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1.Evaluation of Antitumor Activity of Peptide Extracts from Medicinal Plants on the Model of Transplanted Breast Cancer in CBRB-Rb(8.17)1Iem Mice.

[Article in English, Russian]

Tepkeeva II, Moiseeva EV, Chaadaeva AV, Zhavoronkova EV, Kessler YV, Semushina SG, Demushkin VP.

M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Organic Biochemistry, Russian Academy of Sciences, Moscow, Russia.

We studied antitumor effects of peptide extracts from plants on slowly growing mammary adenocarcinoma in CBRB-Rb(8.17)1Iem mice used as a model of breast cancer in humans. The antitumor effect of a single injection of the test peptides was evaluated by the delay of the appearance and growth of palpable breast cancer in mice over 4 weeks. Peptides from Hypericum perforatum and a mixture of Chelidonium majus L., Inula helenium L., Equisetum arvense L., and Inonotus obliquus exhibited maximum activity. Peptide extracts from Frangula alnuc Mill. and Laurus nobilis L. were less active. No antitumor effect of Camelia sinesis Kuntze was detected.

PMID: 19110595 [PubMed - in process]

2. Inulavosin, a Melanogenesis Inhibitor, Leads to Mistargeting of Tyrosinase to Lysosomes and Accelerates its Degradation.

Fujita H, Motokawa T, Katagiri T, Yokota S, Yamamoto A, Himeno M, Tanaka Y.

1Division of Pharmaceutical Cell Biology, Graduate School of Pharmaceutical Sciences, Kyushu University, Higashi-ku, Fukuoka, Japan.

The melanosome is a highly specialized organelle where melanin is synthesized. Tyrosinase and tyrosinase-related protein-1 (Tyrp1) are major melanosomal membrane proteins and key enzymes for melanin synthesis in melanocytes. Inulavosin, a melanogenesis inhibitor isolated from Inula nervosa (Compositae), reduced the melanin content without affecting either the enzymatic activities or the transcription of tyrosinase or Tyrp1 in B16 melanoma cells. To our knowledge, this inhibitor is previously unreported. Electron-microscopic analyses revealed that inulavosin impaired late-stage development of melanosomes (stages III and IV), in which melanin is heavily deposited. However, it did not alter the early stages of melanosomes (stages I and II), when filamentous structure is observed. Immunofluorescence analyses showed that tyrosinase, but not Tyrp1, was specifically eliminated from melanosomes in cells treated with inulavosin. Unexpectedly, inulavosin specifically accelerated the degradation of tyrosinase but not other melanosomal/lysosomal membrane proteins (Tyrp1, Pmel17, and LGP85). The degradation of tyrosinase induced by inulavosin associated with lysosomes but not the proteasome. Interestingly, lysosomal protease inhibitors restored the melanogenesis but not the targeting of tyrosinase to melanosomes in the cells treated with inulavosin. Instead, colocalization of tyrosinase with lysosome-associated membrane protein-1 at late endosomes/multivesicular bodies and lysosomes was accentuated. Taken together, inulavosin inhibits melanogenesis as a result of mistargeting of tyrosinase to lysosomes.Journal of Investigative Dermatology advance online publication, 25 December 2008; doi:10.1038/jid.2008.376.

PMID: 19110539 [PubMed - as supplied by publisher]

3. Apoptosis inducement of bigelovin from Inula helianthus-aquatica on human Leukemia U937 cells.

Zeng GZ, Tan NH, Ji CJ, Fan JT, Huang HQ, Han HJ, Zhou GB.

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650204, China.

Inula helianthus-aquatica C. Y. Wu is a traditional medicinal plant used to treat some cancers in folk herbal medicine of Yunnan, China. Bigelovin, a sesquiterpene lactone isolated from this herb, potently inhibits the growth of a panel of eight cancer cell lines, especially in human monoblastic leukemia U937 cells with an IC(50) value of 0.47 microM. Characteristic morphological features of apoptosis were observed in U937 cells treated with bigelovin. Annexin V and nuclear DNA content distribution assays showed that the percentage of Annexin V positive cells increased to 8.86% (24 h) with 1 microM bigelovin treatment, and cells treated with bigelovin at this concentration apparently arrested at G(0)/G(1) phase compared with the control. These data suggested that cytotoxic effect of bigelovin on U937 cells involves induction of apoptosis, and the cell cycle is arrested at G(0)/G(1) phase. Copyright (c) 2008 John Wiley & Sons, Ltd.

PMID: 19107858 [PubMed - as supplied by publisher]

4. Chemical constituents and pharmacological properties of Radix Inulae.

Huo Y, Shi HM, Wang MY, Li XB.

School of Pharmacy, Shanghai Jiao Tong University, Shanghai, People's Republic of China.

Radix Inulae is used as a gastric and antibacterial agent in traditional Chinese and Tibetan medicines. Most of its chemical constituents have been identified and include a series of sesquiterpenes with various carbon skeletons such as: eudesmanolide, elemanolide, germacranolide, sesquicaranolide, guaianolide and humulane. Certain organic solvent fractions and sesquiterpenes from Radix Inulae have been found to significantly inhibit the growth of tumor cell strains in vitro. They also show antibacterial, cardiovascular and hypoglycaemic as well as insulin-sensitization activities. The present review summarizes research on the chemistry and biological activity of Radix Inulae.

Publication Types: PMID: 18972829 [PubMed - indexed for MEDLINE]

5. Separation and determination of alantolactone and isoalantolactone in traditional Chinese herbs by capillary electrophoresis.

Ketai W, Huitao L, Yunkun Z, Xingguo C, Zhide H, Yucheng S, Xiao M.

Department of Chemistry, Lanzhou University, Lanzhou 730000, People's Republic of China.

A simple micellar electrokinetic chromatography (MEKC) method, using a 20 mM borate buffer (pH 8.0) with 25 mM SDS in the presence of 10% (V/V) methanol, was established for the identification and determination of two isomers, alantolactone (AL) and isoalantolactone (IAL), in the extracts of Inula helenium L. and Inula racemosaHook f. Regression equations revealed linear relationships (correlation coefficients: 0.9990 for AL, 0.9991 for IAL) between the peak area of AL and IAL and their concentration. The relative standard deviations of the migration time and peak area of the two constituents were 1.51, 1.62 and 2.01, 1.98%, respectively. The recoveries of the two constituents ranged between 95-105% for AL and 93-108% for IAL.

PMID: 18968060 [PubMed - in process]

6. Control of Plant Diseases by Extracts of Inula viscosa.

Wang W, Ben-Daniel BH, Cohen Y.

ABSTRACT Leaves of Inula viscosa were collected from the field, dried, and extracted with a mixture of acetone and n-hexane. The oily, water-insoluble pastes obtained after evaporation of the solvents were used for the control of foliar diseases in growth chambers. The pastes, either dissolved in acetone or emulsified in water, effectively controlled downy mildew of cucumber, late blight of potato or tomato, powdery mildew of wheat, and rust of sunflower. Mean effective dose (concentration) required for 90% inhibition of disease values for acetone solutions and water emulsions ranged from 0.68 to 1.02% and 0.65 to 1.00% (wt/vol), respectively. Dry matter content in fresh leaves, paste-extract yield in dry leaves, and disease control efficacy of paste extracts were similar in leaves of I. viscosa collected during May to October, suggesting that, for practical use, harvests can be conducted during most of the growing season. The results show that I. viscosa may be used as an herbal source for fungicidal preparations against foliar diseases caused by pathogens belonging to the families Oomycetes, Ascomycetes, and Basidiomycetes.

