Recent advances in anti-infective drug discovery最新文献

{"title":"Vigilance Needed in Treating Leprosy Patients in Accordance with WHO's AWaRe.","authors":"Pugazhenthan Thangaraju,&nbsp;Hemasri Velmurugan,&nbsp;Sree Sudha Tanguturi Yella,&nbsp;Sajitha Venkatesan","doi":"10.2174/2772434417666220720111849","DOIUrl":"https://doi.org/10.2174/2772434417666220720111849","url":null,"abstract":"<p><strong>Background: </strong>Leprosy is a highly stigmatized disease that can range from a minor skin lesion to life-threatening conditions such as deformities and disability. The World Health Organization (WHO) has developed a tool called \"Access, Watch, and Reserve\" (AWaRe) to reduce antibiotic misuse and abuse.</p><p><strong>Aim: </strong>The purpose of this review is to determine whether the drugs used in the leprosy treatment regimen are complied with the AWaRe programme, in order to improve the quality of hospital antibiotic use and reduce the incidence of antimicrobial resistance (AMR).</p><p><strong>Methods: </strong>We started by looking for antibiotics that are used in the treatment and chemoprophylaxis of leprosy, as defined by the WHO's AWaRe classification. Furthermore, we look for studies on antibiotics that showed sensitivity or less resistance after antimicrobial sensitivity testing (AST) on isolates from infected leprosy ulcers, as well as their AWaRe category.</p><p><strong>Results: </strong>There were 32 studies found, but only 5 of them met the inclusion criteria. They consisted of four cross-sectional studies and one descriptive retrospective study. A total of 19 antibiotics were identified in 5 studies, with 9 (47.4%) antibiotics in the access category, 8 (42.1%) antibiotics in the watch group, and 2 (10.5%) antibiotics in the reserve group.</p><p><strong>Conclusion: </strong>As per our knowledge, this is the first study to explore antibiotics in leprosy treatment, chemoprophylaxis, and complications such as ulcer compliance with the AWaRe programme. Antimicrobial resistance is on the rise, which is a global issue that continues to pose challenges to clinical practices. This review may provide physicians with an overview of the current state of drug prescribing trends in leprosy, whether in accordance with the AWaRe classification in selecting the right drug when the use of antimicrobials is indicated and may also aid in rational drug prescribing.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":" ","pages":"95-102"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40615356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Clinical Profile, Risk Factors, and Therapeutic Outcome of Cavitating Fungal Pneumonia Coinfection in COVID-19 Patients: A Retrospective Analysis.","authors":"Arjun Kumar,&nbsp;Mayank Mishra,&nbsp;Saikat Banerjee,&nbsp;Lokesh Kumar Saini,&nbsp;Prakhar Sharma,&nbsp;Ruchi Dua,&nbsp;Girish Sindhwani","doi":"10.2174/2772434417666220720122042","DOIUrl":"https://doi.org/10.2174/2772434417666220720122042","url":null,"abstract":"<p><strong>Background: </strong>An end to the novel coronavirus disease 2019 (COVID-19) pandemic appears to be a distant dream. To make matters worse, there has been an alarming upsurge in the incidence of cavitating invasive fungal pneumonia associated with COVID-19, reported from various parts of the world including India. Therefore, it remains important to identify the clinical profile, risk factors, and outcome of this group of patients.</p><p><strong>Methods: </strong>Out of 50 moderate to severe COVID-19 inpatients with thoracic computed tomographic (CT) evidence of lung cavitation, we retrospectively collected demographic and clinical data of those diagnosed with fungal pneumonia for further investigation. We determined the association between risk factors related to 30-day and 60-day mortality.</p><p><strong>Results: </strong>Of the 50 COVID-19 patients with cavitating lung lesions, 22 (44 %) were identified to have fungal pneumonia. Most of these patients (n = 16, 72.7 %) were male, with a median (range) age of 56 (38-64) years. On chest CT imaging, the most frequent findings were multiple cavities (n = 13, 59.1 %) and consolidation (n = 14, 63.6 %). Mucormycosis (n = 10, 45.5 %) followed by Aspergillus fumigatus (n = 9, 40.9 %) were the common fungi identified. 30-day and 60-day mortalities were seen in 12 (54.5 %) and 16 (72.7 %) patients, respectively. On subgroup analysis, high cumulative prednisolone dose was an independent risk factor associated with 30-day mortality (p = 0.024).</p><p><strong>Conclusion: </strong>High cumulative prednisolone dose, baseline neutropenia, hypoalbuminemia, multiple cavities on CT chest, leukopenia, lymphopenia and raised inflammatory markers were associated with poor prognosis in severe COVID-19 patients with cavitating fungal pneumonia.