Showing papers in "Natural product sciences in 2011"

Sesquiterpene Derivatives Isolated from Cyperus rotundus L. Inhibit Inflammatory Signaling Mediated by NF-${\kappa}B$

Abstract: The immune system is finely balanced by the activities of pro-inflammatory and anti-inflammatory mediators or cytokines. Unregulated activities of these mediators can lead to the development of various inflammatory diseases. A variety of safe and effective anti-inflammatory agents are available with many more drugs under development. Of the natural compounds, the sesquiterpenes (nootkatone, α-cyperone, valencene and β-selinene) isolated from C. rotundus L. have received much attention because of their potential antiinflammatory effects. However, limited studies have been reported regarding the influence of sesquiterpene structure on anti-inflammatory activity. In the present study, the anti-inflammatory potential of four structurally divergent sesquiterpenes was evaluated in lipopolysaccaride (LPS)-stimulated RAW 264.7 cells, murine macrophages. Among the four sesquiterpenes, α-cyperone and nootkatone, showed stronger anti-inflammatory and a potent NF-κB inhibitory effect on LPS-stimulated RAW 264.7 cells. Molecular analysis revealed that various inflammatory enzymes (iNOS and COX-2) were reduced significantly and this correlated with downregulation of the NF-κB signaling pathway. Additionally, electrophoretic mobility shift assays (EMSA) elucidated that nootkatone and α-cyperone dramatically suppressed LPS-induced NF-κB-DNA binding activity using 32Plabeled NF-κB probe. Hence, our data suggest that α-cyperone and nootkatone are potential therapeutic agents for inflammatory diseases.

Pharmacognostical Evaluation and Phytochemical Standardization of Abrus precatorius L. Seeds

Abstract: The seeds of Abrus precatorius L. (Family- Fabaceae) constitute the drugs Abrus, Gunja, or Ratti in commerce. In the Indian System of Medicine, the seeds are used for sciatica, paralysis, headache, dysentery, diarrhoea, leprosy, ulcer, nervous disorders, alopecia, as well as anti-inflammatory, antidiabetic, antibacterial, antitumor, sexual stimulant and abortifacient. Seeds are poisonous and therefore are used after mitigation. The protein abrin is responsible for the highly toxic properties of seeds. Quantitative HPTLC analysis of the methanolic extract of seeds determined the presence of 0.4018% gallic acid and 0.4009% glycyrrhizin. The present study was undertaken to develop an HPTLC method, as well as ascertain the physico-chemical, morphological and histological parameters to establish the authenticity of A. precatorius seeds.

Anti-oxidative and Antibacterial Constituents from Sedum hybridum

Abstract: Phytochemical studies on the whole extract of Sedum hybridum L., a Mongolian medicinal plant, has been undertaken to isolate active principles responsible for its anti-oxidative and antibacterial activities. Eighteen known compounds, i.e. (1) quercetin, (2) kaempferol, (3) herbacetin-8-O--D-xylopyranoside, (4) myricetin, (5) gossypetin-8-O--D-xylopyranoside, (6) gallic acid, (7) 2,4,6-tri-O-galloyl-D-glucopyranose, (8) 6-O-galloylarbutin, (9) myricetin-3-O--L-arabinofuranoside, (10) quercetin-3-O--L-arabinofuranoside, (11) caffeic acid, (12) ethylgallate, (13) (-) epigallocatechin-3-O-gallate, (14) palmitic acid, (15) stearic acid, (16) stearic acid ethyl ether, (17) -sitosterol and (18) -sitosteryl-O--D-glucopyranose have been isolated and their molecular structures identified by spectroscopic analysis. Thirteen substances including seven flavonol components (1, 2, 3, 4, 5, 9 and 10), five gallic acid derivatives (6, 7, 8, 12 and 13) and caffeic acid (11) exhibited significant, dose-dependent, DPPH radical scavenging activity. Galloyl esters 12 and 13 were revealed to be main active principles for the antibacterial property of the extract of Sedum hybridum L.

Anti-adipogenic Activity of Acer tegmentosum and its Constituent, Catechin in 3T3-L1 Cells

Abstract: In the course of screening anti-adipogenic activity of natural products employing the preadipocyte cell line, 3T3-L1 as an in vitro assay system, the EtOAc fraction of the stem barks of Acer tegmentosum Maxim (Aceraceae) showed significant inhibitory activity on adipocyte differentiation as assessed by measuring fat accumulation using Oil Red O staining. Activity-guided fractionation led to the isolation of active constituent, (+)-catechin. (+)-Catechin showed inhibitory activity on adipocyte differentiation in dose-dependent manner. Further studies with interval treatment demonstrated that (+)-catechin exerted inhibitory activity on adipocyte differentiation via acting on early stage of adipogenesis. Our present study also showed that (+)-catechin significantly inhibited the preadipocyte proliferation. Taken together, these results suggest that (+)-catechin, a constituent of A. tegmentosum might contribute the anti-adipogenic activity of A. tegmentosum.

