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1.
Sci Total Environ ; 915: 170113, 2024 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-38232846

RESUMO

Pesticides are chemical substances of natural or synthetic origin that are used to eradicate pests and insects. These are indispensable in the agricultural processes for better crop production. Pesticide use aims to promote crop yield and protect the crops from diseases and damage. Pesticides must be handled carefully and disposed of appropriately because they are dangerous to people and other species by default. Environmental pollution occurs when pesticide contamination spreads away from the intended plants. Older pesticides such as lindane and dichlorodiphenyltrichloroethane (DDT) may remain in water and soil for a longer time. These accumulate in various parts of the food chain and cause damage to the ecosystem. Biological techniques in the management of pest control such as importation, augmentation, and conservation, and the accompanying procedures are more efficient, less expensive, and ecologically sound than other ways. This review mainly focuses on the consequences on the targeted and non-targeted organisms including the health and well-being of humans by the use of pesticides and their toxicity. The side effects that occur when a pesticide's LD50 exceeds the accepted limit through oral or skin penetration due to their binding to various receptors such as estrogen receptors, GABA, EGFR, and others. These pesticide classes include carbamates, pyrethroids, organochlorides, organophosphorus, and others. The current study seeks to highlight the urgent requirement for a novel agricultural concept that includes a major reduction in the use of chemical pesticides.


Assuntos
Praguicidas , Piretrinas , Humanos , Praguicidas/análise , Ecossistema , Poluição Ambiental , Produtos Agrícolas
2.
Curr Diabetes Rev ; 19(6): e170822207592, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35980059

RESUMO

Diabetes mellitus is a crucial health issue worldwide. The worldwide ubiquity is 8.8% among adults, which is predicted to rise to 10.4% by 2040. Diabetic neuropathy is a long-term complication associated with the diabetes mellitus condition, which primarily targets Schwann cells, peripheral axons and cell bodies (perikarya) in DRG (dorsal root ganglia). It can be accompanied by different factors such as metabolic factors such as insulin resistance, hypertension, obesity, low HDL level, and hypertriglyceridemia. The etiology of DPN is multifactorial. It is caused by hyperglycemia, micro-angiopathy, HbA1c, duration of diabetes, smoking status, high-density lipoprotein cholesterol and hypertension. Also, increased glucose conditions decrease vitamin D levels. Vitamin D, which is involved in neurotrophins such as NGF (nerve growth factor) and NCH (neuronal calcium homeostasis), plays a neuroprotective role in peripheral nerves. Depletionleads to vitamin D deficiency which further develops peripheral neuropathy in diabetic patients. Accumulation of AGEs (advanced glycation end product) plays a significant role in the pathogenesis of sensory neuronal damage. It contributes to microangiopathy and endoneurial vascular dysfunction in peripheral nerves. With vitamin D supplementation, the neuropathy pain scores were improved.


Assuntos
Diabetes Mellitus Tipo 2 , Neuropatias Diabéticas , Deficiência de Vitamina D , Adulto , Humanos , Neuropatias Diabéticas/etiologia , Vitamina D , Deficiência de Vitamina D/complicações , Vitaminas , Obesidade/complicações , Diabetes Mellitus Tipo 2/complicações
3.
J Indian Soc Periodontol ; 21(6): 499-502, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29551871

RESUMO

Correct diagnosis of white lesions of the oral cavity is sometimes difficult, because some oral white lesions behave differently and tend to change their appearance with time. Clinicians often wrongly diagnose such lesions as oral leukoplakias and treat simply. Lesions recur and turn malignant. Proliferative verrucous leukoplakia (PVL) is a distinct form of oral leukoplakia characterized by a high recurrence rate and high rate of transformation into oral squamous cell carcinoma. We present herein a case of PVL which was misdiagnosed as oral leukoplakia and progressed to oral carcinoma.

4.
Future Med Chem ; 9(1): 37-60, 2017 01.
Artigo em Inglês | MEDLINE | ID: mdl-27995810

RESUMO

The finding of promising drugs represents a huge challenge in cancer therapeutics, therefore it is important to seek out novel approaches and elucidate essential cellular processes in order to identify potential drug targets. Studies on DNA repair pathway suggested that an enzyme, PARP, which plays a significant role in DNA repair responses, could be targeted in cancer therapy. Hence, the efficacy of PARP inhibitors in cancer therapy has been investigated and has progressed from the laboratory to clinics, with olaparib having already been approved by the US FDA for ovarian cancer treatment. Here, we have discussed the development of PARP inhibitors, strategies to improve their selectivity and efficacy, including innovative combinational and synthetic lethality approaches to identify effective PARP inhibitors in cancer treatment.


