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Showing papers in "Planta Medica in 1995"


Journal ArticleDOI
TL;DR: The pharmacological properties of the oil support the traditional use of N. sativa and its derived products as a treatment for rheumatism and related inflammatory diseases and is greater than is expected from its content of thymoquinone.
Abstract: Samples of the expressed fixed oil from different sources of Nigella sativa seeds were examined by thin-layer and gas chromatography for content of fixed oils and thymoquinone, and these substances were tested as possible inhibitors of eicosanoid generation and membrane lipid peroxidation The crude fixed oil and pure thymoquinone both inhibited the cyclooxygenase and 5-lipoxygenase pathways of arachidonate metabolism in rat peritoneal leukocytes stimulated with calcium ionophore A23187, as shown by dose-dependent inhibition of thromboxane B2 and leukotriene B4, respectively Thymoquinone was very potent, with approximate IC50 values against 5-lipoxygenase and cyclo-oxygenase of < 1 microgram/ml and 35 micrograms/ml, respectively Both substances also inhibited non-enzymatic peroxidation in ox brain phospholipid liposomes, but thymoquinone was about ten times more potent However, the inhibition of eicosanoid generation and lipid peroxidation by the fixed oil of N sativa is greater than is expected from its content of thymoquinone (ca 02% w/v), and it is possible that other components such as the unusual C20:2 unsaturated fatty acids may contribute also to its anti-eicosanoid and antioxidant activity These pharmacological properties of the oil support the traditional use of N sativa and its derived products as a treatment for rheumatism and related inflammatory diseases

850 citations


Journal ArticleDOI
TL;DR: It is demonstrated that apigenin is a ligand for the central benzodiazepine receptors exerting anxiolytic and slight sedative effects but not being anticonvulsant or myorelaxant.
Abstract: The dried flower heads of Matricaria recutita L. (Asteraceae) are used in folk medicine to prepare a spasmolytic and sedative tea. Our fractionation of the aqueous extract of this plant led to the detection of several fractions with significant affinity for the central benzodiazepine receptor and to the isolation and identification of 5,7,4'-trihydroxyflavone (apigenin) in one of them. Apigenin competitively inhibited the binding of flunitrazepam with a Ki of 4 microM and had no effect on muscarinic receptors, alpha 1-adrenoceptors, and on the binding of muscimol to GABAA receptors. Apigenin had a clear anxiolytic activity in mice in the elevated plusmaze without evidencing sedation or muscle relaxant effects at doses similar to those used for classical benzodiazepines and no anticonvulsant action was detected. However, a 10-fold increase in dosage produced a mild sedative effect since a 26% reduction in ambulatory locomotor activity and a 35% decrement in hole-board parameters were evident. The results reported in this paper demonstrate that apigenin is a ligand for the central benzodiazepine receptors exerting anxiolytic and slight sedative effects but not being anticonvulsant or myorelaxant.

338 citations


Journal ArticleDOI
TL;DR: The results revealed that the anti-inflammatory and analgesic constituents from roots of AP were related to peripheral inhibition of inflammatory substances and to the influence on the central nervous system.
Abstract: In the present study, we extracted Angelica pubescens (AP) with various solvents in order to find the bioactive constituents that demonstrated analgesic and anti-inflammatory effects. The results were obtained as follows: (1) Methanol-, chloroform-, and ethyl acetate-extracts effectively reduced the pain that was induced by 1% acetic acid and a hot plate. (2) Methanol-, chloroform-, and ethyl acetate-extracts reduced the edema that was induced by 3% formalin or 1.5% carrageenan. (3) Sixteen compounds have been isolated and identified from the roots of AP. Among these compounds, columbianadin, columbianetin acetate, bergapten, umbelliferone, and caffeic acid significantly demonstrated anti-inflammatory and analgesic activities at 10 mg/kg. However, only osthole and xanthotoxin revealed anti-inflammatory activity. Isoimperatorin only demonstrated an analgesic effect. These results revealed that the anti-inflammatory and analgesic constituents from roots of AP were related to peripheral inhibition of inflammatory substances and to the influence on the central nervous system.

