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1.
目的 探讨固公果根提取物促进结肠癌细胞凋亡及机制研究。方法 分别采用MTT法、DAPI染色及流式细胞术检测固公果根提取物对结肠癌细胞增殖活性及细胞凋亡的影响;蛋白免疫印迹(Western-Blot)法检测凋亡相关蛋白的活性表达水平。结果 固公果根提取物能显著抑制结肠癌SW620和LOVO细胞增殖,促进两种结肠癌细胞凋亡,上调凋亡相关基因Keap-1、Bax的蛋白表达,下调Nrf2、HO-1以及Bcl2蛋白的表达。结论 固公果根提取物能显著抑制人结肠癌细胞SW620和LOVO增殖、诱导细胞凋亡,其作用机制可能涉及调控凋亡相关基因Bax、Bcl-2表达,且与激活Nrf2氧化应激通路有关。  相似文献   

2.
The bewildering complexity of the relationship between genotype and phenotype in human mitochondrial diseases has delayed an understanding of the related cytopathological mechanisms. To explore the relationship between mitochondrial dysfunction in Dictyostelium discoideum and the related cytopathologies, we determined whether the phenotypic outcomes were similar regardless of which D. discoideum mitochondrial gene was targeted for disruption. The disruption of the mitochondrial genes resulted in a similar pattern of phenotypes to those caused by other mitochondrial defects. These include impairment of phototaxis, multicellular development and growth on plates and in liquid medium. As the reduced growth rates could have been due to defective phagocytic or macropinocytic nutrient uptake, these processes were tested but found to be unaffected. Since mitochondria have been associated with Legionella pathogenesis of human macrophages, it was also determined if mitochondrially diseased Dictyostelium strains were better or worse than healthy cells at supporting the growth of Legionella pneumophila. The results revealed that the mitochondrially diseased strains supported greater L. pneumophila growth than the wild type Dictyostelium strain (AX2). Quantitative Northern blotting showed a significant reduction in the level of expression of the entire mitochondrial genome, regardless of which mitochondrial gene was targeted for disruption, suggesting a generalized deficiency in mitochondrial gene expression and function. The phenotypic outcomes were the same as those shown previously to result from chronic hyperactivity of the energy-sensing protein kinase, AMPK, after knockdown of mitochondrial chaperonin 60.  相似文献   

3.
目的 研究冬虫夏草菌丝体水提醇沉物的体外抗肿瘤活性及其机制。方法 采用热水浸提-醇沉法得到水提物,高效液相色谱仪测定水提醇沉物中腺苷的量;采用MTT法测定其抗肿瘤活性,利用流式细胞仪结合碘化丙锭染色法检测其对细胞周期的抑制。结果 实验表明水提醇沉物能抑制人肝癌HepG2细胞株及大细胞肺癌NCI-H460细胞株的增殖,并呈浓度相关性;半数抑制浓度(IC50)值分别为(1.49±0.19)和(1.67±0.27)mg/mL。细胞周期分析表明,水提醇沉物分别阻滞HepG2及NCI-H460细胞周期于G2/M期、S期,并可诱导上述两种细胞发生凋亡。结论 冬虫夏草水提醇沉物通过阻滞HepG2及NCI-H460细胞周期循环,诱导其凋亡,从而表现出良好的增殖抑制活性。为深入研究冬虫夏草菌丝体水提醇沉物抗肿瘤的机制提供了实验证据。  相似文献   

