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Plant-derived Lignans Synthesis and Bioactivity
Research Guide
What is Plant-derived Lignans Synthesis and Bioactivity?
Plant-derived lignans synthesis and bioactivity refers to the biosynthesis pathways in plants producing lignan compounds such as podophyllotoxin, schisandrin, and arctigenin, along with their pharmacological properties including cytotoxicity, anti-inflammatory effects, and therapeutic potential in cancer, neuroprotection, hepatoprotection, and antimicrobial activities.
Research on plant-derived lignans synthesis and bioactivity encompasses 65,660 works with a focus on enzymatic pathways like those mediated by dirigent proteins and compounds from sources including Schisandra chinensis and Arctium lappa. Key studies highlight stereoselective coupling in lignan formation, as shown by Davin et al. (1997) in 'Stereoselective Bimolecular Phenoxy Radical Coupling by an Auxiliary (Dirigent) Protein Without an Active Center,' which demonstrated regio- and stereospecificity controlled by dirigent proteins during biosynthesis. Bioactivity research emphasizes anticancer and antioxidant effects, with arctigenin from burdock exhibiting free-radical scavenging, as reported by Duh (1998) in 'Antioxidant activity of burdock (Arctium lappa Linné): Its scavenging effect on free‐radical and active oxygen.'
Topic Hierarchy
Research Sub-Topics
Podophyllotoxin Biosynthesis and Derivatives
This sub-topic studies enzymatic pathways and genetic regulation of podophyllotoxin in Podophyllum species, plus semisynthetic anticancer derivatives like etoposide. Researchers engineer microbial production and optimize extraction.
Dirigent Proteins in Lignan Coupling
This sub-topic investigates dirigent proteins' role in stereoselective phenoxy radical coupling for lignan biosynthesis. Researchers characterize protein structures and pathway engineering applications.
Schisandrin Pharmacological Activities
This sub-topic examines hepatoprotective, cardioprotective, and neuroprotective effects of schisandrins from Schisandra chinensis. Researchers elucidate mechanisms via Nrf2 activation and phase II detoxification.
Arctigenin Anti-Inflammatory and Anticancer Effects
This sub-topic covers arctigenin's NF-κB inhibition for inflammation and apoptosis induction in cancers from Arctium lappa. Researchers pursue structure-activity relationships and clinical translation.
Lignan Antioxidant Mechanisms
This sub-topic analyzes radical scavenging, metal chelation, and enzyme modulation by dietary lignans like secoisolariciresinol. Researchers correlate bioavailability with oxidative stress protection.
Why It Matters
Plant-derived lignans contribute to cancer treatment through compounds like podophyllotoxin, a precursor to etoposide, which Hande (1998) detailed in 'Etoposide: four decades of development of a topoisomerase II inhibitor' as achieving clinical success with over 40 years of use. Arctigenin from Arctium lappa shows antioxidant activity by scavenging free radicals and active oxygen, with water extracts demonstrating the strongest effects according to Duh (1998) in 'Antioxidant activity of burdock (Arctium lappa Linné): Its scavenging effect on free‐radical and active oxygen.' Anticancer potential is further evidenced by Cragg and Newman (2005) in 'Plants as a source of anti-cancer agents,' which identifies plants as major suppliers of agents like those derived from lignans, and Choudhari et al. (2020) in 'Phytochemicals in Cancer Treatment: From Preclinical Studies to Clinical Practice,' noting transition of such phytochemicals to clinical use amid rising cancer deaths worldwide.
Reading Guide
Where to Start
'Plants as a source of anti-cancer agents' by Cragg and Newman (2005) first, as it provides a broad foundation on plant-derived compounds like lignans serving as anticancer agents with 2012 citations.
Key Papers Explained
Cragg and Newman (2005) in 'Plants as a source of anti-cancer agents' establishes plants as sources for lignan precursors like podophyllotoxin, which Hande (1998) in 'Etoposide: four decades of development of a topoisomerase II inhibitor' builds on by detailing etoposide's clinical development from such lignans. Davin et al. (1997) in 'Stereoselective Bimolecular Phenoxy Radical Coupling by an Auxiliary (Dirigent) Protein Without an Active Center' explains the biosynthetic mechanism via dirigent proteins, underpinning synthesis of these compounds. Duh (1998) in 'Antioxidant activity of burdock (Arctium lappa Linné): Its scavenging effect on free‐radical and active oxygen' extends to bioactivity of arctigenin from Arctium lappa, connecting biosynthesis to antioxidant applications.
Paper Timeline
Most-cited paper highlighted in red. Papers ordered chronologically.