PMID: 18943791 [PubMed - in process]

7. Extracts of Inula viscosa Control Downy Mildew of Grapes Caused by Plasmopara viticola.

Cohen Y, Wang W, Ben-Daniel BH, Ben-Daniel Y.

ABSTRACT The oily paste extracts of Inula viscosa leaves made with organic solvents were effective in controlling downy mildew caused by Plasmopara viticola in detached leaf tissues of grapes in growth chambers. Thin-layer chromatography of such extracts revealed the presence of 11 Rf regions of which four contained highly effective compounds against the disease. Two major inhibitory compounds, each comprising 10.6% of the total paste weight, were identified as tomentosin and costic acid. An emulsified concentrate formulation of the oily paste extracts provided excellent activity against the disease in the field. The effective dose (concentration) required for 90% control of the disease in treated shoots in the field was below 0.125% (paste in water). No seasonal fluctuations were observed in the control efficacy of six extracts made from I. viscosa leaves harvested during the period of May to July. In whole vines, treated and artificially inoculated, the paste concentration required for 90% control of the disease ranged between 0.30 to 0.37%, whereas in naturally infected vines it was 0.58%. It appears that I. viscosa is a valuable source for fungicidal preparations against downy mildew of grapes. This is the first report on the control of a disease with I. viscosa extracts under field conditions.

PMID: 18943424 [PubMed - in process]

.8. 1,6-O,O-diacetylbritannilactones inhibits IkappaB kinase beta-dependent NF-kappaB activation.

Liu YP, Wen JK, Wu YB, Zhang J, Zheng B, Zhang DQ, Han M.

Department of Biochemistry and Molecular Biology, Institute of Basic Medicine, Hebei Medical University, Shijiazhuang 050017, PR China; Department of Pathology, The Forth Hospital of Hebei Medical University, Shijiazhuang 050017, PR China.

To determine the chemical constituents responsible for pharmacological effects of Inula britannica-F., three specific sesquiterpene lactones in Inula britannica were isolated from chloroform extract and identified, including britannilactone (BL), 1-O-acetylbritannilactone (ABLO), and 1,6-O,O-diacetylbritannilactone (ABLOO). Electrophoretic mobility shift assay (EMSA) was performed to detect the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65. The expressions of IkappaBalpha, pIkappaBalpha, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), IkappaB kinase alpha/beta (IKKalpha/beta) and NF-kappaB kinase (NIK) were detected by Western blot and RT-PCR. We found that acetyl side groups enhanced the inhibitory action of the agents on LPS/IFN-gamma-induced iNOS and COX-2 expression. Their inhibiting activity was positive correlation with the acetyl side group number. The effects of LPS/IFN-gamma were reversed by ABLOO, and BL without acetyl side groups showed only a weak inhibitory action. Further study indicated that ABLOO markedly inhibited the phosphorylation of IKKbeta down to based level, but not IKKalpha, corresponding with decreased in IkappaBalpha degradation and phosphorylation induced by LPS/IFN-gamma, resulting in the suppression of NF-kappaB nuclear translocation and activity. These results suggest that the acetyl moieties add to the lipophilicity, and consequently enhance cellular penetration, so that ABLOO possess the most anti-inflammatory effect and may be a potent lead structure for the development of therapeutic and cytokine-suppressing remedies valuable for the treatment of various inflammatory diseases.

PMID: 18926678 [PubMed - as supplied by publisher]

9. Complete assignments of 1H and 13C NMR spectral data for three sesquiterpenoids from Inula helenium.

Huo Y, Shi H, Wang M, Li X.

School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, PR China.

The complete assignments of all the (1)H and (13)C NMR signals of three sesquiterpene lactones, 4-oxo-5(6),11-eudesmadiene-8,12-olide (1), 4-oxo-11-eudesmaene-8,12-olide (2) and (1(10)E)-5beta-Hydroxygermacra-1(10),4(15),11-trien-8, 12-olide (3), were carried out by various 2D NMR experiments. Compounds 1-3 were isolated from the roots of Inula helenium for the first time. Among them, 1 was identified as a new nor-sesquiterpene lactone, and 2 was isolated from a natural source for the first time. The (13)C-NMR data of compound 3 was also reported for the first time. Copyright (c) 2008 John Wiley & Sons, Ltd.

PMID: 18828151 [PubMed - indexed for MEDLINE]

10.Antioxidant activity of some Jordanian medicinal plants used traditionally for treatment of diabetes.

Al-Mustafa AH, Al-Thunibat OY.

Department of Biology, Faculty of Science, Mutah University, P.O. Box 7, Postal Code 61710, Mutah-Al-Karak, Jordan.

Medicinal plants are being used extensively in Jordanian traditional medicinal system for the treatment of diabetes symptoms. Twenty one plant samples were collected from different Jordanian locations and used for antioxidant evaluation. The level of antioxidant activity was determined by DPPH and ABTS assays in relation to the total phenolic contents of the medically used parts. The most frequently used plant parts as medicines were fruit, shoot and leaves. The total phenolic contents of methanol and aqueous extracts, from plants parts, ranged from 6.6 to 103.0 and 3.0 to 98.6 GAE mg g(-1) of plant part dry weight, respectively. DPPH-TEAC of the methanol extracts of plants parts were varied from 4.1 to 365.0 mg g(-1) of plant dry weight versus 0.6 to 267.0 mg g(-1) in aqueous extracts. Moreover, the mean values of ABTS*- (IC50) varied from 6.9 to 400.0 microg dry weight mL(-1) ABTS in methanol extracts versus 9.8 to 580.5 microg mL(-1) in aqueous extracts. According to their antioxidant capacity, the plants were divided into three categories: high (DPPH-TEAC > or = 80 mg g(-1) ), (i.e., Punica granatum peel, Quercus calliprinos leave, Quercus calliprinos fruit, Cinchona ledgeriana and Juniperus communis leave), moderate (DPPH-TEAC range 20-80 mg g(-1)) (i.e., Salvia fruticosa shoot, Crataegus azarolus stem, Crataegus azarolus leave, Varthemia iphionoides shoot, Artemisia herba-alba shoot, Thymus capitatus shoot, Morus nigra leaves and Arum palaestinum leaves) and low antioxidant plants (DPPH-TEAC < 20 mg g(-1)), (i.e., Matricaria aurea shoot, Artemisia judaica shoot, Teucrium polium shoot, Pinus halepenss pollen grains, Sarcopoterium spinosum root, Crataegus azarolus fruit, Inula viscose shoot and Achillea fragrantissima shoot). The antioxidant activity of these plant's extracts and their potential rule in radical scavenging agreed with their potential use by Jordanian population as a traditional anti-diabetic agents.

