Flavones as a Privileged Scaffold in Drug Discovery: Current Developments

2019 ◽  
Vol 16 (7) ◽  
pp. 968-1001
Author(s):  
Pone K. Boniface ◽  
Ferreira I. Elizabeth
Keyword(s):  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmacological Properties ◽  
Chemical Transformations ◽  
National Library ◽  
Scientific Publications ◽  
Multifactorial Diseases ◽  
Naturally Occurring ◽  
Privileged Scaffold

Background: Flavones are one of the main subclasses of flavonoids with diverse pharmacological properties. They have been reported to possess antimalarial, antimicrobial, anti-tuberculosis, anti-allergic, antioxidant, anti-inflammatory activities, among others. Objective: The present review summarizes the recent information on the pharmacological properties of naturally occurring and synthetic flavones. Method: Scientific publications referring to natural and synthetic flavones in relation to their biological activities were hand-searched in databases such as SciFinder, PubMed (National Library of Medicine), Science Direct, Wiley, ACS, SciELO, Springer, among others. Results: As per the literature, seventy-five natural flavones were predicted as active compounds with reference to their IC50 (<20 µg/mL) in in vitro studies. Also, synthetic flavones were found active against several diseases. Conclusion: As per the literature, flavones are important sources for the potential treatment of multifactorial diseases. However, efforts toward the development of flavone-based therapeutic agents are still needed. The appearance of new catalysts and chemical transformations is expected to provide avenues for the synthesis of unexplored flavones, leading to the discovery of flavones with new properties and biological activities.

scholarly journals Hemisynthesis and Biological Evaluation of Cinnamylated, Benzylated, and Prenylated Dihydrochalcones from a Common Bio-Sourced Precursor

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Cytotoxic Potential ◽  
Naturally Occurring

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.

scholarly journals Review of phytochemistry, biological activities and therapeutic potential of Cleistochlamys kirkii

2020 ◽  
Vol 11 (4) ◽  
pp. 5596-5602
Author(s):  
Alfred Maroyi
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Central Africa ◽  
Indole Alkaloid ◽  
Pharmaceutical Products ◽  
Future Research ◽  
Pharmacological Properties ◽  
Scientific Publications ◽  
Medicinal Uses

Cleistochlamys kirkii (Benth.) Oliv is a shrub or small tree widely used as a traditional medicine in the east and central Africa. Cleistochlamys kirkii is indigenous to Malawi, Mozambique, Tanzania, Zambia and Zimbabwe. This study is aimed at evaluating the phytochemistry, biological activities and therapeutic potential of C. kirkii. Results of the current study are based on data derived from several online databases such as Scopus, Google Scholar, PubMed and Science Direct, and pre-electronic sources such as scientific publications, books, dissertations, book chapters and journal articles. This study revealed that the leaf and root infusion, maceration and decoction of C. kirkii are mainly used as traditional medicines for haemorrhoid wounds, rheumatism and tuberculosis. Phytochemical compounds identified from the species include α,β-unsaturated lactone, acetogenin, benzyl benzoate derivatives, c-benzylated flavanone, heptanolide, an indole alkaloid, phenolics, polyoxygenated cyclohexene and derivatives, sesquiterpene and tetracyclic triterpenes. In vitro studies have confirmed the biological activities of C. kirkii crude extracts and compounds isolated from the species which include antibacterial, antifungal, antiplasmodial and cytotoxicity. Documentation of the medicinal uses, phytochemistry and pharmacological properties of C. kirkii is essential as this information provides baseline data required for future research and development of health-promoting and pharmaceutical products. Cleistochlamys kirkii should be subjected to detailed ethnopharmacological and toxicological evaluations aimed at correlating its medicinal uses with its phytochemistry and pharmacological properties.

scholarly journals Antimicrobial Peptides and Cancer: Potential Use of Antimicrobial-Like Peptides in Chemotherapy

2019 ◽  
pp. 233-242
Author(s):  
Mizejewski GJ
Keyword(s):  
Antimicrobial Peptides ◽  
Human Cancer ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Human Protein ◽  
Potential Candidate ◽  
Host Defense Peptides ◽  
Naturally Occurring

