Effect of quercetin on platelet spreading on collagen and fibrinogen and on multiple platelet kinases

α₂β₁ and α_IIbβ₃ integrins, that support platelet adhesion to collagen and fibrinogen, respectively, share common signaling molecules. The effect of quercetin on platelet static adhesion to collagen and fibrinogen was assessed and correlated with its kinase inhibitory activity. Quercetin strongly abrogated PI3K and Src kinases, mildly inhibited Akt1/2, and slightly affected PKC, p38 and ERK1/2. Quercetin or the combined use of adenosine diphosphate and thromboxane A₂ inhibitors abrogated platelet spreading on these surfaces to a similar extent. We suggest that the inhibitory effect of quercetin on platelet kinases blocks early signaling events preventing a complete platelet spreading.     

In vitro suppression of quercetin on hypertrophy and extracellular matrix accumulation in rat glomerular mesangial cells cultured by high glucose

Quercetin's protective effects on the glomerulosclerosis of diabetic nephropathy (DN) in rat mesangial cells were investigated. The cell cycles, type IV collagen and laminin, TGF-β₁ mRNA, Smad 2/3 and Smad 7, and activities of cell antioxidases were measured. Compared with the high glucose group, quercetin may decrease the cell percentages of G₀/G₁ phase, Smad 2/3 expression, laminin and type IV collagen, and TGF-β₁ mRNA level significantly. The antioxidant capacity, the cell percentages of S phase and Smad 7 expression was significantly increased by quercetin. These results suggest that quercetin is a protective agent against glomerulosclerosis in DN.     

Effect of naturally occurring allyl and phenyl isothiocyanates in the inhibition of experimental pulmonary metastasis induced by B16F-10 melanoma cells

The effect of naturally occurring allyl and phenyl isothiocyanates in the inhibition of B16F-10 melanoma cells-induced metastasis has been studied in C57BL/6 mice. The two compounds were administered by three different modalities. Simultaneous administration of the compounds with tumour induction was found to produce significant reduction in the lung tumour nodule formation; of the two compounds studied, allyl isothiocyanate have shown to be more effective and it produced 93% inhibition of tumour nodules while phenyl isothiocyanate has an inhibition of 77.3%. Prophylactic administration also produces considerable effect but no effect was observed by their administration after the tumour development. Lung collagen hydroxyproline, lung uronic acid, lung hexosamine content, serum sialic acid and serum GGT levels were also estimated and the enhanced levels of these parameters in the control animals were found to be reduced by the simultaneous administration of these isothiocyanates; these data were also correlated with the inhibition of lung tumour nodules produced and the increase in life span of the animals.     

In vitro studies on the selective cytotoxic effect of crocetin and quercetin

Crocetin (5-20 microg/ml), quercetin (10-40 microg/ml), and cisplatin (60-180 microg/ml) used as a positive control drug, were tested against human rhabdomyosarcoma (RD) cells and African green monkey kidney (Vero) cells. The cell viability, morphological changes, and lactate dehydrogenase activity were assessed. RD cell growth was found to be inhibited dose dependently by the three tested compounds. Morphological observation by phase contrast microscopy revealed that both crocetin and quercetin caused intense damage only on the malignant (RD) cells, whereas mild toxic effect was seen with cisplatin also on normal (Vero) cells.     

Isoprenoid-substituted flavonoids from wood of Artocarpus heterophyllus on B16 melanoma cells: Cytotoxicity and structural criteria

As a result of cytotoxicity-guided fractionation, nine flavonoids, artocarpin (1), cudraflavone C (2), 6-prenylapigenin (3), kuwanon C (4), norartocarpin (5), albanin A (6), cudraflavone B (7), brosimone I (8) and artocarpanone (9) were identified from the methanol extract of the wood of Artocarpus heterophyllus, known commonly as Nangka in Indonesia. A structure–activity investigation of the effect of these isolated compounds (1–9) and structurally related compounds on B16 melanoma cells indicated that isoprenoid moiety substitutions in flavonoids enhance their cytotoxicity, and that the position of attachment and the number of isoprenoid-substituent moieties per molecule influence flavonoid cytotoxicity.     

Inhibitory components from the buds of clove (Syzygium aromaticum) on melanin formation in B16 melanoma cells

In the course to find a new whitening agent, we evaluated the methanol extract from bud of clove (Syzygium aromaticum) on melanin formation in B16 melanoma cells. Eugenol and eugenol acetate were isolated as the active compounds and showed melanin inhibition of 60% and 40% in B16 melanoma cell with less cytotoxicity at the concentration of 100 and 200 μg/mL, respectively. Furthermore, an essential oil prepared from the bud of clove, which contain eugenol and eugenol acetate as dominant components, showed melanin inhibition of 50% and 80% in B16 melanoma cells at the concentration of 100 and 200 μg/mL, respectively.     

