头序木叶中三萜化学成分的研究

从头序木（ＡｒａｌｉａｄａｓｙｐｈｙｌａＭｉｑ）叶中分离到６个三萜化合物，用化学方法和波谱（ＵＶ，ＩＲ，ＭＳ，１ＨＮＭＲ，１３ＣＮＭＲ，１３ＣＤＥＰＴ，ＨＭＱＣ，ＨＭＢＣ）分析，确定其中４种化合物的结构，分别为齐墩果酸（Ｉ），１６β羟基１８βＨ齐墩果酸（Ｉ），齐墩果酸２８ＯβＤ吡喃葡萄糖甙（ＩＩ）和１６β羟基１８βＨ齐墩果酸２８ＯβＤ吡喃葡萄糖甙（ＩＶ）。用ＮＯＥＳＹ谱确定化合物Ｉ的立体构型。以上４个化合物均为首次从该植物中分离到，化合物ＩＶ为新化合物。     

太白楤木总皂苷对K562细胞增殖抑制及其作用机制的研究

目的 以人慢性髓系白血病细胞株K562细胞为模型,研究太白楤木的体外抗肿瘤活性及其作用机制.方法 MTT法检测太白楤木总皂苷对K562细胞的增殖抑制作用;单细胞凝胶电泳检测K562细胞DNA损伤;流式细胞术检测K562细胞细胞周期的改变.结果 太白楤木总皂苷对K562细胞增殖具有抑制作用,并呈时间-剂量依赖性;能显著诱导K562细胞DNA损伤;促进凋亡的发生;细胞周期阻滞于S期.结论 太白楤木总皂苷能抑制K562细胞的增殖,诱导凋亡发生,其机制可能与通过诱导K562细胞DNA损伤来改变细胞周期时相的分布有关.     

HPLC法测定龙芽梅木药材中齐墩果酸的含量

目的建立HPLC法测定龙芽梅木药材中齐墩果酸的含量测定方法。方法采用Kromasil C18色谱柱（250mm×4．6mm,5μm）,流动相：乙腈-水-磷酸（80：20：0．42）,检测波长：208nm。结果齐墩果酸在1．164～5．820邮范围内具有良好的线性关系,r=0．9999,平均加样回收率为99．69％,RSD=1.76％（n=5）。结论该方法简单、准确,重复性好,可作为龙芽橡木药材中齐墩果酸的含量测定方法。     

HY253, a novel decahydrofluorene analog,from Aralia continentalis, induces cell cycle arrest at the G1 phase and cytochrome c-mediated apoptosis in human lung cancer A549 cells

Aim of the study

In the course of our screening for novel modulators on cell cycle progression and apoptosis as anticancer drug candidates, we isolated a novel compound HY253 with the molecular structure of 7,8a-divinyl-2,4a,4b,5,6,7,8,8a,9,9a-decahydro-1H-fluorene-2,4a,4b,9a-tetraol from the roots of Aralia continentalis. This study was designed to evaluate the detailed mechanisms of cell cycle arrest and the apoptotic induction of HY253 in human lung cancer A549 cells.

Materials and methods

To investigate the effects of HY253 on cell cycle progression in A549 cells, we measured DNA content of A549 cells treated with 35 μM of HY253 using flow cytometric analysis. Furthermore, TUNEL assay was used to examine apoptotic induction in A549 cells treated with 70 μM of HY253 for 24 and 48 h. The effects of HY253 on apoptosis-associated and cell cycle regulatory proteins in A549 cells were examined using Western blot analysis.

Results

The flow cytometric analysis revealed an appreciable G₁ phase arrest in A549 cells treated with 35 μM of HY253. This HY253-induced G₁ phase arrest is associated with decreased expression of cyclin D and up-regulation of p21^CIP1, via p53 phosphorylation at Ser-15, which resulted in increased hypophosphorylated pRb in A549 cells. Furthermore, TUNEL assay and Western blot analysis revealed an appreciable apoptotic induction in A549 cells treated with 70 μM of HY253 for 48 h. This apoptotic induction in HY253-treated A549 cells is also associated with cytochrome c release from mitochondria which in turn resulted in the activation of caspase-9 and -3, and the cleavage of poly(ADP-ribose) polymerase (PARP).

Conclusions

These results demonstrate that HY253, a novel antiproliferative compound isolated from the roots of Aralia continentalis, induces cell cycle arrest at the G₁ phase and apoptosis in A549 cells. Based on these results, we suggest that HY253 may be a potent cancer chemotherapeutic candidate for use in treating human lung cancer cells via up-regulation and activation of p53 gene.     

辽东楤木叶总皂苷(ETS)对裸鼠A549体外移植瘤抑制率及瘤体相关蛋白COX-2表达影响的实验研究

目的:探讨ETS抗肿瘤作用及机制,为进一步将其开发成新靶点的抗肿瘤药物提供可靠的科学依据。方法:建立A549荷瘤裸鼠动物模型进行体内抑瘤实验,取瘤体,称瘤重,计算肿瘤抑制率;免疫组化二步法检测瘤体内相关蛋白COX-2,CD31抗体检测瘤体微血管密度。结果:ETS能明显抑制裸鼠A549体外移植瘤生长,抑制COX-2的表达,降低微血管密度。结论:研究结果为辽东楤木叶抗肿瘤机理提供了实验依据。     

Effects of Aralia mandshurica and Engelhardtia chrysolepis extracts on some parameters of lipid metabolism in women with nondiabetic obesity

