苦楝子的化学成分研究(Ⅱ)

目的研究苦楝子Melia azedarach醇提物的化学成分。方法采用硅胶色谱技术进行分离纯化,根据理化性质和光谱学方法进行结构鉴定。结果分离得到9种化合物,分别鉴定为21α,25-二甲氧基苦楝酮二醇(1)、苦楝二醇(2)、2,3-二羟基-1-(4-羟基-3-甲氧基)苯基-1-酮(3)、松柏醛(4)、苦楝新醇(5)、(E)-3,3′-二甲氧基-4,4′-二羟基二苯乙烯(6)、5-羟甲基糠醛(7)、原儿茶醛(8)、芦丁(9)。结论化合物1、3、4、7～9系首次从该植物中分离得到。     

金败酱化学成分的研究

目的研究金败酱的化学成分。方法利用各种色谱分离技术进行分离纯化,根据化合物的理化性质和波谱数据进行结构鉴定。结果分离得到4个化合物,分别为:(反)-β-法尼烯[(E)-β-farnesene,Ⅰ],角鲨烯(squalene,Ⅱ)、nar-dostachin(Ⅲ),齐墩果酸(oleanolic acid,Ⅳ)。结论化合物Ⅰ和Ⅱ为首次从该植物中分得。     

中药白及化学成分的研究

目的 :研究中药白及的化学成分。方法 :多种色谱方法分离 ,理化性质和波谱分析鉴定结构。结果 :分离并鉴定了3个化合物 ,3 (4-羟基-3-甲氧基苯)-反式丙烯酸二十六醇酯 (1) ,大黄素甲醚 (2)和环巴拉甾醇 (3)。结论 :化合物 1为新化合物 ,化合物 3为首次从该植物中分离得到。     

UPLC/Q-TOF-MS方法测定黄芪皂苷Ⅰ、Ⅱ、Ⅳ含量并研究水解对黄芪皂苷类成分的影响

本实验采用UPLC/Q-TOF-MS方法结合多变量统计分析(PCA、OPLS-DA),分析不同批次黄芪饮片碱洗前后黄芪皂苷类成分变化趋势及原因。并对黄芪皂苷Ⅰ、Ⅱ、Ⅳ进行含量测定。为以黄芪皂苷类成分作为指标成分进行黄芪饮片及含黄芪中成药质量研究提供了实验依据。本实验采用ACQUITY UPLC C18色谱柱以乙腈-甲酸(1 m L/L)水溶液作为流动相进行梯度洗脱,流速0.45 m L/min,柱温40℃。使用ESI电离源在正、负离子模式下采集数据,应用Masslynx 4.1质谱工作站软件进行分多变量统计分析(PCA、OPLS-DA)。明确了黄芪饮片供试品制备过程氨水洗涤步骤能够使黄芪皂苷Ⅰ、Ⅱ水解脱乙酰基转化为黄芪皂苷Ⅳ。同时应用UPLC/Q-TOF-MS方法测定了黄芪饮片中黄芪皂苷Ⅰ、Ⅱ、Ⅳ含量,该方法简单、快速、重现性较好,可用于黄芪饮片中该三个成分的含量测定。本实验为以黄芪皂苷类成分作为指标成分进行黄芪饮片及含黄芪中成药质量研究提供了实验依据。     

