- 1. Microwaves and tea: new tools to process plant tissue for transmission electron microscopy.
Optimizing sample processing, reducing the duration of the preparation of specimen, and adjusting procedures to adhere to new health and safety regulations, are the current challenges of plant electron microscopists. To address these issues, plant processing protocols for TEM, combining the use of polyphenolic compounds as substitute for uranyl acetate with microwave technology are being developed. In the present work, we optimized microwave-assisted processing of different types of plant tissue for ultrastuctural and immunocytochemical studies. We also explored Oolong tea extract as alternative for uranyl acetate for the staining of plant samples. We obtained excellent preservation of cell ultrastructure when samples were embedded in epoxy resin, and of cell antigenicity, when embedded in LR-White resin. Furthermore, Oolong tea extract successfully replaced uranyl acetate as a counterstain on ultrathin sections, and for in block staining. These novel protocols reduce the time spent at the bench, and improve safety conditions for the investigator. The preservation of the cell components when following these approaches is of high quality. Altogether, they offer significant simplification of the procedures required for electron microscopy of plant ultrastructure....(more)
Carpentier A, et al. J Microsc 2012 Jul;247(1):94-105.
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- 2. Examination of electron stains as a substitute for uranyl acetate for the ultrathin sections of bacterial cells.
Electron staining reagents were examined to find a possible substitute for uranyl acetate (UA) in electron microscopy of bacterial ultrathin sections. Four kinds of stains, platinum blue (Pt-blue), oolong tea extract (OTE), potassium permanganate (KMnO(4)) and phosphotungstic acid (PTA), were examined in comparison with UA either with or without post-staining with lead citrate (Pb). Electron microscopy was performed on sections from Spurr-embedded cells of a Gram-positive bacterium, Bacillus cereus NBRC 13597, and a Gram-negative bacterium, Escherichia coli NBRC 3301. Both Pt-blue and OTE showed staining similar to each other and to that of double staining with UA and Pb in B. cereus, while in E. coli the cytoplasmic membrane appeared less dense when compared with UA and Pb. KMnO(4) stained excessively to some extent, but showed images of the best contrast in the cytoplasmic membrane comparable with UA and Pb among the four reagents. PTA could stain the peptidoglycan layer but gave images of low quality for both bacteria. This study demonstrated that none of the reagents examined showed staining results of the same quality or better than the conventional method with UA and Pb. However, stains of Pt-blue, OTE and KMnO(4) could possibly be an alternative candidate for the UA according to the structure in question....(more)
Yamaguchi K, et al. J Electron Microsc (Tokyo) 2010;59(2):113-8.
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- 3. A novel dietary supplement containing multiple phytochemicals and vitamins elevates hepatorenal and cardiac antioxidant enzymes in the absence of significant serum chemistry and genomic changes.
A novel dietary supplement composed of three well-known phytochemicals, namely, Salvia officinalis (sage) extract, Camellia sinensis (oolong tea) extract, and Paullinia cupana (guarana) extract, and two prominent vitamins (thiamine and niacin) was designed to provide nutritional support by enhancing metabolism and maintaining healthy weight and energy. The present study evaluated the safety of this dietary supplement (STG; S=sage; T=tea; G=guarana) and assessed changes in target organ antioxidant enzymes (liver, kidneys and heart), serum chemistry profiles and organ histopathology in Fisher 344 rats. Adult male and female Fisher 344 rats were fed control (no STG) or STG containing (1X and 7X, 1X=daily human dose) diets and sacrificed after 2 and 4 months. Serum chemistry analysis and histopathological examination of three vital target organs disclosed no adverse influence on protein, lipid and carbohydrate profiles, genomic integrity of the liver and/or the tissue architecture. However, analysis of the most important antioxidant components in the liver, kidney and heart homogenates revealed a dramatic increase in total glutathione concentrations, glutathione peroxidase and superoxide dismutase enzyme activities. Concomitantly, oxidative stress levels (malondialdehyde accumulation) in these three organs were less than control. Organ specific serum markers (ALT/AST for the liver; CPK/AST for the heart; BUN/creatinine for kidneys) and the genomic integrity disclosed no STG-induced alteration. Some of the serum components (lipid and protein) showed insignificant changes. Overall, STG-exposed rats were more active, and the results suggest that STG exposure produces normal serum chemistry coupled with elevated antioxidant capacity in rats fed up to seven times the normal human dose and does not adversely influence any of the vital target organs. Additionally, this study reiterates the potential benefits of exposure to a pharmacologically relevant combination of phytochemicals compared to a single phytochemical entity....(more)
Bulku E, et al. Oxid Med Cell Longev 2010 Mar-Apr;3(2):129-44.
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- 4. Beneficial effects of oolong tea consumption on diet-induced overweight and obese subjects.
OBJECTIVE:
To determine the anti-obesity effects of oolong tea on diet-induced overweight or obesity.
METHODS:
A total of 8 g of oolong tea a day for 6 weeks was ingested by 102 diet-induced overweight or obese subjects. The body fat level of the subjects was determined at the same time by taking body weight, height and waist measurements. The thickness of the subcutaneous fat layer was also determined on the abdomen 3 cm to the right of the navel by the ultrasonic echo method. On the other hand, effects of oolong tea ingestion on plasma triglyceride (TG) and total cholesterol (TC) were determined. Inhibitions of pancreatic lipase by oolong tea extract and catechins in vitro were also determined.
RESULTS:
A total of 70% of the severely obese subjects did show a decrease of more than 1 kg in body weight, including 22% who lost more than 3 kg. Similarly, 64% of the obese subjects and 66% of the overweight subjects lost more than 1 kg during the experiment, and the subcutaneous fat content decreased in 12% of the subjects. The correlation between weight loss and subcutaneous fat decrease in men (r=0.055) was obviously lower than that in women (r=0.440, P<0.01). Body weight loss was signifificantly related to the decrease of the waist size in men (r=0.730, P<0.01) and women (r=0.480, P<0.01). Also, the correlation between subcutaneous fat reduction and decreased waist size was signifificant in women (r=0.554, P<0.01), but not in men (r=0.050, P>0.05). Moreover, the plasma levels of TG and TC of the subjects with hyperlipidemia were remarkably decreased after ingesting oolong tea for 6 weeks. In vitro assays for the inhibition of pancreatic lipase by oolong tea extract and catechins suggest that the mechanism for oolong tea to prevent hyperlipidemia may be related to the regulative action of oolong tea catechins in lipoprotein activity.