Effect of Aerva lanata on solid tumor induced by DLA cells in mice

Aerva lanata whole plant was extracted with petroleum ether, methanol and acetone. The partially TLC-purified fraction (PEF) of petroleum ether extract was proved to be cytotoxic to Dalton's lymphoma ascites (DLA), Ehrlich ascites (EA) and B16F10 cell lines in vitro. Since PEF was found to be more cytotoxic to DLA cell lines, it was used to study the pharmacological effect and its potential to reduce solid tumor induced by DLA cell lines in mice. The result indicated that PEF significantly reduced the development of solid tumor in mice.     

Effect of <Emphasis Type="Italic">Pinus radiate</Emphasis> bark extracts with different molecular weight distributions on cell growth of NIH/3T3 fibroblasts and dendrite retraction of B16 melanoma cells

Hot water extract (HWE) of Pinus radiata bark was separated into monomeric polyphenol (MPP), oligomeric proanthocyanidin (OPA), and polymeric proanthocyanidin (PPA) fractions by monitored chromatography using a Sephadex LH 20 column and an UV detector at 250 nm. The effects of these fractions on NIH/3T3 fibroblasts and B16 melanoma cells were examined by evaluating cell viability, melanogenesis (melanin content), morphological changes, and tyrosinase inhibitory activity. The polyphenolic fractions had a proliferation effect on fibroblasts, with cell growth increasing significantly (P < 0.01) even at the high concentration of 1250 μg/ml. At 125 μg/ml, HWE, MPP, and OPA had no effect on melanogenesis, whereas PPA significantly upregulated melanogenesis (P < 0.05). Melanogenesis was significantly upregulated in melanoma cells treated with these fractions at the high concentration of 600 μg/ml (P < 0.01). B16 melanoma cells cultured with the proanthocyanidin (PA)-rich fractions (HWE, OPA, and PPA) showed marked dendrite retraction, leading to significant morphological transformation. OPA in particular showed colored adhesion on the surface of melanoma cells. All four fractions significantly inhibited mushroom tyrosinase activity when compared to arbutin and ascorbic acid 2-glucoside (P < 0.05). The tyrosinase inhibitory activity of OPA and PPA did not differ significantly (P = 0.11), indicating that the inhibitory effects had a low correlation with molecular weight distribution. The inhibition kinetics of PPA determined using a Lineweaver-Burk plot indicated that PPA is a noncompetitive inhibitor of l-3,4-dihydroxyphenylalanine oxidation by mushroom tyrosinase.     

滨海盐碱地刺槐生长数学模拟

通过对滨海盐碱地23年实生刺槐生长研究,进行树干解析,对刺槐树高、胸径和材积生长规律进行回归模拟。最优模拟方程为:H=-0.372+3.318*lnt;DH=e(-5.518+0.977/t);BV=e(-13.771-0.938/t)。与传统的S型生长曲线不同。并且通过树高、胸径和材积分别有序聚类,将H、DH、BV都分成三类。分析结果与模拟回归吻合较好。     

青钱柳叶提取物对Caco-2细胞二糖酶活性的抑制作用

采用Caco-2细胞模型,分析了青钱柳Cyclocarya paliurus叶水提物、醇提后的水提物、95%醇提物、乙酸乙酯萃取物和正丁醇萃取物5种不同提取物对Caco-2细胞活力的影响及对Caco-2细胞上麦芽糖酶、蔗糖酶、乳糖酶3种二糖酶活性的抑制作用。结果表明,5种不同提取物中除95%醇提物对Caco-2细胞活力产生一定影响外,其余4种提取物对Caco-2细胞基本无毒性,在200 mg·L^-1浓度提取物范围内培养24～72 h后细胞仍能保持较高活力;对3种二糖酶活性抑制作用效果最好的为醇提后的水提物,尤其是对蔗糖酶和乳糖酶的抑制作用更为明显,最高的抑制率分别达到76.35%和60.13%,其次为乙酸乙酯萃取物,对乳糖酶的抑制率最高达54.41%。从青钱柳叶不同方法提取物的制备流程说明多糖类或中等极性的黄酮甙类有可能是青钱柳叶中抑制二糖酶活性的主要组成成分。     

Effect of a standardized extract of red orange juice on proliferation of human prostate cells in vitro

A standardized extract of red orange juice (ROE) was shown to inhibit proliferation of fibroblast and epithelial prostate cells. These data suggest that the antiproliferative properties of ROE cannot be ascribed to cytotoxic effect and highlight its potential usefulness in the management of benign prostatic hyperplasia.     

