Pore-forming peptides: a new treatment option for cancer

2021 ◽  
Vol 28 ◽  
Author(s):  
Zohreh Jahanafrooz ◽  
Ahad Mokhtarzadeh
Keyword(s):  
Significant Proportion ◽  
Safety Evaluation ◽  
Medical Problem ◽  
Resistance Mechanisms ◽  
Bioactive Molecules ◽  
Physical Damage ◽  
Natural Defense ◽  
Target Cell Membrane ◽  
Living Organisms ◽  
Antibacterial And Antifungal

: Cancer, as a remaining challenging medical problem, affects millions of people around the world. Cancer cell resistance is one of the main drawbacks in the complete prosperity of even more sophisticated therapies. Pore-forming peptides (PFPs), a group of natural defense system’s proteins used by nearly whole living organisms as antibacterial and antifungal agents, could also be regarded as novel tumoricidal peptides. PFPs approach entails the use of soluble peptides by assembling on mainly target cell membrane and forming potential death-causing pores. Physical damage induction by natural PFPs or their synthetic derivatives could conquer the resistance mechanisms of tumor cells. Given that peptide drugs involve a significant proportion of the pharmaceutical market primarily because of easy synthesis and safety, evaluation of this nature provided model system as a group of anticancer peptides seems a valuable approach. Here, the mode of action of PFPs and their anticancer mechanism are highlighted which is followed by addressing the anticancer studies using PFPs from various sources along with various applied strategies to obtain selective action of PFPs against cancer cells. Challenges and future perspectives of these promising bioactive molecules in cancer treatment are also provided.

scholarly journals Valorization of Sicanaodorifera (Vell.) Naudin Epicarp as a Source of Bioactive Compounds: Chemical Characterization and Evaluation of Its Bioactive Properties

Foods ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 700
Author(s):  
Bianca R. Albuquerque ◽  
Maria Inês Dias ◽  
Carla Pereira ◽  
Jovana Petrović ◽  
Marina Soković ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Bioactive Compounds ◽  
Food Additives ◽  
Chemical Characterization ◽  
Dry Weight ◽  
Bioactive Molecules ◽  
High Concentration ◽  
Minimal Inhibitory Concentrations ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Fruit bio-residues can be interesting for the recovery of bioactive molecules, such as phenolic compounds, tocopherols, vitamins, among others. These compounds can be targeted at the food industry and used for the development of functional foods or as food additives. In some cases, fruit epicarps are converted into by-products with non-commercial value, and generally, these fruit parts have a higher content in bioactive compounds than the fruit pulp. From this perspective, S. odorifera, a Brazilian fruit, has an inedible epicarp that could be explored to obtain biological compounds. Therefore, the aims of this study were to evaluate the chemical composition and the antioxidant, anti-proliferative, anti-inflammatory, and antimicrobial bioactivities of this by-product. S. odorifera epicarp showed a total of four organic acids, four phenolic compounds, highlighting the high concentration of anthocyanins (24 ± 1 mg/g dry weight (dw)) and high content of tocopherols (366 ± 2 mg/100 g dw). The hydroethanolic extract showed considerable antioxidant activity (EC50 values of 48.2 ± 0.5 and 27 ± 1 µg/mL for TBARS and OxHLIA assays, respectively), as also antibacterial and antifungal activities (minimal inhibitory concentrations (MICs) ≤ 2.2 mg/mL). The results obtained in this study suggest that Sicana odorifera epicarp represents a reliable option for the development of novel natural-based colorants with functional/bioactive proprieties.

Genital elephantiasis and sexually transmitted infections – revisited

2006 ◽  
Vol 17 (3) ◽  
pp. 157-166 ◽  
Author(s):  
Somesh Gupta ◽  
C Ajith ◽  
Amrinder J Kanwar ◽  
Virendra N Sehgal ◽  
Bhushan Kumar ◽  
...  
Keyword(s):  
Sexually Transmitted Infections ◽  
Causative Agent ◽  
Significant Proportion ◽  
Medical Problem ◽  
Nucleic Acid Amplification ◽  
Sexually Transmitted ◽  
Laboratory Facilities ◽  
Laboratory Investigations ◽  
Polymerase Chain ◽  
The Tropics