Publication Types:PMID: 18817155 [PubMed - indexed for MEDLINE]

11. Structural determination of three new eudesmanolides from Inula helenium.

Ma XC, Liu KX, Zhang BJ, Xin XL, Huang J.

School of Pharmaceutical Sciences, Dalian Medical University, Dalian 116027, PR China. maxc1978@sohu.com

Ten sesquiterpenens were isolated from Inula helenium. Among them, three eudesmanolides: 15-hydroxy-11betaH-eudesm-4-en-8beta,12-olide (1), 3alpha-hydroxy-11betaH-eudesm-5-en-8beta,12-olide (2) and 2beta, 11alpha-dihydroxy-eudesm-5-en-8beta,12-olide (3) are new compounds. Their chemical structures were determined by spectral methods including 2D NMR. 2008 John Wiley & Sons, Ltd.

Publication Types: PMID: 18767032 [PubMed - indexed for MEDLINE]
12. Comparison of the therapeutic effects of different compositions of muskone in the treatment of experimental myocardial infarct in rats and analgesia in mice.

Li Y, Zhang J, Li L.

Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing, China.

The aim of this study was to compare the therapeutic effects of muskone, a traditional preparation containing slender Dutchmanspipe root (MCS) used to treat angina pectoris and related conditions, muskone containing inula root (MCI) in place of MCS, and muskone (M) without either slender Dutchmanspipe root (S) or inula root (I) on acute myocardial infarct (AMI) in rats and the pain response in mice. The AMI model was established by ligating the left anterior descending coronary artery (LAD). The AMI rats were treated with MCS, MCI, M, S and I, respectively, before the surgical operation. Plasma endothelin (ET), 6-keto-prostaglandin F(1alpha) (6-keto-PGF(1alpha)), thromboxane (TXB(2)) and myocardial apoptosis were detected, the ratio of 6-keto-PGF(1alpha) level to TXB(2) level (6-keto-PGF(2alpha)/TXB(2)) was calculated, and the infarct size was determined. In the pain relieving study, the prophylactic treatments with MCS, MCI, M, S, I and aspirin were administered to the mice once a day for 5 days, the response latency and the number of abdominal contractions after the stimulus of intraperitoneal injection of acetic acid were recorded. The results show that MCS, MCI and M significantly ameliorated plasma ET, TXB(2), 6-keto-PGF(1alpha) and 6-keto-PGF(2alpha)/TXB(2) levels, reduced infarct size and opposed myocardial apoptosis. Simultaneously, they also significantly reduced the abdominal contractions and also prolonged the response latency induced by acetic acid in the mice. S and I only showed a degree of relieving pain, but their efficacy was weaker than that of MCS, MCI and M, and they had little cardioprotective effect. In conclusion, MCS, MCI and M had a significant cardioprotective and analgesic effect, and they had similar efficacy. S and I only had a secondary analgesic effect. Removing S from the MCS or replacing S with I did not influence the cardioprotective effect and analgesic effect.

Publication Types: PMID: 18729258 [PubMed - indexed for MEDLINE]

13. Identification of As accumulation plant species growing on highly contaminated soils.

Gisbert C, Almela C, Vélez D, López-Moya JR, de Haro A, Serrano R, Montoro R, Navarro-Aviñó J.

Department of Stress Biology, IBMCP, CSIC, Valencia, Spain.

Soils from the alluvial flats of the Turia River, Valencia, Spain, which were highly contaminated by decades of industrial activity, were surveyed for native plant species that could be candidates useful in phytoremediation. Concentrations of heavy metals and arsenic (As) in soils reached 25,000 mg Kg(-1) Pb, 12,000 mg Kg(-1) Zn, 70 mg Kg(-1) Cd, and 13500 mg Kg(-1) As. The predominant vegetation was collected and species identified. Soil samples and the corresponding plant shoots were analyzed to determine the amount of As accumulated by the various plant species. Several were able to tolerate more than 1000 mg Kg(-1) As in the soil. Bassia scoparia (Chenopodiaceae) survive in soil with 8375 mg Kg(-1) As. Arsenic accumulation in shoots of the various plant species investigated ranged from 0.1 to 107 mg Kg(-1) dw. Bassia scoparia (Chenopodiaceae), Inula viscosa (Asteraceae), Solanum nigrum (Solanaceae), and Hirschfeldia incana (Brassicaceae) had the highest values for As accumulation.

Publication Types: PMID: 18710094 [PubMed - indexed for MEDLINE]
14. Nrf2-mediated induction of detoxifying enzymes by alantolactone present in Inula helenium.

Seo JY, Lim SS, Kim JR, Lim JS, Ha YR, Lee IA, Kim EJ, Park JH, Kim JS.

Department of Animal Science and Biotechnology, Kyungpook National University, Deagu 702-701, Republic of Korea.

Our previous study showed that a methanol extract of Inula helenium had the potential to induce detoxifying enzymes such as quinone reductase (QR) and glutathione S-transferase (GST) activity. In this study the methanol extract was further fractionated using silica gel chromatography and vacuum liquid chromatography, to yield pure compounds alantolactone and isoalantolactone as QR inducers. Alantolactone caused a dose-dependent induction of antioxidant enzymes including QR, GST, gamma-glutamylcysteine synthase, glutathione reductase, and heme oxygenase 1 in hepa1c1c7 mouse hepatoma cells. The compound increased the luciferase activity of HepG2-C8 cells, transfectants carrying antioxidant response element (ARE)-luciferase gene, in a dose-dependent manner, suggesting ARE-mediated transcriptional activation of antioxidant enzymes. Alantolactone also stimulated the nuclear accumulation of Nrf2 that was inhibited by phosphatidylinositol 3-kinase (PI3K) inhibitors. In conclusion, alantolactone appears to induce detoxifying enzymes via activation of PI3K and JNK signaling pathways, leading to translocation of Nrf2, and subsequent interaction between Nrf2 and ARE in the encoding genes.

Publication Types:PMID: 18702092 [PubMed - indexed for MEDLINE]

15. Inula crithmoides extract protects against ochratoxin A-induced oxidative stress, clastogenic and mutagenic alterations in male rats.

Abdel-Wahhab MA, Abdel-Azim SH, El-Nekeety AA.

Food Toxicology and Contaminants Department, National Research Centre, El-Tahrir Street, Dokki, Cairo 12622, Egypt. mosaad_abdelwahhab@yahoo.com

Ochratoxin A (OTA) is a mycotoxin often found in cereals and agricultural products. There is unequivocal evidence of renal carcinogenicity of OTA in male rats, although the mechanism of action is unknown. Several reports suggest that exposure to OTA resulted in oxidative stress, genotoxicity and DNA damage. Therefore, the aim of the current study was to evaluate the protective effects of aqueous extract of Inula crithmoides growing in Egypt against OTA-induced mutagenicity and oxidative stress. Forty male Sprague-Dawley rats were divided into four groups and treated for 15 days as follows: control group and the groups treated with OTA (3 mg/kg b.w), I. crithmoides extract alone (370 mg/kg b.w) and OTA+I. crithmoides extract. Blood and tissue samples were collected for different biochemical analyses. Bone marrow micronucleus test and blood for random amplified polymorphism DNA-PCR (RAPD-PCR) method were performed to assess the antigenotoxic effect of the extract. The results indicated that OTA induced toxicological effects typical to those reported in the literature and increased the frequencies of MnPCEs in bone marrow. The RAPD-PCR analysis revealed the appearance of new bands in DNA resulting from genetic alteration. The extract alone was safe and succeeded in counteracting the oxidative stress and protect against the cytotoxicity resulting from OTA.

