Carrot （Daucus carom） is a valuable source of health promoting ingredients such as anthocyanin, carotenes, phenolic compounds etc. These substances are important to man as a source of pharmaceuticals, fragrance, agr...Carrot （Daucus carom） is a valuable source of health promoting ingredients such as anthocyanin, carotenes, phenolic compounds etc. These substances are important to man as a source of pharmaceuticals, fragrance, agrochemicals as well as food additives and used for prevention of many chronic diseases. Since these activities may be correlated with the presence of antioxidant compounds, extract of carrot and carrot callus were evaluated for their anthocyanin, flavonoids and total phenolic content as well as total antioxidant activity. Anthocyanin content was measured by spectrophotometric method. Total phenols and flavonoids were analyzed according to the Folin-Ciocalteu method and total antioxidant activity was assessed by ferric reducing/antioxidant power （FRAP） assay. Anthocyanin, flavonoids and total phenolic content were estimated to be 9.36 mg%, 46.96 mg% and 57.01 mg% for callus and 6.82 mg%, 32.96 mg% and 42.69 mg% for carrot, respectively, on fresh weight basis. The total antioxidant activity for the callus and carrot was found to be 51.13 mg, 118.77 mg, 91.08 mg and 140.08 mg equivalent and 79.40 mg, 184.44 mg, 141.43 mg and 217.52 mg equivalent to gallic acid, vitamin C, butylated hydroxyanisole （BHA） and trolox, respectively, when expressed per 100 g on fresh weight basis. The antioxidant activity of fresh carrot was found to be higher compared to its callus.展开更多
The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as ...The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2 b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2 b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure–activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2 b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2 b receptor, which shed lights on the development of novel drugs as CCR2 b receptor antagonists for preventing inflammation related diseases.展开更多
文摘Carrot （Daucus carom） is a valuable source of health promoting ingredients such as anthocyanin, carotenes, phenolic compounds etc. These substances are important to man as a source of pharmaceuticals, fragrance, agrochemicals as well as food additives and used for prevention of many chronic diseases. Since these activities may be correlated with the presence of antioxidant compounds, extract of carrot and carrot callus were evaluated for their anthocyanin, flavonoids and total phenolic content as well as total antioxidant activity. Anthocyanin content was measured by spectrophotometric method. Total phenols and flavonoids were analyzed according to the Folin-Ciocalteu method and total antioxidant activity was assessed by ferric reducing/antioxidant power （FRAP） assay. Anthocyanin, flavonoids and total phenolic content were estimated to be 9.36 mg%, 46.96 mg% and 57.01 mg% for callus and 6.82 mg%, 32.96 mg% and 42.69 mg% for carrot, respectively, on fresh weight basis. The total antioxidant activity for the callus and carrot was found to be 51.13 mg, 118.77 mg, 91.08 mg and 140.08 mg equivalent and 79.40 mg, 184.44 mg, 141.43 mg and 217.52 mg equivalent to gallic acid, vitamin C, butylated hydroxyanisole （BHA） and trolox, respectively, when expressed per 100 g on fresh weight basis. The antioxidant activity of fresh carrot was found to be higher compared to its callus.
基金supported by the Major Scientific and Technological Special Project for Significant New Drugs Creation(No.2012ZX09504001-001)National Natural Science Foundation of China(No.81102876+2 种基金81430082)the Fundamental Research Funds for the Central Universities(No.2015ZD005)333 high level project of Jiangsu Province(NO.BRA2014245)
文摘The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2 b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2 b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure–activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2 b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2 b receptor, which shed lights on the development of novel drugs as CCR2 b receptor antagonists for preventing inflammation related diseases.
