LC50 Values Research Articles

Identification and biocontrol potential of entomopathogenic nematodes, Steinernema siamkayai occurring in western Thailand against the common cutworm, Spodoptera litura Fabricius (Lepidoptera: Noctuidae) under laboratory and screenhouse conditions

AbstractThe common cutworm, Spodoptera litura, is a serious insect pest of many vegetables and crops worldwide. Entomopathogenic nematodes (EPN) have been utilized as biological control agents for controlling various insect pests, including the larvae of S. litura. Many indigenous EPN have been recognized to be more effective in specific field applications. Among the 160 soil samples collected in undisturbed areas of western Thailand, three samples tested positive for EPN. Three indigenous EPN were identified as Steinernema siamkayai namely, EPNKU63, EPNKU70 and EPNKU85, based on ITS and D2/D3 expansion region analysis of the 28s rRNA genes. Additionally, genetic analysis of the symbiotic bacteria using recA rRNA sequences confirmed their identity as Xenorhabdus stockiae namely, PEPNKU63, PEPNKU70 and PEPNKU85. To evaluate their initial biocontrol potential against the 6th instar larvae of Galleria mellonella, virulence assays were conducted. The application of 100 infective juveniles (IJs)/insects resulted in the mortality of 80–100% of G. mellonella larvae after 72 h. When symbiotic bacteria were applied at 1 × 106 cells/insect, they exhibited 63–93% mortality against G. mellonella larvae after 120 h. In further laboratory tests, three S. siamkayai isolates achieved 100% mortality of 3rd instar Spodoptera litura larvae within 72 h, with LC50 values ranging from 29 to 30 IJs/insect. In screenhouse experiments, it was revealed that all S. siamkayai isolates displayed substantial virulence, ranging from 62% to 74%, against 3rd instar S. litura larvae within 72 h. This study demonstrates the biocontrol potential of S. siamkayai in controlling S. litura larvae.

Characterization of the fragmentation mechanisms in electrospray ionization tandem mass spectrometry of chloroquinoline derivatives with larvicidal activity against Aedes aegypti.

4,7-Dichloroquinoline (DCQ) represents a group of synthetic molecules inspired by natural products with important roles in biological and biomedical areas. This work aimed to characterize DCQ and its derivatives by high-resolution electrospray ionization (ESI) mass spectrometry and tandem mass spectrometry (ESI-MS/MS), supported by theoretical calculations. Biological assays were carried out with DCQ and its derivatives to determine LC50 values against Aedes aegypti larvae. Five DCQ derivatives were synthesized by using previously described protocols. ESI-MS/MS analyses were carried out with a quadrupole/time-of-flight and ion-trap instrument. The proposed gas-phase protonation sites and fragmentation were supported by density functional theory calculations. The larvicidal tests were performed with the Ae. aegypti Rockefeller strain, and the LC50 values were determined by employing five test concentrations. Larval mortality was determined after treatment for 48 h. DCQ bromides or aldehydes (C-3 or C-8 positions), as well as the trimethylsilyl derivative (C-3 position), were prepared. Detailed ESI-MS/MS data revealed heteroatom elimination through an exception to the even-electron rule, to originate open-shell species. Computational studies were used to define the protonation sites and fragmentation pathways. High activity of DCQ and its derivatives against Ae. aegypti larvae was demonstrated. Our results provided a well-founded characterization of the fragmentation reactions of DCQ and its derivatives, which can be useful for complementary studies of the development of a larvicidal product against Ae. aegypti.

Application of General Unified Threshold Models to Predict Time-Varying Survival of Mayfly Nymphs Exposed to Three Neonicotinoids

Pesticide exposure patterns tested in laboratory bioassays often do not match real-world pesticide exposure profiles in edge-of-field waterbodies. Toxicokinetic–toxicodynamic (TKTD) models are therefore increasingly used, as they allow for predictions of the toxic effects under actual time-variable field exposures. The TKTD models from the General Unified Threshold models of Survival (GUTS), for example, are considered ready for use by regulators for calculating the survival rates for any time-variable exposure profile. However, questions remain regarding their predictive power for compounds showing increased toxicity over time, such as neonicotinoid insecticides. The aim of the present study was therefore to compare the GUTS-predicted 28 d toxicity values of three neonicotinoids (imidacloprid, clothianidin, and thiamethoxam) for the common New Zealand mayfly genus Deleatidium spp. with those observed in a previously published study. Overall, the GUTS modeling results underestimated the toxicity values derived experimentally. From the three neonicotinoids, clothianidin showed the best fit between the estimated and observed 28 d LC50 (median-lethal-concentration) values. Shortcomings of the modeling exercise, future research needs, and implications for the application of GUTS models in regulatory risk assessment are discussed.

