Network pharmacology applications to map the unexplored target space and therapeutic potential of natural products

2015 ◽  
Vol 32 (8) ◽  
pp. 1249-1266 ◽  
Author(s):  
Milla Kibble ◽  
Niina Saarinen ◽  
Jing Tang ◽  
Krister Wennerberg ◽  
Sari Mäkelä ◽  
...  
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Therapeutic Potential ◽  
Mechanisms Of Action ◽  
Target Space ◽  
Network Pharmacology ◽  
Computational Approaches ◽  
Natural Product Research

This article reviews key network pharmacology concepts and recent experimental–computational approaches that have been successfully applied to natural product research, including unbiased elucidation of mechanisms of action and systematic prediction of effective therapeutic combinations.

scholarly journals Natural Products: Biochemical-Chemical Characterization, and Evidence for Therapeutic Potential

2015 ◽  
Vol 18 (4) ◽  
Author(s):  
Basil D Roufogalis ◽  
Srinivas Nammi ◽  
Emanuel E Strehler
Keyword(s):  
Natural Products ◽  
Traditional Medicine ◽  
Natural Product ◽  
Human Health ◽  
Therapeutic Potential ◽  
Chemical Characterization ◽  
Special Issue ◽  
Previous Issue ◽  
Prestigious Journal ◽  
Natural Product Research

This Special Issue follows from a previous Issue entitled “Mechanism-Based Development of Natural Products for Human Health” arising from an inaugural conference on Natural Products Development held at Whistler Mountain, Canada from September 21-22, 2012. The timeliness of this issue reflects the continued growth in Natural Product research and the success of the First Issue, as judged from feedback we received and citations received. We were also encouraged by the interest in natural products research in recent years, as exemplified by the recent publication on Traditional Medicine in the prestigious journal Science (1, 2).

scholarly journals Natural products with therapeutic potential in melanoma metastasis

2015 ◽  
Vol 32 (8) ◽  
pp. 1170-1182 ◽  
Author(s):  
A. AlQathama ◽  
J. M. Prieto
Keyword(s):  
Natural Products ◽  
Cancer Treatment ◽  
Therapeutic Potential ◽  
Melanoma Cells ◽  
Mechanisms Of Action ◽  
Melanoma Metastasis ◽  
Pharmacological Effects ◽  
Cytotoxic Compounds

Natural products continue to provide lead cytotoxic compounds for cancer treatment but less attention has been given to antimigratory compounds. We here systematically and critically survey more than 30 natural products with direct in vitro and in vivo pharmacological effects on migration and/or metastasis of melanoma cells and chart the mechanisms of action for this underexploited property.

scholarly journals A practical guide for transparent reporting of research on natural products in the British Journal of Pharmacology : Reproducibility of natural product research

2020 ◽  
Vol 177 (10) ◽  
pp. 2169-2178 ◽  
Author(s):  
Angelo A. Izzo ◽  
Mauro Teixeira ◽  
Steve P.H. Alexander ◽  
Giuseppe Cirino ◽  
James R. Docherty ◽  
...  
Keyword(s):  
Natural Products ◽  
British Journal ◽  
Natural Product ◽  
Practical Guide ◽  
Transparent Reporting ◽  
Natural Product Research

scholarly journals INTRODUCTION - Mechanism-based Development of Natural Products for Human Health

2013 ◽  
Vol 16 (2) ◽  
pp. 123
Author(s):  
Basil D Roufogalis ◽  
Arthur D Conigrave ◽  
Emanuel E Strehler
Keyword(s):  
Natural Products ◽  
Product Development ◽  
Research And Development ◽  
Natural Product ◽  
Mechanisms Of Action ◽  
Pharmaceutical Sciences ◽  
Special Issue ◽  
Active Components ◽  
Health Products ◽  
Natural Medicines

