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Indonesian Journal of Medical Chemistry and Bioinformatics

Abstract

Aedes aegypti (Diptera: Culicidae), the primary vector of dengue, poses a significant public health threat in tropical and subtropical regions. Botanical insecticides and phytochemicals such as β- asarone, derived from essential oils,offer a promising alternative to synthetic larvicides. The rhizome of Acorus calamus L. (sweet flag), traditionally known for its neuroprotective and antioxidant properties, contains β-asarone as its principal bioactive constituent.This study evaluated the larvicidal efficacy of β-asarone and A. calamus rhizome extract against Ae. aegypti larvae, focusing on detoxification enzyme inhibition, midgut histopathology, and in silico molecular interactions.Third- and fourth-instar larvae were exposed to β-asarone and crude extract at concentrations ranging from

0.25 to 24.25 μg/mL. Larval mortality was recorded at 24, 48, and 72 hours post-exposure following WHO guidelines. Activities of acetylcholinesterase (AChE), glutathione-S-transferase (GST), and oxidase were measured using biochemical assays. Midgut histopathological changes were assessed via hematoxylin and eosin staining. Molecular docking (CB-Dock2) was used to evaluate β-asarone interactions with AChE, GST, and oxidase. β-asarone showed significantly higher larvicidal potency (LC₅₀ = 6.768 μg/mL) than the crude extract (LC₅₀ = 54.566 μg/mL). Both treatments markedly inhibited AChE and oxidase and caused extensive midgutdamage, including epithelial degeneration, ruptured peritrophic membrane, and loss of microvilli. These results demonstrate the potential of β-asarone as plant-derived larvicides acting through enzymatic inhibition and midgut disruption, offering a promising strategy for mosquito control.

Bahasa Abstract

Aedes aegypti (Diptera: Culicidae), vektor utama demam berdarah, menimbulkan ancaman kesehatan masyarakat yang signifikan di wilayah tropis dan subtropis. Insektisida nabati dan fitokimia seperti β-asarone, yang berasal dari minyak atsiri, menawarkan alternatif yang menjanjikan untuk larvasida sintetis. Rimpang Acorus calamus L. (sweet flag), yang secara tradisional dikenal karena sifat neuroprotektif dan antioksidannya, mengandung β-asarone sebagai konstituen bioaktif utamanya. Penelitian ini mengevaluasi efikasi larvasida β-asarone dan ekstrak rimpang A. calamus terhadap larva Ae. aegypti, dengan fokus pada penghambatan enzim detoksifikasi, histopatologi usus tengah, dan interaksi molekuler in silico. Larva instar ketiga dan keempat dipaparkan dengan β-asarone dan ekstrakkasar pada konsentrasi berkisar antara 0,25 hingga 24,25 μg/mL. Mortalitas larva dicatat pada 24, 48, dan 72 jam pasca-paparan sesuai pedoman WHO. Aktivitas asetilkolinesterase (AChE), glutathione-S-transferase (GST), dan oksidase diukur menggunakan uji biokimia. Perubahan histopatologi usus tengah dinilai melalui pewarnaanhematoksilin dan eosin. Docking molekuler (CB- Dock2) digunakan untuk mengevaluasi interaksi β-asarone dengan AChE, GST, dan oksidase. β- asarone menunjukkan potensi larvasida yang secara signifikan lebih tinggi (LC₅₀ = 6,768 μg/mL) dibandingkan ekstrak kasar (LC₅₀ = 54,566 μg/mL). Kedua perlakuan tersebut secara signifikan menghambat AChE dan oksidase, serta menyebabkan kerusakan usus tengah yang luas, termasuk degenerasi epitel, ruptur membran peritrofik, dan hilangnya mikrovili. Hasil ini menunjukkan potensi β-asarone sebagai larvasida turunan tumbuhan yang bekerja melalui penghambatan enzimatik dan disrupsi usus tengah, menawarkan strategi yang menjanjikan untuk pengendalian nyamuk.

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