The polysaccharide fraction AIP1 from Artemisia iwayomogi suppresses apoptotic death of the mouse spleen cells in culture

A polysaccharide fraction, AIP1, purified from Artemisia iwayomogi was shown to have immunomodulating and anti-tumor activities in mice. In order to determine how the AIP1 fraction exhibits the immunomodulating activity, the effect of the fraction on the apoptosis of mouse spleen cells was investigated. Treatment of the mouse spleen cells with the AIP1 fraction resulted in the suppression of apoptotic death and an extension of cell survival in culture, indicating that the fraction might modulate the death of spleen cells. Treatment of the mice with the AIP1 fraction in vivo also resulted in less apoptosis of the spleen cells, which indicates the physiological relevance of the anti-apoptosis effect of the fraction in vitro. A mouse gene array was used to determine the profile of the gene expression change showing a pattern of up- and down-regulated genes by the AIP1 treatment. This study provides preliminary information regarding the immunomodulatory mechanism of the AIP1 fraction.     

青蒿药理作用研究进展

青蒿所含化学成分丰富,药用价值高,药理作用广。随着科学技术和研究手段的不断发展与创新,对于青蒿药理作用及其机制的研究也逐渐深入。本文综合近年来国内外相关文献报道,经过整理总结阐述青蒿中主要化学成分抗疟、抗肿瘤、抑菌杀虫、抗炎及免疫调节、抗纤维化、抑制脂肪变性等药理作用及机制,为进一步促进我国中医药行业的发展,同时也为青蒿的合理使用以及临床新用提供更多的理论依据。     

沪产艾蒿鲜叶挥发油成分的GC-MS分析

目的：分析沪产艾蒿鲜叶的挥发性成分,为艾蒿鲜叶的开发利用提供依据.方法：通过水蒸馏法提取艾蒿鲜叶挥发油,用气相色谱一质谱联用技术分析其化学成分。结果：从艾蒿鲜叶挥发油中鉴定了68个成分、主要为大香叶烯D（gennacrene D）、桉叶素（cineole）、石竹烯（caryophyllenene）、侧柏酮（thujone）,占总含量80％以上。结论：沪产艾蒿鲜叶含有的挥发油成分主要为大香叶烯D、桉叶素、石竹烯、侧柏酮,其中侧柏酮为艾蒿鲜叶的最主要成分,与干燥药材的挥发油成分有较大区别,在应用新鲜艾叶时应加以注意。     

Chlorogenic acid, an antioxidant principle from the aerial parts ofArtemisia iwayomogi that acts on 1,1-diphenyl-2-picrylhydrazyl radical

The antioxidant activity ofArtemisia iwayomogi was determined by measuring the radical scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical The methanol extract ofA. iwayomogi showed strong antioxidant activity, and thus fractionated with several solvents. The antioxidant activity potential of the individual fraction was in the order of ethyl acetate>n-butanol>water>chloroform>n-hexane fraction. The ethyl acetate andn-butanol soluble fractions exhibiting strong antioxidant activity were further purified by repeated silica gel and Sephadex LH-20 column chromatography. Antioxidant chlorogenic acid was isolated as one of the active principles from then-butanol fraction, together with the inactive components, 1-octacosanol, scopoletin, scopolin, apigenin 7,4′-di-O-methylether luteolin 6,3′-di-O-methylether (jaceosidin), apigenin 7-methylether (genkwanin), 2,4-dihydroxy-6-methoxyacetophenone 4-O-β-D-glucopyranoside and quebrachitol. The antioxidant activity of chlorogenic acid was comparable to that of L-ascorbic acid, which is a well known antioxidant.     

基于网络药理学的青蒿治疗肾阴虚型糖皮质激素性骨质疏松机制研究

目的 通过网络药理学和体外实验,对青蒿治疗肾阴虚型糖皮质激素性骨质疏松（GIOP）的潜在作用靶点及相关信号通路进行预测和初步验证。方法 通过TCMSP数据库和Uniprot数据库获取青蒿药物靶点并确定目标靶点基因名;通过GeneCards数据库、OMIM数据库和Drugbank数据库获取肾阴虚型GIOP的靶点基因,与药物靶点基因交叉分析获得共同作用靶点基因;利用String数据库构建蛋白质-蛋白质相互作用（PPI）网络,并利用Cytoscape软件进行可视化分析和核心靶点筛选;通过Metascape数据库对所有共同靶点进行基因本体（GO）和京都基因与基因组百科全书（KEGG）富集分析,最后通过体外实验对预测结果进行验证。结果 筛选出98个青蒿治疗肾阴虚型GIOP的作用靶点,其中核心基因17个。GO和KEGG功能富集分析结果表明,青蒿治疗肾阴虚型GIOP与激素应答、细胞死亡的正向调节和细胞外刺激应答等生物过程,以及PI3K/AKT、AGE/RAGE、MAPK和IL-17等信号通路有关,其中PI3K/AKT信号通路上富集的基因数最多。体外实验结果显示,青蒿可以促进地塞米松（DEX）损伤的成...     

