Recent Progress Towards Synthesis of the Indolizidine Alkaloid 195B

2020 ◽  
Vol 17 (2) ◽  
pp. 82-90 ◽  
Author(s):  
Ghodsi Mohammadi Ziarani ◽  
Fatemeh Mohajer ◽  
Zohreh kheilkordi
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Recent Progress ◽  
Human Life ◽  
Natural Compounds ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Biological Perspective ◽  
Highly Active

Background: Natural products have been received attention due to their importance in human life as those are biologically active. In this review, there are some reports through different methods related to the synthesis of the indolizidine 195B which was extracted from poisonous frog; however, due to respect nature, the synthesis of natural compounds such as indolizidine has been attracted much attention among scientists and researchers. Objective: This review discloses the procedures and methods to provide indolizidine 195B from 1989 to 2018 due to their importance as a natural product. Conclusion: There are several methods to give rise to the indolizidine 195B as a natural product that is highly active from the biological perspective in pharmaceutical chemistry. In summary, many protocols for the preparations of indolizidine 195B from various substrates, several reagents, and conditions have been reported from different aromatic and aliphatic.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

scholarly journals Exosome-Based Delivery of Natural Products in Cancer Therapy

2021 ◽  
Vol 9 ◽  
Author(s):  
Hang Song ◽  
Bin Liu ◽  
Bin Dong ◽  
Jing Xu ◽  
Hui Zhou ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Natural Products ◽  
Cancer Therapy ◽  
Natural Product ◽  
Current Knowledge ◽  
Donor Cell ◽  
Natural Compounds ◽  
Cellular Behaviors ◽  
Delivery Vehicles ◽  
Intercellular Communications

A rapidly growing research evidence has begun to shed light on the potential application of exosome, which modulates intercellular communications. As donor cell released vesicles, exosomes could play roles as a regulator of cellular behaviors in up-taken cells, as well as a delivery carrier of drugs for targeted cells. Natural product is an invaluable drug resources and it is used widely as therapeutic agents in cancers. This review summarizes the most recent advances in exosomes as natural product delivery carriers in cancer therapy from the following aspects: composition of exosomes, biogenesis of exosomes, and its functions in cancers. The main focus is the advantages and applications of exosomes for drug delivery in cancer therapy. This review also summarizes the isolation and application of exosomes as delivery carriers of natural products in cancer therapy. The recent progress and challenges of using exosomes as drug delivery vehicles for five representative anti-cancer natural products including paclitaxel, curcumin, doxorubicin, celastrol, and β-Elemene. Based on the discussion on the current knowledge about exosomes as delivery vehicles for drugs and natural compounds to the targeted site, this review delineates the landscape of the recent research, challenges, trends and prospects in exosomes as delivery vehicles for drugs and natural compounds for cancer treatment.

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.

3,4-Dihydroisocoumarins, Interesting Natural Products: Isolation, Organic Syntheses and Biological Activities

2019 ◽  
Vol 16 (1) ◽  
pp. 112-129 ◽  
Author(s):  
Aurelio Ortiz ◽  
Miriam Castro ◽  
Estibaliz Sansinenea
Keyword(s):  
Natural Products ◽  
Biological Activities ◽  
Natural Compounds ◽  
Biologically Active ◽  
Bacterial Strains ◽  
Drug Candidates ◽  
Heterocyclic Molecules ◽  
Naturally Occurring ◽  
Wide Range ◽  
Different Sources

Background:3,4-dihydroisocoumarins are an important small group belonging to the class of naturally occurring lactones isolated from different bacterial strains, molds, lichens, and plants. The structures of these natural compounds show various types of substitution in their basic skeleton and this variability influences deeply their biological activities. These lactones are structural subunits of several natural products and serve as useful intermediates in the synthesis of different heterocyclic molecules, which exhibit a wide range of biological activities, such as anti-inflammatory, antiplasmodial, antifungal, antimicrobial, antiangiogenic and antitumoral activities, among others. Their syntheses have attracted attention of many researchers reporting many synthetic strategies to achieve 3,4-dihydroisocoumarins and other related structures. </P><P> Objective: In this context, the isolation of these natural compounds from different sources, their syntheses and biological activities are reviewed, adding the most recent advances and related developments.Conclusion:This review aims to encourage further work on the isolation and synthesis of this class of natural products. It would be beneficial for synthetic as well as the medicinal chemists to design selective, optimized dihydroisocoumarin derivatives as potential drug candidates, since dihydroisocoumarin scaffolds have significant utility in the development of therapeutically relevant and biologically active compounds.

