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1.
目的:解释显脉香茶菜素和毛叶香茶菜二萜的抗癌活性差别。方法:用MNDO的计算方法对显脉香茶菜素和毛叶香茶二萜的结构进行优化处理,计算结构参数和电子参数。结果:计算表明,显脉香茶菜素存在一个抗癌活性区,此区的活性明显高于毛叶香茶二萜的相应结构区。结论:量化计算较好地解释了显脉香茶菜素具有抗癌活性,而毛叶香茶二萜几乎没有抗癌活性。  相似文献   

2.
T.Fujita等最近从长管香茶菜[Rab-dosia longituba(Miguel)Hara]的叶中分离出两个抗癌活性的新二萜:长管香茶菜素A和B(longikaurin A和B),并测定了结构。本文继续报导从该植物中分得的四个抗菌活性的新二萜——长管香茶菜素C、D、E和F。这四个化合物对Subutilis ATCC6633杆菌的最小抑菌浓度分别为15.6,62.5  相似文献   

3.
通过对香茶菜属植物的两种二萜成分——香茶菜甲素、大叶香茶菜丙进行结构改造,观察它们的生物活性。结果表明,香茶菜甲素酰化物(Ⅱ)能显著提高抗菌作用,比原化合物提高2~3倍;大叶香茶菜丙水解物(Ⅴ)能显著提高细胞毒活性,比原化合物提高2.3倍。  相似文献   

4.
自毛叶香茶菜Rabdosia japonica(Burm.f)Hara的干叶中分离出四个二萜化合物,其中两个是新的二萜,命名为毛叶香茶菜素A和B。通过光谱分析和化学反应转变成已知化合物epinodosin 6和isodonal 8确定了毛叶香茶菜素A和B的结构分别为3和7。初步的抗癌试验表明,3和7都具有明显细胞毒作用。其它两个二萜成分证明为enmenol 4和epinodosinol 5。  相似文献   

5.
目的 探究尾叶香茶菜丙素(Kamebakaurin)对HepG2/ADM(肝癌细胞耐阿霉素耐药株)细胞体外活性.方法 通过2-(2-甲氧基-4-硝基苯基)-3-(4-硝基苯基)-5-(2,4-二磺酸苯)-2H-四唑单钠盐(CCK-8法)测定尾叶香茶菜丙素和阿霉素(ADM)对HepG2/ADM细胞的生长活力抑制率;通过流式细胞术测定尾叶香茶菜丙素对细胞周期和细胞凋亡的影响;运用Transwell小室实验和划痕愈合实验检验尾叶香茶菜丙素对HepG2/ADM细胞迁移能力影响,用实时荧光定量PCR检测耐药相关基因表达,通过蛋白印迹法(Western blotting)分析PTEN-AKT信号通路.结果 尾叶香茶菜丙素对HepG2/ADM细胞的IC50值为62.96μmol/L,ADM在1 mg/mL(184μmol/L)只有26.5%抑制率,说明HepG2/ADM细胞耐药株对尾叶香茶菜丙素敏感度高于阿霉素;尾叶香茶菜丙素诱导肝癌细胞HepG2/ADM细胞的凋亡,阻滞细胞在G2期,且呈浓度依赖性;尾叶香茶菜丙素具有抑制HepG2/ADM细胞穿过小室的能力和平板愈合能力,显示尾叶香茶菜丙素可抑制其迁移能力;Western blotting显示尾叶香茶菜丙素通过抑制MDR1和PENT-AKT通路发挥以上功能.结论 尾叶香茶菜丙素抑制MDR1蛋白表达从而逆转HepG2/ADM细胞对药物的敏感性,通过抑制PENT-AKT通路的激活从而促进HepG2/ADM细胞的凋亡并抑制其迁移能力.  相似文献   

6.
目的为开发香茶菜药材资源提供依据.方法通过茎叶与根茎的性状、薄层色谱试验及熊果酸含量的测定,对香茶菜和大萼香茶菜进行比较.结果香茶菜和大萼香茶菜成分相似,茎叶与根茎的主要成分相同.结论香茶菜和大萼香茶菜可以考虑同等应用.  相似文献   

7.
香茶菜抗癌成分的研究   总被引:9,自引:0,他引:9  
从香茶菜属植物香茶菜Rabdosia amethystoides(Benth) Hara中分得七种成分,其中之一香茶菜甲素为一新的四环二萜,有抗实验肿瘤及抑制金黄色葡萄球菌作用。用光谱法配合衍生物制备,确定甲素为7α,14β=羟基-20α羟甲基-16-贝壳杉烯-11,15=酮乙素为乌苏酸,丙素为β-谷甾醇,己素为硬脂酸,其余成分尚在研究中。  相似文献   

