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穿心莲内酯衍生物的合成及其抗炎免疫活性 总被引:2,自引:0,他引:2
目的合成穿心莲内酯衍生物,并进行抗炎免疫活性研究,比较不同结构穿心莲内酯衍生物的活性。方法以穿心莲内酯(A)为底物合成了14-去氧-11,12-二去氢穿心莲内酯(DDA)、14-去氧穿心莲内酯(DA)、异穿心莲内酯(IA)、穿心莲酸(AA)等穿心莲内酯衍生物。采用蛋清致大鼠足肿胀模型观察穿心莲内酯衍生物的抗炎活性,小鼠碳粒廓清实验观察其免疫活性。结果目标物结构经红外、质谱、核磁共振氢谱确证。穿心莲内酯衍生物A、DDA、DA、IA、AA均有较好的抗炎活性;A、DDA、DA、AA有显著的免疫抑制作用,而IA无免疫抑制作用。结论初步生物活性实验表明:穿心莲内酯类化合物的抗炎活性与双键的位置有关,具有环内双键的穿心莲内酯类化合物较具有环外双键的抗炎活性强,IA的四氢呋喃环可能增强抗炎作用;穿心莲内酯类化合物的免疫抑制作用与双键位置有一定关系,具有环外双键的较具有环内双键的免疫抑制作用强,IA无免疫抑制作用可能与其四氢呋喃环有关;A的五元内酯开环物AA的活性与母体相当,说明五元内酯环打开与否和抗炎免疫作用无关。 相似文献
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穿心莲内酯及其衍生物的药理活性研究进展 总被引:16,自引:0,他引:16
穿心莲内酯是中药穿心莲的主要有效成分之一。具有解热、抗炎、抗病毒、保肝利胆等作用,临床上主要用于治疗小儿肺炎,上呼吸道感染等疾病。随着对穿心莲内酯药理作用研究的不断深入,其临床应用得到不断拓展[1],并在免疫调节、抗肿瘤、抗糖尿病等方面展示了诱人的应用前景。本文重点综述近年来关于穿心莲内酯的抗炎、免疫调节、抗肿瘤、抗心血管疾病和抗消化系统疾病等机理方面的研究进展。1解热抗炎穿心莲内酯、脱氧穿心莲内酯(DA)、新穿心莲内酯(NA)和脱氧二脱氢穿心莲内酯(DDA)对2,4-二硝基酚或内毒素诱导的发热和蛋清诱导的水肿或巴豆… 相似文献
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穿心莲内酯的药理活性作用 总被引:13,自引:0,他引:13
穿心莲内酯为爵床科植物穿心莲中提取得到的二萜内酯类化合物,分子式为C20H30O5,是中药穿心莲的主要有效成分之一。现代药理研究表明穿心莲内酯具有抗菌、抗炎、抗病毒、免疫调节、治疗心脑血管疾病、保肝利胆等作用,并有毒性低、价格便宜的特点。最近研究报道穿心莲内酯对食道癌、前列腺癌、结肠癌和白血病等具有较好的抗肿瘤作用,有望成为一种新的抗癌药物。 相似文献
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穿心莲内酯抗肿瘤作用机制的研究进展 总被引:2,自引:1,他引:2
近年来,穿心莲内酯的研究日益受到重视,穿心莲内酯具有抗肿瘤、消炎抗菌、抗病毒感染等广泛药理作用。在抗肿瘤方面的研究发现穿心莲内酯具有抗胃癌、肝癌、肺癌、乳癌等多种肿瘤的作用。其抗肿瘤的机制可能与诱导肿瘤细胞的凋亡、抑制细胞周期、提高淋巴细胞抗肿瘤活性等方面有关。 相似文献
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Yu-Xia Wang Xiang-Xiang Gu Di Geng Hua-Ying Sun Chun-Mei Wang Gui-Xiang Jiang Xin-Nan Hou Chang-Hua Ma 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
Gecko, a kind of reptile, has been widely used as a traditional Chinese medicine to treat various diseases including cancer in China for thousands of years. The aim of this study was to investigate the anti-tumor effect of AG (aqueous extracts of fresh gecko) on human hepatocellular carcinoma cell Bel-7402 in vitro and mouse H22 hepatocellular in vivo. Further to underlie the molecular mechanism of AG inducing the differentiation of Bel-7402 cells.Materials and methods
AG was obtained by water extracting method and qualitatively analyzed through High Performance Liquid Chromatography. The total protein concentration of AG was measured by BCA (bicinchoninic acid disodium) assay. The anti-tumor activities in vivo were analyzed through H22 (mouse hepatocellular carcinoma cell line H22) tumor xenografts mice. The cytotoxic activity of AG on Bel-7402 cells was evaluated by MTT assays. AFP (alpha fetoprotein) was detected by radioimmunoassay. ALB (albumin), ALP (alkaline phosphatase) and γ-GT (γ-glutamyl transpeptidase) were detected by biochemical methods with commercial kits. While morphological changes were observed through an inverted microscope. Moreover, the expression level of the proteins involved in MAPK (mitogen-activated protein kinase) signal pathway which was closely related to cellular differentiation was assessed by Western blot.Results
AG showed obviously anti-tumor activity in vivo and anti-proliferative activity on Bel-7402 cells in vitro both dose-dependently. The number of clones of Bel-7402 cells treated with AG reduced and the cells were displaying differentiation state such as relatively bigger size and dispersed growth. The biochemical function markers of the cells were significantly changed after being treated with AG. The data showed that AFP secretion of the cells decreased 42.5%, ALB secretion increased 58.9%, the activity of ALP and γ-GT markedly decreased 67.0% and 48.5% separately when the concentration of AG was 10 μl/ml, and those effects were all in a dose-dependent manner. The major original and phosphorylated signal proteins (ERK1/2 (extracellular sigal-regualted kinase 1/2), P38 (p38 MAPK) and JNK1/2 (c-Jun N-terminal kinase 1/2)) involved in MAPK signal pathway were measured and the results showed that AG activated the ERK1/2 of Bel-7402 cells.Conclusions
AG has anti-tumor activity in vivo and inhibits Bel-7402 cell proliferation in vitro through inducing cell differentiation, and the mechanism involves the activation of ERK1/2. 相似文献13.
