丹皮酚抗肿瘤作用机制的研究进展

丹皮酚是牡丹皮的主要活性成分,其抗肿瘤作用的研究已经受到广泛关注。研究报道了丹皮酚对肝癌、胃癌、乳腺癌、卵巢癌等多种肿瘤均具有抗癌作用。丹皮酚主要通过抑制肿瘤细胞增殖,影响肿瘤细胞周期,调控凋亡相关因子及相关通路,抑制肿瘤细胞转移,逆转化疗药物耐药性及放疗增敏发挥抗肿瘤作用。主要综述了丹皮酚抗肿瘤作用机制的最新研究进展。目前丹皮酚抗肿瘤的研究仍处在初步阶段,还需进一步加强对信号转导通路、调控靶点、抑癌基因、联合用药及体内实验等方面的研究。     

丹皮酚对HepA荷瘤小鼠免疫调节和抑瘤作用研究

目的　研究丹皮酚 ( paeonol)的抗肿瘤作用及其机制。方法　建立小鼠移植性肝癌HepA肿瘤模型 ,观察丹皮酚对肿瘤生长的影响。应用放射免疫法检测小鼠血清中IL 2及TNF α含量 ,同时观察丹皮酚对小鼠脾细胞产生IL 2及腹腔巨噬细胞产生TNF α的影响。结果　丹皮酚对小鼠Hep A肿瘤的生长有抑制作用 ,对IL 2及TNF α的生成有促进作用。结论　丹皮酚可能通过促进IL 2及TNF α的生成而发挥抗肿瘤作用     

丹皮酚的研究进展

牡丹皮是一种传统中药,丹皮酚是其主要药效成分。临床上丹皮酚主要外用抗过敏,但近年来研究发现丹皮酚对多种疾病有良好的治疗作用。本文主要综述近年来研究发现的在心血管系统、肝纤维化、抗肿瘤治疗等方面丹皮酚的治疗作用。     

天然抗肿瘤药物有效成分及其作用机理的探讨

目的探讨天然药物抗肿瘤的有效成分及其作用机理,为进一步开发天然抗肿瘤药物提供理论基础。方法通过收集和查找近年来有关天然药物在抗肿瘤方面的报道和研究,整理和总结出天然药物在抗肿瘤方面的有效成分和作用机制。结果天然药物抗肿瘤成分主要有生物碱类,中药多糖类,萜类,醌类,蛋白质类等;对抗肿瘤主要作用机制有对肿瘤细胞的直接杀灭作用;干扰细胞周期;诱导肿瘤细胞的分化;逆转多药耐药性肿瘤细胞的抗凋亡作用;诱导肿瘤细胞凋亡;提高机体免疫力来抗肿瘤等方面进行。结论天然抗肿瘤药物的有效成分类别有多样性,但主要为生物碱类,多糖类等为主;作用机制为直接对肿瘤细胞杀灭作用,干扰细胞生长的各个周期及提高机体免疫力等方面。     

夏枯草抗肿瘤活性成分及其作用机制研究进展

夏枯草作为一味临床常用中药,具有清肝泻火、明目、散结消肿的功效,对甲状腺癌、乳腺癌、肝癌等多种癌症表现出较强的抗肿瘤作用。夏枯草提取物及其有效成分可通过多种途径发挥抗肿瘤作用,其主要途径包括诱导细胞凋亡、抑制细胞侵袭及转移、抑制细胞增殖、诱导自噬、抗肿瘤血管生成、逆转肿瘤多药耐药性和调节免疫功能等。并通过调控miRNA和Wnt/β-catenin、PI3/Akt、AMPK/mTOR/ ULK1、PI3K/Akt/mTOR、RANKL/ RANK/ OPG、PI3K/PTEN/NIS/AKT/mTOR等信号通路,从分子机制上验证了夏枯草提取物具有抗肿瘤作用。本文对夏枯草提取物抗肿瘤的作用机制进行综述,以期为其进一步的研究和应用提供参考。     

丹皮酚体内外抗人食管癌Eca-109细胞增殖及诱导凋亡的作用

目的研究丹皮酚(paeonol,Pae)在体内外对人食管癌细胞Eca-109的抑瘤作用及其对细胞凋亡的影响。方法采用噻唑蓝(MTT)体外试验法和灌胃给药体内抗肿瘤试验。光镜及电镜观察各组的肿瘤组织的形态学变化。应用末端脱氧核苷酸转移酶介导的缺口末端标记(TUNEL)法测定细胞凋亡指数。结果丹皮酚在体外对Eca-109细胞有明显的细胞毒作用,半数抑制浓度(IC50)为0.342mmol·L-1;体内灌胃给予丹皮酚25、50、100和200mg·kg-1对裸鼠移植人食管癌Eca-109的抑制率分别为10.67%、23.54%、27.91%和34.46%;顺铂5mg·kg-1组抑瘤率为58.71%;丹皮酚在100mg·kg-1剂量下与顺铂5mg·kg-1联合用药抑制率为77.91%。光镜下用药组可见较多凋亡的肿瘤细胞。透射电镜下可见肿瘤细胞核染色质浓缩边聚、胞质浓缩、核碎裂以及凋亡小体形成等典型的凋亡表现。用药组凋亡指数较对照组明显增加。结论丹皮酚在体内外具有抑制人食管癌Eca-109细胞增殖及诱导其凋亡作用。     