317 citations


Journal ArticleDOI
TL;DR: These in vitro findings demonstrate that the essential oils provide virucidal activity against enveloped viruses by interfering with the function of virus envelope.
Abstract: The steam distillate prepared from fresh plants of Houttuynia cordata Thunb. (Saururaceae) was found to have direct inhibitory activity against herpes simplex virus type 1 (HSV-1), influenza virus, and human immunodeficiency virus type 1 (HIV-1) without showing cytotoxicity, but not against poliovirus and coxsackie-virus. The loss of viral infectivity was related to the duration of drug treatment. Three major components of the distillate, methyl n-nonyl ketone, lauryl aldehyde, and capryl aldehyde, also inactivated HSV-1, influenza virus, and HIV-1. These in vitro findings demonstrate that the essential oils provide virucidal activity against enveloped viruses by interfering with the function of virus envelope.

196 citations


Journal ArticleDOI
TL;DR: Three triterpenes were isolated from Diospyros leucomelas and identified as betulin, betulinic acid, and ursolic acid and showed anti-inflammatory activity in the carrageenan and serotonin paw edema tests and TPA and EPP ear edema Tests.
Abstract: Three triterpenes were isolated from Diospyros leucomelas and identified as betulin, betulinic acid, and ursolic acid. They showed anti-inflammatory activity in the carrageenan and serotonin paw edema tests and TPA and EPP ear edema tests. The blockade of their effects by progesterone, actinomycin D, and cycloheximide has served to determine the mechanism of action in relationship with that of glucocorticoids. Betulinic acid was the most affected and therefore a mode of action similar to these drugs may be postulated for it.

193 citations


Journal ArticleDOI
TL;DR: Only the last two drugs significantly increased the conversion of labelled acetate to liver cholesterol which indicates a deterrent effect of the allium products against the synthesis of a risk factor.
Abstract: On oral administration of onion (Allium cepa L) and garlic (A sativum L) sulfoxide amino acids viz, S-methylcysteine sulfoxide (SMCS) and S-allylcysteine sulfoxide (SACS) to alloxan-diabetic rats for a month, their diabetic condition, being characterized by glucose intolerance, weight loss, depletion of liver glycogen, etc, was ameliorated as comparable to rats treated with glibenclamide and insulin However, only the last two drugs significantly increased the conversion of labelled acetate to liver cholesterol which indicates a deterrent effect of the allium products against the synthesis of a risk factor

187 citations


Journal ArticleDOI
TL;DR: Four diterpenoids, carnosic acid, carnOSol, rosmanol, and epirosmanol were isolated as antioxidative agents from the leaves of Rosmarinus officinalis and were shown to be effective to protect biological systems against oxidative stresses.
Abstract: Four diterpenoids, carnosic acid (1), carnosol (2), rosmanol (3), and epirosmanol (4), were isolated as antioxidative agents from the leaves of Rosmarinus officinalis by bioassay-directed fractionation. These diterpenoids inhibited superoxide anion production in the xanthine/xanthine oxidase system. Mitochondrial and microsomal lipid peroxidation induced by NADH or NADPH oxidation were also completely inhibited by these diterpenes at the concentration of 3-30 microM. Furthermore, carnosic acid protected red cells against oxidative hemolysis. These phenolic diterpenes were shown to be effective to protect biological systems against oxidative stresses.

176 citations


Journal ArticleDOI
TL;DR: In vitro effect of some constituents of Ginkgo against lipid peroxidation and cell necrosis of isolated rat hepatocytes, and against superoxide anion which is generally implicated in cell damages are compared.
Abstract: Ginkgo biloba extract is known to be efficient in diseases associated with free radical generation. This study compares the in vitro effect of some constituents of Ginkgo against lipid peroxidation and cell necrosis of isolated rat hepatocytes, and against superoxide anion which is generally implicated in cell damages.

