包装、储藏条件对羌活饮片质量的影响

目的研究不同包装、储存条件对羌活饮片内在质量的影响。方法开展1年的留样观察实验,对不同包装、不同储藏条件下的羌活饮片进行含有量测定。UPLC法测定羌活醇、异欧前胡素、绿原酸、阿魏酸、紫花前胡苷和佛手柑内酯的含有量。结果包装材料中,绿原酸的含有量以纸袋包装的较高,紫花前胡苷的含有量以塑料袋包装的较高,羌活醇的含有量则以铝塑复合袋包装的较高,但以铝塑复合袋包装的羌活中异欧前胡素的含有量波动最大;储藏温度中,阿魏酸的含有量高低排序为常温>低温>阴凉,佛手柑内酯的含有量高低排序是阴凉>低温>常温。结论塑料袋包装、低温、光照条件下储存更适宜于羌活饮片内在质量的保存。     

不同商品等级羌活中有机酸和香豆素类化合物的测定

目的比较同一产地不同商品等级羌活中主要有机酸和香豆素类化合物的含有量。方法采用HPLC-DAD法同时测定不同商品等级羌活中绿原酸、阿魏酸、紫花前胡苷、补骨脂素、佛手柑内酯、欧前胡素、羌活醇和异欧前胡素。色谱柱为C18TSK gel ODS-80Ts QA(250 mm×4.6 mm,5μm)。流动相为甲醇(A)-0.3%的冰醋酸水溶液(B),梯度洗脱;体积流量0.6 mL/min,进样量10μL,柱温30℃。结果 8种活性成分在80 min内达基线分离,线性关系良好(R2≥0.9992);平均加样回收率为96.27%～102.44%,RSD≤4.15%。绿原酸和阿魏酸的含有量与传统等级划分方法基本一致,但紫花前胡苷、佛手柑内酯、羌活醇和异欧前胡素的含有量与传统的以外观形态论品质的判断标准有一定的差异。补骨脂素和欧前胡素在所测样品中均未检测出。结论该方法灵敏、准确、可靠、重复性好,可用于羌活药材的质量评价。     

羌活化学成分研究

目的对羌活Notopterygium incisum的化学成分进行研究。方法采用硅胶柱色谱、HPLC以及Sephadex LH-20凝胶柱色谱等方法进行分离纯化,并结合现代波谱学技术对分离得到的化合物进行结构鉴定。结果从羌活的70%乙醇提取物中分离得到14个化合物,分别鉴定为7-羟基香豆素(1)、5,7-二甲氧基香豆素(2)、紫花前胡内酯(3)、佛手酚(4)、佛手柑内酯(5)、异虎耳草素(6)、比克白芷内酯(7)、(+)-顺式凯林内酯(8)、(-)-反式凯林内酯(9)、茴香酸对羟基苯乙酯(10)、5-甲氧基-8-羟基补骨脂内酯(11)、阿魏酸(12)、异欧前胡素(13)和异补骨脂素(14)。结论化合物2、7~9和11为首次从羌活属植物中分离得到。     

羌活化学成分进一步研究

目的：进一步研究裂叶羌活Notopterygium incisum干燥根茎和根的化学成分。方法：采用硅胶柱色谱方法进行分离、纯化，NMR和MS等方法进行结构鉴定。结果：从裂叶羌活干燥根茎和根的甲醇提取物中分离得到24个化合物，分别鉴定为异白菖蒲脑(1)、孕甾烯醇酮(2)、β-谷甾醇(3)、香柑内酯(4)、佛手酚(5)、蛇床素(6)、异欧前胡素(7)、佛手柑素(8)、去甲呋喃羽叶芸香素(9)、紫花前胡苷元(10)、7′-O-甲基异羌活醇(11)、羌活醇(12)、异羌活醇(13)、栓翅芹烯醇(14)、苯乙基阿魏酸酯(15)、茴香酸对羟基苯乙酯(16)、反式-阿魏酸(17)、紫花前胡苷(18)、蔗糖(19)、γ-甲氧基异丁香酚(20)、3，4，5-三甲氧基-反式-桂皮酸(21)、对甲氧基-反式-桂皮酸(22)、4-乙酰氧基-3-甲氧基-反式-桂皮酸(23)和对羟基-反式-桂皮酸(24)。结论：化合物1，14，20～24为首次从裂叶羌活根和根茎中分离得到；化合物1为倍半萜类化合物，化合物14为6，7-呋喃型香豆素，化合物20～24为苯丙素类化合物。     