贺丹皮酚的药理作用研究进展

丹皮酚是牡丹皮、芍药、徐长卿等中药的主要活性成分之一，具有抗心律失常、抗动脉粥样硬化、改善微循环、保护缺血组织、增强免疫力、抗肿瘤作用，还具有抗菌作用和抑制皮肤色素合成的作用，具有良好的开发前景。     

抗肿瘤新星蟾蜍毒素的临床应用及其机制的研究进展

蟾蜍毒素作为传统中药具有多种功效,被广泛应用临床,研究表明其具有抗肿瘤,增强机体免疫力,提高中晚期癌症患者生存质量等作用。本文就蟾蜍毒素抗肿瘤作用及其研究机制方面的最新研究进展作一综述。     

熊果酸抗肿瘤作用研究进展

肿瘤是严重威胁人类健康的恶性疾病,寻找安全有效的抗癌药是治疗肿瘤的关键。熊果酸（UA）是广泛存在于天然植物中的一种五环的三萜类化合物,具有多种生物学活性,包括抗菌、抗结核、保护肝脏、降压、降血糖等作用。近年来其抗肿瘤作用日益受到人们重视。其抗肿瘤机制可通过多种途径进行调节,包括抑制细胞增殖、诱导细胞凋亡、抑制血管生成、抗侵袭、抗突变、抗氧化和免疫调节等作用。本文将近年来国内外对熊果酸抗肿瘤作用的研究进展综述如下。     

牡丹皮及其主要成分丹皮酚的药理作用研究进展

牡丹皮和丹皮酚都具有保肝护肾、降血糖、抗菌消炎、抗心律失常、抗过敏、保护心血管、神经保护、增强免疫力等多种药理作用;另外牡丹皮还具有止血、凝血等作用.牡丹皮药理作用机制的深入研究,将为其临床应用和深度开发提供科学依据.     

CYP1A2 is the major isoform responsible for paeonol O-demethylation in human liver microsomes

1. Paeonol, the primary active component of a traditional Chinese medicine Moutan Cortex, has a wide range of pharmacological activities. In the present study, the metabolism of paeonol by cytochrome P450s (CYPs) was investigated in human liver microsomes.

2. One O-demethylated metabolite was detected in reaction catalysed by human liver microsomes, and was identified as resacetophenone by comparing the tandem mass spectra and the chromatographic retention time with that of the standard compound.

3. The study with a chemical selective inhibitor, cDNA-expressed human CYPs, a correlation assay, and a kinetics study demonstrated that CYP1A2 was the major isoform responsible for the paeonol O-demethylation in human liver microsomes.

     

白屈菜碱的药理作用研究进展

白屈菜碱是白屈菜Chelidonium majus的主要活性成分之一,属于苯并菲啶类生物碱,现作为止痛药应用于临床。随着对白屈菜碱药理作用的深入研究发现,其具有抗肿瘤、镇痛、抗菌、解痉等多种药理作用,且其抗肿瘤作用越来越受到关注。对近年来白屈菜碱药理作用的国内外研究进展做以综述,为其进一步研究与应用提供理论依据。     

Antitumor and Apoptosis Induction Effects of Paeonol on Mice Bearing EMT6 Breast Carcinoma

Paeonol is a major phenolic micromolecular component of Moutan cortex Radicis, a traditional Chinese Medicine. It has shown antitumor effects in previous studies; however, the underlying mechanisms remain unknown. This study investigated the mechanism by giving treatments of placebo, cyclophosphamide, paeonol of 150 and 300 mg/kg to 4 groups of mice bearing EMT6 breast cancer. Apoptosis in tumor cells were confirmed by morphology analysis, including hematoxylin, eosin staining and TUNEL staining. The results showed that the weight of EMT6 breast tumor was significantly reduced in the groups treated with both 150 and 300 mg/kg of paeonol. Immunohistochemical and Western blot results showed that the expression of Bcl-2 was down-regulated while the expression of Bax, caspase 8 and caspase 3 was up-regulated respectively. These results suggest that paeonol exhibits antitumor effects and the mechanism of the inhibition is via induction of apoptosis, regulation of Bcl-2 and Bax expression, and activation of caspase 8 and caspase 3.     