173 citations


Journal ArticleDOI
TL;DR: All triterpenoids were remarkably active against the edema produced by TPA, and the presence of a C-28 or C-30 carboxylic group and an alcoholic group at C- 28 increases the activity in carrageenan- and EPP-induced edemas, respectively.
Abstract: In order to establish the possible relationship between their chemical structures and pharmacological properties, the oral and topical anti-inflammatory activities of ten triterpenoids belonging to the lupane, oleanane, and ursane series, were evaluated. All triterpenoids were remarkably active against the edema produced by TPA. While the basic carbon skeleton has no influence on the activity, the presence of a C-28 or C-30 carboxylic group and an alcoholic group at C-28 increases the activity in carrageenan- and EPP-induced edemas, respectively.

170 citations


Journal ArticleDOI
TL;DR: Isolation of the fruit CH3OH extract of Terminalia citrina yielded five known tannins identified as corilagin, punicalagin, 1,3,6-tri-O-galloyl-beta-D-glucopyranose, chebulagic acid, and 1,2,3
Abstract: Isolation of the fruit CH3OH extract of Terminalia citrina yielded five known tannins identified as corilagin (1) (3), punicalagin (2) (4), 1,3,6-tri-O-galloyl-beta-D-glucopyranose (3) (5), chebulagic acid (4) (6), and 1,2,3,4,6-penta-O-galloyl-beta-D-glucopyranose (5) (7) by comparison of their physical and spectral data with those of authentic samples. These tannins were tested for antimicrobial action.

147 citations


Journal ArticleDOI
TL;DR: A total of 80 lipophilic and hydrophilic extracts obtained from 20 samples of cultured freshwater and terrestrial cyanobacteria were investigated for their biological activities, and 26% exhibited a significant lethal effect against brine shrimp.
Abstract: A total of 80 lipophilic and hydrophilic extracts obtained from 20 samples of cultured freshwater and terrestrial cyanobacteria were investigated for their biological activities. Of all the extracts, 26% exhibited a significant lethal effect against brine shrimp. Out of 54 extracts tested for antimicrobial activity, 78% showed antibacterial and 45% antifungal activities. Of 30 extracts tested for cytotoxicity against KB cells, none was found to be active. Bioassay-guided fractionation of the lipophilic extracts of Fischerella ambigua led to the isolation of three compounds; ambigols A (1) and B (2), and tjipanazole D (3). Compounds 1 and 2 exhibited antibacterial, antifungal, cytotoxic, molluscicidal, and anti-inflammatory, and antiviral activities. Tjipanazole D (3) showed moderate antibacterial properties.

Journal ArticleDOI
TL;DR: Diffractaic acid and usnic acid were identified as the analgesic and antipyretic components of a lichen, Usnea diffracta, and both compounds showed an analgesic effect by the acetic acid-induced writhing and tail-pressure methods in mice.
Abstract: Diffractaic acid and usnic acid were identified as the analgesic and antipyretic components of a lichen, Usnea diffracta. Both compounds showed an analgesic effect by the acetic acid-induced writhing and tail-pressure methods in mice. Regarding the effect on normal body temperature and LPS-induced hyperthermia in mice, diffractaic acid showed a significant effect only on the former and usnic acid only on the latter.

Journal ArticleDOI
TL;DR: Recent in vivo antitumor studies with parthenin and eupatoriopicrin are discussed as well as the reports of the antiulcer activity of dehydroleucodin, and research on the neurotoxicity of repin is highlighted.
Abstract: Aspects of recent research on the biological activities of sesquiterpene lactones (SQLs) are presented. Several SQLs have been identified as important constituents of plants consumed by animals for presumed medicinal value and is a focus of research in zoopharmacognosy. Recent in vivo antitumor studies with parthenin and eupatoriopicrin are discussed as well as the reports of the antiulcer activity of dehydroleucodin. Helenalin has recently been reported to have cardiotonic activity. Research on the neurotoxicity of repin, a compound reported to cause a Parkinson's-like disease in horses, is also highlighted.