CONCLUSIONS:
Oolong tea could decrease body fat content and reduce body weight through improving lipid metabolism. Chronic consumption of oolong tea may prevent against obesity....(more)
He RR, et al. Chin J Integr Med 2009 Feb;15(1):34-41.
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- 5. [Use of the OTE-staining method for ultrathin sections on the example of microsporidia (Protozoa: Microsporidia)].
A novel method for staining ultrathin sections and examining organelles of taxonomic importance in microsporidian parasites was evaluated using oolong tea extract (OTE) and compared with traditional staining with uranyl acetate (UA). All basic intracellular structures of taxonomic significance were effectively stained with the OTE-staining method and additional layers of the polar filament with more clear boundaries between them were revealed. However, greater resolution and higher general contrast of several structures including membranes, layers of the envelope of mature spores, the structure of rough endoplasmic reticulum, Golgi complex, and nuclear chromatin were achieved with traditional UA-staining. The OTE-staining method has the advantage of being safe and preparations can be stored in light at room temperature with no loss in staining properties. However, greater staining time is required. We conclude that the OTE-staining method may be used as an alternative to traditional staining with UA with successful results....(more)
Miller AA, et al. Tsitologiia 2009;51(9):741-7. Russian.
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- 6. Oolong tea extract as a substitute for uranyl acetate in staining of ultrathin sections.
In conventional transmission electron microscopy, uranyl acetate staining is used to enhance the cellular components. However, uranyl acetate is considered a radioactive material that is very toxic if ingested or inhaled and subject to restrictions in many countries. In an attempt to introduce a substitute for uranyl acetate, we evaluated oolong tea extract (OTE) for staining of ultrathin sections. Tissue sections from normal rat liver representing an ideal model organ were processed according to a routine electron microscopic fixation and embedding procedure. Serial ultrathin sections were cut and processed with either routine double electron staining or 0.2% OTE staining for 30-40 min at room temperature followed by lead citrate staining (OTE staining method). Transmission electron microscopy observations revealed that all sub-cellular structures in hepatocytes were clearly visible with OTE staining and the quality of staining was highly compatible with those of routine double staining methods. It is suggested that OTE could be used as a non-radioactive and hazard-free substitute for uranyl acetate in transmission electron microscopy staining....(more)
Sato S, et al. J Microsc 2008 Jan;229(Pt 1):17-20.
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- 7. Suppression of postprandial hypertriglyceridemia in rats and mice by oolong tea polymerized polyphenols.
Oolong tea-polymerized polyphenols (OTPP) are characterized polyphenols produced from semi-fermented tea (oolong tea). In the present study, we evaluated the suppressive effects of oolong tea extract and OTPP on postprandial hypertriglyceridemia in rats and mice. Lymphatic recovery of triglycerides in rats cannulated in the thoracic duct was delayed by the administration of oolong tea extract at 100 and 200 mg per head, and more effectively than with green tea extract. OTPP delayed lymphatic triglyceride absorption at 20 mg/head, though (-)-epigallocatechin gallate (EGCG) did not do so at the same dose. OTPP also suppressed postprandial hypertriglyceridemia after administration of olive oil in mice. The area under the curve (AUC) of plasma triglycerides was significantly decreased, by 53% and 76%, in the 500 and 1,000 mg/kg OTPP groups respectively, as compared with the control group. These results suggest that OTPP is responsible for the suppression of hypertriglyceridemia by ingestion of oolong tea....(more)
Toyoda-Ono Y, et al. Biosci Biotechnol Biochem 2007 Apr;71(4):971-6.
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- 8. Melanogenesis inhibition by an oolong tea extract in b16 mouse melanoma cells and UV-induced skin pigmentation in brownish guinea pigs.
To investigate the new physiological functions of oolong tea, the effects on melanogenesis were studied. An oolong tea extract inhibited melanogenesis without affecting cell growth in B16 mouse melanoma cells. However, the oolong tea extract hardly showed any inhibitory effect on mushroom tyrosinase in a cell-free system. The effects of an oolong tea extract on the intracellular tyrosinase level in B16 cells were therefore studied. All the levels of activity, protein and mRNA were decreased in the oolong tea extract-treated cells. We also investigated the inhibitory effects of oolong tea on the pigmentation induced by ultraviolet B (UVB) by using brownish guinea pigs in vivo. The number of 3,4-dihydroxyphenylalanine (DOPA)-positive melanocytes increased by UVB was repressed by an oral administration of oolong tea. These results imply that oolong tea might be effective in whitening and that its inhibitory effect on melanogenesis was involved in the decrease of intracellular tyrosinase at the mRNA level....(more)
Aoki Y, et al. Biosci Biotechnol Biochem 2007 Aug;71(8):1879-85.
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- 9. Arbuscular mycorrhiza formation in cordate gametophytes of two ferns, Angiopteris lygodiifolia and Osmunda japonica.
Mycorrhizal symbiosis is common among land plants including pteridophytes (monilophytes and lycophytes). In pteridophytes with diplohaplontic life cycle, mycorrhizal formations were mostly reported for sporophytes, but very few for gametophytes. To clarify the mycorrhizal association of photosynthetic gametophytes, field-collected gametophytes of Angiopteris lygodiifolia (Marattiaceae, n = 52) and Osmunda japonica (Osmundaceae, n = 45) were examined using microscopic and molecular techniques. Collected gametophytes were mostly cut into two pieces. One piece was used for light and scanning microscopic observations, and the other for molecular identification of plant species (chloroplast rbcL sequences) and mycorrhizal fungi (small subunit rDNA sequences). Microscopic observations showed that 96 % (50/52) of Angiopteris and 95 % (41/43) of Osmunda gametophytes contained intracellular hyphae with arbuscules and/or vesicles and fungal colonization was limited to the inner tissue of the thick midribs (cushion). Fungal DNA analyses showed that 92 % (48/52) of Angiopteris and 92 % (35/38) of Osmunda have sequences of arbuscular mycorrhizal fungi, which were highly divergent but all belonged to Glomus group A. These results suggest that A. lygodiifolia and O. japonica gametophytes consistently form arbuscular mycorrhizae. Mycorrhizal formation in wild fern gametophytes, based on large-scale sampling with molecular identification of host plant species, was demonstrated for the first time....(more)
Ogura-Tsujita Y, et al. J Plant Res 2013 Jan;126(1):41-50.