BSLT and DPPH Methods to Determine the Potential Toxicity of Archidendron Pauciflorum Skin to Artemia Salina and the Antioxidant Potential as an Early Exploration of Anti-Cancer Drugs

Archidendron pauciflorum skin is a dense waste that pollutes the environment and can be a problem if not properly cleaned. According to previous research, Archidendron pauciflorum skin has a very high potential because it contains flavonoid components and polyphenols with anti-cancer and antibacterial properties. To evaluate the toxicity activity with the BSLT Method and the antioxidant DPPH Method, the scalp is cut into small pieces, dried in the oven at 60 °C, and then macerated for 24 hours in a mixture of methanol and ethyl acetate solvents as well as hexane to produce polar, semipolar, and non-polar chemicals. The fibre from each solvent is collected, and the rotary evaporator is used to evaporate it until a thick extract is produced. According to the final findings of the study, the LC50 value (μg/mL) for each solvent is: the methanol value is 111 ppm, while ethyl acetate is 192 ppm. While for the test of antioxidant activity, significant results were obtained on the methanol solvent with an IC50 value of 51.13 μg/mL The conclusion of this study is that the 24-hour maceration period is the most efficient solvent for toxicity to Artemia salina and antioxidants to continue further research in the search for anti-cancer drugs.

Acaricidal Efficacy of Cassia sieberiana DC (Caesalpinaceae) Stem Bark Aqueous Extract on Hyalomma KOCH, 1844 (Acari: Ixodidae) Reproductive Stages

One of the most significant challenges facing tick control through chemical acaricides is resistance and environmental pollution, encouraging the need for natural plant products that are less toxic and environment friendly. This study was conducted to determine theacaricidal efficacy of Cassia sieberiana stem bark aqueous extract on Hyalomma species using immersion testing for egg-hatchinhibition and adult mortality. Both tests used ascending extract concentrations of 5%, 10%, 15% and 20%, at durations of 1, 2, 3, 4, 5, 6, 7 and 8 hours. Egg-hatch inhibition peaked at 5% concentration at 8hrs, 10% and 15% at 7 and 8hrs and 20% at 5, 6, 7 and 8hrs while adult mortality was highest at 20% concentration. There was a positive correlation between graded extract concentration, immersion period, egg-hatch inhibition and adult mortality. The LC50 values for adult mortality and egg-hatch inhibition were 13.1 mg/mL and 13.7 mg/mL and coefficient of determination were y = 3.7x +1.5 and y = 3.062 + 8.12 respectively. Both LC50 values were almost similar indicating a strong association between extract concentration and acaricidal activity in vitro.

A comparative study on targeted gene expression in zebrafish and its gill cell line exposed to chlorpyrifos.

Chlorpyrifos (CPF) is an organophosphorus-based insecticide, which is known to pose a serious risk to aquatic animals. However, the mechanisms of CPF toxicity in animals still remain unclear. The present investigation aimed to compare the potential effects of CPF in zebrafish (Danio rerio) and its gill cell line (DrG cells). Based on the in vivo study, the LC50 was calculated as 18.03µg/L and the chronic toxic effect of CPF was studied by exposing the fish to 1/10th (1.8µg/L) and 1/5th (3.6µg/L) of the LC50 value. Morphological changes were observed in fish and DrG cells which were exposed to sublethal concentrations of CPF. The results of MTT and NR assays showed significant decline in the survival of cells exposed to CPF at 96h. The production of reactive oxygen species in DrG cells and expression levels of antioxidant markers, inflammatory response genes (cox2a and cox2b), cyp1a, proapoptotic genes (bax), antiapoptotic gene (bcl2), apoptotic genes (cas3 and p53), and neuroprotective gene (ache) were determined in vivo using zebrafish and in vitro using DrG cells after exposure to CPF. Significant changes were found in the ROS production (DrG cells) and in the expression of inflammatory, proapoptotic, and apoptotic genes. This study showed that DrG cells are potential alternative tools to replace the use of whole fish for toxicological studies.