PMID: 18694774 [PubMed - indexed for MEDLINE]

16. Authentication of Saussurea lappa, an endangered medicinal material, by ITS DNA and 5S rRNA sequencing.

Chen F, Chan HY, Wong KL, Wang J, Yu MT, But PP, Shaw PC.

Department of Biochemistry, The Chinese University of Hong Kong, Shatin, Hong Kong, People's Republic of China.

Wild SAUSSUREA LAPPA in the family Asteraceae is a highly endangered plant. On the other hand, the dried root of cultivated S. LAPPA (Radix Aucklandia, Muxiang) is a popular medicinal material for treating various gastrointestinal diseases. In the market, several medicinal plants including VLADIMIRIA BERARDIOIDEA, V. SOULIEI, V. SOULIEI var. MIRABILIS, INULA HELENIUM and I. RACEMOSA in the family Asteraceae and ARISTOLOCHIA DEBILIS in the family Aristolochiaceae have the trade name of Muxiang. To manage the concerned medicinal material, we investigated if the ITS and 5S rRNA intergenic spacers are effective for discriminating S. LAPPA from its substitutes and adulterants. Sequencing results showed that the similarities of ITS-1, ITS-2 and 5S rRNA intergenic spacers among S. LAPPA and related species were 56.3 - 97.8 %, 58.5 - 97.0 %, and 26.4 - 77.9 %, respectively. The intraspecific variation was much lower. There are also several unique changes in the S. LAPPA sequences that may be used as differentiation markers.

Publication Types: PMID: 18537077 [PubMed - indexed for MEDLINE]

17. [Contribution to the study of land-use dynamics in the plains of Macta (Algeria) with the aid of remote sensing and GIS]

[Article in French]

Sitayeb T, Benabdeli K.

Laboratoire de recherche sur les systèmes biologiques et la géomatique, centre universitaire de Mascara, BP 763, Mascara 29000, Algeria. sitayebt@yahoo.fr

The plains of Macta, where the Macta marshes are located, form a wetland with particular ecological characteristics in the Maghreb and are subject to distinct land use dynamics. The plant formations are exposed to multiple forms of degradation, primarily due to climate (period of dryness) and to increasing anthropogenic activities in the area. The new methods of breeding and cultivation contribute to ongoing degradation in this natural ecosystem, with a deterioration of the wetland's biological potentialities. With the aim of safeguarding Macta's marshes, a better knowledge of vegetation distribution patterns and dynamics, together with the interpretation of the remote sensing data and GIS, makes it possible to consider programmes of natural environment restoration and sustainable management. The results of land-use dynamics analysis show a decline in agricultural land use from 33,000 ha in 1958 to 21,000 ha in 2005. Halophytic vegetation currently occupies 47,000 ha, while in 1958 it occupied only 27,000 ha. Tamarix, Inula, Joncus and Scirpus species are experiencing a decrease in surface cover, while Salicornia, Suaeda, and Atriplex are extending their area. To cite this article:

Publication Types: PMID: 18510999 [PubMed - indexed for MEDLINE]

18. Development of a natural preservative system using the mixture of chitosan-Inula helenium L. extract.

Seo SB, Ryu CS, Ahn GW, Kim HB, Jo BK, Kim SH, Lee JD, Kajiuchi T.

Department of International Development Engineering, Tokyo Institute of Technology, 2-12-1 Ookayama, Meguro-ku, Tokyo 152-8552, Japan.

The aim of this study was to develop a new natural preservative system making up for the weak points of chitosan as a preservative. As reported in a previous manuscript (20th IFSCC Congress, Cannes, France, 1998), the minimum inhibitory concentrations (MICs) of water-soluble chitosan against bacteria and yeast were 0.9-3.0 mg mL(-1), whereas MICs of chitosan against Aspergillus niger were over 5.0 mg mL(-1). However, the result of recent study showed that the MICs of Inula helenium L. extract against A. niger were below 1.0 mg mL(-1). Thus, we could develop a new preservative system containing both chitosan and I. helenium L. extract named CI-mixture. MICs of CI-mixture against bacteria and fungi (yeast and mould) were 2.0-4.0 mg mL(-1). When 10.0% of the mixture (the ratio of chitosan to I. helenium L. extract = 7.5% : 2.5%) was applied to cosmetic formulae such as skin lotion, milk lotion, cream and pack, it revealed appropriate preservative efficacy. Our result of the patch test also showed that this preservative system reduced skin irritation by about 30-50%, as compared to the organic preservative system. Therefore, the good natural preservative system including chitosan and Inula helenium L. extract could be incorporated in cosmetic formulations.

PMID: 18498511 [PubMed - in process]

20. Investigation on bioavailability of some essential and toxic elements in medicinal herbs.

Razić S, Dogo S, Slavković L.

Institute of Analytical Chemistry, Faculty of Pharmacy, University of Belgrade, P.O. Box 146, 11221, Belgrade, Serbia. snsn@sezampro.yu

Trace and major elements were determined in medicinal herbs (Cynara scolymus, Matricaria chamomilla, Artemisia absinthium L., Achillea millefolium, and Inula britannica) as well as in rhizosphere soil samples. Based on the results obtained after microwave-acid-assisted digestion (nitric acid + hydrogen peroxide) and single-step extraction (ammonium acetate), the real and potential acidity and redox potential of the soils, uptake, mobility, and bioavailability of potassium, calcium, magnesium, iron, manganese, copper, zinc, nickel, chromium, lead, and cadmium are discussed. By calculating the bioconcentration factors and their deviation from the recommended values, elevated concentrations, were explained in terms of contamination and pollution. The concentrations measured in both plants and soil samples were below maximum allowable concentration ranges considered for the European Union.

Publication Types: PMID: 18408895 [PubMed - indexed for MEDLINE]

21. Quantitative somatic sensory testing and functional imaging of the response to painful stimuli before and after cingulotomy for obsessive-compulsive disorder (OCD).

Greenspan JD, Coghill RC, Gilron I, Sarlani E, Veldhuijzen DS, Lenz FA.

Department of Biomedical Sciences, School of Dentistry, and Program in Neuroscience, University of Maryland, Baltimore, MD, USA.

