Showing papers in "Planta Medica in 1991"
TL;DR: It appears that when given orally, curcumin is far less active than after i.p. administration, and systemic effects seem to be questionable after oral application except that they occur at very low concentrations ofCurcumin, which does not exclude a local action in the gastrointestinal tract.
Abstract: The data reviewed indicate that extracts of Curcuma longa exhibit anti-inflammatory activity after parenteral application in standard animal models used for testing anti-inflammatory activity It turned out that curcumin and the volatile oil are at least in part responsible for this action It appears that when given orally, curcumin is far less active than after ip administration This may be due to poor absorption, as discussed Data on histamine-induced ulcers are controversial, and studies on the secretory activity (HCl, pepsinogen) are still lacking In vitro, curcumin exhibited antispasmodic activity Since there was a protective effect of extracts of Curcuma longa on the liver and a stimulation of bile secretion in animals, Curcuma longa has been advocated for use in liver disorders Evidence for an effect on liver disease in humans is not yet available From the facts that after oral application only traces of curcumin were found in the blood and that, on the other hand, most of the curcumin is excreted via the faeces it may be concluded that curcumin is absorbed poorly by the gastrointestinal tract and/or underlies presystemic transformation Systemic effects therefore seem to be questionable after oral application except that they occur at very low concentrations of curcumin This does not exclude a local action in the gastrointestinal tract
1,714 citations
TL;DR: A comparison of several brands of each type of garlic product revealed a large range in content, indicating the importance of analysis before garlic products are used for clinical investigations or commercial distribution.
Abstract: The content of dialk(en)yl thiosulfinates, including allicin, and their degradation products has been determined by high performance liquid chromatography (HPLC), using the respective determined extinction coefficients, for a number of commercially available garlic products. Quantitation has been achieved for the thiosulfinates; diallyl, methyl allyl, and diethyl mono-, di-, tri-, tetra-, penta-, and hexasulfides; the vinyldithiins; and (E)- and (Z)-ajoene. The thiosulfinates were found to be released only from garlic cloves and garlic powder products. The vinyldithiins and ajoenes were found only in products containing garlic macerated in vegetable oil. The diallyl, methyl allyl, and dimethyl sulfide series were the exclusive constituents found in products containing the oil of steam-distilled garlic. Typical steam-distilled garlic oil products contained about the same amount of total sulfur compounds as total thiosulfinates released from freshly homogenized garlic cloves; however, oil-macerated products contained only 20% of that amount, while garlic powder products varied from 0 to 100%. Products containing garlic powder suspended in a a gel or garlic aged in aqueous alcohol did not contain detectable amounts of these non-ionic sulfur compounds. A comparison of several brands of each type of garlic product revealed a large range in content (4-fold for oil-macerates and 33-fold for steam-distilled garlic oils), indicating the importance of analysis before garlic products are used for clinical investigations or commercial distribution.
243 citations
Metz1
TL;DR: It is concluded that this plant extract exerts central analgesic properties and remained inactive on chronic processes such as Freund's adjuvant-induced rheumatoid arthritis, if inefficacy was observed on rat backpaws edema and on loss of weight, the aqueous extract reduced the inflammatory hyperalgia.
Abstract: Lyophilised aqueous extract of Euphorbia hirta L. (Euphorbiaceae) has been evaluated for analgesic, antipyretic and anti-inflammatory properties in mice and rats, in order to complete its activity profile, after the confirmation of the existence of a central depressant activity particularly expressed by a strong sedative effect, associated with anxiolytic effects. This study leads us to the conclusion that this plant extract exerts central analgesic properties. Such a dose-dependent action was obtained against chemical (writhing test) and thermic (hot plate test) stimuli, respectively, from the doses of 20 and 25 mg/kg and it was inhibited by a naloxone pretreatment, a specific morphinic antagonist compound. An antipyretic activity was obtained at the sedative doses of 100 and 400 mg/kg, on the yeast-induced hyperthermia. Finally, significant and dose-dependent anti-inflammatory effects were observed on an acute inflammatory process (carrageenan-induced edema test in rats) from the dose of 100 mg/kg. On the other hand, plant extract remained inactive on chronic processes such as Freund's adjuvant-induced rheumatoid arthritis, after a chronic treatment during fourteen days at the daily dose of 200 or 400 mg/kg; however, if inefficacy was observed on rat backpaws edema and on loss of weight, the aqueous extract reduced the inflammatory hyperalgia.