滋阴潜阳活血汤对肾性高血压大鼠左室肥厚的影响

目的:探讨滋阴潜阳活血汤对肾性高血压大鼠左室肥厚的影响及作用机制。方法:建立2K1C肾性高血压大鼠模型,随机分为模型组、中药组及假手术对照组。假手术组和模型组:生理盐水80mg.kg-1.d-1,腹腔注射,连续8周;中药组:滋阴潜阳活血汤剂浓缩后40g.kg-1.d-1,连续灌胃给药8周。8周后,分别测定各组大鼠平均颈动脉压(mCAP)、左室舒张末期压(LVEDP)以及左心室压力变化最大速率(LV±dp/dtmax)、左心重与体重比值(LVMI=LVM/BW),放射免疫法测定血浆及局部心肌血管紧张素Ⅱ(AngⅡ),透射电镜观察心肌形态学的变化。结果:①与假手术组相比,模型组大鼠mCAP、LVEDP和LVMI均明显升高(P<0.01),LV+dp/dtmax降低(P<0.05),血浆及心肌AngⅡ显著升高(P<0.01),左室肥厚形成,左室重构发生,心功能下降。②与模型组相比,中药组LV+dp/dtmax和LV-dp/dtmax则明显升高(P<0.01或P<0.05),而mCAP、LVEDP和LVMI则显著降低(P<0.01或P<0.05),血浆及心肌AngⅡ亦显著降低(P<0.01),表明中药组能够降低血压并逆转左室肥厚。③电镜观察:模型组大鼠心室肌丝松散,部分溶解断裂,闰盘增宽;基膜下轻度水肿。与模型组比较,中药组上述病变明显减轻。假手术组未见上述病变。结论:滋阴潜阳活血汤能有效地降低肾性高血压大鼠血压并逆转左室肥厚,其作用机制可能与降低血浆及心肌局部AngⅡ、抑制体内肾素-血管紧张素系统(RAS)代谢有关。     

二陈汤加味对慢性阻塞性肺疾病细支气管壁细胞外基质重塑的影响

目的:观察二陈汤加味对慢性阻塞性肺疾病(COPD)模型大鼠细支气管结构重塑的作用及其机制。方法:50只SD大鼠随机分为正常组、模型组、二陈汤加味低、中、高剂量组(5,10,20 g·kg-1),共5组,每组10只。以香烟烟熏加内毒素脂多糖(LPS)制备大鼠COPD模型。造模成功后,各观察组灌胃给药,检测肺功能,实时荧光定量聚合酶链式反应(Real-time PCR)检测肺组织中基质金属蛋白酶-1(matrix metalloproteinases,MMP-1),MMP-9及金属蛋白酶组织抑制剂-1(tissueinhibitor of metalloproteinase,TIMP-1)mRNA表达,免疫组织化学法(immunohistochemistry,IHC)检测MMP-1,MMP-9,TIMP-1以及Ⅰ型和Ⅲ型胶原在细支气管中的表达。结果:与正常组比较,模型组肺组织匀浆MMP-1,MMP-9,TIMP-1 mRNA表达均显著增强(P0.01),细支气管壁MMP-1,MMP-9,TIMP-1,Ⅰ型及Ⅲ型胶原蛋白的表达均显著增强(P0.05)。与模型组比较,中、高剂量组肺组织匀浆MMP-1,MMP-9,TIMP-1 mRNA表达显著减弱(P0.01),细支气管壁中、高剂量组Ⅰ型和Ⅲ型胶原蛋白的表达明显减弱(P0.05)。结论:二陈汤加味对细支气管管壁细胞外基质(extracellular matrix,ECM)中的胶原有抑制作用。其机制可能与抑制MMP-1,MMP-9,并协调性抑制TIMP-1的表达,阻止细支气管ECM胶原的沉积有关。     

锁阳化学成分的研究

从锁阳中分得两个甾醇类化合物,经化学及光谱方法测定结构为5α-豆甾-9(11)-烯-3β-醇和5α-豆甾-9(11)-烯-3β-醇-二十四碳三烯酸酯,均为首次从该植物中获得。     

蛹虫草子实体抗肿瘤作用的实验研究

本实验以S180 小鼠肉瘤为动物模型 ,对沈阳地区培育的蛹虫草子实体的抗肿瘤作用进行了药效学研究。结果显示 ,该药可明显延长S180 腹水型小鼠的生存率 ,对S180 实体瘤小鼠的肿块生长有一定的抑制作用 ;对S180荷瘤小鼠的肿瘤免疫活性因子TNF - β和IL - 2有明显的促进作用 ,并优于中药复方制剂对照药强力康免疫升白冲剂 (P <0 0 1)。     