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- 10. [Textual research on original plant of Chinese herbal medicine Cyrtomium Rhizome].
Through studies on morphological characteristics, distribution and ecological habitat described in ancient literatures, Osmunda japonica is believed to the original plant of Chinese herbal medicine Cyrtomium Rhizome. Meanwhile, analysis is also made on causes for descriptions that do not comply with characteristics of O. japonica such as toxicity, flowers and fruits, illustrations, indumentums and flakes as well as appearance of other original plants. It is suggested to list O. japonica as the only original plant of Cyrtomium Rhizome and distinguish it from other frequently seen medical plants. Separated studies are also conducted for pesticide effect and active ingredients of Dryoteris Crassrhizomae Rhizome and Woodwardia japonica that show better effects....(more)
Wang M, et al. Zhongguo Zhong Yao Za Zhi 2012 May;37(9):1337-40. Chinese.
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- 11. Cytological features of oogenesis and their evolutionary significance in the fern Osmunda japonica.
The development of the egg and canal cells in the fern Osmunda japonica Thunb. was studied during oogenesis by transmission electron microscopy. The mature egg possesses no fertilization pore and no typical egg envelope. In addition, an extra wall formed around the canal cells during oogenesis and apparently blocked protoplasmic connections between the egg and the canal cells. The periodic acid Schiff (PAS) reaction revealed that the extra wall was most likely composed of polysaccharides. Maturation of the egg was accompanied by the formation of a separation cavity above the egg and by some changes in the morphology of the nucleus and cytoplasmic organelles. The chromatin of the nucleus becomes condensed and the upper surface of the nucleus becomes closely associated with the plasmalemma. Amyloplasts in the egg cytoplasm were numerous and conspicuous, with most in close proximity to the nucleus. Finally, the cytoplasm on one side of the egg became vesiculated and the overlying plasmalemma was easily disrupted. These cytological features of the egg and the canal cells during oogenesis in O. japonica are markedly different from those of the leptosporangiate ferns and suggest a significant evolutionary divergence in reproductive cellular features between Osmundaceae and leptosporangiate ferns....(more)
Cao JG, et al. Sex Plant Reprod 2012 Mar;25(1):61-9.
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- 12. Fertility and precocity of Osmunda x intermedia offspring in culture.
The feasibility of later-generation hybrid production in ferns has not been previously studied, although it is a significant factor in relation to reproductive isolation. Osmunda x intermedia, a hybrid between O. japonica and O. lancea, is semifertile and has moderate spore germination rates. Under the artificial conditions of this study, F2 and F3 offspring were formed. Some of the F2 offspring showed precocity, and some of the F3 offspring also showed precocity. This fertility suggests that introgressive hybridization might be ongoing in nature. This also indicates a currently unknown genetic control over the timing of fertile frond production in Osmunda....(more)
Yatabe Y, et al. J Plant Res 2011 Mar;124(2):265-8.
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- 13. Genetic population structure of Osmunda japonica, rheophilous Osmunda lancea and their hybrids.
Rheophilous Osmunda lancea often hybridizes with a dryland ally, Osmunda japonica, to produce O. x intermedia, forming zonation in riverbanks and the adjacent dryland along flooding frequency clines. This study examined the genetic structure of populations consisting of O. x intermedia and the two parental species by analyzing ten nuclear DNA markers [six cleaved amplified polymorphic sequence (CAPS) markers and three simple sequence repeat (SSR) markers developed from an expressed sequence tag (EST) library, and the sequence of the glyceraldehyde-3-phosphate dehydrogenase gene GapCp] and chloroplast DNA sequences. The results suggest that the nuclear genes of O. japonica and O. lancea are genetically differentiated despite shared polymorphism in their chloroplast DNA sequences. This discrepancy may be attributable to natural selection and recent introgression, although it is not evident if introgression occurs between O. japonica and O. lancea in the examined populations. Our findings of putative F2 hybrids in O. x intermedia support its partial reproducibility, and also suggest that formation of later-generation hybrids generates morphological variation in O. x intermedia. O. lancea plants collected from geographically distant localities were genetically very similar, and it is suggested that O. lancea originated monotopically....(more)
Yatabe Y, et al. J Plant Res 2009 Nov;122(6):585-95.
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- 14. Identification of Dryopteris crassirhizoma and the adulterant species based on cpDNA rbcL and translated amino acid sequences.
Dry rhizome of Dryopteris crassirhizoma Nakai (Dryopteridaceae), also known as Guan Zhong, is a traditional Chinese herbal medicine used in the treatment of viral disease. But the dry rhizomes of Woodwardia JAPONICA (L. f.) Sm., OSMUNDA JAPONICA Thunb. and Cyrtomium fortunei J. Sm. are also used as Guan Zhong in local areas. The adulterants are similar to Dryopteris crassirhizoma. It is difficult to identify the botanical origin of these herbs. In our study, sequences of the cpDNA RBCL gene were determined and analyzed for Dryopteris crassirhizoma and adulterant species, where nineteen molecular markers had been determined. Also, amino acid sequences translated from the RBCL gene were analyzed and four important molecular markers were detected. Based on cpDNA RBCL and translated amino acid sequences, Dryopteris crassirhizoma can easily be distinguished from the other three fern species....(more)
Zhao ZL, et al. Planta Med 2007 Sep;73(11):1230-3.
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- 15. Ploidy chimeras induced in haploid sporophytes of Osmunda claytoniana and Osmunda japonica.