Effect of Citrus bergamia juice on human neuroblastoma cells in vitro and in metastatic xenograft models

Neuroblastoma is the most common extracranial pediatric solid tumor with poor prognosis in children with disseminated stage of disease. A number of studies show that molecules largely distributed in commonly consumed fruits and vegetables may have anti-tumor activity. In this study we evaluate the effect of Citrus bergamia (bergamot) juice (BJ) in vitro and in a spontaneous metastatic neuroblastoma SCID mouse model. Qualitative and quantitative characterizations of BJ flavonoid fractions were performed by RP-HPLC/PDA/MS. We show that BJ significantly affects SK-N-SH and LAN-1 cell proliferation in vitro, but fails to reduce primary tumor weight in vivo. Moreover, BJ reduced cell adhesiveness and invasion of LAN-1 and SK-N-SH cells in vitro and the number of pulmonary metastases under consideration of the number of tumor cells in the blood in mice inoculated with LAN-1 cells in vivo. These effects without any apparent sign of systemic toxicity confirm the potential clinical interest of BJ and lay the basis for further investigation in cancer.     

Sulfated glycofuranans as inhibitors of melanoma lung metastasis

Chemically synthesized (1 5)--d-glucofuranan, (1 5)--d-galactofuranan, (1 5)--d-xylofuranan, (1 5)--L-arabinofuranan, natural xylan, and curdlan were sulfated to investigate their inhibitory activities on B16-BL6 lung metastasis and anticoagulant activities. (1 5)--d-Glucofuranan sulfate, (1 5)--d-galactofuranan sulfate, xylan sulfate, and curdlan sulfate had binding abilities with B16-BL6 melanoma lysate. The inhibitory activities of sulfated polysaccharides on B16-BL6 lung metastasis selected by heparin binding assay were in the order (1 5)--d-galactofuranan sulfate > (1 5)---d-glucofuranan sulfate > xylan sulfate curdlan sulfate. Furthermore, (1 5)--d-galactofuranan sulfate, (1 5)--d-glucofuranan sulfate, and xylan sulfate had not only high inhibitory activity on B16-BL6 lung metastasis but also low anticoagulant activity. The correlation between chemical structure and biological activity is discussed.Part of this paper was presented at the 10th International Synposium on Wood and Pulping Chemistry, Yokohama, Japan, June 1999     

Effect of salt on ROS homeostasis, lipid peroxidation and antioxidant mechanisms in Pinus pinaster suspension cells

? In the Pinus genus, information on the effectiveness of oxidative defence mechanisms during exposure to salt is lacking. The effect of salt stress imposition on ROS homeostasis was investigated using maritime pine (Pinus pinaster Ait.) suspension cells as a model system.

? Cells were maintained in MS-based medium, exposed to salt (50, 100 and 150 mM NaCl) and analysed for biomass production, evidencing a decreasing growth capacity. Use of 100 mM NaCl imposed severe salt stress without affecting cell viability, being chosen for subsequent studies on the ROS homeostasis of salt shock-treated suspension cells.

? Increased total ROS levels were evident on the second day of salt exposure, but a superoxide ion transient burst was immediately noticeable. Additionally, lipid peroxide formation seemed to correlate with superoxide ion breakdown. In-gel superoxide dismutase activity evidenced a FeSOD homodimer with strongly increasing activity between hours 12–48 of salt stress imposition. Subsequently, P. pinaster Fe-Sod1 and csApx1 genes were isolated from a cDNA library and expression was shown to increase within 12–24 h.

? Results show that severe salt treatment generates oxidative stress in P. pinaster cells despite the induction of antioxidant systems, and suggest a putative involvement of ROS in salt stress signalling.

     

Post-emergent herbicidal activity of cineole derivatives

Essential oils are being investigated as potential herbicides or to provide leads to new environmentally and socially acceptable herbicides. Novel hydroxy and ester derivatives of 1,8-cineole and 1,4-cineole were synthesised, by chemical and biological methods, and have shown pre-emergence herbicidal activity against annual ryegrass and radish. Effects on post-emergence activity of these derivatives, as well as 1,8-cineole, eucalyptus oil and the carboxylic acids from which the esters were derived, against annual ryegrass and radish, are reported here. Results suggest that reduced root and shoot growth observed in pre-emergence herbicidal bioassays were due to post-emergence activity rather than delayed germination. All tested substances had a dose-dependent, post-emergence herbicidal activity against annual ryegrass and radish with many derivatives showing improved activity relative to 1,8-cineole and high-cineole eucalyptus oil. However, results do not support the postulate that cineole esters would be more active than their respective carboxylic acid and the hydroxy cineole. Phytotoxicity of ester derivatives may be due to metabolic cleavage of the esters to the hydroxy cineole and carboxylic acid within the plant.     