生脉方类注射剂抗肿瘤药理及临床研究进展

生脉方类注射剂是根据经典古方“生脉散”制成的中药注射剂，主要包括注射用益气复脉（冻干）、生脉注射液和参麦注射液等。生脉方类注射剂具有广泛的药理作用，在改善心脏功能、保护心肌细胞、调节血压、提高机体免疫功能、抗肿瘤等方面都有广泛的应用价值。从药理研究以及临床应用两方面，综述了生脉方类注射剂在肺癌、肝癌、脑癌、结直肠癌、乳腺癌、鼻咽癌等肿瘤治疗中的研究进展，以期为该类注射剂抗肿瘤作用的深入研究以及临床应用提供参考。     

菘蓝属植物化学成分及药理作用研究进展

菘蓝属植物在中国药用历史悠久，其中菘蓝的根和叶即为板蓝根和大青叶。该属植物化学成分多样，主要包括生物碱类、硫代葡萄糖苷类、木脂素类、黄酮类等，具有抗菌、抗病毒、抗内毒素、抗肿瘤、抗炎、免疫增强等药理作用。本文对近40年来国内外有关菘蓝属植物化学成分和药理作用的文献进行系统的总结，为该属植物的进一步研究开发提供参考。     

Synthesis and in vitro cytotoxic evaluation of novel diazaspiro bicyclo hydantoin derivatives in human leukemia cells: A SAR study

Summary  To study the structure activity relationship (SAR) on the cytotoxic activity and probe the structural requirement for the potent antitumor activity, a series of novel diazaspiro bicyclo hydantoin derivatives were designed and synthesized. Their structures were confirmed by ¹H NMR, LCMS and IR analyses. The antiproliferative effect of these compounds were determined against human leukemia, K562 (chronic myelogenous leukemia) and CEM (T-cell leukemia) cells using trypan blue and MTT assay, and the SAR associated with the position of N-terminal substituents in diazaspiro bicyclo hydantoin have also been discussed. It has been observed that these compounds displayed strong, moderate and weak cytotoxic activities. Interestingly, compounds having electron withdrawing groups at third and fourth position of the phenyl ring displayed selectively cytotoxic activities to both the cell lines tested with IC₅₀ value lower than 50 μM. In addition, the cytotoxic activities of the compounds 7(a–o) bearing the substituents at N−3 position of diazaspiro bicyclo hydantoin increases in the order alkene > ester > ether and plays an important role in determining their antitumor activities. The position and number of substituents in benzyl group attached to N−8 of diazaspiro bicyclo hydantoin nucleus interacted selectively with specific targets leading to the difference of biochemical and pharmacological effects.     

Immunomodulatory effect of polysaccharides from submerged cultured Cordyceps gunnii

Context: The genus Cordyceps (Clavicipitaceae) is a group of entomopathogenic fungi that is widely used as tonic food or invigorant with broad-spectrum medicinal properties in China. Cordyceps gunnii (Berk.)Berk (C. gunnii), is also well known as the Chinese rare caterpillar fungus and has similar pharmacological activities with Cordyceps sinensis (C. sinensis). Polysaccharides (PS) from various Cordyceps species have demonstrated many interesting biological activities, including antitumor, immunopotentiation, hypoglycemic, and hypocholesterolemic activities.

Objective: To investigate the effect of C. gunnii PS on the immunostimulatory antitumor function and expression of immune related cytokines in normal, immuno-suppressive, and H22-bearing mice, respectively. Methods: C. gunnii PS were extracted with hot water at 80°C for 2 h. Normal, immuno-suppressive, and H22-bearing mice were treated with PS respectively. By detecting the value of macrophage phagocytic index, proliferation of lymphocytes, natural killer (NK) cell activity and expression of related cytokines, interleukin (IL-4), tumor necrosis factor-α (TNF-a) and interferon-γ (IFN-γ), and tumor inhibition index in H22-bearing mice additionally, the effect of PS on immunostimulatory antitumor function and its mechanism were studied.

Results: The total sugar content of the PS was determined to be 95% after purification. PS markedly increased the thymus and spleen indexes, the macrophage phagocytosis, the proliferation of splenic cells, and the level of IFN-γ and TNF-α. In tumor growth inhibition test, PS showed remarkable inhibition effects.

Conclusion: PS from the C. gunnii could enhance nonspecific immunological function, humoral immunity, cellular immunity in mice, and inhibit tumor growth.     

5个丹皮酚酯的合成和体外抗肿瘤活性研究

丹皮酚与相应的酰氯反应得到5个新的丹皮酚酯,其结构通过光谱法确证.它们的体外抗肿瘤活性通过MTT法和集落形成法进行了评价.初步的体外生物试验结果表明,5-硝基-2-呋喃甲酸的丹皮酚酯对人肿瘤细胞有一定抑制作用,其结果和临床上常用的抗肿瘤药5-Fu相近.     

抗癌及癌化学预防药物的研究:3-α-酮醛香豆素衍生物的合成及其抗致突活性与结构间的关系

α-酮醛及其衍生物在抗病毒、抗肿瘤方面有一定活性。我们合成了18个新的3-α-酮醛香豆素衍生物,研究该类化合物的质谱裂解方式与氢核磁共振谱的特征峰。体外药理筛选发现其中部分化合物有不同程度的抗致突活性,对其构效关系进行了分析,并提出了这类化合物产生抗致突活性的可能亚结构。