Antimicrobial peptides (AMPs) constitute host defense peptides found among insects, fish, amphibians, and mammals including man. The targets of AMPs are gram-negative and gram-positive bacteria, fungi, enveloped viruses, and transformed/cancerous cells. The AMPs are broad spectrum antibiotics which display the propensity to serve as therapeutic agents not only in infectious disease, but also in human cancer. AMPs demonstrate unique properties which include cell membrane penetration, destabilization of biological membranes, ability to form and/or interact with membrane channels, and the capability to modulate host immune responses. The three types of AMPs consists a) naturally-occurring; b) artificially synthesized; and c) cleaved peptide fragments from blood and extracellular matrix proteins. The present treatise presents one such example of an AMP-like peptide derived from a naturally-occurring human protein as a potential candidate for future cancer therapy. The biological activities of human AMP-like peptides as cancer therapeutic agents are reviewed and reported in multiple in vitro and in vivo cancer assays. The possibility of using such human protein-derived peptides as primary and adjunct cancer therapeutic agents is addressed.

scholarly journals Bioactive Compounds of Softwood Bark as Potential Agents against Human Diseases Include the SARS-CoV-2 Virus

2021 ◽  
Vol 12 (5) ◽  
pp. 5860-5869
Keyword(s):  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmaceutical Products ◽  
Cytotoxic Activities ◽  
Naturally Occurring ◽  
New Development ◽  
Main Class ◽  
Natural Drugs ◽  
Human Viruses

In recent years, significant progress has been achieved in developing natural drugs derived from medicinal plants. Multiple in-vitro screening studies reported that some naturally occurring compounds could possess inhibitory activity against various human viruses. The presented work describes significant biological activities of the main class of secondary metabolites such as phenolic compounds and terpenes located in industrially important tree species Norway spruce (Picea Abies) and Scots pine (Pinus Sylvestris). Phytochemicals show promising in vitro antiviral and cytotoxic activities, making them an attractive starting material for new development in various pharmaceutical products. They have the potential to effectively protect human health against cardiovascular diseases, diabetes mellitus, and as therapeutic agents against the SARS-CoV-2 virus.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

scholarly journals Recent Advances in Synthesis of 4-Arylcoumarins

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2417 ◽  
Author(s):  
Jong-Wha Jung ◽  
Nam-Jung Kim ◽  
Hwayoung Yun ◽  
Young Han
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Metal Catalysis ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Formation Type ◽  
Privileged Scaffold ◽  
Acid Catalyzed ◽  
A Minor ◽  
Synthetic Approaches

4-Arylcoumarins (4-aryl-2H-1-benzopyran-2-one), also known as neoflavones, comprise a minor subclass of naturally occurring flavonoids. Because of their broad-spectrum biological activities, arylcoumarins have been attracting the attention of the organic and medicinal chemistry communities, and are considered as an important privileged scaffold. Since the development of Pechmann condensation, a classical acid-catalyzed condensation between phenol and β-keto-carboxylic acid, several versatile and efficient synthetic approaches for 4-arylcoumarins have been reported. This review summarizes recent advances in the synthesis of the 4-arylcoumarin scaffold by classifying them based on the final bond-formation type. In particular, synthetic methods executed under mild and highly efficient conditions, such as solvent-free reactions and transition metal catalysis, are highlighted.

scholarly journals ANTIOXIDANT POTENTIAL OF PIPERIDINE CONTAINING COMPOUNDS-A SHORT REVIEW

2018 ◽  
Vol 11 (8) ◽  
pp. 66
Author(s):  
Manjusha R K ◽  
Shaheen Begum ◽  
Arifa Begum ◽  
Bharathi K
Keyword(s):  
Biological Activities ◽  
Short Review ◽  
Heterocyclic Ring ◽  
Antioxidant Potential ◽  
Naturally Occurring ◽  
Antioxidant Profile ◽  
Antioxidant Agents ◽  
Wide Range ◽  
Privileged Scaffold ◽  
Candidate Molecule