191 citations
TL;DR: It is concluded that the activity of the 5- LOx itself represents the side of inhibition by the gum resin extract, and an inhibition of 5-LOx catalysed mediator synthesis might be involved in the previously reported anti-inflammatory activity in vivo.
Abstract: Suspensions of rat peritoneal polymorphonuclear leukocytes (PMNL) elicited with glycogen were stimulated by calcium and ionophore to produce leukotrienes and 5-HETE from endogenous arachidonic acid (AA). We investigated the effect of ethanolic extracts of the gum resin exudate of Boswellia serrata. A concentration-dependent inhibition of LTB4 and 5-HETE production by different charges of exudate extracts were found. All products of the 5-lipoxygenase (5-LOx) from endogenous arachidonic acid (AA) in PMNL were reduced to the same extent by the extracts tested. The ethanolic extract of the gum resin also decreased 5-LOx mediated metabolisation of exogenously added AA to LTB4 and 5-HETE. Since steroidal-type anti-inflammatory drugs do not exert an immediate effect in the test system used, we conclude that the activity of the 5-LOx itself represents the side of inhibition by the gum resin extract. Therefore, an inhibition of 5-LOx catalysed mediator synthesis might be involved in the previously reported anti-inflammatory activity in vivo.
190 citations
TL;DR: It is concluded that the LH suppressive effect of C.r. extracts observed in menopausal women and ovx rats is caused by at least three different synergistically acting compounds.
Abstract: Remifemin is an ethanolic extract of the rhizome of Cimicifuga racemosa (C.r.) and is used to relieve climacteric hot flushes. In the present study the effects of this preparation on LH and FSH secretion of menopausal women were investigated. After an 8 weeks treatment, LH but not FSH levels were significantly reduced in patients receiving the Cimicifuga extract. To further characterize the endocrinologically active principles of this plant extract, a lipophilic extract of C.r. was prepared and subjected to Sephadex chromatography. Fractions obtained were tested for their ability to reduce LH secretion in ovariectomized (ovx) rats and to compete in vitro with 17 beta-estradiol for estrogen receptor binding sites. Three types of endocrinologically active compounds were obtained: (1) Constituents which were not ligands for the estrogen receptor but suppress LH release after chronic treatment, (2) constituents binding to the estrogen receptor and also suppressing LH release, and (3) compounds which are ligands for the estrogen receptor but without an effect of LH release. It is concluded that the LH suppressive effect of C.r. extracts observed in menopausal women and ovx rats is caused by at least three different synergistically acting compounds.
175 citations
TL;DR: Five previously unreported thiosulfinates have been found, four of which contain the TRANS-1-propenyl group and increase several-fold to over half the content of allicin upon storage of garlic bulbs at 4 degrees C with a concomitant decrease in a gamma-glutamyl peptide.
Abstract: Reversed-phase high Performance liquid chromatography (C18-HPLC) was used to separate and quantitate all the detectable alkyl and alkenyl thiosulfinates, including configurational isomers, of garlic homogenates. Pure thiosulfinates were synthesized or isolated and identified by (1)H-NMR, and their extinction coefficients determined. Some configurational isomers required Separation by silica-HPLC. Five previously unreported thiosulfinates have been found, four of which contain the TRANS-1-propenyl group and increase several-fold to over half the content of allicin upon storage of garlic bulbs at 4 degrees C with a concomitant decrease in a gamma-glutamyl peptide. The variation in thiosulfinate yield between different countries, stores, bulbs, cloves, and storage times was investigated. A method for standardizing the quantitation of allicin yield from garlic is proposed and compared to other methods of allicin analysis.
170 citations
TL;DR: It is suggested that this methanolic extract contains one or more hypoglycemic principles including the main flavanone glycoside, prunin, which can significantly reduce the levels of blood glucose and total lipids in streptozotocin-diabetic rats.
