Abstract
Sesquiterpene lactones are a large group of secondary plant metabolites mostly known from the Asteraceae family. They exert a broad variety of different biological activities. This review attempts to critically summarise the knowledge on the anti-inflammatory and cytotoxic activity of SLs, with a special focus on parthenolide and helenalin. Recent advances on their molecular modes of action, allergic potential and also QSAR studies with SLs are presented. Therapeutic areas are highlighted in which SLs may play a role in the future. Thus, SLs may possess therapeutic relevance as single components for the local treatment of inflammation, such as rheumatoid complaints. In cancer therapy, SLs may be favourable in dual therapy or in the inhibition of leukaemia cell growth. In each case, native SLs serve as leads that have to be optimised in terms of their specificity, pharmacokinetics and absorption, distribution, metabolism and excretion (=ADME) properties. Finally, appropriate in vivo studies will decide whether SLs will become therapeutics or remain interesting research compounds.
Keywords: Helenalin, parthenolide, artemisinin, NF-κB, apoptosis, molecular mechanisms, sensitising effect, Sesquiterpene, Lactones, cancer
Current Drug Targets
Title: Perspectives on Sesquiterpene Lactones in Inflammation and Cancer
Volume: 12 Issue: 11
Author(s): Irmgard Merfort
Affiliation:
Keywords: Helenalin, parthenolide, artemisinin, NF-κB, apoptosis, molecular mechanisms, sensitising effect, Sesquiterpene, Lactones, cancer
Abstract: Sesquiterpene lactones are a large group of secondary plant metabolites mostly known from the Asteraceae family. They exert a broad variety of different biological activities. This review attempts to critically summarise the knowledge on the anti-inflammatory and cytotoxic activity of SLs, with a special focus on parthenolide and helenalin. Recent advances on their molecular modes of action, allergic potential and also QSAR studies with SLs are presented. Therapeutic areas are highlighted in which SLs may play a role in the future. Thus, SLs may possess therapeutic relevance as single components for the local treatment of inflammation, such as rheumatoid complaints. In cancer therapy, SLs may be favourable in dual therapy or in the inhibition of leukaemia cell growth. In each case, native SLs serve as leads that have to be optimised in terms of their specificity, pharmacokinetics and absorption, distribution, metabolism and excretion (=ADME) properties. Finally, appropriate in vivo studies will decide whether SLs will become therapeutics or remain interesting research compounds.
Export Options
About this article
Cite this article as:
Merfort Irmgard, Perspectives on Sesquiterpene Lactones in Inflammation and Cancer, Current Drug Targets 2011; 12 (11) . https://dx.doi.org/10.2174/138945011798109437
DOI https://dx.doi.org/10.2174/138945011798109437 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Gene Transfer to the Central Nervous System: Current State of the Art of the Viral Vectors
Current Genomics Therapeutic Potential of Adipose-derived Stem Cells in the Treatment of Pulmonary Diseases
Current Stem Cell Research & Therapy Recent Advances in the Development of Catalytic Inhibitors of Human DNA Topoisomerase IIα As Novel Anticancer Agents
Current Medicinal Chemistry Regulation and Function of DNA and Histone Methylations
Current Pharmaceutical Design Gamma-Oryzanol – A Multi-Purpose Steryl Ferulate
Current Nutrition & Food Science Epigenetics and Adult Acute Myeloid Leukemia
Current Pharmacogenomics and Personalized Medicine Advances and Challenges in the Synthesis of Highly Oxidised Natural Phenols with Antiviral, Antioxidant and Cytotoxic Activities
Current Medicinal Chemistry Voltage-Gated Sodium Channels: New Targets in Cancer Therapy?
Current Pharmaceutical Design Direct Gene Expression Analysis
Current Pharmaceutical Biotechnology Cell-in-cell phenomenon: A New Paradigm in Life Sciences.
Current Molecular Medicine Cancer Stem Cells: How can we Target them?
Current Medicinal Chemistry Versatile and Valuable Utilization of Amidohydrolase L-glutaminase in Pharma and Food industries: A Review
Current Drug Metabolism Current Options in the Treatment of Mast Cell Mediator-Related Symptoms in Mastocytosis
Inflammation & Allergy - Drug Targets (Discontinued) Discovering Tumor Suppressor Genes Through Genome-Wide Copy Number Analysis
Current Genomics Harnessing the Tumor Suppressor Function of FOXO as an Alternative Therapeutic Approach in Cancer
Current Drug Targets Paris polyphylla: Chemical and Biological Prospectives
Anti-Cancer Agents in Medicinal Chemistry Amino Acid Derived Prodrugs: An Approach to Improve the Bioavailability of Clinically Approved Drugs
Current Topics in Medicinal Chemistry De Novo Design of New Inhibitor of Mutated Tyrosine-Kinase for the Myeloid Leukemia Treatment
Current Pharmaceutical Design Telomere Maintenance as Therapeutic Target in Embryonal Tumours
Anti-Cancer Agents in Medicinal Chemistry The Role of Tumor Suppressor DLC-1: Far From Clear
Anti-Cancer Agents in Medicinal Chemistry