8.
柄叶香茶菜及其甲素体外抑菌的研究杨一兵(湖南省凤凰县人民医院,凤凰416200)朱大元(中科院上海药物研究所,上海200031)唇形科香茶莱属植物中的二萜成分有抗菌消炎、抗肿瘤、抗真菌、抗溃疡、昆虫拒食等活性。国内目前上市的商品约有2~3种如复方冬凌...  相似文献   

9.
从大叶香茶菜Rabdosia macrophylla(Migo)C.W.Wu et H.W.Li干叶中提取、分离得十五种成分,其中数种为具有抗肿瘤或细胞毒活性的二萜。本文报道另一种新二萜成分大叶香茶菜辛素(rabdophyllin H)的结构,并由X线单晶衍射方法证实。大叶香茶菜辛素对QGY-7703肝癌细胞具有抑制作用。  相似文献   

10.
目的为开发香茶菜药材资源提供依据。方法通过茎叶与根茎的性状、薄层色谱试验及熊果酸含量的测定,对香茶菜和大萼香茶菜进行比较。结果香茶菜和大萼香茶菜成分相似,茎叶与根茎的主要成分相同。结论香茶菜和大萼香茶菜可以考虑同等应用。  相似文献   

11.
A spirosecokaurenoid, angustifolin (Ⅰ) was isolated from the leaves of Rabdosia angustifolia (Dunn) Hara (Labiatae) and its structure was established from spectral and chemical evidence. One known diterpenoid, isodonal (V) was also isolated together with β-sitosterol. (Ⅰ) and (Ⅴ) showed in vitro cytotoxicity and in vivo tumor inhibitory activities.  相似文献   

12.
13.
冬凌草甲素为贝壳杉烯型二萜类化合物,具有良好的体外抗肿瘤活性,虽然体外活性强,但由于水溶性差、生物利用度低、口服难以吸收等缺点,极大地限制了其临床应用。为了寻找具有更高活性和更好生物利用度的化合物,以开发新的抗肿瘤药物,综述研究者对冬凌草甲素进行的结构改造和修饰的进展。  相似文献   

14.
The Chinese herbal medicine oridonin has potent anti-inflammatory and antitumor activities. In addition, oridonin treatment effectively suppresses breast cancer growth. However, the underlying mechanisms are poorly defined. Here, we reported that oridonin decreased Treg differentiation in vitro and in vivo. Oridonin inhibition of Treg differentiation was dependent on decreasing TGF-β receptor expression. Oridonin attenuated Tregs’ immunosuppressive ability; thus, oridonin did not inhibit CD8+ T cell proliferation very well in vitro. Oridonin greatly delayed the progression of 4T1 tumors in vivo. In addition, oridonin combined with anti-PD-1 activated a robust antitumor immune response and suppressed 4T1 tumor growth. Therefore, our results indicate that oridonin inhibits TNBC growth by modulating Treg differentiation, which provides new directions for the clinical treatment of TNBC.  相似文献   

15.
瘿花香茶菜二萜成分的研究   总被引:2,自引:0,他引:2  
李广义  王玉兰 《药学学报》1984,19(8):590-592
从瘿花香茶菜Rabdosia rosthornii(Diels)Hara的叶和茎中分离出三种二萜类化合物。其中两种为已知化合物ponicidin和oridonin。另一种为新的二萜化合物。通过理化常数和光谱的分析以及衍生物的制备,测定了其结构,并命名为瘿花香茶菜甲素。  相似文献   

16.
Liver fibrosis is characterized by the activation of hepatic stellate cells (HSCs) and accumulation of the extracellular matrix. There are limitations in the current therapies for liver fibrosis. Recently, oridonin was shown to induce apoptosis in HSCs. Thus, we aimed to determine the roles of oridonin in chronic liver injury and fibrosis. Liver fibrosis was induced by CCl4 in mice injected intraperitoneally with oridonin for 6 weeks. The administration of oridonin significantly attenuated liver injury and reduced ALT levels. In addition, Sirius Red staining and the expression of α-smooth muscle actin (α-SMA) were significantly reduced by oridonin in murine livers with fibrosis. The expression of NLRP3, caspase-1, and IL-1β was downregulated with the oridonin treatment. Furthermore, the expression of F4/80 in liver tissues was also decreased by oridonin treatment. These results demonstrate that oridonin ameliorates chronic liver injury and fibrosis. Mechanically, oridonin may inhibit the activity of the NLRP3 inflammasome and inflammation in the liver. These results highlight the potential of oridonin as a therapeutic agent for liver fibrosis.  相似文献   

