染料木素的研究进展

染料木素是从大豆、三叶草、葛根等植物中提取出来的异黄酮化合物,水溶性和脂溶性都较差,它有多种生理学功能。近年来,国内外学者对其提取分离方法、分析方法、药理作用、结构修饰等方面进行了研究。本文简要综述了这一领域近年来的研究进展,以促使对其的研究和应用。     

HPLC测定槐角总黄酮水解产物中的染料木素

目的 采用HPLC测定槐角总黄酮水解产物中染料木素的含量.方法色谱柱为Kromasil C18柱(150 mm×4.6mm,5μm),柱温28℃,流动相为甲醇-水(60∶40),流速1 mL· min-1,榆测波长260 nm.结果染料木素0.02～0.20μg与内峰面积的线性关系良好(r=0.9999),平均回收率为...     

以槐角为原料制备染料木素的工艺研究

目的制定一种以槐角为原料,适用于工业化生产制备染料木素的最佳工艺。方法以槐角为原料,采取正交实验,确定最佳的槐角苷提取工艺;在单因素考察的基础上,采取正交实验,确定槐角苷水解得到染料木素的最佳条件。结果槐角中槐角苷的最佳提取工艺是:80%乙醇、煎煮120 min、8倍量、提取3次;槐角苷最佳酸解工艺是:用2.5 mol.L-1盐酸乙醇液酸解,料液比为1∶15,酸解温度为90℃,酸解时间为2.5 h。结论该方法经济适用,是可用于大批量生产的制备方法。     

槐角丸中染料木素的高效毛细管电泳测定

目的:建立适合槐角丸中染料木素测定的毛细管电泳方法。方法:采用高效毛细管电泳法。实验时,先分别用0.1 mol·L-1盐酸溶液、0.1 mol·L-1氢氧化钠溶液及运行缓冲液冲洗未涂层弹性石英毛细管(50μm ×43 cm)10 min,然后以槲皮素为内标,运行电压28 kV,运行缓冲液为20 mmo|·L-1磷酸盐缓冲液(pH 9.2),检测波长254 nm,室温下电动进样5 s。结果:染料木素的线性范围为6.25-31.26μg·mL-1(r=0.9994),其高、中、低3个量的加样回收率分别为100.7％,100.1％和99.2％,RSD分别为1.5％,0.63％和1.7％。结论:本法用于测定槐角丸中染料木素的含量快速、简便、准确可靠,有良好的重复性。     

原位生物转化法提高槐角中染料木素的含量

目的 旨在开发一种生物转化工艺,将槐角中的槐角苷等糖苷转化为活性更高的染料木素,从而提高槐角的中药使用价值。方法 用米根霉（Rhizopus oryzae）LJH3菌株的粗酶液生物转化处理槐角,考察了料液比、体系pH、槐角粒径大小和转化时间对提高槐角中染料木素含量的影响。结果 米根霉LJH3的粗酶液转化处理槐角,染料木素含量可显著提高。在较优的转化条件下,即料液比5:100,体系pH 5.0,槐角粒径0.2 mm,30℃条件下转化32 h,染料木素含量提高到36.3 mg?g-1,较未转化时的含量提高了14.5倍。结论 利用米根霉LJH3的粗酶液原位生物转化槐角,染料木素的含量大幅度提高,转化工艺具有方法简单和产率高的优点,有较好的工业化应用价值。     

染料木素的药代动力学研究

总结了国内外近5年有关染料木素的药代动力学研究资料,从吸收、分布、代谢、排泄四个方面进行归纳分析,以指导临床合理用药。     

染料木素的磷酰化结构改造及与溶菌酶的弱相互作用

采用改进的Atherton-Todd反应对染料木素进行磷酰化结构改造，得到了4种新的磷酰化产物，并通过ESI-MS，NMR进行了结构确认，结果发现磷酰化试剂对染料木素羟基的磷酰化具有较好的选择性，反应主要发生在染料木素7位羟基；进一步利用ESI质谱技术，对4种磷酰化染料木素与大分子溶菌酶的弱相互作用进行测定，显示所有的磷酰化产物均与溶菌酶形成非共价复合物。     

刺五加中新的木脂素的结构鉴定

刺五加中新的木脂素的结构鉴定吴立军１）郑健刘湘杰沈燕（沈阳药科大学天然药物研究室，沈阳１１００１５）闫淑梅江黎明孙俊杰王树贵（乌苏里江制药有限公司，虎林１５８４１７）最近，从五加科植物五加〔Ａｃａｎｔｈｏｐａｎａｘｓｅｎｔｉｃｏｓｕｓ（Ｒｕｐｒ．ｅｔ...     

