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1.
Ecotoxicol Environ Saf ; 284: 116908, 2024 Sep 10.
Artículo en Inglés | MEDLINE | ID: mdl-39260219

RESUMEN

Deltamethrin (DLM), in combination with the synergist piperonyl butoxide (PBO), is extensively used in pest control programs due to its potent pesticidal properties and appreciable safety margin. However, various research studies report their adverse effects on non-target organisms. In this study, we investigated the toxicity of DLM, PBO, and a DLM-PBO (3:1) combination on Labeo rohita (L. rohita) fish fingerlings. Fish behavior and mortality rates were recorded at different time intervals up to 96 h for concentrations of 0.003, 0.007, 0.015, 0.031, and 0.062 µg/mL, respectively. Biochemical, hematological, and histopathological studies were carried out. High-performance liquid chromatography (HPLC) was used to detect and quantify residues in fish samples. The LC50 values after 48 h for DLM, PBO, and DLM-PBO exposed fish fingerlings were found to be 0.028, 0.066, and 0.007 µg/mL, respectively. At a concentration of 0.003 µg/mL of DLM, PBO, and DLM-PBO, the treated fish fingerlings exhibited similar behavior to the control group. Hematological parameters, such as red blood cell (RBC) and white blood cell (WBC) counts, were reduced in the treated groups compared to the control. Biochemical parameters showed increased levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), while total serum protein levels decreased in DLM, PBO, and DLM-PBO treated fingerlings. Histopathological examination of liver, gill, and heart tissues revealed lesions with hydropic degeneration in the liver and fusions of gill lamellae in the treated tissues. Fish fingerlings exposed to the DLM-PBO combination appeared highly prone to toxicity compared to those treated with DLM and PBO separately.

2.
Curr Top Med Chem ; 24(18): 1542-1556, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38778617

RESUMEN

Introduced into law enforcement in 1976, the oleoresin capsicum (OC) spray has been labeled as one of the most significant and radical developments in law enforcement. However, epidemiological research on OC health effects is deficient, receiving little public support. The major responses to acute exposure to OC spray can be found in the pulmonary system. The molecular mechanism(s) involved in the action of capsaicinoids, the active constituents in OC, are complex cascades of reactions which end up in necrosis or apoptosis. OC may also damage and deplete biological redox systems in the epithelial lining fluids and within cells and mitochondria, modifying structural proteins and nucleic acids and leading to enzyme inactivation. Since there are no characteristic laboratory tests available for identification or confirmation of OC exposure, and on the basis of prevailing data, reassessment of the health risks of OC exposures in vulnerable populations and in-depth study of the molecular mechanics of receptors is the need of the hour for the development of effective countermeasures. This review aims to consider evidence for adverse effects of OC spray used in ways comparable to their application by law enforcement personnel and civilians, with possible treatment recommendations that are precedent for improved management.


Asunto(s)
Extractos Vegetales , Humanos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Capsicum/química
3.
3 Biotech ; 14(3): 71, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38362592

RESUMEN

In our continuous effort to develop novel antiepileptic drug, a new series of nipecotic acid derivatives having1,3,4-thiadiazole nucleus were designed and synthesized. This study aims to improve the lipophilicity of nipecotic acid by attaching some lipophilic anchors like thiadiazole and substituted aryl acid derivatives. In our previous study, we noticed that the N-substituted oxadiazole derivative of nipecotic acid exhibited significant antiepileptic activity in the rodent model. The synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, Mass, and elemental analysis. The anticonvulsant activity was evaluated by using the maximal electroshock-induced seizure model in rats (MES) and the subcutaneous pentylenetetrazol (scPTZ) test in mice. None of the compounds were found to be active in the MES model whereas compounds (TN2, TN9, TN12, TN13, and TN15) produced significant protection against the scPTZ-induced seizures model. The compounds showing antiepileptic activity were additionally evaluated for antidepressant activity by using the forced swim test, 5-hydroxytryptophan (5-HTP)-induced head twitch test, and learned helplessness test. All the molecules that showed anticonvulsant activity (TN2, TN9, TN12, TN13, and TN15), also exerted significant antidepressant effects in the animal models. The selected compounds were subjected to different toxicity studies. Compounds were found to have no neurotoxicity in the rota-rod test and devoid of hepatic and renal toxicity in 30 days repeated oral toxicity test. Further, a homology model was developed to perform the in-silico molecular docking and dynamics studies which revealed the similar binding of compound TN9 within the active binding pocket and were found to be the most potent anti-epileptic agent. The market expectation for newly developed antiepileptic thiadiazole-based nipecotic acid derivatives is significant, driven by their potential to offer improved therapeutic outcomes and reduced side effects, addressing a critical need in epilepsy treatment. These innovative compounds hold promise for meeting the demand for more effective and safer antiepileptic medications. Supplementary Information: The online version contains supplementary material available at 10.1007/s13205-023-03897-1.