Activity of Methanolic and Hydrolyzed Methanolic Extracts of Ricinus communis (Euphorbiaceae) and Kaempferol against Spodoptera frugiperda (Lepidoptera: Noctuidae)

Spodoptera frugiperda is the main pest of maize. One of the alternatives proposed for its control is the implementation of products of botanical origin, such as those derived from Ricinus communis. In this work, the insecticidal and insectistatic activities of methanolic and hydrolyzed methanolic extracts of the aerial parts of R. communis and kaempferol against S. frugiperda are evaluated. The methanolic extract presented a larval mortality rate of 55% and an accumulated mortality rate of 65% starting at 4000 ppm, with LC50 values of 3503 (larvae) and 2851 (accumulated); meanwhile, from a concentration of 1000 ppm, a decrease in pupa weight at 24 h of 20.5 mg was observed when compared to the control. The hydrolyzed methanolic extract presented a larval mortality and accumulated mortality rate of 60% from a concentration of 1000 ppm, and a decrease in pupa weight at 24 h of 35.31 mg was observed, when compared to the control. For the compound kaempferol 3-β-D-glucopyranoside, a larval mortality rate of 65% and an accumulated mortality rate of 80% were observed from 800 ppm, with LC50 values of 525.2 (larvae) and 335.6 ppm (accumulated); meanwhile, at 300 ppm, a decrease in pupa weight of 25.59 mg after 24 h was observed when compared to the control.

Effects of dietary garlic (Allium sativum) oil on growth performance, haemato-biochemical and histopathology of cypermethrin-intoxicated Nile tilapia (Oreochromis niloticus).

When pesticides are introduced into wetlands by agriculture, fish quickly absorb them through their gills. Pesticides reduce hatchability, impede growth, and antioxidant response, killing fish. Therefore, it's crucial to find effective pesticide mitigation methods for fish. In this study, the effects of garlic (Allium sativum) oil on the growth, haematology, biochemistry and histopathology parameters of Nile tilapia (Oreochromis niloticus) exposed to cypermethrin toxicity were investigated. In the research, cypermethrin was added to the water of the experimental groups at a rate of 1:20 of the LC50 value, and 1.00% garlic oil was added to the fish feed. Fish with an initial weight of 30.26 ± 0.26g were fed for 45 days. At the end of feeding, the final weights were determined as 69.39 ± 0.41 (G1), 61.81 ± 0.65 (G2), 82.25 ± 0.36 (G3), and 75.04 ± 0.68 (G4) grams, respectively. Histopathological examinations revealed serious lesions in the gill, liver, brain, and muscle tissues in the cypermethrin group, whereas these lesions were minimal or absent in the garlic oil group. Garlic oil supplementation had positive effects on growth, haematology, blood biochemistry, hepatosomatic index and histopathological parameters. These findings suggest that garlic oil is a potential protective agent against cypermethrin toxicity.

Testusterol, a new sterol of the sponge species Xestospongia testudinaria from Phu Quoc island, Vietnam

A new sterol, named testusterol (1), and five known compounds (2-6) were isolated from the n-hexane and dichloromethane extracts of the sponge species Xestospongia testudinaria. Their chemical structures were elucidated based on extensive spectroscopic analyses (1D, 2D NMR, ESIMS and HRESIMS) and comparison with published data. The results of in vitro test (utilizing brine shrimp Artemia salina LEACH) showed that three extracts ethanol, dichloromethane, and ethanol/water, significantly inhibited Artemia salina with LC50 values ranging from 6.09 to 16.83 µg/mL. Remarkably, the new compound 1 exhibited potent inhibition against both Gram-positive (Staphyloccocus aureus, Bacillus subtilis, Lactobacillus fermentum), and Gram-negative (Escherichia coli, Salmonella enterica, Pseudomonas aeruginosa) bacteria species, with IC50 values of less than 12.0 nM and MIC ranging from 4.70 to 75.23 nM as determined by the broth-microdilution assay.