Haploid sporophytes of Osmunda claytoniana (2n = x = 22) were apogamously produced from calli when cultivated on a hormone-free medium. Flow cytometric analysis showed that ploidy chimeras were spontaneously produced in a haploid sporophyte of O. claytoniana and those of O. japonica that were obtained in the previous study. In the haploid sporophyte of O. claytoniana, a diploid pinnule and a partially diploid terminal segment were produced in a haploid pinna. In O. japonica, a haploid sporophyte yielded a diploid pinna in a haploid frond, and another haploid sporophyte yielded a diploid pinnule in a haploid pinna. Diploid chimeras were large in size and could be readily distinguished from other haploid parts of the fronds. It is likely that the chimeras were produced clonally from a single diploid cell that established chromosome doubling....(more)
Kawakami SM, et al. J Plant Res 2007 Sep;120(5):641-5.
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- 16. Comparative study of pharmacokinetics and tissue distribution of osthole in rats after oral administration of pure osthole and Libanotis buchtormensis supercritical extract.
ETHNOPHARMACOLOGICAL RELEVANCE:
Libanotis buchtormensis is the source of an important traditional medicine from Shaanxi province of China used in the treatment of many illnesses. Libanotis buchtormensis supercritical extract (LBSE) has analgesic, sedative and anti-inflammatory qualities. Osthole is one of the major bioactive components of LBSE; it is known for its significant anti-tumor, analgesic, and anti-inflammatory properties, it also alleviates hyperglycemia.
AIM OF THE STUDY:
The purpose of the present study was to compare the pharmacokinetics and tissue distribution of osthole in Sprague-Dawley (SD) rats after oral administration of pure osthole and LBSE. The two preparations were administered at the same osthole dose (approximately 130 mg/kg). The results should provide some guidance for the clinical applications of Libanotis buchtormensis.
MATERIALS AND METHODS:
Comparative pharmacokinetics and tissue distribution of osthole in SD rats after oral administration of pure osthole and LBSE were analyzed using reversed-phase high-performance liquid chromatography (RP-HPLC). All pharmacokinetic data were analyzed using 3P97 software. Samples of blood and internal organs (heart, liver, spleen, lungs and kidney) were collected and pretreated according to the experimental schedule. After pretreatment, plasma and tissue samples were extracted using ether-ethyl acetate mixture (3:1, v/v). The concentration of osthole in the plasma and tissues were determined using the RP-HPLC method.
RESULTS:
The procedure described in this paper shows good precision and stability and is suitable for the osthole assays in biological samples. We found that the average plasma concentration-time profile of osthole after oral administration of osthole and LBSE showed a single peak. There were also clear differences between plasma concentrations of osthole after oral administration of pure osthole and LBSE. Non-osthole ingredients in LBSE showed some pharmacokinetic interactions with osthole and hence decreased its absorption levels (p<0.05). Our results show different tissue distribution of osthole in the single and composite administration regimens.
CONCLUSIONS:
This study compares the pharmacokinetic characteristics and tissue distribution of osthole in rats after oral administration of pure osthole and LBSE; the results might be useful in clinical application of this traditional Chinese herbal medicine.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved....(more)
Shi J, et al. J Ethnopharmacol 2013 Jan 9;145(1):25-31.
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- 17. Osthole relaxes pulmonary arteries through endothelial phosphatidylinositol 3-kinase/Akt-eNOS-NO signaling pathway in rats.
Pulmonary arterial hypertension is a life-threatening disease lacking effective therapies. Osthole is a natural coumarin compound isolated from Angelica pubescens Maxim., which possesses hypotensive effect. Although its effects on isolated thoracic aorta (systemic circulating system) are clarified, it remains unclear whether Osthole relaxes isolated pulmonary arteries (PAs) (pulmonary circulating system). The aim of this study was to investigate the effects of Osthole on isolated PAs and the underlying mechanisms. We examined PA relaxation induced by Osthole in isolated human and rat PA rings with force-electricity transducers, the expression and activity of endothelial nitric oxide synthase (eNOS) and protein kinase B (Akt) with western blot, and nitric oxide (NO) production using DAF-FM DA fluorescent indicator. The results showed that Osthole elicited a dose-dependent vasorelaxation activity with phenylephrine-precontracted human and rat PA rings, which can be diminished by endothelium denudation and inhibition of eNOS, while having no effect on rat mesenteric arteries. Osthole increased NO release as well as activation of Akt and eNOS, indicated with increased phosphorylations of Akt at Ser-473 and eNOS at Ser-1177 in endothelial cells. PI3K inhibitor LY294002 also blocked Osthole induced vasodilation. In summary, dilative effect of Osthole was dependent on endothelial integrity and NO production, and was mediated by endothelial PI3K/Akt-eNOS-NO pathway. These may provide a new pulmonary vasodilator for the therapy of pulmonary arterial hypertension....(more)
Yao L, et al. Eur J Pharmacol 2013 Jan 15;699(1-3):23-32.
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- 18. Investigation of the biotransformation of osthole by liquid chromatography/tandem mass spectrometry.
Osthole is an active ingredient and one of the major coumarin compounds that were identified in the genus Cnidium moonnieri (L.) Cussion, the fruit of which was used as traditional Chinese medicine to treat male impotence, ringworm infection and blood stasis conventionally. Recent studies revealed that osthole has diverse pharmacological effects, such as improving male sexual dysfunction, anti-diabetes, and anti-hypertentions. The inhibition of thrombosis and platelet aggregation and protection of central nerve were also observed. On the other hand, the metabolism of osthole has not yet been investigated thoroughly. Herein the biotransformation of osthole in rat was investigated after oral administration of osthole by using efficient and sensitive ultra-performance liquid chromatography-tandem quadrupole-time of flight mass spectrometry (UPLC-QTOF/MS). Eighteen osthole metabolites and the parent drug were detected and identified in rat urine. Fourteen metabolites of osthole were identified and characterized for the first time. Structures of metabolites of osthole were elucidated by comparing fragment pattern under MS/MS scan and change of molecular weight with those of osthole. The main phase I metabolic pathways were summed as 7-demethylation, 8-dehydrogenation, hydroxylation on coumarin and 3,4-epoxide. Sulfate conjugates were detected as phase II metabolites of osthole....(more)
Li J, et al. J Pharm Biomed Anal 2013 Feb 23;74:156-61.
