Phytochemical constituents from the herba of<Emphasis Type="Italic">Artemisia apiacea</Emphasis>

Four compounds of a coumarin, a steroid and two flavonoids were isolated from the herba of Artemisia apiacea by open column chromatography. Their structures were elucidated as artemicapin C, apigenin, daucosterol and cacticin by chemical and spectroscopic analysis. This is the first report of the isolation of these compounds from this plant.     

Inhibitory effects of luteolin isolated from<Emphasis Type="Italic">ixeris sonchifolia</Emphasis> hance on the proliferation of hepg2 human hepatocellular carcinoma cells

We investigated the anti-proliferative effects of luteolin and apigenin, isolated from Ixeris sonchifolia Hance, on HepG2 human hepatocellular carcinoma cells. In MTT assay luteolin showed more efficient anti-proliferative effects on cells than apigenin did. According to propidium iodide staining and flow cytometry studies, we postulated that these effects might be a result of cell cyde arrest. Hence we examined the changes of protein expressions related to cell cycle arrest. Western blotting data demonstrated that the down-regulated expression of CDK4 was correlated to the increase of p53 and CDK inhibitor p21(WAF1/CIP1) protein. These data suggest that luteolin may have potential as an anti-cancer agent.     

苦苣菜的化学成分

目的:研究苦苣菜的化学成分.方法:利用各种色谱技术进行分离纯化,根据化合物的理化性质和光谱数据进行结构鉴定.结果:分离得到10个化合物,分别为:木犀草素(luteolin,Ⅰ)、木犀草素-7-O-β-D-葡萄糖苷(luteolin-7-O-β-D-glucoside,Ⅱ)、芹菜素(apigenin,Ⅲ)、芹菜素-7-O-β-D-葡萄糖醛酸甲酯(apigenin-7-O-β-D-glucuronide methyl ester,Ⅳ)、芹菜素-7-O-β-D-葡萄糖醛酸乙酯(apigenin-7-O-β-D-glucuronide ethyl ester,Ⅴ)、芹菜素-7-O-β-D-葡萄糖醛酸苷(apigenin-7-O-β-D-glucopyranuronide,Ⅵ)、3β-acetoxy-olean-18-ene,germanicolacetate(germanicyl acetate,Ⅶ)、3β-hydroxy-6β,7α,11β-H-eudesm-4-en-6,12- olide(Ⅷ)、齐墩果酸(oleanolic acid,Ⅸ)和正二十六烷醇(1-cerotol,Ⅹ).结论:化合物Ⅳ～Ⅵ、Ⅷ、Ⅹ均为首次从苦苣属植物中分得.     

藤茶化学成分的研究

目的:对藤茶的化学成分进行研究。方法:经反复硅胶、聚酰胺柱色谱及重结晶等手段进行分离,运用UV、MS、NMR等波谱方法进行结构鉴定。结果:分离鉴定了6个化合物,分别为β-谷甾醇(1)、齐墩果酸(2)、橙皮素(3)、二氢槲皮素(4)、山柰酚(5)、芹菜素(6)。结论:橙皮素、山柰酚、芹菜素为首次从该种植物中分离得到。     

HPLC测定香青兰药材中的黄酮类成分

目的 建立测定香青兰药材含量的方法.方法 采用HPLC测定.结果 所测香青兰药材中山奈素、洋芹素、异鼠李素,各成分的线性关系良好,其线性范围分别为6.06～60.60 μg·ml-1(r=0.9996)、3.04～30.40 μg·ml-1(r=0.9997)、2.64～26.40μg·ml-1(r=0.9996).其回收率分别为96.2%(RSD=1.1%)、96.9%(RSD=1.1%)、97.2%(RSD=1.2%)(n=3).结论 所建方法准确、简便,为科学地评价香青兰药材的质量提供了依据.     