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"17 3","pages":"167-177"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10370056","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Colonization by Various Morphological Forms of <i>Helicobacter pylori</i> in the Gingival Sulcus and Antrum of the Stomach.","authors":"Nikita Gladyshev,&nbsp;Maria Taame,&nbsp;Askhab Ibiliev,&nbsp;Yuriy Grukhin,&nbsp;Viacheslav Kravtsov","doi":"10.2174/2772434417666220903093339","DOIUrl":"https://doi.org/10.2174/2772434417666220903093339","url":null,"abstract":"<p><strong>Background: </strong>Helicobacter pylori eradication therapy can be considered effective if the result of its implementation is removed including all roots and rootlets from which surviving H. pylori can repopulate in the gastric mucosa. One of the reasons for the ineffectiveness of eradication therapy can be the continuous presence of viable coccoid forms of H. pylori in the oral cavity. Therefore, anti-Helicobacter eradication therapy should be supplemented by the sanitation of the oral cavity.</p><p><strong>Objectives: </strong>The objective of this study is to determine the frequency of occurrence of H. pylori in the gastric mucosa and in the oral cavity in patients with chronic periodontitis or with chronic gastritis using immunocytochemical method and to evaluate the pathophysiological relationship between periodontitis and HP-associated acid-dependent stomach diseases mediated by H. pylori.</p><p><strong>Methods: </strong>A group of patients with chronic gastritis (70 participants, 46 women, 24 men, age: 24 - 55 years) and another group with chronic periodontitis before the start of surgical treatment (61 participants, 30 women, 31 men, age: 20 - 60 years) were examined for НР bacterial cells using immunocytochemical methods of staining gastric biopsy and exfoliate samples from the gingival sulcus surface. The participants did not take any antimicrobial medication before and during the examination. Routine staining was also performed to view microbiota in smears for both groups. The participants signed a voluntary consent agreement to undergo routine medical examinations and join the study at the Nikiforov Russian Centre of Emergency and Radiation Medicine, EMERCOM of Russia, where the ethical committee was made.</p><p><strong>Results: </strong>Immunocytochemical method could identify all stages of bacillary-coccoid transformation of H. pylori which accounted for 63.4-67.5% of cases. HP-antigenpositive bacteria were found in the oral cavity in both groups of examined patients. It was apparent that spiral forms of H. pylori were dominant over coccoid forms in the gastric mucosa in the antrum of the stomach, whereas coccoid forms of H. pylori were frequently found more in the oral cavity. Helicobacteriosis in the oral cavity was identified in chronic periodontitis.</p><p><strong>Conclusion: </strong>We found certain pathogenetic connections between inflammatory lesions of the oral cavity and diseases of the internal organs of the gastrointestinal tract. Accordingly, we suggest the necessity to use proper medication for oral cavity sanitation along with anti-Helicobacter eradication therapy to influence the HP reservoir in the oral cavity and gingival sulcus. Additionally, bacterial cells of HP reside in the oral cavity in coccoid forms; therefore, the coccoid form of HP should become the second principal target in treating HP.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"17 3","pages":"199-211"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10385370","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hybrid Compounds Containing Carvacrol Scaffold: <i>In Vitro</i> Antibacterial and Cytotoxicity Evaluation.","authors":"Zintle Mbese,&nbsp;Margo Nell,&nbsp;Youmbi T Fonkui,&nbsp;Derek T Ndinteh,&nbsp;Vanessa Steenkamp,&nbsp;Blessing A Aderibigbe","doi":"10.2174/1574891X16666220124122445","DOIUrl":"https://doi.org/10.2174/1574891X16666220124122445","url":null,"abstract":"<p><strong>Background: </strong>The design of hybrid compounds is a distinct approach for developing potent bioactive agents. Carvacrol, an essential oil, exhibits antimicrobial, antifungal, antioxidant, and anticancer activity, making it a good precursor for the development of compounds with potent biological activities. Some patents have reported carvacrol derivatives with promising biological activities.</p><p><strong>Objective: </strong>This study aimed to prepare hybrid compounds containing a carvacrol scaffold with significant antibacterial and anticancer activity.</p><p><strong>Methods: </strong>Esterification reactions between carvacrol and known pharmacophores were performed at room temperature and characterized using ¹H-NMR, ¹³CNMR, and UHPLC-HRMS. In vitro antibacterial study was determined using the microdilution assay and cytotoxicity evaluation using sulforhodamine B staining assay.