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Euphorbia pulcherrima is an important medicinal plant that is used in a traditional system for its curative properties such as analgesic potency, antipyretic, anti-inflammatory, sedation potential, and antidepressant and cure of diseases such as skin diseases. This study deals with the isolation of two flavonoids namely spinacetin (1) and patuletin (2) from chloroform fraction of Euphorbia pulcherrima. The isolated compound spinacetin (1) and patuletin (2) were screened for in vivo anti-inflammatory, analgesic, sedative, and muscle relaxant effects. Compounds 1 and 2 were assessed against hot plate-induced noxious stimuli at various doses which showed excellent (p < 0.05) analgesic effect in a dose-dependent manner. The muscle relaxant activity was determined by traction and inclined screening model, both compounds showed significant muscle relaxant activity with time. The sedative potential of isolated compounds 1 and 2 was determined by the open field model, both compounds showed good sedation (p < 0.05) at 20 mg/kg. The anti-inflammatory potential of compound 1 was recorded by histamine-induced paw edema and carrageen paw edema model, and in both models, compounds 1 and 2 showed strong effect at 20 mg/kg. Binding orientations, binding energy values, and computed inhibition constants (Ki) values revealed that the studied compounds have a good to excellent inhibition potential against μ-opioid receptors and COX-2. [ABSTRACT FROM AUTHOR]

Euphorbia pulcherrima is an important medicinal plant that is used in a traditional system for its curative properties such as analgesic potency, antipyretic, anti-inflammatory, sedation potential, and antidepressant and cure of diseases such as skin diseases. This study deals with the isolation of two flavonoids namely spinacetin (1) and patuletin (2) from chloroform fraction of Euphorbia pulcherrima. The isolated compound spinacetin (1) and patuletin (2) were screened for in vivo anti-inflammatory, analgesic, sedative, and muscle relaxant effects. Compounds 1 and 2 were assessed against hot plate-induced noxious stimuli at various doses which showed excellent (p < 0.05) analgesic effect in a dose-dependent manner. The muscle relaxant activity was determined by traction and inclined screening model, both compounds showed significant muscle relaxant activity with time. The sedative potential of isolated compounds 1 and 2 was determined by the open field model, both compounds showed good sedation (p < 0.05) at 20 mg/kg. The anti-inflammatory potential of compound 1 was recorded by histamine-induced paw edema and carrageen paw edema model, and in both models, compounds 1 and 2 showed strong effect at 20 mg/kg. Binding orientations, binding energy values, and computed inhibition constants (Ki) values revealed that the studied compounds have a good to excellent inhibition potential against μ-opioid receptors and COX-2. [ABSTRACT FROM AUTHOR]

Objective: Adverse metabolic changes associated with loss of ovarian function increase the risk of developing metabolic syndrome and non-alcoholic fatty liver disease (NAFLD) in postmenopausal women. Naringenin improves metabolic disturbances in vitro and in vivo. In the present study, we tested the effects of naringenin on metabolic disturbances resulting from estrogen deficiency in ovariectomized mice. Materials/methods: Ovariectomized C57BL/6 J female mice were fed a control diet (10% calories from fat) for 11 weeks. Mice either continued on the control diet (n = 9) or were switched to the control diet supplemented with 3% naringenin (n = 10) for the next 11 weeks. Energy expenditure was measured by indirect calorimetry and activity was monitored by infrared beam breaks. Intra-abdominal and subcutaneous adiposity was evaluated by magnetic resonance imaging (MRI). Blood biochemical measures of metabolic response included glucose, insulin, adipokines, and lipids. Lipid content in liver and muscle and expression of relevant genes in adipose tissue, liver, and muscle were quantified. Results: Ovariectomized mice fed naringenin exhibited lower fasting glucose and insulin levels compared to controls, with over 50% reduction of intra-abdominal and subcutaneous adiposity. Plasma leptin and leptin mRNA in adipose depots were also decreased in mice fed a naringenin diet. Monocyte chemoattractant protein-1 (MCP1/Ccl2) and interleukin 6 (IL-6/Il6) mRNA expression levels were significantly lower in perigonadal adipose tissue of naringenin-supplemented mice. We also observed that mice fed a naringenin diet had less hepatic lipid accumulation with corresponding alterations of hepatic gene expression associated with de novo lipogenesis, fatty acid oxidation, and gluconeogenesis. Conclusion: Dietary naringenin attenuates many of the metabolic disturbances associated with ovariectomy in female mice. [ABSTRACT FROM AUTHOR]

Objective: Adverse metabolic changes associated with loss of ovarian function increase the risk of developing metabolic syndrome and non-alcoholic fatty liver disease (NAFLD) in postmenopausal women. Naringenin improves metabolic disturbances in vitro and in vivo. In the present study, we tested the effects of naringenin on metabolic disturbances resulting from estrogen deficiency in ovariectomized mice. Materials/methods: Ovariectomized C57BL/6 J female mice were fed a control diet (10% calories from fat) for 11 weeks. Mice either continued on the control diet (n = 9) or were switched to the control diet supplemented with 3% naringenin (n = 10) for the next 11 weeks. Energy expenditure was measured by indirect calorimetry and activity was monitored by infrared beam breaks. Intra-abdominal and subcutaneous adiposity was evaluated by magnetic resonance imaging (MRI). Blood biochemical measures of metabolic response included glucose, insulin, adipokines, and lipids. Lipid content in liver and muscle and expression of relevant genes in adipose tissue, liver, and muscle were quantified. Results: Ovariectomized mice fed naringenin exhibited lower fasting glucose and insulin levels compared to controls, with over 50% reduction of intra-abdominal and subcutaneous adiposity. Plasma leptin and leptin mRNA in adipose depots were also decreased in mice fed a naringenin diet. Monocyte chemoattractant protein-1 (MCP1/Ccl2) and interleukin 6 (IL-6/Il6) mRNA expression levels were significantly lower in perigonadal adipose tissue of naringenin-supplemented mice. We also observed that mice fed a naringenin diet had less hepatic lipid accumulation with corresponding alterations of hepatic gene expression associated with de novo lipogenesis, fatty acid oxidation, and gluconeogenesis. Conclusion: Dietary naringenin attenuates many of the metabolic disturbances associated with ovariectomy in female mice. [ABSTRACT FROM AUTHOR]