The untapped potential of plant sesterterpenoids: chemistry, biological activities and biosynthesis

2021 ◽  
Author(s):  
Kai Guo ◽  
Yan Liu ◽  
Sheng-Hong Li
Keyword(s):  
Natural Product ◽  
Biological Activities ◽  
Product Class

An overall coverage of plant sesterterpenoids including the distribution, chemistry, biological activities, biosynthesis and evolution is provided, highlighting the untapped potential of this enigmatic but promising natural product class in plants.

scholarly journals Exploration of marine natural resources in Indonesia and development of efficient strategies for the production of microbial halogenated metabolites

2021 ◽  
Author(s):  
Hiroyuki Yamazaki
Keyword(s):  
Natural Product ◽  
Protein Tyrosine Phosphatase ◽  
Biological Activities ◽  
Tyrosine Phosphatase ◽  
Osteoblastic Differentiation ◽  
Biological Properties ◽  
Protein Tyrosine Phosphatase 1B ◽  
Productive Performance ◽  
Halogenated Metabolites ◽  
Morphogenetic Protein

AbstractNature is a prolific source of organic products with diverse scaffolds and biological activities. The process of natural product discovery has gradually become more challenging, and advances in novel strategic approaches are essential to evolve natural product chemistry. Our focus has been on surveying untouched marine resources and fermentation to enhance microbial productive performance. The first topic is the screening of marine natural products isolated from Indonesian marine organisms for new types of bioactive compounds, such as antineoplastics, antimycobacterium substances, and inhibitors of protein tyrosine phosphatase 1B, sterol O-acyl-transferase, and bone morphogenetic protein-induced osteoblastic differentiation. The unique biological properties of marine organohalides are discussed herein and attempts to efficiently produce fungal halogenated metabolites are documented. This review presents an overview of our recent work accomplishments based on the MONOTORI study. Graphic abstract

scholarly journals A First Approach to the Chemical Composition and Antioxidant Potential of Guinea-Bissau Propolis

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984413 ◽  
Author(s):  
Soraia I. Falcão ◽  
Mélissa Lopes ◽  
Miguel Vilas-Boas
Keyword(s):  
Antioxidant Activity ◽  
Chemical Composition ◽  
Physicochemical Properties ◽  
Natural Product ◽  
Broad Spectrum ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Antioxidant Potential ◽  
Phenolic Composition ◽  
First Time

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.

scholarly journals Natural Product Repertoire of the Genus Amphimedon

Marine Drugs ◽  
2018 ◽  
Vol 17 (1) ◽  
pp. 19 ◽  
Author(s):  
Nourhan Shady ◽  
Mostafa Fouad ◽  
Mohamed Salah Kamel ◽  
Tanja Schirmeister ◽  
Usama Abdelmohsen
Keyword(s):  
Secondary Metabolites ◽  
Natural Product ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Marine Sponges ◽  
Rich Source ◽  
Undescribed Species ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Complete Survey

Marine sponges are a very attractive and rich source in the production of novel bioactive compounds. The sponges exhibit a wide range of pharmacological activities. The genus Amphimedon consists of various species, such as viridis, compressa, complanata, and terpenensis, along with a handful of undescribed species. The Amphimedon genus is a rich source of secondary metabolites containing diverse chemical classes, including alkaloids, ceramides, cerebrososides, and terpenes, with various valuable biological activities. This review covers the literature from January 1983 until January 2018 and provides a complete survey of all the compounds isolated from the genus Amphimedon and the associated microbiota, along with their corresponding biological activities, whenever applicable.

scholarly journals Vicinal difluorination as a C=C surrogate: an analog of piperine with enhanced solubility, photostability, and acetylcholinesterase inhibitory activity