染料木素的脑保护作用及机制研究进展

染料木素是从大豆、三叶草、葛根等植物中提取出来的异黄酮化合物,为植物雌激素的一种。其化学结构与内源性雌激素相似,能与雌激素胞膜及胞内受体结合发挥作用,如抗肿瘤作用、神经保护作用、调节骨代谢与脂代谢、抗肝纤维化、心血管保护及抗氧化等作用。本文从神经毒性物质诱导的神经元损伤、去卵巢大鼠神经损伤、脑缺血再灌注损伤等方面综述了近年来染料木素对脑损伤的保护作用;文献分析表明,染料木素可通过直接与淀粉样蛋白β(Aβ)结合、抗氧化作用、抑制Ca2+超载、减轻谷氨酸的毒性、降低促炎细胞因子的表达及调节信号转导通路实现对各种因素所致的神经损伤保护效应。     

悬钩子属植物化学成分和药理作用研究新进展

悬钩子属为蔷薇科植物,分布广泛,具有广泛的药用价值。通过查阅大量文献资料,发现悬钩子属植物含有萜类、黄酮类、甾类等化学成分,在抗菌、保肝、抗氧化、抗肿瘤、消炎、镇咳等方面发挥着重要作用。本文综述了近些年来关于悬钩子属的化学成分、药理作用等方面的研究进展,为其进一步开发利用提供参考。     

Kinetics of genistein and its conjugated metabolites in pregnant Sprague-Dawley rats following single and repeated genistein administration.

Diets high in soy-based products are well known for their estrogenic activity. Genistein, the predominant phytoestrogen present in soy, is known to interact with estrogen receptors (ER) alpha and beta and elicits reproductive effects in developing rodents. In the rat, genistein is metabolized predominantly to glucuronide and sulfate conjugates, neither of which is capable of activating ER. Therefore, it is critical to understand the delivery of free and conjugated genistein across the placenta to the fetus following maternal genistein exposure such that the potential fetal exposure to free genistein can be assessed. Genistein (4 or 40 mg/kg) was administered to pregnant Sprague-Dawley rats by oral gavage daily from gestation day (GD) 5 through 19 or on GD 19 alone. Maternal and GD 19 fetal tissues were collected 0.5, 1, 2, 4, 6, 8, 12, and 24 h following administration of the final dose on GD 19. Concentrations of genistein, genistein glucuronide, and genistein sulfate were quantitated by LC-MS/MS. In maternal plasma, genistein glucuronide was the predominant metabolite. In the fetal plasma, genistein glucuronide and genistein sulfate were the primary metabolites. Genistein levels in maternal and fetal plasma were much lower than its conjugates. The concentration of genistein in placental tissue was higher than either conjugate. Fetal concentrations of unconjugated genistein following administration of 40 mg/kg were above the EC50 for ERbeta activation. Repeated administration of 40 mg/kg genistein resulted in minor changes in genistein kinetics in the pregnant rat compared to single administration of the same dose. These data suggest that conjugated forms of genistein are not transported across the placenta. High placental concentrations of genistein indicate the placenta is a potential target organ for genistein action during gestation.     

The protective effect of genistein postconditioning on hypoxia/ reoxygenation-induced injury in human gastric epithelial cells

Aim： The aim of this study was to investigate the protective effect of genistein postconditioning on hypoxia/reoxygenation- induced injury in human gastric epithelial cells and to begin a tentative discussion on the mechanism behind this protection. Methods： A model of hypoxia/reoxygenation-induced injury was established in the human gastric epithelial cell line （GES-1）. All cells in our present study were randomly divided into five groups： a normal control group （N）, a hypoxia/ reoxygenation group （H/R）, a genistein postconditioning group （GP）, a capsazepine＋genistein postconditioning group （C＋GP） and a DMSO vehicle postconditioning group （DM）. The methods used included MTT assays to test cell viability, flow cytometric analyses to quantify the percentage of cell apoptosis, Western blot analyses to measure the protein expression of calcitonin gene-related peptide （CGRP）, Bcl-2, and Bax, and immunocytochemistry assays to detect the expression of CGRP in each group. Results： The MTT assays indicated that the cell viabilities of the groups were 100.0%±0%, 51.4%±4.1%, 66.7%±2.0%, 56.1%±2.8%, and 50.7%±2.4%, respectively. Compared with the H/R group, the viability of the GP group was significantly increased （P〈0.01）. Flow cytometric analysis showed that the cell apoptosis percentage of each group was 2.28%±0.44%, 12.17%±2.15%, 5.40%±1.22%, 10.43%±1.37%, and 11.02%±2.19%, respectively. Western blot analysis demonstrated that CGRP, Bcl-2, and Bax were expressed in normal human gastric epithelial cells. Compared with the H/R group, the GP group exhibited increased expression of CGRP and Bcl-2 and decreased expression of Bax. Immunocytochemistry assays indicated that the number of CGRP-positive cells in the GP group was significantly increased. Conclusion： Genistein postconditioning has a protective effect on hypoxia/reoxygenation-induced injury in human gastric epithelial ceils. The mechanism by which genistein exerts this protection may be via activation of cell     

