- 1. Cis carotenoids: colorful molecules and free radical quenchers.
We present a density functional theory (DFT) and time-dependent density functional theory (TD-DFT) study on the stability, antioxidant properties with respect to the single electron transfer mechanism, and electronic absorption spectra of some isomers (9-cis, 13-cis, and 15-cis) of carotenoids such as astaxanthin, lycopene, and those present in virgin olive oil (lutein, β-carotene, neoxanthin, antheraxanthin, violaxanthin, neochrome, luteoxanthin, mutatoxanthin, and violaxanthin). In general, the calculated relative stability of the cis isomers appears to be in line with experimental observations. It is predicted that the above-mentioned carotenoids (cis and trans isomers) will transfer one electron to the (•)OH radical. However, this transference is not plausible with radicals such as (•)OOH, (•)OC2H5, (•)OOC2H5, (•)NO2, and (•)OOCH2CH═CH2. On the other hand, some carotenoids (β-carotene, lycopene, lutein, astaxanthin, violaxanthin, and antheraxanthin) will likely accept, in a medium of low polarity, one electron from the radical (•)O2(-). However, neoxanthin, auroxanthin, mutatoxanthin, luteoxanthin, and neochrome would not participate in such an electronic transfer mechanism. The TD-DFT studies show that neutral species of the cis and trans isomers maintain the same color. On the contrary, the ionic species undergo a "bleaching" process where the absorption wavelengths shift to longer values (>700 nm). Additionally, the formation of a complex between astaxanthin and Cu(2+) is explored as well as the effect that the metal atom will have in the UV-vis spectrum....(more)
Hernandez-Marin E, et al. J Phys Chem B 2013 Apr 18;117(15):4050-61.
Related Products: Lycopene
- 2. Biosynthesis of highly enriched (13)C-lycopene for human metabolic studies using repeated batch tomato cell culturing with (13)C-glucose.
While putative disease-preventing lycopene metabolites are found in both tomato (Solanum lycopersicum) products and in their consumers, mammalian lycopene metabolism is poorly understood. Advances in tomato cell culturing techniques offer an economical tool for generation of highly-enriched (13)C-lycopene for human bioavailability and metabolism studies. To enhance the (13)C-enrichment and yields of labelled lycopene from the hp-1 tomato cell line, cultures were first grown in (13)C-glucose media for three serial batches and produced increasing proportions of uniformly labelled lycopene (14.3±1.2%, 39.6±0.5%, and 48.9±1.5%) with consistent yields (from 5.8 to 9mg/L). An optimised 9-day-long (13)C-loading and 18-day-long labelling strategy developed based on glucose utilisation and lycopene yields, yielded (13)C-lycopene with 93% (13)C isotopic purity, and 55% of isotopomers were uniformly labelled. Furthermore, an optimised acetone and hexane extraction led to a fourfold increase in lycopene recovery from cultures compared to a standard extraction....(more)
Moran NE, et al. Food Chem 2013 Aug 15;139(1-4):631-9.
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- 3. Ameliorative effect of lycopene against 2,3,7,8-tetrachlorodibenzo-pdioxin- induced rat liver microsomal toxicity: An in vitro study.
The objective of the current study was to investigate the potential oxidative damage of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in hepatic microsomal fractions in vitro and to further elucidate the potential modulatory effect of lycopene. Rat liver microsomes were divided into four groups. Group I served as a control and is incubated with vehicle (toluene). Groups II and IV were incubated with 20 µM lycopene for 1 h before further incubating; groups III and IV with 15 nM of TCDD for further 1 h. Hydrogen peroxide (H2O2) production, lipid peroxidation (LPO), protein carbonyl content and activities of uridine 5'-diphospho-glucuronyltransferase (UDPGT) and P450 were significantly increased. Moreover, the activity of antioxidant enzymes superoxide dismutase, glutathione peroxidase, catalse, glutathione-S-transferase and glutathione reductase as well as the microsomal thiol content were significantly decreased. Incubation with lycopene (group IV) maintained near normal activities of the enzymes, normalized thiol and carbonyl content and significantly reduced LPO and H2O2 production. In conclusion, the findings of the study indicate that TCDD induces a significant oxidative stress in liver microsomes as manifested by increased LPO, H2O2 production, protein carbonyl content and activities of UDPGT and P450 and decreased antioxidant enzymes activities and thiol content. By the reversal of biochemical and oxidative markers toward normalcy, the protective role of lycopene is illuminated in rat liver microsomal toxicity....(more)
Aly HA, et al. Toxicol Ind Health 2013 Apr 15.
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- 4. Comparison of spectrophotometric and HPLC methods for determination of carotenoids in foods.
This report is aimed at intra-laboratory and inter-laboratory comparison of the results obtained during spectrophotometric and HPLC analyses of lycopene, β-carotene and total carotenoids in tomato products and yellow maize flours/grits. Extensive statistical analyses are performed in order to identify the main sources of uncertainties which may occur when using: (i) different techniques/methods/approaches in the same/different laboratories, in various food samples, and (ii) to indicate the facts/conditions under which the biases between results may remain unidentified after applying statistical testing. Our data points to the inertness of t-test to detect significance of differences, particularly at low R values: in general, the higher correlation coefficient, the higher is sensitivity of statistical testing, especially of the paired t-test. Therefore, simple deviation of relationship line slope from unity could be used as additional evaluation parameter. This adds to reliable and objective quality assurance of foods in regard to carotenoids....(more)
Luterotti S, et al. Food Chem 2013 Sep 1;140(1-2):390-7.
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- 5. Lycorine hydrochloride selectively inhibits human ovarian cancer cell proliferation and tumor neovascularization with very low toxicity.
Uncontrolled tumor cell proliferation and robust neovascularization are prominent features of aggressive ovarian cancers. Although great efforts in anti-ovarian cancer therapy have been made in the past 4 decades, the 5-year survival rates for ovarian cancer patients are still poor, and effective drugs to cure ovarian cancer patients are absent. In this study, we evaluated the anti-cancer effects of lycorine hydrochloride (LH), a novel anti-ovarian cancer agent, using the highly-invasive ovarian cancer cell line, Hey1B, as a model. Our data showed that LH effectively inhibited mitotic proliferation of Hey1B cells (half maximal inhibitory concentration=1.2μM) with very low toxicity, resulting in cell cycle arrest at the G2/M transition through enhanced expression of the cell cycle inhibitor p21 and marked down-regulation of cyclin D3 expression. Moreover, LH suppressed both the formation of capillary-like tubes by Hey1B cells cultured in vitro and the ovarian cancer cell-dominant neovascularization in vivo when administered to Hey1B-xenotransplanted mice. LH also suppressed the expression of several key angiogenic genes, including VE-cadherin, vascular endothelial growth factor, and Sema4D, and reduced Akt phosphorylation in Hey1B cells. These results suggest that LH selectively inhibits ovarian cancer cell proliferation and neovascularization and is a potential drug candidate for anti-ovarian cancer therapy....(more)
Cao Z, et al. Toxicol Lett 2013 Apr 12;218(2):174-85.