Iva Mucalo Elena Jovanovski Dario Rahelić Velimir Božikov Željko Romić Vladimir Vuksan 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Substantial pre-clinical and some clinical data are available showing that Asian ginseng (Panax ginseng C.A. Meyer) varieties or its particular ginsenosides exert a vasodilatating effect, thus may modulate vascular function. However, the clinical evidence for American ginseng (Panax quinquefolius L.) is scarce. Therefore, this study evaluates the effect of American ginseng (AG) on arterial stiffness, as measured by augmentation index (AI), and blood pressure (BP), in type 2 diabetes patients with concomitant hypertension.Materials and methods
Using a double-blind, placebo-controlled, parallel design, each participant was randomized to either the selected AG extract or placebo at daily dose of 3 g for 12 weeks as an adjunct to their usual antihypertensive and anti-diabetic therapy (diet and/or medications). AI and BP were measured by applanation tonometry at baseline and after 12 weeks of treatment.Results
A total of 64 individuals with well-controlled essential hypertension and type 2 diabetes (gender: 22 M:42 F, age:63±9.3 years, BP: 145±10.8/84±8.0 mmHg, HbA1c: 7.0±1.3%, fasting blood glucose (FBG): 8.1±2.3 mmol/L) completed the study. Compared to placebo, 3 g of AG significantly lowered radial AI by 5.3% (P=0.041) and systolic BP by 11.7% (P<0.001) at 12 weeks. No effect was observed with diastolic BP.Conclusions
Addition of AG extract to conventional therapy in diabetes with concomitant hypertension improved arterial stiffness and attenuated systolic BP, thus warrants further investigation on long-term endothelial parameters before recommended as an adjunct treatment. 相似文献14.
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Jun Jiang Jae-Jin Kim Dong-Young Kim Myong-Ki Kim Na-Hyun Oh Sushruta Koppula Pyo-Jam Park Dong-Kug Choi Yong-Kook Shin Ick-Hee Kim Tae-Bong Kang Kwang-Ho Lee 《Journal of ethnopharmacology》2012
Ethnopharmacological relevance
Acorus gramineus Solander (Acoraceae, AG), is a widely distributed plant in Asian countries. Rhizome part of this plant has long been used as a traditional medicine for treating various symptoms including central nervous system (CNS) disorders.Aim of study
The anti-neuroinflammatory effect of AG aqueous extract was investigated using in vitro cellular and in vivo Parkinson's disease (PD) mouse model.Materials and methods
Lipopolysaccharide (LPS) is used to stimulate BV-2 microglial cells in vitro and the changes in neuroinflammatory expressional levels were measured using ELISA, Western blotting, RT-PCR and immunofluorescence techniques. In in vivo experiments, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-intoxicated mouse model of PD was developed followed by immunohistochemical analysis of specific brain tissues.Results
LPS-stimulation to BV-2 cells increased the production of nitric oxide (NO) and proinflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-6 and IL-1β. Pretreatment with AG extract inhibited the increased levels of NO and pro-inflammatory cytokines in LPS-stimulated BV-2 cells. Mechanistic study revealed that AG acts via the regulation of nuclear factor kappa B (NF-κB), mitogen-activated protein kinases (MAPKs) and TRIF-dependent signaling pathways. Further, AG protected MPTP-induced neuronal cell death and inhibited neuroinflammation in vivo.Conclusion
Our results indicated that AG extract exerted anti-neuroinflammatory effects against activated microglia mediated insults through multiple signaling pathways and prevented in vivo neuronal cell death in mouse model of PD substantiating the traditional claims for its use in CNS disorders. 相似文献16.