4.
Sci Rep ; 12(1): 2180, 2022 02 09.
Artículo en Inglés | MEDLINE | ID: mdl-35140283

RESUMEN

Mosquito-borne infections like dengue, malaria, chikungunya, etc. are a nuisance and can cause profound discomfort to people. Due to the objectional side effects and toxicity associated with synthetic pyrethroids, N,N-diethyl-3-methylbenzamide (DEET), N,N-diethyl phenylacetamide (DEPA), and N,N-di ethyl benzamide (DEBA) based mosquito repellent products, we developed an essential oil (EO) based mosquito repellent cream (EO-MRC) using clove, citronella and lemongrass oil. Subsequently, a formulation characterization, bio-efficacy, and safety study of EO-MRC were carried out. Expression of Anti-OBP2A and TRPV1 proteins on mosquito head parts were studied by western blotting. In-silico screening was also conducted for the specific proteins. An FT-IR study confirmed the chemical compatibility of the EOs and excipients used in EO-MRC. The thermal behaviour of the best EOs and their mixture was characterized by thermogravimetric analysis (TGA). GC-MS examination revealed various chemical components present in EOs. Efficacy of EO-MRC was correlated with 12% N,N-diethyl benzamide (DEBA) based marketed cream (DBMC). Complete protection time (CPT) of EO-MRC was determined as 228 min. Cytotoxicity study on L-132 cell line confirmed the non-toxic nature of EO-MRC upon inhalation. Acute dermal irritation study, acute dermal dose toxicity study, and acute eye irritation study revealed the non-toxic nature of EO-MRC. Non-target toxicity study on Danio rerio confirmed EO-MRC as safer for aquatic non-target animals. A decrease in the concentration of acetylcholinesterase (AChE) was observed in transfluthrin (TNSF) exposed Wistar rats. While EO-MRC did not alter the AChE concentrations in the exposed animals. Results from western blotting confirmed that Anti-OBP2A and TRPV1 proteins were inhibited in TNSF exposed mosquitoes. Mosquitoes exposed to EO-MRC showed a similar expression pattern for Anti-OBP2A and TRPV1 as the control group. In silico study revealed eight identified compounds of the EOs play significant roles in the overall repellency property of the developed product. The study emphasizes the mosquito repellent activity of EO-MRC, which could be an effective, eco-friendly, and safer alternative to the existing synthetic repellents for personal protection against mosquitoes during field conditions.


Asunto(s)
Repelentes de Insectos/química , Repelentes de Insectos/farmacología , Aceites Volátiles/química , Aceites Volátiles/farmacología , Crema para la Piel/química , Crema para la Piel/farmacología , Acetilcolinesterasa/metabolismo , Animales , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Culicidae , Cymbopogon/química , Composición de Medicamentos , Ojo/efectos de los fármacos , Femenino , Humanos , Repelentes de Insectos/efectos adversos , Masculino , Simulación del Acoplamiento Molecular , Aceites Volátiles/efectos adversos , Aceites de Plantas/química , Conejos , Ratas Wistar , Piel/efectos de los fármacos , Crema para la Piel/efectos adversos , Pruebas de Irritación de la Piel , Syzygium/química , Terpenos/química , Pez Cebra
5.
Toxicol Appl Pharmacol ; 405: 115188, 2020 10 15.
Artículo en Inglés | MEDLINE | ID: mdl-32805267