</p><p><strong>Results: </strong>The FTIR spectra of the carvacrol hybrids revealed prominent bands in the range of 1612-1764 cm^-1 and 1014-1280 cm^-1 due to (C=O) and (C-O) stretching vibrations, respectively. The structures of the carvacrol hybrids were confirmed by ¹H-NMR, ¹³C-NMR, and UHPLC-HRMS analysis, and compound 5 exhibited superior activity when compared to the hybrid compounds against the strains of bacteria used in the study. The in vitro cytotoxicity evaluation showed that compound 3 induced cytotoxicity in all the cancer cell lines; MDA (16.57 ± 1.14 μM), MCF-7 (0.47 ± 1.14 μM), and DU145 (16.25 ± 1.08 μM), as well as the normal breast cells, MCF-12A (0.75± 1.30 μM). Compound 7 did not induce cytotoxicity in the cell lines tested (IC₅₀ > 200 μM).</p><p><strong>Conclusion: </strong>The modification of carvacrol through hybridization is a promising approach to develop compounds with significant antibacterial and anticancer activity.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"17 1","pages":"54-68"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39858726","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Potential Role of the Serotonin Transporter as a Drug Target against Parasitic Infections: A Scoping Review of the Literature.","authors":"Mahbobeh Montazeri, Mahdi Fakhar, Masoud Keighobadi","doi":"10.2174/1574891X16666220304232301","DOIUrl":"10.2174/1574891X16666220304232301","url":null,"abstract":"<p><strong>Background: </strong>Several in vitro and in vivo biological activities of serotonin, 5- hydroxytryptamine (5-HT), as a bioactive molecule, and its transporter (5-HT-Tr) were evaluated in parasitic infections.</p><p><strong>Objective: </strong>Herein, the roles of 5-HT and 5-HTR in helminths and protozoan infections with medical and veterinary importance are reviewed.</p><p><strong>Methods: </strong>We searched information in 4 main databases and reviewed published literature about the serotonin transporter's role as a promising therapeutic target against pathogenic parasitic infections between 2000 and 2021.</p><p><strong>Results: </strong>Based on recent investigations, 5-HT and 5-HT-Tr play various roles in parasite infections, including biological function, metabolic activity, organism motility, parasite survival, and immune response modulation. Moreover, some of the 5-HT-TR in Schistosoma mansoni showed an excess of favorite substrates for biogenic amine 5-HT compared to their mammalian hosts. Furthermore, the main neuronal protein related to the G protein-coupled receptor (GPCR) was identified in S. mansoni and Echinococcus granulosus, playing main roles in these parasites. In addition, 5-HT increased in toxoplasmosis, giardiasis, and Chagas disease. On the other hand, in Plasmodium spp., different forms of targeted 5-HTR stimulate Ca²⁺ release, intracellular inositol triphosphate (ITP), cAMP, and protein kinase A (PKA) activity.</p><p><strong>Conclusion: </strong>This review summarized the several functional roles of the 5-HT and the importance of the 5-HT-TR as a drug target with minimal harm to the host to fight against helminths and protozoan infections. Hopefully, this review will shed light on research regarding serotonin transporter-based therapies as a potential drug target soon.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"7 1","pages":"23-33"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85195634","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Utility of Walk Tests in the Progression of Mild COVID-19 Infection at a Tertiary Hospital in North India.","authors":"Souradeep Chowdhury,&nbsp;Tamoghna Ghosh,&nbsp;Aastha Goel,&nbsp;Anupam K Singh,&nbsp;Arvind Kumar,&nbsp;Naveet Wig","doi":"10.2174/2772434417666220630112737","DOIUrl":"https://doi.org/10.2174/2772434417666220630112737","url":null,"abstract":"<p><strong>Introduction: </strong>There have been 214 million confirmed cases of COVID-19 worldwide, with a total death tally of 4.4 million. The current study aims to determine the predictive value of various scores in the assessment of progression of mild COVID-19 infection at a tertiary care hospital in North India.</p><p><strong>Methods: </strong>The study population consisted of adults (age more than 18 years) with a confirmed diagnosis of COVID-19 by RT-PCR on nasopharyngeal specimens. Patients with only mild illness were enrolled. After the patients were admitted to the isolation ward, the presenting history, comorbidity status, vital signs and laboratory parameters were recorded. The 3 and 6 minutes walk test was performed daily from admission till discharge or progression of the severity of COVID- 19, and it was used to calculate Borg Dyspnoea Score (BDS) and National Early Warning Score (NEWS2) scores.