Related Experiment Video
Updated: May 1, 2026
07:14
Ookluc: A Plasmodium berghei Line for Identifying Transmission-blocking Compounds
Published on: July 11, 2025
578
Potential antimalarial derivatives from astraodorol
Pitak Nasomjai1, Kittibhorn Arpha, Sirirath Sodngam
1Natural Products Research Unit, Centre of Excellence for Innovation in Chemistry, Department of Chemistry, Faculty of Science, Khon Kaen University, Khon Kaen, 40002, Thailand, nphita@kku.ac.th.
Archives of Pharmacal Research
|April 22, 2014
Summary
Modified Astraodorol compounds from Astraeus odoratus show potent antimalarial activity. Several derivatives displayed significant efficacy against malaria parasites, with some also exhibiting moderate cytotoxicity against cancer cell lines.
Area of Science:
- Natural Product Chemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Astraodorol, a lanostane-type triterpene from Astraeus odoratus, is a potential lead compound.
- Triterpenes are known for diverse biological activities, including antimalarial properties.
Purpose of the Study:
- To synthesize novel Astraodorol derivatives.
- To evaluate the antimalarial and cytotoxic activities of these derivatives.
Main Methods:
- Chemical synthesis of ten Astraodorol derivatives.
- In vitro evaluation of antimalarial activity using IC50 values.
- In vitro assessment of cytotoxicity against various cancer and normal cell lines (NCI-H187, KB, MCF-7, Vero).
Main Results:
- Seven derivatives (compounds 5, 6, 7a, 7c, 7e, 7f, 7g) showed strong antimalarial activity (IC50 values ranging from 3.23 to 4.85 µg/mL).
- Compounds 7a, 7c, and 7e exhibited moderate cytotoxicity against NCI-H187 cells (IC50 values 9.84–34.28 µg/mL).
- Compound 7e displayed moderate cytotoxicity against KB, MCF-7, and Vero cell lines (IC50 values 16.94–49.60 µg/mL).
Conclusions:
- Chemical modification of Astraodorol yields potent antimalarial compounds.
- Derivative 7e shows a promising balance of antimalarial activity and moderate cytotoxicity, warranting further investigation.
Related Concept Videos
01:15Anthelminthic Agents
103
Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
103
01:11Aryldiazonium Salts to Azo Dyes: Diazo Coupling
3.2K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
3.2K
01:15Antifungal Agents
119
Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to...
119
01:29Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
3.2K
Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
3.2K
01:16Adrenergic Agonists: Chemistry and Structure-Activity Relationship
3.9K
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
3.9K
01:19Antiasthma Drugs: Leukotriene Modifiers
2.2K
Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Leukotriene modifiers work through two distinct mechanisms:
2.2K