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- 6. Lycorine hydrochloride inhibits metastatic melanoma cell-dominant vasculogenic mimicry.
Melanoma cells actively participate in tumor angiogenesis and vasculogenic mimicry. However, anti-angiogenic therapy in patients with melanoma has not shown a significant survival gain. Thus, new anti-melanoma angiogenic and vasculogenic drugs are highly desired. Using the metastatic melanoma cell line C8161 as a model, we explored melanoma vasculogenic inhibitors and found that lycorine hydrochloride (LH) effectively suppressed C8161 cell-dominant formation of capillary-like tubes in vitro and generation of tumor blood vessels in vivo with low toxicity. Mechanistic studies revealed that LH markedly hindered expression of VE-cadherin in C8161 cells, but did not affect expression of six other important angiogenic and vasculogenic genes. Luciferase assays showed that LH significantly impeded promoter activity of the VE-cadherin gene in a dose-dependent manner. Together, these data suggest that LH inhibits melanoma C8161 cell-dominant vasculogenic mimicry by reducing VE-cadherin gene expression and diminishing cell surface exposure of the protein....(more)
Liu R, et al. Pigment Cell Melanoma Res 2012 Sep;25(5):630-8.
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- 7. Integration of transcriptome, proteome and metabolism data reveals the alkaloids biosynthesis in Macleaya cordata and Macleaya microcarpa.
BACKGROUND:
The Macleaya spp., including Macleaya cordata and Macleaya microcarpa, are traditional anti-virus, inflammation eliminating, and insecticide herb medicines for their isoquinoline alkaloids. They are also known as the basis of the popular natural animal food addictive in Europe. However, few studies especially at genomics level were conducted on them. Hence, we performed the Macleaya spp. transcriptome and integrated it with iTRAQ proteome analysis in order to identify potential genes involved in alkaloids biosynthesis.
METHODOLOGY AND PRINCIPAL FINDINGS:
We elaborately designed the transcriptome, proteome and metabolism profiling for 10 samples of both species to explore their alkaloids biosynthesis. From the transcriptome data, we obtained 69367 and 78255 unigenes for M. cordata and M. microcarpa, in which about two thirds of them were similar to sequences in public databases. By metabolism profiling, reverse patterns for alkaloids sanguinarine, chelerythrine, protopine, and allocryptopine were observed in different organs of two species. We characterized the expressions of enzymes in alkaloid biosynthesis pathways. We also identified more than 1000 proteins from iTRAQ proteome data. Our results strongly suggest that the root maybe the organ for major alkaloids biosynthesis of Macleaya spp. Except for biosynthesis, the alkaloids storage and transport were also important for their accumulation. The ultrastructure of laticifers by SEM helps us to prove the alkaloids maybe accumulated in the mature roots.
CONCLUSIONS/SIGNIFICANCE:
To our knowledge this is the first study to elucidate the genetic makeup of Macleaya spp. This work provides clues to the identification of the potential modulate genes involved in alkaloids biosynthesis in Macleaya spp., and sheds light on researches for non-model medicinal plants by integrating different high-throughput technologies....(more)
Zeng J, et al. PLoS One 2013;8(1):e53409.
Related Products: Macleaya Cordata Extract
- 8. [Comparison of sanguinarine production in suspension cultures of the Papaveraceae plants].
Intact plants of the Papaveraceae family are producers of a whole range of benzylisoquinoline alkaloids, which are used in pharmaceutical industry. In vitro cultures derived from plants of the Papaveraceae do not have the ability to produce such a broad spectrum of alkaloids, only the biosynthetic pathway leading to sanguinarine is active. This study deals with the preparation of in vitro cultures of Papaver somniferum, Eschscholtzia californica, Chelidonium majus and Macleaya cordata. Their sanguinarine production abilities were tested and compared. The lowest amounts of sanguinarine from all cultures tested were accumulated in suspension cultures of the opium poppy (0.45-0.55 μg in 1 g of fresh weight). Eschscholtzia californica, Chelidonium majus and Macleaya cordata cultures produced similar amounts of sanguinarine (18.0-22.7 μg; 20.5-26.3 μg; 15.4-20.3 μg in 1 g of fresh weight, resp.). The elicitation study used a biotic stressor, Botrytis cinerea hydrolysate. In all cultures treated, an increase in sanguinarine accumulation was observed. Of all cultures tested, the most intensive response was observed in the opium poppy cultures, although the amount of sanguinarine in the elicited poppy cultures was lower than in the non-elicited samples of the other cultures....(more)
Bilka F, et al. Ceska Slov Farm 2012 Dec;61(6):267-70. Czech.
Related Products: Macleaya Cordata Extract
- 9. In vitro assessment of Macleaya cordata crude extract bioactivity and anticancer properties in normal and cancerous human lung cells.
The purpose of this study is to assess the bioactivity and anticancer properties of Macleaya cordata crude extract in vitro using normal fetal lung fibroblast MRC5 and adenocarcinomic epithelial cell A549 as model systems,. Treatment of extract induced cell detachment, rounding, and irregularity in shape, in both normal and adenocarcinomic human lung cells, in accompanied of significant reduction in cell proliferation. The data indicated that necrosis appeared to be involved in compromising cell growth in both types of lung cells since membrane permeability and cell granularity were elevated. Although apoptosis was evident, the responses were differential in normal and diseased lung cells. Viability of treated MRC5 cells was reduced in a dose-dependent manner, demonstrating that the normal lung cells are sensitive to the extract. Surprisingly, A549 viability was slightly elevated in response to extract exposure at low concentration, implying that cells survived were metabolically active; the viability was reduced accordingly to treatment at higher concentrations. The present findings demonstrate that the crude extract of M. cordata contains agents affecting the functioning of normal and diseased lung cells in vitro. The observed cytotoxic effects against adenocarcinomic lung cells validate the potential of using M. cordata as herbal intervention in combined with conventional chemotherapy for lung cancer treatment.
Copyright © 2012 Elsevier GmbH. All rights reserved....(more)
Liu M, et al. Exp Toxicol Pathol 2012 Dec 11.
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- 10. Management of gastrointestinal mucositis due to cancer therapies in pediatric patients: results of a case series with SAMITAL(®).
BACKGROUND:
Gastrointestinal mucositis is a common debilitating complication of chemotherapy and one for which there is currently no effective long-term treatment.
OBJECTIVES:
To report our experience with the use of SAMITAL(®), a new oral suspension formulation based on the combination of three standardized extracts from Vaccinium myrtillus, Macleaya cordata fruits and Echinacea angustifolia roots in the prevention and treatment of chemotherapy-induced gastrointestinal mucositis in pediatric patients.
METHODS:
20 pediatric patients undergoing chemotherapy for a range of oncological conditions were followed. Patients initially received oral SAMITAL(®) to treat gastrointestinal mucositis and were then given SAMITAL(®) prophylactically to prevent recurrences with successive cycles of chemotherapy.