2020 ◽  
Author(s):  
Yuvixza Lizarme-Salas ◽  
Alexandra Daryl Ariawan ◽  
Ranjala Ratnayake ◽  
Hendrik Luesch ◽  
Angela Finch ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Natural Product ◽  
Inhibitory Activity ◽  
Drug Target ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Aqueous Solubility ◽  
Hydrocarbon Chain ◽  
Lead Compound ◽  
Enhanced Solubility

Piperine, a natural product derived from peppercorns, has a variety of biological activities that make it an attractive lead compound for medicinal chemistry. However, piperine has some problematic physicochemical properties including poor aqueous solubility and a susceptibility to UV-induced degradation. In this work, we designed an analog of piperine in which the central conjugated hydrocarbon chain is replaced with a vicinal difluoroalkane moiety. We show that this fluorinated analog of piperine has superior physicochemical properties, and it also has higher potency and selectivity towards one particular drug target, acetylcholinesterase. This work highlights the potential usefulness of the threo-difluoroalkane motif as a surrogate for E-alkenes in medicinal chemistry.

scholarly journals Making drugs out of sunlight and ‘thin air’: an emerging synergy of synthetic biology and natural product chemistry

2020 ◽  
Vol 42 (4) ◽  
pp. 34-39
Author(s):  
Michael J. Stephenson ◽  
Anne Osbourn
Keyword(s):  
Natural Products ◽  
Synthetic Biology ◽  
Natural Product ◽  
Large Scale ◽  
Production Systems ◽  
Biological Activities ◽  
Structural Complexity ◽  
Scale Production ◽  
Natural Product Chemistry ◽  
Product Chemistry

Nature has long served as a rich source of structurally diverse small organic molecules with medicinally relevant biological activities. Despite the historical success of these so-called natural products, the enthusiasm of big pharma to explore these compounds as leads in drug design has waxed and waned. A major contributor to this is their often inherent structural complexity. Such compounds are difficult (often impossible) to access synthetically, a hurdle that can stifle lead development and hinder sustainable large-scale production of promising leads for clinical evaluation. However, in recent years, an emerging synergy between synthetic biology and natural product chemistry offers the potential for a renaissance in our ability to access natural products for drug discovery and development. Advances in genome sequencing, bioinformatics and the maturing of heterologous expression platforms are increasing, enabling the study, and ultimately, the manipulation of plant biosynthetic pathways. The triterpenes are one of the most structurally diverse families of natural products and arguably one of the most underrepresented in the clinic. The plant kingdom is the richest source of triterpene diversity, with >20,000 triterpenes reported so far. Transient expression of genes for candidate enzymes and pathways in amenable plant species is emerging as a powerful and rapid means of investigating and harnessing the plant enzymes involved in generating this diversity. Such platforms also have the potential to serve as production systems in their own right, with the possibility of upscaling these discoveries into commercially useful products using the same overall basic procedure. Ultimately, the carbon source for generation of high-value compounds in plants is photosynthesis. Therefore, we could, with the help of plants, be producing new medicines out of sunlight and ‘thin air’ in green factories in the not too distant future.

scholarly journals Parthenin—A Sesquiterpene Lactone with Multifaceted Biological Activities: Insights and Prospects

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5347
Author(s):  
Amarpreet Kaur ◽  
Shalinder Kaur ◽  
Rupali Jandrotia ◽  
Harminder Singh ◽  
Daizy Batish ◽  
...  
Keyword(s):  
Natural Product ◽  
Sesquiterpene Lactone ◽  
Secondary Metabolite ◽  
Biological Activities ◽  
Present Review ◽  
Parthenium Hysterophorus ◽  
Medicinal Properties ◽  
Scientific Fields ◽  
Comprehensive Discussion

