scholarly journals Therapeutic Potential of Glycosyl Flavonoids as Anti-Coronaviral Agents

2021 ◽  
Vol 14 (6) ◽  
pp. 546
Author(s):  
Patrícia I. C. Godinho ◽  
Raquel G. Soengas ◽  
Vera L. M. Silva
Keyword(s):  
Potential Role ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Antiviral Agent ◽  
Research Area ◽  
Therapeutic Agents ◽  
Cellular Functions ◽  
Wide Range ◽  
Low Toxicity ◽  
Socio Economic Impact

The COVID-19 pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has spread all over the world, creating a devastating socio-economic impact. Even though protective vaccines are starting to be administered, an effective antiviral agent for the prevention and treatment of COVID-19 is not available yet. Moreover, since new and deadly CoVs can emerge at any time with the potential of becoming pandemics, the development of therapeutic agents against potentially deadly CoVs is a research area of much current interest. In the search for anti-coronaviral drugs, researchers soon turned their heads towards glycosylated flavonoids. Glycosyl flavonoids, widespread in the plant kingdom, have received a lot of attention due to their widely recognized antioxidant, anti-inflammatory, neuroprotective, anticarcinogenic, antidiabetic, antimicrobial, and antiviral properties together with their capacity to modulate key cellular functions. The wide range of biological activities displayed by glycosyl flavonoids, along with their low toxicity, make them ideal candidates for drug development. In this review, we examine and discuss the up-to-date developments on glycosyl flavonoids as evidence-based natural sources of antivirals against coronaviruses and their potential role in the management of COVID-19.

scholarly journals Recent Updates on the Synthesis of Bioactive Quinoxaline-Containing Sulfonamides

2021 ◽  
Vol 11 (12) ◽  
pp. 5702
Author(s):  
Ali Irfan ◽  
Sajjad Ahmad ◽  
Saddam Hussain ◽  
Fozia Batool ◽  
Haseeba Riaz ◽  
...  
Keyword(s):  
Literature Review ◽  
Biomedical Applications ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmacological Activities ◽  
Lead Compounds ◽  
Structure Activity ◽  
Wide Range ◽  
Sulfonamide Group

Quinoxaline is a privileged pharmacophore that has broad-spectrum applications in the fields of medicine, pharmacology and pharmaceutics. Similarly, the sulfonamide moiety is of considerable interest in medicinal chemistry, as it exhibits a wide range of pharmacological activities. Therefore, the therapeutic potential and biomedical applications of quinoxalines have been enhanced by incorporation of the sulfonamide group into their chemical framework. The present review surveyed the literature on the preparation, biological activities and structure-activity relationship (SAR) of quinoxaline sulfonamide derivatives due to their broad range of biomedical activities, such as diuretic, antibacterial, antifungal, neuropharmacological, antileishmanial, anti-inflammatory, anti-tumor and anticancer action. The current biological diagnostic findings in this literature review suggest that quinoxaline-linked sulfonamide hybrids are capable of being established as lead compounds; modifications on quinoxaline sulfonamide derivatives may give rise to advanced therapeutic agents against a wide variety of diseases.

scholarly journals Neuroprotective Effects, Biological Activities and Therapeutic Potential of Phytochemicals: A Comprehensive Review

2020 ◽  
pp. 1-11
Author(s):  
Xi-jun Wang ◽  
Shi Qiu ◽  
Aihua Zhang ◽  
Jian-hua Miao ◽  
Hui Sun ◽  
...  
Keyword(s):  
Natural Products ◽  
Neurological Disorders ◽  
Chemical Biology ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Neuroprotective Effects ◽  
Alternative Medicines ◽  
Pharmacological Targets ◽  
The World

The incidence of neurological disorders is growing in the world together with an increased lifespan. Nowadays, there are still no effective treatments for neurodegenerative pathology, which make necessary to search for new therapeutic agents. Natural products, most of them used in phytochemicals from herbal medicine, are considered promising alternatives for the treatment of neurodegenerative diseases. Numerous herbs have been applied to neurodegenerative disease treatments as complementary and alternative medicines. In the 21st century, omics-coupled functional pharmacology was developed for neurodegenerative drug discovery from natural products. In this article, we firstly provide the latest understanding of neurological disorders on risk factors, category, diagnosis and treatment, and then specially present an overview of natural products in neuroprotective effects research from chemical biology to pharmacological targets, and also discuss the natural products application and future challenge.

scholarly journals Molecular Targets Involved in the Neuroprotection Mediated by Terpenoids

