Therapeutic effects and mechanisms of total flavonoids of Turpinia Arguta Seen on adjuvant arthritis in rats

AIM: To investigate the therapeutic effects and mechanisms of total flavonoids of Turpinia Arguta Seen (TFS) on adjuvant arthritis in rats. METHODS: The model of adjuvant arthritis was induced by injection of Freund's Complete Adjuvant (FCA). Secondary paw swelling of AA rats was measured with volume meter and polyarthritis index were scored. The splenocyte proliferation, (interleukin-1) IL-1 and interleukin-2 (IL-2) production were assayed by cell proliferation assay. Prostaglandin E(2) (PGE(2)) production was determined by radioimmunoassay. RESULTS: TFS (80, 160, 320 mg/kg, i.g.) could significantly inhibit secondary inflammatory reaction (secondary swelling, multiple arthritis, pathologic change of ankle arthritis) in AA rats. The results in vivo showed that the low response of splenocytes to concanavalin A (Con A) and lipopolysaccharide (LPS) and the decreased IL-2 synthesis were restored in AA rats treated with TFS (160, 320 mg/kg, i.g.), while the elevated IL-1 and PGE(2) released from peritoneal macrophages (PMphi) were also reduced. CONCLUSION: TFS has significant therapeutic effect on AA rats, which might be relate to its immunoregulatory actions.     

山香圆叶中黄酮苷类成分及其抗炎活性研究

应用大孔树脂、聚酰胺、Sephadex LH-20,HPLC等各种色谱技术对山香圆叶95％乙醇提取物经乙酸乙酯萃取后的水部位进行分离纯化,分离得到8个黄酮苷类化合物,采用NMR等谱学方法分别鉴定为:野漆树苷(1),女贞苷(2),刺槐素-7-O-[β-D-吡喃葡萄糖基-(1→6)-α-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(3),刺槐素-7-O-[α-L-吡喃鼠李糖基(1→6)-o-L-吡喃鼠李糖基-(1→2)]-β-D-吡喃葡萄糖苷(密蒙花新苷,4),木犀草素-7-O-α-L-吡喃鼠李糖基-(1→2)-β-D-吡喃葡萄糖苷(5),金圣草素-7-O-α-L-吡喃鼠李糖基-(1→2)β-D-吡喃葡萄糖苷(6),刺槐素-7-O-α-L-吡喃鼠李糖基-(1→2)β-D-吡喃葡萄糖苷(蒙花苷,7),芹菜素6,8-二-C-β-D-吡喃葡萄糖苷(8).其中化合物3～8为首次从该植物中分离获得.采用脂多糖(LPS)刺激RAM264.7巨噬细胞炎症模型对分离得到的化合物进行抗炎活性评价,结果表明化合物2,3在1x10-5 mol.L-1浓度下,对LPS刺激RAW264.7细胞NO生成的抑制率分别为33.7％和23.8％,提示化合物2,3具有较弱的抗炎活性.     

Extracts of Actinidia arguta stems inhibited LPS-induced inflammatory responses through nuclear factor–κB pathway in Raw 264.7 cells

The inflammatory response protects our body from bacteria and tumors, but chronic inflammation driven by the persistent activation of macrophages can lead to serious adverse effects including gastrointestinal problems, cardiac disorders, and a sore throat. Part of the ongoing research is focused on searching for antiinflammatory compounds from natural sources, so we investigated the effects of hardy kiwis (Actinidia arguta, Lauraceae) stems on inflammation induced by lipopolysaccharide (LPS) in Raw 264.7 cells to test the hypothesis that antiinflammatory effects of A. arguta stems were exerted through the inhibition of the nuclear factor (NF)-κB pathway. The methanol extract of A. arguta (20 μg/mL) stems lowered nitric oxide production in LPS-stimulated Raw 264.7 cells by 40%. It was then partitioned with hexane, chloroform, ethyl acetate, butanol, and water based on the polarity of each compound. Among the 5 layers, the chloroform layer had the greatest inhibitory effect on LPS-stimulated nitric oxide production and inducible nitric oxide synthase mRNA expression in Raw 264.7 cells. However, the levels of prostaglandin E2 and cyclooxygease 2 were not altered. On the other hand, treatment of cells with the chloroform layer of A. arguta before LPS stimulation also reduced the mRNA expression of proinflammatory cytokines including tumor necrosis factor α and interleukin 1β. Nuclear translocation of NF-κB p50 and p65 subunits induced by LPS was also inhibited by treatment with the chloroform layer of A. arguta. This was accompanied with the reduced phosphorylation of mitogen-activated protein kinases including extracellular signal-regulated protein kinase 1/2, c-Jun N-terminal protein kinase, and p38. Taken together, these results suggest that chloroform layer of A. arguta exerted antiinflammatory effects by the inhibition of mitogen-activated protein kinase phosphorylation and nuclear translocation of NF-κB.     

软枣猕猴桃根的化学成分研究

[目的]研究软枣猕猴桃根的化学成分.[方法]反复采用硅胶和反相硅胶柱等色谱技术分离纯化化合物,根据化合物的理化性质和波谱学数据进行分析,鉴定化学结构.[结果]从软枣猕猴桃根中分离得到4个化合物,分别鉴定为白桦脂酸(1)、对羟基苯乙醇(2)、儿茶素(3)和表儿茶素(4).[结论]化合物2为首次从该植物中分离得到.     

软枣猕猴桃的化学成分和药理活性研究进展

软枣猕猴桃为猕猴桃科猕猴桃属多年生落叶藤本植物,在我国东北三省的分布最为广泛.其果实、根、茎叶均可入药,具有抗肿瘤、抗辐射、提高免疫功能等药理活性.研究表明,软枣猕猴桃全株含有挥发油、三萜、黄酮、多糖等化学成分.综述了近年来从软枣猕猴桃果实、根、茎叶中分离到的挥发油类、三萜类、黄酮类等化学成分,及其肿瘤抑制、抗辐射、提...     

