The Effects of Galangin on a Mouse Model of Vitiligo Induced by Hydroquinone

Galangin, the main active component of Alpinia officinarum Hance, was tested in a mouse model of vitiligo induced in C57BL/6 mice by the topical application of 2 mL of 2.5% hydroquinone daily to shaved areas (2 × 2 cm) of dorsal skin for 60 days. Thirty days after the final application of hydroquinone, galangin (0.425, and 4.25 mg/kg) was administered orally for 30 days. The hair colour darkened when it grew back after treatment, and histological analysis showed that the number of melanin‐containing hair follicles had increased after treatment with all doses of galangin groups and 8‐methoxypsoralen (8‐MOP, the positive control) compared with the untreated vitiligo group (p < 0.05). The number of skin basal layer melanocytes and melanin‐containing epidermal cells had also increased significantly with the application of 4.25 mg/kg of galangin. The concentration of tyrosinase (TYR) in serum was found to have increased, whereas the content of malondialdehyde and the activity of cholinesterase had decreased after treatment with all doses of galangin and 8‐MOP, compared with control (p < 0.05). The expression of TYR protein in treated areas of skin also increased with the application of 4.25 mg/kg galangin and 8‐MOP. In conclusion, the results showed that galangin was able to improve vitiligo induced by hydroquinone in mice, with the activity related to concentrations of TYR, expression of TYR protein, activity of malondialdehyde and content of cholinesterase. Galangin may therefore be a potential candidate for the treatment of vitiligo, subject to further investigation. Copyright © 2014 John Wiley & Sons, Ltd.     

不同质量分数高良姜素对人黑色素瘤A375细胞黑素合成及相关基因表达的影响

目的研究不同质量分数高良姜素对人黑色素瘤A375细胞黑素合成及酪氨酸酶基因(TYR)、酪氨酸酶相关蛋白-1(TRP-1)、酪氨酸酶相关蛋白-2(TRP-2)mRNA和蛋白表达的影响。方法采用MTT法测定细胞增殖,左旋多巴氧化法测定酪氨酸酶活性,NaOH裂解法测定黑素合成,采用RT-PCR法、Western-blotting法检测A375细胞中TYR、TRP-1、TRP-2mRNA和蛋白表达。结果 90%高良姜素浓度为1.0～10.0μmol/L对A375细胞具有显著的促增殖作用(P<0.01),而在浓度为20.0μmol/L时,无促A375细胞增殖作用(P>0.05),浓度为0.5～20.0μmol/L均能促进酪氨酸酶活性的升高(P<0.05、0.01),浓度为1.0～20μmol/L具有显著促进黑素升高的作用(P<0.05、0.01),且随着浓度的增加呈增强趋势;99%高良姜素浓度在0.5～20.0μmol/L具有显著促进A375细胞增殖和酪氨酸酶活性升高作用(P<0.01),而对黑素合成无促进作用(P>0.05)。90%高良姜素对TYR、TRP-1 mRNA表达基本无影响,1.0μmol/L时上调TRP-2 mRNA表达(P<0.05);99%高良姜素能上调TYR、TRP-1及TRP-2 mRNA表达;二者均促进TYR蛋白表达,但对TRP-1及TRP-2蛋白表达基本无影响。结论 99%高良姜素能够促进A375细胞增殖及酪氨酸酶活性升高,可能是通过上调TYR、TRP-1、TRP-2的mRNA表达和TYR蛋白表达实现的;而90%高良姜素能够显著促进细胞增殖、酪氨酸酶活性升高及黑素增加,表明90%高良姜素能够促进黑素的合成,但不是通过调节TYR、TRP-1、TRP-2的mRNA表达,可能是通过促进TYR蛋白表达实现的。     

总黄酮、高良姜素和白杨素含量指标综合优选蜂胶前处理方法

目的建立蜂胶含量分析的最佳前处理方法。方法采用单因素及L9(34)正交设计试验,以总黄酮、高良姜素、白杨素成分的含量变化为评价指标,对各流程进行优化,筛选最佳前处理方法。结果最佳前处理方法:药材粉末用95%乙醇50℃超声提取2次,每次30 min。结论该方法准确可靠,能作为蜂胶含量分析前处理方法。     