4.
目的 研究桦褐孔菌Inonotus obliquus水提物的毒理学性质,探究其是否具有相关生理和生殖毒性。方法 急性毒性试验,ICR小鼠,一次ig给予桦褐孔菌水提物1.00、2.00、3.00、4.00、5.00 g/kg,连续观察14 d。30 d喂养试验,Wistar大鼠,每次ig给予桦褐孔菌水提物1.50、2.00、2.50 g/kg,连续给药30 d。小鼠精子畸形试验,ICR雄性小鼠,每次ig给予桦褐孔菌水提物1.00、2.50、5.00 g/kg,连续给药5 d,给药后第35天颈椎脱臼法处死实验小鼠,取双侧附睾制片,染色,统计精子畸形率。结果 急性毒性试验,实验组小鼠给药30 min后,静伏少动,背毛竖立,出现腹泻症状,无动物死亡,实验动物24 h后恢复正常。30 d喂养试验,受试动物体质量和食物利用率与对照组相比差异不显著。脏器系数、血常规和血液生化相关指标也在正常范围内波动。病理学检查未发现组织器官的明显病变。小鼠精子畸形试验,所有实验组的精子畸形率均显著低于环磷酰胺处理的阳性对照组,桦褐孔菌水提物5.00 g/kg组小鼠精子畸形率较对照组有上升趋势。结论 桦褐孔菌水提物未表现出明显的生理毒性,但在高剂量时可能具有一定的生殖毒性。  相似文献   

5.
The effect of triethyllead (TriEL) on motile activity, structure of cytoskeleton and chemotaxis of Dictyostelium discoideum amoebae in developing concentration gradients of folic acid (FA) and cAMP has been studied. It was observed that 3 μM TriEL had little or no effect on locomotion and chemotactic response of cells, whereas 5 μM TriEL strongly reduced the motile activity of Dictyostelium discoideum amoebae and inhibited their chemotaxis towards cAMP, but not towards FA. FA was found to restore the motile activity of Dictyostelium discoideum, inhibited by TriEL. A similar effect was observed in the presence of other antioxidants, i.e. ascorbic acid and sodium selenite, suggesting that oxidative stress may be involved in the action of TriEL. Moreover, the treatment of Dictyostelium amoebae with 5 μM TriEL caused disruption of microtubules while 3 μM TriEL had little effect on their structure. FA caused restoration of microtubules only in some cells within 1 h of incubation, i.e. when the directional movement of cells towards this chemoattractant was already observed. However, their organization was significantly different from that observed in the untreated cells, suggesting that microtubule undisturbed organisation may be not necessary for Dictyostelium discoideum amoebae locomotion and chemotaxis  相似文献   

6.
目的 建立荜茇提取物中5个生物碱含量测定方法,并评估该提取物对垂体后叶素所致大鼠实验性心肌缺血的影响。方法 采用HPLC法同时测定5个生物碱的含量;采用经舌下静脉注射垂体后叶素造成急性心肌缺血模型,以造模前后T波变化绝对值、心率及其变化百分率为观测指标,评估荜茇提取物大、中、小三个剂量组对大鼠实验性心肌缺血的影响。结果 3批荜茇提取物中胡椒碱平均含量为56.1%、49.7%、51.6%;N-异丁基-2E,4E-十八烷二烯酰胺平均含量为4.48%、4.21%、4.28%;几内亚胡椒碱平均含量为0.461%、0.378%、0.396%;荜茇明碱平均含量为1.73%、1.67%、1.70%;胡椒酰胺平均含量为0.554%、0.461%、0.493%。荜茇提取物大、中、小剂量组均有降低T波变化绝对值的作用;除大剂量组在个别时间点有降低心率的作用之外,其它各实验组在各时间点对心率变化率无显著影响。结论 所建立的生物碱含量测定分析方法可准确测定荜茇提取物中5个生物碱的含量;药效试验证明荜茇提取物具有较好的抗心肌缺血活性。  相似文献   

7.
目的 氮素是中药材有效成分积累的重要影响元素,为探讨不同氮源对丹参Salvia miltiorrhiza和藏丹参Salvia castanea毛状根生长和活性成分积累的影响。方法 分别采用硝酸铵、水解乳蛋白、蛋白胨、牛肉浸膏、酪蛋白和酵母提取物6种氮源处理对丹参和藏丹参毛状根的影响,分析毛状根生长及活性成分积累的变化。结果 硝酸铵最有利于2种丹参毛状根的生长。水解乳蛋白能够显著促进丹酚酸类成分的积累,与硝酸铵对照相比,丹参迷迭香酸和丹酚酸B含量分别提高了2.94倍和3.27倍,藏丹参二者含量分别提高了13.74倍和2.01倍。酵母提取物对2种丹参毛状根二氢丹参酮Ι和隐丹参酮积累的促进效果最为显著,水解乳蛋白能显著促进丹参根中丹参酮IIA的积累,牛肉浸膏则对藏丹参中丹参酮IIA积累的促进作用最为显著。结论 硝酸铵是2种丹参毛状根生长的最佳氮源,水解乳蛋白是丹酚酸积累的最佳氮源,不同氮源对4种丹参酮的影响不一致,丹参和藏丹参对不同氮源的响应也不一致。该研究不仅对丹参毛状根规模化培养及活性成分工业化生产具有一定指导意义,也对藏丹参资源的开发利用提供了借鉴作用。  相似文献   

