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1.
Exp Parasitol ; 223: 108076, 2021 Apr.
Article in English | MEDLINE | ID: mdl-33460625

ABSTRACT

The present study was conducted to assess the mosquitocidal efficiency of compound isolated from Blumea mollis (D. Don) Merr against Culex quinquefasciatus. Eggs and larvae of Cx. uinquefasciatus were exposed to different concentrations 0.5, 1.0, 1.5 and 2.0 ppm of compounds prepared using DMSO. Compound 1 was identified as (4R, 5S)-4-hydroxy-7-tigloyloxy carvotanacetone, from which new derivative was synthesized and confirmed as (4R, 5S)-4-acetoxy-7-tigloyloxy carvotanacetone. Both the compounds presented larvicidal and ovicidal activities. Compounds 1 and 2 at 2-ppm concentration showed 64% and 78% larval mortality in 24 h, respectively. The LC50and LC90values of compounds 1 and 2 on Cx. quinquefasciatus larvae were 1.73, 1.27 and 4.59, 3.33 ppm, respectively. The eluted compound 1 and synthesized compound 2 presented 68% and 77% of ovicidal activity, respectively, against eggs of Cx. quinquefasciatus at 120 h post-treatment. Histopathological studies of the compound-treated larvae revealed serious damage on the larval midgut cells. Furthermore, compounds 1 and 2 was tested for toxicity study and the results showed both the compounds were found to be harmless to non-target organism Poecilia reticulata. Computational analysis of compound 2 showed strong binding interaction with the AChE1 of Cx. quinquefasciatus. These results clearly suggest that compounds from Blumea mollis could act as good mosquitocidal agents against Cx.quinquefasciatus and compound 2 was first time reported.


Subject(s)
Asteraceae/chemistry , Culex , Insecticides , Monoterpenes/isolation & purification , Mosquito Vectors , Plant Extracts/isolation & purification , Acetylcholinesterase/chemistry , Animals , Biological Assay , Computer Simulation , Esters , Insecticides/chemistry , Insecticides/isolation & purification , Larva , Lethal Dose 50 , Ligands , Molecular Docking Simulation , Ovum , Plant Extracts/pharmacology , Poecilia
2.
Nat Prod Res ; 35(24): 5744-5751, 2021 Dec.
Article in English | MEDLINE | ID: mdl-33059480

ABSTRACT

The present study was aimed to isolate active constituents from Blumea axillaris (Lam.) DC (Asteraceae) against phytopathogenic fungi. Bioactivity guided fractionation of the successive n-hexane, chloroform and methanol extract led to the isolation of the monoterpene ester (4 R,5S)-4-hydroxy-7-tigloyloxycarvotanacetone (1). The compound 1 was converted into acetyl derivative (2). The acetyl derivative (2) and the parent compound 1 were tested again phytopathogenic fungi by using mycelial inhibition and minimal inhibitory concentration values were found out by the broth microdilution method. The acetyl derivative (2) showed the highest antifungal activity against Rhizoctonia solani and Aspergillus niger. Based upon in vitro results, compound 1 was tested against Fusarium oxyporum (wilting disease) and compound 2 was tested against R. solani (leaf blight disease) in vivo using the foliar spray method. Both compounds had no phytotoxicity and also in silico docking study showed that both compounds were binding similarly as commercial fungicide carbendazim.


Subject(s)
Asteraceae , Fusarium , Antifungal Agents/pharmacology , Esters , Fungi , Molecular Docking Simulation , Monoterpenes/pharmacology , Plant Diseases
3.
Exp Parasitol ; 204: 107719, 2019 Sep.
Article in English | MEDLINE | ID: mdl-31255572

ABSTRACT

The present study was aimed to check the mosquitocidal activity of tiliamosine isolated from Tiliacora acuminata (Lam.) Hook. f. & Thom against immature stages of Culex quinquefasciatus. Eggs and larvae of Cx. quinquefasciatus were exposed to different concentrations of tiliamosine - 0.5, 1.0, 1.5 and 2.0 ppm - prepared using DMSO. The compound tiliamosine showed good larvicidal activity with LC50 and LC90 values of 1.13 and 2.85 ppm respectively, against third-instar larvae of Cx. quinquefasciatus at 24 h. In control, the larvae exhibited normal movement. Tiliamosine exhibited 91% ovicidal activity at 2.0 ppm concentration after 120 h post-treatment. Lowest concentration of tiliamosine (0.5 ppm) showed 19% egg mortality. Histopathology study of the compound-treated larvae showed serious damage on the larval midgut cells. The treated larvae showed restless movement which was different from that of the control larvae. The larvae exhibited malformation in development. The compound tiliamosine was harmless to non-target organisms P. reticulata and Dragon fly nymph at tested concentrations. The compound was highly active and inhibited AChE in a concentration-dependent manner. Computational analysis of the tiliamosine had strong interaction with AChE1 of Cx. quinquefasciatus. This report clearly suggests that the isolated compound can be used as an insecticide to control mosquito population and thus prevent the spread of vector-borne diseases.


Subject(s)
Benzylisoquinolines/pharmacology , Culex/drug effects , Insecticides/pharmacology , Menispermaceae/chemistry , Mosquito Vectors/drug effects , Plant Extracts/pharmacology , Animals , Culex/growth & development , Filariasis/prevention & control , Filariasis/transmission , Larva/drug effects , Lethal Dose 50 , Ligands , Molecular Docking Simulation , Mosquito Vectors/growth & development , Odonata/drug effects , Ovum/drug effects , Poecilia
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