聚乙二醇修饰高良姜素纳米结构脂质载体处方优化及口服药动学评价

目的 优化聚乙二醇修饰高良姜素纳米结构脂质载体(pegylated gallerythrine nanostructured lipid carriers,PEG-GalNLCs)处方,并进行体外释药行为和体内药动学评价。方法 采用乳化法制备PEG-Gal-NLCs。Box-Behnken设计-效应面法(Box Behnken design-response surface methodology,BBD-RSM)筛选PEG-Gal-NLCs最优处方,测定包封率、载药量、粒径及ζ电位。将PEG-Gal-NLCs混悬液制备成冻干粉,X射线粉末衍射(X-ray powder diffraction,XRPD)法分析高良姜素在PEG-Gal-NLCs冻干粉中的存在形式。考察PEG-Gal-NLCs冻干粉在模拟胃肠液中的释药行为,并对释药模型进行拟合。SD大鼠按50 mg/kg剂量ig后采血,HPLC法测定血药浓度,计算主要药动学参数及相对生物利用度。结果 PEG-Gal-NLCs最佳处方为聚乙二醇-单硬脂酸酯(PEG₂₀₀₀-SA)占载体的质量分数为16%、载体与药物比...     

辽西蜂胶黄酮类化学成分的研究

 目的：开发辽西蜂胶的药用资源，寻找具有药理活性的成分，分离鉴定辽西蜂胶中的黄酮类化合物。方法：采用加压硅胶柱层析等方法提取分离辽西蜂胶中黄酮类成分，用紫外、红外、核磁、质谱4种光谱法对其成分进行分析鉴定。结果：从辽西蜂胶中分离到7种黄酮类化合物，经光谱鉴定分别为白杨素(chrysin Ⅰ;4H-1-benzopyran-4-one,5,7-dihydroxy-2-phenyl-Ⅰ)、良姜素(izatpinin Ⅱ;4H-1-benzopyran-4-one,3,5-dihydroxy-7-methoxy-2-phenyl-Ⅱ)、高良姜素(galangin Ⅲ;4H-1-benzopyran-4-one,3,5,7-trihydroxy-2-phenyl-Ⅲ)、金合欢素［acacetin Ⅳ;4H-1-benzopyran-4-one,5,7-dihydroxy-2-(4-methoxyphenyl)-Ⅳ］、洋芹素［apigenin Ⅴ;4H-1-benzopyran-4-one,5,7-dihydroxy-2-(4-hydroxyphenyl)-Ⅴ］、山萘素［kaempferol Ⅵ;4H-1-benzopyran-4-one,3,5,7-trihydroxy-2-(4-hydroxy-phenyl)-Ⅵ］、鼠李素［rhamnetin Ⅶ;4H-1-benzopyran-4-one,2-(3,4-dihydroxyphenyl)-3,5-dihydroxy-7-methoxy-Ⅶ］。结论：首次报道了辽西蜂胶黄酮类化学成分，其中化合物Ⅱ，Ⅳ，Ⅴ，Ⅵ，Ⅶ为首次从蜂胶中发现。     

基于斑马鱼模型的高良姜素安全性评价研究

目的 评价高良姜素（GA）对斑马鱼整体形态及心、肝、肾主要脏器的影响。方法 采用不同浓度（1、2、4、6、8、12、18、28、30、32、64 μmol·L^-1）高良姜素处理受精后48 h（48 hpf）的斑马鱼,给药24、48 h后（24、48 hpe）,计算斑马鱼死亡率和畸形率;显微镜下观察高良姜素对斑马鱼形态、心率、心包面积、静脉窦-动脉球（SV-BA）距离、肝脏、卵黄囊吸收及眼部水肿情况的影响。结果 斑马鱼暴露在1、2、4、6、8、12 μmol·L^-1浓度下的高良姜素均无死亡;24 hpe,高良姜素对斑马鱼的半数致死浓度（LC⁵⁰）为30 μmol·L^-1;48 hpe的LC⁵⁰为28 μmol·L^-1。与空白对照组比较,24 hpe ,浓度≥ 8 μmol·L^-1的高良姜素处理斑马鱼畸形率显著上升（P<0.05）;48 hpe,浓度≥6 μmol·L^-1的高良姜素处理斑马鱼畸形率显著升高（P<0.01）。与空白对照组相比,4 μmol·L^-1及以下浓度的高良姜素对斑马鱼形态及心、肝、肾无明显影响。与空白对照组相比,在24 hpe,8 μmol·L^-1高良姜素组斑马鱼发育评分、相对体长显著降低（P<0.001）,心脏出现轻微的心包水肿、心包面积显著增加（P<0.05）、心率及SV-BA距离无明显变化,肝脏面积和肝脏荧光强度显著减小（P< 0.001）,卵黄囊面积显著增加（P<0.001）,肾脏无明显变化;在48 hpe,6 μmol·L^-1浓度及以上高良姜素组发育评分显著降低（P<0.05、0.001）,斑马鱼心脏出现轻微的心包水肿、心包面积显著增加（P<0.001）、心率显著减小（P<0.01）、SV-BA距离显著增加（P< 0.01）,肝脏面积和肝脏荧光强度显著减小（P<0.01、0.001）,卵黄囊面积显著增加（P<0.01、0.001）,8 μmol·L^-1组相对体长显著降低（P<0.001）。结论 高良姜素在4 μmol·L^-1及以下对斑马鱼无毒性影响;6 μmol·L^-1及以上浓度对斑马鱼有轻微的心脏毒性和肝脏毒性,在临床应用中要合理控制用量。     