8.
目的 比较长花滇紫草和团花滇紫草75%乙醇提取物的体外抗氧化及抗菌活性。方法 采用ABTS法、FRAP法、邻苯三酚自氧化法测定体外抗氧化能力,并采用肉汤连续稀释法初步考察了2种藏紫草体提取物体外对15种不同菌株的抗菌作用。结果 不同浓度藏紫草的75%乙醇提取物对ABTS自由基和超氧阴离子都有较强的清除能力,与BHT阳性药相当或略高于BHT;总还原力随取物浓度增加而增强;2种藏紫草的提取物对革兰阳性菌有一定的抗菌活性,但对肠杆菌科菌株及铜绿假单胞菌均未见抗菌作用。结论 2种来源的藏紫草均具有一定的体外抗氧化和抗菌作用。  相似文献   

9.
李攀  韩佳  张世鹏  张帆 《药学研究》2018,37(10):562-564
目的 比较同源饮片川乌、黑附片、白附片与天雄之间急性毒性及其所引发毒性表现的差异性。方法 采用急毒实验方法测定小鼠灌胃生川乌和黑附片提取物的半数致死量(LD50)和天雄提取物的药物最大耐受量(MTD),同时对白附片提取物做限度实验并观察小鼠毒性表现。结果 生川乌和黑附片半数致死量测定结果分别为4.55 g饮片/kg和78.71 g饮片/kg;天雄药物最大耐受量测定结果为34.19 g饮片/kg;白附片提取物以5 g·kg-1的剂量灌胃小鼠,引起严重毒性反应,但不能引起小鼠死亡。4种饮片引起的毒性表现十分相似,可能累及神经、呼吸和循环等多个系统,不同的是除白附片外,其他3种饮片均可使小鼠发生眼球突出、惊厥甚至死亡反应。结论 4种饮片的急性毒性由大到小依次为生川乌、黑附片、天雄和白附片。虽然其引发的毒性表现十分类似,但是在严重程度上略有差异。  相似文献   

10.
Purpose. The intestinal epithelial cell line Caco-2 possesses the H+/ dipeptide cotransport system responsible for uptake of oral cephalosporins. In this study, the transport characteristics of ceftibuten were examined from the viewpoint of cell growth in the Caco-2 cells. Methods. The uptake of cephalosporins by Caco-2 cell monolayers grown on plastic dishes was measured and analyzed kinetically. Results. The uptake of ceftibuten was increased by lowering pH of the incubation medium and was inhibited by excess dipeptide. The transport activity of ceftibuten was dependent on the duration of culture, being maximal on the 14th day after inoculation. Kinetic analysis revealed that the development of ceftibuten uptake was due to not only a decrease in Km but also to an increase in Vmax value. Conclusions. The uptake of ceftibuten is mediated by the apical H+/ dipeptide cotransport system which is regulated by cell growth and/or differentiation in the Caco-2 cells.  相似文献   

11.
目的 观察、追踪毛冬青抑制口腔常见致龋菌(变形链球菌和具核梭杆菌)的有效部位和成分。方法 通过系统溶剂萃取、大孔树脂及硅胶柱色谱分离等方法以及质谱和核磁共振等鉴定技术,结合液体二倍稀释法,研究毛冬青不同部位及单体对变形链球菌和具核梭杆菌的最低抑菌浓度(MIC),1%玉洁纯作为阳性对照药。结果 毛冬青三萜总皂苷和冬青素对两种主要口腔致病菌均具有一定的抑制作用,特别对变形链球菌具有显著地抑制效果。结论 毛冬青三萜总皂苷和冬青素对变形链球菌具有很强的抑制作用,具有开发成为抗龋齿的保健牙膏或药品的潜力。  相似文献   