Comparative Effects of Elettaria cardamomum Essential Oil and Its Nanoliposomal State on Mortality of Anopheles stephensi Larvae

Background: Malaria has remained the most dreadful vector-borne disease; hence, vector control is the most affordable and achievable approach to mitigate the disease burden. Due to the emergence of resistance and environmental pollu­tion, herbal larvicides are considered an alternative to chemical types. Also, nanotechnology has been proposed as a prom­ising solution to improve the efficiency of plant larvicides. This study aimed to develop an effective herbal larvi­cide.  
 Methods: The chemical composition of Elettaria cardamomum essential oil (EO) was first investigated. Nanolipo­somes containing the EO were then prepared using the ethanol injection method. After that, the larvicidal efficacy of the EO and its liposomal state were compared against Anopheles stephensi in laboratory conditions.
 Results: Alpha-terpinyl acetate (77.59%), eucalyptol (4.38%), nerolidol (2.96%), linalool (1.77%), and limonene (1.69%) were the five major compounds of the EO. Nanoliposomes containing the EO with a particle size of 73±5 nm and a zeta potential of -16.3±0.8 mV were prepared. Additionally, the ATR-FTIR analysis verified the successful load­ing of the EO into nanoliposomes. The larvicidal activity of nanoliposomes exhibited remarkable potency, with an LC50 value of 14.35 (10–18) µg/mL, significantly more potent than the non-formulated EO, which had an LC50 value of 33.47 (28–39) µg/mL against Anopheles stephensi larvae.
 Conclusion: The nanoliposomes containing E. cardamomum EO showed promising efficacy against An. stephensi lar­vae. It could thus be considered for further application against other species of mosquitoes.

Binary mixture of ionic liquid and span 80 for oil spill remediation: Synthesis and performance evaluation

The synthesis of new surfactants helps to mitigate the environmental and financial effects of oil spills by providing efficient cleanup options. Herein, this study provides the development of a binary mixture of Span 80 and Choline myristate [Cho][Mys], a surface-active ionic liquid (SAIL) as green dispersant for oil spill remediation. The synergistic interaction at a 60:40 (w/w) ratio significantly lowered the critical micelle concentration (cmc) to 0.029 mM. Dispersion efficiency tests with Arab crude oil showed optimal performance at a 60:40 ratio of Span 80 and [Cho][Mys] (1:25 dispersant to oil ratio, v/v), achieving 81.16 % dispersion effectiveness in the baffled flask test. The binary mixture demonstrated superior emulsion stability (6 h) and the lowest interfacial tension (1.12 mN/m). Acute toxicity experiments revealed the dispersant's practical non-toxicity with an LC50 value of 600 mg/L. Overall, this environmentally benign surfactant combination shows promise as a safe and effective oil spill dispersant.

Co-exposure to deltamethrin and cyazofamid: variations in enzyme activity and gene transcription in the earthworm (Eisenia fetida).

Pesticide formulations are typically applied as mixtures, and their synergistic effects can increase toxicity to the organisms in the environment. Despite pesticide mixtures being the leading cause of pesticide exposure incidents, little attention has been given to assessing their combined toxicity and interactions. This survey purposed to reveal the cumulative toxic effects of deltamethrin (DEL) and cyazofamid (CYA) on earthworms (Eisenia fetida) by examining multiple endpoints. Our findings revealed that the LC50 values of DEL for E. fetida, following 7- and 14-day exposures, ranged from 887.7 (728-1095) to 1552 (1226-2298) mg kg-1, while those of CYA ranged from 316.8 (246.2-489.4) to 483.2 (326.1-1202) mg kg-1. The combinations of DEL and CYA induced synergistic influences on the organisms. The contents of Cu/Zn-SOD and CarE showed significant variations when exposed to DEL, CYA, and their combinations compared to the untreated group. Furthermore, the mixture administration resulted in more pronounced alterations in the expression of five genes (hsp70, tctp, gst, mt, and crt) associated with cellular stress, carcinogenesis, detoxification, and endoplasmic reticulum compared to single exposures. In conclusion, our comprehensive findings provided detailed insights into the cumulative toxic effects of chemical mixtures across miscellaneous endpoints and concentration ranges. These results underscored the importance of considering mixture administration during ecological risk evaluations of chemicals.

