https://zenodo.org/record/1004771/files/Cushnie%20et%20al%20%282014%29%20post-peer%20reviewed%20version.pdf

Alkaloids: an overview of their antibacterial, antibiotic-enhancing and antivirulence activities.

Microbial resistance to classical antibiotics and its rapid progression have raised serious concern in the treatment of infectious diseases. Recently, many studies have been directed towards finding promising solutions to overcome these problems. Phytochemicals have exerted potential antibacterial activities against sensitive and resistant pathogens via different mechanisms of action. In this review, we have summarized the main antibiotic resistance mechanisms of bacteria and also discussed how phytochemicals belonging to different chemical classes could reverse the antibiotic resistance. Next to containing direct antimicrobial activities, some of them have exerted in vitro synergistic effects when being combined with conventional antibiotics. Considering these facts, it could be stated that phytochemicals represent a valuable source of bioactive compounds with potent antimicrobial activities.

/pdf/review-on-plant-antimicrobials-a-mechanistic-viewpoint-4pdgd1lkce.pdf

Review on plant antimicrobials: a mechanistic viewpoint

Antibiotic-resistant microorganisms have been an ever-growing concern over the past years. This has led researchers to direct their attention onto plants to be able to discover new possible antimicrobial compounds. The Middle East encompasses a wide spectrum of plant diversity with over 20,000 different species in habitats ranging from deserts to snow-capped mountains. Several plant secondary metabolites and their derivatives have been identified as possible antimicrobial agents. Among the secondary metabolites studied, alkaloids and polyphenols have shown strong antimicrobial activity. Polyphenols are one of the most numerous and diverse group of secondary metabolites; their antioxidant properties provide the basis for antimicrobial effects. Alkaloids provided the underlying structure for the development of several antibiotics with a diverse range of action. The ability of some plant secondary metabolites to act as resistance-modifying agents is a promising field in mitigating the spread of bacterial resistance.

/pdf/antimicrobial-activity-of-polyphenols-and-alkaloids-in-285mheylmj.pdf

Antimicrobial Activity of Polyphenols and Alkaloids in Middle Eastern Plants.

https://cyberleninka.org/article/n/144647.pdf

New agents for the treatment of drug-resistant Mycobacterium tuberculosis

Mannich bases in medicinal chemistry and drug design.

1,5-Diphenyl pyrroles were previously identified as a class of compounds endowed with high in vitro efficacy against M. tuberculosis. To improve the physical chemical properties and drug-like parameters of this class of compounds, a medicinal chemistry effort was undertaken. By selecting the optimal substitution patterns for the phenyl rings at N1 and C5 and by replacing the thiomorpholine moiety with a morpholine one, a new series of compounds was produced. The replacement of the sulfur with oxygen gave compounds with lower lipophilicity and improved in vitro microsomal stability. Moreover, since the parent compound of this family has been shown to target MmpL3, mycobacterial mutants resistant to two compounds have been isolated and characterized by sequencing the mmpL3 gene; all the mutants showed point mutations in this gene. The best compound identified to date was progressed to dose-response studies in an acute murine TB infection model. The resulting ED(99) of 49 mg/Kg is within the range of commonly employed tuberculosis drugs, demonstrating the potential of this chemical series. The in vitro and in vivo target validation evidence presented here adds further weight to MmpL3 as a druggable target of interest for anti-tubercular drug discovery.

/pdf/improved-bm212-mmpl3-inhibitor-analogue-shows-efficacy-in-2hacyzjnn0.pdf

Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection.

Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases.

The biological diversity of nature is the source of a wide range of bioactive molecules. The natural products, either as pure compounds or as standardized plant extracts, have been a successful source of inspiration for the development of new drugs. The present work was carried out to investigate the cytotoxicity, antiviral and antimycobacterial activity of the methanol extract and of four identified limonoids from the fruits of Melia azedarach (Meliaceae). The extract and purified limonoids were tested in cell-based assays for antiviral activity against representatives of ssRNA, dsRNA and dsDNA viruses and against Mycobacterium tuberculosis. Very interestingly, 3-α-tigloyl-melianol and melianone showed a potent antiviral activity (EC50 in the range of 3–11μM) against three important human pathogens, belonging to Flaviviridae family, West Nile virus, Dengue virus and Yellow Fever virus. Mode of action studies demonstrated that title compounds were inhibitors of West Nile virus only when added during the infection, acting as inhibitors of the entry or of a very early event of life cycle. Furthermore, 3-α-tigloyl-melianol and methyl kulonate showed interesting antimycobacterial activity (with MIC values of 29 and 70 μM respectively). The limonoids are typically lipophilic compounds present in the fruits of Melia azeradach. They are known as cytotoxic compounds against different cancer cell lines, while their potential as antiviral and antibacterial was poorly investigated. Our studies show that they may serve as a good starting point for the development of novel drugs for the treatment of infections by Flaviviruses and Mycobacterium tuberculosis, for which there is a continued need.

