scholarly journals Brevinin-1GHd: a novel Hylarana guentheri skin secretion-derived Brevinin-1 type peptide with antimicrobial and anticancer therapeutic potential

2020 ◽  
Vol 40 (5) ◽  
Author(s):  
Yangyang Jiang ◽  
Yue Wu ◽  
Tao Wang ◽  
Xiaoling Chen ◽  
Mei Zhou ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Human Cancer ◽  
Wide Spectrum ◽  
Antimicrobial Properties ◽  
Skin Secretion ◽  
Anticancer Activities ◽  
Peptide Analog ◽  
Wide Range ◽  
Low Cytotoxicity ◽  
Short Time

Abstract Host-defense antimicrobial peptides (AMPs) from amphibians are usually considered as one of the most promising next-generation antibiotics because of their excellent antimicrobial properties and low cytotoxicity. In the present study, one novel Brevinin-1 type peptide, Brevinin-1GHd, was isolated and characterized from the skin secretion of the frog, Hylarana guentheri. Brevinin-1GHd was found to possess a wide range of antimicrobial activity through penetrating the bacterial membrane within a short time while showing low hemolysis at bactericidal concentrations, even against the resistant strains. It also inhibited and eradicated biofilms that are thought to be closely related to the rise in resistance. Meanwhile, Brevinin-1GHd exhibited wide-spectrum anti-proliferation activity toward human cancer lines. Taken together, these results indicate that Brevinin-1GHd with its excellent antimicrobial and anticancer activities is a promising candidate for a novel antibiotic agent, and study of its structure–activity relationships also provided a rational template for further research and peptide analog design.

scholarly journals Redox Modulation at Work: Natural Phytoprotective Polysulfanes From Alliums Based on Redox-Active Sulfur

2018 ◽  
Vol 4 (5) ◽  
pp. 397-407 ◽  
Author(s):  
Awais Anwar ◽  
Emma Gould ◽  
Ryan Tinson ◽  
Javaid Iqbal ◽  
Chris Hamilton
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Therapeutic Potential ◽  
Antimicrobial Properties ◽  
Molecular Targets ◽  
Cancer Cell Lines ◽  
Special Focus ◽  
Anticancer Activities ◽  
Comprehensive Overview ◽  
Anticancer Properties

Abstract Purpose of review This article provides a brief overview of natural phytoprotective products of allium with a special focus on the therapeutic potential of diallyl polysulfanes from garlic, their molecular targets and their fate in the living organisms. A comprehensive overview of antimicrobial and anticancer properties of published literature is presented for the reader to understand the effective concentrations of polysulfanes and their sensitivity towards different human pathogenic microbes, fungi, and cancer cell lines. Recent findings The article finds polysulfanes potentials as new generation novel antibiotics and chemo preventive agent. The effective dose rates of polysulfanes for antimicrobial properties are in the range of 0.5–40 mg/L and for anticancer 20–100 μM. The molecular targets for these redox modulators are mainly cellular thiols as well as inhibition and/or activation of certain cellular proteins in cancer cell lines. Summary Antimicrobial and anticancer activities of polysulfanes published in the literature indicate that with further development, they could be promising candidates for cancer prevention due to their selectivity towards abnormal cells.

scholarly journals Modification Strategy of D-leucine Residue Addition on a Novel Peptide from Odorrana schmackeri, with Enhanced Bioactivity and In Vivo Efficacy

Toxins ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 611
Author(s):  
Aifang Yao ◽  
Yingxue Ma ◽  
Xiaoling Chen ◽  
Mei Zhou ◽  
Xinping Xi ◽  
...  
Keyword(s):  
Methicillin Resistant Staphylococcus Aureus ◽  
Therapeutic Potential ◽  
Wild Type ◽  
Anticancer Activities ◽  
Gram Positive Bacteria ◽  
Leucine Residue ◽  
Low Cytotoxicity ◽  
High Cytotoxicity

Brevinins are a well-characterised, frog-skin-derived, antimicrobial peptide (AMP) family, but their applications are limited by high cytotoxicity. In this study, a wild-type des-Leu2 brevinin peptide, named brevinin-1OS (B1OS), was identified from Odorrana schmackeri. To explore the significant role of the leucine residue at the second position, two variants, B1OS-L and B1OS-D-L, were designed by adding L-leucine and D-leucine residues at this site, respectively. The antibacterial and anticancer activities of B1OS-L and B1OS-D-L were around ten times stronger than the parent peptide. The activity of B1OS against the growth of Gram-positive bacteria was markedly enhanced after modification. Moreover, the leucine-modified products exerted in vivo therapeutic potential in an methicillin-resistant Staphylococcus aureus (MRSA)-infected waxworm model. Notably, the single substitution of D-leucine significantly increased the killing speed on lung cancer cells, where no viable H838 cells survived after 2 h of treatment with B1OS-D-L at 10 μM with low cytotoxicity on normal cells. Overall, our study suggested that the conserved leucine residue at the second position from the N-terminus is vital for optimising the dual antibacterial and anticancer activities of B1OS and proposed B1OS-D-L as an appealing therapeutic candidate for development.