RESUMEN

Cardiopulmonary functions such as respiratory depression, severe irritation, inflamed respiratory tract, hyperventilation and, tachycardia are the most affected ones when it comes to the riot control agent oleoresin capsicum (OC) exposure. However, no studies have been done to elucidate the mechanism underlying deterioration of the combined cardiopulmonary functions. Parameters such as acute respiratory, cardiac, parameters and ultrasonography (USG) measurements were investigated in an in vivo setup using Wistar rats at 1 h and 24 h post inhalation exposure to 2%, 6% and 10% OC, whereas, cell migration in rat peritoneal mast cells (RPMCs), metabolomics and eosinophil peroxidase (EPO) activity in bronchoalveolar lavage fluid (BALF) were investigated in an in vitro setup. Results obtained from electrophysiological recording indicated that OC exposure produces apnea and decrease in mean arterial pressure (MAP) was obtained from hemodynamic parameters whereas cardiac parameters assessment revealed increase in the level of cardiac output (CO) and decrease in stroke volume (SV) with recovery towards the post-exposure period. A decrease in the percentage area of certain fatty acid pathway metabolites in BALF appropriately linked the lung injury following OC exposure which was further cemented by increasing concentration of EPO. Histopathology and SEM also proved to be favorable techniques for the detection of OC induced physiological cardiac and pulmonary modifications respectively. Furthermore, Boyden chamber experiment established the chemoattractant property of OC. It may be concluded from the above studies that these newly reported facets may be utilized pharmacologically to mitigate cardiopulmonary adverse effects owing to OC exposure.


Asunto(s)
Corazón/efectos de los fármacos , Corazón/fisiopatología , Exposición por Inhalación/efectos adversos , Pulmón/efectos de los fármacos , Pulmón/fisiopatología , Extractos Vegetales/toxicidad , Sustancias para Control de Disturbios Civiles/toxicidad , Animales , Biomarcadores/metabolismo , Líquido del Lavado Bronquioalveolar/química , Electrocardiografía , Corazón/diagnóstico por imagen , Hemodinámica/efectos de los fármacos , Pulmón/diagnóstico por imagen , Pulmón/metabolismo , Masculino , Miocardio/metabolismo , Miocardio/patología , Extractos Vegetales/farmacocinética , Ratas , Ratas Wistar , Pruebas de Función Respiratoria , Sustancias para Control de Disturbios Civiles/farmacocinética , Distribución Tisular
6.
Acta Trop ; 210: 105620, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32649995

RESUMEN

Housefly, Musca (M) domestica L. (Diptera: Muscidae) is a pervasive insect that transmits a variety of pathogens to humans and livestock. Although numerous synthetic pesticides are available to combat houseflies, their ecological and toxicological concerns have led to the exploration of natural products as safer alternatives. The present work was designed to develop an essential oil based controlled-release evaporating tablet (EO-CRT) and investigate its repellency against M. domestica. This study assesses the toxicological impacts of the EO-CRT following its sub-chronic inhalation exposure. Briefly, repellent activity of fourteen essential oils viz. lemon grass, bergamot, mentha, basil, camphor, lavender, clove, patchouli, rosemary, cinnamon, eucalyptus, citronella, jasmine and wild turmeric against M. domestica were screened using the 'Y'-tube olfactometer. The synergistic activity of the best four oils, under preliminary screening, were further evaluated by double and triple blending. The best combination of three oils were finalized for optimization with 17-run, 3-factor, 3-level Box-Behnken design. This was then employed to construct polynomial models and predict the best optimized formulation EO-CRT. EO-CRT was characterized by Differential Scanning Calorimetry (DSC) and Gas Chromatography-Mass Spectroscopy (GC-MS). The efficacy of the EO-CRT against M. domestica was assessed by attraction and repellent assay. Chest X-ray, histopathology and scanning electron microscopy of the exposed lung was performed to study EO-CRT's sub-chronic toxicity on Wistar rats. The EO-CRT showed slow release up to a period of 10 days at room temperature, exhibited 100% repellency (%Error=1.237) against M. domestica and was found to possess all the characteristics of an ideal formulation. Sub-chronic toxicity study further revealed the non-toxic nature of the EO-CRT. Thus, our study provides an assurance that the formulated EO-CRT could be effective not only in repelling the nuisance pest, M. domestica, in human dwellings, but also in minimizing the mechanical transmission of pathogens by it.


