scholarly journals Lessons from Exploring Chemical Space and Chemical Diversity of Propolis Components

2020 ◽  
Vol 21 (14) ◽  
pp. 4988 ◽  
Author(s):  
Trong D. Tran ◽  
Steven M. Ogbourne ◽  
Peter R. Brooks ◽  
Norberto Sánchez-Cruz ◽  
José L. Medina-Franco ◽  
...  

Propolis is a natural resinous material produced by bees and has been used in folk medicines since ancient times. Due to it possessing a broad spectrum of biological activities, it has gained significant scientific and commercial interest over the last two decades. As a result of searching 122 publications reported up to the end of 2019, we assembled a unique compound database consisting of 578 components isolated from both honey bee propolis and stingless bee propolis, and analyzed the chemical space and chemical diversity of these compounds. The results demonstrated that both honey bee propolis and stingless bee propolis are valuable sources for pharmaceutical and nutraceutical development.

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984413 ◽  
Author(s):  
Soraia I. Falcão ◽  
Mélissa Lopes ◽  
Miguel Vilas-Boas

Propolis is a natural product derived from plant resins collected by honeybees and used in the beehive as a construction and defensive material. The broad spectrum of biological activities is dependent on the chemical diversity of its composition which is determined by the floral sources at the site of collection. For the first time, the chemical composition of Guinean propolis as well as its physicochemical properties, phenolic composition, and antioxidant activity was assessed. Eight compounds were identified through LC/DAD/ESI-MS n , mostly isoflavonoids, resembling Nigerian and Brazilian red propolis from the genus Dalbergia.


eLife ◽  
2017 ◽  
Vol 6 ◽  
Author(s):  
Tal Luzzatto-Knaan ◽  
Neha Garg ◽  
Mingxun Wang ◽  
Evgenia Glukhov ◽  
Yao Peng ◽  
...  

Natural product screening programs have uncovered molecules from diverse natural sources with various biological activities and unique structures. However, much is yet underexplored and additional information is hidden in these exceptional collections. We applied untargeted mass spectrometry approaches to capture the chemical space and dispersal patterns of metabolites from an in-house library of marine cyanobacterial and algal collections. Remarkably, 86% of the metabolomics signals detected were not found in other available datasets of similar nature, supporting the hypothesis that marine cyanobacteria and algae possess distinctive metabolomes. The data were plotted onto a world map representing eight major sampling sites, and revealed potential geographic locations with high chemical diversity. We demonstrate the use of these inventories as a tool to explore the diversity and distribution of natural products. Finally, we utilized this tool to guide the isolation of a new cyclic lipopeptide, yuvalamide A, from a marine cyanobacterium.


2021 ◽  
Vol 9 (2) ◽  
pp. 311
Author(s):  
Alison H. Hughes ◽  
Florent Magot ◽  
Ahmed F. Tawfike ◽  
Cecilia Rad-Menéndez ◽  
Naomi Thomas ◽  
...  

With more than 156,000 described species, eukaryotic algae (both macro- and micro-algae) are a rich source of biological diversity, however their chemical diversity remains largely unexplored. Specialised metabolites with promising biological activities have been widely reported for seaweeds, and more recently extracts from microalgae have exhibited activity in anticancer, antimicrobial, and antioxidant screens. However, we are still missing critical information on the distinction of chemical profiles between macro- and microalgae, as well as the chemical space these metabolites cover. This study has used an untargeted comparative metabolomics approach to explore the chemical diversity of seven seaweeds and 36 microalgal strains. A total of 1390 liquid chromatography-mass spectrometry (LC-MS) features were detected, representing small organic algal metabolites, with no overlap between the seaweeds and microalgae. An in-depth analysis of four Dunaliella tertiolecta strains shows that environmental factors may play a larger role than phylogeny when classifying their metabolomic profiles.


2016 ◽  
Vol 12 ◽  
pp. 1250-1268 ◽  
Author(s):  
Andrew W Truman

Ribosomally synthesised and post-translationally modified peptides (RiPPs) are a large class of natural products that are remarkably chemically diverse given an intrinsic requirement to be assembled from proteinogenic amino acids. The vast chemical space occupied by RiPPs means that they possess a wide variety of biological activities, and the class includes antibiotics, co-factors, signalling molecules, anticancer and anti-HIV compounds, and toxins. A considerable amount of RiPP chemical diversity is generated from cyclisation reactions, and the current mechanistic understanding of these reactions will be discussed here. These cyclisations involve a diverse array of chemical reactions, including 1,4-nucleophilic additions, [4 + 2] cycloadditions, ATP-dependent heterocyclisation to form thiazolines or oxazolines, and radical-mediated reactions between unactivated carbons. Future prospects for RiPP pathway discovery and characterisation will also be highlighted.