scholarly journals UV Curable Coatings Based on Urethane Acrylates Containing Eugenol and Evaluation of Their Antimicrobial Activity

Coatings ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 1556
Author(s):  
Paulina Bednarczyk ◽  
Agnieszka Wróblewska ◽  
Agata Markowska-Szczupak ◽  
Paula Ossowicz-Rupniewska ◽  
Małgorzata Nowak ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Protective Coatings ◽  
Antimicrobial Properties ◽  
Uv Curing ◽  
Industrial Applications ◽  
High Reactivity ◽  
Uv Curable ◽  
Gram Positive Bacteria ◽  
Wide Range ◽  
Short Time

This work presents studies on the obtaining of UV-curable coatings with antimicrobial activity. Urethane acrylates (UAs) have excellent physicochemical properties including high reactivity in systems with radical photoinitiators in the presence of UV radiation and good balance between hardness and flexibility in the formed coatings. At the same time, eugenol is well known as the compound hindering the growth of various microorganisms. Hence, the materials obtained by the modification of UA resins with eugenol can be used to protect various surfaces, especially against microorganisms. This study aimed to examine the influence of the amount of eugenol on the chemical, physical, thermal, and mechanical properties of the obtained UA coatings and find the conditions at which the optimal properties for industrial applications such coatings can be achieved. These materials were successfully obtained. Taking into account that eugenol is a very cheap reactant, and it can be obtained from natural sources by the simple distillation method, the proposed method combined the good points of obtaining protective coatings by UV curing with the utilization of vegetable, renewable reactants (biomass), such as components giving special properties to these materials, in this case, antimicrobial properties. In this study, photoreactive coatings with antimicrobial properties for the following microorganisms: fungi (C. albicans), Gram-positive bacteria (S. epidermidis) as well as Gram-negative bacteria (E. coli), were obtained. The obtained coatings were cured over a short time. They were colorless and characterized by a wide range of properties and applications.

scholarly journals Cell Culture Systems for Assessing Toxicity and Chemotherapeutic Potential of Phytochemical Antioxidants

2021 ◽  
Author(s):  
Peace C. Asuzu ◽  
Nicholas Trompeter ◽  
Samuel A. Besong ◽  
Carlton R. Cooper ◽  
Alberta N.A. Aryee
Keyword(s):  
Cell Culture ◽  
Phenolic Compounds ◽  
Therapeutic Potential ◽  
Human Cancer ◽  
Antioxidant Properties ◽  
Chemotherapeutic Agents ◽  
Culture Systems ◽  
Cell Culture Systems ◽  
Wide Range

This review article seeks to provide relevant information about the applicability of cell-based assays in assessing cytotoxicity of phytochemicals in light of several traditional methods available. Phenolic compounds and other phytochemicals are significant resources for drug discovery and development, thus underlining the enormous potentials of plant-derived natural products for the prevention and management of oxidative stress associated with cancer and other diseases. These effects have been linked to the content of phytochemicals such as phenolic compounds and their antioxidant properties. The abundance and complexity of these bio-constituents highlight the need for well-defined methods for the in vitro characterization and quantification of extracts and/or preparations that can translate to in vivo effects. Cell culture systems provide a useful model for basic research and a wide range of clinical in vitro studies and physiological processes as well as assessing the toxicity and therapeutic potential of compounds including plant extracts with potential medicinal benefits. Their use in cancer research provide a useful insight into possible therapeutic properties of phytochemicals at the cellular level. This approach has been instrumental in the initial stages of developing chemotherapeutic agents where human cancer cell lines are used as experimental models. These models have continued to contribute to elucidating specific requirements for certain biochemical events associated with proliferation, metabolism, loss of cell viability/apoptosis. Cell culture systems remain a promising tool in natural product development.

scholarly journals Antimicrobial Activity of Endophytic Fungi Isolated from Eryngium foetidum, an Ethnomedicinal Plant of Assam

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Rajreepa Talukdar ◽  
Kumananda Tayung
Keyword(s):  
Antimicrobial Activity ◽  
Endophytic Fungi ◽  
Wide Spectrum ◽  
Fungal Endophytes ◽  
Antimicrobial Properties ◽  
Malt Extract ◽  
Alternative Source ◽  
Wide Range ◽  
Test Organisms ◽  
Leaf Tissues