Evaluating acute toxicity of amino acid ionic liquids towards Poecilia reticulata fish for designing sustainable chemical processes

An acute toxicity study assessed the LC50 values for eight different amino acid ionic liquids (AAILs), featuring two cations, tetrabutylphosphonium [P4444] and tetrabutylammonium [N4444], coupled with four anions [PHE], [ASP], [SER], and [GLY]. According to the OECD 203 standard for acute fish toxicity tests with guppy fish (Poecilia reticulata, all the AAILs exhibited low toxicity levels, and were practically nontoxic and harmless. The LC50 values surpassed 100 mg/L and 1000 mg/L. This study provides valuable insights for industrial professionals in utilizing tetrabutylphosphonium-based amino acid ionic liquids [P4444] [AA] and tetrabutylammonium-based amino acid ionic liquids [N4444][AA] in chemical processes, indicating their safety in aquatic environments. These promising results highlight the potential of incorporating these AAILs into diverse chemical processes while ensuring minimal ecological impact.

Bifenox induces hepatotoxicity and vascular toxicity in zebrafish embryos via ROS production and alterations in signaling pathways

Existing evidence shows that currently used pesticides pose toxicological risks to exposed wildlife. Chemically, bifenox belongs to diphenyl ethers, a well-known group of herbicides. Its mechanism of action primarily involves inducing lipid peroxidation and blocking protoporphyrinogen oxidases. Toxicity of diphenyl ether herbicides has been elucidated in animal cells; however, in vivo toxicological evaluations of bifenox are required to determine its unexpected effects. This study aimed to determine the negative effects of bifenox, and its effects on higher eukaryotes. We found that early stages of zebrafish embryo exposed to bifenox demonstrated increased mortality and physiological defects, based on the LC50 value. Bifenox severely inhibited blood vessel growth by reducing key elements of complex connectivity; fluorescently tagged transgenic lines (fli1a:EGFP) showed morphological changes. Additionally, transgenic lines that selectively identified hepatocytes (fabp10a:DsRed) showed reduced fluorescence, indicating that bifenox may inhibit liver development. To evaluate the level of oxidative stress, we used 2′,7′-dichlorofluorescein diacetate (DCFH-DA) probes in zebrafish embryos to identify the underlying mechanisms causing developmental damage. Our findings demonstrate that exposure to bifenox causes abnormalities in the hepatic and cardiovascular systems during zebrafish embryogenesis. Therefore, this study provides new information for the evaluation of toxicological risks of bifenox in vertebrates.

Miniaturized IPD bandpass filter with controllable transmission zero based on modified lumped T‐section

AbstractIn this letter, a miniaturized bandpass filter (BPF) with controllable transmission zero (TZ) based on one lumped T‐section is proposed. To enhance rejection in the BPF, a modified T‐section circuit is introduced to generate a controllable TZ that can be readily adjusted by the LC values. To validate the performance, the proposed BPF is fabricated using integrated passive device technology on silicon. The measurement results show that the achievable bandwidth covers 2.4–2.5 GHz, with an insertion loss less than 2.6 dB and a measured return loss less than −15 dB. The fabricated BPF has a compact size of 1.3 mm × 0.8 mm (i.e., 0.0113 λ0 × 0.0069 λ0). The simulated and measured results of the BPF are in reasonably good agreement.

Description of Solvent-Extractable Chemicals in Thermal Receipts and Toxicological Assessment of Bisphenol S and Diphenyl Sulfone.

