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Microwave-Assisted Extraction of Phenolic Compounds and Antioxidants for Cosmetic Applications Using Polyol-Based Technology
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Chemically engineered extracts: source of bioactive compounds.

I Ayelen Ramallo1, Mario O Salazar, Luciana Mendez

  • 1Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Instituto de Química de Rosario, Argentina.

Accounts of Chemical Research
|March 2, 2011
PubMed
Summary
This summary is machine-generated.

Chemically engineering natural product mixtures creates novel compounds with diverse biological activities. This approach enhances drug discovery by diversifying molecular scaffolds and generating new lead compounds.

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A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
07:59

A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products

Published on: October 4, 2019

Area of Science:

  • Medicinal Chemistry
  • Natural Products Chemistry
  • Drug Discovery

Background:

  • Natural products are privileged scaffolds in drug discovery due to their evolutionary refinement.
  • Distinguishing structural properties exist between natural and synthetic compounds, including chiral centers and heteroatom content.
  • Recurring natural product scaffolds offer unique bioactivity not found in current drugs.

Purpose of the Study:

  • To prepare libraries of semisynthetic compounds, termed chemically engineered extracts (CEEs), via diversification of natural product mixtures.
  • To explore the chemical modification of common reactive fragments in natural products to alter extract composition.
  • To investigate the generation of novel biological activities through chemical diversification.

Main Methods:

  • Identification of common reactive functional groups in natural products using the Dictionary of Natural Products.
  • Chemical transformation of natural product mixtures to incorporate nitrogen, sulfur, and bromine.
  • Isolation and characterization of bioactive compounds from the resulting CEEs.

Main Results:

  • CEEs exhibited altered composition and biomolecular properties compared to parent natural products.
  • A semisynthetic β-glucosidase inhibitor was isolated from a CEE derived from reaction with benzenesulfonyl chloride.
  • An antifungal pyrazole and an acetylcholinesterase inhibitor were identified from CEEs generated using hydrazine and bromination, respectively.

Conclusions:

  • Chemical diversification of natural product mixtures can generate novel biological activities.
  • The CEE approach offers a powerful strategy for library preparation in drug discovery.
  • Judicious experimental design allows for control and potential development of CEEs for research and therapeutic applications.