Planta Medica ◽  
2019 ◽  
Vol 85 (17) ◽  
pp. 1304-1315 ◽  
Author(s):  
Laura González-Cofrade ◽  
Beatriz de las Heras ◽  
Luis Apaza Ticona ◽  
Olga M. Palomino
Keyword(s):  
Therapeutic Potential ◽  
Cell Damage ◽  
Biological Activities ◽  
Neuronal Cell ◽  
Molecular Targets ◽  
Research Activity ◽  
Neuroprotective Effects ◽  
Therapeutic Value ◽  
Wide Range ◽  
Drug Leads

AbstractNatural products and their derivatives represent the most consistently successful source of drug leads. Terpenoids, a structurally diverse group, are secondary metabolites widely distributed in nature, endowed with a wide range of biological activities such as antibacterial, anti-inflammatory, antitumoral, or neuroprotective effects, which consolidate their therapeutic value. During the last decades, and taking into consideration the prevalence of aging-related diseases, research activity into the neuroprotective effects of these types of compounds has increased enormously. Several signaling pathways involved in neuroprotection are targets of their mechanism of action and mediate their pleiotropic protective activity in neuronal cell damage. In the present review, molecular basis of the neuroprotection exerted by terpenoids is presented, focusing on preclinical evidence of the therapeutic potential of diterpenoids and triterpenoids on neurodegenerative disorders. By acting on diverse mechanisms simultaneously, terpenoids have been emphasized as promising multitarget agents.

scholarly journals Research Progress on the Antitumor Effect of Polysaccharides from Fungus Used in Traditional Chinese Medicine

2021 ◽  
Vol 5 (5) ◽  
pp. 7-10
Author(s):  
Ru Xiang ◽  
Bing Xu
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Antitumor Effect ◽  
Biological Activities ◽  
Research Progress ◽  
Cancer Breast ◽  
Wide Range ◽  
Low Toxicity ◽  
Fungal Polysaccharides ◽  
Cancer Côlon

Cancer is a serious threat to human health. Fungal polysaccharide is a polar biological macromolecule with low toxicity. It has a wide range of biological activities, including immune regulation, antitumor activity, and antiviral activity. In recent years, the research results have shown that polysaccharides from fungus in traditional Chinese medicine have excellent antitumor effect in liver cancer, gastric cancer, breast cancer, colon cancer, esophageal cancer, and lung cancer. Therefore, the research and development of fungal polysaccharides are of great significance for the development of antitumor drugs in the future.

scholarly journals A Review on Therapeutic Potential of Protease Inhibitors from Medicinal Plants

2019 ◽  
pp. 1-11
Author(s):  
R. N. N. Gamage ◽  
K. D. K. P. Kumari
Keyword(s):  
Protease Inhibitor ◽  
Protease Inhibitors ◽  
Blood Clotting ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Geographical Location ◽  
Therapeutic Agents ◽  
Human Diseases ◽  
Plant Protease ◽  
Protease Specificity

Most of the currently available therapeutic agents, particularly for cardiovascular disorders and cancers are very expensive and induce some serious side effects. Some of these drugs have also become less effective due to the emergence of antibiotic resistance. There is a necessity and great demand for the development of novel efficacious plant-based agents that are of pharmacologically effective. In this connection, this review focuses on therapeutic potential of plant protease inhibitors. Protease inhibitors are of a particular concern at present due to their potent ability to inhibit protease enzymes that are involved in pathogenesis of various human diseases. In addition to their function as protein-degrading enzymes, protease inhibitors are now well-known for their capability to involve in many biological activities as signaling molecules. Plant protease inhibitors are also engaged in several physiological and pathological processes, such as blood clotting, inflammation, immune regulation, apoptosis and carcinogenesis. Therefore, isolation of plant protease inhibitors and evaluation of their therapeutic capacity against chronic human diseases have become a major research interest. Nevertheless, protease inhibitor content and protease specificity vary significantly even in the same plant species depending on the geographical location and environmental factors. Consequently, it is important to identify potent therapeutic potential of each plant protease inhibitor on human health individually.

scholarly journals The Phylum Bryozoa as a Promising Source of Anticancer Drugs

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 477 ◽  
Author(s):  
Figuerola ◽  
Avila
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Anticancer Properties ◽  
Antitumor Compounds ◽  
Wide Range ◽  
Drug Synthesis ◽  
Low Toxicity ◽  
Promising Source

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, which are filter-feeding, aquatic invertebrates often characterized by a calcified skeleton, are an excellent source of pharmacologically interesting compounds including well-known chemical classes such as alkaloids and polyketides. This review covers the literature for secondary metabolites isolated from marine cheilostome and ctenostome bryozoans that have shown potential as cancer drugs. Moreover, we highlight examples such as bryostatins, the most known class of marine-derived compounds from this animal phylum, which are advancing through anticancer clinical trials due to their low toxicity and antineoplastic activity. The bryozoan antitumor compounds discovered until now show a wide range of chemical diversity and biological activities. Therefore, more research focusing on the isolation of secondary metabolites with potential anticancer properties from bryozoans and other overlooked taxa covering wider geographic areas is needed for an efficient bioprospecting of natural products.