Research on thermal receipts has previously focused on the toxic effects of dermal exposure from the most publicized developers (e.g., bisphenol A (BPA) and bisphenol S (BPS)), while no studies have reported on the other solvent-extractable compounds therein. Diphenyl sulfone (DPS) is a sensitizer added to thermal receipts, but little is known about DPS concentrations in receipts or potential toxicity. Here, we quantified BPA, BPS, and DPS concentrations and tentatively identified the solvent-extractable compounds of thermal receipts collected from three South Dakota (USA) cities during 2016-2017. An immortalized chicken hepatic cell line, cultured as 3D spheroids, was used to screen effects of DPS, BPS, and 17ß estradiol (E2; 0.1-1000µM) on cell viability and gene expression changes. These chemicals elicited limited cytotoxicity with LC50 values ranging from 113 to 143µM, and induced dysregulation in genes associated with lipid and bile acid homeostasis. Taken together, this study generated novel information on solvent-extractable chemicals from thermal receipts and toxicity data for DPS.

Molecular mechanisms for selective action of afidopyropen to Myzus persicae and Coccinella septempunctata.

Afidopyropen is a novel insecticide with high selectivity between sucking insects such as the peach aphids Myzus persicae and natural enemies like the seven-spotted lady beetle Coccinella septempunctata. However, the mechanisms of selective action for afidopyropen remain unknown. The LC50 values of afidopyropen to the 1st-4th instar larvae and adult C. septempunctata were 372- to more than 7267-fold higher than that to adult M. persicae. Though the activity of cytochrome P450s in M. persicae was 6.1- to 7.5-fold higher than that in C. septempunctata, the latter has much higher activities of carboxylesterase (CarEs) and glutathione S-transferases (GSTs), and the crude enzyme of C. septempunctata and M. persicae showed similar metabolism efficiency to afidopyropen. Molecular docking results demonstrated that afdopyropen showed higher binding affinity to the vanilloid-type transient receptor potential (TRPV) channel of M. persicae (-9.1 kcal/mol) than to that of C. septempunctata (-8.2 kcal/mol). And the EC50 value of afdopyropen to the TRPV channel of C. septempunctata (41 360 nM) was 19 885-fold higher than that in M. persicae (2.08 nM). Our results demonstrated that the significantly different sensitivity of M. persicae and C. septempunctata TRPV channel to afidopyropen play a key role in the high selectivity of afidopyropen. These findings provide new insights into the selective mechanisms of afidopyropen against insect pests and natural enemies as well as the theory support for coordinated application of chemical control and biological control. © 2024 Society of Chemical Industry.

Assessment of the chemical profile and potential biocontrol of Amphora coffeaeformis against foodborne pathogens and Culex pipiens L. to ensure food safety

AbstractThe extensive use of synthetic antibiotics and insecticides in controlling microbes and insect spreads led to a build‐up of resistance strains and caused negative impacts on human health through bioaccumulation in food and the environment. The present study assessed the antimicrobial activity of Amphora coffeaeformis (A. coffeaeformis) ethanolic extract against foodborne pathogenic microbes as well as assessed its ability to control Culex pipiens L. (C. pipiens) larvae. The gas chromatography–mass spectrum (GC/MS) and high‐performance liquid chromatography (HPLC) analysis showed that A. coffeaeformis extract was rich with phenolic compounds, organosulfur compounds, carboxylic acids, amino acids, organic quinoline, dipeptide and monosaccharide. The extract of A. coffeaeformis showed antibacterial capability against all tested bacteria, with minimal inhibition concentration (MIC) values ranging from 20.2 to 66.7 g/mL, as well as antifungal effects against all tested mycotoxigenic fungi, with MIC values ranging from 113.62, 68.95 and 49.37 μg/mL mg/mL. Furthermore, the extract showed high larvicidal activity against C. pipiens larvae at 24, 48, and 72 h, respectively. LC50 values decreased gradually with the treatment period. Likewise, the adult emergence and growth index were significantly negatively related to increasing extract concentrations. Moreover, the extract exhibited a noteworthy depletion in the reproductive potential and increased sterility index of C. pipiens females developed of treated larvae. Besides a reduction in egg hatching percent, increase pupal malformations, increase and adult abnormalities. C. pipiens biochemical markers; glutathione‐S‐transferase, carboxylesterase, acetylcholinesterase, α‐esterase and cytochrome P‐450 showed significant alteration after the extract exposure. Overall, these findings promise the application possibility of A. coffeaeformis extract as a biopreservator against foodborne pathogens and as bioinsecticides for mosquito control as well.