Abstract: Blood glucose and total lipid levels in rats with streptozotocin-induced diabetes were determined after intraperitoneal administration of a methanolic extract of Prunus davidiana Fr. stems and its main component, prunin (= naringenin 7-O-beta-D-glucoside). From the data obtained it was concluded that intraperitoneal administration of the methanolic extract and prunin produced a significant hypoglycemic effect. Total blood lipids were also decreased by these substances. Thus, it is suggested that this methanolic extract contains one or more hypoglycemic principles including the main flavanone glycoside, prunin, which can significantly reduce the levels of blood glucose and total lipids in streptozotocin-diabetic rats.
165 citations
TL;DR: The results indicate that the relaxant activity of the lyophilized decoction is independent of the integrity of the vascular endothelium and it seems likely that at least one other principle is to be found in the olive leaf which is either a vasodilator itself or else potentiates the Relaxant effect of oleuropeoside.
Abstract: We studied the importance of the smooth vascular muscle endothelium in the vasodilator action of the decoction of olive (Olea europaea) leaf. The decoction caused relaxation of isolated rat aorta preparations both in the presence (IC50 1.12 +/- 0.33 mg/ml) and in the absence (IC50 1.67 +/- 0.16 mg/ml) of endothelium. The results indicate that the relaxant activity of the lyophilized decoction is independent of the integrity of the vascular endothelium. We also showed that oleuropeoside is a component responsible for vasodilator activity but, from the results, it seems likely that at least one other principle is to be found in the olive leaf which is either a vasodilator itself or else potentiates the relaxant effect of oleuropeoside.
151 citations
TL;DR: Protozoa are responsible for a number of serious tropical diseases including amoebiasis, leishmaniasis, malaria, and trypanosomiasis and the potential of plants to produce new clinical agents is discussed.
Abstract: Protozoa are responsible for a number of serious tropical diseases including amoebiasis, leishmaniasis, malaria, and trypanosomiasis. New drugs are required for the treatment of these diseases and the potential of plants to produce new clinical agents is discussed.
145 citations
TL;DR: The present study indicates that glycyrrhizin is not an ROS scavenger but exerts an anti-inflammatory action by inhibiting the generation of ROS by neutrophils, the most potent inflammatory mediator at the site of inflammation.
Abstract: The effect of glycyrrhizin on inflammatory mediators such as neutrophil functions including reactive oxygen species (ROS) generation was examined. Glycyrrhizin significantly decreased neutrophil-generated O2-, H2O2 and OH in a dose-dependent manner. However, the drug did not reduce any of the ROS generated in a cell-free, xanthine-xanthine oxidase system. The drug did not affect neutrophil chemotaxis or phagocytosis, either. The present study indicates that glycyrrhizin is not an ROS scavenger but exerts an anti-inflammatory action by inhibiting the generation of ROS by neutrophils, the most potent inflammatory mediator at the site of inflammation.
133 citations
TL;DR: The caffeic acid derivatives including the major compounds rosmarinic acid and 2,3-dicaffeoyltartaric acid predominated over the flavones in an aqueous MeOH extract that was comparable to a herbal tea.
Abstract: ORTHOSIPHON ARISTATUS (Orthosiphonis folium DAB 9) was studied with regard to its phenolic constituents. Twenty compounds were isolated and identified on the basis of their spectral characteristics. The compounds included nine lipophilic flavones, two flavonol glycosides, and nine caffeic acid derivatives. The presence of the recently reported methylripariochromene A could not be confirmed. All compounds identified were quantified by HPLC. The caffeic acid derivatives including the major compounds rosmarinic acid and 2,3-dicaffeoyltartaric acid (67% of total identified phenolics) predominated over the flavones (33%) in an aqueous MeOH extract. The predominance of the caffeic acid derivatives was even more pronounced in a hot water extract (94.5% of total identified phenolics) that was comparable to a herbal tea.
TL;DR: Caffeic acid and ferulic acid inhibited lipid peroxidation induced by superoxide anion and these effects were comparable to those of superoxide dismutase or DL-alpha-tocopherol.
