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).

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.

Clinical Applications of Antimicrobial Peptides (AMPs): Where do we Stand Now?

2020 ◽  
Vol 27 (2) ◽  
pp. 120-134 ◽  
Author(s):  
Mithoor Divyashree ◽  
Madhu K. Mani ◽  
Dhanasekhar Reddy ◽  
Ranjith Kumavath ◽  
Preetam Ghosh ◽  
...  
Keyword(s):  
Antimicrobial Peptides ◽  
Molecular Mechanisms ◽  
Metabolic Diseases ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Noncommunicable Diseases ◽  
Multi Drug Resistance ◽  
Food Preservatives ◽  
Pharmaceutical Industries

: In this era of multi-drug resistance (MDR), antimicrobial peptides (AMPs) are one of the most promising classes of potential drug candidates to combat communicable as well as noncommunicable diseases such as cancers and diabetes. AMPs show a wide spectrum of biological activities which include antiviral, antifungal, anti-mitogenic, anticancer, and anti-inflammatory properties. Apart from these prospective therapeutic potentials, the AMPs can act as food preservatives and immune modulators. Therefore, AMPs have the potential to replace conventional drugs and may gain a significant global drug market share. Although several AMPs have shown therapeutic potential in vitro or in vivo, in most cases they have failed the clinical trial owing to various issues. In this review, we discuss in brief (i) molecular mechanisms of AMPs in various diseases, (ii) importance of AMPs in pharmaceutical industries, (iii) the challenges in using AMPs as therapeutics and how to overcome, (iv) available AMP therapeutics in market, and (v) AMPs under clinical trials. Here, we specifically focus on the therapeutic AMPs in the areas of dermatology, surgery, oncology and metabolic diseases.

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

In-silico screening of 2,3-diphenylquinozaline derivatives as C-met kinase inhibitors

2017 ◽  
Vol 4 (3) ◽  
pp. 41-45
Author(s):  
Nehla Yahcoob ◽  
Baskar Lakshmanan ◽  
Jyothi Achuthanandhan ◽  
Vijayakumar Balakrishnan
Keyword(s):  
Binding Energy ◽  
Tyrosine Kinase ◽  
In Silico ◽  
Kinase Inhibitors ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Binding Interaction ◽  
In Silico Screening ◽  
Sar Study

Quinoxaline, an important class of heterocylic compounds drawn greater attention due to their wide spectrum of biological activities. They are considered as an important chemical scaffold for anticancer drug design  due to their potential inhibitory activity against  C-met tyrosine kinase. C-met kinase inhibitors  are a class of small molecules that having therapeutic potential in  the treatment of various types of cancers. The present study aims to focus on the chemistry of quinoxaline derivatives, their potential activities against C-met tyrosine kinase, and in-silico screening of designed compounds. A series of twelve compounds were designed and docked against C-met tyrosine kinase for their binding energy. All compounds were found to be interacting  well with the protein. Compound NQ1 was found to have good binding energy showing an estimated Ki value of  1.1μm.  SAR  study indicated the presence of an electron withdrawing substitution on  benzilidine  phenyl ring of quinoxaline greatly improves its binding interaction with the protein.

New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation

2018 ◽  
Vol 18 (1) ◽  
pp. 75-87 ◽  
Author(s):  
Michelyne Haroun ◽  
Christophe Tratrat ◽  
Katerina Kositzi ◽  
Evangelia Tsolaki ◽  
Anthi Petrou ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Antimicrobial Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Synthesis Methods ◽  
Design Synthesis ◽  
Benzothiazole Derivatives

Background: Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. Objective: The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. Methods: The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. Results: The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. Conclusion: The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.

scholarly journals Identification of Mutations Conferring Tryptanthrin Resistance to Mycobacterium smegmatis

Antibiotics ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 6
Author(s):  
Svetlana G. Frolova ◽  
Ksenia M. Klimina ◽  
Ravinder Kumar ◽  
Aleksey A. Vatlin ◽  
Deepak B. Salunke ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Transcriptional Regulator ◽  
Test System ◽  
Comparative Genomic ◽  
Promising Alternative ◽  
Main Challenge

Tuberculosis (TB), caused by Mycobacterium tuberculosis, is a global burden, responsible for over 1 million deaths annually. The emergence and spread of drug-resistant M. tuberculosis strains (MDR-, XDR- and TDR-TB) is the main challenge in global TB-control, requiring the development of novel drugs acting on new biotargets, thus able to overcome the drug-resistance. Tryptanthrin is a natural alkaloid, with great therapeutic potential due to its simple way of synthesis and wide spectrum of biological activities including high bactericidal activity on both drug-susceptible and MDR M. tuberculosis strains. InhA was suggested as the target of tryptanthrins by in silico modeling, making it a promising alternative to isoniazid, able to overcome drug resistance provided by katG mutations. However, neither the mechanism of action of tryptanthrin nor the mechanism of resistance to tryptanthrins was ever confirmed in vitro. We show that the MmpS5-MmpL5 efflux system is able to provide resistance to tryptanthrins using an in-house test-system. Comparative genomic analysis of spontaneous tryptanthrin-resistant M. smegmatis mutants showed that mutations in MSMEG_1963 (EmbR transcriptional regulator) lead to a high-level resistance, while those in MSMEG_5597 (TetR transcriptional regulator) to a low-level one. Mutations in an MFS transporter gene (MSMEG_4427) were also observed, which might be involved in providing a basal level of tryptanthrins-resistance.