12.
目的 评价50种中药甲醇提取物对嗜水气单胞菌的体外抑菌效果以及抗生物膜生成活性。方法 采取甲醇浸提的方法制备中药甲醇提取物,计算提取率;利用多功能酶标仪检测600nm处的吸光度(A600)值测定各提取物(0.1、0.2、0.4、0.8、1.6、3.2mg·mL-1)作用16h对嗜水气单胞菌的抑菌率;结晶紫染色法结合多功能酶标仪测定各提取物的抗生物膜活性。结果 苏木、白芍、侧柏叶等32种中药甲醇提取物对嗜水气单胞菌抑菌效果明显,其中苏木甲醇提取物的抑菌效果最显著,最大抑菌率达95.56%,起效质量浓度为0.1mg·mL-1;石菖蒲、大青叶、广藿香等20种中药甲醇提取物明显抑制嗜水气单胞菌生物被膜的生成,其中白芍的最大抑制率达96.78%。结论 夏枯草、野菊花、大青叶、赤芍、石菖蒲、地肤子、连翘、苏木、肉桂、女贞子、白芍、甘草、肉豆蔻、鸡血藤、乌药、莪术、侧柏叶17种中药对嗜水气单胞菌同时具有抑菌和抑制生物膜生长活性。  相似文献   

13.
目的 对木香茎叶提取物化学成分进行初步检识,研究其对小鼠肠推进和胃排空的影响。方法 制备木香茎叶水、乙醇、乙醚提取物,化学反应检识木香茎叶化学成分;以小鼠为研究对象,新斯的明和阿托品诱导小鼠胃肠亢进和抑制状态,ig给予0.5 g/kg木香茎叶水提物、醇提物,用改良的酚红法测定其对胃肠正常、亢进、抑制状态小鼠胃排空率和小肠推进率的影响。结果 木香茎叶醇提物、水提物均能够显著提高正常小鼠小肠酚红推进率(P<0.05、0.01),显著降低新斯的明所致胃肠亢进状态下的小鼠小肠酚红推进率(P<0.05),且醇提物的作用较强;两提取物使阿托品所致抑制状态下小鼠小肠推进率进一步降低,且差异显著(P<0.05),两提取物之间无明显差异;两种提取物对三种状态下的胃排空都发挥显著抑制作用(P<0.05、0.01)。化学成分检识表明,木香茎叶中含蛋白、糖、挥发油、黄酮、内酯、皂苷、生物碱和鞣质等多种成分,但何种成分与小肠推进和胃排空有关尚不确定。结论 木香茎叶提取物对正常小鼠的小肠推进功能具有一定的促进作用,对新斯的明所致小肠推进亢进有抑制作用,对阿托品所致小肠推进抑制有加剧作用,其对肠道的促进作用可能与M胆碱受体有关;对正常和亢进小鼠的胃排空有抑制作用,对阿托品所致胃排空抑制有加剧作用。  相似文献   

14.
Abstract

Bisphosphonates effectively inhibit osteoclastic bone resorption in diseases characterized by excessive bone loss. Liposome-encapsulated clodronate (dichloromethylene bisphosphonate) also is known to inactivate phagocytic cells in vivo, and inhibit the growth of macrophage-like RAW 264 cells in vitro. The macrophage suppressive effect of liposomal clodronate is of interest in autoimmune diseases, like rheumatoid arthritis, in which phagocytic cells are involved in inflammatory processes. Earlier in vivo studies suggested that liposomal clodronate is a far more potent inactivator of macrophages than liposomal forms of two other bisphosphonate compounds, pamidronate (3-amino-l-hydroxypropylidene bisphosphonate), and etidronate (l-hydroxyethylidene-l, l-bisphosphonate). We examined the growth inhibitory properties of these three bisphosphonates with macrophage-like RAW 264 cells and with other types of cells in vitro. All three bisphosphonates encapsulated in liposomes effectively inhibited the growth of RAW 264 and CV1-P cells, while free drugs were 20-1000 times less potent growth inhibitors. Also, high extracellular calcium concentrations enhanced the potency of bisphosphonates for RAW 264 cells, indicating that, in addition to liposomes, the uptake of bisphosphonates by macrophages is mediated also by calcium. In all formulations, pamidronate was the most potent compound for the cells, with the exception of CV1-P cells, for which liposomal clodronate was the most potent. The effects of liposomal drugs were selective for highly endocytotic cells. The results suggest that liposome-encapsulated bisphosphonates could provide a specific tool to affect the function of macrophages and all three of these bisphosphonates are potentially effective as macrophage suppressors in autoimmune diseases.  相似文献   

