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1.
Biomed Pharmacother ; 108: 547-557, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30243088

RESUMO

The use of phytochemicals in control of human diseases have been considerable public and scientific interest in current days. Syringic acid (SA), a phenolic compound often found in fruits and vegetables and which is synthesized via shikimic acid pathway in plants. It shows a wide range of therapeutic applications in prevention of diabetes, CVDs, cancer, cerebral ischemia; as well as it possess anti-oxidant, antimicrobial, anti-inflammatory, antiendotoxic, neuro and hepatoprotective activities. It has an effective free radical scavenger and alleviates the oxidative stress markers. The therapeutic property of SA is attributed by the presence of methoxy groups onto the aromatic ring at positions 3 and 5. The strong antioxidant activity of SA may confer its beneficial effects for human health. SA has the potential to modulate enzyme activity, protein dynamics and diverse transcription factors involved in diabetes, inflammation, cancer and angiogenesis. In vivo experimental data and histopathological studies on SA activity has delineated its possible therapeutic mechanisms. Besides usage in biomedical field, SA has greater industrial applications in bioremediation, photocatalytic ozonation, and laccase based catalysis. The present review deals about SA natural sources, biosynthesis, bioavailability, biomedical applications (in vivo and in vito. The review addresses basic information about molecular mechanisms, therapeutic and industrial potential of SA.


Assuntos
Ácido Gálico/análogos & derivados , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Disponibilidade Biológica , Ácido Gálico/farmacologia , Ácido Gálico/uso terapêutico , Humanos , Estresse Oxidativo/efeitos dos fármacos
2.
OMICS ; 17(11): 568-83, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24044363

RESUMO

Nature has been a provenance of medicinal agents for thousands of years. Resveratrol (RESL) is a naturally occurring polyphenolic compound in food stuffs such as peanuts, seeds, berries, grapes, and beverages (red wine). RESL has received significant attention due to a plethora of in vitro and in vivo reports on its cancer chemopreventive and therapeutic properties. In the present study, diacetate RESL derivative (RESL43) was synthesized. The RESL43 displayed potent cytotoxicity and triggered apoptosis in U937 cells as evidenced by poly (ADP-ribose) polymerase (PARP) cleavage, DNA fragmentation, morphological changes, and activation of FasR and FasL genes. The electrophoretic mobility shift assay revealed the suppression NFkB activity in U937 cells after treatment with RESL43 in corroboration with the deactivation of NFkB dependent genes such as IL-8, TNFR, and TNFα. Furthermore, molecular docking and dynamics studies have shown that RESL and RESL43 might exert their inhibitory activity on NFkB by altering the intramolecular binding abilities between DNA and NFkB. Taken together, RESL43 can have greater putative activity than parental RESL in a context of cancer chemoprevention and therapeutics. We suggest that the diacetate resveratrol derivative RESL43 warrants further evaluation in preclinical and clinical bridging studies in the near future.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Estilbenos/farmacologia , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Sítios de Ligação , Linhagem Celular Tumoral , DNA/metabolismo , Fragmentação do DNA , Proteína Ligante Fas/genética , Proteína Ligante Fas/metabolismo , Humanos , Interleucina-8/genética , Interleucina-8/metabolismo , Simulação de Acoplamento Molecular , NF-kappa B/antagonistas & inibidores , NF-kappa B/genética , NF-kappa B/metabolismo , Neoplasias/prevenção & controle , Poli(ADP-Ribose) Polimerases/genética , Poli(ADP-Ribose) Polimerases/metabolismo , Ligação Proteica/efeitos dos fármacos , Receptores do Fator de Necrose Tumoral/genética , Receptores do Fator de Necrose Tumoral/metabolismo , Resveratrol , Estereoisomerismo , Estilbenos/síntese química , Estilbenos/química , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
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