</p><p><strong>Results: </strong>Our study consisted of 50 patients with 34 (68%) males, and the mean (SD) age of the patient population was 28.1 (6.4) years. The most common symptoms were fever, sore throat, and cough. All laboratory parameters were within normal ranges for all the patients. 96% recovered without progression, while only 4% of them progressed to moderate illness. Results of the 3 and 6 minutes walk tests, BDS and NEWS2 scores showed improvement over the course of the hospital stay.</p><p><strong>Conclusion: </strong>Although the walk tests and the scores improved over time, they failed to predict the disease progression.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"17 3","pages":"159-166"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10369658","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Physicochemical Properties, Antioxidant and Antimicrobial Activities of Ethiopian Sweet Basil (<i>Ocimum basilicum</i> L.) Leaf and Flower Oil Extracts.","authors":"Getachew Yibeltal,&nbsp;Zekeria Yusuf,&nbsp;Mulugeta Desta","doi":"10.2174/2772434417666220720121051","DOIUrl":"https://doi.org/10.2174/2772434417666220720121051","url":null,"abstract":"<p><strong>Background: </strong>The occurrence of multidrug resistant pathogenic microbes has initiated the development of natural antimicrobial agents from plants. Oils from herbal sources have drawn scientific interest due to their potential source of bioactive compounds.</p><p><strong>Objective: </strong>This study was aimed to examine the physicochemical and biological activities including antioxidant and antimicrobial potential of the oil extracted from basil leaves and flowers.</p><p><strong>Methods: </strong>The physicochemical properties of the oil extracts were measured based on oil yield, specific gravity, acid value, free fatty acids and peroxide values whilst the antioxidant activities were assessed by ascorbic acid, DPPH (2, 2- diphenyl-1-picrylhydrazyl), and hydrogen peroxide free radical scavenging activities. The antimicrobial experiment was conducted based on disc diffusion and broth dilution methods.</p><p><strong>Results: </strong>The result of antioxidant activity of Ocimum basilicum indicated significantly higher DPPH (86.45%) for leaf oil extract. The strongest antibacterial activity with maximum zone of inhibition (15.47 mm), minimum inhibitory concentration MIC (0.09 μg/ml), and corresponding minimum bactericidal concentration MBC (0.19 μg/ml) was exhibited by the flower oil extract against Staphylococcus aureus ATCC-25923. The strongest antifungal activity with maximum zone of inhibition (15.90 mm), MIC (0.125 μg/ml, the least value), and minimum fungicidal concentration MFC (0.09 μg/ml) were recorded for leaf oil against Candida albicans.</p><p><strong>Conclusion: </strong>It can be concluded from the present study that the sweet basil flower and leaf oil extracts can be potential antioxidant, antibacterial, and antifungal agents.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":" ","pages":"131-138"},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40615357","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Meet Our Section Editor","authors":"S. Sardari","doi":"10.2174/277243441601210319102350","DOIUrl":"https://doi.org/10.2174/277243441601210319102350","url":null,"abstract":"[1] Baker ZK, Sardari S. Molecularly imprinted polymer (Mip) applications in natural product studies based on medicinal plant and secondary metabolite analysis. Iranian Biomed J 2021; 25(2): 68-77. [2] Sardari S, Shahidi S. Thiamine pyrophosphate riboswitch regulation: a new possible mechanism involved in the action of nalidixic acid. Turkish J Biochem 2020; 45(6), pp. 777-84. [3] Madanchi H, Ebrahimi Kiasari R, Seyed Mousavi SJ, Johari B, Shabani AA, Sardari S. Design and Synthesis of Lipopolysaccharide-Binding Antimicrobial Peptides Based on Truncated Rabbit and Human CAP18 Peptides and Evaluation of Their Action Mechanism. Probiotics Antimicrob Proteins 2020; 12(4): 1582-1593. [4] Mazaheri S, Talebkhan Y, Mahboudi F, Nematollahi L, Cohan RA, Ardakani EM, Bayat E, Sabzalinejad M, Sardari S, Torkashvand F. Improvement of Certolizumab Fab′ properties by PASylation technology. Scientific Reports 2020; 10(1): 18464. [5] Nazeri S, Zakeri S, Mehrizi AA, Sardari S, Djadid ND. Measuring of IgG2c isotype instead of IgG2a in immunized C57BL/6 mice with Plasmodium vivax TRAP as a subunit vaccine candidate in order to correct interpretation of Th1 versus Th2 immune response. Exp Parasitol 2020; 216: 107944. [6] Madanchi H, Sardari S, Shajiee H, Taherian S, Ashkar M, Johari B, Shabani AA, Sharafi S. Design of new truncated derivatives based on direct and reverse mirror repeats of first six residues of Caerin 4 antimicrobial peptide and evaluation of their activity and cytotoxicity. Chem Biol Drug Des 2020; 96(2): 801-11. [7] Hassan M, Ghaffari