硅胶柱色谱-高速逆流色谱法分离纯化羌活中佛手柑内酯

目的 以羌活的根和根茎为原料,建立硅胶柱色谱-高速逆流色谱(HSCCC)法制备分离羌活中佛手柑内酯的方法.方法 羌活粗提物先经过硅胶柱色谱初步分离,富集目标化合物;组分Q5再经过HSCCC分离,以正己烷-醋酸乙酯-甲醇-水(5∶5∶4∶5)为溶剂系统,上相为固定相,下相为流动相;经气-质及核磁共振氢谱、碳谱鉴定化合物的结构.结果 经过HSCCC分离后,从300 mg Q5样品中一次性分离得到佛手柑内酯37.6 mg,经HPLC检测其质量分数达到99.1％.结论 该方法操作简便、高效,为制备高纯度的佛手柑内酯提供了一条新途径.     

HPLC法测定羌活中阿魏酸的含量

目的建立羌活中阿魏酸含量的测定方法。方法采用高效液相色谱法。结果阿魏酸在18.82～188.2μg范围内具有良好的线性关系,平均回收率为98.68%,RSD=1.50%(n=6)。结论该方法灵敏、准确、专属性强,可作为羌活的质量控制指标之一。     

羌活抗炎质量标志物的挖掘及资源评价

目的 基于生物合成途径及网络药理学理念,从“化学成分-靶点”角度对羌活具有抗炎作用的质量标志物(qualitymarker,Q-Marker)进行预测,建立基于Q-Marker的羌活药材质量评价方法。方法 首先通过生物合成途径筛选可能的Q-Marker;其次采用中药系统药理学数据库与分析平台(traditional Chinese medicine systems pharmacology,TCMSP)预测和筛选羌活的化学成分及潜在作用靶点,然后在人类基因数据库Genecards及OMIM中检索抗炎相关靶基因,利用Cytoscape软件构建“成分-靶点”网络模型,筛选出羌活抗炎作用的Q-Marker;再次采用分子对接技术对筛选出的化合物与靶点(PTGS2)进行对接;最后采用UHPLC同时测定来自不同基原和不同产地的羌活的Q-Marker以评价其资源品质;结果 紫花前胡苷、香叶木苷、佛手柑内酯、羌活醇、异欧前胡素等化合物是羌活抗炎作用的主要活性物质,可作为Q-Marker的主要选择。分子对接结果证实紫花前胡苷、香叶木苷、佛手柑内酯、羌活醇、异欧前胡素等Q-Marker与PTGS2水解酶的结合能低,构象稳定。建立了基于UHPLC-DAD测定羌活Q-Marker的方法,15批不同基原和产地的样品,紫花前胡苷质量分数为0.05～14.84 mg/g,香叶木苷质量分数0.04～3.88 mg/g,佛手柑内酯质量分数为0.07～0.32 mg/g,羌活醇质量分数为0.10～16.76 mg/g,异欧前胡素质量分数为0.20～7.99 mg/g。结论 基于生物合成途径、网络药理、分子对接和UHPLC预测并分析羌活抗炎Q-Marker的方法科学、可行,为羌活的质量标准提升和资源品质评价提供新思路。     

祛湿活络片质量标准研究

目的:研究祛湿活络片的质量标准。方法:用薄层色谱法检查当归、羌活、牛膝;用HPLC法测定阿魏酸的含量。结果:该药每片含阿魏酸不得低于0.03mg。结论:该定量方法快速灵敏,稳定可靠。     

紫花前胡的化学成分研究

目的 对紫花前胡Peucedanum decursivum的化学成分进行研究.方法 采用95％乙醇提取,经多种色谱方法分离纯化,利用质谱、核磁共振等现代波谱技术鉴定结构.结果 从紫花前胡95％乙醇提取物的醋酸乙酯萃取物中分离得到12个化合物,分别鉴定为异佛手柑内酯(1)、佛手柑内酯(2)、茴芹内酯(3)、异茴芹内酯(4)、二氢欧山芹醇乙酯(5)、6-牛防风素(6)、前胡香豆素E(7)、花椒毒素(8)、甲氧基欧芹酚(9)、阿魏酸(10)、β-谷甾醇(11)、补骨脂素(12).结论 化合物1、4、5为首次从前胡属植物中分离得到,化合物2、3、6～10、12为首次从该植物中分离得到.     