RESULTS:
SAMITAL(®) significantly decreased gastrointestinal mucositis grade after the first episode with a reduction of mean scores from 3.2 ± 0.7 at baseline to 0.4 ± 0.6 at the end of treatment (p < 0.001). SAMITAL(®) reduced pain, mucosal erosions, bleeding and dysphagia/feeding impairment. SAMITAL(®) improved patients' overall condition and quality of life after the first administration and lowered the need for parenteral nutrition. Importantly, it allowed chemotherapy cycles to be continued without complications.
CONCLUSION:
Results from this case series suggest that SAMITAL(®) may play an important role in the prevention and treatment of chemotherapy-induced gastrointestinal mucositis in children and adolescents and as such warrants investigation in controlled studies....(more)
Bertoglio JC, et al. Future Oncol 2012 Nov;8(11):1481-6.
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- 11. [Comparative cytogenetic study of the forms of Macleaya cordata (Willd.) R. Br. from different localities].
A comparative cytogenetic study of two introduced forms of Makleaya cordata (Willd.) R. Br. = syn. Bocconia cordata Willd. grown in different ecological and geographical regions (Moscow and Donetsk areas) was carried out. In the study, a complex of methods utilizing various chromosomal markers, i.e., C- and DAPI-banding technique, fluorescence in situ hybridization (FISH) with probes of26S and 5S rDNA, as well as estimation of the total area of C-positive regions (C-HCH) in prophase nucleoli and meiosis analysis, was used. In the karyotypes (2n = 20), each chromosome was identified on the basis of C-banding and FISH patterns and the chromosome ideograms were built. Pericentrometric and telomeric C-positive bands in chromosomes of the Moscow form karyotype were found to be smaller and intercalary bands, larger than the corresponding bands in the M. cordata form grown in Donetsk. It was found that the content of C-HCH in prophase nucleoli in the form of M. cordata grown in Donetsk was higher than in the form grown in Moscow. In both forms sites of 26S rDNA and 5s rDNA were localized on satellite chromosome 1 and on chromosome 4 respectively but the signals were more intensive in the plant form grown in Donetsk. The results of this study enable selecting M. cordata forms for use in pharmacology and recommending them for cultivation in various ecological and geographical regions....(more)
Samatadze TE, et al. Genetika 2012 Jan;48(1):72-9. Russian.
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- 12. Induction of heme oxygenase-1 by Macleaya cordata extract and its constituent sanguinarine in RAW264.7 cells.
Macleaya cordata (plume poppy) is used in traditional Chinese medicine for its anti-inflammatory and antibacterial activities. In this study, we examined whether M. cordata extract and/or its major alkaloid constituents, protopine, allocryptopine, sanguinarine and chelerythrine activate the Nrf2 signalling pathway which regulates the expression of cytoprotective enzymes including heme oxygenase-1 (HO-1) and thioredoxin 1. In murine macrophage RAW264.7 cells, M. cordata extract increased both mRNA and protein levels of HO-1. Of the alkaloids examined, only sanguinarine appeared to be responsible for these effects. At the concentration of 2 μM, sanguinarine induced nuclear accumulation of Nrf2, increased the expression of Hmox1 gene encoding HO-1 and elevated HO-1 protein levels. Sanguinarine-induced Hmox1 mRNA expression was suppressed by SB203580, a pharmacologic inhibitor of p38 mitogen-activated protein kinases (p38 MAPKs). The upregulation of HO-1 in RAW264.7 cells by sanguinarine was, however, accompanied by decrease in cell viability. Nonetheless, sanguinarine at micromolar, non-cytotoxic concentrations elevated protein levels of HO-1 and thioredoxin 1 in primary cultures of human hepatocytes. We conclude that sanguinarine may, under appropriate conditions, increase the capacity of the enzymatic antioxidant defence system via activation of the p38 MAPK/Nrf2 pathway.
Copyright © 2011 Elsevier B.V. All rights reserved....(more)
Vrba J, et al. Fitoterapia 2012 Mar;83(2):329-35.
Related Products: Macleaya Cordata Extract
- 13. [Screen for natural benzylisoquinoline alkaloids against tumor].
OBJECTIVE:
To search for natural benzylisoquinoline alkaloids against tumor.
METHOD:
In this study, taken DNA as target, a method was developed for screening of natural benzylisoquinoline alkaloids against tumor from traditional Chinese medicine by the use of centrifugal ultrafiltration combined with HPLC technology. The anti-tumor activity for the compounds screened was evaluated in vitro.
RESULT:
Nine compounds interacted with DNA were discovered and identified from Macleaya cordata, Chelidonium majus, Coptis chinensis, and the proliferation of four types of human solid cancer cell lines was markedly inhibited by these compounds.
CONCLUSION:
The developed method was considered to be suitable for screening of natural benzylisoquinoline alkaloids against tumor from traditional Chinese medicine....(more)
Zhang Z, et al. Zhongguo Zhong Yao Za Zhi 2011 Oct;36(19):2684-8. Chinese.
Related Products: Macleaya Cordata Extract
- 14. Mercury distribution in the soil-plant-air system at the Wanshan mercury mining district in Guizhou, Southwest China.
The level of mercury bioaccumulation in wild plants; the distribution of bioavailable Hg, elemental Hg, and total Hg in soil; and the concentration of total gaseous Hg (TGM) in ambient air was studied at three different mining sites (SiKeng [SK], WuKeng [WK], and GouXi [GX]) in the Wanshan mercury mining district of China. Results of the present study showed that the distribution of soil total Hg, elemental Hg, bioavailable Hg, and TGM varies across the three mining sites. Higher soil total Hg (29.4-1,972.3 mg/kg) and elemental Hg (19.03-443.8 mg/kg) concentrations were recorded for plots SK and WK than for plot GX. Bioavailable Hg was lower at plot SK and GX (SK, 3-12 ng/g; GX, 9-14 ng/g) than at plot WK (11-1,063 ng/g), although the TGM concentration in the ambient air was significantly higher for plot GX (52,723 ng/m(3) ) relative to WK (106 ng/m(3) ) and SK (43 ng/m(3)). Mercury in sampled herbage was elevated and ranged from 0.8 to 4.75 mg/kg (SK), from 2.17 to 34.38 mg/kg (WK), and from 47.45 to 136.5 mg/kg (GX). Many of the sampled plants are used as fodder or for medicinal purposes. High shoot Hg concentrations may therefore pose an unacceptable human health risk. Statistical analysis of the recorded data showed that the Hg concentration in plant shoots was positively correlated with TGM and that the Hg concentration in roots was positively correlated with the bioavailable Hg concentration in the soil. The bioaccumulation factor (BAF) in the present study was defined with reference to the concentration of bioavailable Hg in the soil (Hg([root]) /Hg([bioavail])). Three plant species, Macleaya cordata L., Achillea millefolium L., and Pteris vittata L., showed enhanced accumulation of Hg and therefore may have potential for use in the phytoremediation of soils of the Wanshan mining area.
Copyright © 2011 SETAC....(more)
Wang J, et al. Environ Toxicol Chem 2011 Dec;30(12):2725-31.