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- 19. Coumarins from the Herb Cnidium monnieri and Chemically Modified Derivatives as Antifoulants against Balanus albicostatus and Bugula neritina Larvae.
In the search for new environmental friendly antifouling (AF) agents, four coumarins were isolated from the herbal plant Cnidium monnieri, known as osthole (1), imperatorin (2), isopimpinellin (3) and auraptenol (4). Furthermore, five coumarin derivatives, namely 8-epoxypentylcoumarin (5), meranzin hydrate (6), 2'-deoxymetranzin hydrate (7), 8-methylbutenalcoumarin (8), and micromarin-F (9) were synthesized from osthole. Compounds 1, 2, 4, 7 showed high inhibitory activities against larval settlement of Balanus albicostatus with EC(50) values of 4.64, 3.39, 3.38, 4.67 μg mL-1. Compound 8 could significantly inhibit larval settlement of Bugula neritina with an EC(50) value of 3.87 μg mL-1. The impact of functional groups on anti-larval settlement activities suggested that the groups on C-5' and C-2'/C-3' of isoamylene chian could affect the AF activities....(more)
Wang ZC, et al. Int J Mol Sci 2013 Jan 9;14(1):1197-206.
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- 20. Osthole protects lipopolysaccharide-induced acute lung injury in mice by preventing down-regulation of angiotensin-converting enzyme 2.
The renin-angiotensin-aldosterone system (RAAS) plays an important role in the pathogenesis of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS). Angiotensin converting enzyme 2 (ACE2) plays a protective role in acute lung injury. Osthole, a natural coumarin derivative extracted from traditional Chinese medicines, is known to have anti-inflammatory effect, but the effect of osthole on the ALI is largely unknown. The aim of this study is to explore whether and by what mechanisms osthole protects lipopolysaccharide(LPS)-induced acute lung injury. Herein, we found that osthole had a beneficial effect on LPS-induced ALI in mice. As revealed by survival study, pretreatment with high doses of osthole reduced the mortality of mice from ALI. Osthole pretreatment significantly improved LPS-induced lung pathological changes, reduced lung wet/dry weight ratios and total protein in BALF. Osthole also inhibited the release of inflammatory mediators TNF-α and IL-6. Meanwhile, osthole markedly prevented the loss of ACE2 and Ang1-7 in lung tissue of ALI mice. ACE2 inhibitor blocked the protective effect of osthole in NR 8383 cell lines. Taken together, our study showed that osthole improved survival rate and attenuated LPS-induced ALI and ACE2 may play a role in it....(more)
Shi Y, et al. Eur J Pharm Sci 2013 Mar 12;48(4-5):819-24.
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- 21. A rapid and sensitive LC-MS/MS method for the determination of osthole in rat plasma: application to pharmacokinetic study.
Osthole, a major component isolated from the fruit of Cnidium monnieri (L.) Cusson, has been widely used in traditional Chinese medicine. We developed and validated a rapid and sensitive LC-MS/MS method for the quantification of osthole in rat plasma. Sample preparation involved simple liquid-liquid extraction by ethyl acetate after addition of imperatorin as internal standard (IS). The analyte was separated using a C18 column with the mobile phase of methanol-0.1% formic acid (80:20, v/v) at a flow rate of 0.4 mL/min. The elutes were detected under positive electrospray ionization in multiple reaction monitoring mode. The method was sensitive with 0.5 ng/mL as the lower limit of detection. Good linearity was obtained over the range of 1.0-500.0 ng/mL. The intra and inter-batch accuracy for osthole in rat plasma samples ranged from 99.5 to 108.1% and the variation was <8.9%. The stability, extraction efficiency and matrix effect were also acceptable. This method was successfully applied to the pharmacokinetic study of osthole in rat after intravenous and oral administration. Copyright © 2013 John Wiley & Sons, Ltd....(more)
Yun F, et al. Biomed Chromatogr 2013 May;27(5):676-80.
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- 22. Simultaneous determination of scopoletin, psoralen, bergapten, xanthotoxin, columbianetin acetate, imperatorin, osthole and isoimperatorin in rat plasma by LC-MS/MS for pharmacokinetic studies following oral administration of Radix Angelicae Pubescentis e
A rapid and sensitive bioassay based on liquid chromatography tandem mass spectrometry (LC-MS/MS) has been developed and validated for the simultaneous determination of eight coumarins in rat plasma. The liquid-liquid extraction method with ethyl acetate was used to prepare the plasma samples after addition of warfarin as an internal standard (IS). Chromatographic separation was performed on an Eclipse plus C18 column (100mm×4.6mm, 1.8μm) using gradient elution when 1mM ammonium acetate aqueous solution - acetonitrile was used as the mobile phase. The lower limit of quantitation (LLOQ) of each coumarin was lower than 2.16ngmL(-1). Intra-day and inter-day precisions were less than 15%. The accuracies were in the range of 88.9-117%. The mean recoveries of coumarins and IS were higher than 84%. The method was successfully applied to a pharmacokinetic study of eight coumarins in rats after oral administration of radix angelicae pubescentis....(more)
Chang YX, et al. J Pharm Biomed Anal 2013 Apr 15;77:71-5.
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- 23. Osthole ameliorates renal ischemia-reperfusion injury in rats.
BACKGROUND:
Renal ischemia-reperfusion (I/R) injury is a major cause of acute kidney injury. The pathogenetic mechanisms underlying I/R injury involve oxidative stress and apoptosis. Osthole, a natural coumarin derivative, has been reported to possess antioxidant and antiapoptotic activities. This study aimed to investigate the potential effects of osthole on renal I/R injury in an in vivo rat model.
MATERIALS AND METHODS:
We induced renal I/R injury by clamping the left renal artery for 45 min followed by reperfusion, along with a contralateral nephrectomy. We randomly assigned 54 rats to three groups (18 rats/group): sham-operated, vehicle-treated I/R, and osthole-treated I/R. We treated rats intraperitoneally with osthole (40 mg/kg) or vehicle (40 mg/kg) 30 min before renal ischemia. We harvested serum and kidneys at 1, 6, and 24 h after reperfusion. Renal function and histological changes were assessed. We also determined markers of oxidative stress and cell apoptosis in kidneys.
