Semi-synthetic zwitterionic rifamycins: a promising class of antibiotics; survey of their chemistry and biological activities

RSC Advances ◽  
2016 ◽  
Vol 6 (115) ◽  
pp. 114758-114772 ◽  
Author(s):  
Krzysztof Bujnowski ◽  
Ludwik Synoradzki ◽  
Radosław C. Darłak ◽  
Thomas A. Zevaco ◽  
Eckhard Dinjus
Keyword(s):  
Pathogenic Bacteria ◽  
Biological Activities ◽  
Gram Positive ◽  
Important Group ◽  
Highly Active ◽  
Macrocyclic Antibiotics

Rifamycins are an important group of macrocyclic antibiotics highly active against tuberculosis and various other Gram-positive pathogenic bacteria.

scholarly journals BIOLOGICAL ACTIVITIES OF ALTERNARIA SP. RL4 – A POTENT ENDOPHYTIC FUNGUS ASSOCIATED WITH RAUVOLFIA SERPENTINA L. BENTH.

2018 ◽  
Vol 11 (11) ◽  
pp. 178
Author(s):  
Ranjan Ghosh ◽  
Soma Barman ◽  
Pavan Kumar Jgs ◽  
Narayan C Mandal
Keyword(s):  
Mode Of Action ◽  
Pathogenic Bacteria ◽  
Biological Activities ◽  
Fungal Endophytes ◽  
Radical Scavenging ◽  
New Drugs ◽  
Bioactive Metabolites ◽  
Gram Positive ◽  
Rauvolfia Serpentina ◽  
Alternaria Sp

Objectives: Endophytic fungi are considered as an important source of bioactive metabolites. The present study focused on the isolation of potent endophytic fungal strains from well-known medicinal plant Rauvolfia serpentina L. Benth. having biological activities.Materials & Methods: Fungal endophytes were isolated from aerial parts of the plant and the potent strain was selected on the basis of antibacterial activities of cell-free supernatant (CFS). Ethyl acetate (EA) extraction of CFS was done and mode of action of EA fraction was checked against pathogenic bacteria. EA fraction was also analyzed by thin-layer chromatography (TLC). In addition, antioxidant activity was checked by 1,1-Diphenyl- 2-picrylhydrazyl-free radical scavenging assay and anticancer activity was checked against breast cancer cell line MCF-7 by MTT assay.Results: Among the different endophytic fungal isolates, CFS of Alternaria sp. RL4 produced prominent zones of inhibition against numbers of Gram-positive pathogenic bacteria including Staphylococcus aureus (12±0.5 mm) and Listeria monocytogenes (17±2.0 mm). Massive reductions in bacterial CFS were noticed upon treatment with EA fraction (2 mg/ml). It also showed strong cidal mode of action against Gram-positive organisms. TLC analysis revealed the production of two different compounds with antibacterial potentials. In addition, EA fraction of RL4 showed very good antioxidant property with an IC50 value of 49.80±2.11μg/ml. MTT assay also suggested the anticancerous properties of EA fraction of RL4.Conclusion: Alternaria sp. RL4 could be a very good source of bioactive compounds for the development of new drugs.

scholarly journals Application of nano-curcumin as a natural antimicrobial agent against Gram-positive pathogens

2021 ◽  
Vol 13 (1) ◽  
pp. 110-126
Author(s):  
Ruchi Sankhwar ◽  
Shilpi Yadav ◽  
Abhishek Kumar ◽  
Ravi Kr. Gupta
Keyword(s):  
Pathogenic Bacteria ◽  
Biological Activities ◽  
Aqueous Solubility ◽  
Gram Positive ◽  
Curcumin Nanoparticles ◽  
Superficial Skin ◽  
Potential Applications ◽  
Conventional Antibiotics

Gram-positive bacteria cause various diseases from the superficial skin to deep tissue infections. The capability of causing numerous diseases is due to the production of virulence factors which are tightly regulated by the virulence genes. Various Gram-positive pathogenic bacteria e.g. Staphylococcus, Mycobacterium, and Listeria are capable of causing lethal infections in humans and animals. Conventional antibiotics, targeted antibiotics, and combinatorial drugs are used as therapeutic agents against Gram-positive pathogens. Due to intricate virulence pathway bacteria readily adopt resistance to available drugs. Therefore, there is need to develop some alternative approaches to combat these infections. Various natural extracts are effective against pathogenic bacteria with or without the available drugs. Curcumin is a natural extract of Curcuma longas rhizome, known as turmeric. Curcumin shows various biological activities such as antimicrobial, antioxidant and anti-inflammatory. It also shows strong antibacterial activity against Gram-positive and few Gram-negative bacteria. Besides all these beneficial applications, major drawbacks of curcumin are poor aqueous solubility and less bioavailability. However, drug delivery approaches including nanoformulation are developed to increase its stability in vitro and in vivo settings. The present review article focused on the translation of potential applications of curcumin in various diseases specifically caused by Gram-positive pathogens. Various methods used for the formulations of curcumin nanoparticles, combinatorial strategies with curcumin nanoparticles and their application in the prevention of infections have been discussed. The present article also discusses the future aspects of curcumin-nanoparticles and its use as an alternative therapeutic approach against pathogens.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

scholarly journals An Insight into Saponins from Quinoa (Chenopodium quinoa Willd): A Review