A Panoramic Review of Benzimidazole Derivatives and Their Potential Biological Activity

2022 ◽  
Vol 22 ◽  
Author(s):  
Hiram Hernández-López ◽  
Christian Jairo Tejada-Rodríguez ◽  
Socorro Leyva-Ramos
Keyword(s):  
Biological Activity ◽  
Hydrophobic Interactions ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Benzimidazole Derivatives ◽  
Drug Candidate ◽  
Hydrogen Bond Donor ◽  
Wide Range ◽  
Donor Acceptor ◽  
Potent Drug

Abstract: The therapeutic potential of the benzimidazole nucleus dates back to 1944, being and important heterocycle system due to its presence in a wide range of bioactive compounds such as antiviral, anticancer, antibacterial, and so on, where optimization of substituents in this class of pharmacophore has resulted in many drugs. Its extensive biological activity is due to its physicochemical properties like hydrogen bond donor-acceptor capability,  stacking interactions, coordination bonds with metals as ligands and hydrophobic interactions; properties that allow them to easily bind with a series of biomolecules, including enzymes and nucleic acids, causing a growing interest in these types of molecules. This review aims to present an overview to leading benzimidazole derivatives, as well as to show the importance of the nature and type of substituents at the N1, C2, and C5(6) positions, when they are biologically evaluated, which can lead to obtaining potent drug candidate with significant range of biological activities.

scholarly journals Revisiting the Therapeutic Potential of Bothrops jararaca Venom: Screening for Novel Activities Using Connectivity Mapping

Toxins ◽  
2018 ◽  
Vol 10 (2) ◽  
pp. 69 ◽  
Author(s):  
Carolina Nicolau ◽  
Alyson Prorock ◽  
Yongde Bao ◽  
Ana Neves-Ferreira ◽  
Richard Valente ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Rna Extraction ◽  
Breast Adenocarcinoma ◽  
South American ◽  
Snake Venoms ◽  
Bothrops Jararaca ◽  
Drug Classes ◽  
Wide Range ◽  
Activity Screening

Snake venoms are sources of molecules with proven and potential therapeutic applications. However, most activities assayed in venoms (or their components) are of hemorrhagic, hypotensive, edematogenic, neurotoxic or myotoxic natures. Thus, other relevant activities might remain unknown. Using functional genomics coupled to the connectivity map (C-map) approach, we undertook a wide range indirect search for biological activities within the venom of the South American pit viper Bothrops jararaca. For that effect, venom was incubated with human breast adenocarcinoma cell line (MCF7) followed by RNA extraction and gene expression analysis. A list of 90 differentially expressed genes was submitted to biosimilar drug discovery based on pattern recognition. Among the 100 highest-ranked positively correlated drugs, only the antihypertensive, antimicrobial (both antibiotic and antiparasitic), and antitumor classes had been previously reported for B. jararaca venom. The majority of drug classes identified were related to (1) antimicrobial activity; (2) treatment of neuropsychiatric illnesses (Parkinson’s disease, schizophrenia, depression, and epilepsy); (3) treatment of cardiovascular diseases, and (4) anti-inflammatory action. The C-map results also indicated that B. jararaca venom may have components that target G-protein-coupled receptors (muscarinic, serotonergic, histaminergic, dopaminergic, GABA, and adrenergic) and ion channels. Although validation experiments are still necessary, the C-map correlation to drugs with activities previously linked to snake venoms supports the efficacy of this strategy as a broad-spectrum approach for biological activity screening, and rekindles the snake venom-based search for new therapeutic agents.

One-pot Synthesis of Betulin Triterpenoid Quaternized Pyridine Derivatives and their Antimicrobial Activity

2019 ◽  
Vol 17 (1) ◽  
pp. 79-84 ◽  
Author(s):  
Elvira Rifovna Shakurova ◽  
Darina Alexandrovna Pozdnyakova ◽  
Elena Valeryevna Tretyakova ◽  
Lyudmila Vyacheslavovna Parfenova
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Effective Interaction ◽  
Inhibition Zone ◽  
Pyridine Derivatives ◽  
One Pot ◽  
Biological Targets ◽  
Wide Range ◽  
Low Toxicity ◽  
Antibacterial And Antifungal