A New Antioxidant from the Marine Sponge-derived Fungus Aspergillus versicolor

Abstract: A chemical investigation of the marine-derived fungi Aspergillus versicolor led to the isolation of a new aromatic polyketide (1), The structure was elucidated by spectroscopic analysis, and its radical-scavenging activity, reducing power, and inhibitory activity to lipid oxidation were investigated. Those activities of compound 1 were compared with standard antioxidants such as butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), tertiarybutylhydroquinone (TBHQ), and ascorbic acid (VC). Compound 1 showed antioxidant activity comparable to that of BHA, and siginificantly higher than that of BHT.

Inhibition of Rat Lense Aldose Reductase by Flavonoids from Dandelions

Abstract: The purpose of this study was to evaluate the therapeutic potential of naturally occurring aldose reductase (AR) inhibitors isolated from Korean native plants. The MeOH extract and stepwise polarity fractions of dandelions were tested on rat lens AR inhibition in vitro. Of these, the EtOAc fractions from the leaves of dandelions (Traxacum coreanum, T. officinale, and T. ohwianum) exhibited an AR inhibitory activity (IC50 values, 2.37, 1.73 and 2.68 mg/ml, respectively). A chromatography of the EtOAc fraction from the leaves of T. coreanum led to the further isolation of two flavonoids identified as luteolin and luteolin 7-O-glucopyranoside. These compounds exhibited strong AR inhibitory activity, with IC50 values of 0.15 and 1.05 mM, respectively. These results suggested that luteolin is a potent AR inhibitor within dandelions and that it could be a useful lead compound in the development of a novel AR inhibitory agent against diabetic complications.

Chemical Constituents of Abies koreana Leaves with Inhibitory Activity against Nitric Oxide Production in BV2 Microglia Cells

Abstract: Eleven compounds were isolated from fresh leaves of Abies koreana (Pinaceae), and structures of these compounds were determined to be 3-hydroxy-2-methyl-4-pyrone (1), maltol-3-O-β-D-glucoside (2), (-)-epicatechin (3), naringenin 7-O-β-D-glucopyranoside (4), naringenin-7-O-rhamnoglucoside (5), kaempferol 3-O-β-D-glucopyranoside (6), (+)-isolariciresinol (7), secoisolariciresinol (8), rhododendrol (9), ferulic acid (10) and 4-(4-hydroxyphenyl)butan-2-one (rheosmin) (11) by comparing 1H-, 13C-NMR and MS spectroscopic data with reference values. Compounds 3, 5, 7, 8, 9, 10, 11 were isolated for the first time from A. koreana. Among eleven isolates, compounds 1, 7 and 11 showed inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV-2 microglia in a concentration dependent manner.

Articles : Analysis of the Components of Guibitang and Fermented Guibi-tang and their Ability to Inhibit Angiotensin-converting Enzyme

Abstract: Guibi-tang is a traditional medicine used for the treatment of colds. We investigated the levels of several compounds in Guibi-tang before and after fermentation with Lactobacillus and tested their ability to inhibit angiotensin-converting enzyme. Six known compounds (decursin, decursinol angelate, nodakenin, liquiritin, formononetin, and 6-gingerol) and 2 unidentified compounds were detected in Guibi-tang (GB) and fermented Guibi-tang (FGB) by an established HPLC-DAD method. The levels of the 6 known compounds were decreased after fermentation. FGB showed more potent inhibition of angiotensin-converting enzyme activity than GB. In conclusion, fermentation with Lactobacillus affects the content of several compounds in GB and improves its angiotensin-converting enzyme inhibitory activity.

Superoxide Radical Scavengers from the Whole Plant of Veronica peregrina

Abstract: In the course of screening for antioxidant compounds by measuring the radical scavenging effect on 1,1-diphenyl- 2-picrylhydrazyl (DPPH), a total extract from the whole plant of Veronica peregrina (Scrophulariaceae) was found to show potent antioxidant activity Subsequent activity-guided fractionation of the methanolic extract led to the isolation of six phenolic compounds including chrysoeriol (1), diosmetin (2), 4-hydroxybenzoic acid (3), apigenin (4), caffeic acid methylester (5) and protocatechuic acid (6) Their structures were elucidated by spectroscopic studies Compounds 1-5 were isolated for the first time from this plant Compounds 5 and 6 showed significant antioxidative effects in DPPH free radical scavenging and superoxide quenching activity assays

Isolation and Biological Activities of an Alkaloid Compound (3-methylcanthin-5, 6-dione) from Picrasma quassiodes (D. Don) Benn.

