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1.
Mini Rev Med Chem ; 13(12): 1769-77, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23432381

RESUMO

Curcumin, a natural diaryl heptanoid continues to be used as an alternative medicinal agent in many parts of South East Asia for treatment of many ailments. It can be usually obtained from substituted aryl aldehydes and acetylacetone and this route enables synthesis of a diverse set of curcumin analogues. Numerous analogues have been synthesized and tested by several researchers to investigate their activity against known biological targets and to improve upon the pharmacological and ADME profile by modifying substitutions on aromatic rings, ß-diketone moiety and two flanking double bonds conjugated to the ß-diketone moiety. Successful synthesis of such derivatives with modifications has resulted in the development of potential anticancer candidates that target various stages in cancer cell growth and development. Based on the evidences in modifications of these three functional elements, we have attempted to summarize the structure activity relationship of molecules which can be further utilized by researchers in medicinal chemistry in exploring the structure of curcumin.


Assuntos
Antineoplásicos/química , Curcumina/análogos & derivados , Antineoplásicos/síntese química , Antineoplásicos/toxicidade , Apoptose/efeitos dos fármacos , Curcumina/síntese química , Curcumina/toxicidade , Humanos , Cetonas/química , Relação Estrutura-Atividade
2.
Toxicol Int ; 18(1): 31-4, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21430918

RESUMO

A total of 160 White Leghorns of 20 wk age were divided randomly into eight groups. Groups 1, 3, 4 and 5 were fed basal feed and the rest were fed 5% vanaspati supplemented feed until 42 wk of age. From 42 to 54 wk, groups 3, 4 and 5 were fed 1% ferrous sulfate, 100 ppm chlorpyrifos (CPS) and 100 ppm cadmium, respectively, along with basal feed and groups 6, 7 and 8 were fed similar stressors, respectively, along with 5% vanaspati. Groups 1 and 2 served as controls for basal feed and 5% vanaspati feed. Alkaline phosphatase (ALP), alanine transaminase (ALT), total protein, albumin, globulin, A/G ratio, total cholesterol, high density cholesterol (HDL), triglycerides, creatinine, hemagglutination inhibition (HI) titer, and phytohemagglutination (PHA) index were studied. Supplementation of vanaspati resulted in a significant reduction in PHA, cholesterol, albumin and HI titer. Cadmium significantly increased ALP, AST, creatinine and paradoxically increased HDL cholesterol and HI titers. Vanaspati along with cadmium showed similar effects. Administration of CPS lowered PHA index, whereas supplementation along with vanaspati decreased the HI titers and increased the PHA index. Supplementation of vanaspati alone and in combination revealed harmful effects and aggravated the toxicities of CPS and cadmium. Hence, it is concluded that consumption of vanaspati could be harmful.

3.
Toxicol Int ; 17(2): 49-51, 2010 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21170244

RESUMO

Cadmium (Cd) toxicity was studied in broilers, and efficacy of Emblica officinalis (500 ppm in feed), vitamin E (300 ppm in feed), and stressroak (1 g/kg feed) were evaluated for prophylactic and therapeutic management of Cd toxicity. One-day-old male broiler chicks were randomly divided into eight groups consisting of 10 chicks in each. Groups 1 and 2 were maintained as plain control and Cd (100 ppm in feed) toxic control (for six weeks). Groups 3, 4, and 5 were maintained on a combination of Cd (100 ppm in feed) and Emblica officinalis, vitamin E, and stressroak for six weeks. Groups 6, 7, and 8 were maintained with Cd for the first four weeks and on Emblica officinalis, vitamin E, and stressroak during the subsequent two weeks without Cd. Body weights, feed consumed, Feed conversion ratio (FCR), and glulathione (GSH) were significantly (P<0.05) decreased, whereas the activities of antioxidant enzymes (catalase and Superoxide dismutase (SOD)) and concentration of Thiobarbituric acid reacting substances (TBARS) were significantly (P<0.05) increased in toxic control group. After treatment with Emblica officinalis, vitamin E, and stressroak in groups 6, 7, and 8 during last two weeks and discontinuation of Cd, the parameters revealed improvement. From this study, it is concluded that Cd induces toxicity by oxidative stress, and supplementing Emblica officinalis, vitamin E, and stressroak in feed is useful in preventing and treating the toxicity.

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