Asunto(s)
Moscas Domésticas/efectos de los fármacos , Repelentes de Insectos/farmacología , Aceites Volátiles/farmacología , Animales , Preparaciones de Acción Retardada/farmacología , Femenino , Masculino , Aceites Volátiles/toxicidad , Ratas , Ratas Wistar , Comprimidos/farmacología
7.
Acta Trop ; 210: 105573, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32505595

RESUMEN

Mosquitoes (Diptera; Culicidae) are a biting nuisance and are of economic and health importance, especially for people living in tropical countries like India. Given the environmental concerns and health hazards of synthetic insecticides, development of natural products for the control of mosquito and mosquito-borne diseases are needed. In view of this, an essential oil based novel liquid vaporizer formulation with citronella and eucalyptus oils has been developed using a computer aided Artificial Neural Network and Particle Swarm Optimization (ANN-PSO) algorithm approach, aiming to predict the best optimized formulation (OF). Following the development, OF was characterized by Fourier Transform-Infra Red (FT-IR) spectroscopy and gas chromatography-mass spectroscopy (GC-MS). The efficacy of the OF was assessed against two major mosquito vectors viz. Anopheles stephensi and Aedes albopictus using a Peet-Grady chamber. Finally, toxicological impacts of the OF following its inhalation were investigated as per the Organization for Economic Co-operation and Development (OECD) guidelines. The results revealed all the ideal characteristics of the OF which were found to provide a slow release of up to 450 h at room temperature. Most importantly, the OF, exhibited 50% mosquito knock down (KT50) within 11.49±1.34 and 14.15±2.15 min against An. stephensi and Ae. albopictus respectively. Toxicity assessment showed a non toxic nature of the OF following inhalation. Thus the present development would be beneficial for controlling both An. stephensi and Ae. albopictus without any associated health hazards.


Asunto(s)
Cymbopogon , Eucalyptus , Insecticidas/administración & dosificación , Control de Mosquitos/métodos , Nebulizadores y Vaporizadores , Aceites Volátiles/administración & dosificación , Aedes , Animales , Anopheles
8.
Exp Lung Res ; 46(3-4): 81-97, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32131645

RESUMEN

Aim: The use of oleoresin capsicum (OC) sprays, due to their irreversible health effects has now grown into a matter of heated debate. In the present study, the early phase pulmonary events involving chemotactic and inflammatory mediators after short-exposure duration to OC have been presented.Materials and methods: Female Wistar rats used in the evaluation of respiratory parameters at 1 h, 3 h, and 24 h post-exposure, were sacrificed for the evaluation of blood cell counts, BALF cytokine estimation, lung capillary leakage, study of oxidative stress and histopathology of the lungs.Results: Results confirmed a dose-dependent effect of OC exposure on serum clinical chemistry and hematological parameters. Subsequent upregulation of IL-l and TNF-α indicated lung's responses to acute oxidant-induced injury and inflammation after OC exposure. Significant alterations in the pulmonary levels of reactive oxygen intermediates were seen following the inhalation of OC. Infiltration of polymorphonuclear leukocytes, mostly neutrophils, into the site of infection was evident in the cytocentrifuged samples of BALF. Histological samples of rat lung sections revealed the recruitment of inflammatory cells in the airways and around blood vessels in the subepithelium of conducting airways.Conclusion: Results of the present study demonstrated that, exposure to OC spray may mitigate inflammatory response and development of acute lung injury in rats. However, it can be concluded that although OC spray causes pulmonary hazards in the aforementioned concentrations, it can be used as a non-lethal riot control agent in minimal concentration. Understanding the in-depth mechanism of action in the molecular and receptor level will help in developing effective antagonist against OC.