Eyngium foetidum L. is a medicinal plant widely used by ethnic tribal communities of Assam as an alternative source of medicine for the treatment of various diseases. The present investigation was undertaken with an aim to isolate, identify and assess the antimicrobial activity of endophytic fungi associated with the healthy leaf tissues of E. foetidum. The endophytic fungi were isolated three different media, namely, Potato Dextrose Agar (PDA), Malt Extract Agar (MEA) and Water Agar (WA) media and from three different sites. Altogether, 84 endophytic fungal isolates were isolated from 150 segments of leaf tissues. Dominant endophytes were found to be fungi belonging to the genus Colletotrichum, followed by non-sporulating members grouped under mycelia sterilia. Other fungal genera that were isolated as endophytes were Scopulariopsis, Cladosporium, Stemphylium, Penicilllium and Alternaria. The endophytic fungi thus isolated were studied for antimicrobial activity against some clinically significant human pathogenic test organisms. Ethyl acetate extracts of all endophytes exhibited antimicrobial activity by inhibiting at least one out of all the test pathogens. Amongst the isolated fungi, extracts obtained from three endophytes showed wide-spectrum activity against all the test organisms. The fungal endophytes were identified as Scopulariopsis sp., Penicillium sp. and a sterile isolate morphotype strain EF6. The study indicated that E. foetidum harbours a wide range of endophytes with antimicrobial properties and further detailed investigation of the compound present in them would lead to their potential therapeutic applications as a new source of medicine.

scholarly journals Evaluation of antimicrobial and anticancer activities of three peptides identified from the skin secretion of Hylarana latouchii

2021 ◽  
Author(s):  
Yan Lin ◽  
Tianxing Lin ◽  
Ningna Cheng ◽  
Shuting Wu ◽  
Jiancai Huang ◽  
...  
Keyword(s):  
Malignant Tumors ◽  
Human Cancer ◽  
Multidrug Resistant ◽  
Biologically Active ◽  
Helical Conformation ◽  
Resistant Bacteria ◽  
Skin Secretion ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Close Relationship

Abstract The skins of frogs of the family Ranidae are particularly rich sources of biologically active peptides, among which antimicrobial peptides (AMPs) constitute the major portion. Some of these have attracted the interest of researchers because they possess both antimicrobial and anticancer activities. In this study, with ‘shotgun’ cloning and MS/MS fragmentation, three AMPs, homologues of family brevinin-1 (brevinin-1HL), and temporin (temporin-HLa and temporin-HLb), were discovered from the skin secretion of the broad-folded frog, Hylarana latouchii. They exhibited various degrees of antimicrobial and antibiofilm activities against test microorganisms and hemolysis on horse erythrocytes. It was found that they could induce bacteria death through disrupting cell membranes and binding to bacterial DNA. In addition, they also showed different potencies towards human cancer cell lines. The secondary structure and physicochemical properties of each peptide were investigated to preliminarily reveal their structure–activity relationships. Circular dichroism spectrometry showed that they all adopted a canonical α-helical conformation in membrane-mimetic solvents. Notably, the prepropeptide of brevinin-1HL from H. latouchii was highly identical to that of brevinin-1GHd from Hylarana guentheri, indicating a close relationship between these two species. Accordingly, this study provides candidates for the design of novel anti-infective and antineoplastic agents to fight multidrug-resistant bacteria and malignant tumors and also offers additional clues for the taxonomy of ranid frogs.

scholarly journals Flavonoids as Phytoestrogenic Components of Hops and Beer

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4201 ◽  
Author(s):  
Tomasz Tronina ◽  
Jarosław Popłoński ◽  
Agnieszka Bartmańska
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Hormone Replacement ◽  
Antimicrobial Properties ◽  
Prenylated Flavonoids ◽  
Humulus Lupulus L ◽  
Estrogen Activity ◽  
Potential Applications ◽  
Beer Production

The value of hops (Humulus lupulus L.) in beer production has been undisputed for centuries. Hops is rich in humulones and lupulones which gives the characteristic aroma and bitter taste, and preserves this golden drink against growing bacteria and molds. Besides α- and β-acids, the lupulin glands of hop cones excrete prenylated flavonoids, which exhibit a broad spectrum of biological activities and therefore has therapeutic potential in humans. Recently, interest in hops was raised due to hop prenylated flavanones which show extraordinary estrogen activities. The strongest known phytoestrogen so far is 8-prenylnaringenin (8-PN), which along with 6-prenylanaringenin (6-PN), 6,8-diprenylnaringenin (6,8-DPN) and 8-geranylnaringenin (8-GN) are fundamental for the potent estrogen activity of hops. This review provides insight into the unusual hop phytoestrogens and shows numerous health benefits associated with their wide spectrum of biological activities including estrogenic, anticancer, neuropreventive, antinflamatory, and antimicrobial properties, which were intensively studied, and potential applications of these compounds such as, as an alternative to hormone replacement therapy (HRT).