Abstract: The effects of phenolcarboxylic acids, caffeic acid, p-coumaric acid, and ferulic acid on the generation of superoxide anion and the production of lipid peroxide induced by superoxide anion were studied. Only ferulic acid anion among the phenolcarboxylic acids scavenged superoxide. Caffeic acid and ferulic acid inhibited lipid peroxidation induced by superoxide anion. These effects were comparable to those of superoxide dismutase or DL-alpha-tocopherol.
Metz1
TL;DR: This study on the aqueous extract of E. californica shows that this plant reduced the behavioural parameters measured in a familiar environment test in mice at doses above 100 mg/kg and in non-familiar environment tests (staircase test) at dosesAbove 200mg/kg, validates its traditional sedative properties.
Abstract: Eschsholzia californica Cham. is a traditional medicinal plant of the Indians used by the rural population of California for its analgesic and sedative properties. Our study on the aqueous extract shows that this plant reduced the behavioural parameters measured in a familiar environment test in mice (novelty preference, locomotion and rearings in two compartments test) at doses above 100 mg/kg and in non-familiar environment tests (staircase test) at doses above 200 mg/kg. This finding validates its traditional sedative properties confirmed by the sleeping induction at doses above 100 mg/kg. Furthermore, when administered at a dose a of 25 mg/kg, E. californica appeared to also have an anxiolytic action since it produced an increase of the number of steps climbed by mice in the staircase test (anticonflict effect) and that of the time spent by animals in the lit box when they were confronted with the light/dark choice situation. Before evaluation of the behavioural effects, it was verified that our aqueous extract did not induce any toxic effect when administered i.p. and p.o.
TL;DR: Whether tetrahydropapaveroline serves as a precursor of morphinanes in mammals, as has been found in opium poppies, remains to be elucidated.
Abstract: beta-Carbolines occur in man and rat. The concentration in various tissues is about 100 to 1000 times lower than that of classical neurotransmitters. Administration of beta-carbolines in animals induces overlapping but not identical activity profiles. The molecular modes of action differ. For example, harman (1-methyl-beta-carboline) acts as an endogenous inhibitor of monoamine oxidase [E.C. 1.4.3.4.], subtype A, whereas norharman (beta-carboline) probably acts by stimulation of a specific beta-carboline receptor which is different from the benzodiazepine-GABA receptor complex. There is substantial evidence that tetrahydroisoquinolines occur under physiological conditions as well. Whether tetrahydropapaveroline serves as a precursor of morphinanes in mammals, as has been found in opium poppies, remains to be elucidated.
TL;DR: Twenty unsaturated sesquiterpene dialdehydes were tested for antimicrobial, algaecidal, cytotoxic, and mutagenic activity; the most active compounds were: isovelleral (7), isoisoveLLeral (8), velleral(20), and methylmarasmate (6).
Abstract: Twenty unsaturated sesquiterpene dialdehydes were tested for antimicrobial, algaecidal, cytotoxic, and mutagenic activity. In addition to the known antifungal activity, polygodial (1) also exhibited antibacterial and cytotoxic activity; epipolygodial (2) was slightly less active. The most active compounds were: isovelleral (7), isoisovelleral (8), velleral (20), and methylmarasmate (6). With the exception of velleral (20), they also exhibited mutagenic activity in the Salmonella/microsome assay. Derivatization to less polar compounds usually increased the antimicrobial and cytotoxic effects and reduced mutagenicity, while the introduction of hydroxyl groups had the reverse effect.
TL;DR: Chalcones 6 and 7 were proved to have anti-tumor-promoting activity in mouse skin carcinogenesis induced by 7,12-dimethylbenz[a]anthracene (DMBA) plus TPA, and both chal Cones may reveal anti-Tumor Promoting activity via the modulation of calmodulin involved systems.