The dietary flavonoids apigenin and (-)-epigallocatechin gallate enhance the positive modulation by diazepam of the activation by GABA of recombinant GABA(A) receptors

The dietary flavonoids apigenin, genistein and (-)-epigallocatechin gallate (EGCG) inhibited the activation by GABA (40 microM) of recombinant human alpha1beta2gamma2L GABA(A) receptors expressed in Xenopus laevis oocytes with IC(50) values of 8, 30 and 15 microM, respectively. Apigenin and genistein also acted as GABA antagonists at flumazenil-insensitive alpha1beta2 GABA(A) receptors, indicating that they were not acting as negative modulators through flumazenil-sensitive benzodiazepine sites on GABA(A) receptors. In addition to these GABA(A) antagonist effects, a novel second order modulatory action was found for apigenin and EGCG on the first order enhancement of GABA responses by diazepam. Apigenin (1 microM) and EGCG (0.1 microM) enhanced the modulatory action of diazepam (3 microM) on the activation by GABA (5 microM) of recombinant human alpha1beta2gamma2L GABA(A) receptors by up to 22% and 52%, respectively. This was not found with genistein, nor was it observed with enhancement by allopregnanolone or pentobarbitone.     

间歇低氧对幼鼠纹状体边缘区p38MAPK和超微结构的影响及芹菜素的干预作用

目的:研究间歇低氧对幼鼠纹状体边缘区p38MAPK及超微结构的影响及芹菜素的干预作用。方法:SPF级健康雄性SD幼鼠(3~4周龄)40只,随机分为4组:间歇低氧2周组(IH组)、对照组(C组)、芹菜素 二甲基亚砜组(Q组)和二甲基亚砜组(R组)。建立间歇低氧幼鼠模型,以RT-PCR法和Westernblot法分别测幼鼠纹状体内侧边缘区p38MAPK mRNA和磷酸化p38MAPK(p-p38)蛋白的表达,并电镜观察超微结构的改变。结果:IH组幼鼠纹状体边缘区的p38MAPK mRNA及p-p38蛋白均明显高于C组(P均<0.01),Q组的表达则明显低于R组(P均<0.01),电镜下IH组和R组纹状体边缘区组织细胞核膜模糊不清晰,染色质浓缩、边聚,线粒体肿胀空泡化,Q组和C组无明显变化。结论:间歇低氧可激活幼鼠脑区p38MAPK,进而引起超微结构的改变,而芹菜素可至少部分抑制这种激活,这可能对减轻间歇低氧后纹状体边缘区等脑区损伤具有积极意义。     

Estimation of Apigenin, an Anxiolytic Constituent, in Turnera aphrodisiaca

An HPTLC densitometric method has been developed to estimate apigenin in Turnera aphrodisiaca aerial and its segregated parts (leaves, stems, flowers and fruits) so that plant can be standardized on the basis of its bioactive marker. The apigenin content in methanol extract of T. aphrodisiaca aerial parts was found to be about fourteen times less than acid hydrolyzed methanol extract of the plant indicating the presence of most of apigenin in glycosidic form. Amongst different plant parts, flowers possessed maximum content of apigenin followed by leaves. The apigenin content was also determined in three marketed formulations of T. aphrodisiaca viz., NLK, DWSG and SBL. DWSG contained higher content of apigenin. Aerial parts of the plant were collected at bimonthly intervals over a period of one year in the months of January, March, May, July, September and November. The plant material collected in September showed maximum content of apigenin.     

