Apoptosis inducing activity of viscin, a lipophilic extract from Viscum album L

Detection of antiproliferative activity and bioactivity-guided fractionation of viscin, a lipophilic extract from Viscum album L., led to the isolation of betulinic acid, oleanolic acid and ursolic acid as active components. Viscin, betulinic acid, oleanolic acid and ursolic acid inhibited growth and induced apoptotic cell death in Molt4, K562 and U937 leukaemia cells. The growth inhibitory effect of viscin was more pronounced in Molt4 and U937 cells (IC50 (concentration that inhibited cell proliferation by 50%): 118 +/- 24 and 138 +/- 24 microg mL(-1)) than in K562 cells (IC50: 252 +/- 37 microg mL(-1)). Oleanolic acid was the least effective in all cell lines (7.5-45.5% inhibition at 10 microg mL(-1)) and ursolic acid the most active in Molt4 and U937 cells (81.8 and 97.8% inhibition, respectively, at 5 microg mL(-1)). A dose-dependent loss of membrane phospholipid asymmetry associated with apoptosis was induced in all cell lines as shown in flow cytometry by the externalization of phosphatidylserine and morphological changes in cell size and granularity. There were differences in individual cell lines' response towards the apoptosis-inducing effect of viscin, betulinic acid, oleanolic acid and ursolic acid. The triterpenoids beta-amyrin, beta-amyrinacetate, lupeol, lupeolacetate, beta-sitosterol and stigmasterol, and the fatty acids oleic acid, linoleic acid, palmitic acid and stearic acid were also present in the lipophilic extract.     

Studies on the biological activity of stubomycin

Stubomycin showed direct cytotoxic activity on mammalian cells, yeast, and fungi, and rapid hemolytic activity on mouse erythrocytes. The rate and extent of the cytotoxic and hemolytic activities decreased at lower temperatures. Studies with radioactive precursors revealed that a marginal cytocidal concentration of the antibiotic inhibited synthesis of DNA, RNA, and protein of leukemic cells at almost the same rate. Stubomycin did not show any mutagenicity on mammalian cells and bacteria i.e. the induction of revertants on six bacterial strains, and chromosomal aberrations, sister chromatid exchanges, and the induction of cells resistant to 6-thioguanine on Chinese hamster cells (DON D-6). The antagonistic effect of various kinds of lipids including phospholipids, cholesterol, olive oil and squalene was studied. Significant antagonism of stubomycin against anti-Saccharomyces cerevisiae activity was observed with phospholipids except for egg lecithin and with cholesterol. The primary action of the antibiotic seems to be to change the cell surface and ultimately the lysis and death of the cells.     

Studies on the estrogenic activity of a coffee extract

Ethyl ether extracts derived from coffee were tested for in vitro estrogenic and in vivo uterotropic activities. Coffee extracts, unlike tea and cocoa, were found to actively compete with 17 beta-estradiol for uterine cytosol binding sites. The biologically active fractions possessed an unique ultraviolet absorbance spectrum that excluded them from containing flavonoid, coumestan, or resorcyclic acid lactone constituents. Coffee extracts administered to immature female mice for 3 d in feeding studies displayed significant (p less than 0.05) uterotropic responses, which were similar to results obtained in mice treated with a standard 17 beta-estradiol dose. Additional studies in mice disclosed that coffee extracts did not reduce the uterotropic effect normally induced by 17 beta-estradiol when administered simultaneously with estradiol. The complete estrogenic effects of coffee constituents, coupled with their failure to inhibit a biological response evoked by estradiol, strongly suggest that coffee contains constituent(s) that are weakly estrogenic.     

Chemical composition and biological activity of a fraction of meadowsweet extract

Studies of the chemical composition of a butanol fraction of an extract from the above-ground part of the meadowsweet in 70% ethanol yielded five substances which were flavonoids (quercetin, isoquercetin, quercetin 4′-glucoside, rutin) and phenolcarboxylic acids (gallic acid). The fraction was found to have nootropic actions, with antiamnestic, antihypoxic, antioxidant, and adaptogenic activities. Studies of the antioxidant properties of the individual compounds showed that isoquercetin, quercetin 4′-glucoside, and rutin were more active than dihydroquercetin and ascorbic acid.     