Piperidine is a saturated heterocyclic ring, considered as a privileged scaffold in view of its role in wide range of biological activities. Piperidine is good candidate molecule for obtaining potent antioxidant agents. The planar nature of this heterocyclic nucleus allows the introduction of substituent groups at different positions on the ring. In the present review, the antioxidant profile of piperidine containing compounds has been focused. The compounds were classified into naturally occurring piperidines, unsaturated piperidines, N-substituted piperidines, piperamides, piperanols, piperidine oximes, and hydrazides.

scholarly journals Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

2019 ◽  
Vol 20 (17) ◽  
pp. 4238 ◽  
Author(s):  
Yaqi Ren ◽  
Chunlan Wang ◽  
Jiakun Xu ◽  
Shuaiyu Wang
Keyword(s):  
Furan Ring ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coffee Beans ◽  
Anti Cancer ◽  
Underlying Mechanisms ◽  
Target Alternative ◽  
Anti Inflammation

Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

scholarly journals Marine Terpenic Endoperoxides

Marine Drugs ◽  
2021 ◽  
Vol 19 (12) ◽  
pp. 661
Author(s):  
Irene Torres-García ◽  
Josefa L. López-Martínez ◽  
Manuel Muñoz-Dorado ◽  
Ignacio Rodríguez-García ◽  
Miriam Álvarez-Corral
Keyword(s):  
Total Synthesis ◽  
Marine Invertebrates ◽  
Biological Activities ◽  
Structural Features ◽  
Naturally Occurring ◽  
Organic Extracts ◽  
Pharmaceutical Uses ◽  
Potential Use ◽  
Dioxane Ring

Organic extracts of marine invertebrates, mainly sponges, from seas all over the world are well known for their high in vitro anticancer and antibiotic activities which make them promising sources of compounds with potential use as pharmaceutical leads. Most of the structures discovered so far have a peculiar structural feature in common: a 1,2-dioxane ring. This is a highly reactive heterocycle that can be considered as an endoperoxide function. Together with other structural features, this group could be responsible for the strong biological activities of the substances present in the extracts. Numerous research programs have focused on their structural elucidation and total synthesis since the seventies. As a consequence, the number of established chiral centres and the similarity between different naturally occurring substances is increasingly higher. Most of these compounds have a terpenoid nature, mainly diterpene and sesterterpene, with several peculiar structural features, such as the loss of one carbon atom. Although there are many reviews dealing with the occurrence of marine peroxides, their activities, or potential pharmaceutical uses, no one has focused on those having a terpene origin and the endoperoxide function. We present here a comprehensive review of these compounds paying special attention to their structural features and their biological activity.

γ-Hydroxybutenolide Containing Marine Natural Products and Their Synthesis: A Review

2020 ◽  
Vol 23 (22) ◽  
pp. 2436-2468
Author(s):  
Supriya Tilvi ◽  
Safia Khan ◽  
Mahesh S. Majik
Keyword(s):  
Natural Products ◽  
Phospholipase A2 ◽  
Marine Natural Products ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Marine Sponges ◽  
Molecular Structures ◽  
Pharmacological Properties ◽  
Secretory Phospholipase A2 ◽  
Biological Studies

: γ-Hydroxybutenolides (γ-HB) is an important structural core found in many bioactive marine natural products (MNPS). The γ-HB core containing NPS served as an inspiration to medicinal chemists to undertake designing of the new synthetic strategies to construct γ-HB core. Subsequently, it further results in the development of novel physiological and therapeutic agents. The most notable example includes manoalides, cacospongionolides, petrosaspongioide M and dysidiolide from marine sponges possessing anti-inflammatory properties. γ-HB containing MNPS were known to possess various pharmacological properties such as antimicrobial (acantholide B), cytotoxic (acantholide A-E, spongianolide A), inhibitors of secretory phospholipase A2 (cladocorans A and B), BACE inhibitors (ianthellidone G), etc. Moreover, the γ-HB moiety was explored as antifouling agents as well. Owing to their numerous biological activities and attractive molecular structures, there are lots of advances in the synthetic methodology of these compounds. This review gives the account on isolation and biological studies of MNPS with γ-HB skeleton as a core unit. Furthermore, the synthesis of selective γ-HB containing bioactive MNPS like manoalide, secomanoalide, cacospongionolides, luffarielloide and dysidiolide were highlighted in the article.

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