The effects of oral treatment with Aralox phytopreparation containing Aralia mandshurica (Araliaceae) and Engelhardtia chrysolepis (Juglandaceae) extracts on some parameters of lipid metabolism was studied in women with nondiabetic obesity receiving low-caloric diet. Our randomized placebo-controlled study comprising 32 volunteers showed that aralox treatment led to a decrease in total body weight and fat weight, reduced perilipin content in adipocytes and plasma triglyceride content, and stimulated activity of hormone-sensitive lipase. __________ Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 141, No. 3, pp. 320–323, March, 2006     

辽东楤木叶总皂苷对人胃癌BGC细胞凋亡的影响

目的:探讨辽东楤木叶总皂苷(ETS)对人胃癌BGC细胞凋亡的影响。方法:采用MTT比色法测定辽东楤木叶总皂苷在体外对人胃癌BGC细胞增殖的影响;激光共聚焦显微镜观察FITC-Annexin V/PI双染法检测辽东楤木叶总皂苷作用于人胃癌BGC细胞后引起细胞凋亡的形态特征。结果:MTT比色法结果表明,辽东楤木叶总皂苷各剂量组能不同程度抑制人胃癌BGC细胞的增殖,激光共聚焦FITC-Annexin V/PI双染法检测辽东楤木叶总皂苷可诱导人胃癌BGC细胞出现凋亡早、中、晚期的细胞形态。凋亡早期仅细胞膜呈绿色,细胞核不染色;凋亡中、晚期则细胞膜呈绿色,细胞核呈红色。结论:辽东楤木叶总皂苷能够有效抑制癌细胞增殖、诱导凋亡,具有明显的抗肿瘤作用。     

楤木单体的结构改造及抗炎活性研究

目的对楤木Aralia elata中的单体成分金盏花苷E进行结构改造,并对其结构改造后的类似物进行体外抗炎活性研究。方法以天然易得的齐墩果酸为起始原料,经苷元28位羧基保护、3位糖苷化、28位羧基脱保护、28位羧基酰胺化、胺基侧链酰胺化、糖基苯甲酰基脱保护、甲叉基脱保护共7步反应制得目标化合物,利用巨噬细胞RAW264.7模型评价化合物的抗炎活性。结果设计并合成了10个金盏花苷E的结构类似物G1~G5和H1~H5,均经谱学技术确证结构。生物活性实验结果表明,10个化合物对RAW264.7细胞呈现不同程度的抗炎活性,其中化合物G1~G4、H1~H3的抗炎活性优于先导物。结论化合物G1~G5和H1~H5均为未见文献报道的新化合物,具有潜在的抗炎活性,值得深入研究。     

太白楤木总皂苷对小鼠急性酒精性肝损伤的干预作用

目的 探讨太白楤木总皂苷对小鼠急性酒精性肝损伤的保护作用及其机制。方法 将健康昆明小鼠60只随机分为空白组（生理盐水）、模型组（生理盐水）、阳性对照组（联苯双酯,125mg/kg）、太白楤木总皂苷高、中、低剂量组（400、200、100mg/kg）,每组10只,雌雄分开饲养,灌胃给药。除空白组外,其余各组每日上午给予56°北京二锅头（10mg/kg）灌胃,下午给予干预治疗,连续7天。末次给药8h后,检测小鼠肝脏指数,血清及肝组织中丙氨酸氨基转移酶（ALT）、天门冬氨酸氨基转移酶（AST）含量,肝组织中超氧化物歧化酶（SOD）活性、丙二醛（MDA）含量,HE染色观察肝组织病理改变。结果 与模型组比较,太白楤木总皂苷不同浓度治疗组均能够降低酒精性肝损伤小鼠血清及肝组织中ALT、AST水平（P<0.01）,升高肝组织SOD活性（P<0.01）,降低MDA含量（P<0.05）;肝组织HE染色显示,太白楤木总皂苷可明显减轻小鼠肝损伤的病变程度。结论 太白楤木总皂苷对急性酒精性肝损伤小鼠具有一定的保护作用,其作用机制可能与对抗自由基生成,抑制氧化应激来实现抑制抗氧化应激有关。     

Three new triterpenoid saponins from Aralia echinocaulis

Objective: To study the active ingredients in the root bark of Aralia echinocaulis. Methods: Three triterpenoid saponins were separated from the 70% ethanol extracts and purified by column chromatography and their structures were determined by spectroscopic analysis. Compound 1 and 3 were evaluated for antioxidant activity by the in vitro DPPH free radical scavenging ability and the protective effect of OH- induced DNA oxidative damage. Results: Compound 1 was a new type of triterpenoid saponin, named as echinocaulisaglycone 3-O-β-D-glucopyranoside (echinocaulisaponin A), and it had good antioxidant activity. Compound 2 was similar to compound 1, named as 1-hydroxyl-echinocaulisaglycone 3-O-β-D-glucopyranoside (echinocaulisaponin B). Compound 3 was also a new type of triterpenoid saponin, named as echinocaulisaglycone II 3-O-α-L-arabinopyranosyl-(1”→4’)-β-D-glucopyranosiduronic acid (echinocaulisaponin C), and its antioxidant activity was weaker than compound 1. Conclusion: In this study, three new compounds were discovered and two of them were carried out in vitro anti-oxidation studies, laying the foundation for further research on the treatment of related diseases (cardiovascular disease, arthritis, age-related macular degeneration, etc.) through anti-oxidation or quenching free radical function.