RESULTS:
Osthole treatment significantly attenuated renal dysfunction and histologic damage induced by I/R injury. The I/R-induced elevation in kidney malondialdehyde level decreased, whereas reduced kidney superoxide dismutase and catalase activities were markedly increased. Moreover, osthole-treated rats had a dramatic decrease in apoptotic tubular cells, along with a decrease in caspase-3 and an increase in the Bcl-2/Bax ratio.
CONCLUSIONS:
Osthole treatment protects murine kidney from renal I/R injury by suppressing oxidative stress and cell apoptosis. Thus, osthole may represent a novel practical strategy to prevent renal I/R injury.
Copyright © 2013 Elsevier Inc. All rights reserved....(more)
Zheng Y, et al. J Surg Res 2013 Feb 1.
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- 24. Combined anticancer activity of osthole and cisplatin in NCI-H460 lung cancer cells in vitro.
Drug combination therapies are common practice in the treatment of cancer. Cisplatin is the most active chemotherapeutic agent for lung cancer treatment. Osthole is a natural compound extracted from a number of medicinal plants. To determine whether osthole enhances the anticancer effect of cisplatin in human lung cancer, we treated NCI-H460 cells with osthole alone or in combination with cisplatin and evaluated cell growth and apoptosis using 3-(4,5-dimethyl thiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assay, flow cytometry and fluorescence microscopy. The results showed that, in comparison with single agent treatment, the combination of osthole and cisplatin resulted in greater efficacy in growth inhibition and apoptosis induction. Western blot analysis revealed that the combination effect of osthole and cisplatin was due to regulation of the Bcl-2 family proteins. Findings of this investigation suggested that osthole combined with cisplatin is a potential clinical chemotherapeutic approach in human lung cancer....(more)
Xu XM, et al. Exp Ther Med 2013 Mar;5(3):707-710.
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- 25. Osthole Improves Spatial Memory Deficits in Rats via Hippocampal α 1-Adrenergic and D 1 /D 2 Receptors.
The present study evaluated the effect of osthole, an active ingredient isolated from Cnidium monnieri L. Cusson, on spatial memory deficits caused by central neurotoxins using the Morris water maze in rats. The involvement of catecholaminergic receptors on the memory-enhancing effect of osthole in rat hippocampus was further investigated by intrahippocampal injection of catecholaminergic receptor antagonists. Intracisternal injection of osthole (10 μ g/brain) improved the spatial performance and working memory impairments caused by the catecholaminergic neurotoxin 6-hydroxydopamine. No significant differences in swimming speeds were observed among sham, neurotoxin-induced, and osthole-treated groups. Intracisternal osthole injection also attenuated the spatial performance and working memory impairments caused by the α 1 receptor antagonist phenoxybenzamine, the D1 receptor antagonist SCH 23390, and the D2 receptor antagonist sulpiride. Therefore, we demonstrated that the effect of osthole on improving spatial memory deficits may be related to the activation of hippocampal α 1 and D1/D2 receptors....(more)
Lin LW, et al. Evid Based Complement Alternat Med 2013;2013:273682.
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- 26. Human ether-a-go-go-related gene channel blockers and its structural analysis for drug design.
The human ether-a-go-go-related gene (hERG) is a K+ channel protein mainly expressed in the heart and the nervous systems and its blockade by non-cardiovascular acting drugs resulted in tachycardia and sudden death. In this present review, we have focused the physicochemical properties responsible for the hERG blocking activity of structurally different compounds. The reported research works showed that the hydrophobicity on the van der Waals (vdW) surface of the molecules (aroused from the aromatic ring) necessary for the hERG blocking activity along with topological and electronic properties. The quinolizidine alkaloids (natural products) such as oxymatrine, sophoridine, sophocarpine and matrine carry the common molecular structure of O=C=N-C-C-C-N that possessed positive ionotropic effect and hERG blocking activity. Acehytisine hydrochloride (previously named Guangfu base A) was isolated from the root of Aconitum coreanum (Levl.), is an anti-arrhythmic drug in phase IV clinical trial. The isoquinoline alkaloid, neferine (Nef) induces a concentration-dependent decrease in current amplitude (IC50 of 7.419 MM). Most of these natural product compounds contain non-flexible aromatic structures but have significant activity due to the presence of optimum hydrophobicity. Recent research works revealed that Eag and hERG channels are expressed by a variety of cancer cell lines and tissues. The Eag channel showed an oncogenic potential while hERG channels are associated with more aggressive tumors and have a role in mediating invasion. This review concluded that the consideration of physicochemical properties necessary for the hERG blocking activity will guide to develop novel drugs with less cardiotoxicity....(more)
Narayana Moorthy NS, et al. Curr Drug Targets 2013 Jan 1;14(1):102-13.
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- 27. Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.
The human ether-a-go-go-related gene (hERG) encodes the rapidly activating, delayed rectifier potassium channel (IKr) important for cardiac repolarization. Dysfunction of the hERG channel can cause Long QT Syndrome (LQTS). A wide variety of structurally diverse therapeutic compounds reduce the hERG current by acute direct inhibition of the hERG current or/and selective disruption of hERG protein expression. Arsenic trioxide (As(2)O(3)), which is used to treat acute promyelocytic leukemia, can cause LQTS type 2 (LQT2) by reducing the hERG current through the diversion of hERG trafficking to the cytoplasmic membrane. This cardiotoxicity limits its clinical applications. Our aim was to develop cardioprotective agents to decrease As(2)O(3)-induced cardiotoxicity. We reported that superfusion of hERG-expressing HEK293 (hERG-HEK) cells with matrine (1, 10 μM) increased the hERG current by promoting hERG channel activation. Long-term treatment with 1 μM matrine or oxymatrine increased expression of the hERG protein and rescued the hERG surface expression disrupted by As(2)O(3). In addition, Matrine and oxymatrine significantly shortened action potential duration prolonged by As(2)O(3) in guinea pig ventricular myocytes. These results were ascribed to the up-regulation of hERG at both mRNA and protein levels via an increase in the expression of transcription factor Sp1, an established transactivator of the hERG gene. Therefore, matrine and oxymatrine may have the potential to cure LQT2 as a potassium channel activator by promoting hERG channel activation and increasing hERG channel expression....(more)
Zhang Y, et al. Biochem Pharmacol 2013 Jan 1;85(1):59-68.