Abstract: An alkaloid, 3-methylcanthin-5, 6-dione, was isolated from the stem of Picrasma quassioides (D. Don) Benn. and characterized by comprehensive analyses of its 1D and 2D NMR spectra. It was also evaluated for its cytotoxic activity in vitro against three human cancer cell lines (MDA-MB-231, HT-29 and NCI-N87), using MTT assays. We found that 3-methylcanthin-5, 6-dione exhibited significant anti-inflammatory activity via inhibiting NO production induced in LPS-stimulated murine macrophage RAW264.7 cells. The antioxidant activity of 3-methylcanthin-5, 6-dione was measured by DPPH free radical scavenging assays, hydroxyl radical scavenging assays and reducing power assays. Our results showed that 3-methylcanthin-5, 6-dione has significant biological activities.

Antimicrobial Effects of Lonicera japonica against Gram Positive and Gram Negative Anaerobic Bacteria

Abstract: It has been shown that the butanol extract of Lonicera japonica has antimicrobial and other potentially useful biological activities. The purpose of this study was to determine the in vitro activity of Lonicera japonica compared to other antimicrobial agents against anaerobic bacteria. Specifically, the in vitro activity of the butanol extract was investigated against 104 clinical isolates of anaerobic bacteria using an agar dilution method and the results were compared to erythromycin, cefoxitin, imipenem, clindamycin, and metronidazole. It was found that Lonicera japonica and imipenem were the most active antimicrobial agents tested.

Aldose Reductase Inhibition by Luteolin Derivatives from Parasenecio pseudotaimingasa

Abstract: Effects of the extract and fractions from Parasenecio pseudotaimingasa on rat lens aldose reductase (AR) inhibition have been investigated. Among them, the n-BuOH fraction was exhibited good inhibitory potencies (IC50 value 1.42 μg/ml). Phytochemical constituents were isolated from the n-BuOH fraction by open column chromatography. Their structures were elucidated as luteolin-7-O-rutinoside (1) and luteolin-7-Oglucoside (2) on the basis of spectroscopic analysis. Compounds 1 and 2 exhibited strong AR inhibitory activity, with IC50 values of 2.37 and 1.05 μM, respectively. This is the first report on the isolation of compounds 1 and 2 from P. pseudotaimingasa. These results suggest that P. pseudotaimingasa could be a useful material in the development of a novel AR inhibitory agent against diabetic complications.

Articles : Quantitative Analysis of Compounds in Fermented Insampaedok-san and Their Neuroprotective Activity in HT22 Cells

Abstract: Insampaedok-san is a traditional medicine used for the treatment of colds. We investigated several compounds in Insampeadok-san, and tested their neuroprotective and anti-oxidative activities after fermentation with Lactobacillus. The amounts of four marker compounds (ferulic acid, hesperidin, 6-gingerol and glycyrrhizin) and unidentified compounds in Insampaedok-san (IS) and fermented Insampaedok-san (FIS) were measured and compared by an established HPLC-DAD method. Neuroprotective activity of IS and FIS extracts was evaluated and compared after glutamate-induced neurotoxicity in HT22 cells. Anti-oxidative activity of IS and FIS was also compared in DPPH free radical, hydroxyl radical and hydrogen peroxide scavenging activity assays. Contents of two compounds, ferulic acid and glycyrrhizin were decreased while 6-gingerol was increased by fermentation. FIS showed more potent neuroprotective activity than IS. DPPH, hydroxyl radical and hydrogen peroxide scavenging was slightly increased by FIS when compared to IS. In conclusion, fermentation with Lactobacillus can vary the amounts of the marker compounds in IS and improve neuroprotective and anti-oxidative activities of IS.