Asunto(s)
Exposición por Inhalación/efectos adversos , Pulmón/efectos de los fármacos , Extractos Vegetales/toxicidad , Edema Pulmonar/inducido químicamente , Sustancias para Control de Disturbios Civiles/toxicidad , Animales , Citocinas/sangre , Femenino , Estrés Oxidativo , Extractos Vegetales/inmunología , Edema Pulmonar/sangre , Ratas Wistar , Sustancias para Control de Disturbios Civiles/inmunología
9.
Braz. J. Pharm. Sci. (Online) ; 56: e18806, 2020. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1249156

RESUMEN

Ethnomedicinal survey documents the traditional practices of Tetrastigma angustifolia leaves in the management of diabetes in the North-eastern region of India. The present study was aimed at isolation of possible antidiabetic principle(s) from T. angustifolia leaves and evaluation of antidiabetic efficacy of isolated compound(s) in experimental animal model. The methanolic extract of T. angustifolia leaves was obtained by Soxhlet extraction method and subjected to silica gel column chromatography (100-200 mesh). Fraction 18-176 chloroform:methanol (70:30) yielded a pale yellow colored compound. The structure of pure compound was elucidated with the help of UV, IR, NMR and Mass spectrometric/techniques. The antioxidant activity of the isolated compound was evaluated in vitro by various radical scavenfing assay methods.. Oral acute toxicity study was carried out according to OECD guideline 423 in Wistar rats. The antidiabetic efficacy of the isolated compound was evaluated in STZ-induced diabetic rats at the dose of 5 mg/kg b.w. for duration of 21 days. The present study reports a new flavocnoid compound isolated from the methanolic extract of T. angustifolia leaves and identified as 8-hydroxyapigenin 7-O-D-glucopyranoside. The flavonoid compound exhibited potent antidiabetic (hypoglicemic) activity in STZ-induced diabetic rats with promising antioxidant (radical scavenging activity) potential in vitro.


Asunto(s)
Flavonoides/análisis , Hojas de la Planta/efectos adversos , Vitaceae/clasificación , Técnicas In Vitro/instrumentación , Cromatografía , Modelos Animales , Dosificación/efectos adversos , Hipoglucemiantes/farmacología , Antioxidantes/análisis
10.
Regul Toxicol Pharmacol ; 97: 209-224, 2018 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-29969653

RESUMEN

In the recent years, growing concern about the potential toxicity of synthetic repellents has led to the development of environmentally safe non-toxic insect control methods. Present investigation explores the toxicological impacts of ethyl anthranilate-loaded mosquito repellent patch (EAMRP) on respiratory system following acute and sub-chronic inhalation exposure in Wistar rats. Lungs parameters such as enhanced pause, tidal volume, respiration rate, inspiration time, and expiration time were determined using whole body plethysmograph. X-ray, scanning electron microscopy and histology were utilized to study the morphology and microscopical architecture of lungs. Hematological and serum biochemical markers were estimated. Cytokines such as IL-1ß, IL-2, and IL-12 were also estimated in bronchoalveolar lavage fluid using ELISA kits. Finally, acute oral and dermal toxicity studies were carried out to study the accidental or intentional poisoning due to the ingestion and skin contact of EAMRP, respectively. The findings demonstrate that inhalation exposure to EAMRP did not pose any significant dose related toxicity in above mentioned experiments. Further, no appreciable toxicity was observed in both acute oral and dermal exposure. Thus, these results revealed the non toxic nature of EAMRP in preclinical studies. Hence, EAMRP can be used successfully as an alternative to existing synthetic repellents without any potential health hazards.