This Special Issue of the Journal of Pharmacy and Pharmaceutical Sciences arises from an inaugural conference on “Mechanism-Based Natural Product Development” held at Whistler Mountain, Canada on September 21-22, 2012. The aim of the conference was to bring together scientists from various disciplines to discuss the development of new therapeutic products from natural medicines based on mechanistic and related scientific studies. It provided an opportunity to explore new directions in natural medicine research and development, with the ultimate objective of leading to greater integration of natural and conventional synthetic pharmaceutical medicines for the health of the community worldwide. The concept for this conference and the Special Issue has come from the growing interest internationally in traditional and natural medicinal health products in recent years. It may, at first, appear surprising that developed countries are re-embracing natural product research and development. There are of course many reasons for this, including growing community interest in natural products providing improved health and wellbeing, the growing difficulty and cost of maintaining a pipeline of effective and, above all, safe new products for chronic diseases in the mainstream pharmaceutical industry, and the knowledge that many of our small drug pharmaceutical medicines have come from plants and other organisms. But as traditional natural product medicines increasingly enter the mainstream, the call for evidence to support their use also grows louder. Essential to the acceptance of natural medicines are the validation of their traditional uses and identification, isolation and structural characterization of their active components, together with the elucidation of their mechanisms of biological action, adverse effects, and identification of their molecular targets. These requirements provide the focus of this Special Issue. Scientific investigation and development of new health products requires the joining together of many disciplines, including chemistry, pharmacology, pharmacognosy and cell and molecular biology, as well as integration with clinical medicine. Natural product medicines are expected to be multi-component and multi-targeted. Are they effective, safe and properly standardized in their existing formulations? Are there opportunities to isolate single active components for standardization and conventional drug discovery and development? Answering these questions requires collaboration between scientific disciplines focused on a common goal. In line with the aims of the conference, the Special Issue has incorporated review and original research articles related to mechanisms of action in a number of therapeutic areas, mostly from invited speakers at the Whistler conference. Other articles were unsolicited submissions to the Journal that satisfy the scope of the issue. Articles range from reports on efforts to work with traditional owners in the appropriate cultural context, to develop new therapeutics based on traditional literature, to discover new medicinal products, to develop new pharmaceuticals based on the isolation of active chemical components, to develop new methods of delivery, and to identify mechanisms of action. The medical 'territory' includes cancer, heart disease, diabetes and related chronic inflammatory diseases, pain pathways, deafness and infertility. Other articles investigate the quality and safety of products by the application of current analytical methods, the potential for interactions of natural products (e.g., cranberry) with pharmaceutical medicines and the variability of a selection of similar natural product medicines with regard to their contents of therapeutically beneficial and marker compounds, as claimed on the product labels. In addition, the issue includes the abstracts of posters that formed an important part of the conference, especially from postgraduate students and postdoctoral fellows. These are included as Proceedings. We are indebted to the scientists who willingly gave their time and resources to attend the Whistler conference and, in many cases, submitted manuscripts for inclusion in this Special Issue. The delegates and contributors came from many places, near and far, to make this inaugural conference on mechanism-based natural product development a success. Such a conference and the subsequent proceedings in the Special issue are not possible without the work of many. We thank the organizing and scientific committee for their support and valuable suggestions. A conference of this scope would not be possible without sponsorship; this includes especially the National Health Products Research Society of Canada, the Canadian Society for Pharmaceutical Sciences and several Universities. Major support, without program or editorial input, was provided by SOHO Flordis International (SFI). We commend them for believing in the quest for clinically proven and research-based products based on an understanding of underlying mechanisms. The support of Purapharm International is also gratefully acknowledged. We would like to dedicate this Special Issue to Professor Allan SY Lau of the University of Hong Kong, who contributed enthusiastically to the organization of the conference and its program, but was ultimately unable to attend due to his untimely passing. Professor Lau was a pioneer in the integration of natural and orthodox medical studies and his inspiration will be greatly missed. Basil D Roufogalis, Arthur D Conigrave and Emanuel E Strehler Co-Guest Editors

scholarly journals Ecopharmacognosy: Exploring The Chemical And Biological Potential Of Nature For Human Health