Advanced Directions
Current research emphasizes dirigent protein roles in stereoselective lignan synthesis from Davin et al. (1997) and bioactivity in cancer via podophyllotoxin derivatives as in Hande (1998), with exploration of enzymatic pathways for schisandrin and arctigenin. The field covers cytotoxicity and anti-inflammatory effects across 65,660 works, focusing on plant sources like Schisandra chinensis and Arctium lappa.
Papers at a Glance
| # | Paper | Year | Venue | Citations | Open Access |
|---|---|---|---|---|---|
| 1 | Plants as a source of anti-cancer agents | 2005 | Journal of Ethnopharma... | 2.0K | ✓ |
| 2 | Phytochemicals in Cancer Treatment: From Preclinical Studies t... | 2020 | Frontiers in Pharmacology | 988 | ✓ |
| 3 | Phytochemistry of the genus Piper | 1997 | Phytochemistry | 945 | ✕ |
| 4 | Etoposide: four decades of development of a topoisomerase II i... | 1998 | European Journal of Ca... | 927 | ✕ |
| 5 | Immunomodulation and Anti-Cancer Activity of Polysaccharide-Pr... | 2000 | Current Medicinal Chem... | 864 | ✕ |
| 6 | Stereoselective Bimolecular Phenoxy Radical Coupling by an Aux... | 1997 | Science | 735 | ✕ |
| 7 | Antioxidant Effects of Some Ginger Constituents | 1993 | Journal of Food Science | 718 | ✕ |
| 8 | Natural products for cancer chemotherapy | 2010 | Microbial Biotechnology | 714 | ✓ |
| 9 | Antioxidant activity of burdock (<i>Arctium lappa</i> Linné): ... | 1998 | Journal of the America... | 677 | ✕ |
| 10 | The Role of Polyphenols in Abiotic Stress Response: The Influe... | 2021 | Plants | 615 | ✓ |
Frequently Asked Questions
What role do dirigent proteins play in lignan biosynthesis?
Dirigent proteins control regio- and stereospecificity in bimolecular phenoxy radical coupling during lignan biosynthesis without an active center. Davin et al. (1997) in 'Stereoselective Bimolecular Phenoxy Radical Coupling by an Auxiliary (Dirigent) Protein Without an Active Center' showed they produce stereoselective products unlike racemic mixtures from laccases alone. This mechanism is essential for lignin and lignan formation in plants.
How do lignans from Arctium lappa exhibit antioxidant activity?
Water extracts of Arctium lappa (burdock) yield the greatest extract amount with the strongest antioxidant activity, scavenging free radicals and active oxygen. Duh (1998) in 'Antioxidant activity of burdock (Arctium lappa Linné): Its scavenging effect on free‐radical and active oxygen' confirmed hot water extracts as particularly effective. This supports their use in medicinal applications.
What is the connection between podophyllotoxin and cancer treatment?
Podophyllotoxin from plants serves as a precursor to etoposide, a topoisomerase II inhibitor used in chemotherapy. Hande (1998) in 'Etoposide: four decades of development of a topoisomerase II inhibitor' outlined its development and clinical application over four decades. Plants remain key sources for such anticancer agents per Cragg and Newman (2005).
Which plant sources are prominent in lignan research?
Prominent sources include Schisandra chinensis for schisandrin, Arctium lappa for arctigenin, and plants yielding podophyllotoxin. Keywords in the field highlight these alongside Arctium lappa and medicinal plants. Cragg and Newman (2005) in 'Plants as a source of anti-cancer agents' emphasize plants as primary suppliers of lignan-derived anticancer compounds.
What bioactivities are associated with plant-derived lignans?
Lignans display cytotoxicity, anti-inflammatory, antioxidant, anticancer, neuroprotective, hepatoprotective, and antimicrobial activities. Choudhari et al. (2020) in 'Phytochemicals in Cancer Treatment: From Preclinical Studies to Clinical Practice' link them to cancer progression mechanisms. The field covers 65,660 works on these pharmacological effects.
Open Research Questions
- ? How do dirigent proteins achieve stereoselectivity in lignan coupling without enzymatic active sites?
- ? What enzymatic pathways optimize podophyllotoxin yield from plant sources for etoposide production?
- ? Which lignan structures from Schisandra chinensis and Arctium lappa best confer neuroprotective and hepatoprotective effects?
- ? How do gut microbiota interactions modulate lignan bioactivity in therapeutic contexts?
- ? What modifications enhance lignan cytotoxicity against specific cancer types via topoisomerase inhibition?
Recent Trends
The field comprises 65,660 works on lignan biosynthesis and bioactivity, with high-citation papers like Cragg and Newman at 2012 citations underscoring sustained interest in plant anticancer agents.
2005Choudhari et al. with 988 citations reflects recent preclinical-to-clinical transitions for phytochemicals including lignans.
2020No preprints or news from the last 12 months available, indicating steady focus on established pathways like dirigent protein-mediated coupling from Davin et al. .
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