Background: A wide range of biological activity, relatively low toxicity and multiple pharmacological effects of triterpenoids are major advantages of these compounds in the prevention and treatment of various diseases. They include the lupane- type triterpenoids that proved to be a promising platform for the synthesis of analogs with a wide range of biological activities, including anti-inflammatory, antitumor, antiparasitic and antiviral properties. The main disadvantage complicating the use of all known derivatives of lupane acids in medical practice is low bioavailability associated with poor solubility in biologic fluids, limiting their effective interaction with the biological targets. Objective: The objective of this study is the synthesis of new amphiphilic betulin derivatives on the base of pyridinium salts with antifungal and antibacterial activity. Methods: In this study we have developed an effective one-pot method for the preparation of new quaternized pyridine derivatives 4-6 of the betulinic series based on the reaction of the initial triterpenes 1-3 with the Tempo+Br3 - reagent in the pyridine. The synthesized and initial compounds were tested for their antimicrobial and antifungal activity. Results: The data presented in this document indicate that all synthesized compounds 4-6 exhibited high activity against both gram-positive Staphylococcus aureus bacteria and gram-negative Pseudomonas aeruginosa strains, as well as Candida albicans and Cryptococcus neoformans fungi with the >90% coverage of the inhibition zone. The best result in a series of compounds 4-6 was found for the derivative 6 at the minimum inhibitory concentration of 1 µg/ml against S. aureus bacteria, C. albicans and C. neoformans fungi at the concentration of 8 µg/ml. Conclusion: Thus, we have demonstrated the first example of the pyridine quaternization using the betulin triterpenoids as the lipophilic substrates and Tempo+Br3 - cation. The obtained quaternized pyridine analogs of betulin triterpenes showed high antibacterial and antifungal activity in comparison with the initial compounds.

scholarly journals Dendropanax Morbiferus and Other Species from the Genus Dendropanax: Therapeutic Potential of Its Traditional Uses, Phytochemistry, and Pharmacology

Antioxidants ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 962
Author(s):  
Rengasamy Balakrishnan ◽  
Duk-Yeon Cho ◽  
In Su-Kim ◽  
Dong-Kug Choi
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Safety Evaluation ◽  
Biological Properties ◽  
Comprehensive Analysis ◽  
Flowering Plant ◽  
High Concentration ◽  
Medicinal Uses ◽  
Wide Range ◽  
Bioactive Ingredients

The Dendropanax genus is a kind of flowering plant in the family of Araliaceae that encompasses approximately 91 to 95 species. Several Dendropanax species are used as traditional medicinal plants, extensively used Korea and South America and other parts of the world. Almost every part of the plant, including the leaves, bark, roots, and stems, can be used as traditional medicine for the prevention and management of a broad spectrum of health disorders. This paper sought to summarizes the ethnopharmacological benefits, biological activities, and phytochemical investigations of plants from the genus Dendropanax, and perhaps to subsequently elucidate potential new perspectives for future pharmacological research to consider. Modern scientific literature suggests that plants of the Dendropanax genus, together with active compounds isolated from it, possess a wide range of therapeutic and pharmacological applications, including antifungal, anti-complement, antioxidant, antibacterial, insect antifeedant, cytotoxic, anti-inflammatory, neuroprotective, anti-diabetic, anti-cancer, and anti-hypouricemic properties. The botanical descriptions of approximately six to 10 species are provided by different scientific web sources. However, only six species, namely, D. morbiferus, D. gonatopodus, D. dentiger, D. capillaris, D. chevalieri, and D. arboreus, were included in the present investigation to undergo phytochemical evaluation, due to the unavailability of data for the remaining species. Among these plant species, a high concentration of variable bioactive ingredients was identified. In particular, D. morbifera is a traditional medicinal plant used for the multiple treatment purposes and management of several human diseases or health conditions. Previous experimental evidence supports that the D. morbifera species could be used to treat various inflammatory disorders, diarrhea, diabetes, cancer, and some microbial infections. It has recently been reported, by our group and other researchers, that D. morbifera possesses a neuroprotective and memory-enhancing agent. A total of 259 compounds have been identified among six species, with 78 sourced from five of these species reported to be bioactive. However, there is no up-to-date information concerning the D. morbifera, its different biological properties, or its prospective benefits in the enhancement of human health. In the present study, we set out to conduct a comprehensive analysis of the botany, traditional medicinal history, and medicinal resources of species of the Dendropanax genus. In addition, we explore several phytochemical constituents identified in different species of the Dendropanax genus and their biological properties. Finally, we offer comprehensive analysis findings of the phytochemistry, medicinal uses, pharmacological actions, and a toxicity and safety evaluation of the D. morbifera species and its main bioactive ingredients for future consideration.

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