Abstract: Potent anti-tumor promoter activity has been found in the nonpolar extracts of the root of "Ashita-Ba", Angelica keiskei Koidz. (Umbelliferae), which is eaten as a vegetable in Japan. From this active fraction, two angular furanocoumarins, archangelicin (1) and 8(S),9(R)-9-angeloyloxy-8,9-dihydrooroselol (2), three linear furanocoumarins, psoralen (3), bergapten (4) and xanthotoxin (5), and three chalcones, 4-hydroxyderricin (6), xanthoangelol (7) and a novel chalcone named ashitaba-chalcone (8), were isolated. Among these compounds, two angular type furanocoumarins, 1 and 2, and three chalcones, 6-8, suppressed 12-O-tetradecanoylphorbol-13-acetate (TPA)-stimulated 32Pi-incorporation into phospholipids of cultured cells, whereas coumarins 3-5 were less effective. In addition, chalcones 6 and 7 were proved to have anti-tumor-promoting activity in mouse skin carcinogenesis induced by 7,12-dimethylbenz[a]anthracene (DMBA) plus TPA. Since chalcones 6 and 7 showed calmodulin-interacting property, both chalcones may reveal anti-tumor-promoting activity via the modulation of calmodulin involved systems. These chalcones may be useful to develop the effective method for cancer prevention.
Metz1
TL;DR: The plant extract induced the sleep in mice after treatment with an infrahypnotic dose of pentobarbital and potentialised the sleep induced by a hypnotic dose in mice.
Abstract: A lyophilised hydroalcoholic extract of Melissa officinalis L. (Lamiaceae) has been evaluated for behavioral effects in mice. According to the traditional use of M. officinalis, sedative properties have been confirmed for low doses by the decrease of behavioral parameters measured in a non-familiar environment test (staircase test) and in a familiar environment test (two compartment test). With high doses, a peripheral analgesic activity was obtained by reducing the acetic acid-induced pain (writhing test); moreover, the plant extract induced the sleep in mice after treatment with an infrahypnotic dose of pentobarbital and potentialised the sleep induced by a hypnotic dose of pentobarbital.
TL;DR: A xanthone was isolated from the hexane fraction of the Swertia chirayita plant and identified as 1,8-dihydroxy-3,5-dimethoxyxanthone (swerchirin) which has a very significant blood sugar lowering effect in fasted, fed, glucose loaded, and tolbutamide pretreated albino rat models.
Abstract: A xanthone was isolated from the hexane fraction of the Swertia chirayita plant and identified as 1,8-dihydroxy-3,5-dimethoxyxanthone (swerchirin). It has a very significant blood sugar lowering effect in fasted, fed, glucose loaded, and tolbutamide pretreated albino rat models. The ED50 for 40% blood sugar lowering in CF male albino rats (body weight 140-165 g) is 23.1 mg/kg/oral. The possibility of its application in clinical therapy for diabetes mellitus needs exploration.
TL;DR: Genotoxic properties of essential oils from Anthemis nobilis, Artemisia dracunculus, and Salvia officinalis were studied with Bacillus subtilis rec-assay and Salmonella/microsome reversion assay and DNA-damaging activity was demonstrated to be due to the estragol component of the oil.
Abstract: Genotoxic properties of essential oils from Anthemis nobilis L., Artemisia dracunculus L., Salvia officinalis L., Salvia sclarea L., Satureja hortensis L., Satureja montana L., Thymus capitatus L., Thymus citriodorus Schreb., Thymus vulgaris L., Citrus bergamia Risso, were studied with Bacillus subtilis rec-assay and Salmonella/microsome reversion assay. The essential oil of Artemisia dracunculus L. "Piemontese" turned out to be active in the rec-assay but not in the Salmonella test. DNA-damaging activity was demonstrated to be due to the estragol component of the oil. Advantages of the combined use of these two short-term microbial assays in genotoxic studies are discussed.
TL;DR: The effects of the constituent sesquiterpene glycosides 1-3 and polyhydroxylated triterpenoids 5-6 isolated by MeOH extraction of Eriobotrya japonica were studied in genetically diabetic mice and normoglycemic rats.
Abstract: The effects of the constituent sesquiterpene glycosides 1-3 and polyhydroxylated triterpenoids 5-6 isolated by MeOH extraction of Eriobotrya japonica were studied in genetically diabetic mice (C57BL/KS-db/db/Ola) and normoglycemic rats. The sesquiterpene glycoside 3 and the polyhydroxylated triterpenoids 5 and 6 produced a marked inhibition of glycosuria. Furthermore, 5 and 6 were able to reduce blood glucose levels in normoglycemic rats. While there are already some data reported on hypoglycemic activity of polyhydroxylated triterpenoids, there are no previous data showing hypoglycemic activity of sesquiterpene glycosides.