Journal ArticleDOI
TL;DR: Two phenanthrenes were isolated from the aerial part of Dendrobium nobile Lindl and were found to be cytotoxic against A549, SK-OV-3, and HL-60 cell lines and antitumor activity on the life span of ICR mice intraperitoneally implanted with 1 x 10(6) cells of sarcoma 180.
Abstract: Two phenanthrenes were isolated from the aerial part of Dendrobium nobile Lindl. and their structures were identified to be 4,7-dihydroxy-2-methoxy-9,10-dihydrophenanthrene (1) and denbinobin (2), among which the former has been first isolated from this plant. These two compounds were found to be cytotoxic against A549 (human lung carcinoma), SK-OV-3 (human ovary adenocarcinoma), and HL-60 (human promyelocytic leukemia) cell lines. Compound 1 also showed antitumor activity on the life span of ICR mice intraperitoneally implanted with 1 x 10(6) cells of sarcoma 180.

Journal ArticleDOI
TL;DR: The results indicate that this representative class of polyphenols of Echinacea species protects collagen from free radical damage through a scavenging effect on reactive oxygen species and/or C-, N-, S-centered secondary radicals, and provide an indication for the topical use of extracts from Echinace species for the prevention/treatment of photodamage of the skin by UVA/UVB radiation.
Abstract: The protective effect of caffeoyl derivatives (echinacoside, chlorogenic acid, chicoric acid, cynarine, and caffeic acid, typical constituents of Echinacea species) on the free radical-induced degradation of Type III collagen has been investigated. The macromolecule was exposed to a flux of oxygen radicals (superoxide anion and hydroxyl radical) generated by the xanthine/xanthine oxidase/Fe2+/EDTA system and its degradation assessed qualitatively by SDS-PAGE and quantitatively as the amount of soluble peptides (according to the 4-hydroxyproline method) released from native collagen after oxidative stress. The SDS-PAGE pattern of native collagen is markedly modified by free radical attack, with formation of a great number of peptide fragments with molecular masses below 97 kDa: in the presence of microM concentrations of echinacoside, there is a complete recovery of the native profile. Collagen degradation was, in fact, dose-dependently inhibited by all the compounds, with the following order of potency: echinacoside approximately chicoric acid > cynarine approximately caffeic acid > chlorogenic acid, with IC50 ranging from 15 to 90 microM. These results indicate that this representative class of polyphenols of Echinacea species protects collagen from free radical damage through a scavenging effect on reactive oxygen species and/or C-, N-, S-centered secondary radicals, and provide an indication for the topical use of extracts from Echinacea species for the prevention/treatment of photodamage of the skin by UVA/UVB radiation, in which oxidative stress plays a crucial role.

Journal ArticleDOI
TL;DR: Almost all of the tested alkaloids showed cytotoxic activity against fibroblastic LMTK cells, and mesembrenone showed some specificity against Molt4 cells in comparison to LMTk cells, while lycorenine was found to be the most cytot toxic compound against HepG2 hepatoma.
Abstract: 25 Amaryllidaceae alkaloids belonging to different skeletal types were evaluated for their cytotoxic activity against one murine non-tumoral cell line (LMTK) and two human tumoral cell lines (Molt4 and HepG2) according to established protocols. Significant differences of activity related with the type of skeleton of the tested alkaloids could be observed. Pretazettine (22) was among the most active compound among the 25 tested alkaloids on the Molt4 lymphoid cells, but was inactive against HepG2 hepatoma. On the other hand, lycorenine (11) was found to be the most cytotoxic compound against HepG2 hepatoma, even though it appears to be active against Molt4 cells. Almost all of the tested alkaloids showed cytotoxic activity against fibroblastic LMTK cells. Only mesembrenone (25) showed some specificity against Molt4 cells in comparison to LMTK cells.

Journal ArticleDOI
TL;DR: Artemisinin levels in all studies were found to be highest at anthesis, and Artemisinin content was 4- to 11-fold higher in inflorescences than in leaves.
Abstract: Cuttings of a clone of A. annua L. (Asteraceae), grown under 16 h photoperiod for 55 days were transferred to six photoperiod treatments in the greenhouse. Under short photoperiods (8, 10, or 12 h), plants flowered after two weeks; plants under long photoperiods (16, 20, or 24 h) remained vegetative until termination of treatment after 10 weeks. When plants grown under long photoperiod treatments were transferred to 8-h photoperiod, flowering occurred 2 weeks later. Flower induction in plants grown under field conditions occurred when the photoperiod was determined to the 13.3 h. Artemisinin levels in all studies were found to be highest at anthesis. Artemisinin content was 4- to 11-fold higher in inflorescences than in leaves.