羊胎免疫调节因子生物活性的研究

目的探讨不同相对分子质量 (Mr)及不同工艺方法获得的山羊羊胎免疫调节因子 (GEIF)生物活性效果。方法运用Ea玫瑰花环试验和T淋巴细胞转化试验进行对比分析。结果超滤法提取GEIF ,不同Mr(30 0 0、5 0 0 0和 10 0 0 0 )Ea玫瑰花环恢复率和T淋巴细胞转化率之间没有明显差异 ;超滤法提取GEIF ,Ea玫瑰花环恢复率和T淋巴细胞转化率均高于透析法。结论采用超滤法提取GEIF生物活性优于透析法 ,不同Mr 提取GEIF生物活性无明显差异。     

Safety assessment of sandalwood oil (Santalum album L.).

Sandalwood (Santalum album L.) is a fragrant wood from which oil is derived for use in food and cosmetics. Sandalwood oil is used in the food industry as a flavor ingredient with a daily consumption of 0.0074 mg/kg. Over 100 constituents have been identified in sandalwood oil with the major constituent being alpha-santalol. Sandalwood oil and its major constituent have low acute oral and dermal toxicity in laboratory animals. Sandalwood oil was not mutagenic in spore Rec assay and was found to have anticarcinogenic, antiviral and bactericidal activity. Occasional cases of irritation or sensitization reactions to sandalwood oil in humans are reported in the literature. Although the available information on toxicity of sandalwood oil is limited, it has a long history of oral use without any reported adverse effects and is considered safe at present use levels.     

Anti-asthmatic activity of an ethanol extract from Saururus chinensis

As an attempt to find bioactive medicinal herbs exerting anti-asthmatic activity, the effects of an ethanol extract from the parts of Saururus chinensis were evaluated in both in vitro and in vivo. The ethanol extract of S. chinensis (ESC) inhibited generation of the cyclooxygenase-2 (COX-2) dependent phases of prostaglandin D(2) in bone marrow-derived mast cells in a concentration-dependent manner with an IC(50) value of 14.3 microg/ml. ESC also inhibited leukotriene C(4) production with an IC(50) value of 0.3 microg/ml. This demonstrates that ESC has COX-2/5-lipoxygenase dual inhibitory activity. In addition, this compound inhibited degranulation reaction in a dose dependent manner, with an IC(50) value of 1.3 microg/ml. An ovalbumin induced mouse asthmatic animal model was used to determine its in vivo anti-asthmatic activity. The oral administration (50-200 mg/kg) of ESC reduced the number of infiltrated eosinophil in a bronchoalveolar lavage fluid. Furthermore, ESC (100 mg/kg) inhibited the eotaxin and IL-4 mRNA expression levels. These results suggest that the anti-asthmatic activity of S. chinensis might in part occur via the inhibition of eicosanoid generation, degranulation as well as the down regulation of IL-4 and eotaxin mRNA expression.     

藜的化学成分研究

目的:对黎Chenopodium L.的抗过敏活性成分进行研究。方法;利用色谱的方法分离成分,利用光谱和化学方法鉴定其化学结构。结果:从藜的种子中分离得到3个化合物,经光谱和化学分析,鉴定为28-氧-β-D-吡喃葡萄糖基-齐墩果酸-3-氧-β-D-吡喃葡萄糖醛酸甙(1)、20-羟基蜕皮酮(2)和芦丁(3)。结论:化合物1,2和3均为首次从该植物分离得到。     

Investigation of the oil extract of Schizandra seeds

A method for production and standardization of the oil extract of Schisandra chinensis seed has been developed based on isolation of the lignan fraction (with the major constituent schizandrol A) by aqueous ethanol (20%) and spectrophotometric assay. Solutions used for the quantitative assay are concentrated and then used for TLC (qualitative analysis). HPLC data showed that the concentration of the lignan fraction (schizandrol A) amounts to 0.08–0.11%, which is close to that in commercial tincture (about 0.09%) and that the proposed oil extract can be used as a neurotonic stimulant in the same doses as the tincture. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 42, No. 3, pp. 28–31, March, 2008.     