The middle cingulate cortex (MCC) has been implicated in pain processing by studies of cingulotomy for chronic pain and imaging studies documenting increased MCC blood flow in response to acute pain. The only previous report of quantitative sensory testing following cingulotomy described increased intensity and unpleasantness ratings of painful hot and cold stimuli in a single patient with psychiatric disease. We now report a case in which perception of pain and temperature was assessed before and after cingulotomy for obsessive-compulsive disorder (OCD). Positron emission tomographic (PET) studies of the blood flow response to acute pain were carried out using a single subject design which allowed for statistical evaluation of postoperative blood flow changes in this case. Postoperatively, the patient demonstrated increased intensity and unpleasantness ratings of painful thermal waterbath stimuli. The PET studies demonstrated preoperative contact heat pain-evoked activation of the bilateral MCC/SMA (supplementary motor area) and the left (contralateral) fronto-parietal operculum. Postoperative pain-evoked activation was demonstrated in the right (ipsilateral) parasylvian cortex but not of the MCC/SMA. Prior studies of forebrain lesions, and of cortical synchrony during the application of painful stimuli suggest the presence of functional connectivity between components of the MCC/SMA and the fronto-parietal opercula. Therefore present results suggest that cingulate lesions disinhibit ipsilateral parasylvian cortex and so are independent evidence of functional connectivity between these cortical areas, the defining characteristic of modules in a pain network.

Publication Types: PMID: 18328752 [PubMed - indexed for MEDLINE]
22. Inositol angelates from the whole herb of Inula cappa.

Zou ZM, Xie HG, Zhang HW, Xu LZ.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100094, China. zhongmeizou@hotmail.com

A new inositol derivative, cis-1,2,3,5-trans-4,6-inositol-2,3,6-triangelate(1) along with the known l-inositol-1,2,3,5-tetra angelate(2), was isolated from the ethanolic extract of the whole plant Inula cappa and identified on the spectroscopic analysis.

PMID: 18314278 [PubMed - indexed for MEDLINE]

23[Nephrotoxicity of Radix Aristolochice and it's substitution material Radix Inulae in rats]

[Article in Chinese]

Qiao HX, Liu YY, Wu LM, Li LD.

Institute of Chinese Herb Medicine, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

OBJECTIVE: To evaluate the toxicity of Radix Aristolochiae and Radix Inulae, and to supply the toxicity experimental data that Radix Inulae supersedes Radix Aristolochiae in clinic. METHOD: A long dose of Radix Aristolochice and Radix Inulae was given intragastrically to rats for six months, then drug withdrawal for a month. The hematology and biochemical indicators were measured, and the pathologic changes of kidney, liver, stomach and urinary bladder were examined. RESULT: The rats of Radix Aristolochice showed serious toxic responses of renal tubule atrophy and necrosis, meanwhile, the levels of BUN, Cr and NAG were increased obviously. Hepatonecrosis, renal tubular necrosis, gastric carcinoma and bladder carcinoma were discovered with pathologic assaying. But the rats of Radix Inulae did not. CONCLUSION: Radix Aristolochiae could damage kidney and liver, and cause gastric carcinoma and bladder carcinoma by intensive toxicity. Radix Inulae could take the place of Radix Aristolochiae to use in clinic.

Publication Types: PMID: 18161302 [PubMed - indexed for MEDLINE]
24. Authentication of Radix Aucklandiae and its substitutes by GC-MS and hierarchical clustering analysis.

Shum KC, Chen F, Li SL, Wang J, But PP, Shaw PC.

Department of Biochemistry, Institute of Chinese Medicine, The Chinese University of Hong Kong, Shatin, NT, Hong Kong, China.

Radix Aucklandiae (Muxiang in Chinese), the dried root of Aucklandia lappa, is used as a medicinal material for digestive system disorders in traditional Chinese medicine for centuries. Owing to the similarity of morphologies and trade names, Radix Vladimiriae (Chuan-Muxiang), the roots of Vladimiria souliei and V. souliei var. cinerea, and Radix Inulae (Tu-Muxiang), the roots of Inula helenium and Inula racemosa, as well as the renal toxic aristolochic acid containing Radix Aristolochiae (Qing-Muxiang), the roots of Aristolochia debilis and Aristolochia contorta, are often used confusedly as the substitutes of Radix Aucklandiae. In order to ensure the effective and safe utility of Radix Aucklandiae, a GC-MS method was developed to generate the chemical profiles of essential oils of Radix Aucklandiae and its substitutes. In addition, hierarchical clustering analysis was used to compare the similarities of these chemical profiles. It was found that all the samples of A. lappa have similar chemical profiles and were clustered into one group, while the samples of Radix Vladimiriae, Radix Inulae, and Radix Aristolochiae were clustered into their own independent groups, respectively, suggesting that together with hierarchical clustering analysis, chemical profiles of essential oils generated by GC-MS could objectively discriminate Radix Aucklandiae from its common substitutes.

Publication Types:PMID: 18004716 [PubMed - indexed for MEDLINE]

25. Antiviral activity of some Tunisian medicinal plants against Herpes simplex virus type 1.

Sassi AB, Harzallah-Skhiri F, Bourgougnon N, Aouni M.

Laboratoire des Maladies Transmissibles et Substances Biologiquement Actives, Faculte de Pharmacie, rue Avicenne, Monastir, Tunisia. ahlem_ben_sassi@yahoo.fr

Fifteen species of Tunisian traditional medicinal plants, belonging to 10 families, were selected for this study. They were Inula viscosa (L.) Ait and Reichardia tingitana (L.) Roth ssp. discolor (Pom.) Batt. (Asteraceae), Mesembryanthemum cristallinum L. and M. nodiflorum L. (Aizoaceae), Arthrocnemum indicum (Willd.) Moq., Atriplex inflata Muell., A. parvifolia Lowe var. ifiniensis (Caball) Maire, and Salicornia fruticosa L. (Chenopodiaceae), Cistus monspeliensis L. (Cistaceae), Juniperus phoenicea L. (Cupressaceae), Erica multiflora L. (Ericaceae), Frankenia pulverulenta L. (Frankeniaceae), Hypericum crispum L. (Hypericaceae), Plantago coronopus L. ssp. eu-coronopus Pilger var. vulgaris G.G. (Plantaginaceae) and Zygophyllum album L. (Zygophyllaceae). Fifty extracts prepared from those plants were screened in order to assay their antiviral activity against Herpes simplex virus type 1 (HSV-1), using neutral red incorporation. Extracts from eight plants among these 15 showed some degree of antiviral activity, while the methanolic extract of E. multiflora was highly active with EC(50) of 132.6 microg mL(-1). These results corroborate that medicinal plants from Tunisia can be a rich source of potential antiviral compounds.

PMID: 17999339 [PubMed - indexed for MEDLINE]

26. Induction of G2/M arrest and apoptosis by sesquiterpene lactones in human melanoma cell lines.

Rozenblat S, Grossman S, Bergman M, Gottlieb H, Cohen Y, Dovrat S.

The Mina & Everard Goodman Faculty of Life Sciences, Bar-Ilan University, Ramat-Gan 52900, Israel.