Assuntos
Antineoplásicos/farmacologia , Neoplasias/tratamento farmacológico , Neoplasias/enzimologia , Inibidores de Poli(ADP-Ribose) Polimerases/farmacologia , Poli(ADP-Ribose) Polimerases/metabolismo , Antineoplásicos/química , Humanos , Inibidores de Poli(ADP-Ribose) Polimerases/química
5.
Chin J Integr Med ; 2015 Sep 09.
Artigo em Inglês | MEDLINE | ID: mdl-26354747

RESUMO

Use of phyto-medicine and digitalization of phyto-compounds has been fallen enthralling field of science in recent years. Quercetin, a flavonoid with brilliant citron yellow pigment, is typically found in fruits and leafy vegetables in reasonable amount. Quercetin's potentials as an antioxidant, immune-modulator, antiinflammatory, anti-cancer, and others have been the subject of interest in this review. Although, profiling the insights in to the molecular characterization of quercetin with various targets provided the loop-holes in understanding the knowledge for the aforementioned mechanisms, still necessitates research globally to unearth it completely. Thus, the available science on the synthesis and significant role played by the old molecule - quercetin which does wonders even now have been vividly explained in the present review to benefit the scientific community.

6.
Mini Rev Med Chem ; 13(12): 1812-35, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-24032508

RESUMO

In the last few decades, a lot of work has been done on heterocycles, especially the imidazole ring, to obtain a scaffold with potential pharmacological properties such as antibacterial, antifungal, anticancer, antiviral, antidiabetic and others, with lesser side effects. The search for new biologically active imidazoles continues to be an interesting area of investigation in medicinal chemistry. The present paper aims to bring together and discuss the wealth of information on antibacterial profile of imidazoles. So it can be employed for future development to obtain new potent drug molecules.


Assuntos
Antibacterianos/química , Imidazóis/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Imidazóis/síntese química , Imidazóis/farmacologia , Patentes como Assunto , Relação Estrutura-Atividade
7.
J Enzyme Inhib Med Chem ; 24(3): 763-70, 2009 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18720190

RESUMO

A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines. Compound 6 has shown interesting cytotoxicity (IC(50) = 5.67 microm) in ovarian cancer, while compound 10 exhibited promising cytotoxicity in ovarian (IC(50) = 6.1 microm) and oral (IC(50) = 4.17 microm) cancers. These compounds could be of use in designing new anti-cancer agents.


Assuntos
Amidas/síntese química , Amidas/farmacologia , Aminoácidos/química , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Desenho de Fármacos , Amidas/química , Antineoplásicos/química , Linhagem Celular , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Neoplasias Bucais/patologia , Neoplasias Ovarianas/patologia
8.
Bioorg Med Chem Lett ; 18(18): 5058-62, 2008 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-18752941

RESUMO

A new series of betulinic acid derivatives have been synthesized by introducing heterocyclic ring between C-2 and C-3 positions of betulinic acid. Further modifications were also carried out by reduction of C-20(29) unsaturated bond and substitution of C-28 carboxyl group by ester and amide linkage to enhance the selectivity. Compound 11 resulted in IC(50) of 2.44, 2.5, and 2.7 microg/ml on MIAPaCa, PA-1, and SW620 cancer cell lines, respectively. Compound 38 resulted in IC(50) of 0.67 microg/ml on MIAPaCa cell line.


Assuntos
Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/farmacologia , Triterpenos/síntese química , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Técnicas de Química Combinatória , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Concentração Inibidora 50 , Masculino , Estrutura Molecular , Triterpenos Pentacíclicos , Relação Estrutura-Atividade , Triterpenos/química , Ácido Betulínico
9.
Bioorg Med Chem Lett ; 17(23): 6660-4, 2007 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-17950602

RESUMO

Several 1,8-naphthyridine-3-carboxamide derivatives (8-23) were synthesized and tested for in vitro cytotoxicity against eight cancer cell lines and a normal cell line. Compound 12 exhibited high cytotoxicity (IC(50)=1.37microM) in HBL-100 (breast) cell line while compounds 17 (IC(50)=3.7microM) and 22 (IC(50)=3.0microM) have shown high cytotoxicity in KB (oral) and SW-620 (colon) cell lines, respectively. The synthesized 1,8-naphthyridine-3-carboxamides were also evaluated for anti-inflammatory and myeloprotective activities, indicated by modulation in cytokine and chemokine levels secreted by dendritic cells.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Antineoplásicos/síntese química , Mediadores da Inflamação/farmacologia , Naftiridinas/síntese química , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Humanos , Mediadores da Inflamação/antagonistas & inibidores , Células K562 , Células KB , Camundongos , Células NIH 3T3 , Naftiridinas/farmacologia
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