茶皂素改性衍生物制备与应用研究进展

茶皂素是一种性能优良的天然非离子型表面活性剂,因其优良的物理性能、独特的化学结构及含有大量的活性基团,故能采用物理、化学方法对其进行改性处理,以制备茶皂素改性衍生物产品,这些产品可广泛应用于环境控制、表面活性剂、环保农药、阻燃剂等领域。为了拓宽茶皂素应用研究的新领域,文中简述了国内外对茶皂素单体结构的研究情况,介绍了几个利用茶皂素采用物理处理、化学改性等方法制备茶皂素改性衍生物的研究实例,阐述了茶皂素改性衍生产品的研究开发现状;并对以茶皂素为高产量林源生物质资源制备开发新型材料、功能产品的研究进行了初步的展望。     

Phytochemical potential of Eruca sativa for inhibition of melanoma tumor growth

Solvent extracts from the aerial and root parts and seed oil from E. sativa (rocket salad) were assayed for anticancer activity against melanoma cells. The seed oil (isothiocyanates rich) significantly (p < 0.01) reduced the tumor growth comparable to the control. Remarkably, the seed oil inhibited melanoma growth and angiogenesis in mice without any major toxicity. The findings qualify seed oil for further investigations in the real of cancer prevention and treatment.     

Isolation and structural elucidation of 3,4',5,7-tetraacetyl quercetin from Adina cordifolia (Karam ki Gaach)

3,4',5,7-tetraacetyl quercetin (1) was isolated from the heartwood of Adina cordifolia. The structure was elucidated on the basis of spectral evidence.     

Phytic acid enhances the oral absorption of isorhamnetin,quercetin, and kaempferol in total flavones of Hippophae rhamnoides L.

AimTotal flavones of Hippophae rhamnoides L. (TFH) have a clinical use in the treatment of cardiac disease. The pharmacological effects of TFH are attributed to its major flavonoid components, isorhamnetin, kaempferol, and quercetin. However, poor oral bioavailability of these flavonoids limits the clinical applications of TFH. This study explores phytic acid (IP₆) enhancement of the oral absorption in rats of isorhamnetin, kaempferol, and quercetin in TFH.MethodsIn vitro Caco-2 cell experiments and in vivo pharmacokinetic studies were performed to investigate the effects of IP₆. The aqueous solubility and lipophilicity of isorhamnetin, quercetin, and kaempferol were determined with and without IP₆, and mucosal epithelial damage resulting from IP₆ addition was evaluated by MTT assays and morphology observations.ResultsThe P_app of isorhamnetin, kaempferol, and quercetin was improved 2.03-, 1.69-, and 2.11-fold in the presence of 333 μg/mL of IP₆, respectively. Water solubility was increased 22.75-, 15.15-, and 12.86-fold for isorhamnetin, kaempferol, and quercetin, respectively, in the presence of 20 mg/mL IP₆. The lipophilicity of the three flavonoids was slightly decreased, but their hydrophilicity was increased after the addition of IP₆ in the water phase as the logP values of isorhamnetin, kaempferol, and quercetin decreased from 2.38 ± 0.12 to 1.64 ± 0.02, from 2.57 ± 0.20 to 2.01 ± 0.04, and from 2.39 ± 0.12 to 1.15 ± 0.01, respectively. The absorption enhancement ratios were 3.21 for isorhamnetin, 2.98 for kaempferol, and 1.64 for quercetin with co-administration of IP₆ (200 mg/kg) in rats. In addition, IP₆ (200 mg/kg, oral) caused neither significant irritation to the rat intestines nor cytotoxicity (400 μg/mL) in Caco-2 cells.ConclusionsThe oral bioavailability of isorhamnetin, kaempferol, and quercetin in TFH was enhanced by the co-administration of IP₆. The main mechanisms are related to their enhanced aqueous solubility and permeability in the presence of IP₆. In summary, IP₆ is a potential absorption enhancer for pharmaceutical formulations that is both effective and safe.     

造林方式对油松造林效果的影响

为探索适合辽西半干旱区油松的最佳造林方式,对容器苗造林、塑料袋保苗造林、裸根造林3种方式进行比较试验。结果表明:容器苗造林方式下苗木保水性好,造林的成活率及保存率最高,造林的成本显著低于裸根造林;塑料袋保苗造林方式下苗木的保水性、成活率等均好于裸根造林方式,其造林成本最低。