Natural Products - From Bioactive Molecules to Human Health [Working Title]

2020 ◽  
2007 ◽  
Vol 2 (10) ◽  
pp. 1214-1234 ◽  
Author(s):  
Filippos Ververidis ◽  
Emmanouil Trantas ◽  
Carl Douglas ◽  
Guenter Vollmer ◽  
Georg Kretzschmar ◽  
...  

2021 ◽  
Vol 01 ◽  
Author(s):  
Dinesh Kumar Patel

Background: Natural products and their derived phytochemicals have been used in the medicine and gaining importance in the modern medicine due to their therapeutic potential and health beneficial effect on human disorders. Plenty of herbal drug based products are available in the market and playing an important role in the human health care system due to their health beneficial properties in human being. In the modern age we can find many herbal based products in the market mainly prepared from the natural products and used for the prevention and treatment of various human disorders. Benzylisoquinoline alkaloids are the important class of alkaloidal compounds and the better example are morphine, codeine, sanguinarine, berberine and canadine which are mainly known for their medicinal value in the medicine. Methods: Hydrastis canadensis is the important medicinal plant found to contain a significant amount of canadine, hydrastine and berberine. In the present investigation, numerous scientific databases such as Google, Pubmed, Science direct etc. have been searched to collect the important scientific information of canadine and analyzed to know the health beneficial aspect of canadine in the medicine. All the collected scientific information data’s were analyzed and have been categorized into mainly pharmacological and analytical aspects. Results: From the analysis of the collected scientific information, it was found that Hydrastis canadensis contain significant amount of canadine with many more phytochemical including canadaline, hydrastidine, isohydrastidine etc. Pharmacological activity data analysis revealed the biological importance of Hydrastis canadensis in the medicine for their traditional uses against gastritis, colitis, duodenal ulcers, loss of appetite, liver disease, bile secretion disorder, snake bites and vaginitis in the medicine. However, scientific data analysis of canadine revealed their effectiveness for their acetylcholinesterase inhibitory activity, anti-cancer, anti-microbial, anti-allergic activity and anti-oxidant activity. Different modern analytical tools have been used in the modern medicine for the isolation and quantification of canadine in the Hydrastis canadensis. Conclusion: Present investigation revealed the medicinal importance and pharmacological activities of a canadine in the medicine for the treatment of numerous human health complications. These scientific data will be helpful to the scientist to know the biological importance of canadine in the medicine against various forms of human complications.


Author(s):  
Beatriz de las Heras Polo

Natural products have historically contributed to drug discovery as a source of bioactive molecules, due to their great diversity and structural complexity. They have provided “lead” molecules for the development of drugs in different therapeutic areas, with a very prominent representation in the treatment of pain and inflammation, coagulation disorders, metabolic disorders, as well as in the treatment of cancer and infectious diseases. In recent decades there has been a paradigm shift in drug discovery strategies that has allowed the identification of new active natural products in therapeutic targets. Combinatorial Chemistry and biological tests (High Throughput Screening), together with the development of computational techniques, have contributed decisively to the design and optimization of libraries of natural product derivatives based on their biological activity. In parallel, technological advances in the field of Omics sciences and in data processing lead to a multidimensional approach in the drug discovery process. These powerful tools will allow the analysis of the pharmacological potential of natural products and their derivatives for the conversion of these molecules to active products with low toxicity. In the Precision Medicine era, natural products continue to be molecules with great potential in pharmaceutical development, since, unlike other therapeutic strategies, they have a favorable cost-benefit ratio, which will allow their future use in this discipline.


2021 ◽  
Vol 12 ◽  
Author(s):  
Ermelinda Botticella ◽  
Daniel Valentin Savatin ◽  
Francesco Sestili

Cereals represent an important source of beneficial compounds for human health, such as macro- and micronutrients, vitamins, and bioactive molecules. Generally, the consumption of whole-grain products is associated with significant health benefits, due to the elevated amount of dietary fiber (DF). However, the consumption of whole-grain foods is still modest compared to more refined products. In this sense, it is worth focusing on the increase of DF fractions inside the inner compartment of the seed, the endosperm, which represents the main part of the derived flour. The main components of the grain fiber are arabinoxylan (AX), β-glucan (βG), and resistant starch (RS). These three components are differently distributed in grains, however, all of them are represented in the endosperm. AX and βG, classified as non-starch polysaccharides (NSP), are in cell walls, whereas, RS is in the endosperm, being a starch fraction. As the chemical structure of DFs influences their digestibility, the identification of key actors involved in their metabolism can pave the way to improve their function in human health. Here, we reviewed the main achievements of plant biotechnologies in DFs manipulation in cereals, highlighting new genetic targets to be exploited, and main issues to face to increase the potential of cereals in fighting malnutrition.