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- 15. Effects of dietary addition of Macleaya cordata alkaloid extract on growth performance, caecal indices and breast meat fatty acids profile in male broilers.
The aim of this experiment was to investigate whether a low-dietary application (15 mg/kg) of an alkaloid preparation containing quaternary benzo[c]phenanthridine alkaloids and obtained from Macleaya cordata (Sangrovit) influenced caecal metabolism, growth performance and long-chain fatty acid composition of breast meat. One-day-old broiler chicks (Cobb 500) were fed a diet without supplement or with a 15 mg/kg dose of Sangrovit (C and A groups respectively) for 5 weeks. Although the A treatment was not accompanied by an enhanced final body weight of broilers, the intake of a diet with Sangrovit influenced the caecal microflora activity. The addition of Sangrovit to a diet decreased potentially harmful β-glucuronidase and β-glucosidase activities (p<0.05 and p=0.075 respectively), and at the same time led to a significant increase in activities of bacterial glycolytic enzymes α-glucosidase, α-galactosidase, β-galactosidase in comparison to the control group. The concentration of total short-chain fatty acids in the caecal digesta was increased in the A treatment contributing to the tendency towards lower caecal pH (p=0.078). The analysis of breast meat fatty acids showed that the dietary application of Sangrovit evoked some changes in contents of monounsaturated fatty acids (MUFA) and polyunsaturated fatty acids (PUFA) contents. The applied dosage of Sangrovit caused an increase in the sum of MUFA and the tendency towards lower PUFA sum (p<0.05 and p=0.062 respectively) as in relation with the C group. Although the nutritionally relevant n-6/n-3 PUFA and the (PUFA+MUFA)/saturated fatty acids ratios remained similar in both groups, further research is postulated to establish the effect of this preparation on meat quality. To sum up, despite of a lack of the improvement in final body weight, a low dose of dietary Sangrovit was found to exert positive effects on the caecal metabolism of the broilers.
© 2010 Blackwell Verlag GmbH....(more)
Juskiewicz J, et al. J Anim Physiol Anim Nutr (Berl) 2011 Apr;95(2):171-8.
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- 16. Effect of sanguinarine from the leaves of Macleaya cordata against Ichthyophthirius multifiliis in grass carp (Ctenopharyngodon idella).
The ciliate Ichthyophthirius multifiliis is one of the most pathogenic parasites of fish maintained in captivity. In this study, effects of crude extracts, fractions, and compounds from the leaves of Macleaya cordata against I. multifiliis were investigated under in vitro conditions by bioactivity-guided isolation method. The dried ethanol extract of M. cordata was extracted successively in a separating funnel with petroleum ether, ethyl acetate, chloroform and n-butanol. Among them, only the chloroform extract showed promising activity and therefore, was subjected to further separation and purification using various chromatographic techniques. Four compounds were isolated from chloroform extract, but only one compound showed potent activity. The structure of the active compound was elucidated as sanguinarine by hydrogen, carbon-13 nuclear magnetic resonance spectrum and electron ionization mass spectrometry. In vitro antiparasitic efficacy tests exhibited that sanguinarine was 100% effective against I. multifiliis at a concentration of 0.7 mg l(-1), with LC(50) and LC(90) values of 0.437 and 0.853 mg l(-1) after 4 h of exposure. In vivo antiparasitic efficacy tests showed that the number of I. multifiliis on the gills in the treatment group (in 0.9 mg l(-1) sanguinarine) was reduced by 96.8%, in comparison to untreated group at 25°C for 48 h. Mortality of fish did not occur in the treatment group during the trail, although 40% of untreated fish died. Our results indicate that the studied plant extracts, as well as sanguinarine might be potential sources of new antiparasitic drug for the control of I. multifiliis....(more)
Yao JY, et al. Parasitol Res 2010 Oct;107(5):1035-42.
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- 17. The effect of zinc acetate and magnolia bark extract added to chewing gum on volatile sulfur-containing compounds in the oral cavity.
OBJECTIVE:
A controlled, clinical, double-blind study was conducted to assess the efficacy of a sugar-free chewing gum containing zinc acetate and magnolia bark extract (MBE) on oral volatile sulfur-containing compounds (VSC) versus a placebo sugar-free chewing gum for two hours.
METHODS:
To participate in the study, subjects had to have at least 24 of their teeth, no report of oral and systemic diseases, and no removable dentures. All 168 eligible participants had to avoid any professional oral hygiene, refrain from taking medicine for two weeks, and not be menstruating. They were also instructed not to brush their teeth and tongue, smoke, drink alcohol, or eat onion, garlic, or licorice for the six-hour period before the visit and during the test. Moreover, to join the protocol, they had to show a VSC score of > or = 75 ppb at the baseline measurement. One-hundred and twenty-three subjects (67 men and 56 women, mean age 37) met the criteria at baseline and were entered into either the test or control group by assignment from a table of randomized numbers. The test chewing gum (2.23 g) contained zinc acetate 0.012% and magnolia bark extract 0.15% in weight; the control gum was equivalent without these active agents. The OralChroma device was utilized to evaluate total oral VSC. Their levels were recorded at baseline, after ten minutes of mastication, after one hour, and after two hours. Data were analyzed with SPSS software and the level of significance was set at alpha = 0.05.
RESULTS:
One-hundred and twenty-three subjects completed the trial (62 in the control group and 61 in the test group); none reported problems linked to zinc acetate or magnolia bark extract. The mean percentage reductions from baseline at the end of the 10-minute chewing were 31.2% in the control group (p < 0.05) and 50.9% in the test group (p < 0.05). One hour later the reductions were 6.9% in the control group and 27.6% in the test group (p < 0.05); two hours later the reductions were 2.3% in the control group and 13.6% in the test group. The comparison of the two groups after baseline adjustment showed a statistically significant difference (p < 0.05) in VSC reductions between the test and control chewing gums at the end of the mastication period and after one hour.
CONCLUSION:
Chewing gum containing zinc acetate and magnoliabark extract can significantly reduce the oral VSC levels for more than one hour. Moreover, the test chewing gum reduces oral VSC significantly more than a control chewing gum....(more)
Porciani PF, et al. J Clin Dent 2012;23(3):76-9.
Related Products: Magnolia Bark Extract
- 18. Randomized controlled study on clinical efficacy of isoflavones plus Lactobacillus sporogenes, associated or not with a natural anxiolytic agent in menopause.
AIM:
The aim of this paper was to evaluate the activity of magnolia bark extract added to isoflavones and lactobacilli in menopausal women with typical menopausal symptoms and concomitant borderline psychoaffective and/or sleep alterations, of severity not requiring a psychopharmacological therapy.
METHODS:
Menopausal women were enrolled in a multicenter, controlled, parallel-group study and randomized to E (isoflavones 60 mg + Lactobacillus sporogenes + calcium and vitamin D3 - Estromineral, Rottapharm Madaus) versus ES (magnolia bark extract + E - Estromineral serena) 1 tablet/night for 12 weeks.