Asunto(s)
Líquido del Lavado Bronquioalveolar/química , Repelentes de Insectos/toxicidad , Pulmón/efectos de los fármacos , ortoaminobenzoatos/toxicidad , Animales , Culicidae , Citocinas/análisis , Citocinas/biosíntesis , Ensayo de Inmunoadsorción Enzimática , Femenino , Exposición por Inhalación , Repelentes de Insectos/administración & dosificación , Repelentes de Insectos/química , Pulmón/metabolismo , Pulmón/patología , Masculino , Conejos , Ratas , Ratas Wistar , ortoaminobenzoatos/administración & dosificación , ortoaminobenzoatos/química
11.
Biomed Pharmacother ; 96: 1501-1512, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29198921

RESUMEN

Capsaicin, a well known vanilloid, has shown evidence of an ample variety of biological effects which make it the target of extensive research ever since its identification. In spite of the fact that capsaicin causes health hazards in quite a few ways, yet, the verity cannot be ignored that capsaicin has several therapeutic implications. In patients with hypersensitive bladders, vesical instillation of 1 mM capsaicin markedly improved urinary frequency and urge incontinence. Again, administration of capsaicin favors an augmentation in lipid mobilization and a decrease in adipose tissue mass. Topical capsaicin cream as well decreases postsurgical neuropathic pain and is preferred by patients over a placebo among other therapies. Several in vitro studies have revealed that capsaicin results in growth arrest in some transformed cell lines. Furthermore, capsaicin has been proven to be an undeniably exciting molecule and remains a valuable drug for alleviating pain and itch. It has been recognized that capsaicinoids are the most potential agonists of capsaicin receptor (TRPV1). However, vanilloids could exert the beneficial effects not only through the receptor-dependent pathway but also through the receptor-independent one. The involvement of serotonin, neuropeptide Substance P and somatostatin in the pharmacological actions of capsaicin has been expansively investigated. Better understanding of the established TRPV1 receptor mechanism as well as exploring other possible receptor mechanism may publicize other new clinical efficacies of capsaicin. Further, clinical studies are required in several of these conditions to establish the efficacy of capsaicin.


Asunto(s)
Capsaicina/farmacología , Capsaicina/uso terapéutico , Animales , Humanos , Canales Catiónicos TRPV/metabolismo
12.
J Food Drug Anal ; 25(4): 968-975, 2017 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-28987374

RESUMEN

Compromised stability of pharmaceutical formulations loaded with volatiles is a serious problem associated with devices designed to deliver volatile compounds. The present study has been focused to evaluate the stability potential of matrix-type polymeric patches composed of volatile ethyl anthranilate for prophylaxis against vector-borne diseases. Ethyl anthranilate-loaded matrix-type polymeric patches were fabricated by solvent evaporation method on an impermeable backing membrane and attached to temporary release liners. Stability testing of the polymeric patches was performed as per the International Conference on Harmonization (ICH) guidelines for 6 months under accelerated conditions. In addition, the quantification of residual solvents was also performed as per the ICH guidelines. After conducting the stability studies for 6 months, the optimized patches showed the best possible results with respect to uniformity of drug content, physical appearance, and other analytical parameters. Furthermore, the amount of residual solvent was found well below the accepted limit. Thus, the present report outlined the analytical parameters to be evaluated to ensure the stability of a certain devices consisting of volatile compounds.


Asunto(s)
Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/instrumentación , Preparaciones Farmacéuticas/química , Polímeros/química , ortoaminobenzoatos/química , Estabilidad de Medicamentos
13.
Biomed Pharmacother ; 95: 84-94, 2017 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-28826101