175 γ-谷维素的抗炎作用

γ-谷维素为米糠中的油脂成分,其主要成分为环阿尔廷基阿魏酸酯、24-亚甲基环阿尔廷基阿魏酸酯等。γ-谷维素具有抗氧化、抗菌、抗肿瘤等药理作用。近年研究表明,羌活、苍术中的阿魏酸酯具有抑制LPO和COX的活性。本次在研究γ-谷维素中阿魏酸酯对LPO或COX作用的同时,探讨了其对佐剂关节炎的作用。     

Evaluation of Inhibitory Effects of Caffeic acid and Quercetin on Human Liver Cytochrome P450 Activities

When herbal drugs and conventional allopathic drugs are used together, they can interact in our body which can lead to the potential for herb–drug interactions. This work was conducted to evaluate the herb–drug interaction potential of caffeic acid and quercetin mediated by cytochrome P450 (CYP) inhibition. Human liver microsomes (HLMs) were added to each selective probe substrates of cytochrome P450 enzymes with or without of caffeic acid and quercetin. IC₅₀, Ki values, and the types of inhibition were determined. Both caffeic acid and quercetin were potent competitive inhibitors of CYP1A2 (Ki = 1.16 and 0.93 μM, respectively) and CYP2C9 (Ki = 0.95 and 1.67 μM, respectively). Caffeic acid was a potent competitive inhibitor of CYP2D6 (Ki = 1.10 μM) and a weak inhibitor of CYP2C19 and CYP3A4 (IC₅₀ > 100 μM). Quercetin was a potent competitive inhibitor of CYP 2C19 and CYP3A4 (Ki = 1.74 and 4.12 μM, respectively) and a moderate competitive inhibitor of CYP2D6 (Ki = 18.72 μM). These findings might be helpful for safe and effective use of polyphenols in clinical practice. Our data indicated that it is necessary to study the in vivo interactions between drugs and pharmaceuticals with dietary polyphenols. Copyright © 2014 John Wiley & Sons, Ltd.     

Phytochemical and Pharmacological Investigations on Nymphoides indica Leaf Extracts

Nymphoides indica (L.) Kuntze (Menyanthaceae) is traditionally used in the Indian subcontinent. However, scientific data reporting its constituents are poor. This study aimed at evaluating its phytochemical constituents and various biological activities. Phytochemical investigations of the extracts and fractions resulted in the isolation of 5 lipophilic compounds, i.e. azelaic (nonanedioic) acid (1) and 4‐methyl‐heptanedioic acid (3), hexadecanoic (2) and stearic acid (5) and the fatty alcohol hexadecanol (4); 3 seco‐iridoids, i.e. 7‐epiexaltoside (6), 6″,7″‐dihydro‐7‐epiexaltoside (7) and menthiafolin (8); 3 flavonoids, i.e. 3,7‐di‐O‐methylquercetin‐4′‐O‐β‐glucoside (9), 3‐O‐methylquercetin‐7‐O‐β‐glucoside (10) and 3,7‐di‐O‐methylquercetin (11); scopoletin (12) and ferulic acid (13); and the monoterpenoids foliamenthoic acid (14) and 6,7‐dihydrofoliamenthoic acid methyl ester (15). Compounds 1–5 showed moderate antimicrobial activities, whereas compound 9 presented mild antiprotozoal activities against Trypanosoma brucei (IC₅₀ 8 μM), Leishmania infantum (IC₅₀ 32 μM) and Trypanosoma cruzi (IC₅₀ 30 μM). Antiglycation activity was shown by compounds 7 (IC₅₀ 0.36 mM), 10 (IC₅₀ 0.42 mM) and 15 (IC₅₀ 0.61 mM). Finally α‐glucosidase inhibition was shown by compounds 7, 9, 11 and 13–15. It could be concluded that N. indica leaf extracts possess mild to moderate antimicrobial, antiprotozoal, antioxidant and antidiabetic activities. Copyright © 2016 John Wiley & Sons, Ltd.     