RESULTS:
In 91 gynecological centers, 634 women were treated (300 with E and 334 with ES), mean age 53.1 years and Body Mass Index (BMI) 25.2 kg/m2; 28% were past hormone replacement therapy HRT users and 3.3% had had a previous breast cancer. Both treatments significantly reduced versus baseline the symptoms tested at 0, 4, 8 and 12 weeks. E and ES showed a similar efficacy on hot flushing, nocturnal sweating with awakenings, palpitations and vaginal dryness. ES was more active on insomnia, irritability, anxiety, depressed mood, asthenia and loss of libido. Woman's well-being and physician's final judgment were positive in >70% in both groups. The rate of adverse events was 1% with E (metrorrhagia, cramps and constipation) and 1.2% with ES (gastralgia, blood loss, constipation and breast tension).
CONCLUSION:
Isoflavones are effective in improving the classical menopause symptoms. The clinical activity of magnolia bark extract on the relevant psycho-affective symptoms, particularly anxiety, irritability and insomnia, was evident. ES in the mild psychical alterations that can occur in climacterium avoids to run the known dependence risks linked to psychopharmacological agents withdrawals....(more)
Agosta C, et al. Minerva Ginecol 2011 Feb;63(1):11-7.
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- 19. Preparation of nanoparticles of Magnolia bark extract by rapid expansion from supercritical solution into aqueous solutions.
A rapid expansion from supercritical solution into aqueous solution (RESSAS) technology was presented for the micronization of Chinese medicinal material. Magnolia bark extract (MBE) obtained by supercritical carbon dioxide (scCO) extraction technology was chosen as the experimental material. RESSAS process produced 303.0 nm nanoparticles (size distribution, 243.6-320.5 nm), which was significantly smaller than the 55.3 µm particles (size distribution, 8.3-102.4 µm) prepared by conventional mechanical milling. The effect of process parameters, including extraction temperature (30 °C, 40 °C, 50 °C), extraction pressure (200, 250, 300 bar) and nozzle size (50, 100, 200 µm), on the size distribution of nanoparticles was investigated. The characteristics of nanoparticles and materials were also studied by scanning electron microscopy (SEM) and laser light scattering (LLS). This study demonstrates that RESSAS is applicable for preparing nanoparticles of MBE at low operating temperature; the process is simple without any residual solvent....(more)
He S, et al. J Microencapsul 2011;28(3):183-9.
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- 20. Effect of a sugar-free chewing gum containing magnolia bark extract on different variables related to caries and gingivitis: a randomized controlled intervention trial.
The effect of magnolia bark extract (MBE) on different variables related to caries and gingivitis administered daily through a sugar-free chewing gum was evaluated. The study was performed with healthy adult volunteers at high risk for caries as a randomized double-blind interventional study. 120 subjects with a salivary mutans streptococci (MS) concentration ≥10(5) CFU/ml and presence of bleeding on probing >25% were enrolled and divided into three groups: magnolia, xylitol and control. The study design included examinations at baseline, after 7 days, after 30 days of gum use and 7 days after the end of gum use. Plaque pH was assessed using the strip method following a sucrose challenge. Area under the curve (AUC(5.7) and AUC(6.2)) was recorded. Whole saliva was collected and the number of salivary MS (CFU/ml) was counted. Bleeding on probing was recorded as a proxy of dental plaque. Data were analyzed using ANOVA repeated measures. Magnolia gum significantly reduced plaque acidogenicity, MS salivary concentration and gingival bleeding compared to xylitol and control gums. Subjects from the magnolia and xylitol groups showed both MS concentration (p = 0.01 and 0.06, respectively) and AUC(5.7) (p = 0.01 and 0.04, respectively) to be significantly lower compared to baseline. Thirty-day use of a chewing gum containing MBE showed beneficial effects on oral health, including reduction of salivary MS, plaque acidogenicity and bleeding on probing....(more)
Campus G, et al. Caries Res 2011;45(4):393-9.
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- 21. Micronization of magnolia bark extract with enhanced dissolution behavior by rapid expansion of supercritical solution.
A rapid expansion of supercritical solution (RESS) technology was presented for the micronization of Chinese medicinal material. Magnolia bark extract (MBE) obtained by supercritical carbon dioxide (scCO(2)) extraction technology was chosen as the experimental material. RESS process produced 4.7 microm size MBE microparticles (size distribution, 0.2-24.1 microm), which was significantly smaller than the 55.3 microm size particles (size distribution, 8.3-102.4 microm) obtained from conventional mechanical milling. Dissolution rate study showed that drug dissolution was significantly enhanced by the RESS progress. At 90 min, the amount dissolved of mechanical milling MBE was 6.37 mg x l(-1), which was significantly lower than that of micronized MBE (14.77 mg x l(-1)), according to the results of ANOVA (p<0.01). The effect of extraction temperature (30, 40, 50 degrees Celsius), extraction pressure (200, 250, 300 bar) and nozzle size (50, 100, 200 microm) on the size distribution of microparticles was investigated. The characteristics of microparticles were also studied by differential scanning calorimetry (DSC), infrared spectroscopy (IR), scanning electron microscopy (SEM), and image analysis. This study demonstrates that RESS is applicable for preparing microparticles of MBE at low operating temperature; the process is simple without residual solvent....(more)
He S, et al. Chem Pharm Bull (Tokyo) 2010 Feb;58(2):154-9.
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- 22. [Micronization of magnolia bark extract by RESS as well as dissolution and pharmacokinetics evaluation].
The purpose of this study is to explore the feasibility and superiority of using rapid expansion of supercritical solution (RESS) technology in the field of traditional Chinese medicine. The extract of magnolia bark (EMB) was obtained by supercritical carbon dioxide (SCF-CO2) extraction technology. Microparticles of EMB were manufactured by RESS technology. The effects of operating temperature and pressure on the contents of the active ingredient in the particles were evaluated by HPLC. The effect of expansion conditions on the particle size distribution of EMB particles was investigated. The smallest sample (mean size: 4.7 microm) was obtained under the RESS condition: pressure of 25 MPa, temperature of 50 degrees C and a nozzle size of 100 microm. The characteristics of microparticles were also studied by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and image analysis. The dissolution rate study showed that microparticles had a significantly faster dissolution rate than normal material particles. After oral raw EMB suspension, the mean areas under the plasma concentration-time curves (AUC(0-t)) of honokiol and magnolol were found to be (4.23 +/- 0.36) and (5.46 +/- 0.57) mg x h x L(-1), respectively, which were increased significantly, i.e. (5.41 +/- 0.63) and (7.24 +/- 0.83) mg x h x L(-1) when micronized EMB suspension was administered orally in SD rats (P < 0.05). Similarly, the mean maximum plasma concentrations of honokiol and magnolol increased from (1.55 +/- 0.22) and (2.35 +/- 0.14) mg x L(-1) (raw EMB) to (2.31 +/- 0.17) and (2.84 +/- 0.21) mg x L(-1) (micronized EMB), respectively. The results of t-test demonstrated that AUC(0-t) and Cmax value for honokiol and magnolol was significantly increased with the micronization compared to raw EBM (P < 0.05). This study demonstrated that the RESS was applicable for preparing microparticles of EMB at low operating temperature. The process was simple, free of environment pollution and without residual solvent....(more)
He S, et al. Yao Xue Xue Bao 2009 May;44(5):532-9. Chinese.