Malignant melanoma is a highly aggressive tumor which frequently resists chemotherapy, therefore, the search for new agents for its treatment is of great importance. In this study, we purified the sesquiterpene lactones (SLs), Tomentosin and Inuviscolide from Inula viscosa (Compositae) leaves and studied their anti-cancer potency against human melanoma cell lines in order to develop new agents for melanoma treatment. SLs inhibited the proliferation of three human melanoma cell lines: SK-28, 624 mel and 1363 mel in a dose-dependent manner. We further investigated SLs mechanism of action using SK-28 as a representative cell line model. SLs caused cell-cycle arrest at G(2)/M, accompanied by the appearance of a sub-G0 fraction, indicative of apoptotic cell death. Induction of apoptosis was further confirmed by changes in membrane phospholipids, changes in mitochondrial membrane potential (DeltaPsi) and by detection of Caspase-3 activity. Rapid inhibitory phosphorylation of Cdc2 (Thr14 and Tyr15) was seen early after treatment, followed by a later decrease in the expression level of both Cyclin b1 and Cdc2. Induction of p53 and p21(waf1) proteins and phosphorylation of p53 at Ser15 were also detected early after treatment. The anti-apoptotic proteins, p65 subunit of nuclear factor kappaB (NF-kappaB), and Survivin were reduced in a dose-dependent manner. Taken together, these changes partially explain the ability of the SLs to induce G(2)/M arrest and apoptosis. Induction of apoptosis by Tomentosin and Inuviscolide in human aggressive melanoma cell lines has high pharmacological value and implies that SLs might be developed as new agents for melanoma treatment.

Publication Types: PMID: 17919456 [PubMed - indexed for MEDLINE]

27. Acetylbritannilactone suppresses lipopolysaccharide-induced vascular smooth muscle cell inflammatory response.

Liu YP, Wen JK, Zheng B, Zhang DQ, Han M.

Department of Biochemistry and Molecular Biology, Institute of Basic Medicine, Hebei Medical University, No. 361, Zhongshan East Road, Shijiazhuang, 050017, PR China.

To investigate the mechanism of action by which a new anti-inflammatory active compound, 1-O-acetylbritannilactone (ABL) isolated from Inula britannica-F., inhibits inflammatory responses in vascular smooth muscle cells (VSMCs). Enzyme immunoassay was used to measure the levels of prostandin E(2) (PGE(2)) production. Immunocytochemistry staining and Western blot analysis were performed to detect the nuclear translocation of nuclear factor-kappaB (NF-kappaB) p65 and the expression of IkappaB-alpha, pIkappaB-alpha and cyclooxygenase-2 (COX-2). Electrophoretic mobility shift assays (EMSA) were used to detect DNA-binding activity of NF-kappaB in VSMCs. ABL (5, 10, 20 micrommol/l) had several concentration-dependent effects, including inhibition of lipopolysaccharide (LPS)-induced PGE(2) production and COX-2 expression, and blockade of NF-kappaB activation and translocation. These effects were owing to reductions in IkappaB-alpha phosphorylation and degradation induced by LPS. In addition, ABL directly inhibited the binding of active NF-kappaB to specific DNA cis-element. These results indicate that ABL is a potent inhibitor of LPS-stimulated VSMC inflammatory responses through blockade of NF-kappaB activity and inhibition of inflammatory gene COX-2 expression.

Publication Types: PMID: 17915214 [PubMed - indexed for MEDLINE]

28. Induction of detoxifying enzyme by sesquiterpenes present in Inula helenium.

Lim SS, Kim JR, Lim HA, Jang CH, Kim YK, Konishi T, Kim EJ, Park JH, Kim JS.

Regional Innovation Center and Department of Food Science and Nutrition, Hallym University, Chuncheon, Republic of Korea.

Our previous study showed that the methanolic extract of Inula helenium (elecampane) had the potential to induce detoxifying enzymes such as quinine reductase (QR) and glutathione S-transferase. In this study we further fractionated the methanolic extract into hexane-, dichloromethane-, butanol-, and water-soluble fractions according to polarity. The hexane fraction showed the highest QR-inducing activity and also induced glutathione S-transferase in a dose-dependent manner. Its potential to induce the reporter activity suggested an antioxidant response element-mediated mechanism of action in the induction of phase II detoxifying enzymes. Intraperitoneal injection of the hexane fraction of I. helenium into ICR mice caused a significant increase of QR activity in liver, kidney, small intestine, and stomach. Sesquiterpenes, isolated from the hexane fraction, appeared to be major components responsible for QR induction. Among the seven compounds tested in this study, alantolactone, isoalantolactone, and 5alpha-epoxyalantolactone significantly induced QR activity in both Hepa1c1c7 and BPRc1 cells. In conclusion, sesquiterpenes, including alantolactone, isoalantolactone and 5-epoxyalantolactone, present in I. helenium merit further evaluation as chemopreventive agents.

Publication Types:PMID: 17887945 [PubMed - indexed for MEDLINE]

29. The cultivation bias: different communities of arbuscular mycorrhizal fungi detected in roots from the field, from bait plants transplanted to the field, and from a greenhouse trap experiment.

Sýkorová Z, Ineichen K, Wiemken A, Redecker D.

Institute of Botany, University of Basel, Hebelstrasse 1, 4056 Basel, Switzerland.

The community composition of arbuscular mycorrhizal fungi (AMF) was investigated in roots of four different plant species (Inula salicina, Medicago sativa, Origanum vulgare, and Bromus erectus) sampled in (1) a plant species-rich calcareous grassland, (2) a bait plant bioassay conducted directly in that grassland, and (3) a greenhouse trap experiment using soil and a transplanted whole plant from that grassland as inoculum. Roots were analyzed by AMF-specific nested polymerase chain reaction, restriction fragment length polymorphism screening, and sequence analyses of rDNA small subunit and internal transcribed spacer regions. The AMF sequences were analyzed phylogenetically and used to define monophyletic phylotypes. Overall, 16 phylotypes from several lineages of AMF were detected. The community composition was strongly influenced by the experimental approach, with additional influence of cultivation duration, substrate, and host plant species in some experiments. Some fungal phylotypes, e.g., GLOM-A3 (Glomus mosseae) and several members of Glomus group B, appeared predominantly in the greenhouse experiment or in bait plants. Thus, these phylotypes can be considered r strategists, rapidly colonizing uncolonized ruderal habitats in early successional stages of the fungal community. In the greenhouse experiment, for instance, G. mosseae was abundant after 3 months, but could not be detected anymore after 10 months. In contrast, other phylotypes as GLOM-A17 (G. badium) and GLOM-A16 were detected almost exclusively in roots sampled from plants naturally growing in the grassland or from bait plants exposed in the field, indicating that they preferentially occur in late successional stages of fungal communities and thus represent the K strategy. The only phylotype found with high frequency in all three experimental approaches was GLOM A-1 (G. intraradices), which is known to be a generalist. These results indicate that, in greenhouse trap experiments, it is difficult to establish a root-colonizing AMF community reflecting the diversity of these fungi in the field roots because fungal succession in such artificial systems may bias the results. However, the field bait plant approach might be a convenient way to study the influence of different environmental factors on AMF community composition directly under the field conditions. For a better understanding of the dynamics of AMF communities, it will be necessary to classify AMF phylotypes and species according to their life history strategies.