Genital elephantiasis is an important medical problem in the tropics. It usually affects young and productive age group, and is associated with physical disability and extreme mental anguish. The majority of cases are due to filariasis; however, a small but significant proportion of patients develop genital elephantiasis due to bacterial sexually transmitted infections (STIs), mainly lymphogranuloma venereum (LGV) and donovanosis. STI-related genital elephantiasis should be differentiated from elephantiasis due to other causes, including filariasis, tuberculosis, haematological malignancies, iatrogenic, or dermatological diseases. Laboratory investigations like microscopy of tissue smear and nucleic acid amplification test for donovanosis, and serology and polymerase chain reaction for LGV may help in the diagnosis, but in endemic areas, in the absence of laboratory facilities, diagnosis largely depends on clinical characteristics. The causative agent of LGV, Chlamydia trachomatis serovar L1–L3, is a lymphotropic organism which leads to the development of thrombolymphangitis and perilymphangitis, and lymphadenitis. Long-standing oedema, fibrosis and lymphogranulomatous infiltration result in the final picture of elephantiasis. Elephantiasis in donovanosis is mainly due to constriction of the lymphatics which are trapped in the chronic granulomatous inflammatory response generated by the causative agent, Calymmatobacterium (Klebsiella) granulomatis. The LGV-associated genital elephantiasis should be treated with a prolonged course of doxycycline given orally, while donovanosis should be treated with azithromycin or trimethoprim-sulphamethoxazole combination given for a minimum of three weeks. Genital elephantiasis is not completely reversible with medical therapy alone and often needs to be reduced surgically.

scholarly journals Antibiotic Resistances of Starter and Probiotic Strains of Lactic Acid Bacteria

2006 ◽  
Vol 73 (3) ◽  
pp. 730-739 ◽  
Author(s):  
Anja S. Hummel ◽  
Christian Hertel ◽  
Wilhelm H. Holzapfel ◽  
Charles M. A. P. Franz
Keyword(s):  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Resistance Genes ◽  
Evaluation System ◽  
Genetic Basis ◽  
Safety Evaluation ◽  
Resistance Mechanisms ◽  
Resistance Testing ◽  
Gene Probe ◽  
Erythromycin Resistance

ABSTRACT The antibiotic resistances of 45 lactic acid bacteria strains belonging to the genera Lactobacillus, Streptococcus, Lactococcus, Pediococcus, and Leuconostoc were investigated. The objective was to determine antibiotic resistances and to verify these at the genetic level, as is currently suggested by the European “qualified presumption of safety” safety evaluation system for industrial starter strains. In addition, we sought to pinpoint possible problems in resistance determinations. Primers were used to PCR amplify genes involved in β-lactam antibiotic, chloramphenicol, tetracycline, and erythromycin resistance. The presence of ribosomal protection protein genes and the ermB gene was also determined by using a gene probe. Generally, the incidences of erythromycin, chloramphenicol, tetracycline, or β-lactam resistances in this study were low (<7%). In contrast, aminoglycoside (gentamicin and streptomycin) and ciprofloxacin resistances were higher than 70%, indicating that these may constitute intrinsic resistances. The genetic basis for ciprofloxacin resistance could not be verified, since no mutations typical of quinolone resistances were detected in the quinolone determining regions of the parC and gyrA genes. Some starter strains showed low-level ampicillin, penicillin, chloramphenicol, and tetracycline resistances, but no known resistance genes could be detected. Although some strains possessed the cat gene, none of these were phenotypically resistant to chloramphenicol. Using reverse transcription-PCR, these cat genes were shown to be silent under both inducing and noninducing conditions. Only Lactobacillus salivarius BFE 7441 possessed an ermB gene, which was encoded on the chromosome and which could not be transferred in filter-mating experiments. This study clearly demonstrates problems encountered with resistance testing, in that the breakpoint values are often inadequately identified, resistance genes may be present but silent, and the genetic basis and associated resistance mechanisms toward some antibiotics are still unknown.

scholarly journals Enantioselectivity Effects in Clinical Metabolomics and Lipidomics