2014 ◽  
Vol 3 (1) ◽  
pp. 1 ◽  
Author(s):  
Geoffrey A. Cordell
Keyword(s):  
Health Care ◽  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
Developed Countries ◽  
Biologically Active ◽  
Minor Role ◽  
Natural Product Research ◽  
Biological Potential ◽  
The World

“Why didn’t they develop natural product drugs in a sustainable manner at the beginning of this century?”  In 2035, when about 10.0 billion will inhabit Earth, will this be our legacy as the world contemplates the costs and availability of synthetic and gene-based products for primary health care?  Acknowledging the recent history of the relationship between humankind and the Earth, it is essential that the health care issues being left for our descendants be considered in terms of resources. For most people in the world, there are two vast health care “gaps”, access to quality drugs and the development of drugs for major global and local diseases.  Consequently for all of these people, plants, in their various forms, remain a primary source of health care.  In the developed countries, natural products derived from plants assume a relatively minor role in health care, as prescription and over-the-counter products, even with the widespread use of phytotherapeutical preparations.  Significantly, pharmaceutical companies have retrenched substantially in their disease areas of focus.  These research areas do not include the prevalent diseases of the middle- and lower-income countries, and important diseases of the developed world, such as drug resistance. What then is the vision for natural product research to maintain the choices of drug discovery and pharmaceutical development for future generations?  In this discussion some facets of how natural products must be involved globally, in a sustainable manner, for improving health care will be examined within the framework of the new term “ecopharmacognosy”, which invokes sustainability as the basis for research on biologically active natural products.  Access to the biome, the acquisition, analysis and dissemination of plant knowledge, natural product structure diversification, biotechnology development, strategies for natural product drug discovery, and aspects of multitarget therapy and synergy research will be discussed.  Options for the future will be presented which may be significant as countries decide how to develop approaches to relieve their own disease burden, and the needs of their population for improved access to medicinal agents.

scholarly journals Development of an agar-plug cultivation system for bioactivity assays of actinomycete strain collections

PLoS ONE ◽  
2021 ◽  
Vol 16 (11) ◽  
pp. e0258934
Author(s):  
Nico Ortlieb ◽  
Elke Klenk ◽  
Andreas Kulik ◽  
Timo Horst Johannes Niedermeyer
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Microtiter Plate ◽  
Growth Media ◽  
Natural Product Research ◽  
Solid Media ◽  
Agar Plug ◽  
Strain Collection ◽  
Actinomycete Strain ◽  
Initial Medium

Natural products are an important source of lead compounds for the development of drug substances. Actinomycetes have been valuable especially for the discovery of antibiotics. Increasing occurrence of antibiotic resistance among bacterial pathogens has revived the interest in actinomycete natural product research. Actinobacteria produce a different set of natural products when cultivated on solid growth media compared with submersed culture. Bioactivity assays involving solid media (e.g. agar-plug assays) require manual manipulation of the strains and agar plugs. This is less convenient for the screening of larger strain collections of several hundred or thousand strains. Thus, the aim of this study was to develop a 96-well microplate-based system suitable for the screening of actinomycete strain collections in agar-plug assays. We developed a medium-throughput cultivation and agar-plug assay workflow that allows the convenient inoculation of solid agar plugs with actinomycete spore suspensions from a strain collection, and the transfer of the agar plugs to petri dishes to conduct agar-plug bioactivity assays. The development steps as well as the challenges that were overcome during the development (e.g. system sterility, handling of the agar plugs) are described. We present the results from one exemplary screening campaign targeted to identify compounds inhibiting Agr-based quorum sensing where the workflow was used successfully. We present a novel and convenient workflow to combine agar diffusion assays with microtiter-plate-based cultivation systems in which strains can grow on a solid surface. This workflow facilitates and speeds up the initial medium throughput screening of natural product-producing actinomycete strain collections against monitor strains in agar-plug assays.

scholarly journals Type S Non Ribosomal Peptide Synthetases for the rapid generation of tailor-made peptide libraries