Oleanolic acid prevents glucocorticoid-induced hypertension in rats

The present study was designed to evaluate the antihypertensive activity of oleanolic acid isolated from Viscum articulatum, Burm. (Loranthaceae) in glucocorticoid (dexamethasone)‐induced hypertension in rats and to propose a probable mechanism of action for this effect. Male Wistar rats (300–350 g) received dexamethasone (20 μg/kg/day s.c.) or saline (vehicle) for 10 days. In a prevention study, the rats received oleanolic acid (60 mg/kg i.p.) for 5 days, followed by dexamethasone or saline for 10 days. During this period the systolic blood pressure and body weight were evaluated on alternate days. At the end of the experiment, the weight of the thymus gland, plasma nitrate/nitrite (nitric oxide metabolites) concentration and cardiac lipid peroxidation value were determined. Oleanolic acid (60 mg/kg i.p.) significantly prevented a rise in the systolic blood pressure and cardiac lipid peroxidation level after administration of dexamethasone (p < 0.01 and p < 0.05, respectively) without showing any significant effect on the dexamethasone‐induced change in body and thymus weights. The decrease in concentration of plasma nitrate/nitrite due to dexamethasone was prevented significantly in the group treated with oleanolic acid (p < 0.05). These findings suggest that oleanolic acid (60 mg/kg i.p.) prevents dexamethasone‐induced hypertension in rats, which may be attributed to its antioxidant and nitric oxide releasing action. Copyright © 2011 John Wiley & Sons, Ltd.     

忍冬藤质量标准研究

 目的建立RP-HPLC测定忍冬藤中绿原酸、咖啡酸、当药苷和马钱子苷含量的方法,并以此对忍冬藤进行质量控制。方法色谱柱为Aglient Extend-C_{18(4.6 mm×250 mm,5μm);流动相为甲醇-0.4%醋酸水溶液(26∶74);流速1.0 mL·min^-1,检测波长240 nm。结果绿原酸、咖啡酸、当药苷和马钱子苷的线性范围和相关系数分别为23.5～470 mg·L^-1,r=0.999 9;12～240 mg·L^-1,r=0.999 7;10.5～210 mg·L^-1,r=0.999 9;13～260 mg·L^-1,r=0.999 8。平均回收率分别为97.7%(RSD=2.23%),96.6%(2.29%),95.0%(2.26%),103.3%(2.93%)。结论本方法简单、快速、可靠,可用于忍冬藤药材的质量控制。}     

小飞蓬化学成分的研究

 目的研究小飞蓬的化学成分。方法应用溶剂法进行提取,采用硅胶柱色谱和凝胶柱色谱Sephadex LH-20进行分离纯化,通过理化方法和波谱数据分析进行结构鉴定。结果从体积分数70%乙醇提取物中分离并鉴定了12个化合物,分别为α-香树脂醇(Ⅰ)、β-香树脂醇(Ⅱ)、β-谷甾醇(Ⅲ)、表木栓醇(Ⅳ)、齐墩果酸(Ⅴ)、菠甾醇-3-O-葡萄糖苷(Ⅵ)、3,5,7,3′,4′-五羟基黄酮(Ⅶ)、槲皮素-3-O-α-L-鼠李糖苷(Ⅷ)、芦丁(Ⅸ)、野黄芩苷(Ⅹ)、黄芩苷(Ⅺ)、绿原酸(Ⅻ)。结论12个化合物均为首次从该植物中分离得到。     

Evaluation of the Wound Healing Properties of Hancornia speciosa Leaves

The leaves of Hancornia speciosa Gomes (Apocynaceae), a medicinal species found in the Brazilian cerrado biome, are traditionally used to treat wounds and inflammatory disorders. The goal of the present study was to investigate the in vitro wound healing properties of ethanolic extract of H. speciosa leaves and its isolated compounds, using the scratch assay, and to evaluate their effects on the release of the pro‐inflammatory cytokine tumor necrosis factor (TNF‐α) by lipopolysaccharide (LPS)‐stimulated human acute monocytic (THP‐1) cells. H. speciosa ethanolic extract significantly increased (42.8% ± 5.4 at 25 µg/mL) cell migration and proliferation of fibroblasts compared with control cells, as well as the isolated compounds bornesitol (80.8% ± 5.1) and quinic acid (69.1% ± 6.2), both assayed at 50 μM. TNF‐α release by LPS‐stimulated THP‐1 cells was significantly reduced by the ethanolic extract (62.9% ± 8.2, i.e. 1791.1 ± 394.7 pg/mL) at 10 µg/mL, bornesitol (48.9% ± 0.9, i.e. 2461.6 ± 43.1 pg/mL) at 50 μM, and quinic acid (90.2% ± 3.4, i.e. 473.5 ± 164.4 pg/mL) and rutin (82.4% ± 5.6, i.e. 847.0 ± 271.8 pg/mL) at 10 μM. These results provided evidences to support the traditional use of H. speciosa leaves to treat wounds and inflammatory disorders. Copyright © 2015 John Wiley & Sons, Ltd.     