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5231
Author(s):  
Regina V. Oliveira ◽  
Ana Valéria C. Simionato ◽  
Quezia B. Cass
Keyword(s):  
Drug Targets ◽  
Method Development ◽  
Bioactive Molecules ◽  
Bioactive Metabolites ◽  
Clinical Samples ◽  
Therapeutic Approaches ◽  
Biochemical Mechanisms ◽  
Living Organisms ◽  
Novel Drug

Metabolomics and lipidomics have demonstrated increasing importance in underlying biochemical mechanisms involved in the pathogenesis of diseases to identify novel drug targets and/or biomarkers for establishing therapeutic approaches for human health. Particularly, bioactive metabolites and lipids have biological activity and have been implicated in various biological processes in physiological conditions. Thus, comprehensive metabolites, and lipids profiling are required to obtain further advances in understanding pathophysiological changes that occur in cells and tissues. Chirality is one of the most important phenomena in living organisms and has attracted long-term interest in medical and natural science. Enantioselective separation plays a pivotal role in understanding the distribution and physiological function of a diversity of chiral bioactive molecules. In this context, it has been the goal of method development for targeted and untargeted metabolomics and lipidomic assays. Herein we will highlight the benefits and challenges involved in these stereoselective analyses for clinical samples.

scholarly journals Microbial bioremediation of heavy metals

2021 ◽  
Vol 75 (2) ◽  
pp. 103-115
Author(s):  
Ana Volaric ◽  
Zorica Svircev ◽  
Dragana Tamindzija ◽  
Dragan Radnovic
Keyword(s):  
Heavy Metals ◽  
Heavy Metal ◽  
Heavy Metal Resistance ◽  
Pilot Scale ◽  
Resistance Mechanisms ◽  
Metal Resistance ◽  
Novel Technologies ◽  
Living Organisms ◽  
Microbial Bioremediation ◽  
Physical And Chemical

Heavy metal pollution is one of the most serious environmental problems, due to metal ions persistence, bioavailability, and toxicity. There are many conventional physical and chemical techniques traditionally used for environmental clean-up. Due to several drawbacks regarding these methods, the use of living organisms, or bioremediation, is becoming more prevalent. Biotechnological application of microorganisms is already successfully implemented and is in constant development, with many microbial strains successfully removing heavy metals. This paper provides an overview of the main heavy metal characteristics and describes the interactions with microorganisms. Key heavy metal resistance mechanisms in microorganisms are described, as well as the main principles and types of heavy metal bioremediation methods, with details on successful pilot scale bioreactor studies. Special attention should be given to indigenous bacteria isolated from the polluted environments since such species are already adapted to contamination and possess resistance mechanisms. Utilization of bacterial biofilms or consortia could be advantageous due to higher resistance and a combination of several metabolic pathways, and thus, the possibility to remove several heavy metals simultaneously. Novel technologies covered in this review, such as nanotechnology, genetic engineering, and metagenomics, are being introduced to the field of bioremediation in order to improve the process. To conclude, bioremediation is a potentially powerful solution for cleaning the environment.

scholarly journals Macroalgae as a Source of Valuable Antimicrobial Compounds: Extraction and Applications

Antibiotics ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 642
Author(s):  
Aurora Silva ◽  
Sofia A. Silva ◽  
M. Carpena ◽  
P. Garcia-Oliveira ◽  
P. Gullón ◽  
...  
Keyword(s):  
Electric Fields ◽  
Consumer Preferences ◽  
Biological Properties ◽  
Nutritional Composition ◽  
Bioactive Molecules ◽  
Special Role ◽  
Antimicrobial Compounds ◽  
Extraction Techniques ◽  
Antifouling Coating ◽  
Antibacterial And Antifungal