15.
目的 比较大黄不同萃取物对成年雌性大鼠体质量及下丘脑、垂体结构的影响,进而筛选大黄生殖毒性主要萃取物。方法 采用极性梯度萃取法制备大黄水提物、氯仿萃取物、醋酸乙酯萃取物、正丁醇萃取物和水溶物,雌性成年大鼠随机分为对照组、大黄水提物组和各萃取物组,各组给药剂量均相当于大黄生药4.00 g/kg,连续ig给药60 d;计算大鼠给药前后体质量增长率;光镜下观察大鼠下丘脑弓状核神经元和垂体促性腺细胞病理学变化。结果 大黄水提物组大鼠体质量增长率低于对照组(P<0.05),其余各萃取物组明显高于对照组(P<0.01);大黄水提物组大鼠下丘脑弓状核神经元出现染色质边际化,核膜界限不清,胞浆尼氏体溶解,也可见鬼影细胞,腺垂体细胞整体数目减少,细胞排列欠规则,细胞间窦状毛细血管增多,其余各萃取物组下丘脑弓状核和腺垂体未见明显病变。结论 长期大剂量ig大黄水提物可使大鼠体质量增长率降低,导致下丘脑弓状核和腺垂体发生形态学病理变化;其余各萃取物却使大鼠体质量增长率明显升高,且对下丘脑弓状核和腺垂体的组织结构影响不大。  相似文献   

16.
目的 建立常山胡柚皮黄酮类成分的指纹图谱,并对指纹图谱特征指纹峰成分与其抗氧化活性进行相关性分析。方法 采用高效液相色谱法建立常山胡柚皮黄酮类成分的指纹图谱,采用DPPH清除氧自由基能力进行体外抗氧化活性研究,对指纹图谱中的特征指纹峰成分含量及其抗氧化活性进行多元线性回归分析,初步推断指纹图谱与抗氧化活性的谱效相关性。结果 胡柚皮提取物总黄酮成分、指纹图谱特征指纹峰成分(柚皮苷与新橙皮苷)的含量与其抗氧化活性之间存在显著的线性关系。胡柚皮提取物中柚皮苷含量与其DPPH自由基的清除率呈正相关(P<0.01),而新橙皮苷含量与其DPPH自由基的清除率略呈正相关(P<0.05)。结论 柚皮苷和新橙皮苷等黄酮类化合物可能是常山胡柚皮抗氧化作用的主要物质基础。  相似文献   