RESUMEN

BACKGROUND: Despite the availability of synthetic antidiabetic drugs, diabetes mellitus is still affecting millions of people with increasing rate of disease incidence and mortality throughout the world. Ethnomedicinal survey documents the traditional usefulness of Callicarpa arborea Roxb. stem bark in the management of diabetes mellitus. MATERIALS AND METHODS: In our study, hydro-alcoholic extract (HAE) of Callicarpa arborea stem bark was prepared according to WHO guidelines for herbal drugs, and screened for antidiabetic activity in streptozotocin (STZ)-induced diabetic rats. Acute oral toxicity and in vitro antioxidant activity studies along with phytochemical analyses of HAE were also carried out. RESULTS: Acute oral toxicity study indicated that HAE was safe up to a dose of 2000mg/kg body weight of rats. Results of antidiabetic activity study revealed that HAE of C. arborea stem bark possesses significant (p<0.05) hypoglycemic activity compared to normal control group in experimental rats. Histological observations of treated pancreas and liver tissues confirmed the antidiabetic efficacy of HAE. In antioxidant activity, HAE exhibited significant radical scavenging activity. CONCLUSION: From results, it can be concluded that HAE of C. arborea stem bark may have possible role as herbal antioxidants in the prevention and/or treatment of oxidative stress-induced diabetes mellitus. The antioxidant property of plant phenolic and flavonoid contents present in HAE might be responsible for the antidiabetic efficacy of C. arborea stem bark.


Asunto(s)
Antioxidantes/farmacología , Callicarpa/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Corteza de la Planta/química , Extractos Vegetales/farmacología , Animales , Antioxidantes/química , Hipoglucemiantes/efectos adversos , Hipoglucemiantes/química , Extractos Vegetales/efectos adversos , Extractos Vegetales/química , Tallos de la Planta , Ratas , Superóxidos
14.
Acta Trop ; 174: 56-63, 2017 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-28666890

RESUMEN

Growing concern on the application of synthetic mosquito repellents in the recent years has instigated the identification and development of better alternatives to control different mosquito-borne diseases. In view of above, present investigation evaluates the repellent activity of ethyl anthranilate (EA), a non-toxic, FDA approved volatile food additive against three known mosquito vectors namely, Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus under laboratory conditions following standard protocols. Three concentration levels (2%, 5% and 10% w/v) of EA were tested against all the three selected mosquito species employing K & D module and arm-in-cage method to determine the effective dose (ED50) and complete protection time (CPT), respectively. The repellent activity of EA was further investigated by modified arm-in-cage method to determine the protection over extended spatial ranges against all mosquito species. All behavioural situations were compared with the well-documented repellent N,N-diethylphenyl acetamide (DEPA) as a positive control. The findings demonstrated that EA exhibited significant repellent activity against all the three mosquitoes species. The ED50 values of EA, against Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus were found to be 0.96%, 5.4% and 3.6% w/v, respectively. At the concentration of 10% w/v, it provided CPTs of 60, 60 and 30min, respectively, against Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus mosquitoes. Again in spatial repellency evaluation, EA was found to be extremely effective in repelling all the three tested species of mosquitoes. Ethyl anthranilate provided comparable results to standard repellent DEPA during the study. Results have concluded that the currently evaluated chemical, EA has potential repellent activity against some well established mosquito vectors. The study emphasizes that repellent activity of EA could be exploited for developing effective, eco-friendly, acceptable and safer alternative to the existing harmful repellents for personal protection against different hematophagous mosquito species.


Asunto(s)
Aedes/efectos de los fármacos , Anopheles/efectos de los fármacos , Culex/efectos de los fármacos , Repelentes de Insectos/farmacología , Mosquitos Vectores/efectos de los fármacos , ortoaminobenzoatos/farmacología , Animales , Proteínas del Tejido Nervioso/efectos de los fármacos , Proteínas de Xenopus/efectos de los fármacos
15.
J Chromatogr Sci ; 55(6): 645-653, 2017 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-28334923

RESUMEN

A simple, accurate and sensitive reversed-phase high-performance liquid chromatographic (RP-HPLC) method has been developed for the estimation of ethyl 2-aminobenzoate (EAB) in a matrix type monolithic polymeric device and validated as per the International Conference on Harmonization guidelines. The analysis was performed isocratically on a ZORBAX Eclipse plus C18 analytical column (250 × 4.4 mm, 5 µm) and a diode array detector (DAD) using acetonitrile and water (75:25 v/v) as the mobile phase by keeping the flow-rate constant at 1.0 mL/min. Determination of EAB was not interfered in the presence of excipients. Inter- and intra-day relative standard deviations were not higher than 2%. Mean recovery was between 98.7 and 101.3%. Calibration curve was linear in the concentration range of 0.5-10 µg/mL. Limits of detection and quantification were 0.19 and 0.60 µg/mL, respectively. Thus, the present report put forward a novel method for the estimation of EAB, an emerging insect repellent, by using RP-HPLC technique.