In the last few decades, attention on new natural antimicrobial compounds has arisen due to a change in consumer preferences and the increase in the number of resistant microorganisms. Macroalgae play a special role in the pursuit of new active molecules as they have been traditionally consumed and are known for their chemical and nutritional composition and their biological properties, including antimicrobial activity. Among the bioactive molecules of algae, proteins and peptides, polysaccharides, polyphenols, polyunsaturated fatty acids and pigments can be highlighted. However, for the complete obtaining and incorporation of these molecules, it is essential to achieve easy, profitable and sustainable recovery of these compounds. For this purpose, novel liquid–liquid and solid–liquid extraction techniques have been studied, such as supercritical, ultrasound, microwave, enzymatic, high pressure, accelerated solvent and intensity pulsed electric fields extraction techniques. Moreover, different applications have been proposed for these compounds, such as preservatives in the food or cosmetic industries, as antibiotics in the pharmaceutical industry, as antibiofilm, antifouling, coating in active packaging, prebiotics or in nanoparticles. This review presents the main antimicrobial potential of macroalgae, their specific bioactive compounds and novel green extraction technologies to efficiently extract them, with emphasis on the antibacterial and antifungal data and their applications.

Antimicrobial Peptides: An Approach to Combat Resilient Infections

2020 ◽  
Vol 17 (4) ◽  
pp. 542-552 ◽  
Author(s):  
Debaprasad Parai ◽  
Pia Dey ◽  
Samir K. Mukherjee
Keyword(s):  
Antimicrobial Peptides ◽  
Developmental Stages ◽  
Rapid Development ◽  
Resistance Mechanisms ◽  
New Drugs ◽  
Bacterial Strains ◽  
Common People ◽  
Wide Range ◽  
Microbial Infections ◽  
Living Organisms

Background:It was apparent by the end of 1980s that the success against the threats of bacterial pathogens on public health was an illusion, with the rapid development of resistant strains more than the discovery of new drugs. As a consequence, the remedial services were in the backfoot position of being on the losing side of this never-ending evolutionary war. The quest for new antibiotics to overcome resistance problems has long been a top research priority for the researchers and the pharmaceutical industry. However, the resistance problems remain unresolved due to the abrupt misuse of antibiotics by common people, which has immensely worsened the scenario by disseminating antibiotic-resistant bacterial strains around the world.Objective:Thus, immediate action is needed to measure emerging and re-emerging microbial diseases having new resistance mechanisms and to manage their rapid spread among the common public by means of novel alternative metabolites.Conclusion:Antimicrobial Peptides (AMPs) are short, cationic peptides evolved in a wide range of living organisms and serve as the essential part of the host innate immunity. For humans, these effector molecules either can directly kill the foreign microbes or modulate the host immune systems so that the human body could develop some resistance against the microbial infections. In this review, we discuss their history, structural classifications, modes of action, and explain their biological roles as anti-infective agents. We also scrutinize their clinical potentiality, current limitations in various developmental stages and strategies to overcome for their successful clinical applications.

Biological Significance of Imidazole-based Analogues in New Drug Development

2020 ◽  
Vol 17 (5) ◽  
pp. 574-584 ◽  
Author(s):  
Pratiksha N. Chopra ◽  
Jagdish K. Sahu
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Biological Significance ◽  
Water Soluble ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Ring Structures ◽  
Antibacterial And Antifungal ◽  
Therapeutic Compounds ◽  
Synthetic Medicinal

In the field of heterocyclic medicinal chemistry, especially five-membered ring structures containing a nitrogen atom, imidazole core is an imperative aromatic heterocycle which is usually present in naturally occurring products and synthetic bioactive molecules. The occurrence of imidazole moiety in therapeutic compounds may be beneficial in terms of improving water-soluble properties due to its two nitrogen atoms which leads to the creation of hydrogen bonds. The imidazole nucleus has also been recognized as an important isostere of triazole, pyrazole, thiazole, tetrazole, oxazole, amide etc. for the purpose of designing and development of various biologically active molecules. Moreover, imidazole core as an attractive binding site could interact with diverse cations and anions as well as biomolecules through different reactions in the human biological system thus displaying extensive biological activities. This effort thoroughly provides a wide-ranging assessment in current drug discovery and developments of imidazolebased analogues in the entire series of synthetic medicinal chemistry as antibacterial and antifungal, anticancer, anti-tubercular, analgesic and anti-inflammatory, anti-neuropathic, antihypertensive, anti-allergic, anti-parasitic, antiviral, antidepressant, anti-obesity and so on, altogether with their prospective approaches in diagnostic and pathological field. It is expected that the present review will be supportive on behalf of new opinions in the search for rational strategies of more efficacious and less toxic medicinal agents and drugs containing imidazole core.