TL;DR: Licochalcone A, from the root of Glycyrrhiza inflata Beta (Leguminosae) (Xin-jiang liquorice) showed anti-inflammatory action towards mouse ear edema induced by arachidonic acid (AA) and 12-O-tetradecanoylphorbol 13-acetate (TPA) by topical application.
Abstract: Licochalcone A, 3-a,a-dimethylallyl-4,4'-dihydroxy-6-methoxychalcone, from the root of Glycyrrhiza inflata Beta (Leguminosae) (Xin-jiang liquorice) showed anti-inflammatory action towards mouse ear edema induced by arachidonic acid (AA) and 12-O-tetradecanoylphorbol 13-acetate (TPA) by topical application. Anti-tumour promoting action of licochalcone A was also observed in vivo for mouse skin papilloma initiated by dimethylbenz[a]anthracene (DMBA) and promoted by TPA. It inhibited in vitro 32Pi-incorporation to phospholipids in HeLa cells promoted by TPA. A competitive interaction of licochalcone A with the TPA-receptors in the cell membrane has been suggested.
TL;DR: Picroliv, the hepatoprotective principle of the plant Picrorhiza kurroa, showed a dose-dependent choleretic effect in conscious rats and anaesthetised guinea pigs and possessed a marked anticholestatic effect against paracetamol- and ethynylestradiol-induced cholestasis.
Abstract: Picroliv, the hepatoprotective principle of the plant Picrorhiza kurroa, showed a dose-dependent (1.5-12 mg/kg x 7) choleretic effect in conscious rats and anaesthetised guinea pigs. It also possessed a marked anticholestatic effect against paracetamol- and ethynylestradiol-induced cholestasis. It antagonised the changes in bile volume as well as the contents (bile salts and bile acids). Silymarin, a known hepatoprotective agent, was tested simultaneously for comparison. Picroliv was found to be a more potent choleretic and anticholestatic agent than silymarin.
TL;DR: It is suggested that the quassinoid mode of antimalarial action is not a simple cytotoxic effect and lends support to further investigation of the structure activity relationships within this group of compounds.
Abstract: A microdilution technique was developed for the assessment of in vitro cytotoxicity against KB cells derived from a human epidermoid carcinoma of the nasopharynx. The test was used to determine the cytotoxicity of a series of quassinoids, isolated from Brucea javanica, and which have previously been shown to demonstrate activity against Plasmodium falciparum. The 50% effective dose (ED50) for 7 quassinoids tested against KB ranged from 0.008 microgram/ml for bruceantin, the most cytotoxic of the compounds tested to greater than 5 micrograms/ml for bruceolide, the least toxic tested. The activities of the quassinoids against KB did not parallel the known activities of the quassinoids against Plasmodium falciparum suggesting that the quassinoid mode of antimalarial action is not a simple cytotoxic effect and lends support to further investigation of the structure activity relationships within this group of compounds.
TL;DR: Monodesmosides were found to be as effective on promastigote forms as the reference compound (pentamidine) and against amastigotes forms only hederagenin exhibited a significant activity which was equivalent to that of thereference compound (N-methylglucamine antimonate).
Abstract: Antileishmanial activity is reported for the first time for saponins of ivy, Hedera helix L., in vitro on promastigote and amastigote forms of Leishmania infantum and Leishmania tropica. The compounds tested were an extract containing 60% of saponic complex (CS 60), the bidesmosides hederasaponin B, C, and D (saponin K10), their corresponding monodesmosides alpha-, beta-, and delta-hederin, and hederagenin. CS 60 and bidesmosides have shown no effect. Monodesmosides were found to be as effective on promastigote forms as the reference compound (pentamidine). Against amastigote forms only hederagenin exhibited a significant activity which was equivalent to that of the reference compound (N-methylglucamine antimonate).