Asunto(s)
Benzocaína/análisis , Cromatografía Líquida de Alta Presión/métodos , Cromatografía de Fase Inversa/métodos , Repelentes de Insectos/análisis , Modelos Lineales , Membranas Artificiales , Polímeros/química , Reproducibilidad de los Resultados , Sensibilidad y Especificidad
16.
Acta Trop ; 167: 216-230, 2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-28040483

RESUMEN

Mosquito being the major medically important arthropod vector; requires utmost attention to reduce the sufferings and economic consequences of those living in the endemic regions. This is only possible by minimising the human-mosquito contact by an absolute preventing measure. However, unfortunately, such absolute measures are yet to be developed despite enormous efforts and huge investments worldwide. In the absence of vaccines for number of mosquito-borne diseases, repellents could be an attractive option for both military personal and civilians to minimise the risk of contacting different mosquito-borne diseases. However, to achieve this golden goal, the detailed knowledge of a particular repellent is must, including its mode of repellency and other relevant informations. Here, in the present article, an effort has been made to convey the best and latest information on repellents in order to enhance the knowledge of scientific community. The review offers an overview on mosquito repellents, the novel discoveries, and areas in need of attention such as novel repellent formulations and their future prospective.


Asunto(s)
Vectores Artrópodos/efectos de los fármacos , Culicidae/efectos de los fármacos , Repelentes de Insectos/uso terapéutico , Animales , Humanos , Estudios Prospectivos
17.
Food Chem Toxicol ; 48(1): 326-35, 2010 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-19852998

RESUMEN

The present study was undertaken to evaluate the protective effect of aqueous extract of Corchorus olitorius leaves (AECO) against sodium arsenite-induced toxicity in experimental rats. The animals exposed to sodium arsenite at a dose of 10mg/kg body weight p.o. for 10days exhibited a significant inhibition (p<0.01) of hepatic and renal antioxidant enzymes namely superoxide dismutase, catalase, glutathione-S-transferase, glutathione peroxidase and glutathione reductase. In addition, arsenic intoxication significantly decreased (p<0.01) the level of reduced glutathione and increased (p<0.01) the levels of oxidized glutathione and thiobarbituric acid reactive substances in selected tissues. Treatment with AECO at doses of 50 and 100mg/kg body weight p.o. for 15days prior to arsenic intoxication significantly improved hepatic and renal antioxidant markers in a dose dependant manner. AECO treatment also significantly reduced the arsenic-induced DNA fragmentation of hepatic and renal tissues. Histological studies on the ultrastructural changes of liver and kidney supported the protective activity of the AECO. The results concluded that the treatment with AECO prior to arsenic intoxication has significant role in protecting animals from arsenic-induced hepatic and renal toxicity.


Asunto(s)
Arsenitos/antagonistas & inhibidores , Arsenitos/toxicidad , Corchorus/química , Compuestos de Sodio/antagonistas & inhibidores , Compuestos de Sodio/toxicidad , Animales , Catalasa/metabolismo , Fragmentación del ADN , Flavonoides/análisis , Flavonoides/farmacología , Glutatión/metabolismo , Glutatión Peroxidasa/metabolismo , Riñón/efectos de los fármacos , Riñón/metabolismo , Riñón/patología , Pruebas de Función Renal , Peroxidación de Lípido/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Pruebas de Función Hepática , Masculino , Estrés Oxidativo/efectos de los fármacos , Fenoles/análisis , Fenoles/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Polifenoles , Quercetina/farmacología , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismo , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo
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