Parthenin, a sesquiterpene lactone of pseudoguaianolide type, is the representative secondary metabolite of the tropical weed Parthenium hysterophorus (Asteraceae). It accounts for a multitude of biological activities, including toxicity, allergenicity, allelopathy, and pharmacological aspects of the plant. Thus far, parthenin and its derivatives have been tested for chemotherapeutic abilities, medicinal properties, and herbicidal/pesticidal activities. However, due to the lack of toxicity–bioactivity relationship studies, the versatile properties of parthenin are relatively less utilised. The possibility of exploiting parthenin in different scientific fields (e.g., chemistry, medicine, and agriculture) makes it a subject of analytical discussion. The present review highlights the multifaceted uses of parthenin, on-going research, constraints in the practical applicability, and the possible workarounds for its successful utilisation. The main aim of this comprehensive discussion is to bring parthenin to the attention of researchers, pharmacologists, natural product chemists, and chemical biologists and to open the door for its multidimensional applications.

scholarly journals Di-2-ethylhexylphthalate May Be a Natural Product, Rather than a Pollutant

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Aurelio Ortiz ◽  
Estibaliz Sansinenea
Keyword(s):  
Natural Product ◽  
Human Health ◽  
Phthalic Acid ◽  
Biological Activities ◽  
Points Of View ◽  
Natural Metabolite

Di-2-ethylhexylphtalate is an ester of phthalic acid that has been used as plasticizer in many materials. Due to the extended use, it has been persistently found in different environments being classified as a pollutant with some risks for human health. However, in the last years, it has been found that this compound is produced by plants or microorganisms like bacteria or fungi. This finding opened a serious debate about the origin of this compound and questioned if it is a real pollutant or a natural metabolite with some biological activities that could help us in several ways. This review tries to give some data of the different points of view about this question.

scholarly journals Synthesis of Multi-Substituted Pyrrole Derivatives Through [3+2] Cycloaddition with Tosylmethyl Isocyanides (TosMICs) and Electron-Deficient Compounds

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2666 ◽  
Author(s):  
Zhengning Ma ◽  
Zicheng Ma ◽  
Dawei Zhang
Keyword(s):  
Natural Product ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Cycloaddition Reaction ◽  
Synthesis Methods ◽  
Pyrrole Derivatives ◽  
The Past ◽  
Different Types ◽  
Product Structures ◽  
Core Framework

Pyrrole and its polysubstituted derivatives are important five-membered heterocyclic compounds, which exist alone or as a core framework in many pharmaceutical and natural product structures, some of which have good biological activities. The Van Leusen [3+2] cycloaddition reaction based on tosylmethyl isocyanides (TosMICs) and electron-deficient compounds as a substrate, which has been continuously developed due to its advantages such as operationally simple, easily available starting materials, and broadly range of substrates, is one of the most convenient methods to synthetize pyrrole heterocycles. In this review, we discuss the different types of two carbon synthons in the Van Leusen pyrrole reaction and give a summary of the progress of these synthesis methods in the past two decades.

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.

A Review on Recent Developments in the Anticancer Potential of Oleanolic acid and its analogs (2017-2020)

2021 ◽  
Vol 21 ◽  
Author(s):  
Nidhi Gupta
Keyword(s):  
Clinical Trials ◽  
Natural Product ◽  
Oleanolic Acid ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Pentacyclic Triterpenoid ◽  
Recent Developments ◽  
Anti Inflammatory ◽  
Pharmaceutical Properties

: Oleanolic acid (OA) is a pentacyclic triterpenoid class of natural product known to possess a broad range of biological activities, specifically, anticancer. Considering the anticancer potential of OA, a large number of analogs have been prepared by several researchers through modifications at C-3, C-12 and C-28 –COOH to develop the potent anticancer agents with improved cytotoxicity and pharmaceutical properties. Some of the synthesized derivatives have been assessed in clinical trials also. This review summarizes the most recent synthetic and biological efforts in the development of oleanolic acid and its analogs during the period 2017-2020. Reports published during this period revealed that both OA and its analogs possess a remarkable potential for the development of effective anticancer agents along with several others such as anti-inflammatory, anti-viral, anti-microbial and anti-diabetic agents.

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