Limonoids from the fruits of Chisocheton erythrocarpus and their mosquito larvicidal activities

Phytochemical study of the fruits of Chisocheton erythrocarpus (Hiern) allowed the identification of eight undescribed limonoids, namely erythrocarpines O – V (1 – 6, 7a and 7b), along with seven known compounds. The structures of these compounds were elucidated based on spectroscopic and HRMS data, along with electronic circular dichroism to configure the absolute configuration. Erythrocarpines O and P are γ-hydroxybutenolide analogs of mexicanolide-type limonoids while erythrocarpine Q – V are phragmalin-type limonoids possessing a 1,29-oxymethylene bridge with either benzoyl or cinnamoyl moiety in their structures. Mosquito larvicidal activity revealed that crude DCM extract of C. erythrocarpus possessed a good larvicidal effect against Aedes aegypti larvae in 48 hours (LC50 = 153.0 ppm). Subsequent larvicidal activity of isolated compounds indicated that erythrocarpine G (10) and 14-deoxyxyloccensin K (11) were responsible for the enhanced larvicidal effect of the extract, reporting LC50 values of 18.55 ppm and 41.16 ppm, respectively. Moreover, residual activity testing of the crude DCM extract revealed that the duration of its larvicidal effects is up to 14 days, where it maintained a 98 % larval mortality throughout the test period, under laboratory conditions.

Anthelmintic screening of Bangladeshi medicinal plants and related phytochemicals using in vitro and in silico methods: An ethnobotanical perspective

Ethnopharmacological relevanceInfections caused by parasitic worms or helminth continue to pose a great burden on human and animal health, particularly in underdeveloped tropical and subtropical countries where they are endemic. Current anthelmintic drugs present serious limitations and the emergence of drug resistance has made it increasingly challenging to combat such infections (helminthiases). In Bangladesh, medicinal plants are often used by indigenous communities for the treatment of helminthiases. Knowledge on such plants along with screening for their anthelmintic activity has the potential to lead to the discovery of phytochemicals that could serve as novel molecular scaffolds for the development of new anthelminthic drugs. Aim of the studyThe purpose of this study was i) to conduct an ethnobotanical survey to gather data on Bangladeshi medicinal plants used in the treatment of helminthiases, ii) to test plants with the highest use values for their in vitro anthelmintic activity, and iii) to carry out in silico screening on phytochemicals present in the most active plant extract to investigate their ability to disrupt β-tubulin function in helminths. MethodsThe ethnobotanical survey was conducted across three sub-districts of Bangladesh, namely Mathbaria, Phultala and Khan Jahan Ali. The in vitro screening for anthelmintic activity was performed in a motility test using adult Haemonchus contortus worms. Virtual screening using PyRx was performed on the phytochemicals reported from the most active plant, exploring their interactions with the colchicine binding site of the β-tubulin protein target (PDB ID: 1SA0). ResultsThe survey respondents reported a total of 32 plants for treating helminthiases. Based on their use values, the most popular choices were Ananas comosus (L.) Merr., Azadirachta indica A.Juss., Carica papaya L., Citrus maxima (Burm.) Merr., Curcuma longa L., Momordica charantia L., Nigella sativa L. and Syzygium cumini (L.) Skeels. In vitro anthelmintic testing revealed that A. indica leaves and bark had the highest activity with LC50 values of 16 mg/mL in both cases. Other plant extracts also exhibited good anthelmintic activity with LC50 values ranging from 16 to 52 mg/mL, while the value for albendazole (positive control) was 8.39 mg/mL. The limonoids nimbolide and 28-deoxonimbolide showed a binding affinity of −8.9 kcal/mol, and satisfied all drug-likeness parameters. The control ligand N-deacetyl-N-(2-mercaptoacetyl)colchicine had a binding affinity of −6.9 kcal/mol. ConclusionFurther in silico and in vitro studies are warranted on the identified limonoids to confirm the potential of these derivatives as novel drug templates for helminthiases. The current study supports the need for an ethnobotanical survey-based approach to discover novel drug templates for helminthiases.