A Carbohydrate Fraction, AIP1, from Artemisia Iwayomogi Reduces the Action Potential Duration by Activation of Rapidly Activating Delayed Rectifier K+ Channels in Rabbit Ventricular Myocytes

We investigated the effects of a hot-water extract of Artemisia iwayomogi, a plant belonging to family Compositae, on cardiac ventricular delayed rectifier K⁺ current (I_K) using the patch clamp technique. The carbohydrate fraction AIP1 dose-dependently increased the heart rate with an apparent EC₅₀ value of 56.1±5.5 µg/ml. Application of AIP1 reduced the action potential duration (APD) in concentration-dependent fashion by activating I_K without significantly altering the resting membrane potential (IC₅₀ value of APD₅₀: 54.80±2.24, IC₅₀ value of APD₉₀: 57.45±3.47 µg/ml). Based on the results, all experiments were performed with 50 µg/ml of AIP1. Pre-treatment with the rapidly activating delayed rectifier K⁺ current (I_Kr) inhibitor, E-4031 prolonged APD. However, additional application of AIP1 did not reduce APD. The inhibition of slowly activating delayed rectifier K⁺ current (I_Ks) by chromanol 293B did not change the effect of AIP1. AIP1 did not significantly affect coronary arterial tone or ion channels, even at the highest concentration of AIP1. In summary, AIP1 reduces APD by activating I_Kr but not I_Ks. These results suggest that the natural product AIP1 may provide an adjunctive therapy of long QT syndrome.     

A new sesquiterpene from <Emphasis Type="Italic">Artemisia vulgaris</Emphasis>

The dichloromethane extract of the air-dried leaves of Artemisia vulgaris afforded a new sesquiterpene 1, caryophyllene oxide, phytyl fatty acid esters, squalene, stigmasterol and sitosterol. The structure of 1 was elucidated by extensive one- and two-dimensional nuclear magnetic resonance spectroscopy.     

青蒿鞣质抗单纯疱疹病毒机理初探

目的探讨青蒿鞣质(CTA)抗单纯疱疹病毒2型(HSV-2)的作用机理。方法采用细胞病变效应(CPE)抑制法和MTT法，以阿昔洛韦(ACV)为阳性对照药物，研究青蒿鞣质在体外对HSV-2的直接杀灭、病毒感染阻断、不同时间感染后的CPE抑制效果。结果CTA对病毒具有明显的直接杀灭作用，可以阻断病毒的吸附过程和抑制病毒在细胞内的复制，而且CTA对病毒的抑制作用受病毒吸附时间的影响很小，具有明显的治疗作用，其效果与阳性对照药物无环乌苷(ACV)相当。结论CTA体外抗HSV-2作用可以通过多种途径发挥作用。     

In vitro anti-plasmodial and in vivo anti-malarial activity of some plants traditionally used for the treatment of malaria by the Meru community in Kenya

Extracts of seven medicinal plant species used for treatment of malaria in traditional/cultural health systems of the Ameru people in Kenya were tested in vitro and in vivo against Plasmodium falciparum (D6 and W2 strains) and P. berghei, respectively. Of the plants tested, 28.57% were highly active (IC₅₀ <10 μg/ml) and 42.86% moderately active (IC₅₀ 10–50 μg/ml), while 28.57% had weak activity of 50–125 μg/ml in vitro. The water and methanol extracts of Boscia salicifolia Oliv. and Artemisia afra Jacq. (ex-Willd.) were the most active against both the chloroquine (CQ)-sensitive (D6) and the CQ-resistant (W2) P. falciparum strains. Artemisia afra and Rhus natalensis Bernh. (ex-Krauss) exhibited the highest parasite clearance and chemo-suppression (>70%) in vivo (in mice). The plants with high in vitro anti-plasmodial (low IC₅₀ values) and high anti-malarial activity (high chemo-suppression) in vivo are potential sources of novel anti-malarial drugs.     