Journal ArticleDOI
TL;DR: The ensemble of results suggests that the hepatoprotection afforded by Sch B pretreatment may mainly be attributed to the enhancement in the functioning of the hepatic GSH anti-oxidant system, possibly through stimulating the activities of GSH related enzymes.
Abstract: Pretreating female Balb/c mice with schisandrin B (Sch B) at increasing daily doses (1-4 mmol/kg) for 3 days caused dose-dependent increases in hepatic glutathione S-transferase (GST) and glutathione reductase (GRD) activities However, the activities of glucose-6-phosphate dehydrogenase (G6PDH), Se-glutathione peroxidase (GPX), and gamma-glutamylcysteine synthetase (GCS) were down-regulated to varying degrees in a dose-dependent manner While there were biphasic changes in hepatic reduced glutathione (GSH) level as well as susceptibility of hepatic tissue homogenates to in vitro peroxide-induced GSH depletion, a gradual decrease in hepatic malondialdehyde content was observed The beneficial effect of Sch B on the hepatic GSH anti-oxidant system became more evident after CCl4 challenge The same Sch B pretreatment regimen caused a dose-dependent protection against carbon tetrachloride (CCl4)-induced hepatotoxicity The hepatoprotection was associated with significant enhancement in hepatic GSH status, as indicated by the substantial increase in tissue GSH levels and the corresponding decrease in susceptibility of tissue homogenates to GSH depletion Where the activities of GST and GRD were increased linearly over non-CCl4 control values, there was also a gradual elevation in G6PDH activity upon administration of increasing doses of Sch B In contrast, GPX activity was moderately down-regulated The ensemble of results suggests that the hepatoprotection afforded by Sch B pretreatment may mainly be attributed to the enhancement in the functioning of the hepatic GSH anti-oxidant system, possibly through stimulating the activities of GSH related enzymes

Journal ArticleDOI
TL;DR: DNA from dried or fresh roots of three medicinal Panax species and their adulterants were amplified by AP-PCR or RAPD and analysis of the degree of similarity of the fingerprints confirmed that P. ginseng is more closely related to P. quinquefolius than toP.
Abstract: DNA from dried or fresh roots of three medicinal Panax species and their adulterants were amplified by AP-PCR or RAPD. Fingerprints for P. ginseng or P. quinquefolius were found to be consistent irrespective of plant source or age. On the other hand, very different fingerprints were obtained from adulterants. Hence the PCR approach may be used as a means to authenticate the concerned Panax species. Analysis of the degree of similarity of the fingerprints confirmed that P. ginseng is more closely related to P. quinquefolius than to P. notoginseng.

Journal ArticleDOI
TL;DR: The results confirm the involvement of SDF in the hypoglycemic effect of T. foenum graecum seeds, however, compound(s) other than SDF is (are) also involved in thehypoglycemic activity.
Abstract: The whole powder of Trigonella foenum graecum seeds and its extracts were tested for their hypoglycemic effect on normal and diabetic model rats. The powder, its methanol extract, and the residue remaining after methanol extraction had significant hypoglycemic effects when fed simultaneously with glucose. The water extract of the methanol extractive-free residue of the seed powder showed significant hypoglycemic activity at different prandial states. The Soluble Dietary Fibre (SDF) fraction showed no effect on the fasting blood glucose levels of nondiabetic or NIDDM model rats. However, when fed simultaneously with glucose, it showed a significant hypoglycemic effect (p < 0.05) in NIDDM model rats. Chemical analysis showed that the major constituent of the SDF is a galactomannan. The results confirm the involvement of SDF in the hypoglycemic effect of T. foenum graecum seeds. However, compound(s) other than SDF is (are) also involved in the hypoglycemic activity.