壮丽含笑活性成分的提取分离及抗菌活性的研究

用溶剂提取和色谱技术进行分离（柱层析LSC,薄层层析TLC）壮丽含笑中具有抗菌活性的活性段,并用琼脂打孔法和二倍稀释法测定其活性段对标准金黄色葡萄球菌、标准大肠埃希菌、标准铜绿假单胞菌、标准白色念珠菌以及临床分离得到的耐甲氧西林金黄色葡萄球菌的体外抑菌效果。利用活性导向继续分离有活性的色谱段并追踪到活性单体。这对从植物中寻找抗MRSA的活性成分具有指导意义。     

In vitro anthelmintic activity of Melia azedarach naturalized in Argentina

The anthelmintic activity of the drupe extracts of Melia azedarach L. (Meliaceae) growing in Argentina was tested against tapeworms, hookworms, nodular worms and earthworms, and was shown to be better than the standards piperazine phosphate and hexylresorcinol against tapeworms and hookworms, respectively.     

Antibacterial effect of Melia azedarach flowers on rabbits

A methanol extract of Melia azedarach flowers showed potent antibacterial action in rabbits suffering from a skin infection produced by Stapyhlococcus aureus. The healing effects were found comparable to neomycin.     

Partially purified leaf extracts of Melia azedarach L. inhibit tacaribe virus growth in neonatal mice

Neonatal mice, inoculated intraperitoneally with 10³ PFU of Tacaribe virus, died after developing a typical encephalitis. The administration of partially purified extracts of Melia azedarach L. (Ma) fresh green leaves, in seven doses by the same route, reduced virus spread which normally involves the kidneys, liver and brain. Mortality fell to 50% in treated mice and viral titres in brain were at least 3 logs lower than those of untreated mice. Surviving mice mounted a humoral immune response. High levels of neutralizing antibodies were present up to 60 days post-infection when the animals were killed. Ma administration exerts a marked decrease in circulating interferon levels of infected mice. Thus, at day 6 post-infection the amount of acid resistant interferon in treated animals was eight times lower than in those untreated. The antiviral effect of Ma in vivo is clearly stated in this murine-arenavirus model.     

An antiviral principle present in a purified fraction from Melia azedarach L. leaf aqueous extract restrains herpes simplex virus type 1 propagation

Meliacine (MA), an antiviral principle isolated from leaves of Melia azedarach L., exhibits potent antiviral activity against herpes simplex virus type 1 (HSV-1) by inhibiting specific infected-cell polypeptides (ICPs) produced late in infection. Some of these are involved in DNA synthesis and in the assembly of nucleocapsids. The present report provides additional evidence to elucidate the mode of action of MA against HSV-1. Time-of-addition experiments confirmed that MA affects a late event in the multiplication cycle of HSV-1. We showed that MA diminished the synthesis of viral DNA and inhibited the spread of infectious viral particles when HSV-1 that expresses beta-galactosidase activity was used. In addition, the lack of a protein with an apparent MW of 55 KD was detected in MA-treated cell extracts. Ultrastructural analysis of infected cells showed that, in the case of MA treatment, a large number of unenveloped nucleocapsids accumulated in the cytoplasm and a minor proportion of mature virus was found in cytoplasmic vesicles.These findings suggest that MA exerts an antiviral action on both the synthesis of viral DNA and the maturation and egress of HSV-1 during the infection of Vero cells.     

Therapeutic effect of meliacine,an antiviral derived from Melia azedarach L., in mice genital herpetic infection

Since natural products are considered powerful sources of novel drug discovery, a partially purified extract (meliacine) from the leaves of Melia azedarach L., a plant used in traditional medicine in India for the treatment of several diseases, has been studied. Meliacine exhibits a potent antiviral effect against several viruses without displaying cytotoxicity. The purpose of the present study was to evaluate the therapeutic effect of intravaginal administration of meliacine in a mouse model of genital herpetic infection. BALB/c female mice were infected with MS or G strains of Herpes Simplex Virus type 2 and then treated with meliacine topically. An overall protective effect was observed. Animal survival increased, the severity of the disease was reduced, life span was extended and virus shedding in vagina fluids was diminished. In addition, meliacine reduced the amount of virus that migrated to the brain and vaginal fluids presented higher levels of IFN‐γ and TNF‐α than untreated infected mice. These results indicate that meliacine could be an alternative therapeutic compound against HSV‐2 genital infection. Copyright © 2009 John Wiley & Sons, Ltd.     