15-14C标记青蒿素的合成

15-¹⁴C]Artemisinin(8) was prepared by the biosynthesis of[15-¹⁴C]dihydroartemisic acid(14) which was synthesized from diketone in 6 steps. A supernatant liquidprepared from the tender leaves of ripe Shanghai Qinghao(Artemisia annua L.)was incubated with themixture of compounds l3 and l4(100 mg, total activity 3. 26 MBq, 13:14=1:1) at 30℃ or 37℃ for 4 hr. After the addition of natural artemisinin(100 mg) ,the mixture was heated at l00℃for5min , and extracted with chloroform(method A)or petroleum ether(bp. 60～90℃, method B).Theextract was evaporated and the residue was recrystallized(method B)or purified py preparative thinlayer chromatography(methed The crude product was recrystallized from methylene chloride—Petroleum ether to yield 8 with constant specific radioactivity. The mean rate of incorporation in runs1～8was l.17%。The possible influence factors of the biotransformation were studied. The incuhation temperaturewas considered as a key factor.     

3,5-O-二咖啡酰基奎宁酸的制备及其对HeLa细胞的抗增殖活性研究

目的 制备高纯度3，5-O-二咖啡酰基奎宁酸，并评价其对人宫颈癌HeLa细胞的抗增殖活性。方法 采用柱色谱提取法和中压液相色谱法从奇蒿花中分离、纯化得到高纯度的3，5-O-二咖啡酰基奎宁酸。采用MTT法评价该化合物对人宫颈癌HeLa细胞的体外抗增殖活性。结果 柱色谱提取的提取率和中压液相色谱法的回收率分别为99.0%，61.2%，总回收率为54.0%。随着3，5-O-二咖啡酰基奎宁酸浓度升高，HeLa细胞存活率下降，细胞形态损伤增加，受试药物的IC₅₀值为26.5µg·mL^-1。结论 本研究提供了一种简单、高效、节能的3，5-O-二咖啡酰基奎宁酸制备方法。3，5-O-二咖啡酰基奎宁酸对HeLa细胞具有一定的体外抗增殖活性。     

Composition of the essential oil from the root of <Emphasis Type="Italic">Artemisia annua</Emphasis>

Upon hydrodistillation, dried roots of Artemisia annua L. cultivar Jwarharti gave a pleasantly fragrant essential oil with a yield of 0.25%. GC and GC–MS analyses of the oil enabled the identification of 52 components representing 83.2% of the oil. The oil was rich in sesquiterpenes and oxygenated sesquiterpenes and had cis-arteannuic alcohol (25.9%), (E)-β-farnesene (6.7%), β-maaliene (6.3%), β-caryophyllene (5.5%), caryophyllene oxide (4.4%) and 2-phenylbenzaldehyde (3.5%) as its major components. The oil was found to possess considerable fumigant activity and ability to repel adult Tribolium castaneum beetles.     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

复方中药延缓秀丽线虫衰老的作用研究

目的 以模式动物秀丽线虫为模型,对以黄芪等为主要成分的复方汤剂开展抗衰老活性研究。方法 先检测原始汤剂对秀丽线虫的寿命延长作用,然后对原始汤剂进行萃取分离获得不同提取部位再检测各部位对秀丽线虫寿命的影响,同时采用薄层色谱法鉴定原始汤剂及其提取部位的代表性化学成分。结果 原始复方汤剂及其多糖萃取部位具有延缓秀丽线虫衰老的作用,毛蕊花糖苷、芦丁、黄芪甲苷等化合物是复方汤剂的代表性化学成分。结论 本文复方汤剂通过多糖成分发挥其抗衰老作用。     

Yomogin, an inhibitor of nitric oxide production in LPS-activated macrophages

In activated macrophages the inducible form of nitric oxide synthase (i-NOS) generates high amounts of toxic mediator, nitric oxide (NO) which contributes to the circulatory failure associated with septic shock. A sesquiterpene lactone compound (yomogin) isolated from medicinal plantArtemisia princeps Pampan inhibited the production of NO in LPS-activated RAW 264.7 cells by suppressing i-NOS enzyme expression. Thus, yomogin may be a useful candidate for the development of new drugs to treat endotoxemia and inflammation accompanied by the overproduction of NO.     

Studies on protective effect of DA-9601,Artemisia asiatica extract, on acetaminophen- and CCI4-induced liver damage in rats

The hepatoprotective effect of DA-9601, a quality-controlled extract ofArtemisia asiatica, on liver damage induced by acetaminophen (APAP) and carbon tetrachloride (CCI₄) was investigated by means of serum-biochemical, hepatic-biochemical, and histopathological examinations. Doses of DA-9601 (10, 30, or 100mg/kg) were administered intragastrically to each rat on three consecutive days i.e. 48 h, 24 h and 2 h before a single administration of APAP (640 mg/kg, i.p.) or CCl₄ (2 ml/kg, p.o.). Four h and 24 h after hepatotoxin treatment, the animals were sacrificed for evaluation of liver damage. Pretreatment of DA-9601 reduced the elevation of serum ALT, AST, LDH and histopathological changes such as centrilobular necrosis, vacuolar degeneration and inflammatory cell infiltration dose-dependently. DA-9601 also prevented APAP- and CCl₄-induced hepatic glutathione (GSH) depletion and CCl₄-induced increase of hepatic malondialdehyde (MDA), a parameter of lipid peroxidation, in a dose-dependent manner. These findings suggest that pretreatment with DA-9601 may reduce chemically induced liver injury by complex mechanisms which involve prevention of lipid peroxidation and preservation of hepatic GSH.     