Journal ArticleDOI
TL;DR: The essential oil, (R)-5-hydroxypyrrolidin-2-one, as well as the previously isolated rosmarinic acid and dehydropodophyllotoxine contributed to the antibacterial effects of H. verticillata.
Abstract: Several extracts of Hyptis verticillata and isolated compounds were evaluated for their anti-inflammatory, antibacterial, antisecretory, and cytotoxic properties. The aerial parts yielded (R)-5-hydroxypyrrolidin-2-one and essential oil with the main components alpha-pinene, beta-pinene, and thymol. Spectroscopic methods (UV, IR, 1H-NMR, 13C-NMR, mass, CD) fully characterized (R)-5-hydroxypyrrolidin-2-one, as it was isolated by a bioassay guided fractionation. The essential oil, (R)-5-hydroxypyrrolidin-2-one, as well as the previously isolated rosmarinic acid and dehydropodophyllotoxine contributed to the antibacterial effects of H. verticillata. Furthermore, rosmarinic acid showed significant capillary stabilizing effects. Sideritoflavone inhibited prostaglandin synthase to a significant extent and had antisecretory effects comparable to those of NPPB. The cytotoxicity of the aqueous extract, as demonstrated using KB and HT 29 cell lines, may be of toxicological relevance in cases of internal application.

Journal ArticleDOI
TL;DR: The compounds tested showed low toxicity and a pharmacological profile similar to other NSAI substances on reducing the edema induced by carrageenan and contractions induced by phenyl-p-quinone; the most active compounds were 1 and 2.
Abstract: Aethiopinone (1), an o-naphthoquinone diterpene from Salvia aethiopis L. roots and two hemisynthetic derivatives 2 and 3 have been evaluated for toxicity, anti-inflammatory, analgesic, antipyretic, and haemostatic activities. The compounds tested showed low toxicity and a pharmacological profile similar to other NSAI substances on reducing the edema induced by carrageenan and contractions induced by phenyl-p-quinone; the most active compounds were 1 and 2. In the same way and as expected with these types of substances, the bleeding time increased. In the TPA-induced ear inflammation model, the three compounds showed a moderate reduction of edema, and 1 produced a significant increase in the reaction time against thermal painful stimuli in the tail immersion test. The results demonstrated strong anti-inflammatory, peripheral and central analgesic properties for 1, as well as antiedematose topical action and peripheral analgesic properties for 2 and 3.

Journal ArticleDOI
TL;DR: The results indicate that the molecular mechanism of hepatoprotection afforded by FS pretreatment may involve the facilitation of GSH regeneration via the GRD-catalyzed and NADPH-mediated reaction.
Abstract: The effect of a lignan-enriched extract of the fruits of Schisandra chinensis (FS) on hepatic glutathione (GSH) status was examined in both control and carbon tetrachloride (CCl4)-treated rats. FS treatment caused a dose-dependent enhancement in hepatic GSH status, as evidenced by significant increases in hepatic GSH level and activities of hepatic glucose-6-phosphate and glutathione reductase (GRD), as well as a decreased susceptibility of hepatic tissue homogenates to in vitro peroxide-induced GSH depletion. The beneficial effect of FS treatment on hepatic GSH status became more evident after CCl4 challenge. Pretreating rats with FS extract at increasing daily doses ranged from 0.2 to 3.2 g/kg for 3 days caused a dose-dependent protection against the CCl4-induced impairment in hepatic GSH status. The enhancement in hepatic GSH status was associated with corresponding decreases in tissue malondialdehyde levels and plasma alanine aminotransferases activities, indicating a significant reduction in the extent of oxidative hepatocellular damage. Our results indicate that the molecular mechanism of hepatoprotection afforded by FS pretreatment may involve the facilitation of GSH regeneration via the GRD-catalyzed and NADPH-mediated reaction.

