Biological evaluation of bioavailable amphiphilic polymeric conjugate based-on natural products: diosgenin and curcumin

2019 ◽  
Vol 69 (2) ◽  
pp. 73-84 ◽  
Author(s):  
Sevinc Ilkar Erdagi ◽  
Cavit Uyanik
Keyword(s):  
Natural Products ◽  
Biological Evaluation ◽  
Polymeric Conjugate

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

scholarly journals Natural product fragment combination to performance-diverse pseudo-natural products

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Michael Grigalunas ◽  
Annina Burhop ◽  
Sarah Zinken ◽  
Axel Pahl ◽  
José-Manuel Gally ◽  
...  
Keyword(s):  
Natural Products ◽  
Product Design ◽  
Natural Product ◽  
Chemical Space ◽  
Biological Evaluation ◽  
Product Structure ◽  
Biologically Relevant ◽  
Biologically Relevant Chemical Space

AbstractNatural product structure and fragment-based compound development inspire pseudo-natural product design through different combinations of a given natural product fragment set to compound classes expected to be chemically and biologically diverse. We describe the synthetic combination of the fragment-sized natural products quinine, quinidine, sinomenine, and griseofulvin with chromanone or indole-containing fragments to provide a 244-member pseudo-natural product collection. Cheminformatic analyses reveal that the resulting eight pseudo-natural product classes are chemically diverse and share both drug- and natural product-like properties. Unbiased biological evaluation by cell painting demonstrates that bioactivity of pseudo-natural products, guiding natural products, and fragments differ and that combination of different fragments dominates establishment of unique bioactivity. Identification of phenotypic fragment dominance enables design of compound classes with correctly predicted bioactivity. The results demonstrate that fusion of natural product fragments in different combinations and arrangements can provide chemically and biologically diverse pseudo-natural product classes for wider exploration of biologically relevant chemical space.

scholarly journals The myxocoumarins A and B fromStigmatella aurantiacastrain MYX-030

2013 ◽  
Vol 9 ◽  
pp. 2579-2585 ◽  
Author(s):  
Tobias A M Gulder ◽  
Snežana Neff ◽  
Traugott Schüz ◽  
Tammo Winkler ◽  
René Gees ◽  
...  
Keyword(s):  
Natural Products ◽  
Structure Elucidation ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Antifungal Properties ◽  
Structural Framework ◽  
Stigmatella Aurantiaca ◽  
Promising Source ◽  
Active Natural

The myxobacterial strainStigmatella aurantiacaMYX-030 was selected as promising source for the discovery of new biologically active natural products by our screening methodology. The isolation, structure elucidation and initial biological evaluation of the myxocoumarins derived from this strain are described in this work. These compounds comprise an unusual structural framework and exhibit remarkable antifungal properties.

Total synthesis and biological evaluation of ustiloxin natural products and two analogs

2006 ◽  
Vol 16 (18) ◽  
pp. 4804-4807 ◽  
Author(s):  
Pixu Li ◽  
Cory D. Evans ◽  
Erin M. Forbeck ◽  
Haengsoon Park ◽  
Ruoli Bai ◽  
...  
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and direct comparison of the anticancer activities of phomopsolides D and E and two 7-oxa-/7-aza-analogues

MedChemComm ◽  
2019 ◽  
Vol 10 (7) ◽  
pp. 1205-1211
Author(s):  
Alhanouf Z. Aljahdali ◽  
Seth A. Freedman ◽  
Jana Scott ◽  
Miaosheng Li ◽  
George A. O'Doherty
Keyword(s):  
Natural Products ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Synthesis And Biological Evaluation

The synthesis and biological evaluation of two phomopsolide natural products (D and E) and two analogues is presented.

Synthesis, characterization and in vitro biological evaluation of [Ru(η6-arene)(N,N)Cl]PF6 compounds using the natural products arenes methylisoeugenol and anethole

2015 ◽  
Vol 782 ◽  
pp. 131-137 ◽  
Author(s):  
Ricardo A. Delgado ◽  
Antonio Galdámez ◽  
Joan Villena ◽  
Patricio G. Reveco ◽  
Franz A. Thomet
Keyword(s):  
Natural Products ◽  
Biological Evaluation

Synthesis of Carbohydrate-based Natural Products from Leonurus japonicus and their Biological Evaluation as Anti-oxidants

2014 ◽  
Vol 67 (10) ◽  
pp. 1461 ◽  
Author(s):  
Evette Clayton ◽  
Mitchell Hattie ◽  
Aleksandra W. Debowski ◽  
Keith A. Stubbs
Keyword(s):  
Natural Products ◽  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Biological Evaluation

Natural products are important materials that have found a wide variety of uses, especially in medicine. Traditional Chinese medicine (TCM) has especially taken advantage of natural products and compounds found in Leonurus, a species of herb used extensively in TCM to treat various ailments. Herein we describe the synthesis of three natural products from Leonurus japonicus and our investigation of their hepatoprotective properties.

scholarly journals Profiled tea extracts exemplifying the importance of characterizing food bioactives: opinion piece

2019 ◽  
Vol 5 ◽  
pp. 1-5 ◽  
Author(s):  
Shiming Li ◽  
Alexander Gosslau ◽  
Klaus Lange ◽  
Chi-Tang Ho
Keyword(s):  
Natural Products ◽  
Single Molecule ◽  
Functional Foods ◽  
Biological Effects ◽  
Biological Evaluation ◽  
Therapeutic Agents ◽  
Therapeutic Effects ◽  
Chemical Identification ◽  
Component Identification

Natural products from food and herbs have been used as functional food and medicine for centuries, much earlier than any of the current single molecule drugs in the market. Historically, natural products are the dominant resources of current global pharmaceutical market. Examples include world’s most commonly used drugs such as aspirin, penicillin and taxol. In viewing the increasing attraction and exponentially growing need for functional foods and effective medicines, the potential for natural products to serve as safe and effective preventive and therapeutic agents is of much interest. However, the importance in the phytochemical characterization of plant origin and associated extracts containing multiple phytochemicals in research and product development in this field has been plagued by overwhelmingly focusing on their biological effects. More than often inconsistent and invalid biological results are provided without chemical component identification and validation. Hence it is vital to characterize and identify the ingredients in the plant extracts – food bioactives- that play critical roles in promoting health or having therapeutic effects. The combination of chemical identification and biological evaluation is the key to having valid and consistent results in elucidating health beneficial properties of a plant or its extracts and also a key to have a meaningful comparison among similar studies due to the use of the same standard. Herein, we use tea as examples demonstrating the importance of phytochemical profiling and associated bioactive property of functional foods.

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