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- 28. Kinetics and computational docking studies on the inhibition of tyrosinase induced by oxymatrine.
A combination of enzymatic inhibition kinetics and computational prediction was employed to search for an effective inhibitor of tyrosinase. We found that oxymatrine significantly inhibited tyrosinase, and that this reaction was not accompanied by detectable conformational changes. Kinetic analysis showed that oxymatrine reversibly inhibited tyrosinase in a mixed-type manner. Measurements of intrinsic and ANS-binding fluorescences showed that oxymatrine did not induce any conspicuous changes in the tertiary structure. We also conducted a docking simulation between tyrosinase and oxymatrine using two docking programs, Dock6.3 and AutoDock4.2 (binding energy was -118.81 kcal/mol for Dock6 and -8.04 kcal/mol for AutoDock4). The results also suggested that oxymatrine interacts mostly with the residues of CYS83 and HIS263 in the active site of tyrosinase. This strategy of predicting tyrosinase inhibition by simulation of docking coupling with kinetics may prove useful in screening for potential tyrosinase inhibitors. Knowledge of tyrosinase inhibition can provide medical, cosmetic, and agricultural applications. Our study suggests that oxymatrine is an important agent for various applications related to pigment formation....(more)
Liu XX, et al. Appl Biochem Biotechnol 2013 Jan;169(1):145-58.
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- 29. Effect of oxymatrine, the active component from Radix Sophorae flavescentis (Kushen), on ventricular remodeling in spontaneously hypertensive rats.
PURPOSE:
To examine the effects of oxymatrine (OMT) on ventricular remodeling in spontaneous hypertension rat (SHR) and the underlying mechanism.
METHODS:
SHRs were divided into four groups: SHR control, SHR+40 mg/kg captopril, SHR+30 mg/kg OMT and SHR+60 mg/kg OMT. Normotensive age-matched WKY rats were assigned to two groups: WKY control, WKY+30 mg/kg OMT. The rats were orally administered with the corresponding drugs or drinking water for 21 weeks. Mean arterial blood pressure (MAP) and heart rate (HR) were measured. The left ventricular weight index (LVWI) and heart weight index (HWI) were determined. Myocardium tissue was stained with picric acid/Sirius red for measurement of collagen content measurements. The concentrations of serum norepinephrine and angiotensin II (Ang II) in myocardium were determined. Real-time RT-PCR was used to detect the mRNA expressions of transforming growth factor-β1 (TGF-β1), collagen types I, III and angiotensin converting enzyme (ACE). Western blots were performed to determine bioactivities of extracellular signal regulated kinase (ERK1/2), c-Jun N-terminal kinase (JNK/SAPK), p38 mitogen-activated protein kinases (p38 MAPK) and phospho-specic protein kinase C (PKC).
RESULTS:
In the SHR, hypertension, myocardium hypertrophy, more cardiac fibrosis, higher concentrations of serum norepinephrine and myocardium Ang II were observed. OMT treatment lowered the blood pressure, reduced the concentrations of serum norepinephrine and myocardium Ang II, favorably decreased the measured gravimetric parameters, decreased the interstitial and perivascular collagen deposition, attenuated the collagen of type I and III accumulation, downregulated the mRNA expression of ACE and TGF-β1, and suppressed the phosphorylation of ERK 1/2, JNK and p38 MAPK in SHRs.
CONCLUSION:
OMT prevents ventricular remodeling in SHR. The mechanisms may be related to inhibiting the gene overexpression of ACE and TGF-β1, suppressing the activation of signaling pathways of ERK 1/2, JNK and p38 MAPK.
Copyright © 2012 Elsevier GmbH. All rights reserved....(more)
Huang XY, et al. Phytomedicine 2013 Feb 15;20(3-4):202-12.
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- 30. Neuroprotective effects of oxymatrine against excitotoxicity partially through down-regulation of NR2B-containing NMDA receptors.
Oxymatrine (OMT) is a major bioactive component derived from Sophora flavescens Ait (kushen), which is widely used in Chinese medicine. Recent studies have shown that it has neuroprotective effects; however, its underlying mechanisms remain unclear. We focus on the mechanisms of pharmacologic action in OMT by detecting its pharmacological properties against focal cerebral ischemia in vivo and NMDA-induced neurotoxicity in vitro. OMT prevented cerebral ischemic injury in mice induced via a 2 h middle cerebral artery occlusion and a 24 h reperfusion, in vivo. In vitro cultured neurons challenged with N-methyl-D-aspartate (NMDA, 200 μM) for 30 min showed significant decrease in the viability of neurons; however, OMT was able to protect neurons against induced neurotoxicity via NMDA exposure. Western blot analysis revealed that OMT decreased the expression of Bax and repaired the balance of pro- and anti-apoptotic proteins. Furthermore, OMT significantly reversed the up-regulation of NR2B and inhibited the calcium overload in the cultured neurons after challenging the NMDA. OMT showed partial protection in the cortical neurons via down-regulation of NR2B containing NMDA receptors and up-regulation of Bcl-2 family. Our results provide new insights into the development of natural therapeutic anti-oxidants against ischemia....(more)
Zhang K, et al. Phytomedicine 2013 Feb 15;20(3-4):343-50.
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- 31. Combining Oxymatrine or Matrine with Lamivudine Increased Its Antireplication Effect against the Hepatitis B Virus In Vitro.
