The second-generation curcumin analogue RL71 elicits G2/M cell cycle arrest and apoptosis in canine osteosarcoma cells

Canine osteosarcoma is an aggressive cancer, comprising 85% of canine bone neoplasms. Current treatment practices of surgery and chemotherapy increase 1-year survival by only 45%. The curcumin analogue RL71, has demonstrated potent in vitro and in vivo efficacy in several models of human breast cancer through increased apoptosis and cell cycle arrest. Thus, the present study aimed to investigate efficacy of curcumin analogues in two canine osteosarcoma cell lines. Osteosarcoma cell viability was assessed using the sulforhodamine B assay and mechanisms of action were determined by analysing the levels of cell cycle and apoptotic regulatory proteins via Western blotting. Further evidence was obtained using flow cytometry to detect cell cycle distribution and the number of apoptotic cells. RL71 was the most potent curcumin analogue with EC₅₀ values of 0.64 ± 0.04 and 0.38 ± 0.009 μM (n = 3) in D-17 (commercial) and Gracie canine osteosarcoma cells, respectively. RL71 significantly increased the ratio of cleaved-caspase 3 to pro-caspase 3 and the level of apoptotic cells at the 2× and 5× EC₅₀ concentration (p < 0.001, n = 3). Furthermore, at the same concentration, RL71 significantly increased the number of cells in the G2/M phase. In conclusion, RL71 has potent cytotoxic activity in canine osteosarcoma cells triggering G2/M arrest and apoptosis at concentrations achievable in vivo. Future research should further investigate molecular mechanisms for these changes in other canine osteosarcoma cell lines prior to in vivo investigation.     

The effect of Curcuma longa extracted (curcumin) on the quality of cryopreserved boar semen

The aim of this study was to determine the optimal concentration of curcumin needed for cryopreservation of boar semen. Semen samples (n = 9) were collected from nine Duroc boars which having proven fertility were used for routine artificial insemination. Semen samples were collected and divided into six groups (groups A‐F) according to various concentrations of curcumin in freezing extender (i.e. 0, 0.125, 0.25, 0.50, 0.75 and 1.0 mmol/L, respectively). The semen was frozen by traditional liquid nitrogen vapor method and stored at ?196°C in the liquid nitrogen tank. After storage, frozen semen samples were thawed at 50°C for 12 s and evaluated for progressive motility, viability and acrosome integrity. The present results indicated that the addition of curcumin at 0.25 (group C) or 0.50 mmol/L curcumin (group D) yielded the higher percentage of progressive motility (33.3 and 36.1%, respectively) (P < 0.001). A significantly higher percentage of acrosome integrity was found in groups B (29.7%), C (31.1%) and D (30.2%) than in the other groups (P < 0.01). However, there was no significant difference in percentage of viability among groups. In conclusion, addition to the freezing extender of curcumin during cryopreservation at a concentration of 0.25 or 0.50 mmol/L is the optimal concentration of curcumin for improving the quality (i.e. increased progressive motility and acrosome integrity) of cryopreserved boar semen.     

酶辅助乳化制备姜黄素脂肪乳研究

选用碱性蛋白酶辅助乳化,利用酶解膨化大豆粉产生的蛋白和磷脂作为乳化剂制备了天然姜黄素脂肪乳。通过流体动力学半径及其分布的测量、激光共聚焦显微镜观察和荧光光谱分析等来表征脂肪乳粒径、电位、微观结构及脂肪乳内蛋白的荧光强度变化,以氧化稳定性、包埋率和生物利用率来评价脂肪乳的稳定性能和对姜黄素的负载效果。结果表明,随着姜黄素添加量的增加,脂肪乳平均粒径先增加、后趋于稳定,在添加量为0.6%时,平均粒径为1127.42nm,电位绝对值最大,为38.67mV。激光共聚焦显微镜观察结果表明,乳液中油滴和蛋白分布比较均匀,形成了包裹较好的液滴。在0.6%添加量下的脂肪乳储存14d时的氧化稳定性最好,POV值最小,仅为3.15mmol/kg,储存21d时TBARS值为0.56mmol/kg;姜黄素包埋率高达72.58%,经体外消化后生物利用率为55.22%。荧光光谱分析表明,过量的姜黄素会使脂肪乳中蛋白质的荧光强度显著降低。因此,在姜黄素添加量为0.6%时,通过酶辅助法可制备稳定性较高、运载效果较好的脂肪乳。     

姜黄素的理化特性、抗氧化功能及其在肉鸡生产中的应用

姜黄素是从姜科植物姜黄中提取的一种多酚类活性物质,具有多种生物学功能.近几年,姜黄素作为天然抗氧化剂对机体抗氧化功能的影响引起了人们的广泛关注,其作为一种绿色、新型的饲料添加剂应用于肉鸡生产也成为了国内外的研究热点之一.本文主要介绍了姜黄素的理化性质、生物利用率、抗氧化功能及其在肉鸡生产中的应用现状.     