R, Sardari S, Farahani YF, Mohebbi S. Discovery of novel isatin-based thiosemicarbazones: synthesis, antibacterial, antifungal, and antimycobacterial screening. Res Pharm Sci 2020; 15(3): 281-90. [8] Ghadam M, Sardari S, Shokrgozar MA, Mahdavi MS. Design of anti-angiogenic peptidomimetics and evaluation their biological activity by in vitro assays. Avicenna J Med Biotechnol 2020; 12(2): 91-8. [9] Beiranvand E, Ostad SN, Ardakani EM, Torkashvand F, Sardari S, Vaziri B. In vivo evaluation of carvedilol cardiac protection against trastuzumab cardiotoxicity. Drug Res 2020; 70(4): 165-9. [10]Ghavami G, Sardari S. Synergistic effect of vitamin C with cisplatin for inhibiting proliferation of gastric cancer cells. Iranian Biomed J 2020; 24(2): 119–127.","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"66 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83964472","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhancement of the Anti-biofilm Activity of Gold Nanoparticles- Itraconazole Conjugates in Resistant Candida glabrata.","authors":"Ensieh Lotfali,&nbsp;Mahsa Fattahi,&nbsp;Reza Ghasemi,&nbsp;Farzan Zakermashhadi,&nbsp;Mohammad Shafiei,&nbsp;Mojgan Borzouie,&nbsp;Mohammad Mahdi Rabiei","doi":"10.2174/2772434416666210607144543","DOIUrl":"https://doi.org/10.2174/2772434416666210607144543","url":null,"abstract":"<p><strong>Introduction: </strong>Onychomycosis, also called tinea unguium, is a common fungal infection affecting the nails. After dermatophytes, Candida species are recognized as second-line pathogens responsible for this infection. The treatment of onychomycosis requires a long time and is associated with high rates of recurrence. Antifungal medicines conjugated with gold (Au-NP) nanoparticle are the possible platforms for the reduction of drug resistance.</p><p><strong>Methods: </strong>In the present study, we reported the in-vitro antifungal activity of itraconazole (ITZ) - Au conjugates, time-kill studies, and biofilm-producing ability of six ITZ-resistant C. glabrata.</p><p><strong>Results: </strong>3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium bromide (MTT) quantitative results revealed that four out of six resistant isolates studied able to form biofilms in vitro. ITZ-Au conjugates were more effective than ITZ or Au nanoparticle alone, and the time-kill tests pointed to the suitable effect of ITZ-Au conjugate.</p><p><strong>Conclusion: </strong>The present study concluded that ITZ-Au conjugates have an inhibitory effect on the biofilm of resistant C. glabrata isolates. Further studies are needed to compare the ex-vivo onychomycosis model.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":" ","pages":"137-147"},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39767962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Multipotentiality of Luliconazole against Various Fungal Strains: Novel Topical Formulations and Patent Review.","authors":"Ayushi Mahajan,&nbsp;Lakhvir Kaur,&nbsp;Gurjeet Singh,&nbsp;Ravi Kumar Dhawan,&nbsp;Lovepreet Singh","doi":"10.2174/2772434416666211111105854","DOIUrl":"https://doi.org/10.2174/2772434416666211111105854","url":null,"abstract":"<p><p>Luliconazole is a broad-spectrum antifungal agent with impactful fungicidal and fungistatic activity. It has shown exceptional potency against miscellaneous fungal strains like Candida, Aspergillus, Malassezia, Fusarium species and various dermatophytes. Luliconazole belongs to class II of the Biopharmaceutical Classification System with low aqueous solubility. Although it is available conventionally as 1% w/v topical cream, it has limitations of lower skin permeation and shorter skin retention. Therefore, nanoformulations based on various polymers and nanostructure carriers can be employed to overcome the impediments regarding topical delivery and efficacy of luliconazole. In this review, we have tried to provide insight into the literature gathered from authentic web resources and research articles regarding recent research conducted on the subject of formulation development, patents, and future research requisites of luliconazole. Nanoformulations can play a fundamental role in improving topical delivery by escalating dermal localization and skin penetration. Fabricating luliconazole into nanoformulations can overcome the drawbacks and can efficiently enhance its antimycotic activity. It has been concluded that luliconazole has exceptional potential in the treatment of various fungal infections, and therefore, it should be exploited to its maximum for its innovative application in the field of mycology.</p>","PeriodicalId":74643,"journal":{"name":"Recent advances in anti-infective drug discovery","volume":"16 3","pages":"182-195"},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39881725","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}