The protective effect of genistein postconditioning on hypoxia/reoxygenation-induced injury in human gastric epithelial cells

Aim:

The aim of this study was to investigate the protective effect of genistein postconditioning on hypoxia/reoxygenation-induced injury in human gastric epithelial cells and to begin a tentative discussion on the mechanism behind this protection.

Methods:

A model of hypoxia/reoxygenation-induced injury was established in the human gastric epithelial cell line (GES-1). All cells in our present study were randomly divided into five groups: a normal control group (N), a hypoxia/reoxygenation group (H/R), a genistein postconditioning group (GP), a capsazepine+genistein postconditioning group (C+GP) and a DMSO vehicle postconditioning group (DM). The methods used included MTT assays to test cell viability, flow cytometric analyses to quantify the percentage of cell apoptosis, Western blot analyses to measure the protein expression of calcitonin gene-related peptide (CGRP), Bcl-2, and Bax, and immunocytochemistry assays to detect the expression of CGRP in each group.

Results:

The MTT assays indicated that the cell viabilities of the groups were 100.0%±0%, 51.4%±4.1%, 66.7%±2.0%, 56.1%±2.8%, and 50.7%±2.4%, respectively. Compared with the H/R group, the viability of the GP group was significantly increased (P<0.01). Flow cytometric analysis showed that the cell apoptosis percentage of each group was 2.28%±0.44%, 12.17%±2.15%, 5.40%±1.22%, 10.43%±1.37%, and 11.02%±2.19%, respectively. Western blot analysis demonstrated that CGRP, Bcl-2, and Bax were expressed in normal human gastric epithelial cells. Compared with the H/R group, the GP group exhibited increased expression of CGRP and Bcl-2 and decreased expression of Bax. Immunocytochemistry assays indicated that the number of CGRP-positive cells in the GP group was significantly increased.

Conclusion:

Genistein postconditioning has a protective effect on hypoxia/reoxygenation-induced injury in human gastric epithelial cells. The mechanism by which genistein exerts this protection may be via activation of cellular vanilloid receptor subtype 1, resulting in the generation of an endogenous protection substance, CGRP.     

染料木黄酮植物性雌性激素治疗骨质疏松研究进展简

本综述通过检索GoogleScholar以及Sci—enceDirect查阅大量近10年的相关文献,对染料木黄酮抗骨质疏松机制、抗骨质疏松药效、药代动力学以及安全性多角度综述分析。结果表明染料木黄酮具有类似雌性激素作用,与雌性激素受体α的结合力大于雌性激素受体β的结合力,且发挥抗骨质疏松作用的主要作用受体是雌性激素受体α,在抗骨质疏松研究中无论是体内还是体外都具有较强的药理作用;其药理活性作用机制包括抑制骨髓巨噬细胞向破骨细胞转化的能力,抑制破骨细胞的增殖生长能力,诱导破骨细胞的凋亡,同时促进成骨细胞的增殖生长能力。骨质疏松的治疗效果确切,而毒副作用则明显的低于双磷酸盐和特立帕肽。植物雌性激素染料木黄酮可能在未来骨质疏松治疗过程中具有成为一线治疗药物的潜质。     