/pdf/limonoids-from-melia-azedarach-fruits-as-inhibitors-of-3onf8pgtyr.pdf

Limonoids from Melia azedarach fruits as inhibitors of flaviviruses and mycobacterium tubercolosis

Herpes simplex virus (HSV) is one of the most common viral diseases in humans. Herpes simplex virus 1 (HSV-1) and Herpes simplex virus 2 (HSV-2) have been distinguished by clinical manifestations and biological and serological criteria. Several drugs have proved useful in the treatment of many specific infections, but viral strains resistant to these drugs have been increasingly identified [1]. In order to find less toxic antiviral agents, many researchers have addressed plant products. Indeed, many plant extracts and their secondary metabolites are known in the literature for their antiviral activity [2, 3]. Bituminaria bituminosa L. (syn. Psoralea bituminosa L., Leguminosae) is a perennial herb widespread in the Mediterranean area, known in Italy as “trifoglio bituminoso”; the fresh leaves are used in folk medicine as vulnerary, cicatrizing, and disinfectant agent [4, 5]. Plants of the genus Bituminaria are known as source of furanocoumarins and flavonoids [6, 7]. In our previous phytochemical study [8], three pterocarpans (erybraedin C and the new bitucarpins A and B) together with plicatin B were isolated and identified from B. bituminosa aerial parts. Erybraedin C and bitucarpin A showed cytotoxicity in different cell lines [9], induced apoptosis in colon carcinoma cell lines, and exhibited anti-clastogenic activity in lymphocytes [10, 11]; erybraedin C showed inhibitory activity against human topoisomerase I [12] and significant antioxidant activity [13]. The antiviral activity of the pterocarpan compounds, isolated from different plant sources, has been reported in the literature [14, 15], and some of these derivatives were active against HSV-2 [16]. In the present investigation, the antiviral activity of a few B. bituminosa extracts and their isolates erybraedin C (1), bitucarpin A (2), and plicatin B (3) is reported for the first time. The tested extracts were characterized in their quantitative chemical composition by HPLC-DAD-MS analysis.

HPLC-DAD-MS Analysis and Antiviral Activity of Different Extracts and Isolated Constituents from Bituminaria bituminosa

Handle everyday research tasks with reliable, citation-backed results

Your personal Research Agent to handle research tasks with citation-backed results

Popular Tasks used by Researchers

How can I help with your research?

Meet SciSpace

Get more enhanced response by uploading the PDFs you want me to reference.

No relevant PDFs in your library

SciSpace is the AI research assistant for academics. Run systematic literature reviews on 280M+ papers, and write papers with cited sources. Trusted by 1M+ students, PhDs & researchers.

SciSpace | AI for Research

Analyze PDFs

Code & Manuscripts

Funding & Grants

Literature & Patents

Medical & Clinical Data

Systematic Review

Visualize & Present

Web & Data

Build a Google Scholar-like website for your research.

Build a website

Create charts and images for your research

Create a Chart

Write a paper for submission to a journal

Draft a manuscript

Patent Search

Design eye-catching scientific posters in minutes.

Scientific Poster Generation

Systematic Literature Review

One task is running at the moment. Your messages will be shown right after.

Drag and drop or click here to browse

Loved by <highlight>1 million+</highlight> researchers

Extract a list of specific topics and their sources from unstructured text

Topics

Compare and analyze relevant papers that matches with your search

Papers

Get insights from PDFs and bookmarked papers from your library

My library

Recent searches

Try searching for:

Catch AI-generated content in scholarly and non-scholarly content

{ai} Detector

Ai Writer

Get PDF Summaries, highlighted text explanations 

Chat with PDF

Effortlessly create in-text citations and bibliographies in APA and 2,500 other formats

Citation generator

Get explanations, summaries, and answers on academic papers

Ease up your research workflow with {scispace}'s cohort of exciting AI tools

Elevate your academic writing skills and convey your ideas the way you want

Paraphraser

Explore our range of reading and writing tools

Your file is being prepared and should be ready in a few minutes. If it's a large file, it might take a bit longer. You can close this window, and we'll email you the file when it's done.

You have reached a maximum limit of <strong>{limit}</strong> columns in the table. Remove at least <strong>1</strong> column to add or create another one.

E Agus

Author Tools

Chat about Author

Papers

Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection.

Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases.

Limonoids from Melia azedarach fruits as inhibitors of flaviviruses and mycobacterium tubercolosis

HPLC-DAD-MS Analysis and Antiviral Activity of Different Extracts and Isolated Constituents from Bituminaria bituminosa