A bioassay for mosquito repellency against Aedes aegypti: method validation and bioactivities of DEET analogues

Title
A bioassay for mosquito repellency against Aedes aegypti: method validation and bioactivities of DEET analogues
Author(s)
용철순김정선[김정선]김석용[김석용]김준호[김준호]김대덕[김대덕]안영준[안영준]얀 알렉산더[얀 알렉산더]
Keywords
INSECT REPELLENTS; FIELD-EVALUATION; ESSENTIAL OILS; LACTIC-ACID; DIPTERA; CULICIDAE; FORMULATIONS; PERMETHRIN; MECHANISMS; EFFICACY
Issue Date
201001
Publisher
WILEY-BLACKWELL PUBLISHING, INC
Citation
JOURNAL OF PHARMACY AND PHARMACOLOGY, v.62, no.1, pp.91 - 97
Abstract
Objectives Vector-borne diseases are still a major mortality factor in Africa and Southeast Asia and effective mosquito repellents are therefore needed. An efficient and safe in-vitro assay system using artificial blood and skin substitute could facilitate the development of novel repellents, as most assays currently rely on human subjects or vertebrate whole blood. Moreover, examining the skin permeation profiles could provide safer mosquito repellents. The new assay system could serve as an initial system for testing new repellent candidates upon validation with DEET and its analogues. Methods N,N-Diethyl-meta-toluamide (DEET) and five analogues were synthesised and used to validate a novel in-vitro bioassay using artificial blood and collagen membrane. Repellency against Aedes aegypti was correlated with lipophilicity and skin permeation. Key findings The new in-vitro assay showed good reproducibility (interday relative standard deviation <10% at high concentrations). Four of the five DEET analogues showed repellency similar or superior to that of DEET. Repellency correlated linearly with lipophilicity but stronger repellents tended to permeate skin better. Conclusions The new in-vitro assay using blood substitute and collagen membrane significantly simplifies screening of possible mosquito repellents. Lipophilicity as well as skin permeation profiles should be considered before testing of compounds that are candidates for mosquito repellents.
URI
http://hdl.handle.net/YU.REPOSITORY/23027http://dx.doi.org/10.1211/jpp/62.01.0010
ISSN
0022-3573
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약학대학 > 약학부 > Articles
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