苦楝皮化学成分研究

目的:研究苦楝皮Melia azedarach L.的化学成分。方法:采用硅胶柱色谱技术分离纯化,通过光谱学方法鉴定化合物的结构。结果:分离并鉴定出7个化合物,分别为4,8-二羟基-1-四氢萘醌(isosclerone,Ⅰ),梣酮(fraxinellone,Ⅱ),苦楝皮萜酮(kulinone,Ⅲ),苦楝萜酮内酯(kulactone,Ⅳ),南岭楝酮B(dubione B,Ⅴ),苦楝酸(kulonic acid,Ⅵ)和β-谷甾醇(β-sitosterol,Ⅶ),丁二酸(succinic,Ⅷ),5-(羟甲基)-2-呋喃甲醛[5-(hydroxymethyl)-2-furaldehyde,Ⅸ]。结论:化合物Ⅰ,Ⅷ和Ⅸ系首次从该植物中分得。     

川楝子的化学成分研究

 目的研究川楝子的化学成分。方法采用硅胶、凝胶柱色谱等方法对川楝子的化学成分进行分离,运用波谱分析技术和理化常数对照等方法对化合物结构进行鉴定。结果分离鉴定了16个化合物,分别鉴定为表松脂醇(1),clema-phenol A(2),medioresinol(3),(±)balanophonin(4),evofolin-B(5),槲皮素(6),异槲皮苷(7),芦丁(8),阿魏酸(9),对羟基苯甲醛(10),松柏醛(11),丁香酸(12),异香草酸(13),对羟基苯甲酸(14),5-羟甲基糠醛(15)和cirsiumaldehyde(16)。结论化合物6为首次从川楝子中分离得到,其余化合物均为首次从楝属植物中分离得到。     

In vitro antimicrobial efficacy of leaf essential oils of Chukrasia tabularis Adr Juss and Melia dubia Cav (Meliaceae)

The essential oils of Chukrasia tabularis and Melia dubia were tested for their antimicrobial activity against ten different pathogenic microorganisms responsible for human pathologies using standard antimicrobial assays. Chukrasia tabularis leaf oil exhibited strong antibiotic activities against Proteus vulgaris and Fusarium oxysporum and did not show any activity against the tested bacteria. Melia dubia leaf essential oil exhibited bacteriostatic and fungistatic activities against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Fusarium oxysporum and Candida albicans respectively. The inhibitory activities of both essential oils are comparable with that of respective standards.     

构树皮中的酚性化合物研究

目的:研究构树皮的酚性化学成分。方法:通过硅胶柱层析、ODS柱、Sephadex LH-20等色谱技术对构树皮的化学成分进行分离纯化,并根据理化性质与波谱数据对化合物进行结构鉴定。结果:从构树皮中分离鉴定了11个酚性化合物,分别为:松脂素-4'-O-β-D-吡喃葡萄糖苷(1)、黑立脂素苷(2)、松脂素-4'-O-β-D-吡喃葡糖基-4″-O-β-D-呋喃芹菜苷(3)、di-O-methylcrenatin(4)、leonuriside A(5)、3,4,5-三甲氧基苯基-β-D-吡喃葡萄糖苷(6)、kelampayoside A(7)、咖啡酸甲酯(8)、槲皮素(9)、槲皮素-3-O-α-L-吡喃鼠李糖苷(10)、对羟基苯甲酸-β-D-吡喃葡萄糖酯苷(11)。结论:其中,化合物4~8、10、11为首次从该植物中分离得到。