随着真菌感染日渐增多,白念珠菌的防治成为当前抗真菌感染的重点。该研究拟探讨中药单体穿心莲内酯(AG)对白念珠菌生物膜分散的影响。实验以微孔板结合医用导管片构建白念珠菌生物膜模型,分别通过XTT减低法和平板法发现1 000,500,250 mg·L-1AG能不同程度的影响白念珠菌生物膜分散细胞的活性;以扫描电镜观察导管片残余生物膜形态结构,发现1 000,500,250 mg·L-1AG能剂量依赖性的诱导白念珠菌生物膜的分散,且分散出的细胞以酵母相为主;实时荧光定量PCR(qRT-PCR)法检测发现AG使HSP90表达上调,使UME6和PES1表达下调。该研究表明AG能一定程度的诱导白念珠菌生物膜分散。 相似文献
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鬼臼毒素及其衍生物新型制剂抗肿瘤作用研究进展 总被引:3,自引:3,他引:0
随着新辅料、新技术、新载体的不断涌现,鬼臼毒素及其衍生物的新剂型的研究呈现出广阔的前景.概述了鬼臼毒素在脂质体纳米粒、层状双氢氧物、聚合物胶束等新型载药系统中对多种肿瘤细胞的抗肿瘤作用;同时介绍了鬼臼毒素衍生物依托泊苷微球、口服微乳、纳米脂质体、β-环糊精包合物等新剂型在抗肿瘤研究中的靶向治疗、增加疏水性药物的溶解度、缓释作用方面的应用.随着鬼臼毒素及其衍生物的新型靶向制剂的进一步研究,可在降低毒副作用的同时增强其抗肿瘤作用,为合理开发鬼臼毒素及其衍生物的新剂型提供了研究基础. 相似文献
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LC Faccin-Galhardi KA Yamamoto S Ray B Ray RE Carvalho Linhares C Nozawa 《Journal of ethnopharmacology》2012,142(1):86-90
Ethnopharmacological relevance
Azadirachta indica A. Juss, popularly known as neem, has been extensively used in Ayurvedic medicine by Indian population for over 2000 years. It is used traditionally for the healing of various diseases. Natural products and their derivatives provide an excellent source for new anti-viral drugs.Aim of the study
The present study aims at evaluating the activity of two polysaccharides (P1 and P2) isolated from the leaves of Azadirachta indica and their chemical sulfated derivatives (P1S and P2S) against poliovirus type 1 (PV-1).Materials and methods
The cytotoxicity of the compounds was analyzed by MTT and the antiviral effect was determined by plaque reduction assay in different protocols.Results
The polysaccharides did not show any cytotoxic effects on HEp-2 cells at the highest tested concentration (200 μg/ml) and exhibited significant antiviral activity with inhibitory concentrations (IC50) of 80 μg/ml, 37.5 μg/ml, 77.5 μg/ml, and 12.1 μg/ml for P1, P1S, P2 and P2S, respectively, and the selectivity indexes (SI) ranged from 18 to 131.9. The compounds demonstrated better inhibitory effect when added concomitantly with the virus infection with a dose-dependent curve inhibition. Lesser effect was observed when the compounds were added after viral infection and the least effect at pre-treatment.Conclusions
We suggested that the polysaccharides obtained from Azadirachta indica act against PV-1 by inhibiting the initial stage of viral replication. Importantly, original polysaccharides showed better virucidal effect than their sulfated derivatives at all tested concentrations. This study provides a scientific basis for the past and present ethnomedical uses of this plant. 相似文献19.
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穿心莲内酯对表皮葡萄球菌生物被膜作用初探 总被引:4,自引:2,他引:2
目的:通过穿心莲内酯对表皮葡萄球菌生物被膜抑制作用的研究,为表皮葡萄球菌生物被膜菌引起的相关感染提供新的治疗途径。方法:体外构建表皮葡萄球菌生物被膜,以红霉素作为阳性对照药,利用XTT减低法评价穿心莲内酯对表皮葡萄球菌初始黏附及生物被膜内细菌代谢的影响,显微镜下观察该药对表皮葡萄球菌生物被膜的形态学影响,刚果红培养基法检测穿心莲内酯对PIA(polysacchatide interc-ellular adhesion,胞间多糖黏附素)形成的影响。结果:穿心莲内酯1 000,100,10 mg.L-1对表皮葡萄球菌的黏附均有抑制作用,质量浓度大于31.25 mg.L-1对生物被膜内细菌代谢有明显抑制作用,质量浓度为250 mg.L-1时对表皮葡萄球菌生物被膜的形态有显著影响,质量浓度为10 mg.L-1时对PIA的形成无影响。结论:穿心莲内酯对表皮葡萄球菌生物被膜的形成有显著抑制作用,但效果不及红霉素。 相似文献