Journal ArticleDOI
TL;DR: From the data of chemical analysis of a herb's constituents and its external appearance, one can postulate not only the quality but also the origin of the herb.
Abstract: A total of 37 commercial samples of Ginseng Radix, the origins of which belonged to Panax ginseng C. A. Meyer, P. quinquefolia Linn. (American ginseng), and P. notoginseng Burkill (sanchi-ginseng), respectively, were collected from the Taiwan herbal markets. The contents of nine ginsenosides, Rb(1), Rb(2), Rc, Rd, Re, Rf, Rg(1), Rg(2), R(0), and three malonylginsenosides, mRb(1), mRb(2), mRc, in these samples were determined by high-performance liquid chromatography. It was found that the saponin contents in P. notoginseng and P. quinquefolia were generally higher than in P. ginseng. The ginsenosides that were of the highest contents in the white-ginseng, red-ginseng, and shihchu-ginseng samples of P. ginseng were Rb(1) and Rg(1); those in the root-hair of P. ginseng were Rb(1) and Re, those in P. notoginseng were Rb(1), Rg(1) and Rd, and those in P. quinquefolia were Rb(1), Re, and mRb(1). Among the samples, those of P. quinquefolia did not contain Rf and Rg(2), whilst those of shihehu-ginseng and red-ginseng of P. ginseng contained none or only traces of the malonylginsenosides. From the data of chemical analysis of a herb's constituents and its external appearance, we can postulate not only the quality but also the origin of the herb.

Journal ArticleDOI
TL;DR: The ethanolic extract of the aerial parts of Centaurea scoparia Sieb.
Abstract: The ethanolic extract of the aerial parts of Centaurea scoparia Sieb. (Asteraceae) afforded five polyoxygenated flavones apigenin, luteolin, salvigenin, cirsimaritin, and hispidulin, the two lignans (-)-matairesinol and (-)-arctigenin together with omega-hydroxypropioguaiacone and vanillin. The structure elucidations of the isolated compounds are based on spectroscopic methods including 1D- and 2D-NMR spectra. Some proton and carbon signals are revised or newly reported.

Journal ArticleDOI
TL;DR: Findings suggest that stigmasterol and beta-sitosterol may account, at least in part, for the antinociceptive actions reported previously for the hydroalcoholic extract of Phyllanthus corcovadensis.
Abstract: The antinociceptive actions of the steroid compounds isolated from the leaves, stems, and roots of P. corcovadensis have been investigated in mice. Stigmasterol, stigmasterol acetate, beta-sitosterol, and aspirin (3-100 mk/kg, i.p.) inhibited, in a dose-related manner, acetic acid-induced abdominal constriction in mice with ID50s of 16, 11, 9, and 24 mg/kg, respectively. In the formalin test, stigmasterol and stigmasterol acetate (10-100 mg/kg, i.p.) caused graded inhibition of both the neurogenic (first phase) and inflammatory phases (second phase) of formalin-induced pain. However, both compounds were more effective in relation of the second phase of the formalin test with ID50 values of 26 and 41 mg/kg, respectively. Furthermore, both steroids failed to affect the edematogenic response of the formalin test. Given orally, stigmasterol and stigmasterol acetate (50-200 mg/kg) also exhibited significant though less potent analgesic action against both acetic acid- and formalin-induced nociception in mice. In addition, stigmasterol (up to 100 mg/kg, i.p.), in contrast to morphine (10 mg/kg, s.c.), had no analgesic effect in either tail-flick or hot-plate models. These findings suggest that stigmasterol and beta-sitosterol may account, at least in part, for the antinociceptive actions reported previously for the hydroalcoholic extract of Phyllanthus corcovadensis.

Journal ArticleDOI
TL;DR: In this paper, three structurally related acid amides, N-trans-feruloyltyramine (1), N-p-coumaroy ltyramines (2), and N-Trans-caffeoylytramine(3), were isolated from the stem parts of Annona montana (Annonaceae).
Abstract: Three structurally related acid amides, N-trans-feruloyltyramine (1), N-p-coumaroyltyramine (2), and N-trans-caffeoyltyramine (3), one lignan, (-)-syringaresinol (4), one aromatic aldehyde, syringaldehyde (5), and two steroids, beta-sitosterol and beta-sitosterol-beta-D-glucoside were isolated from the stem parts of Annona montana (Annonaceae). N-trans-Caffeoyltyramine (3) is a new natural compound. These compounds and their acetate derivatives were subjected to the antiplatelet aggregation and cytotoxicity bioassay where some of them showed significant activities.