17.
目的探讨冬凌草甲素对人肝癌细胞Huh-7索拉非尼(Sor)耐药细胞株Huh-7/Sor的影响及其作用机制。方法体外培养Huh-7/Sor细胞株,qRT-PCR检测miR-217和ABCC1 mRNA的表达水平,Western blotting检测ABCC1蛋白的表达水平;用冬凌草甲素处理Huh-7/Sor细胞后,CCK-8法检测细胞活力,Annexin V/PI染色检测细胞凋亡,Western blotting检测凋亡蛋白和ABCC1的表达水平;数据库预测miR-217与ABCC1的结合位点,转染miR-217 mimic或inhibitor后检测ABCC1的蛋白水平,荧光素酶报告基因检测ABCC1 3‘UTR区域活性。结果与Huh-7细胞相比,Huh-7/Sor细胞中miR-217的表达水平显著下调,ABCC1的表达水平显著上调(P<0.05);冬凌草甲素能抑制Huh-7/Sor细胞的增殖,促进细胞凋亡,上调miR-217的表达水平,抑制ABCC1的表达(P<0.05);miR-217能与ABCC1 3‘UTR区域结合,抑制ABCC1的蛋白表达水平(P<0.05)。结论冬凌草甲素能通过上调miR-217而抑制ABCC1的表达,进而抑制Huh-7/Sor细胞增殖,诱导凋亡。  相似文献   

18.
Oridonin, the major terpene isolated from Rabdosia rubescens, has been used as dietary supplement. Recently, it has been known to exhibit anti-inflammatory effect. This study we employed an in vitro model of LPS-stimulated human gingival fibroblasts to investigate the anti-inflammatory effects and mechanism of oridonin. Oridonin (10–30 μg/mL) was administrated 1 h before LPS treatment. The results showed that oridonin significantly inhibited inflammatory mediators PGE2, NO, IL-6, and IL-8 production. Immunoblotting experiments revealed that oridonin reduced the expression of phosphorylation levels of NF-κB p65 and IκBα. Furthermore, the expression of PPARγ was up-regulated by the treatment of oridonin. Further studies showed that PPARγ inhibitor GW9662 could reverse the inhibition of oridonin on PGE2, NO, IL-6, and IL-8 production. In conclusion, oridonin inhibited LPS-induced microglia activation through activating PPARγ.  相似文献   

19.
Our previous studies indicated that oridonin, a diterpenoid isolated from Rabdosia rubescens, induced human melanoma A375-S2 cell apoptosis. In this study, we investigated whether the proapoptotic effect of oridonin on A375-S2 cells would depend on an interference with function of the insulin-like growth factor 1 (IGF-1) receptor, a plasma membrane receptor critical for the survival or antiapoptotic ability in melanoma cells. We found that IGF-1 receptor (IGF-1R) signaling was a potential survival pathway against a low concentration of 20 μmol/L oridonin-induced apoptosis in A375-S2 cells. The activation of Ras or its downstream effector p38 mitogen-activated protein kinase (p38 MAPK) was shown to be necessary for IGF-1-mediated protection, but the activation of phosphatidylinositol-3-OH kinase (PI3 kinase) or extracellular signal-regulated kinase (ERK) did not correlate with the regulation of survival. However, in the presence of 40 μmol/L (IC50 at 24 h) oridonin, A375-S2 cells could not be protected by IGF-1 from apoptosis, accompanied by a severe impairment of IGF-1R expression. Therefore, we concluded that the proapoptotic activity of oridonin was partially attributed to its repression of IGF-1R signaling. In addition, p53 was supposed to be a pivotal transducer of proapoptotic and survival signaling pathway in this system.  相似文献   

20.
Two new ent-kaurane diterpenoids, dayecrystals D–E (12), together with nine known compounds, isojaponin A (3), rabdosin A (4), lushanrubescensin J (5), wikstroemioidin B (6), maoyecrystal C (7), rabdosin B (8), isodonal (9), shikokianin (10), and effusanin A (11), were isolated from the leaves of Isodon macrophyllus. The structures of the new compounds were elucidated using 1D and 2D NMR spectroscopy. The 13C-NMR spectral data of compound 4 are reported for the first time. All of the compounds were tested for their cytotoxicities against DU145 and LoVo human tumor cells. Compounds 4, 10, and 11 showed inhibitory effects on DU145 cells with IC50 values 5.90, 4.24, and 3.16 μM, and LoVo cells with IC50 values 14.20, 17.55, and 3.02 μM, respectively.  相似文献   

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