天然产物5,7-二甲氧基木犀草素的合成

5,7-二甲氧基木犀草素是中药枳椇中一种黄酮类主要化合物之一。本文以芦丁为原料,经水解还原得到木犀草素,再经羟基保护、醚化及脱保护基等反应合成了5,7-二甲氧基木犀草素,总收率为7.9%。其结构经1HNMR和13C NMR表征。     

比色法测定白花蛇舌草中总黄酮含量的研究

目的:选择一种比色法作为白花蛇舌草总黄酮的最优测定方法。方法:以芦丁为标准品,通过直接测定法、硝酸铝法、氯化铝法3种检测方法的比较,确定一种检测方法作为白花蛇舌草总黄酮的测定最优方法。结果:经过比较,选择氯化铝法作为测定白花蛇舌草总黄酮含量更好,在410nm波长下测定,样品在0.05mg~0.3mg范围内,其浓度与吸光度呈良好的线性关系,相关系数R=0.9997,平均加样回收率为99.84%,RSD=1.31%(n=5),稳定性、精密度和重现性均理想。结论:氯化铝显色法的大部分指标都好于其他两种比色法,且分析时间较短,准确度高,因此三氯化铝比色法更适合白花蛇舌草总黄酮含量的测定。     

高效液相色谱法测定山楂总黄酮提取物中芦丁和金丝桃苷的含量

目的建立高效液相色谱法测定山楂总黄酮提取物中芦丁和金丝桃苷的含量的方法。方法采用HPLC法,色谱柱Kromasil C18色谱柱（4．6mm×250mm,7μm）;流动相为甲醇-0．4％磷酸溶液（30：70）,流速1．0mL／min;柱温25℃;检测波长359nm。结果芦丁在0．05μg-0．51μg（r=0．9999）范围内线性关系良好,平均回收率为100．4％（RSD=1．2％）;金丝桃苷为0．062μg-0．62μg（r=0．9997）范围内线性关系良好,平均回收率为99．0％（RSD=1．8％）。结论该方法简便、灵敏、可靠、准确、重现性好,可用于山楂提取物的含量测定。     

基于网络药理学和分子对接的黄蜀葵花干预糖尿病肾病的作用机制研究

目的 运用网络药理学和分子对接的方法研究黄蜀葵花干预糖尿病肾病的多成分、多靶点、多通路作用机制,旨在为其基础研究及临床应用提供依据.方法 通过ETCM、HERB数据库结合文献报道,筛选黄蜀葵花活性成分,并通过PharmMapper数据库预测其潜在靶点,建立靶点数据库.通过Genecards、OMIM、Drugbank、...     

Antioxidant activity and cytotoxicity of Cyrtosperma johnstonii extracts on drug sensitive and resistant leukemia and small cell lung carcinoma cells

Context: The number of patients with cancer is increasing. New therapeutic agents to overcome drug-resistant tumors are urgently needed. Cyrtosperma johnstonii N.E. Br. (Araceae) is used for treatment of cancer in Thai traditional medicine. This study aimed to evaluate antioxidant activity and cytotoxicity of C. johnstonii extracts on human cancer cells.

Materials and methods: Dried powder of C. johnstonii rhizomes was extracted with several solvents. The 0.1?mg/ml extract solution was tested for antioxidant activity by 2,2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant power (FRAP) assays. Color formation from 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide was used to determine cell viability. Standardization of the extract was performed by high-performance liquid chromatography (HPLC) with photodiode array detector at 254 and 360?nm. Cell cycle arrest was evaluated by flow cytometry after 5?min, 12?h and 24?h treated with 20 µg/ml of the acetone extract.

Results: The acetone extract exhibited the highest phenolic content and antioxidant activity (TEAC and EC values = 19.2?±?0.14 and 19.2?±?0.31?mM/mg, respectively). The IC₅₀ values for leukemia ranged from 11?±?1 to 29?±?3 µg/ml and from 5?±?2 to 6?±?0 µg/ml for small cell lung carcinoma cells. Cell cycle arrest occurred at the G2/M phase followed by apoptosis. HPLC analysis revealed that rutin is the major constituents of the extract.

Discussion and conclusion: The acetone extract of C. johnstoni is a promising source of natural antioxidants and anticancer. The extract inhibits cancer cells effectively with less effect on normal cells.     

脉络通胶囊质量标准

目的:提高脉络通胶囊的质量标准。方法:采用TLC法鉴别制剂中丹参、山楂、川芎、地龙,采用HPLC同时测定葛根素、芦丁、丹酚酸B含量。色谱条件为:Kromasil 100-5C18色谱柱(4.6 mm×250 mm,5μm),柱温35℃,以甲醇(A)-1%冰醋酸溶液梯度洗脱(0~45 min,25%~45%A,45~55 min,45%~25%A),流速1.0 mL·min-1,检测波长254 nm。结果:TLC可鉴别丹参、山楂、川芎、地龙。葛根素的进样量在0.130 6~1.959 6μg呈现良好的线性,r=0.999 9;平均加样回收率97.77%,RSD 0.70%;芦丁的进样量在1.054 2~15.813 6μg呈现良好的线性,r=0.999 9;平均加样回收率98.66%,RSD0.89%;丹酚酸B的进样量在0.184 9~2.773 2μg呈现良好的线性,r=0.999 5;平均加样回收率99.55%,RSD 1.15%。结论:该法专属性强,重复性好,结果准确,可用于控制脉络通胶囊质量。     

Vasorelaxant and antihypertensive effect of Cocos nucifera Linn. endocarp on isolated rat thoracic aorta and DOCA salt-induced hypertensive rats

Ethnopharmacological relevance

The fruits of Cocos nucifera Linn. (Arecaceae) have long been used in traditional medicine for the treatment of cardio-metabolic disorders.