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1059 ◽  
Author(s):  
Khadija El Hazzam ◽  
Jawhar Hafsa ◽  
Mansour Sobeh ◽  
Manal Mhada ◽  
Moha Taourirte ◽  
...  
Keyword(s):  
Heat Treatment ◽  
Bitter Taste ◽  
Biological Activities ◽  
Chenopodium Quinoa ◽  
Toxic Effects ◽  
Mechanical Abrasion ◽  
Important Group ◽  
The Past ◽  
Wide Range ◽  
Insight Into

Saponins are an important group found in Chenopodium quinoa. They represent an obstacle for the use of quinoa as food for humans and animal feeds because of their bitter taste and toxic effects, which necessitates their elimination. Several saponins elimination methods have been examined to leach the saponins from the quinoa seeds; the wet technique remains the most used at both laboratory and industrial levels. Dry methods (heat treatment, extrusion, roasting, or mechanical abrasion) and genetic methods have also been evaluated. The extraction of quinoa saponins can be carried out by several methods; conventional technologies such as maceration and Soxhlet are the most utilized methods. However, recent research has focused on technologies to improve the efficiency of extraction. At least 40 saponin structures from quinoa have been isolated in the past 30 years, the derived molecular entities essentially being phytolaccagenic, oleanolic and serjanic acids, hederagenin, 3β,23,30 trihydroxy olean-12-en-28-oic acid, 3β-hydroxy-27-oxo-olean-12en-28-oic acid, and 3β,23,30 trihydroxy olean-12-en-28-oic acid. These metabolites exhibit a wide range of biological activities, such as molluscicidal, antifungal, anti-inflammatory, hemolytic, and cytotoxic properties.

scholarly journals Effects of Growth Phase and Extracellular Slime on Photodynamic Inactivation of Gram-Positive Pathogenic Bacteria

2004 ◽  
Vol 48 (6) ◽  
pp. 2173-2178 ◽  
Author(s):  
Faten Gad ◽  
Touqir Zahra ◽  
Tayyaba Hasan ◽  
Michael R. Hamblin
Keyword(s):  
Stationary Phase ◽  
Pathogenic Bacteria ◽  
Capsular Polysaccharide ◽  
Photodynamic Inactivation ◽  
Wild Type ◽  
Gram Positive ◽  
Slime Production ◽  
Subsequent Exposure ◽  
Cationic Compounds ◽  
Extracellular Slime

ABSTRACT The emergence of antibiotic resistance among pathogenic bacteria has led to efforts to find alternative antimicrobial therapeutics to which bacteria will not be easily able to develop resistance. One of these may be the combination of nontoxic dyes (photosensitizers [PS]) and visible light, known as photodynamic therapy, and we have reported its use to treat localized infections in animal models. While it is known that gram-positive species are generally susceptible to photodynamic inactivation (PDI), the factors that govern variation in degrees of killing are unknown. We used isogenic pairs of wild-type and transposon mutants deficient in capsular polysaccharide and slime production generated from Staphylococcus epidermidis and Staphylococcus aureus to examine the effects of extracellular slime on susceptibility to PDI mediated by two cationic PS (a polylysine-chlorin e6 conjugate, pL-c e6 , and methylene blue [MB]) and an anionic molecule, free c e6 , and subsequent exposure to 665-nm light at 0 to 40 J/cm2. Free c e6 gave more killing of mutant strains than wild type, despite the latter taking up more PS. Log-phase cultures were killed more than stationary-phase cultures, and this correlated with increased uptake. The cationic pL-c e6 and MB gave similar uptakes and killing despite a 50-fold difference in incubation concentration. Differences in susceptibility between strains and between growth phases observed with free c e6 largely disappeared with the cationic compounds despite significant differences in uptake. These data suggest that slime production and stationary phase can be obstacles against PDI for gram-positive bacteria but that these obstacles can be overcome by using cationic PS.