scholarly journals Structure elucidation and biosynthesis of fuscachelins, peptide siderophores from the moderate thermophileThermobifida fusca

2008 ◽  
Vol 105 (40) ◽  
pp. 15311-15316 ◽  
Author(s):  
Eric J. Dimise ◽  
Paul F. Widboom ◽  
Steven D. Bruner
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Gene Cluster ◽  
Structure Elucidation ◽  
Biochemical Characterization ◽  
Gene Clusters ◽  
Biologically Active ◽  
Biosynthetic Gene ◽  
Nonribosomal Peptide

Bacteria belonging to the order Actinomycetales have proven to be an important source of biologically active and often therapeutically useful natural products. The characterization of orphan biosynthetic gene clusters is an emerging and valuable approach to the discovery of novel small molecules. Analysis of the recently sequenced genome of the thermophilic actinomyceteThermobifida fuscarevealed an orphan nonribosomal peptide biosynthetic gene cluster coding for an unknown siderophore natural product.T. fuscais a model organism for the study of thermostable cellulases and is a major degrader of plant cell walls. Here, we report the isolation and structure elucidation of the fuscachelins, siderophore natural products produced byT. fusca. In addition, we report the purification and biochemical characterization of the termination module of the nonribosomal peptide synthetase. Biochemical analysis of adenylation domain specificity supports the assignment of this gene cluster as the producer of the fuscachelin siderophores. The proposed nonribosomal peptide biosynthetic pathway exhibits several atypical features, including a macrocyclizing thioesterase that produces a 10-membered cyclic depsipeptide and a nonlinear assembly line, resulting in the unique heterodimeric architecture of the siderophore natural product.

scholarly journals Applying a Chemogeographic Strategy for Natural Product Discovery from the Marine Cyanobacterium Moorena bouillonii

Marine Drugs ◽  
2020 ◽  
Vol 18 (10) ◽  
pp. 515
Author(s):  
Christopher A. Leber ◽  
C. Benjamin Naman ◽  
Lena Keller ◽  
Jehad Almaliti ◽  
Eduardo J. E. Caro-Diaz ◽  
...  
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Feature Detection ◽  
Polyketide Synthase ◽  
Biologically Active ◽  
Combinatorial Biosynthesis ◽  
Marine Cyanobacterium ◽  
Natural Product Discovery ◽  
Fragmentation Patterns

The tropical marine cyanobacterium Moorena bouillonii occupies a large geographic range across the Indian and Western Tropical Pacific Oceans and is a prolific producer of structurally unique and biologically active natural products. An ensemble of computational approaches, including the creation of the ORCA (Objective Relational Comparative Analysis) pipeline for flexible MS1 feature detection and multivariate analyses, were used to analyze various M. bouillonii samples. The observed chemogeographic patterns suggested the production of regionally specific natural products by M. bouillonii. Analyzing the drivers of these chemogeographic patterns allowed for the identification, targeted isolation, and structure elucidation of a regionally specific natural product, doscadenamide A (1). Analyses of MS2 fragmentation patterns further revealed this natural product to be part of an extensive family of herein annotated, proposed natural structural analogs (doscadenamides B–J, 2–10); the ensemble of structures reflect a combinatorial biosynthesis using nonribosomal peptide synthetase (NRPS) and polyketide synthase (PKS) components. Compound 1 displayed synergistic in vitro cancer cell cytotoxicity when administered with lipopolysaccharide (LPS). These discoveries illustrate the utility in leveraging chemogeographic patterns for prioritizing natural product discovery efforts.

scholarly journals Recent advancements in synthetic methodologies of 3-substituted phthalides and their application in the total synthesis of biologically active natural products

RSC Advances ◽  
2020 ◽  
Vol 10 (21) ◽  
pp. 12626-12652 ◽  
Author(s):  
Amardeep Awasthi ◽  
Mandeep Singh ◽  
Garima Rathee ◽  
Ramesh Chandra
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Natural Product ◽  
Contextual Information ◽  
Natural Product Synthesis ◽  
Biologically Active ◽  
Synthetic Methodologies ◽  
Active Natural

We have provided contextual information on the chemistry of 3-substituted phthalides and their significance in natural product synthesis.