17.
Abstract

Extracts from Pittocaulon. spp. (Asteraceae) have been used in folk medicine to treat many ailments, particularly as anti-inflammatory and antimicrobial. Neither the bioactive components responsible nor the mechanisms involved have been evaluated. Here we report the antibacterial activities of their methanol and CH2Cl2 extracts and the effects on some fungal strains treated with CH2Cl2 extracts from root, stems, and flowers of P. praecox. (Cav.) H. Rob. & Brett., P. hintonii. H. Rob. & Brett., P. filare. (McVaugh) H. Rob. & Brett, P. velatum. (Greenm) H. Rob. & Brett., and P. bombycophole. (Bullock) H. Rob. & Brett. Thirteen extracts were obtained with MeOH and CH2Cl2 solvents from aerial parts and roots of five Pittocaulon. spp. for the first time in this species, and their antimicrobial activities were determined. The antimicrobial activities of these extracts were evaluated against the bacteria Staphylococcus aureus., Staphylococcus epidermidis., Bacillus subtilis., and Vibrio cholerae. (one El Tor strain, and a clinic case CDC-V12). Additionally, the CH2Cl2 extract was evaluated against Aspergillus niger., Fusarium moniliforme., Fusarium sporotrichum., Rizoctonia solanii., and Trichophyton mentagrophytes.. The most sensitive bacteria against these extracts were B. subtilis., S. epidermidis., and V. cholerae., a key bacterium in contaminated water. However, CH2Cl2 extracts from P. praecox., P. bombycophole., and P. hintonii. exhibited a significant antifungal activity against the fungal strains F. sporotrichum., R. solanii., and T. mentagrophytes.: at 1000 μg per disk, these extracts completely inhibited the mycelial growth of these fungi.  相似文献   

18.
Watanabe  Jim  Haba  Masami  Yuasa  Hiroaki 《Pharmaceutical research》1995,12(7):1092-1095
Purpose and Methods. The uptake of fractionated 3H-heparin by isolated rat Kupffer cells was examined to determine the uptake mechanism. Results. The association of fractionated 3H-heparin was concentration-dependent with a dissociation constant of 3.4 nM and a maximum association capacity of 1.3 pmol/106 cells, suggesting the involvement of a specialized mechanism. Although 2,4-dinitrophenol inhibited neither the association nor internalization of fractionated 3H-heparin, lowering the temperature from 37°C to 4°C reduced the internalization of fractionated 3H-heparin by 70% without affecting the association. Conclusions. It is suggested that the uptake mechanism may differ from receptor-mediated endocytosis of polypeptides and be mediated by scavenger receptors, because organic anions, and several ligands of scavenger receptors, as well as several heparin analogs, inhibit the binding of fractionated 3H-heparin to Kupffer cells, while phenylarsine oxide, which is known to inhibit the receptor-mediated or absorptive endocytosis of polypeptides, inhibits neither the association nor internalization of fractionated 3H-heparin.  相似文献   

19.
青蒿鞣质抗单纯疱疹病毒机理初探   总被引:4,自引:0,他引:4       下载免费PDF全文
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。  相似文献   

20.
目的 研究青天葵甲醇提取物(Nervilia fordii methanol extracts,NFME)体外对鼻咽癌CNE-2细胞的凋亡作用及其作用机制。方法 MTT法检测不同浓度(0,0.25,0.5,1,2,3 mg·mL-1)的NFME处理CNE-2细胞24,48 h对CNE-2细胞生长抑制率的影响;克隆原形成试验观察NFME对CNE-2细胞克隆形成率的影响;Hoechst凋亡染色观察NFME对CNE-2细胞凋亡的影响;Western blotting测定NFME作用下caspase-3、ERK1/2和c-Raf蛋白磷酸化水平的变化。结果 MTT试验结果显示,与对照组相比,在给药24 h时0.5 mg·mL-1的NFME就能抑制CNE-2细胞的增殖(P<0.05),抑制率为12.64%。而在给药48 h时0.25 mg·mL-1的NFME就能抑制CNE-2细胞增殖(P<0.05),抑制率为22.43%;克隆原形成能力试验表明,0.25 mg·mL-1的NFME能够抑制CNE-2细胞集落的形成(P<0.05);Hoechst33258凋亡染色观察到0.25 mg·mL-1的NFME作用24 h能够观察到CNE-2细胞发生凋亡(P<0.05),凋亡率达到17.91%;Western blotting结果表明0.5 mg·mL-1的NFME能使CNE-2细胞中caspase-3发生剪切,随着给药浓度增加其剪切作用越明显(P<0.01),同时0.5 mg·mL-1的NFME能够降低CNE-2细胞中ERK1/2和c-Raf蛋白的磷酸化水平(P<0.05)。结论 青天葵甲醇提取物能抑制鼻咽癌CNE-2细胞的增殖并诱导其发生凋亡,其作用机制可能与抑制ERK信号通路有关。  相似文献   

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