Abstract
Plants are one of the most important resources for the discovery of new drugs. The potential of natural compounds as new drug leads is clearly illustrated by the discovery and development of many modern medicines. This is an encouraging factor that drives natural products research in the vegetable kingdom. Neocryptolepine is a tetracyclic nitrogen heterocycle isolated from the African climber Cryptolepis sanguinolenta, which is widely used in traditional African medicine in many countries of Central and West Africa. The natural product is one of the representative examples of the small family of indolo[2,3-b]quinoline alkaloids, being endowed of multiple biological activities, including DNA-binding and inhibition of the enzyme topoisomerase II. It is also cytotoxic, antibacterial, antifungal and molluscicidal, also displaying antiprotozoal activity, particularly as antitrypanosomal, antileishmanial, antischistosomal and antiplasmodial. Some of these activities have been related to the product’s ability to bind to DNA and to inhibit topoisomerase II; however, the exact mechanisms behind all of the observed bioactivities have not been comprehensively clarified. Major research activities regarding neocryptolepine have been focused into two seemingly opposite fields, related to its cytotoxic and antimalarial properties. Optimization of the natural product as a cytotoxic agent implied improvements in its bioavailability and activity, while the need of non-cytotoxic compounds guided the design and optimization of antimalarial agents. Therefore, the aim of the present article is to systematically review the current knowledge about the diversity of the biological activities related to neocryptolepine, its analogs and derivatives.
Keywords: Antimalarial activity, Bioactive natural product derivatives, Cytotoxicity, DNA binding compounds, Neocryptolepine (cryptotakieine).
Current Topics in Medicinal Chemistry
Title:Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
Volume: 15 Issue: 17
Author(s): Enrique L. Larghi, Andrea B. J. Bracca, Abel A. Arroyo Aguilar, Daniel A. Heredia, Jorgelina L. Pergomet, Sebastian O. Simonetti and Teodoro S. Kaufman
Affiliation:
Keywords: Antimalarial activity, Bioactive natural product derivatives, Cytotoxicity, DNA binding compounds, Neocryptolepine (cryptotakieine).
Abstract: Plants are one of the most important resources for the discovery of new drugs. The potential of natural compounds as new drug leads is clearly illustrated by the discovery and development of many modern medicines. This is an encouraging factor that drives natural products research in the vegetable kingdom. Neocryptolepine is a tetracyclic nitrogen heterocycle isolated from the African climber Cryptolepis sanguinolenta, which is widely used in traditional African medicine in many countries of Central and West Africa. The natural product is one of the representative examples of the small family of indolo[2,3-b]quinoline alkaloids, being endowed of multiple biological activities, including DNA-binding and inhibition of the enzyme topoisomerase II. It is also cytotoxic, antibacterial, antifungal and molluscicidal, also displaying antiprotozoal activity, particularly as antitrypanosomal, antileishmanial, antischistosomal and antiplasmodial. Some of these activities have been related to the product’s ability to bind to DNA and to inhibit topoisomerase II; however, the exact mechanisms behind all of the observed bioactivities have not been comprehensively clarified. Major research activities regarding neocryptolepine have been focused into two seemingly opposite fields, related to its cytotoxic and antimalarial properties. Optimization of the natural product as a cytotoxic agent implied improvements in its bioavailability and activity, while the need of non-cytotoxic compounds guided the design and optimization of antimalarial agents. Therefore, the aim of the present article is to systematically review the current knowledge about the diversity of the biological activities related to neocryptolepine, its analogs and derivatives.
Export Options
About this article
Cite this article as:
Larghi L. Enrique, Bracca B. J. Andrea, Arroyo Aguilar A. Abel, Heredia A. Daniel, Pergomet L. Jorgelina, Simonetti O. Sebastian and Kaufman S. Teodoro, Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs, Current Topics in Medicinal Chemistry 2015; 15 (17) . https://dx.doi.org/10.2174/1568026615666150427113937
DOI https://dx.doi.org/10.2174/1568026615666150427113937 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...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
- Announcements
Related Articles
-
SARS-CoV-2 and its Predicted Potential Natural Inhibitors: A Review and Perspective
Coronaviruses Diagnostic Stewardship in Times of COVID-19 Pandemic
Infectious Disorders - Drug Targets Inhibitors of the Mitochondrial Electron Transport Chain and de novo Pyrimidine Biosynthesis as Antimalarials: The Present Status
Current Medicinal Chemistry The Family B1 GPCR: Structural Aspects and Interaction with Accessory Proteins
Current Drug Targets Editorial [Hot Topic: NMDA Receptors as Targets in Medicinal Chemistry (Guest Editor: Dr. William Metz)]
Current Topics in Medicinal Chemistry Typical and Atypical Imaging Findings of Abdominal Teratomas
Current Medical Imaging Recent Structure-Activity Studies of the Peptide Hormone Urotensin-II, a Potent Vasoconstrictor
Current Medicinal Chemistry Effects of Highly Active Antiretroviral Therapy on HIV-1-Associated Oral Complications
Current HIV Research Patent Selections:
Recent Patents on Anti-Infective Drug Discovery The Etiology of Hypertension in the Metabolic Syndrome Part Two: The Gene-Environment Interaction
Current Vascular Pharmacology Antagonism by Bioactive Polyphenols Against Inflammation: A Systematic View
Inflammation & Allergy - Drug Targets (Discontinued) Recent Developments of Solid State Detectors for Medical Imaging Applications
Recent Patents on Medical Imaging Patents in Targets and Drugs for Unbalanced Cytokine and Chemokine Network Mediated Disorders
Recent Patents on Inflammation & Allergy Drug Discovery Identification of Antifungal Agents Using Combinatorial Approach: An Overview$
Current Medicinal Chemistry - Anti-Infective Agents Endothelial Chemokines in Autoimmune Disease
Current Pharmaceutical Design Regulatory Strategies for Cell Death in Neurological Diseases
CNS & Neurological Disorders - Drug Targets Recent Findings Confirm LIM Domain Kinases as Emerging Target Candidates for Cancer Therapy
Current Cancer Drug Targets Technology-Dependent Children: The Chronically Ventilated Child
Current Pediatric Reviews Some Implications of Receptor Kinase Signaling Pathway for Development of Multitargeted Kinase Inhibitors
Current Radiopharmaceuticals Challenges of Covid-19 on Adolescent Psychiatric Service Provision in an Independent Inpatient and Outpatient Setting
Adolescent Psychiatry