软枣猕猴桃超氧化物歧化酶的分离纯化与特性研究

目的从软枣猕猴桃果实中提取纯化超氧化物歧化酶 (SOD) ,并对其特性进行研究。方法先以硫酸铵分级沉淀 ,后经DE 5 2纤维素柱色谱 ,磷酸缓冲液进行梯度洗脱。结果得SOD干粉 0 .918mg ,其分子量约为 30 6 0 0D ,亚基分子量约为 15 2 0 0D ,最大紫外吸收波长为 2 5 4nm。结论软枣猕猴桃果实含丰富的SOD。     

藤梨根乙酸乙酯提取物对人食管癌细胞生长的抑制作用

目的 观察藤梨根乙酸乙酯提取物对培养的人食管癌Eca-109细胞的生长抑制作用,探讨藤梨根对人食管癌细胞的作用机制.方法 MTT比色法检测藤梨根乙酸乙酯提取物在不同浓度（1 μg/ml,10 μg/ml,100 μg/ml）及不同时间（2 h,48h,72 h）对Eca-109细胞生长抑制作用,TUNEL法检测其对癌细胞生长的诱导凋亡效应,免疫组化SP法检测凋亡相关蛋白Bax及Bcl-2的表达.结果 ①藤梨根乙酸乙酯提取物对人食管癌Eca-109细胞的生长抑制作用随着药物浓度的升高和作用时间的延长而增强,其生长抑制率可达到77.5%.②提取物对瘤细胞有明显的凋亡效应,而在对照组,未见有明显凋亡现象.③提取物对瘤细胞作用24 h,48 h,72 h后分别与对照组比较,用药组Bax蛋白表达明显增强（P＜0.01）;同时伴有Bcl-2表达的减弱,在72 h后最明显,差异有显著意义（P＜0.01）.结论 藤梨根乙酸乙酯提取物能有效抑制人食管癌Eca-109细胞生长.     

藤梨根诱导人食管癌Eca-109细胞凋亡的调节机制

目的研究藤梨根（Actinidia arguta）抑制人食管癌Eca-109细胞增殖和诱导凋亡的机制。方法采用MTT比色法,检测藤梨根正丁醇药液在不同浓度（1μg/ml、10μg/ml、100μg/ml等）及不同时间（24 h、48 h、72 h等）对Eca-109细胞生长抑制作用;采用免疫组化SP法,检测凋亡相关蛋白Bax、Bcl-2及Caspase的表达。结果藤梨根正丁醇药液对人食管癌Eca-109细胞的生长抑制作用,随着药物浓度的升高和作用时间的延长而增强,其生长抑制率可达87.2%。瘤细胞作用24 h﹑48 h﹑72 h后分别与对照组比较,用药组Bax蛋白表达明显增强（P〈0.01）;同时伴有Bcl-2表达减弱7,2 h后最明显,差异有显著意义（P〈0.01）。藤梨根正丁醇药液促进Caspase-3、Caspase-9表达明显增强,而对Caspase-8表达影响较小。结论藤梨根可通过下调Bcl-2表达,激活Caspase-9、Caspase-3诱导Eca-109细胞凋亡。     

山香圆叶药材中鞣花酸的提取分离与含量测定

目的:建立山香圆叶药材中鞣花酸的制备工艺及含量测定方法,比较不同产地山香圆叶药材中鞣花酸的含量。方法:采用溶剂提取、大孔树脂及反相硅胶柱色谱和重结晶等提取分离手段得到鞣花酸对照品;用高效液相色谱法测定山香圆叶药材中鞣花酸的含量,Ultimate XB-C18色谱柱(4.6 mm×250 mm,5μm),流动相乙腈-0.1%磷酸(19∶81),流速1.0 mL·min-1,检测波长254 nm,柱温30℃。结果:所得鞣花酸的纯度在98.5%以上,鞣花酸进样量在0.020 0~0.400 8μg线性关系良好(r=0.999 8),平均回收率为101.25%;10个产地的山香圆叶中鞣花酸含量在0.37%~1.56%。结论:提取分离工艺得到的鞣花酸纯度高,可作为含量测定用对照品;含量测定方法简便、快速、定量准确,可用于山香圆叶中鞣花酸的含量测定;不同产地山香圆叶药材中鞣花酸的含量差异明显,为山香圆叶药材的资源开发提供了参考依据。     

山香圆颗粒联合抗病毒颗粒治疗小儿急性上呼吸道感染的临床疗效和安全性

目的：观察山香圆颗粒联合抗病毒颗粒治疗小儿急性上呼吸道感染的临床疗效和安全性观察。方法：将812例急性上呼吸道感染患儿随机分组,其中治疗组406例,给予山香圆颗粒联合抗病毒颗粒治疗;对照组406例,给予抗病毒颗粒治疗;疗程均为3d。观察两组患儿临床治疗效果以及不良反应情况。并对比其流涕及鼻塞停止时间、退热时间、咽部充血消失时间以及咳嗽停止时间。结果：治疗组各项临床时间指标均短于对照组,差异具有统计学意义（ P＜0．05）;两组患儿治疗过程中及治疗后均无不良反应发生;治疗组总有效率为91．6％,高于对照组的78．3％,差异显著（ P＜0．05）。结论：山香圆颗粒联合抗病毒颗粒治疗小儿急性上呼吸道感染安全性较高,临床疗效显著,无不良反应情况发生,值得临床推广应用。