Antiviral activity of an extract derived from roots of Eleutherococcus senticosus

A liquid extract from Eleutherococcus senticosus roots inhibited the productive replication of human rhinovirus (HRV), respiratory syncytial virus (RSV) and influenza A virus in cell cultures infected with these viruses, all of which belong to the RNA type viruses. Analysis of virus production after treatment of the infected cells using plaque-reduction assays showed a strong antiviral activity of the Eleutherococcus extract. In contrast, no effect was detected using the same protocol for cells infected with the DNA viruses, adenovirus (Adeno 5) or herpes simplex type 1 virus (HSV 1). Pre-treatment of cells did not inhibit either virus adsorption or virus replication. The results of the study demonstrate that the Eleutherococcus extract inhibited the replication of all RNA viruses studied so far. This antiviral activity remained stable under the conditions used for drug preparation and storage.     

Anti-inflammatory activity of an extract of Petasites hybridus in allergic rhinitis

Previous studies have suggested that histamine and leukotrienes (LTs) play an important pathobiological role in IgE-mediated allergic diseases. In vitro studies suggested that an extract of Petasites hybridus (Ze339) blocks LT synthesis in monocytes and granulocytes. Petasins are considered to be the pharmacologically active fraction within Ze339. Patients suffering from allergic rhinitis received three times a day two tablets of Ze339 standardized to 8 mg petasins within a time period of 1 week. After 5 days of treatment, Ze339 significantly improved primary end points, which were day- and nighttime nasal symptoms. Nasal resistance, which was measured by rhinomanometry, gradually decreased as a consequence of Ze339 treatment reaching normal levels after 5 days (rhinomanometry: from 403.5+/-62.0 to 844.8+/-38.8 ml). Levels of inflammatory mediators in nasal fluids and serum were measured 90 min after drug administration every day in the morning. After 5 days of treatment, a significant reduction of histamine (from 153.7+/-32.1 to 53.0+/-8.4 pg/ml) and LT levels (LTB4: from 313.1+/-46.5 to 180.6+/-32.2 pg/ml; cysteinyl-LT: from 137.0+/-42.2 to 70.1+/-16.5 pg/ml) could be observed. Moreover, quality-of-life scores significantly improved. The drug had no effect on the distribution of lymphocyte subpopulations in the blood as well as on the capacity of blood leukocytes to generate cytokines and lipid mediators. These results suggest that Ze339 is effective in treating allergic rhinitis patients by decreasing levels of nasal inflammatory mediators.     

Chemotherapy modulates the biological activity of breast cancer patients plasma: The protective properties of black chokeberry extract

In breast cancer patients (before and during anti-cancer therapy) oxidative/nitrative damage to various molecules is observed. Furthermore, anti-cancer treatments may also influence the hemostatic properties of blood platelets and plasma. The aim of our study was to assess the effect of oxidative/nitrative stress (estimated by measurements of the levels of carbonyl groups and 3-nitrotyrosine in proteins – ELISA and C-ELISA methods, respectively; lipid peroxidation and total antioxidant level – TAS) on the selected parameters of hemostatic activity of plasma (the process of fibrin polymerization and lysis) collected from breast cancer patients after surgery and after various phases of chemotherapy (doxorubicin and cyclophosphamide). Subsequently, we also evaluated the level of oxidative/nitrative stress and hemostatic activity in plasma from these patients in the presence of the commercial extract of Aronia melanocarpa (Aronox®) in vitro. Patients were hospitalized in Department of Oncological Surgery and Department of Chemotherapy in Medical University of Lodz, Poland. We observed increased levels of biomarkers of oxidative/nitrative stress in plasma from patients with breast cancer (before or after surgery and after various phases of chemotherapy) in comparison to healthy group. Our further experiments demonstrated the hemostatic activity of plasma from the investigated patients differs from hemostatic properties of plasma obtained from healthy volunteers. We also recognize the existence of a relationship between oxidative stress (measured by the level of carbonyl groups) and changes of hemostasis in breast cancer patients after I and IV phases of chemotherapy. Moreover, the obtained results showed that the commercial extract from A. melanocarpa berries significantly reduced, in in vitro system, the oxidative/nitrative stress and hemostasis changes in plasma from breast cancer patients, after surgery and different phases of chemotherapy. Considering the data presented in this study, we suggest that the oxidative/nitrative stress in plasma obtained from breast cancer patients (not only before or after the surgery, but also after various phases of doxorubicin and cyclophosphamide chemotherapy) may induce changes of hemostatic activity, which may contribute to thrombosis in these patients. Our results also suggest that the commercial extract of A. melanocarpa may be regarded as a promising new source of bioactive antioxidant natural compounds for breast cancer patients.