2019 ◽  
Vol 05 ◽  
Author(s):  
Atul Sharma ◽  
Devender Pathak

Keeping this fact that study of a body is biology but life is all about chemicals and chemical transformations, many medicinal chemist start research in finding new and novel chemical compounds which having pharmacological activities. Most of those chemical compounds which are having active pharmacological effects are heterocyclic compounds. Heterocyclic compounds clutch a particular place among pharmaceutically active natural and synthetic compounds. The ability to serve both as biomimetics and reactive pharmacophores of heterocyclic nuclei is incredible and it has principally contributed to their unique value as traditional key elements of numerous drugs. These heterocyclic nuclei offer a huge area for new lead molecules for drug discovery and for generation of activity relationships with biological targets to enhance pharmacological effects. For these reasons, it is not surprising that this structural class has received special attention in drug discovery. The hydrogen bond acceptors and donors arranged in a manner of a semi-rigid skeleton in heterocyclic rings and therefore they can present a varied display of significant pharmacophores. Lead identification and optimization of drug target probable can be achieved by generation of chemical diversity produced by derivatization of heterocyclic pharmacophores with different groups or substituents. A tricyclic carbazole nucleus is an integral part of naturally occurring alkaloids and synthetic derivatives, possessing various potential biological activities such as anticancer, antimicrobial and antiviral. Binding mechanism of carbazole with target receptor as a molecule or fused molecule exhibits the potential lethal effect.


Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 488
Author(s):  
Afrah E. Mohammed ◽  
Zainab H. Abdul-Hameed ◽  
Modhi O. Alotaibi ◽  
Nahed O. Bawakid ◽  
Tariq R. Sobahi ◽  
...  

By the end of the twentieth century, the interest in natural compounds as probable sources of drugs has declined and was replaced by other strategies such as molecular target-based drug discovery. However, in the recent times, natural compounds regained their position as extremely important source drug leads. Indole-containing compounds are under clinical use which includes vinblastine and vincristine (anticancer), atevirdine (anti-HIV), yohimbine (erectile dysfunction), reserpine (antihypertension), ajmalicine (vascular disorders), ajmaline (anti-arrhythmic), vincamine (vasodilator), etc. Monoterpene Indole Alkaloids (MIAs) deserve the curiosity and attention of researchers due to their chemical diversity and biological activities. These compounds were considered as an impending source of drug-lead. In this review 444 compounds, were identified from six genera belonging to the family Apocynaceae, will be discussed. These genera (Alstonia, Rauvolfia, Kopsia, Ervatamia, and Tabernaemontana, and Rhazya) consist of 400 members and represent 20% of Apocynaceae species. Only 30 (7.5%) species were investigated, whereas the rest are promising to be investigated. Eleven bioactivities, including antibacterial, antifungal, anti-inflammatory and immunosuppressant activities, were reported. Whereas cytotoxic effect represents 47% of the reported activities. Convincingly, the genera selected in this review are a wealthy source for future anticancer drug lead.


Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.


Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 335
Author(s):  
Xia Yan ◽  
Jing Liu ◽  
Xue Leng ◽  
Han Ouyang

Sinularia is one of the conspicuous soft coral species widely distributed in the world’s oceans at a depth of about 12 m. Secondary metabolites from the genus Sinularia show great chemical diversity. More than 700 secondary metabolites have been reported to date, including terpenoids, norterpenoids, steroids/steroidal glycosides, and other types. They showed a broad range of potent biological activities. There were detailed reviews on the terpenoids from Sinularia in 2013, and now, it still plays a vital role in the innovation of lead compounds for drug development. The structures, names, and pharmacological activities of compounds isolated from the genus Sinularia from 2013 to March 2021 are summarized in this review.


Environments ◽  
2021 ◽  
Vol 8 (6) ◽  
pp. 59
Author(s):  
Omar Al-Dulaimi ◽  
Mostafa E. Rateb ◽  
Andrew S. Hursthouse ◽  
Gary Thomson ◽  
Mohammed Yaseen

More than 50% of the UK coastline is situated in Scotland under legislative jurisdiction; therefore, there is a great opportunity for regionally focused economic development by the rational use of sustainable marine bio-sources. We review the importance of seaweeds in general, and more specifically, wrack brown seaweeds which are washed from the sea and accumulated in the wrack zone and their economic impact. Rules and regulations governing the harvesting of seaweed, potential sites for harvesting, along with the status of industrial application are discussed. We describe extraction and separation methods of natural products from these seaweeds along with their phytochemical profiles. Many potential applications for these derivatives exist in agriculture, energy, nutrition, biomaterials, waste treatment (composting), pharmaceuticals, cosmetics and other applications. The chemical diversity of the natural compounds present in these seaweeds is an opportunity to further investigate a range of chemical scaffolds, evaluate their biological activities, and develop them for better pharmaceutical or biotechnological applications. The key message is the significant opportunity for the development of high value products from a seaweed processing industry in Scotland, based on a sustainable resource, and locally regulated.


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