Some recent clinical reports have shown that the combination of oxymatrine, a phyto-derived drug, with lamivudine (3TC) could improve its curative effect against hepatitis B virus (HBV) infection. However, the experimental data in support of this combination strategy are lacking. In this study, we investigated the anti-HBV activity of the combination of 3TC and either oxymatrine or matrine on HepG2 2.2.15 in vitro. The activities of the combination and the solo compound, each in different concentrations, were compared on the 3rd, 6th, and 9th experimental days. The cytotoxicity results showed that the nontoxic concentrations of both oxymatrine and matrine to HepG2 2.2.15 cells were 800 μg/mL. We found that the single use of oxymatrine below 100 μg/ml, matrine below 200 μg/ml, and 3TC below 30 μg/ml showed weak inhibitory effects on the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV-DNA in culture media; the combination of 3TC (30 μg/ml) with oxymatrine (100 μg/ml) or matrine (100 μg/ml) showed significant inhibitory effects that were higher than or equivalent to the single use of 3TC at 100 μg/ml. The results provide a new impetus to develop novel, multicomponent anti-HBV drugs through the combination of natural products with nucleoside analogs to enhance their activity....(more)
Ma ZJ, et al. Evid Based Complement Alternat Med 2013;2013:186573.
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- 32. Oxymatrine protects against myocardial injury via inhibition of JAK2/STAT3 signaling in rat septic shock.
Oxymatrine (OMT), an alkaloid extracted from Sophora japonica (kushen), is used to treat inflammatory diseases and various types of cancer in traditional Chinese medicine. However, the cellular and molecular mechanisms underlying the antiinflammatory activity of OMT remain poorly understood. The present study explored the protective effect of OMT on myocardial injury in rats with septic shock by inhibiting the activation of the janus kinasesignal transducer and activator of transcription (JAK/STAT) signaling pathway. OMT treatment was found to significantly inhibit the activation of JAK2 and STAT3 in myocardial tissue. It also attenuated the expression of proinflammatory cytokines, including interleukin1β and tumor necrosis factorα. In addition, OMT exhibited antiinflammatory properties as heart function and myocardial contractility was improved and pathological and ultrastructural injury was prevented in myocardial tissue induced by septic shock. The results indicate that OMT exhibits substantial therapeutic potential for the treatment of septic shockinduced myocardial injury through inhibition of the JAK2/STAT3 signaling pathway....(more)
Zhang M, et al. Mol Med Rep 2013 Apr;7(4):1293-9.
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- 33. Oxymatrine Prevents NF-κB Nuclear Translocation And Ameliorates Acute Intestinal Inflammation.
Oxymatrine is a traditional Chinese herbal product that exhibits anti-inflammatory effects in models of heart, brain and liver injury. We investigated the impact of oxymatrine in an acute model of intestinal injury and inflammation. Oxymatrine significantly decreased LPS-induced NF-κB-driven luciferase activity, correlating with diminished induction of Cxcl2, Tnfα and Il6 mRNA expression in rat IEC-6 and murine BMDC. Although oxymatrine decreased LPS-induced p65 nuclear translocation and binding to the Cxcl2 gene promoter, this effect was independent of IκBα degradation/phosphorylation. DSS-induced weight loss and histological damage were ameliorated in oxymatrine-treated C57BL/6-WT-mice. While this effect correlated with reduced colonic Il6 and Il1β mRNA accumulation, global NF-κB activity as measured in NF-κB(EGFP) mice was unaffected. Our data demonstrate that oxymatrine reduces LPS-induced NF-κB nuclear translocation and activity independently of IκBα status, prevents intestinal inflammation through blockade of inflammatory signaling and ameliorates overall intestinal inflammation in vivo....(more)
Guzman JR, et al. Sci Rep 2013 Apr 9;3:1629.
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- 34. [Effect of oxymatrine on vascular calcification of humans umbilical vein smooth muscle cells and its underlying mechanism].
OBJECTIVE:
To observe the effect of oxymatrine (OMT) on calcification of humans umbilical vein smooth muscle cells and its underlying mechanism.
METHOD:
Human umbilical vein smooth muscle cells (HUSMCs) were calcified by beta-giycerophos-phosphate (beta-GP) and then divided into 6 groups: the control group, the calcification group, the pure OMT group, and lower, middle and higher-dosage OMT groups. Cell calcification were observed by Von Kossa staining, calcium content in HUSMCs were determined by the colorimetric method, the alkaline phosphatase (ALP) activity in HUSMCs were determined by phenyl diphosphate-2-sodium, the osteocalcin (OC) level in HUSMCs were determined by radioimmunossay, the transforming growth factor-beta1 (TGF-beta1) level in HUSMC culture medium and the content changes in psmad2/3 and smad2/3 were determined by the ELISA method, and the expression of Core binding factor alpha1 (Cbfalpha1) protein in HUSMCs were determined by western blot method.
RESULT:
Compared with the control group, the calcification group showed a great number of black granules among the smooth muscle cells and significant increase in the content of calcium and OC and the activity of ALP; OMT intervention can decrease the content of calcium, OC, TGF-beta1, psmad2/3 and Cbfalpha1 and the activity of ALP. And high-dosage OMT group had better effect than middle and low-dosage groups.
CONCLUSION:
OMT can effectively inhibit beta-GP-induced HUSMC calcification and its effect on reducing TGF-beta1, psmad2/3 and Cbfalpha1 may be one of its mechanisms in inhibiting HVSMC calcification....(more)
Wang X, et al. Zhongguo Zhong Yao Za Zhi 2012 Apr;37(7):1002-6. Chinese.
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- 35. Observation of antinociceptive effects of oxymatrine and its effect on delayed rectifier K? currents (Ik) in PC12 cells.
In order to observe antinociceptive effect of Oxymatrine (OMT) and its effect on voltage-activated K(+) channel, the acetic acid-induced abdominal contraction model of mouse was used to test the antinociceptive effect in vivo, and in vitro, the delayed rectifier K(+) currents (Ik) in PC12 cells (rat pheochromocytoma cells) was recorded using the automated patch-clamp method. The results indicated that after application of OMT, the number of acetic acid-induced animal abdominal contraction was significantly decreased, Ik in PC12 cells was significantly decreased, and showed a concentration-dependent manner. After application of OMT, both the activation and inactivation curves of Ik of PC12 cells were shifted to negative potentials. This study revealed that OMT showed antinociceptive effect in mice. The inhibition of voltage-activated K(+) channel might be one of mechanisms in which the enhanced both activation and inactivation of K(+) channel were involved and might play important roles....(more)
Wang Y, et al. Neurochem Res 2012 Oct;37(10):2143-9.
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