单羰基姜黄素类似物对Ⅱ型糖尿病大鼠非酒精性脂肪肝的治疗作用研究

[目的]研究单羰基姜黄素类似物(代号B06)对Ⅱ型糖尿病大鼠非酒精性脂肪肝糖脂代谢紊乱的影响。[方法]应用高糖高脂饲料喂养,小剂量STZ干扰建立Ⅱ型糖尿病大鼠模型[1],并随机分模型组、A75治疗组、C66治疗组、正常对照组,各组均灌胃治疗12周;检测各组大鼠血生化指标[2]。[结果]单羰基姜黄素类似物能明显改善试验性Ⅱ型糖尿病大鼠的血糖升高,FINS明显低于模型组;肝脏TC、血清TG、TC有明显的降低作用,对血清HDL有明显的升高作用,有统计学意义;[结论]单羰基姜黄素类似物对Ⅱ型糖尿病大鼠非酒精性脂肪肝有一定的治疗作用。     

姜黄素作为饲料添加剂的研究进展

姜黄素是从姜科植物中提取的一种天然活性物质,具有保护肠黏膜、抗氧化、调节代谢、抑菌抗炎等功能。姜黄素作为一种多效的天然活性物质,已逐渐取代抗生素在饲料中得到广泛应用。文章主要从姜黄素的理化性质、生理功能及其在饲料中的应用等方面作以综述。     

姜黄素嘧啶酮衍生物的合成及杀螨活性

在明确姜黄素具有杀螨活性,且其结构中的双羰基并非是起杀螨作用的关键基团的基础上,设计、合成了4个新颖的姜黄素嘧啶酮衍生物,其结构经红外光谱、核磁共振氢谱和质谱分析确认。生物活性测定结果表明:4个目标化合物均表现出优于母体化合物姜黄素的杀螨活性,处理48 h后,活性最好的4,6-二 -2-嘧啶酮(3a)对朱砂叶螨Tetranychus cinnabarinus和柑橘全爪螨Panoychus cotri的LC50值分别为487.5和200.3 mg/L,其毒力约为姜黄素的4倍;而处理72 h后,化合物 3a 对朱砂叶螨的LC50值为40.7 mg/L,其毒力约为姜黄素的14倍。     

不同乳化剂对姜黄素乳液理化稳定性的影响

姜黄素具有许多生物活性功能,但较差的溶解度和稳定性限制了其在食品和医药领域的应用。为筛选出具有良好稳定性的姜黄素乳液,本研究以亚麻籽油为姜黄素的油相载体,经高压均质法制备出姜黄素乳液中研究卵磷脂、吐温-80、阿拉伯胶和乳清分离蛋白4种食品级乳化剂对姜黄素乳液的理化特性和贮藏稳定性的影响,从包埋率、浊度、粒径、电位等方面进行稳定性评价。结果表明,吐温-80稳定的姜黄素乳液中姜黄素包埋率较高(76.98%),浊度和平均粒径最小,分别为848.0 NTR、214.23±1.52 nm;同时在贮藏期内姜黄素乳液的平均粒径变化最小,增长不到1%,贮藏稳定性表现良好。同时,4℃低温条件下姜黄素保留率最高,达到88.02%。结果表明,选用吐温-80作为乳化剂,姜黄素乳液具有最好的溶解性和稳定性,这为今后姜黄素在食品工业中的广泛应用提供了新思路。     

短链葡聚糖-姜黄素纳米乳液的制备及结构表征

利用短链葡聚糖(short glucan chains,SGC)的螺旋空间结构来包埋姜黄素(curcumin,CUR)。通过使用高剪切分散乳化机高速剪切溶液5 min,用纳米均质机在50 MPa压力下高压均质经剪切后的乳液2次制备成纳米乳液以提高其包埋率和载药量。XRD (x-ray diffraction)和TGA (thermogravimetric analysis)很好的验证了包合物的形成,通过TGA、SEM (scanning electron microscopy)、激光粒径分析仪等各种表征分析得出短链葡聚糖-姜黄素纳米乳液制备成功,所制得的乳液对姜黄素的包埋率和载药量都高于短链葡聚糖-姜黄素包合物,分别达到了71.11%和12.07%,说明制备成纳米乳液对姜黄素的包埋率和载药量都有了明显的提高。所制备的纳米乳液的粒径小于300 nm,粒径分布均一,Zeta电位观测表明所制得的乳液的稳定性有所提高。为提高食品及医药领域姜黄素的生物利用率提供了一定的参考意义。     

姜黄素纳米混悬剂的制备及其表征

为了提高姜黄素的水溶性,采用高压均质法制备姜黄素纳米混悬剂,优化了姜黄素纳米混悬剂的制备工艺。利用红外光谱(IR)、紫外光谱(UV)、X射线衍射(XRD)、透射电镜(TEM)和高效液相色谱(HPLC)对姜黄素纳米混悬剂进行了理化性质和化学结构的分析。结果表明:当均质压力100 MPa,循环次数30次时,姜黄素纳米混悬剂的平均粒径为(171.00±8.56)nm,一致性系数为(0.69±0.05);IR、UV、XRD、TEM和HPLC分析表明,姜黄素纳米混悬剂冻干粉的化学结构未见明显改变,姜黄素纳米粒子为不规则的球状晶体,结晶度显著降低。姜黄素纳米混悬剂冻干粉在水中的溶解度达62.85 mg/L,比姜黄素原粉提高了90.48倍;姜黄素纳米混悬剂冻干粉体外溶出速率也明显提高,120 min时溶出度已达80%。研究表明高压均质法适用于姜黄素纳米混悬剂的制备。