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1.
Exp Parasitol ; 251: 108550, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37230323

RESUMO

The control of mosquito breeding is an essential step towards the reduction of vector-borne disease outbreaks. Synthetic larvicidal agents produce resistance in vectors and cause safety concerns in humans, animals and aquatic species. The drawback of synthetic larvicides opened a new avenue for natural larvicidal agents, but poor dosage accuracy, need for frequent applications, low stability and sustainability are the major challenges with them. Hence, this investigation aimed to overcome those drawbacks by developing bilayer tablets loaded with neem oil to prevent mosquito breeding in stagnant water. The optimised batch of neem oil-bilayer tablets (ONBT) had 65%w/w hydroxypropyl methylcellulose K100M and 80%w/w ethylcellulose in its composition. After the completion of 4th week, 91.98 ± 0.871% azadirachtin was released from the ONBT, which was followed by a subsequent drop in the in vitro release. ONBT reported long-term larvicidal efficacy (>75%) and a good deterrent effect which was better than neem oil-based marketed products. The acute toxicity study on a non-target fish model (Poecilia reticulata), OECD Test No.203 confirmed the safety of the ONBT on non-target aquatic species. The accelerated stability studies predicted a good stability profile for the ONBT. The neem oil-based bilayer tablets can be used as an effective tool for the control of vector-borne diseases in society. The product may be a safe, effective and eco-friendly replacement for the existing synthetic as well as natural products in the market.


Assuntos
Aedes , Inseticidas , Óleos Voláteis , Doenças Transmitidas por Vetores , Humanos , Animais , Mosquitos Vetores , Larva , Comprimidos
2.
Drug Dev Res ; 81(8): 1048-1056, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32767369

RESUMO

Malaria is a communicable disease which is caused by protozoan's mainly Plasmodium species (P. falciparum, P. ovale, P. vivax, P. malariae and P. knowlesi). The increasing resistance of Plasmodium to available malarial drugs poses a great responsibility for the researchers in the field of malaria. To overcome this problem of resistance, this study aimed to design and synthesize a new class of antimalarial agent with chalcone as the main moiety. Chalcones, a member of flavanoid family, consist of two aromatic rings of 1,3-diphenyl-2-propen-1-one linked by a three carbon α,ß-unsaturated carbonyl system. Five derivatives were designed and among them one was selected. The CC2 was then synthesized by esterification of Para amino acetophenone followed by treatment with hydrazide to form 2-(4 acetylphenoxy)acetohydrazide. This was then coupled with 2-Bromo substituted Diazotized esterified anilines, which was finally linked with substituted benzaldehyde to yield CC2. These were then structurally verified by Infra Red (IR) and Nuclear Magnetic Resonance (NMR) spectroscopy. The chalcone was then tested for in vitro growth inhibition assays using SYBR GREEN-1 Based assay and IC50 values were identified. The compound CC2 showed quite promising antimalarial activity by inhibiting cysteine protease enzyme. The acute toxicity studies of the compound were carried out as per OECD guideline 425 and the results showed no toxic signs and symptoms indicating CC2 as a safe and less toxic compound.

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