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- 23. Evaluation of magnolia bark extract in chromosomal aberration assays.
Magnolia bark extract (MBE) has been used historically in traditional Chinese and Japanese medicines, and more recently as a component of dietary supplements and cosmetic products. The genotoxic potential of MBE was studied in two in vitro chromosomal aberration assays. In Chinese hamster ovary (CHO) cells, exposure for 3 h to MBE at concentrations of 0-30 microg/ml in the absence of a metabolic activation system (S9) and 0-7 microg/ml with S9 did not induce chromosomal aberrations, whereas higher concentrations were cytotoxic and did not allow for analysis of aberrations. Extended exposure for 18 h without metabolic activation at concentrations up to 15 microg/ml also resulted in a negative response. In V79 cells derived from Chinese hamster lung tissue, treatment for 6h with concentrations up to 52 and 59 microg/ml in the absence and presence of S9, respectively, did not increase the incidence of chromosomal aberrations compared to negative controls. Furthermore, MBE exposure for 24 h without metabolic activation did not induce aberrations. The results of these studies demonstrate that MBE is not genotoxic under the conditions of the in vitro chromosomal aberration assays in CHO and V79 cells, and support the safety of MBE....(more)
Zhang B, et al. Mutat Res 2008 Jul 31;654(2):133-7.
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- 24. Evaluation of the in vitro and in vivo genotoxicity of magnolia bark extract.
Magnolia bark extract (MBE) is an extract of the dried stem, root, or branch bark of magnolia trees that has been used historically in traditional Chinese and Japanese medicines, and more recently as a component of dietary supplements and cosmetic products. To study the genotoxic potential of MBE, a bacterial reverse mutation assay and an in vivo micronucleus test were conducted. Compositional analysis of the test substance revealed that MBE contains 94% magnolol and 1.5% honokiol. MBE exerted no mutagenic activity in various bacterial strains of Salmonella typhimurium and in Escherichia coli WP2 uvrA, either in the absence or presence of metabolic activation at all doses tested. In the micronucleus test, various doses of MBE did not affect the proportions of immature to total erythrocytes, nor did it increase the number of micronuclei in the immature erythrocytes of Swiss albino mice. The results of these studies demonstrate that MBE is not genotoxic under the conditions of the in vitro bacterial reverse mutation assay and the in vivo micronucleus test, and support the safety of MBE for dietary consumption....(more)
Li N, et al. Regul Toxicol Pharmacol 2007 Dec;49(3):154-9.
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- 25. Evaluation of short-term and subchronic toxicity of magnolia bark extract in rats.
Magnolia bark has been traditionally used in Chinese and Japanese medicines, and its extract is a constituent of currently marketed dietary supplements and cosmetic products. The safety of magnolia bark extract (MBE) was assessed in short-term and subchronic studies. In a 21-day pilot study, rats were administered MBE at levels of 0, 60, 120, 240 or 480 mg/kg body weight (bw)/day in the diet. There were no treatment-related effects in clinical observations, macroscopic or microscopic findings, hematological, clinical chemistry, urinalysis, or organ weight measurements, and there were no deaths or significant differences in body weight and weight gain. In the 90-day study, rats were administered 0, 60, 120 or 240 mg MBE/kg bw/day in the diet. No mortality, ophthalmic abnormalities or treatment-related findings in clinical observations, hematology, coagulation or organ weight measurements were observed. There were no treatment-related macroscopic or microscopic findings. Differences between treated and control groups in body weight, weight gain, food consumption and utilization, clinical chemistry and urinalysis parameters were not considered toxicologically significant as they were not dose-related and/or because values remained within historical control ranges. These results support the safety of MBE for oral consumption....(more)
Liu Z, et al. Regul Toxicol Pharmacol 2007 Dec;49(3):160-71.
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- 26. Compressed mints and chewing gum containing magnolia bark extract are effective against bacteria responsible for oral malodor.
Flavors and natural botanic extracts are often used in chewing gum and compressed mints for breath freshening and relief of oral malodor. The oral malodor is a result of bacterial putrification of proteinaceous materials from food or saliva. In this study, magnolia bark extract (MBE) and its two main components, magnolol and honokiol, were evaluated by the minimum inhibition concentration (MIC) test. The inhibitory effect of MBE mint was further evaluated by a kill-time assay study. In addition, an in vivo study was performed on nine healthy volunteers postlunch. Saliva samples were taken before and after subjects consumed mints and gum, with and without MBE. Listerine mouthwash was included as a positive control. The testing results indicated that MBE and its two main constituents demonstrated a strong germ-kill effect against bacteria responsible for halitosis and also Streptococcus mutans, bacteria involved in dental caries formation. The MIC of magnolol, honokiol, and MBE on Porphyromonas gingivalis, Fusobacterium nucleatum, and S. mutans ranged from 8 to 31 microg/mL. Kill-time assay results indicated that mints containing 0.2% MBE reduced more than 99.9% of three oral bacteria within 5 min of treatment. The in vivo study demonstrated that MBE containing mints reduced total salivary bacteria by 61.6% at 30 min and 33.8% at 60 min postconsumption. In comparison, the flavorless mint reduced total salivary bacteria by 3.6% at 30 min and increased total bacteria by 47.9% at 60 min. The MBE containing chewing gum reduced total salivary bacteria by 43.0% at 40 min, while placebo gum reduced total salivary bacteria by 18.0%. In conclusion, MBE demonstrated a significant antibacterial activity against organisms responsible for oral malodor and can be incorporated in compressed mints and chewing gum for improved breath-freshening benefits....(more)
Greenberg M, et al. J Agric Food Chem 2007 Nov 14;55(23):9465-9.
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- 27. Enhancing the bioavailability of magnolol in rabbits using melting solid dispersion with polyvinylpyrrolidone.
Abstract Objective: Preparation of magnolol-loaded amorphous solid dispersion was investigated for improving the bioavailability. Materials and methods: A solid dispersion of magnolol was prepared with polyvinylpyrrolidone K-30 (PVP) by melting method, and the physical properties were characterized by using differential scanning calorimetry, powder X-ray diffractometry, Fourier transformation-infrared spectroscopy and scanning electron microscope. In addition, dissolution test was also performed. Subsequently, the bioavailability of magnolol pure compound, its physical mixture and solid dispersion were compared in rabbits. The blood samples withdrawn via marginal ear vein at specific time points were assayed by HPLC method. Results: Oral administration of the solid dispersion of magnolol with PVP significantly increased the systemic exposures of magnolol and magnolol sulfates/glucuronides by 80.1% and 142.8%, respectively, compared to those given with magnolol pure compound. Conclusion: Magnolol-loaded amorphous solid dispersion with PVP has demonstrated enhanced bioavailability of magnolol in rabbits....(more)
Lin SP, et al. Drug Dev Ind Pharm 2013 Feb 1.