Biosynthesis of Silver Nanoparticles by Punica Granatum Peel Extract and their Biological Activity on different Pathogenic Bacteria

2021 ◽  
Vol 19 (9) ◽  
pp. 38-45
Author(s):  
Hussein H. Al-Turnachy ◽  
Fadhilk. alibraheemi ◽  
Ahmed Abd Alreda Madhloom ◽  
Zahraa Yosif Motaweq ◽  
Nibras Yahya Abdulla
Keyword(s):  
Antimicrobial Activity ◽  
Silver Nanoparticles ◽  
Biological Activity ◽  
Pathogenic Bacteria ◽  
Punica Granatum ◽  
Gram Positive ◽  
Gram Negative ◽  
Inhibition Zones ◽  
Peel Extract

The present study was included the assessment of the antimicrobial activity of AgNPs synthesized by Punica granatum peel extract against pathogenic bacteria by testing warm aqueous P. granatum peel extract and silver nanoparticles. Punica granatum indicated potency for AgNP extracellular nanobiosynthesis after addition of silver nitrate (AgNO3) 4mM to the extract supernatant, in both concentrations (100mg and 50mg). The biogenic AgNPs showed potency to inhibit both gram-negative and gram-positive bacterial growth. Zons of inhibition in (mm) was lesser in gram-positive than gram-negative bacteria. The resulted phytogenic AgNPs gave higher biological activity than warm aqueous Punica granatum peel extract. The inhibition zone of the phytogenic AgNPs on E. coli reached 17.53, 22.35, and 26.06 mm at (0.1, 0.5, and 1) mg/ml respectively. While inhibition zones of Punica warm aqueous extract reached 5.33, 10.63, and 16.08 mm at the same concentrations. phytogenic AgNPs gave smaller inhibition zones in gram-positive than gram- negative. Cytotoxic activity of the phytogenic AgNPs was assayed in vitro agaist human blood erythrocytes (RBCs), spectroscopic results showed absorbance at 540 nm hemolysis was observed. In general, AgNPs showed least RBCs hemolysis percentage, at 1 mg/ml concentration, hemolysis percentage was (4.50%). This study, concluded that the Punica granatum peel extract has the power of synthses of AgNPs characterized by broad spectrum antimicrobial activity with cyto-toxicity proportional to AgNPs concentration.

Antimicrobial activity of Pycnarrhena cauliflora (Miers.) Diels. methanol extract

2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Positive Control ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Methanolic Extracts

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.

Effectiveness of Trisodium Phosphate, Acidified Sodium Chlorite, Citric Acid, and Peroxyacids against Pathogenic Bacteria on Poultry during Refrigerated Storage

2007 ◽  
Vol 70 (9) ◽  
pp. 2063-2071 ◽  
Author(s):  
ELENA del RÍO ◽  
REBECA MURIENTE ◽  
MIGUEL PRIETO ◽  
CARLOS ALONSO-CALLEJA ◽  
ROSA CAPITA
Keyword(s):  
Citric Acid ◽  
Salmonella Enteritidis ◽  
Pathogenic Bacteria ◽  
Trisodium Phosphate ◽  
Sodium Chlorite ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Microbial Group ◽  
And Control

The effects of dipping treatments (15 min) in potable water or in solutions (wt/vol) of 12% trisodium phosphate (TSP), 1,200 ppm acidified sodium chlorite (ASC), 2% citric acid (CA), and 220 ppm peroxyacids (PA) on inoculated pathogenic bacteria (Listeria monocytogenes, Staphylococcus aureus, Bacillus cereus, Salmonella Enteritidis, Escherichia coli, and Yersinia enterocolitica) and skin pH were investigated throughout storage of chicken legs (days 0, 1, 3, and 5) at 3 ± 1°C. All chemical solutions reduced microbial populations (P < 0.001) as compared with the control (untreated) samples. Similar bacterial loads (P > 0.05) were observed on water-dipped and control legs. Type of treatment, microbial group, and sampling day influenced microbial counts (P < 0.001). Average reductions with regard to control samples were 0.28 to 2.41 log CFU/g with TSP, 0.33 to 3.15 log CFU/g with ASC, 0.82 to 1.97 log CFU/g with CA, and 0.07 to 0.96 log CFU/g with PA. Average reductions were lower (P < 0.001) for gram-positive (0.96 log CFU/g) than for gram-negative (1.33 log CFU/g) bacteria. CA and ASC were the most effective antimicrobial compounds against gram-positive and gram-negative bacteria, respectively. TSP was the second most effective compound for both bacterial groups. Average microbial reductions per gram of skin were 0.87 log CFU/g with TSP, 0.86 log CFU/g with ASC, 1.39 log CFU/g with CA, and 0.74 log CFU/g with PA for gram-positive bacteria, and 1.28 log CFU/g with TSP, 2.03 log CFU/g with ASC, 1.23 log CFU/g with CA, and 0.78 log CFU/g with PA for gram-negative bacteria. With only a few exceptions, microbial reductions in TSP- and ASC-treated samples decreased and those in samples treated with CA increased throughout storage. Samples treated with TSP and samples dipped in CA and ASC had the highest and lowest pH values, respectively, after treatment. The pH of the treated legs tended to return to normal (6.3 to 6.6) during storage. However, at the end of storage, the pH of legs treated with TSP remained higher and that of legs treated with CA remained lower than normal.

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