scholarly journals Algae-Derived Bioactive Molecules for the Potential Treatment of SARS-CoV-2

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2134
Author(s):  
Md. Asraful Alam ◽  
Roberto Parra-Saldivar ◽  
Muhammad Bilal ◽  
Chowdhury Alfi Afroze ◽  
Md. Nasir Ahmed ◽  
...  
Keyword(s):  
Viral Infections ◽  
Extreme Environments ◽  
Research Area ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Defense Compounds ◽  
Natural Defense ◽  
Starting Point ◽  
Significant Public Health ◽  
Health Experts

The recently emerged COVID-19 disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has adversely affected the whole world. As a significant public health threat, it has spread worldwide. Scientists and global health experts are collaborating to find and execute speedy diagnostics, robust and highly effective vaccines, and therapeutic techniques to tackle COVID-19. The ocean is an immense source of biologically active molecules and/or compounds with antiviral-associated biopharmaceutical and immunostimulatory attributes. Some specific algae-derived molecules can be used to produce antibodies and vaccines to treat the COVID-19 disease. Algae have successfully synthesized several metabolites as natural defense compounds that enable them to survive under extreme environments. Several algae-derived bioactive molecules and/or compounds can be used against many diseases, including microbial and viral infections. Moreover, some algae species can also improve immunity and suppress human viral activity. Therefore, they may be recommended for use as a preventive remedy against COVID-19. Considering the above critiques and unique attributes, herein, we aimed to systematically assess algae-derived, biologically active molecules that could be used against this disease by looking at their natural sources, mechanisms of action, and prior pharmacological uses. This review also serves as a starting point for this research area to accelerate the establishment of anti-SARS-CoV-2 bioproducts.

scholarly journals LC-MS Phytochemical Screening, In Vitro Antioxidant, Antimicrobial and Anticancer Activity of Microalgae Nannochloropsis oculata Extract

Separations ◽  
2020 ◽  
Vol 7 (4) ◽  
pp. 54
Author(s):  
Adil Farooq Wali ◽  
Yusra Al Dhaheri ◽  
Jayachithra Ramakrishna Pillai ◽  
Ahlam Mushtaq ◽  
Padma G. M. Rao ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Morphological Changes ◽  
Radical Scavenging ◽  
In Vitro Models ◽  
Nannochloropsis Oculata ◽  
Bioactive Molecules ◽  
Dependent Manner ◽  
Minimum Fungicidal Concentration ◽  
Antibacterial And Antifungal

Nowadays, marine microalgae are recognized to be a considerably novel and rich origin of bioactive moieties utilized in the sectors of nutraceuticals and pharmaceuticals. In the present study, Nannochloropsis oculata extract (AME) was associated with a wide variety of pharmacological studies such as in vitro antioxidant, antibacterial, and antifungal and anticancer activity (MDA-MB-231) in cancer cells through in vitro models. In the study, the chemical composition and structure of the bioactive compounds found in the AME extract were studied using the LC-MS technique. The results of the anticancer activity showed a decrease in the percentage of cell viability of the MDA-MB-231 cells in a concentration- and time-dependent manner (400 μg/mL at 24 h, 300 μg/mL at 48 h, and 200 μg/mL at 72 h). We have also observed morphological changes in the cells that could be associated with treatment with AME extract. Our observation of the AME extract-treated MDA-MB231 cells under light microscopy showed that when the concentration increased, the number of cells began to decrease. As far as LC-MS analysis is concerned, it showed the presence of the bioactive molecules was terpenoids along with carotenoids, polyphenolic and fatty acids. The result revealed that the AME extract exhibited noteworthy in vitro free radical scavenging potential, with an IC50 value of 52.10 ± 0.85 µg/L in DPPH assay, 122.84 ± 2.32 µg/mL in H2O2 assay and, 96.95 ± 1.68 µg/mL in ABTS assay. The activity was found to be highly significant against bacteria (Gram-positive and negative) and moderately significant against fungal strain with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC)/minimum fungicidal concentration (MFC) values between 15.63 and 500 µg/mL.

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