Journal ArticleDOI
TL;DR: The methanolic extract from the root of Scutellaria baicalensis Georgi and its flavonoids, wogonin, baicalein, and baicalin expressed a preferential effect on the synthesis of collagen and total protein in fibroblasts, in contrast to growth factors which increased only the synthesisation of total protein.
Abstract: The methanolic extract from the root of Scutellaria baicalensis Georgi and its flavonoids, wogonin, baicalein, and baicalin were evaluated for anti-inflammatory action and the activatory effect on gingival fibroblasts. In LPS-induced production of IL-1 beta, three flavonoids at 1 microgram/ml expressed a significant (> 50%) inhibitory effect, similar to that of prednisolone. Moreover, the flavonoids inhibited IL-1 beta-induced synthesis of PGE2 and LTB4 considerably, although the effect of wogonin on LTB4 synthesis was marginal. In addition, three flavonoids exerted a moderate inhibition (33-36%) of collagenolytic activity, comparable to 40% inhibition by tetracycline. Meanwhile, the cellular activity of fibroblasts was augmented remarkably (40%) by baicalein (2) and slightly by baicalin (3) or wogonin (1). Consistent with the cellular activation, flavonoids enhanced the synthesis of both collagen and total protein in fibroblasts, in contrast to growth factors which increased only the synthesis of total protein. Although the effects of the methanolic extract resembled those of the flavonoids, the extract expressed a preferential effect on the synthesis of collagen and total protein.

Journal ArticleDOI
TL;DR: Compounds 1 and 4, the major phenylethanoid in the herb of P. asiatica L., showed inhibitory effects on arachidonic acid-induced mouse ear edema.
Abstract: The five phenylethanoids, acteoside (1), cistanoside F (2), lavandulifolioside (3), plantamajoside (4) and isoacteoside (5) were isolated from the herb of Plantago lanceolata L. (Plantaginaceae). Compounds 1, the major phenylethanoid in the herb of P. lanceolata L., and 4, the major phenylethanoid in the herb of P. asiatica L., showed inhibitory effects on arachidonic acid-induced mouse ear edema.

Journal ArticleDOI
TL;DR: FA and IFA are novel and potent inhibitors of murine IL-8 production and might act as one of the main components of anti-inflammatory rhizoma of Cimicifuga species.
Abstract: We investigated the effect of ferulic acid (FA) and isoferulic acid (IFA), which are active components of the rhizoma of Cimicifuga species used frequently as anti-inflammatory drugs in Japanese Oriental medicines, on murine interleukin-8 (IL-8) production in response to influenza virus infections in vitro and in vivo by antibody-sandwich enzyme-linked immunosorbent assay. In the in vitro study, the murine macrophage cell line RAW 264.7 was infected with influenza virus at a dose of 10 plaque forming units (PFU)/cell and cultured in the presence or absence of drugs. Both FA and IFA reduced the IL-8 levels in the 20-h conditioned medium in comparison with control in a dose-dependent manner. The effect of IFA was greater than that of FA: IL-8 levels were reduced to 43% and 56% of the control in the presence of 100 micrograms/ml of IFA and FA, respectively. In the in vivo study, mice were infected with 1,000 PFU of virus and received daily oral administrations of Cimicifuga heracleifolia extract (5 mg/mouse/day), FA (0.5 mg/mouse/day), IFA (0.125 mg/mouse/day), or phosphate buffered saline. The three drugs showed a tendency to reduce IL-8 levels in bronchoalveolar lavage (BAL) obtained 2 days after infection. Moreover, both FA and IFA also significantly reduced the number of exuded neutrophils into BAL. However, the drug administrations did not affect the virus yields in BAL. These data suggest that FA and IFA are novel and potent inhibitors of murine IL-8 production and might act as one of the main components of anti-inflammatory rhizoma of Cimicifuga species.