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- 28. Maximizing dermal targeting and minimizing transdermal penetration by magnolol/honokiol methoxylation.
Magnolol and honokiol, predominant active compounds in the family Magnoliaceae, are known to exhibit strong anti-inflammatory activities against dermal disorders. We attempted to modify the structures of magnolol and honokiol by methoxylation to optimize the skin delivery ability. Absorption of these permeants into and through the skin was performed at both an infinite dose and saturated solubility. Superoxide anion and elastase released from human neutrophils were the biomarkers used to examine anti-inflammatory potencies of these permeants. The safety of the permeants was evaluated by keratinocyte viability and in vivo bioengineering techniques. Topical magnolol and honokiol at an infinite dose (7.5 mM) showed skin accumulations of 0.22 and 0.16 nmol/mg, respectively. Methoxylation significantly enhanced their skin absorption. Deposition amounts of dimethylmagnolol and dimethylhonokiol were respectively 15- and 7-fold greater than those of magnolol and honokiol. Contrary to the skin accumulation results, the transdermal penetration across skin decreased following methoxylation. No transdermal delivery occurred for dimethylhonokiol. Skin uptake of 4'-O-methylhonokiol was 2-fold higher than that of 2-O-methylhonokiol, although they are isomers. Methoxylated permeants demonstrated selective absorption into follicles, which showed 3-5-fold higher follicular amounts compared to magnolol and honokiol. The relative order of anti-inflammatory activities was honokiol>2-O-methylmagnolol>dimethylhonokiol>magnolol. The other compounds exhibited negligible or negative responses in activated neutrophils. Magnolol and honokiol induced slight but significant keratinocyte cytotoxicity and stratum corneum disruption. Daily administration of methoxylated permeants, especially dimethylhonokiol, produced no skin irritation for up to 7 days. Methoxylated magnolol and honokiol can be efficient and safe candidates for treating inflammatory skin disorders....(more)
Lin CF, et al. Int J Pharm 2013 Mar 10;445(1-2):153-62.
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- 29. Screening active anti-breast cancer compounds from Cortex Magnolia officinalis by 2D LC-MS.
Most of the anti-breast cancer drugs are often limited owing to drug resistance and serious adverse reactions. Therefore, development of more targeted and low toxic drugs from traditional Chinese medicines for breast cancer are needed. At the same time, establishment of fast and effective drug screening methods are urgently required. We describe here a 2D LC method of MDA-MB-231 cell membrane chromatography combined with HPLC/MS for recognition, separation, and identification of target components from traditional Chinese medicine Cortex Magnolia officinalis. The MDA-MB-231 cells membrane was used to prepare the chromatographic stationary phase in the first dimension. The active compounds had a retention characteristic on the cell membrane chromatography model (10 × 2.0 mm, 5 μm). The retention fractions were enriched using an online C(18) column (10 × 1.0 mm, 5 μm) and were analyzed by the second dimension RP chromatography. Finally, the activity of the retention fractions was tested through in vitro experiments. Results showed that the retention fractions were honokiol and magnolol and the inhibition rate on MDA-MB-231 cell growth were 23 and 64 μM, respectively. These results support the conclusion that this coupled analytical technique could be an efficient method in drug discovery....(more)
Hou X, et al. J Sep Sci 2013 Feb;36(4):706-12.
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- 30. Magnolol Protects Against Oxidative Stress-Mediated Neural Cell Damage by Modulating Mitochondrial Dysfunction and PI3K/Akt Signaling.
Magnolol, an orally available compound from Magnolia officinalis used widely in traditional herbal medicine against a variety of neuronal diseases, possesses potent antioxidant properties and protects the brain against oxidative damage. The aim of the work is to examine the protective mechanisms of magnolol on human neuroblastoma SH-SY5Y cells against apoptosis induced by the neurotoxin acrolein, which can cause neurodegenerative disorders by inducing oxidative stress. By investigating the effect of magnolol on neural cell damage induced by the neurotoxin acrolein, we found that magnolol pretreatment significantly attenuated acrolein-induced oxidative stress through inhibiting reactive oxygen species accumulation caused by intracellular glutathione depletion and nicotinamide adenine dinucleotide phosphate oxidase activation. We next examined the signaling cascade(s) involved in magnolol-mediated antiapoptotic effects. The results showed that acrolein induced SH-SY5Y cell apoptosis by activating mitochondria/caspase and MEK/ERK signaling pathways. Our findings provide the first evidence that magnolol protects SH-SY5Y cells against acrolein-induced oxidative stress and prolongs SH-SY5Y cell survival through regulating JNK/mitochondria/caspase, PI3K/MEK/ERK, and PI3K/Akt/FoxO1 signaling pathways....(more)
Dong L, et al. J Mol Neurosci 2013 Feb 14.
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- 31. Magnolol suppresses hypoxia-induced angiogenesis via inhibition of HIF-1α/VEGF signaling pathway in human bladder cancer cells.
The hypoxic environment in tumors is an important factor causing tumor angiogenesis by activating the key transcription factor, hypoxia-inducible factors-1α (HIF-1α). Magnolol isolated from Magnolia officinalis has been reported to exhibit an anticancer activity via elevation of apoptosis. However, whether magnolol inhibits tumor angiogenesis remains unknown. In the present study, we demonstrated that magnolol significantly inhibited angiogenesis in vitro and in vivo evidenced by the attenuation of hypoxia and vascular endothelial growth factor (VEGF)-induced tube formation of human umbilical vascular endothelial cells, vasculature generation in chicken chorioallantoic membrane and Matrigel plug. In hypoxic human bladder cancer cells (T24), treatment with magnolol inhibited hypoxia-stimulated H2O2 formation, HIF-1α induction including mRNA, protein expression, and transcriptional activity as well as VEGF secretion. Additionally, the enhanced degradation of HIF-1α protein via enhancing prolyl hydroxylase activity and the decreased newly-synthesized HIF-1α protein in hypoxic T24 cells may involve the reduction of HIF-1α protein accumulation by magnolol. Interestingly, magnolol also acts as a VEGFR2 antagonist, and subsequently attenuates the down-stream AKT/mTOR/p70S6K/4E-BP-1 kinase activation both in hypoxic T24 cells and tumor tissues. As expected, administration of magnolol greatly attenuated tumor growth, angiogenesis and the protein expression of HIF-1α, VEGF, CD31, a marker of endothelial cells, and carbonic anhydrase IX, an endogenous marker for hypoxia, in the T24 xenograft mouse model. Collectively, these findings strongly indicate that the anti-agngiogenic activity of magnolol is, at least in part, mediated by suppressing HIF-1α/VEGF-dependent pathways, and suggest that magnolol may be a potential drug for human bladder cancer therapy....(more)
Chen MC, et al. Biochem Pharmacol 2013 May 1;85(9):1278-87.