硅胶表面高良姜素分子印迹聚合物的制备及其吸附性能

目的利用表面分子印迹技术制备硅胶表面高良姜素分子印迹聚合物(MIP)。方法采用(3-氨丙基)三甲氧基硅烷对硅胶进行改性,并以改性硅胶为载体,高良姜素为模板分子,甲基丙烯酸(MAA)为功能单体,N,N′-亚甲基二丙烯酰胺(MBA)为交联剂,在优化实验条件下利用表面接枝聚合法合成高良姜素表面分子印迹聚合物(MIP)。采用红外光谱、扫描电镜对聚合物进行表征,静态吸附及竞争性吸附研究聚合物的吸附性能。结果最佳制备条件为高良姜素与MAA的物质的量比为1∶4,MAA与MBA的物质的量比为1∶7,反应温度40℃,反应时间12 h。红外光谱和扫描电镜结果显示,印迹聚合物成功接枝到硅胶表面上并出现了对高良姜素分子产生选择性识别的孔穴和位点。吸附实验表明,该MIP对高良姜素分子具有特异的识别性和较好的亲和性,相对于对照物灯盏花素和木犀草素,MIP对高良姜素的选择性系数分别为11.2和5.3。结论 MIP对高良姜素识别性好、选择性强,为中药中黄酮类化合物的分离、提取提供了一种新方法。     

The effect of dietary polyphenols on the epigenetic regulation of gene expression in MCF7 breast cancer cells

The CpG island methylator phenotype is characterized by DNA hypermethylation in the promoters of several suppressor genes associated with the inactivation of various pathways involved in tumorigenesis. DNA methylation is catalyzed by specific DNA methyltransferases (DNMTs). Dietary phytochemicals particularly catechol-containing polyphenols were shown to inhibit these enzymes and reactivate epigenetically silenced genes.     

Effect of Alpinia officinarum Hance rhizome extract on spermatogram factors in men with idiopathic infertility: A prospective double‐blinded randomised clinical trial

Despite scientific advances, many of the treatments in male infertility remained indeterminate. In recent years, the attention to herbal remedies as an effective treatment for male infertility is considerable. We designed this study to determine the effects of Alpinia officinarum on the results of semen analysis in men with idiopathic infertility. In this clinical trial, seventy‐six participants with idiopathic infertility were included in the intervention (plant treatment: n = 31; placebo: n = 29). Participants were randomised to take capsules containing dried extract of A. officinarum rhizome or placebo on a daily (total daily dosage of 300 mg) basis for 3 months. After 12 weeks of intervention, the sperm count and total number of spermatozoa with normal morphology were increased in participants treated with A. officinarum extract compared with the placebo group. The mean sperm count was initially 52 × 10⁶ ± 24 × 10⁶/ml which changed to 71 × 10⁶ ± 23 × 10⁶/ml, after intervention (p = 0.043). Also, the mean percentage of spermatozoa with normal morphology was 14.34% ± 9.16% before the treatment which significantly increased to 19% ± 14.89% (p < 0.001). Alpinia officinarum, a traditional medicine remedy, can be effective in the improvement of sperm morphology and sperm count in idiopathic infertility without causing adverse effects.     

RP-HPLC测定蜂胶中乔松素、白杨素和高良姜素的含量

目的: 采用反相高效液相色谱法测定蜂胶中乔松素、白杨素和高良姜素的含量。方法: 使用YMC-C₁₈色谱柱(4.6 mm×250 mm,5 μm),流动相乙腈-0.1%磷酸(40:60),流速1.0 mL·min^-1,检测波长,乔松素290 nm,白杨素和高良姜素268 nm,柱温30℃。结果: 乔松素、白杨素和高良姜素分别在4.266~426.6,4.59~459,4.322~432.62 mg·L^-1线性关系良好,平均回收率(n=6)分别为98.28%,98.82%,100.77%,RSD分别为0.89%,0.90%,1.32%。结论: 方法简便、准确、重复性好,可为蜂胶的质量控制提供实验依据。