Computer-Assisted Drug Virtual Screening Based on the Natural Product Databases

2019 ◽  
Vol 20 (4) ◽  
pp. 293-301 ◽  
Author(s):  
Baoyu Yang ◽  
Jing Mao ◽  
Bing Gao ◽  
Xiuli Lu
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Virtual Screening ◽  
Small Molecules ◽  
Natural Product ◽  
Drug Screening ◽  
Biologically Active ◽  
Computer Assisted ◽  
Toxicity Prediction ◽  
Protein Target

Background:Computer-assisted drug virtual screening models the process of drug screening through computer simulation technology, by docking small molecules in some of the databases to a certain protein target. There are many kinds of small molecules databases available for drug screening, including natural product databases.Methods:Plants have been used as a source of medication for millennia. About 80% of drugs were either natural products or related analogues by 1990, and many natural products are biologically active and have favorable absorption, distribution, metabolization, excretion, and toxicology.Results:In this paper, we review the natural product databases’ contributions to drug discovery based on virtual screening, focusing particularly on the introductions of plant natural products, microorganism natural product, Traditional Chinese medicine databases, as well as natural product toxicity prediction databases.Conclusion:We highlight the applications of these databases in many fields of virtual screening, and attempt to forecast the importance of the natural product database in next-generation drug discovery.

A hybrid approach to new molecular scaffolds

2013 ◽  
Vol 85 (6) ◽  
pp. 1185-1202 ◽  
Author(s):  
Kalanidhi Palanichamy ◽  
Krishna P. Kaliappan
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Hybrid Approach ◽  
Biologically Active ◽  
Cycloaddition Reactions ◽  
Molecular Scaffolds ◽  
Biological Features ◽  
Key Steps ◽  
Hybrid Scaffolds ◽  
Active Natural

Our various efforts toward the synthesis of a set of novel sugar hybrid scaffolds of several biologically active natural products such as taxol, steroids, β-lactams, and otteliones are presented. We have shown the application of the hybrid approach to design and rapidly generate a library of novel natural product-like compounds, which may have interesting biological features, using metathesis and/or cycloaddition reactions as key steps.

scholarly journals Accessing Nature’s diversity through metabolic engineering and synthetic biology

F1000Research ◽  
2016 ◽  
Vol 5 ◽  
pp. 397 ◽  
Author(s):  
Jason R. King ◽  
Steven Edgar ◽  
Kangjian Qiao ◽  
Gregory Stephanopoulos
Keyword(s):  
Natural Products ◽  
Metabolic Engineering ◽  
Synthetic Biology ◽  
Natural Product ◽  
Chemical Space ◽  
Single Step ◽  
Enzyme Engineering ◽  
Biologically Active ◽  
Combinatorial Biosynthesis ◽  
Pathway Engineering

In this perspective, we highlight recent examples and trends in metabolic engineering and synthetic biology that demonstrate the synthetic potential of enzyme and pathway engineering for natural product discovery. In doing so, we introduce natural paradigms of secondary metabolism whereby simple carbon substrates are combined into complex molecules through “scaffold diversification”, and subsequent “derivatization” of these scaffolds is used to synthesize distinct complex natural products. We provide examples in which modern pathway engineering efforts including combinatorial biosynthesis and biological retrosynthesis can be coupled to directed enzyme evolution and rational enzyme engineering to allow access to the “privileged” chemical space of natural products in industry-proven microbes. Finally, we forecast the potential to produce natural product-like discovery platforms in biological systems that are amenable to single-step discovery, validation, and synthesis for streamlined discovery and production of biologically active agents.

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