Aim of the study

To evaluate the ethanolic extract of Cocos nucifera Linn. endocarp (CNE) for its vasorelaxant activity on isolated rat aortic rings and antihypertensive effects in deoxycorticosterone acetate (DOCA) salt-induced hypertensive rats.

Materials and methods

Cocos nucifera Linn. endocarp was extracted with ethanol and characterized by HPLC. CNE was examined for its in vitro vascular relaxant effects in isolated norepinephrine, phenylephrine or potassium chloride pre-contracted aortic rings (both intact endothelium and denuded). In vivo anti-hypertensive studies were conducted in DOCA salt-induced uninephrectomized male Wistar rats.

Results

Removal of endothelium or pretreatment of aortic rings (intact endothelium) with l-NNA (10 μM) or ODQ (10 μM) followed by addition of contractile agonists prior to CNE significantly blocked the CNE-induced relaxation. Indomethacin (10 μM) and atropine (1 μM) partially blocked the relaxation, whereas glibenclamide (10 μM) did not alter it. CNE significantly reduced the mean systolic blood pressure in DOCA salt-induced hypertensive rats (from 185.3 ± 4.7 mmHg to 145.6 ± 6.1 mmHg). The activities observed were supported by the polyphenols, viz. chlorogenic acid, vanillic acid and ferulic acid identified in the extract.

Conclusions

These findings reveal that the vasorelaxant and antihypertensive effects of CNE, through nitric oxide production in a concentration and endothelium-dependent manner, is due to direct activation of nitric oxide/guanylate cyclase pathway, stimulation of muscarinic receptors and/or via cyclooxygenase pathway.     

秋海棠属药材的质量标准研究

目的:建立秋海棠属药材中芦丁的含量测定方法,为完善秋海棠属药材的质量标准提供理论依据。方法:采用HPLC,色谱柱Diamonsil(钻石)-C18(4.6 mm×250 mm,5μm);流动相甲醇-0.5%磷酸溶液梯度洗脱;柱温30℃;检测波长257nm。结果:秋海棠属药材因种类、产地及药用部位不同,其芦丁的含量存在差异,以贵州开阳南江峡谷产盾叶秋海棠地上部分中芦丁的含量为最高;不同部位中芦丁的含量分布为叶、茎>根茎。结论:方法简便易行、重复性好、结果准确,可作为秋海棠属药材中芦丁的含量测定方法。秋海棠药材入药建议以地上部分更为合理。     

Rutin inhibits human leukemia tumor growth in a murine xenograft model in vivo

Numerous studies have shown that rutin has anticancer effects. We have previously reported that rutin induced cell cycle arrest and apoptosis in murine leukemia WEHI‐3 cells in vitro and in vivo. However, there are no data showing that rutin inhibits human leukemia HL‐60 cells in vivo in a murine xenograft animal model. Human leukemia HL‐60 cells were implanted into mice and treated with vehicle (1% DMSO), rutin (120 mg/kg of body weight) or vinblastine (120 μg/kg of body weight). Compounds and agents were injected once every four days intraperitoneally (i.p.) for 36 days. Treatment with 120 mg/kg of rutin or with 120 μg/kg of vinblastine resulted in a reduction of tumor weight and volume when compared with the control groups. Tumor size in xenograft mice treated with 120 mg/kg of rutin was significantly smaller than that in the untreated‐control group. These novel findings indicate that rutin inhibits tumor growth in a xenograft animal model. Rutin may be useful in treating leukemia but certainly much more research is needed. © 2011 Wiley Periodicals, Inc. Environ Toxicol, 2012.     

HPLC法同时测定芦笋黄酮中5个黄酮苷的含量

目的:建立反相高效液相色谱法同时测定芦笋黄酮中槲皮素-3-O-葡萄糖-芸香糖苷、芦丁、异鼠李素-3-O-葡萄糖-芸香糖苷、烟花苷和水仙苷的含量。方法:采用Diamonsil(钻石)C18柱(200 mm×4.6 mm,5μm),流动相为乙腈-甲醇-0.1%醋酸水(8∶16∶76),流速1.0 mL.min-1,柱温30℃,检测波长260 nm。结果:芦笋黄酮中槲皮素-3-O-葡萄糖-芸香糖苷、芦丁、异鼠李素-3-O-葡萄糖-芸香糖苷、烟花苷和水仙苷浓度分别在30.38～70.88μg.mL-1(r=0.9996)、60.75～141.75μg.mL-1(r=0.9995)、29.40～68.60μg.mL-1(r=0.9997)、29.63～69.13μg.mL-1(r=0.9996)、18.00～42.00μg.mL-1(r=0.9998)范围内与峰面积呈良好的线性关系。方法的加样回收率(n=6)分别为99.4%,99.2%,99.2%,102.6%,101.4%;RSD分别为2.0%,1.6%,1.8%,1.3%,2.2%。结论:本法快速、简便、准确,重复性好,适用于芦笋黄酮的质量控制。