快速高分辨液相色谱-质谱联用技术分析2型糖尿病大鼠口服四君子汤的药代动力学

研究四君子汤在2型糖尿病大鼠体内的药代动力学。将四君子汤水提物以18 g/kg给正常大鼠和2型糖尿病大鼠灌胃,分别在不同时间点取尿液和粪便,检测其成分及代谢产物的含量;比较正常大鼠和2型糖尿病大鼠的药代动力学参数。采用快速高分辨液相色谱-质谱联用技术对人参皂苷Rc、甘草甜素及其脱糖代谢物进行表征。结果表明,四君子汤中人参皂苷Rc和甘草甜素在2型糖尿病大鼠体内的累计排泄率均高于正常大鼠,大部分人参皂苷通过尿液排出体外、粪便代谢为稀有人参皂苷;大部分甘草甜素在尿液和粪便中转化为甘草次酸,2型糖尿病大鼠与正常大鼠人参皂苷Rc和甘草甜素的药代动力学参数存在明显差异。初步总结了四君子汤在体内的药代动力学机制和代谢途径。本分析方法具有高度自动化,灵敏性和准确性,这将有助于四君子汤的临床研究的不断发展。

Protective effects of Ecklonia cava extract on the toxicity and oxidative stress induced by hair dye in in-vitro and in-vivo models

Oxidative hair dyes containingρ-phenylenediamine(PPD)are reported to induce an allergic reaction by promoting oxidative stress when absorbed through the skin.Despite the associated risk,these hair dyes remain popular owing to their convenience and sharpness of color.This makes it important to minimize the cytotoxicity and oxidative stress induced by PPD-containing hair dyes.Ecklonia cava extract has been evaluated in different studies for its protective effects against external stress in fibroblasts and keratinocytes.Our study was aimed at using in-vitro and in-vivo models to investigate the extract’s effects on cytotoxicity of and oxidative stress induced by PPD-containing hair dyes.Analysis of CIEL*a*b*Color space was first used to determine the range of E.cava extract that would not interfere with the coloring ability of the dye upon addition.Subsequently,the set ranges of E.cava extract(5% and 7%)were added to the hair dye and their toxicity assessed by evaluating the viability of fibroblasts and keratinocytes.The effects on developmental phenotypes and induction of oxidative stress by hair dye were evaluated and compared with those of hair dyes containing different contents of E.cava extract using an in-vivo zebrafish model.Our results showed that E.cava extract in hair dye could significantly decrease the cytotoxicity and levels of oxidative stress caused by hair dyes containing PPD in both in-vitro and in-vivo models.These results suggest that the addition of 7% E.cava extract to 250μg/mL hair dye does not interfere with the coloring ability of the dye while showing significant protective eff ects against the hair dye.The study proposes that the use of E.cava extract as an adduct to hair dyes containing PPD reduces the cytotoxicity and oxidative stress induced by these hair dyes.

Anti-oxidant and anti-inflammatory activities of ultrasonicassistant extracted polyphenol-rich compounds from Sargassum muticum

Polypehnol is an important,potentially bioactive component of Sargassum muticum.In this study,ultrasonic assisted extraction of polyphenol-rich substances was performed using a 38%ethanol solution at a solid:liquid ratio of 1:30 at 68℃ for 32min,determined by single-factor and response surface methodology(RSM)optimization.The content of polyphenol was 5.66mg/g in the crude extract.Further extraction showed that the polyphenol mainly distributed in ethyl acetate(SKEE)and water phases(SKEW).The anti-oxidation test by electron spin resonance(ESR)spectrum showed that the SKEE had the strongest scavenging activity on DPPH(1,1-diphenyl-2-picrylhydrazyl)and alkyl radicals.SKEE was shown noncytotoxic but could inhibit the generation of cellular ROS,showing protective effects in H2O2 and AAPHinduced Vero cells and UV-B irradiated HaCaT cells.SKEE also signifi cantly inhibited the release of NO of LPS-induced RAW 264.7 cells.Therefore,the polyphenol-rich extracts in ethanol and ethyl acetate showed excellent anti-oxidant and anti-infl ammatory activities,which is beneficial to the development of high-value bio-substances.