Publication Types: PMID: 17879101 [PubMed - indexed for MEDLINE]

30. Cytotoxic germacranolide sesquiterpene from Inula cappa.

Xie HG, Chen H, Cao B, Zhang HW, Zou ZM.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

A new germacranolide, inulacappolide (1), was isolated from the EtOH extract of the whole plant of Inula cappa along with 16 known compounds. The structure of inulacappolide was a rare 1(10)-saturated type of germacran-6,12-olide, identified as 2alpha-acetoxy-3beta-hydroxy-9beta-angeloyloxygermacra-4-en-6alpha,12-olide by spectral analysis (IR, HR-ESI/MS, (1)H-NMR, (13)C-NMR, HMQC, HMBC, NOESY). In vitro, it showed antiproliferative effects against human cervical cancer HeLa, human leukemia K562 and human nasopharyngeal carcinoma KB cell lines with IC(50) values of 1.2 microM, 3.8 microM and 5.3 microM, respectively.

PMID: 17666855 [PubMed - indexed for MEDLINE]

31. Antiproliferative activity of Hungarian Asteraceae species against human cancer cell lines. Part I.

Réthy B, Csupor-Löffler B, Zupkó I, Hajdú Z, Máthé I, Hohmann J, Rédei T, Falkay G.

Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.

Aqueous and organic extracts of 25 selected species from four tribes of Hungarian Asteraceae were screened in vitro for antiproliferative activity against HeLa (cervix epithelial adenocarcinoma), A431 (skin epidermoid carcinoma) and MCF7 (breast epithelial adenocarcinoma) cells, using the MTT assay. Twenty five of the 228 tested extracts from different parts of the species of Astereae (6), Inuleae (3), Heliantheae (5) and Anthemideae (11) demonstrated a substantial antiproliferative effect (at least 50% inhibition of cell proliferation) at 10 microg/mL against one or more of the cell lines. Complete dose-response curves were generated and IC(50) values were calculated for these active extracts, and their direct cytotoxic effects were determined. In summary, 11 of the tested 25 plants were found to be active and 4 of them (Anthemis ruthenica, Erigeron canadensis, Erigeron annuus and Inula ensifolia) had not been studied previously for either active compounds or anticancer properties. Copyright (c) 2007 John Wiley & Sons, Ltd.

Publication Types: PMID: 17661336 [PubMed - indexed for MEDLINE]

32. Effects of naturally occurring dihydroflavonols from Inula viscosa on inflammation and enzymes involved in the arachidonic acid metabolism.

Hernández V, Recio MC, Máñez S, Giner RM, Ríos JL.

Departament de Farmacologia, Facultat de Farmacia, Universitat de València, Av. Vicent Andrés Estellés s/n. 46100 Burjassot, Spain.

The anti-inflammatory properties of three flavanones isolated from Inula viscosa, sakuranetin, 7-O-methylaromadendrin, and 3-acetyl-7-O-methylaromadendrin, have been tested both in vitro and in vivo. Acute inflammation in vivo was induced by means of topical application of 12-O-tetradecanoylphorbol 13-acetate (TPA) to mouse ears or by subcutaneous injection of phospholipase A(2) (PLA(2)) into mouse paws. The test compounds were evaluated in vitro for their effect on both the metabolism of arachidonic acid and on the release and/or activity of enzymes involved in the inflammatory response such as elastase, myeloperoxidase (MPO), and protein kinase C (PKC). The most active compounds in vivo against PLA(2)-induced paw oedema were 7-O-methylaromadendrin (ED(50)=8 mg/kg) and sakuranetin (ED(50)=18 mg/kg). In contrast, the most potent compound against TPA-induced ear oedema was 3-acetyl-7-O-methylaromadendrin (ED(50)=185 microg/ear), followed by sakuranetin (ED(50)=205 microg/ear). In vitro, the latter compound was the most potent inhibitor of leukotriene (LT) B(4) production by peritoneal rat neutrophils (IC(50)=9 microM) and it was also the only compound that directly inhibited the activity of 5-lipoxygenase (5-LOX). 3-Acetyl-7-O-methylaromadendrin also inhibited LTB(4) production (IC(50)=15 microM), but had no effect on 5-LOX activity. The only flavanone that inhibited the secretory PLA(2) activity in vitro was 7-O-methylaromadendrin. This finding may partly explain the anti-inflammatory effect observed in vivo, although other mechanisms such as the inhibition of histamine release by mast cells may also be implicated. Sakuranetin at 100 microM was found to inhibit elastase release, although this result is partly due to direct inhibition of the enzyme itself. At the same concentration, 7-O-methylaromadendrin only affected the enzyme release. Finally, none of the flavanones exhibited any effect on MPO or PKC activities. Taken together, these findings indicate that sakuranetin may be a selective inhibitor of 5-LOX.

Publication Types: PMID: 17658557 [PubMed - indexed for MEDLINE]

33. Sesquiterpene compounds from Inula viscosa.

Dipartimento di Chimica Organica, Università degli Studi di Palermo, Parco d'Orleans II, Italy.

Two new compounds, 2,5-dihydroxyisocostic acid and 2,3-dihydroxycostic acid together with three known sesquiterpene compounds, Isocostic acid, Carabrone and Tomentosin, have been isolated from the acetone extract of Inula viscosa (L.) Aiton. The structures of all new compounds were determined by spectroscopic methods, in particular 1D and 2D (1)H- and (13)C-NMR. The (13)C-NMR spectra of Isocostic acid and of Tomentosin are reported here for the first time.

Publication Types: PMID: 17654288 [PubMed - indexed for MEDLINE]

34. [Effects of series of Muskone on heart hemodynamics and myocardial consumption of oxygen in experimental dogs]

[Article in Chinese]

Zhang YT, Ma K, Zhang JY, Li YK, Wu LM, Li XR, Pan L, Gao HL, Li LD.

Xiyuan Hospital, China Academy of Chinese Medicine Sciences, Beijing 100091, China.

OBJECTIVE: To observe the effects of series of Muskone (the muskone includes Slender Dutchmanspipe Root, Inula Root and neither kind of Common Aucklandia Root) on the heart hemodynamics and myocardial consumption of oxygen in experimental dogs, and to explain its pharmacological action on cardiovascular system. METHOD: Arterial blood pressure, coronary blood flow, resistance in coronary artery, total peripheral resistance, work of left artrium and oxygen consumption index of the cardiac muscles were observed in anaesthetic dogs. RESULT: The series of Muskone decreased arterial blood pressure significantly, dilated coronary artery and peripheral arteries significantly, increased coronary blood flow, decreased resistance in coronary artery, improved the work of left artrium, the oxygen availability of cardiac muscles and the complaisance of arteries in cardiac muscles.

Publication TypePMID: 17639986 [PubMed - indexed for MEDLINE]

35.[Studies on the chemical constituents from Inula cappa (II)]

[Article in Chinese]

Guo QL, Yang JS, Liu JX.

Institute of Medicinal Plant Development, Peking Union Medical College & Chinese Academy of Medical science, Beijing 100094, China. guo-ql@163.com

OBJECTIVE: To study the chemical constituents of the root of Inula cappa. METHOD: The compounds were isolated and purified by recrystallization and chromatography with silica gel column and Sephadex LH-20 column. Their structures were identified by physico-chemical properties and spectral analysis. RESULTS: Seven compounds were isolated as scopolin (I), octacosanoic acid (II), tritriacontane (III), (2S,3S,4R,8E)-2-[(2'R)-2'-hydroxydocosanosylamino]-octadecane-1,3,4-triol(IV),(2S,3S,4R,8E)-2-[(2'R)-2'-hydroxytricosanosylamino]-octadecane-1,3,4-triol(V), (2S,3S,4R,8E)-2-[(2'R)-2'-hydroxytetracosanosylamino]-octadecane-1,3,4-triol(VI), (2S,3S,4R,8E)-2-[(2'R)-2'-hydroxypentacosanosylamino]-octadecane-1,3,4-triol(VIII), (2S,3S,4R,8E)-2-[(2'R)-2'-hydroxyhexacosanosylamino]-octadecane-1,3,4-triol(VIII). CONCLUSION: All compounds were isolated from Inula cappa for the first time.