Metz1
TL;DR: Dried hydro-alcoholic extract of Peumus boldus has been evaluated for hepatoprotective, choleretic and anti-inflammatory effects in mice and rats, in order to validate or to invalidate traditional therapeutic indications.
Abstract: Dried hydro-alcoholic extract of Peumus boldus (Monimiaceae) has been evaluated for hepatoprotective, choleretic and anti-inflammatory effects in mice and rats, in order to validate or to invalidate traditional therapeutic indications. This extract exerted a significant hepatoprotection of tert-butyl hydroperoxide-induced hepatotoxicity in isolated rat hepatocytes (in vitro technique) by reducing the lipid peroxidation and the enzymatic leakage of LDH; this in vitro efficacy was reinforced by a significant hepatoprotection on CCl4-induced hepatotoxicity in mice (in vivo technique), the plant extract reducing the enzymatic leakage of ALAT. Boldine, the main alkaloid of P. boldus appears to be implicated in this hepatoprotective activity. Choleretic effects, often mentioned in traditional indications, have not been confirmed in rats. Finally, significant and dose-dependent anti-inflammatory effects were obtained on an acute inflammatory process (carrageenan-induced edema test in rats). Boldine does not appear to be involved in such properties.
TL;DR: A water-soluble crude polysaccharide fraction prepared from the root of Bupleurum falcatum L. (Japanese name = Saiko) prevented HCl/ethanol induced ulcerogenesis in mice significantly and lost most of its activity after treatment with periodate or digestion with endo-polygalacturonase indicating that the polygalactic region and/or the molecular mass may contribute to activity.
Abstract: A water-soluble crude polysaccharide fraction (BR-1) prepared from the root of Bupleurum falcatum L (Japanese name = Saiko) prevented HCl/ethanol induced ulcerogenesis in mice significantly BR-1 was fractionated into four polysaccharide fractions (BR-2, BR-3, BR-4, and BR-5) by the addition of cetyltrimethylammonium bromide, and the strongly acidic polysaccharide fraction BR-2 showed the most potent inhibition of gastric lesion formation When BR-2 was further fractionated by anion-exchange chromatography, the most potent anti-ulcer activity was observed in the pectin-like polysaccharide, bupleuran 2IIc Bupleuran 2IIc was homogeneous as determined by electrophoresis and gel filtration Bupleuran 2IIc was composed mainly of galacturonic acid with small proportions of arabinose, rhamnose, and galactose, and its average relative molecular mass was estimated to be 63,000 d BR-2 lost most of its activity after treatment with periodate or digestion with endo-polygalacturonase indicating that the polygalacturonan region and/or the molecular mass may contribute to activity
TL;DR: This new phloroglucinol derivative 1 was fungicidal against Cladosporium cucumerinum in a TLC bioassay and found to exert an interesting antimalarial activity in an in vitro test system.
Abstract: The new phloroglucinol derivative 1 has been isolated from the light petroleum ether extract of the aerial parts of Hypericum calycinum. Its structure has been established by means of 1 H- and 13 C-NMR spectroscopy and by nOe, MHQC, and HMBC experiments on its monomethyl ether derivative 3. Compound 1 was fungicidal against Cladosporium cucumerinum in a TLC bioassay. In addition, this new phloroglucinol derivative was also found to exert an interesting antimalarial activity in an in vitro test system
TL;DR: T-cadinol was shown to have a concentration-dependent smooth muscle relaxing effect on the isolated guinea pig ileum and a dose-dependent inhibitory effect on cholera toxin-induced intestinal hypersecretion in mice.
Abstract: Fractionation of an ethyl acetate extract of scented myrrh (resin of Commiphora guidottii Chiov., Burseraceae), using the guinea pig ileum test to monitor pharmacological activity, resulted in isolation of the sesquiterpene (+)-T-cadinol. High field NMR spectroscopy yielded new detailed 1 H- and 13 C-NMR data for the compound. T-cadinol was shown to have a concentration-dependent smooth muscle relaxing effect on the isolated guinea pig ileum and a dose-dependent inhibitory effect on cholera toxin-induced intestinal hypersecretion in mice