2021 ◽  
Author(s):  
Nadya Abbood ◽  
Tien Duy Vo ◽  
Jonas Watzel ◽  
Kenan A. J. Bozhueyuek ◽  
Helge B. Bode
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
De Novo ◽  
Chemical Space ◽  
Biologically Relevant ◽  
Peptide Synthetases ◽  
Medical Needs ◽  
Natural Product Research ◽  
Rapid Generation ◽  
Traditional Natural

Bacterial natural products in general, and non-ribosomally synthesized peptides in particular, are structurally diverse and provide us with a broad range of pharmaceutically relevant bioactivities. Yet, traditional natural product research suffers from rediscovering the same scaffolds and has been stigmatised as inefficient, time-, labour-, and cost-intensive. Combinatorial chemistry, on the other hand, can produce new molecules in greater numbers, cheaper and in less time than traditional natural product discovery, but also fails to meet current medical needs due to the limited biologically relevant chemical space that can be addressed. Consequently, methods for the high throughput generation of new-to-nature natural products would offer a new approach to identifying novel bioactive chemical entities for the hit to lead phase of drug discovery programms. As a follow-up to our previously published proof-of-principle study on generating bipartite type S non-ribosomal peptide synthetases (NRPSs), we now envisaged the de novo generation of non-ribosomal peptides (NRPs) on an unreached scale. Using synthetic zippers, we split NRPS in up to three subunits and rapidly generated different bi- and tripartite NRPS libraries to produce 49 peptides, peptide derivatives, and de novo peptides at good titres up to 145 mgL-1. A further advantage of type S NRPSs not only is the possibility to easily expand the created libraries by re-using previously created type S NRPS, but that functions of individual domains as well as domain-domain interactions can be studied and assigned rapidly.

scholarly journals Trypanocidal Essential Oils: A Review

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4568 ◽  
Author(s):  
Mayara Castro de Morais ◽  
Jucieudo Virgulino de Souza ◽  
Carlos da Silva Maia Bezerra Filho ◽  
Silvio Santana Dolabella ◽  
Damião Pergentino de Sousa
Keyword(s):  
Experimental Data ◽  
Natural Products ◽  
Essential Oils ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Important Group

Trypanosomiases are diseases caused by parasitic protozoan trypanosomes of the genus Trypanosoma. In humans, this includes Chagas disease and African trypanosomiasis. There are few therapeutic options, and there is low efficacy to clinical treatment. Therefore, the search for new drugs for the trypanosomiasis is urgent. This review describes studies of the trypanocidal properties of essential oils, an important group of natural products widely found in several tropical countries. Seventy-seven plants were selected from literature for the trypanocidal activity of their essential oils. The main chemical constituents and mechanisms of action are also discussed. In vitro and in vivo experimental data show the therapeutic potential of these natural products for the treatment of infections caused by species of Trypanosoma.

A Recent Look into Natural Products that have Potential to Inhibit Cholinesterases and Monoamine Oxidase B: Update for 2010-2019

2020 ◽  
Vol 23 (9) ◽  
pp. 862-876
Author(s):  
Hayrettin O. Gulcan ◽  
Ilkay E. Orhan
Keyword(s):  
Natural Products ◽  
Monoamine Oxidase ◽  
Natural Product ◽  
Biological Activities ◽  
Treatment Options ◽  
Monoamine Oxidase B ◽  
Chemical Structures ◽  
Natural Agents ◽  
Natural Product Research ◽  
Multiple Receptors

With respect to the unknowns of pathophysiology of Alzheimer’s Disease (AD)-, and Parkinson’s Disease (PD)-like neurodegenerative disorders, natural product research is still one of the valid tools in order to provide alternative and/or better treatment options. At one hand, various extracts of herbals provide a combination of actions targeting multiple receptors, on the other hand, the discovery of active natural products (i.e., secondary metabolites) generally offers alternative chemical structures either ready to be employed in clinical studies or available to be utilized as important scaffolds for the design of novel agents. Regarding the importance of certain enzymes (e.g. cholinesterase and monoamine oxidase B), for the treatment of AD and PD, we have surveyed the natural product research within this area in the last decade. Particularly novel natural agents discovered within this period, concomitant to novel biological activities displayed for known natural products, are harmonized within the present study.

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