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- 32. Anti-hepatitis B virus lignans from the root of Streblus asper.
Four new lignans, strebluslignanol F (1), (7'R,8'S,7″R,8″S)-erythro-strebluslignanol G (2), isomagnaldehyde (3) and isostrebluslignanaldehyde (4), along with 12 known lignans (5-16) were isolated from the ethyl acetate-soluble part of MeOH extract of the root of Streblus asper. Their structures were elucidated through various spectroscopic methods, including 1D NMR ((1)H NMR, (13)C NMR), 2D NMR (HMQC, HMBC and NOESY) and HRMS. The stereochemistry at the chiral centers was determined using CD spectra, as well as analyses of coupling constants and optical rotation data. The isolated lignans were evaluated for their anti-HBV activities in vitro using the HBV transfected HepG2.2.15 cell line. The most active lignans, (7'R,8'S,7″R,8″S)-erythro-strebluslignanol G, magnolol, isomagnolol and isolariciresinol, exhibited significant anti-HBV activities with IC50 values of 1.58, 2.03, 10.34 and 3.67 μM, respectively, for HBsAg with no cytotoxicity, and of 3.24, 3.76, 8.83 and 14.67 μM, respectively, for HBeAg with no cytotoxicity. (7'R,8'S,7″R,8″S)-erythro-Strebluslignanol G and magnolol showed significant anti-HBV activities to inhibit the replication of HBV DNA with the IC50 values of 9.02 and 8.67 μM, respectively....(more)
Li J, et al. Bioorg Med Chem Lett 2013 Apr 1;23(7):2238-44.
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- 33. Magnolol Pretreatment Prevents Sepsis-Induced Intestinal Dysmotility by Maintaining Functional Interstitial Cells of Cajal.
The purpose of this study was to investigate the mechanism by which magnolol treatment prevents lipopolysaccharide (LPS)-induced septic dysmotility in mice. Sepsis was induced by intravenous tail vein injection of LPS (4 mg/kg body weight). Animals were divided into three groups: the magnolol-treated septic group, the placebo-treated septic group, and the control group. Intestinal transit and circular smooth muscle contraction were measured 12 h after LPS injection, and immunocytochemisty was performed to study the morphology of interstitial cells of Cajal (ICCs). Stem cell factor (SCF) expression and c-kit phosphorylation were determined by Western blot analysis, and the mRNA levels of inducible NO synthase (iNOS) were determined by RT-PCR. Nitric oxide (NO) content, superoxide dismutase (SOD) activity, and malondialdehyde (MDA) concentration were detected using commercial kits. Intestinal transit and muscular contractility were significantly lower in the LPS-treated group than in the control group. Immunocytochemical experiments showed that the total number of ICCs, and the total and average lengths of the ICC processes were significantly decreased in the LPS-treated group compared with those in the control group. In LPS-treated animals, magnolol pretreatment significantly accelerated intestinal transit, increased circular muscle contraction, and prevented ICC morphology changes. Phosphorylation of c-kit and expression of SCF were significantly downregulated in LPS-treated animals compared with control animals. Magnolol pretreatment prevented sepsis-induced decreases in c-kit phosphorylation and SCF expression in LPS-treated animals. Magnolol pretreatment prevented the sepsis-induced increase in NO concentration, iNOS expression, and MDA concentration, and decrease in SOD activity in LPS-treated animals. Our results suggest that magnolol treatment prevents sepsis-induced intestinal dysmotility by regulating SCF/c-kit and NO signaling to maintain functional ICCs....(more)
Miao B, et al. Inflammation 2013 Feb 24.
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- 34. Effects of magnolol on impairment of learning and memory abilities induced by scopolamine in mice.
Alzheimer's disease (AD), one of the most common forms of dementia, is primarily ascribed to the cholinergic deficits and neuronal dysfunction. Magnolol (Mag), a bioactivator extracted from Magnolia officinalis, has protective effects on cholinergic neurons, but the specific mechanism remains unknown. To further evaluate the therapeutic effects of Mag on the learning and memory impairment in a scopolamine (Scop)-induced mouse model, the passive avoidance and the Morris water maze tests, the measurement of the ratio of brain/hippocampus to body weight, activities of acetyl cholinesterase (AChE), superoxide dismutase (SOD), total nitric oxide synthase (total NOS) and the content of methane dicarboxylic aldehyde (MDA) in hippocampus homogenate as well as the immunefluorescence staining of the AChE positive nerve fibers were performed. Therapeutically treated with Mag, the impaired abilities of learning and memory of the Scop-induced mice were almost restored to the native levels. The restored AChE, total NOS and SOD activities and the MDA level were observed, with a relatively normal density of AChE positive nerve fibers in hippocampus CA3 molecular layer. The improving efficacy of Mag on learning and memory impairment induced by Scop is dose-dependent, indicating that Mag has potential neuroprotective effects against neuronal impairment and memory dysfunction induced by Scop in mice. The underlying mechanisms may be associated with the anti-oxidative effects of Mag and its protective effects on hippocampus cholinergic neurons....(more)
Li YS, et al. Biol Pharm Bull 2013 May 1;36(5):764-71.
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- 35. P27/Kip1 Is Responsible for Magnolol-Induced U373 Apoptosis in Vitro and in Vivo.
Previously, we demonstrated that magnolol, a hydroxylated biphenyl compound isolated from the bark of Magnolia officinalis , at low concentrations (3-10 μM) exerted an antiproliferation effect in colon cancer, hepatoma, and glioblastoma (U373) cell lines through upregulation of the p21/Cip1 protein. Magnolol at a higher concentration of 100 μM, however, induced apoptosis and upregulated p27/Kip1 expression in U373. In the present study, we further studied whether the increased p27/Kip1 expression contributes to the magnolol-induced apoptosis in U373. Our data show that knock-down of p27/Kip1 expression significantly suppressed the magnolol-induced apoptosis, suggesting that p27/Kip1 might play an important role in the regulation of magnolol-induced apoptosis. This notion was further supported by demonstrating that magnolol induced an increase of the caspase activity in U373 in vitro and in vivo, and these effects were abolished by pretransfection of the cell with p27/Kip1 siRNA. To delineate the possible signaling pathways involved in the magnolol-induced increases of p27/Kip1 expression and apoptosis, we found that magnolol (100 μM) increased the levels of phosphorylated cSrc (p-cSrc), p-ERK, p-p38 MAP kinase (p-p38 MAPK), and p-AKT but not p-JNK in U373. Moreover, pretreatment of U373 with a cSrc inhibitor (PP2), a PI3K inhibitor (LY294002), an ERK inhibitor (PD98059), or a p38 MAPK inhibitor (SB203580) but not a JNK inhibitor (SP600125) significantly reduced the magnolol-induced increases of p27/Kip1 protein levels and apoptosis. Taken together, our data suggest that magnolol at a higher concentration of 100 μM induced apopotosis in U373 cells through cSrc-mediated upregulation of p27/Kip1....(more)
Chen LC, et al. J Agric Food Chem 2013 Mar 7.
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