2021 ◽  
Author(s):  
Keisuke Fujiyama ◽  
Naoki Kato ◽  
Suyong Re ◽  
Kiyomi Kinugasa ◽  
Kohei Watanabe ◽  
...  

SummaryMolecular chirality, discovered by Louis Pasteur in the middle of the 19th century1, is found in most primary and secondary metabolites. Particularly, the so-called natural products are rich in chiral centres2. The stereochemistry of natural products is strictly recognized in living organisms, and is thus closely related to their biological functions. The Diels–Alder (DA) reaction, which forms a six-membered ring with up to four chiral centres, is a fundamental practical reaction for C–C bond formation in synthetic chemistry3. Nature has also adopted this reaction to elaborate the complex structures of natural products using enzymes derived from various progenitor proteins4-7. Although enzymes catalysing the DA reaction, Diels–Alderases (DAases), have attracted increasing attention, little is known about the molecular mechanism by which they control the stereochemistry and perform catalysis. Here, we solved the X-ray crystal structures of a pair of decalin synthases, Fsa2 and Phm7, that catalyse intramolecular DA reactions to form enantiomeric decalin scaffolds during biosynthesis of the HIV-1 integrase inhibitor equisetin and its stereochemical opposite, phomasetin8,9. Based on the crystal structures, docking simulations followed by all-atom molecular dynamics simulations provided dynamic binding models demonstrating the folding of linear polyenoyl tetramic acid substrates in the binding pocket of these enzymes, explaining the stereoselectivity in the construction of decalin scaffolds. Site-directed mutagenesis studies verified the binding models and, in combination with density functional theory calculations, clarified how hydrophilic amino acid residues in the Phm7 pocket regulate and catalyse the stereoselective DA reaction. This study highlights the distinct molecular mechanisms of the enzymatic DA reaction and its stereoselectivity experimentally and computationally. We anticipate that clarified molecular mechanism herein provides not only the basic understanding how these important enzymes work but also the guiding principle to create artificial enzymes that produce designer bioactive molecules.


2013 ◽  
Vol 16 (2) ◽  
pp. 125
Author(s):  
Basil D Roufogalis ◽  
Arthur D Conigrave

Mechanism-Based Development of Natural Products in Human Health


2019 ◽  
Vol 19 (28) ◽  
pp. 2567-2578 ◽  
Author(s):  
Rajeev K. Singla ◽  
Ashok K. Dubey

Background: Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. Methods: A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofilms produced by Candida spp. The databases explored were from PubMed and Google Scholar. The abstracts and full text of the manuscripts from the literature were analyzed and included if found significant. Results: Medicinal plants from the order Lamiales, Apiales, Asterales, Myrtales, Sapindales, Acorales, Poales and Laurales were reported to inhibit the biofilms formed by Candida spp. From the microbiological sources, lactobacilli, Streptomyces chrestomyceticus and Streptococcus thermophilus B had shown the strong biofilm inhibition potential. Further, the diverse nature of the compounds from classes like terpenoids, phenylpropanoid, alkaloids, flavonoids, polyphenol, naphthoquinone and saponin was found to be significant in inhibiting the biofilm of Candida spp. Conclusion: Natural products from both plant and microbial origins have proven themselves as a goldmine for isolating the potential biofilm inhibitors with a specific or multi-locus mechanism of action. Structural and functional characterization of the bioactive molecules from active extracts should be the next line of approach along with the thorough exploration of the mechanism of action for the already identified bioactive molecules.


Amino Acids ◽  
2015 ◽  
Vol 48 (3) ◽  
pp. 849-858 ◽  
Author(s):  
Adina-Elena Segneanu ◽  
Daniel Damian ◽  
Iosif Hulka ◽  
Ioan Grozescu ◽  
Athanasios Salifoglou

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