不同剂量染料木黄酮及其代谢产物在大鼠胆汁中的排泄动力学

目的研究不同剂量染料木黄酮及其葡糖醛酸化代谢产物在大鼠胆汁内的排泄动力学。方法将染料木黄酮制成混悬液，分别按6.25，12.5和50 mg·kg^-1给大鼠灌胃，于灌胃后不同时间收集胆汁，用葡糖醛酸酶溶液处理胆汁。采用高效液相色谱法测定胆汁中染料木黄酮及其葡糖醛酸化代谢产物的浓度。结果3种剂量6.25，12.5和50 mg·kg^-1分别给药后，累积以原形从胆汁排泄的药物分别为(42.56±6.54)，(75.17±18.87)和(126.60±34.78) μg，累积经胆汁排泄的总药物(原形药物+葡糖醛酸化药物)分别为(108.46±35.23)，(423.46±158.31)和(853.74±320.84) μg，葡糖醛酸化代谢产物分别占胆汁排泄总量(原形药物+葡糖醛酸化药物)的60.76%，82.25%和85.17%。结论染料木黄酮在大鼠胆汁中主要以葡糖醛酸结合形式排泄，原形药物及其葡糖醛酸化代谢产物在大鼠胆汁中的排泄呈现明显的非线性剂量依赖性特征。     

Management of severe osteoporosis

Introduction: Severe osteoporosis represents a disease of high mortality and morbidity. Recognition of what constitutes and causes severe osteoporosis and aggressive intervention with pharmacological agents with evidence to reduce fracture risk are outlined in this review.

Areas Covered: This review is a blend of evidence obtained from literature searches from PubMed and The National Library of Medicine (USA), clinical experience and the author’s opinions. The review covers the recognition of what constitutes severe osteoporosis, and provides up-to-date references on this sub-set of high risk patients.

Expert Opinion: Severe osteoporosis can be classified by using measurements of bone densitometry, identification of prevalent fractures, and, knowledge of what additional risk factors contribute to high fracture risk. Once recognized, the potential consequences of severe osteoporosis can be mitigated by appropriate selection of pharmacological therapies and modalities to reduce the risk for falling.     

Effects of genistein aglycone in osteoporotic, ovariectomized rats: a comparison with alendronate, raloxifene and oestradiol

Background and purpose:     

不同剂量染料木黄酮及其代谢产物在大鼠尿中的排泄

目的:研究不同剂量染料木黄酮及其葡萄糖醛酸化代谢产物在大鼠尿中的排泄动力学。方法:将染料木黄酮制成混悬液,按6.25、12.5、50mg.kg-1给大鼠灌胃,于灌胃后不同时间收集尿液,用葡萄糖醛酸酶溶液处理尿液。采用高效液相色谱法测定尿液中染料木黄酮及其葡萄糖醛酸化代谢产物的浓度。结果:6.25、12.5、50 mg.kg-1时,累积以原形经尿液排泄的药物分别为34.79±10.83、187.30±69.96和213.56±30.58μg,累积经尿液排泄的总药物(原形药物+葡萄糖醛酸化药物)分别为217.79±52.06、583.05±106.92和1108.37±88.14μg,累积经尿液排泄的葡萄糖醛酸化代谢产物分别占尿液排泄总量的84.03%、67.88%和80.73%。结论:染料木黄酮在大鼠尿液中主要以葡萄糖醛酸结合形式排泄,原形及其葡萄糖醛酸化代谢产物的排泄呈现明显的非线性剂量依赖性特征。     

染料木素对维甲酸模型大鼠骨密度和微量元素的影响

目的　观察染料木素对维甲酸模型大鼠骨密度和微量元素的影响。方法　维甲酸 70 mg·kg- 1灌胃两周(正常对照组给予等量生理盐水 )后 ,各组大鼠给药如下 :正常对照组和模型组 ig等容量生理盐水 ;骨疏康组以5 .0 g· kg- 1 的骨疏康灌胃 ,染料木素大、中、小剂量组分别以 1 8.0 ,9.0和 4.5 mg· kg- 1 灌胃给药。并分别于0 ,1 ,2 ,4,8,1 2周从各组取 8只大鼠 ,测量大鼠体质量 ,股骨、胫骨长度和质量 ,测定股骨、胫骨和腰椎骨密度和胫骨中微量元素含量。结果　 1染料木素可增加维甲酸模型大鼠的体质量 ,并明显增加维甲酸大鼠的左股骨、左胫骨质量和长度 ( P <0 .0 5或 P <0 .0 1 ) ;2增强维甲酸模型大鼠的骨密度 ( P <0 .0 5或 P <0 .0 1 ) ;3可明显升高维甲酸模型大鼠微量元素含量 ( P<0 .0 5或 P <0 .0 1 )。结论　染料木素可使维甲酸模型大鼠的骨密度显著增加 ,并使骨质微量元素明显增加 ,对治疗骨质疏松症有很好的疗效