芹菜素纳米乳对肝纤维化的治疗作用

目的 研究芹菜素纳米乳对肝纤维化大鼠的治疗作用,并对其作用机制进行初步研究.方法 采用四氯化碳(CCl4)复制大鼠肝纤维化模型,90只SD大鼠经适应性饲养1周后,随机分为6组,每组15只.正常组以2 mL/kg橄榄油皮下注射;模型组以25％CCl4橄榄油为造模剂,按2 mL/kg皮下注射;治疗组分3组,在皮下注射25％CCl4橄榄油的同时灌胃给予芹菜素纳米乳25、50、100 mg/kg,1次/d;阳性对照组给予造模剂的同时给予水飞蓟宾100 mg/kg.每周造模2次(间隔2d),连续8周.末次给药后24 h,取大鼠血清和肝脏,观察芹菜素纳米乳对大鼠血清肝功能指标ALT和AST,肝纤维化指标透明质酸(HA)、层黏连蛋白(LN)、Ⅳ型胶原(Ⅳ-C)、Ⅲ型前胶原(PCⅢ)和肝组织中丙二醛(MDA)、羟脯氨酸(Hyp)、超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-Px),转化因子-β1(TGF-β1)、金属蛋白酶抑制因子-1(TIMP-1)、α-平滑肌肌动蛋白(α-SMA)表达的影响.结果 芹菜素纳米乳能显著降低ALT、AST、LN、PCⅢ、Ⅳ-C水平(F=13.851、6.877、5.352、7.469、20.874,P均＜0.01),升高SOD和GSH-PX活性,降低Hyp含量(F=5.470、20.734、195.76,P均＜0.01),显著降低TIMP-1、TGF-β1和α-SMA的表达(F=82.281、72.359和91.226,P＜0.01).结论 芹菜素纳米乳对CC14致肝纤维化大鼠具有一定的治疗作用,其作用机制可能与抗脂质过氧化反应、影响TGF-β1、TIMP-1、α-SMA表达有关.     

Regulation of IGF-I production and proliferation of human leiomyomal smooth muscle cells by Scutellaria barbata D. Don in vitro: isolation of flavonoids of apigenin and luteolin as acting compounds

Scutellaria barbata D. Don (Lamiaceae) (SB) is a perennial herb, which is natively distributed throughout Korea and southern China. This herb is known in traditional Chinese Medicine as Ban-Zhi-Lian and traditional Korean medicine as Banjiryun, respectively. SB has been used as an anti-inflammatory and antitumor agent. We aimed to determine the expression of growth factor molecules for growth inhibition after treatment of SB in two different human myometrial smooth muscle cell (SMC)s and leiomyomal SMCs. Water-soluble ingredients of SB, myometrial SMCs, and the leiomyomal cell lines were used in vitro. SB significantly reduced cell numbers in culture and arrested cell proliferation, and also induced apoptosis, indicating that the presence of an intact apoptotic pathway was demonstrated in these cells by SB. Uterine leiomyoma is the most common benign smooth muscle cell tumor of the myometrium. The expression of insulin-like growth factor-I (IGF-I) was measured at the mRNA and protein level in myometrium and leiomyomal cells with and without treatment with a water extract of SB for 3 days. IGF-I mRNA expression was significantly higher in leiomyomal cells than in myometrium cells. The IGF-I protein was more abundant in leiomyomal cells than in myometrium. When SB was treated to the cells, the IGF-I protein concentrations in myometrial and leiomyomal cells from the SB-treated cells were similar. The results indicated that IGF-I expression is probably associated with a proliferation of leiomyomal cells than myometrium. However, SB down-regulated the IGF-I expression where IGF-I contributes to the selective growth of the leiomyoma. Therefore, growth modulation of LMs by SB occurs via mechanisms dependent of apoptosis. The raw materials were extracted and subjected to functional isolation for the active molecules in the present assay systems. The five flavonoids were isolated and the chemical structures of resveratrol, baicalin, berberine, apigenin, and luteolin were determined. The effects of resveratrol, baicalin, and berberine on the above parameters have not been significantly evidenced, whereas apigenin and luteolin were effective. The anti-proliferative compounds apigenin and luteolin belong to the flavones, a class of flavonoids and are characterized as selectively inhibitors of the growth of LM cells. Our findings suggest that flavonoids of apigenin and luteolin are potentially useful for the development of therapeutic treatments of cancer. These data also suggest that SB reduces tumor volume with inducing a concomitant increase in the rate of apoptosis.