In the search for toxic compounds against Aedes aegypti L. (Diptera: Culicidae) larvae, a collection of commercially available aromatic and aliphatic diversely substituted compounds were selected and evaluated. p-Cymene exhibited the highest larvicidal potency LC₅₀ = 51 ppm, whereas 1,8-cineole exhibited the lowest activity value LC₅₀ = 1419 ppm. To aid future work on the search for larvicidal compounds, the structure-toxicity relationships of this collection have been evaluated. The presence of lipophilic groups results in an overall increase in potency. In general, the presence of hydroxyl groups resulted in less potent compounds. However, methylation of such hydroxyls led to an overall increase in potency. The most potent compounds showed comparably good larvicidal activity in A. aegypti larvae as other terpenes, which we assume to be the result of the increased lipophilicity.

Download full-text PDF

Source
http://dx.doi.org/10.1089/vbz.2009.0158DOI Listing

Publication Analysis

Top Keywords

structure-toxicity relationships
8
compounds aedes
8
aedes aegypti
8
aegypti larvae
8
increase potency
8
potent compounds
8
compounds
6
toxic effects
4
effects structure-toxicity
4
relationships phenylpropanoids
4

Similar Publications

Enhancing toxicity prediction for natural products in herbal medicine and dietary supplements: Integrating (Q)STR models and in vitro assays.

Toxicol Appl Pharmacol

December 2024

Department of Predictive Toxicology, Korea Institute of Toxicology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, Republic of Korea; Department of Human and Environmental Toxicology, University of Science and Technology, Daejeon, Republic of Korea; Department of Environmental Health, Harvard T.H. Chan School of Public Health, Boston, MA, USA. Electronic address:

New approach methods (NAMs) are required to predict human toxicity effectively, particularly due to limitations in conducting in vivo studies. While NAMs have been established for various industries, such as cosmetics, pesticides, and drugs, their applications in natural products (NPs) are lacking. NPs' complexity (multiple ingredients and structural differences from synthetic compounds) complicates NAM development.

View Article and Find Full Text PDF

Toxicity assessment and i-QSTTR analysis of ionic liquids on D. magna, D. rerio, and R. subcapitata.

Sci Total Environ

December 2024

School of Pharmacy, Lanzhou University, Lanzhou 730000, China; Hubei Key Laboratory of Environmental and Health Effects of Persistent Toxic Substances, School of Environment and Health, Jianghan University, Wuhan 430056, China. Electronic address:

The study aimed to assess the impacts of ionic liquids (ILs) as innovative alternatives to traditional organic solvents on aquatic environments and human health. Five machine learning methods, including multiple linear regression (MLR), partial least squares regression (PLS), random forest regression (RF), support vector regression (SVR), and extreme gradient boosting (XGBoost), were used to construct the prediction models of the toxicity of ILs to D. magna, D.

View Article and Find Full Text PDF

In vitro nephrotoxicity and structure-toxicity relationships of eight natural aristolactams.

Toxicon

December 2024

Department of Natural Medicine, School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address:

Article Synopsis
  • - The study investigates the nephrotoxic effects of eight natural aristolactams (ALs) on HK-2 human kidney cells, highlighting their structural similarities to aristolochic acids (AAs), which raises safety concerns due to wider distribution of ALs in plants.
  • - Results from MTT and ELISA assays indicate that all tested ALs exhibit nephrotoxicity, with AL Ⅰ, AL BⅡ, and velutinam showing the strongest cytotoxic effects, while structure-toxicity relationships reveal key functional groups influencing their toxicity levels.
  • - The study found that the most harmful ALs not only cause increased kidney injury marker levels (KIM-1) and oxidative stress but also promote fibrosis
View Article and Find Full Text PDF

Structural toxicity relationship (STR) of linezolid to mitigate myelosuppression and serotonergic toxicity.

Bioorg Med Chem

November 2024

Division of Computer Aided Drug Design, Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule 425405, Maharashtra, India. Electronic address:

Article Synopsis
  • * Linezolid is an effective drug in the BPaL regimen for treating these resistant TB strains, but its use can be limited due to side effects like myelosuppression and MAO inhibition.
  • * Research is focusing on modifying Linezolid and its analogues to reduce toxic effects while maintaining their antibacterial effectiveness, leading to the development of safer alternatives for treating drug-resistant TB.
View Article and Find Full Text PDF

First Report on Cationic Triphenylphosphonium Compounds as Mitochondriotropic HR Ligands with Antioxidant Properties.

Antioxidants (Basel)

November 2024

Departamento de Farmacia, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Santiago 7820436, Chile.

Article Synopsis
  • - Neurodegenerative diseases are increasingly prevalent, prompting research for new treatments; a series of six novel compounds were synthesized to target mitochondrial oxidative stress and show potential as therapeutic agents.
  • - These compounds displayed varying affinities for their target, with one compound achieving notable affinity comparable to an existing drug, and demonstrated antioxidant properties, although their effectiveness was only low to moderate.
  • - The research included evaluation of these compounds' effects on neuroblastoma cells, revealing a clear link between chemical structure and toxicity, alongside computational studies aimed at refining their design for better therapeutic utility.
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!