Modulation of tumour necrosis factor-α-induced cytotoxicity by polyphenols

The effects of several aromatic compounds on tumour necrosis factor-α (TNF)-induced cytotoxicity in murine fibroblast L929 cells were studied. Those phenolics which bear the O -dihydroxy aromatic structure (catechols), i.e. caffeic acid, catechol, 3,4-dihydroxybenzoic acid, dopamine and noradrenaline effectively inhibited TNF-induced cytotoxicity in a concentration dependent manner. Related compounds (cinnamic acid, 3,4-dimethoxycinnamic acid, 2,4-dihydroxybenzoic acid, ferulic acid, 3-hydroxy-4-methoxybenzoic acid and p -hydroxybenzoic acid) which lack the catecholic functional group failed to protect cells from TNF cytotoxicity. All concentrations of catechols which effectively inhibited the TNF-induced cytotoxicity were also protective as a post treatment, suggesting an effect at some step(s) in the TNF-signal transduction pathway following receptor activation. © 1997 John Wiley & Sons, Ltd.     

The analgesic-antiinflammatory extract from Araujia sericifera lacks ulcerogenic activity on stress-gastric damage model

The present study evaluates the ulcerogenic activity of the hexane extract from dry fruits of Araujia sericifera in an experimental model of cold-restraint stress. Treatment of rats with 200 mg/kg (i.p.) of hexane extract did not affect the gastric lesions induced by cold-restraint stress. However, it was confirmed that a dose of 300 mg/kg (i.p.) of acetylsalicylic acid (ASA) which induced a similar analgesic-antiinflammatory effect, increased significantly the level of gastric damage. Thus, the hexane extract from the fruits of A. sericifera seems to possess analgesic-antiinflammatory properties which are not linked to gastrolesive effects.     

白花泡桐叶三萜类化学成分研究

 目的 对白花泡桐叶的三萜类化学成分进行分离与鉴定。方法 利用硅胶柱色谱进行分离纯化,通过波谱分析鉴定其结构。结果 从白花泡桐叶的乙酸乙酯部分分离鉴定了11个三萜类化合物,分别鉴定为：2α,3β,19β-三羟基-乌苏酸-28-O-β-D-吡喃半乳糖苷（1,3α-羟基-乌苏酸（2,19α-羟基-乌苏酸（坡模酸（3,乌苏酸（熊果酸（4,23-羟基-乌苏酸（5,2α,3α-二羟基-12-烯-28-乌苏酸（6,3β,28-二羟基-乌苏烷（7,2α,3α,23-三羟基-12-烯-28-乌苏酸（8,2α, 3β, 19, 23-四羟基-12-烯-28-乌苏酸（9,2α-羟基-齐墩果酸（山楂酸（10,arjunic acid（11。结论 化合物3,5～11为首次从该植物中分离得到。     

Analgesic and anti-inflammatory activities of the crude hydroalcoholic extract obtained from the bark of Hymenaea martiana

Experiments were designed to examine the analgesic and anti-inflammatory activities of the crude hydroalcoholic extract (CE) of Hymenaea martiana. The CE of H. martiana (25-200 mg/kg, i.p.) caused a graded inhibition of hindpaw oedema induced by carrageenan, PAF-acether (PAF), serotonin (5-HT), dextran and histamine (HIS). However, the CE given orally up to 500 mg/kg had no effect on the agonist-induced hindpaw oedema. The CE given intraperitoneally, but not orally, caused a graded and pronounced inhibition of His, 5-HT, bradykinin (BK) and PAF-induced increase of vascular permeability. When the CE was given orally (300 mg/kg) once a day for 15 days it caused a significant increase of agonist-induced increase of vascular permeability. The CE given either by p.o. or by i.p. routes (100-800 mg/kg) dose-dependently inhibited arachidonic acid (AA)-induced ear oedema in mice, being significantly more potent when it was given by the latter route. In contrast, CE at the same doses, failed to inhibit croton-oil-induced ear oedema in mice. The CE of H. martiana given by either i.p. or p.o. routes caused a marked and dose-dependent antinociceptive activity as revealed by its antagonistic action against acetylcholine, acetic acid or AA-induced writhing responses in mice, being more effective when given intraperitoneally. These results, and those previously reported with the CE of H. martiana in the isolated preparations, provide strong experimental support which argues in favour of the beneficial use of this plant extract in folk medicine. The exact mechanism that underlies its analgesic and anti-inflammatory profiles remains unclear, but may result from its ability to inhibit the generation of lipoxygenase and/or cyclooxygenase products of the arachidonic acid pathway.