Faculty Opinions recommendation of Natural products as probes in pharmaceutical research.

2015 ◽  
Author(s):  
Jean-Jacques Sanglier
Keyword(s):  
Natural Products ◽  
Pharmaceutical Research

scholarly journals Deliberations on Natural Products and Future Directions in the Pharmaceutical Industry

2021 ◽  
Vol 75 (7) ◽  
pp. 620-633
Author(s):  
Kathrin Buntin ◽  
Peter Ertl ◽  
Dominic Hoepfner ◽  
Philipp Krastel ◽  
Edward J. Oakeley ◽  
...  
Keyword(s):  
Natural Products ◽  
Chemical Space ◽  
Pharmaceutical Research ◽  
Gene Clusters ◽  
Drug Market ◽  
Special Equipment ◽  
Research Areas ◽  
Biological Target ◽  
Synthetic Derivative ◽  
Fungal Genes

Natural Products (NPs) are molecular' special equipment ' that impart survival benefits on their producers in nature. Due to their evolved functions to modulate biology these privileged metabolites are substantially represented in the drug market and are continuing to contribute to the discovery of innovative medicines such as the recently approved semi-synthetic derivative of the bacterial alkaloid staurosporin in oncology indications. The innovation of low molecular weight compounds in modern drug discovery is built on rapid progress in chemical, molecular biological, pharmacological and data sciences, which together provide a rich understanding of disease-driving molecular interactions and how to modulate them. NPs investigated in these pharmaceutical research areas create new perspectives on their chemical and biological features and thereby new chances to advance medical research. New methods in analytical chemistry linked with searchable NP-databases solved the issue of reisolation and enabled targeted and efficient access to novel molecules from nature. Cheminformatics delivers high resolution descriptions of NPs and explores the substructures that systematically map NP-chemical space by sp3-enriched fragments. Whole genome sequencing has revealed the existence of collocated gene clusters that form larger functional entities together with proximate resistance factors thus avoiding self-inhibition of the encoded metabolites. The analysis of bacterial and fungal genes provides tantalizing glimpses of new compound-target pairs of therapeutic value. Furthermore, a dedicated investigation of structurally unique, selectively active NPs in chemical biology demonstrates their extraordinary power as shuttles between new biological target spaces of pharmaceutical relevance.

scholarly journals A Promiscuous Halogenase for the Derivatization of Flavonoids

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6220
Author(s):  
Dominik Kolling ◽  
Marc Stierhof ◽  
Constanze Lasch ◽  
Maksym Myronovskyi ◽  
Andriy Luzhetskyy
Keyword(s):  
Natural Products ◽  
Biological Activities ◽  
Substrate Recognition ◽  
Pharmaceutical Research ◽  
Homology Model ◽  
Downstream Processing ◽  
Modern Drug ◽  
Frankia Alni ◽  
Synthetic Approaches ◽  
Drug Leads

Halogenation often improves the bioactive properties of natural products and is used in pharmaceutical research for the generation of new potential drug leads. High regio- and stereospecificity, simple reaction conditions and straightforward downstream processing are the main advantages of halogenation using enzymatic biocatalysts compared to chemical synthetic approaches. The identification of new promiscuous halogenases for the modification of various natural products is of great interest in modern drug discovery. In this paper, we report the identification of a new promiscuous FAD-dependent halogenase, DklH, from Frankia alni ACN14a. The identified halogenase readily modifies various flavonoid compounds, including those with well-studied biological activities. This halogenase has been demonstrated to modify not only flavones and isoflavones, but also flavonols, flavanones and flavanonols. The structural requirements for DklH substrate recognition were determined using a feeding approach. The homology model of DklH and the mechanism of substrate recognition are also proposed in this paper.

Natural products as probes in pharmaceutical research

2015 ◽  
Vol 43 (2-3) ◽  
pp. 249-260 ◽  
Author(s):  
Esther K. Schmitt ◽  
D. Hoepfner ◽  
P. Krastel
Keyword(s):  
Natural Products ◽  
Pharmaceutical Research

2-Methoxy-6-Acetyl-7-Methyljuglone: A Bioactive Phytochemical with Potential Pharmacological Activities

2021 ◽  
Vol 21 ◽  
Author(s):  
Atif Ali Khan Khalil ◽  
Asma Saleem Qazi ◽  
Abdul Nasir ◽  
Mi-Jeong Ahn ◽  
Muhammad Ajmal Shah ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Cancer Progression ◽  
Pharmaceutical Research ◽  
Medicinal Products ◽  
Pharmacological Activities ◽  
Potential Efficacy ◽  
Medicinal Properties ◽  
Jnk Activation ◽  
Anti Hiv

: Natural products have been the focus of biomedical and pharmaceutical research to develop new therapies in recent years. 2-methoxy-6-acetyl-7-methyljuglone (2-methoxystypandrone, MAM), a natural bioactive juglone derivative, is known to have various levels of pharmacotherapeutic efficacies as an anti-inflammatory, anticancer, antioxidant, antimicrobial, and anti-HIV activity. MAM fights cancer progression by inducing apoptosis, necroptosis, and deregulating signaling pathways through H2O2-induced JNK/iNOS/NO and MAPK, ERK1/2 pathways, JNK activation, and the RIP1/RIP3 complex. In this review, we summarize the pharmacological importance of MAM in the field of drug discovery. Furthermore, this review not only emphasizes the medicinal properties of MAM but also discusses its potential efficacy in future medicinal products.

Application of Molecular Docking in Studies on the Binding Mechanism of Three Enzymes with Natural Products

2016 ◽  
pp. 81-126
Author(s):  
Hua-jin Zeng ◽  
Ran Yang ◽  
Ling-bo Qu
Keyword(s):  
Molecular Structure ◽  
Natural Products ◽  
Molecular Docking ◽  
Biological Activities ◽  
Pharmaceutical Research ◽  
Inhibitory Effect ◽  
Binding Mechanism ◽  
Biologically Relevant ◽  
Useful Knowledge

Enzymes play an important role in many biologically relevant processes and are some attractive targets in the therapy and pharmaceutical research. The interaction between drugs and enzymes in vitro might account for a variety of biological processes and has attracted scientists' great interest for several decades. Investigation of the interaction can explore their mechanism of biological activities and provide useful knowledge for optimizing molecular structure of drug, prescriptions and route of administration and it can also provide the information for their bioavailability and bioactivity. In this chapter, the bindings of natural products (including flavionoids and coumarins) with three enzymes, including pepsin, hyaluronidase and acetylcholinesterase, were investigated by fluorescence spectroscopy and molecular docking. The present studies provide direct evidence at a molecular level to understand the mechanism of inhibitory effect of natural products against enzymes.

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