Background <p>The prevalence of malaria and other mosquito menace in Lagos State and many other parts of Nigeria has becomes so alarming. <i>Citrus limon</i> seeds have limited exploration, unlike the leaves, juice and the peels which are burnt as repellent and have been widely explored. This study was conducted to evaluate the repellent and cytotoxic effects of three known lipids, a known flavonoid and a novel fatty acid isolated from the n-hexane fraction <i>C. limon</i>.</p> Methods <p>The structures of the compounds were determined based on spectroscopic (IR, 1-D, 2-D NMR) and mass spectrometric experiments. Isolated compounds were evaluated for cytotoxicity and <i>Anopheles gambiae</i> mosquito repellent effects, using brine shrimp lethality assay (safety cut-off, LC<sub>50</sub> &gt; 100&#xa0;µg/mL), and human bait method, respectively, while N,N-diethyl-meta-toluamide (DEET) and acetone were used as positive and negative controls, respectively. Repellent activity data were analysed using one-way ANOVA at α<sub>0.05</sub>.</p> Results <p>Compounds 1–5 identification gave, Palmitic acid (1), 14-Oxotricosanoic acid (2), n-Octyl stearate (3), 4-heptadec-7-enyloxy)carbonyl)butanoic acid (4) and 6,8 dimethoxy-3-undecyl-1H-[2]benzopyran-1-one (5). Compounds (1, 2 and 4) showed some level of toxicity with LC<sub>50</sub> values less than 100&#xa0;µg/mL, while compounds 3 and 5 are considered safe because of their LC<sub>50</sub> values, that are greater than 100&#xa0;µg/mL. Compound 4 and 5 are the most promising mosquito repellent agents at 5&#xa0;mg/mL optimum concentration with repellencies of 77.87% and 75.15%, respectively, as compared to the standard, DEET (100%).</p> Conclusion <p>The results offer additional scientific justification for the local usage of <i>Citrus limon</i> as mosquito repellent.</p>

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Isolation, identification and characterization of compounds from the n-hexane fraction of Citrus limon seeds: cytotoxic and mosquito repellent activities

  • Mukaram Akintunde Adeniyi-Akee,
  • Emmanuel Oloruntoba Yeye,
  • Adibe Kingsley Mbachu,
  • Kolade Ibrahim,
  • Ogunyemi Oderinlo,
  • Paul Matthew Osamudiamen,
  • Sunday Olakunle Idowu,
  • Olapeju O. Aiyelaagbe,
  • Olajire Aremu Adegoke

摘要

Background

The prevalence of malaria and other mosquito menace in Lagos State and many other parts of Nigeria has becomes so alarming. Citrus limon seeds have limited exploration, unlike the leaves, juice and the peels which are burnt as repellent and have been widely explored. This study was conducted to evaluate the repellent and cytotoxic effects of three known lipids, a known flavonoid and a novel fatty acid isolated from the n-hexane fraction C. limon.

Methods

The structures of the compounds were determined based on spectroscopic (IR, 1-D, 2-D NMR) and mass spectrometric experiments. Isolated compounds were evaluated for cytotoxicity and Anopheles gambiae mosquito repellent effects, using brine shrimp lethality assay (safety cut-off, LC50 > 100 µg/mL), and human bait method, respectively, while N,N-diethyl-meta-toluamide (DEET) and acetone were used as positive and negative controls, respectively. Repellent activity data were analysed using one-way ANOVA at α0.05.

Results

Compounds 1–5 identification gave, Palmitic acid (1), 14-Oxotricosanoic acid (2), n-Octyl stearate (3), 4-heptadec-7-enyloxy)carbonyl)butanoic acid (4) and 6,8 dimethoxy-3-undecyl-1H-[2]benzopyran-1-one (5). Compounds (1, 2 and 4) showed some level of toxicity with LC50 values less than 100 µg/mL, while compounds 3 and 5 are considered safe because of their LC50 values, that are greater than 100 µg/mL. Compound 4 and 5 are the most promising mosquito repellent agents at 5 mg/mL optimum concentration with repellencies of 77.87% and 75.15%, respectively, as compared to the standard, DEET (100%).

Conclusion

The results offer additional scientific justification for the local usage of Citrus limon as mosquito repellent.