scholarly journals Pharmaceutical and Nutraceutical Potential Applications of Sargassum fulvellum

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Jian Liu ◽  
Sibusiso Luthuli ◽  
Qifang Wu ◽  
Mingjiang Wu ◽  
Jong-il Choi ◽  
...  
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
Brown Seaweed ◽  
Industrial Applications ◽  
Anticancer Effects ◽  
Sargassum Fulvellum ◽  
Potential Applications ◽  
Potential Component ◽  
Anti Inflammatory ◽  
Urinary Problems

Sargassum fulvellum is a brown seaweed of the Sargassaceae family which has been demonstrated to exhibit antipyretic, analgesic, antiedema, antimicrobial, antioxidant, antitumor, neuroprotective, anticoagulative, anti-inflammatory, and hepatoprotective activities. It has been widely used as a food additive and as a medicine in oriental medicine to treat lumps, dropsy, swelling, testicular pains, and urinary problems. S. fulvellum has been identified as a potential producer of a wide spectrum of natural compounds such as carotenoids, fucoidans, and phlorotannins, showing different biological activities in various industrial applications including pharmaceutical, nutraceutical, cosmeceutical, and functional food. However, the promising health effects associated with the extracts and compounds isolated from S. fulvellum have not been reviewed to date. The present review thus focuses on the biological activity of S. fulvellum as reported by previous publications, which include antioxidant, anticoagulant, anti-inflammatory, neuroprotective, immunomodulatory, antidiabetic, and anticancer effects. Thus, this review might serve to increase the utilization of this invaluable natural source as a potential component in pharmaceutical and nutraceutical applications.

scholarly journals FLAVONOLS HPLC ANALYSIS, IN VITRO BIOLOGICAL ACTIVITIES IN SELECTED HUMULUS LUPULUS L. GENOTYPES

2013 ◽  
Vol 12 (2) ◽  
pp. 129-140
Author(s):  
Maria Maliarova ◽  
Tibor Maliar ◽  
Jana Girmanova ◽  
Jozef Lehotay ◽  
Jan Kraic
Keyword(s):  
Biological Activities ◽  
Humulus Lupulus ◽  
Point Of View ◽  
Raw Material ◽  
Humulus Lupulus L ◽  
Bitter Acids ◽  
High Level ◽  
Beer Production ◽  
Structural Classes

Abstract The Humulus lupulus L. is well known as necessary raw material for beer production. The main structural classes of chemical compounds identified from hop cones include terpenes, bitter acids, prenylated chalcones, and flavonol glycosides. They were subjects of presented work. The content of quercetin was found in the range 490 - 1092 μg/g and that of kaempferol from 218 to 568 μg/g of the dry hop cones. The content of isorhamnetin was very low in all varieties. From biological activities in vitro point of view, relative high level of inhibition activity was observed for six hop genotypes - Zlatan, Lučan, and the Oswald's clones 31, 70, 71, 72, 114 on both enzymes thrombin and urokinase, but without correlation to analyzed flavonols content. In spite of this, antioxidant activity, measured by both the BCLM and HPE methods, was found high and seem to be in correlation with content of analyzed flavonols. Particularly the Oswald's clone 114 expressed very potent biological activities. In general, obtained results indicate that hop cones are valuable material also for other application others than beer production.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

Current Advances in the Biological Activity of Polysaccharides in Dendrobium with Intriguing Therapeutic Potential

2018 ◽  
Vol 25 (14) ◽  
pp. 1663-1681 ◽  
Author(s):  
Chun-Ting Lee ◽  
Heng-Chun Kuo ◽  
Yung-Hsiang Chen ◽  
Ming-Yen Tsai
Keyword(s):  
Biological Activity ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Biological Effects ◽  
Herbal Medicines ◽  
Research Field ◽  
Protective Effects ◽  
Pharmacological Effects ◽  
The Family ◽  
Anti Tumor Activity

The polysaccharides in many plants are attracting worldwide attention because of their biological activities and medical properties, such as anti-viral, anti-oxidative, antichronic inflammation, anti-hypertensive, immunomodulation, and neuron-protective effects, as well as anti-tumor activity. Denodrobium species, a genus of the family orchidaceae, have been used as herbal medicines for hundreds of years in China due to their pharmacological effects. These effects include nourishing the Yin, supplementing the stomach, increasing body fluids, and clearing heat. Recently, numerous researchers have investigated possible active compounds in Denodrobium species, such as lectins, phenanthrenes, alkaloids, trigonopol A, and polysaccharides. Unlike those of other plants, the biological effects of polysaccharides in Dendrobium are a novel research field. In this review, we focus on these novel findings to give readers an overall picture of the intriguing therapeutic potential of polysaccharides in Dendrobium, especially those of the four commonly-used Denodrobium species: D. huoshanense, D. offininale, D. nobile, and D. chrysotoxum.

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