<Emphasis Type="Italic">In Vitro</Emphasis> antioxidant and anti-inflammatory activities of Jaceosidin from <Emphasis Type="Italic">Artemisia princeps</Emphasis> Pampanini <Emphasis Type="Italic">cv.</Emphasis> Sajabal

Oxidized low-density lipoprotein (oxLDL) plays a key role in the inflammatory processes of atherosclerosis. Jaceosidin isolated from the methanolic extracts of the aerial parts of Artemisia princeps Pampanini cv. Sajabal was tested for antioxidant and anti-inflammatory activities. Jaceosidin inhibited the Cu²⁺-mediated LDL oxidation with IC₅₀ values of 10.2 μM in the thiobarbituric acid-reactive substances (TBARS) assay as well as the macrophage-mediated LDL oxidation. The antioxidant activities of jaceosidin were exhibited in the conjugated diene production, relative electrophoretic mobility, and apoB-100 fragmentation on copper-mediated LDL oxidation. Jaceosidin also inhibited the generation of reactive oxygen species (ROS) concerning in regulation of NF-κB signaling. And jaceosidin inhibited nuclear factor-kappa B (NF-κB) activity, nitric oxide (NO) production, and suppressed expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-induced RAW264.7 macrophages.     

Screening and isolation of antibiotic resistance inhibitors from herb materials IV-resistance inhibitors fromAnetheum graveolens andAcorus gramineus

The hexane fractions from methanolic extracts ofAnetheum graveolens L. (Umbelliferae) andAcorus gramineus Soland. (Araceae) revealed potent inhibitory activities against the resistance of multi-drug resistantStaphylococcus aureus SA2 when combined with ampicillin (Am) or chloramphenicol (Cm). As active principles, carvone and the liquid mixture containing carvone fromAnetheum graveolens L. and a liquid mixture mainly consisting of benzoic acid phenylmethyl ester (benzyl benzoate) fromAcorus gramineus Soland. were identified. They showed resistance inhibition at the level of 20–50 μg/ml when combined with 100 or 50 μg/ml of Am or Cm, respectively.     

Inhibitors of inducible nitric oxide synthase expression from<Emphasis Type="Italic">artemisia iwayomogi</Emphasis>

Nitric oxide (NO) is an important bioactive agent that mediates a wide variety of physiological and pathophysiological events. NO overproduction by inducible nitric oxide synthase (iNOS) results in severe hypotension and inflammation. This investigation is part of a study to discover new iNOS inhibitors from medicinal plants using a macrophage cell culture system. Two sesquiterpenes (1 and 2) were isolated from Artemisia iwayomogi (Compositae) and were found to inhibit NO synthesis (IC50 3.64 microg/mL and 2.81 microg/mL, respectively) in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Their structures were identified as 3-O-methyl-isosecotanapartholide (1) and iso-secotanapartholide (2). Compounds 1 and 2 inhibited the LPS-induced expression of the iNOS enzyme in the RAW 264.7 cells. The inhibition of NO production via the down regulation of iNOS expression may substantially modulate the inflammatory responses.     

蛹虫草菌丝体多糖与子实体多糖体外免疫调节活性的研究

目的 分析蛹虫草菌丝体多糖（mycelia polysaccharides of Cordyceps militaris,MPS）与蛹虫草子实体多糖（polysaccharides from fruiting body of Cordyceps militaris,FPS）的体外免疫活性。方法 以RAW264.7细胞株为受试对象,从细胞增殖、中性红吞噬能力、NO释放水平角度系统考察不同浓度的MPS与FPS的免疫调节活性,并分析其量化关系。结果 MPS与FPS均可明显促进RAW264.7细胞株的增殖、对中性红的吞噬能力和NO释放水平,且均呈现出浓度依赖性的特征。二者对RAW264.7细胞株增殖的促进作用无显著性差异,但在免疫调节最佳作用浓度方面却存在一定差异,MPS在100μg·mL^-1时表现出最好的细胞吞噬能力,而FPS在200μg·mL^-1时表现出最高的细胞吞噬能力。结论 MPS与FPS均具有显著的体外免疫活性。