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

Isoform-Selective PI3K Inhibitors for Various Diseases

2020 ◽  
Vol 20 (12) ◽  
pp. 1074-1092 ◽  
Author(s):  
Rammohan R.Y. Bheemanaboina
Keyword(s):  
Intracellular Signaling ◽  
Kinase Inhibitors ◽  
Therapeutic Potential ◽  
Type I ◽  
Selective Inhibitors ◽  
Pi3k Inhibitors ◽  
Wide Range ◽  
Lipid Kinases ◽  
Isoform Selectivity

Phosphoinositide 3-kinases (PI3Ks) are a family of ubiquitously distributed lipid kinases that control a wide variety of intracellular signaling pathways. Over the years, PI3K has emerged as an attractive target for the development of novel pharmaceuticals to treat cancer and various other diseases. In the last five years, four of the PI3K inhibitors viz. Idelalisib, Copanlisib, Duvelisib, and Alpelisib were approved by the FDA for the treatment of different types of cancer and several other PI3K inhibitors are currently under active clinical development. So far clinical candidates are non-selective kinase inhibitors with various off-target liabilities due to cross-reactivities. Hence, there is a need for the discovery of isoform-selective inhibitors with improved efficacy and fewer side-effects. The development of isoform-selective inhibitors is essential to reveal the unique functions of each isoform and its corresponding therapeutic potential. Although the clinical effect and relative benefit of pan and isoformselective inhibition will ultimately be determined, with the development of drug resistance and the demand for next-generation inhibitors, it will continue to be of great significance to understand the potential mechanism of isoform-selectivity. Because of the important role of type I PI3K family members in various pathophysiological processes, isoform-selective PI3K inhibitors may ultimately have considerable efficacy in a wide range of human diseases. This review summarizes the progress of isoformselective PI3K inhibitors in preclinical and early clinical studies for anticancer and other various diseases.

Phytochemical, Pharmacological Activities and Ayurvedic Significances of Magical Plant Mimosa pudica Linn

2020 ◽  
Vol 17 ◽  
Author(s):  
Vijay Kumar
Keyword(s):  
Therapeutic Potential ◽  
Wide Spectrum ◽  
Chemical Constituents ◽  
Future Research ◽  
Mimosa Pudica ◽  
Pharmacological Activities ◽  
Medicinal Uses ◽  
Traditional Medicines ◽  
Crude Extracts ◽  
Anti Cancer

: Mimosa pudica Linn is an integrated part of Traditional Medicines Systems of India, China, Africa, Korea and America. It has been used from centuries in traditional medicines to cure different diseases like fever, diabetes, constipation, jaundice, ulcers, biliousness, and dyspepsia. It is an important ingredient of wide class of herbal formulations. To assess the scientific evidence for therapeutic potential of Mimosa pudica Linn and to identify the gaps for future research. The available information on the ethno-medicinal uses, phytochemistry, pharmacology and toxicology of Mimosa pudica Linn was collected via a library and electronic searches in Sci-Finder, Pub-Med, Science Direct, Google Scholar for the period, 1990 to 2020. In traditional medicinal systems, variety of ethno-medicinal applications of Mimosa pudica Linn has been noticed. Phytochemical investigation has resulted in identification of 40 well known chemical constituents, among which alkaloids, phenols and flavionoids are the predominant groups. The crude extracts and isolates have exhibited a wide spectrum of in vitro and in vivo pharmacological activities including anti-cancer, anti-inflammation, osteoporosis, neurological disorders, hypertension etc.. To quantify the Mimosa pudica Linn and its formulations, analytical techniques like HPLC and HPTLC has shown dominancy with good range of recovery and detection limit. Mimosa pudica Linn is the well-known herb since an ancient time. The pharmacological results supported some of the applications of Mimosa pudica Linn in traditional medicine systems. Perhaps, the predominance of alkaloids, phenols and flavionoids are responsible for the pharmacological activities the crude extracts and isolates of Mimosa pudica Linn. Further, there is need to isolate and evaluate the active chemical constituents of Mimosa pudica Linn having significant medicinal values. In future, it is important to study the exact mechanism associated with the phytochemicals of Mimosa pudica Linn especially on anti-cancer activities. Notably, toxicity studies on Mimosa pudica Linn are limited which are to be explored in future for the safe application of Mimosa pudica Linn and its formulations.

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