is imperative to shift the focus towards the marine environment for potential bioactive compounds that could be utilized to tackle antimicrobial resistance. Current research trends also indicate the huge strides in research involving marine environment for drug discovery. The objective of this review article is to provide an overview of marine resources, recently reported research from marine resources, challenges, future research prospects in the marine environment.

Matched MeSH terms: Anti-Infective Agents/therapeutic use

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