Publication Types: PMID: 17539299 [PubMed - indexed for MEDLINE]

36. Inhibition of pro-inflammatory enzymes by inuviscolide, a sesquiterpene lactone from Inula viscosa.

Máñez S, Hernández V, Giner RM, Ríos JL, Recio Mdel C.

Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Avinguda Vicent Andrés Estellés s/n, 46100 Burjassot, Spain. manez@uv.es

This work concerns the pharmacological activity of inuviscolide, a sesquiterpenoid from Inula viscosa. It exerts inhibitory effects on elastase, cyclooxygenase 1 and secretory phospholipase A(2). Furthermore, it reduces the skin leukocyte infiltration in a murine model of dermatitis induced by repeated application of 12-O-tetradecanoylphorbol 13-acetate.

Publication Types: PMID: 17490829 [PubMed - indexed for MEDLINE]

37. Suppression of the NF-kappaB signalling pathway by ergolide, sesquiterpene lactone, in HeLa cells.

Chun JK, Seo DW, Ahn SH, Park JH, You JS, Lee CH, Lee JC, Kim YK, Han JW.

College of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.

We have previously reported that ergolide, a sesquiterpene lactone isolated from Inula britannica, suppresses inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression by inhibiting nuclear factor-kappaB (NF-kappaB) in RAW 264.7 macrophages. In this study, we show that ergolide suppresses the DNA binding activity of NF-kappaB and nuclear translocation of NF-kappaB p65 subunit, leading to the inhibition of NF-kappaB-dependent gene transcription in 12-O-tetradecanoylphorbol 13acetate (TPA)-stimulated HeLa cells. We also show that ergolide decreases the degradation and phosphorylation of IkappaB, an inhibitory protein of NF-kappaB, and this effect is accompanied by a simultaneous reduction of IkappaB kinase (IKK) activity. However, ergolide does not inhibit in-vitro IKK activity directly, suggesting the possible involvement of upstream IKK kinases in the regulation of NF-kappaB activation. Furthermore, ergolide-mediated protein kinase Calpha (PKCalpha) inhibition is involved in reduction of NF-kappaB inhibition, as demonstrated by the observation that dominant negative PKCalpha, but not p44/42 MAPK and p38 MAPK, inhibits TPA-stimulated reporter gene expression. Taken together, our results suggest that ergolide suppresses NF-kappaB activation through the inhibition of PKCalpha-IKK activity, providing insight for PKCalpha as a molecular target for anti-inflammatory drugs.

Publication Types: PMID: 17430640 [PubMed - indexed for MEDLINE]

38. Toward understanding the influence of soil metals and sulfate content on plant thiols.

Hunaiti AA, Al-Oqlah A, Shannag NM, Abukhalaf IK, Silvestrov NA, von Deutsch DA, Bayorh MA.

Department of Biological Sciences, Yarmouk University, Irbid, Jordan. ahunaiti@ju.edu.jo

Plants respond to increased concentrations of metals by a number of mechanisms, including chelation with phytochelatins (PCs). Soil specimens and plants (Veronica anagalis-aquatica, Typha domingensis, Cynodon dactylon, Chenopodium album, Rumex dentatus, Amaranthus gracilis, Chenopodium murale, Inula viscosa) leaves were collected from two sites in northern Jordan and subsequently metals (cadmium, copper, and lead), sulfate, and PC (from leaves) levels were determined. One of these sites was contaminated with metals and the other served as a control site. The contaminated site had elevated cadmium, copper, lead, and sulfate levels. This increase of metal and sulfate levels in the soil at the contaminated site correlated with a rise in plant total glutathione (GSH(T)) and cysteine (CYS(T)). These increases were not attributed to an elevation in total phytochelatin levels. However, a significant increase in the ratio of short-chain phytochelatins to the total phytochelatin stores was observed. The individual effects of metals and sulfate on glutathione, short-chain PCs and long-chain PCs levels were dissimilar.

Publication Types: PMID: 17365609 [PubMed - indexed for MEDLINE]

39. Cardiac activity of isolated constituents of Inula racemosa.

Lokhande PD, Dhaware BS, Jagdale SC, Chabukswar AR, Mulkalwar SA.

The Center for Advanced Studies, Department of Organic Chemistry, University of Pune, India. pdlokhande@rediffmail.com

Roots of the plant Inula racemosa are used as folk medicine in east Asia and Europe. Inula racemosa in combination with Commiphora mukul was reported to cure myocardial ischemia. However, systematic investigation of the plant for its specific role in heart diseases has not been conducted so far. In the present study, we have reported the isolation of four major constituents A, B, C and D along with some minor constituents from the plant Inula racemosa. Among the major constituent, constituent Dhas been selected first from spectral data and studied for its cardiac activity on isolated frog heart. The experimental data show that constituent D decreases heart rate and force of contraction at 40 mcg/ml. Actions of Adrenaline are blocked by constituent D and it also acts as an agonist for Propranolol. The studies indicate that constituent D produces a negative ionotropic and negative chronotropic effect on frog's heart. These studies can be utilized as a cardiac marker for exploring the cardiac activity of the plant Inula racemosa.

PMID: 17317650 [PubMed - indexed for MEDLINE]

40.Involvement of MAPK, Bcl-2 family, cytochrome c, and caspases in induction of apoptosis by 1,6-O,O-diacetylbritannilactone in human leukemia cells.

Pan MH, Chiou YS, Cheng AC, Bai N, Lo CY, Tan D, Ho CT.

Department of Seafood Science, National Kaohsiung Marine University, Kaohsiung, Taiwan. mhpan@mail.nkmu.edu.tw

1,6-O,O-diacetylbritannilactone (OODBL) isolated from Inula britannica, exhibits potent antitumor activity against several human cancer cell lines. However, the molecular mechanism of OODBL in the induction of anticancer activity is still unclear. In the present study, we demonstrated that OODBL induced the occurrence of apoptosis in human leukemic (HL-60) cells and cell arrest at the S phase. On the other hand, activation of caspase-8, -9, and -3, phosphorylation of Bcl-2 and Bid, and increased release of cytochrome c from mitochondria into cytosolic fraction were detected in OODBL-treated HL-60 cells. We further demonstrated that production of reactive oxygen species (ROS), activation of mitogen-activated protein kinase (MAPK) and c-Jun N-terminal kinase (JNK) signaling pathways may play an important role in OODBL-induced apoptosis. The results from the present study highlight the molecular mechanisms underlying OODBL-induced anticancer activity.

Publication Types: PMID: 17262884 [PubMed - indexed for MEDLINE]


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