Validation of High-Performance Liquid Chromatography Analysis on Phenolic Substances of Cirsium setidens and Sedative Effect of Pectolinarin as the Active Principle

Abstract: This study was performed to determine the composition of phenolic substances contained in the leaves of Cirsium setidens (Compositae), validate the high-performance liquid chromatography (HPLC) method, and determine the in vivo sedative effect of the main component pectolinarin. Six phenolic compounds isolated from C. setidens were spectroscopically identified as chlorogenic acid (1), hyperoside (2), 3,4-di-O-caffeoylquinic acid (3), caffeic acid methyl ester (4), linarin (5), and pectolinarin (6) and then used as standard compounds for HPLC analysis. HPLC proved to be precise, accurate, and sensitive for the simultaneous analysis of the phenolic substances. In particular, six compounds showed good regression (R2 > 0.999) within test ranges and recovery was in the range of 95.4 - 104.8%. The content of pectolinarin was considerably higher (156.48 mg/g) than those of other phenolic substances including the other flavone glycoside, linarin (18.99 mg/g). The contents of other phenolic substances, in order, were chlorogenic acid (8.41 mg/g), 3,4-di-O-caffeoylquinic acid (5.74 mg/g), hyperoside (4.33 mg/g), and caffeic acid methyl ester (0.51 mg/g). Oral administration with compound 6 (10 and 20 mg/kg) enhanced the sleeping time induced by pentobarbital in mice, indicating that it has a sedative effect.

Anti-allergic Effects of Schizonepeta tenuifolia on Mast Cell-Mediated Allergy Model

Abstract: 【Immediate-type hypersensitivity is involved in many allergic diseases such as asthma, allergic rhinitis and anaphylaxis. The discovery of drugs for the treatment of allergic disease is an important subject in human health. Stimulation of mast cells releases inflammatory mediators, such as histamine and pro-inflammatory cytokines with immune regulatory properties. We investigated the effect of the aqueous extract of Schizonepeta tenuifolia (AEST) (Labiatae) on the immediate-type allergic reaction. AEST inhibited compound 48/80-induced systemic allergic reaction. AEST attenuated immunoglobulin E (IgE)-mediated skin allergic reaction and histamine release from human mast cell line (HMC-1) cells. In addition, AEST decreased the gene expression and secretion of pro-inflammatory cytokines in phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore A23187 (A23187)-stimulated HMC-1 cells. Our results indicate that AEST inhibits the mast cell-derived allergic reactions and involvement of histamine and pro-inflammatory cytokines in these effects.】

Tyrosinase Inhibitory Constituents of Morus bombycis Cortex

Abstract: Tyrosinase is one of the important enzymes in the mammalian melanin synthesis. In the process of melanin synthesis, tyrosine is oxidized to DOPA (3,4-dihydroxyphenylalanine), and DOPA is further oxidized to dopaquinone. Tyrosinase is an enzyme catalyzing this oxidation of tyrosine, so chemicals that inhibit the activity of tyrosinase can be used as skin whitening agents. In this study, we isolated five constituents from the 80% MeOH extract of Morus bombycis cortex by bioactivity-guided fractionation. We performed mushroom tyrosinase inhibition assay. As a result, 7,2`,4`-trihydroxyflavanone (1), 2`,4`,2,4,-tetrahydroxychalcone (2), and oxyresveratrol (3) showed the more potent inhibitory effect compared to kojic acid, a well-known skin whitening agent with antityrosinase effect. Moracinoside M (4) and moracin M-3`-O-β-D-glucopyranoside (5) also showed the moderate tyrosinase inhibitory activities.

Isolation of Prenylated Isoflavonoids from Cudrania tricuspidata Fruits that Inhibit A2E Photooxidation

Abstract: High-performance liquid chromatography coupled to an online ABTS+-based assay (online HPLCABTS+) system was used to determine the principal antioxidants in Cudrania tricuspidata fruits. Six prenylated isoflavonoids (1-6) were isolated from C. tricuspidata fruits according to the online HPLC-ABTS+ system. The structures of isolated compounds, alpiniumisoflavone (1), 6,8-diprenylorobol (2), 6,8-diprenylgenistein (3), pomiferin (4), 4`-methylalpiniumisoflavone (5), and osajin (6) were identified by their retention time, UV spectra, ESI-MS, and NMR data. Among these compounds, 6,8-diprenylorobol (2) and pomiferin (4) reduced A2E photooxidation in a dose dependent manner.

Natural Compounds with Antioxidant Activity: Recent Findings from Studies on Medicinal Plants

Abstract: Reactive oxygen species potentially cause damage to cellular components including lipids, protein and DNA; this oxidative damage plays a key role in the pathogenesis of neurodegenerative disease, cardiovascular disease, metabolic disease and cancer. On the basis of the oxidative stress hypothesis, a number of studies have been performed to search for an efficient and safe antioxidant. Although in vitro studies have provided promising results, only a limited number of natural and synthetic antioxidants have been developed for clinical application due to their low efficacy and side-effects. Thus, the discovery of new antioxidants with marked efficacy and safety has attracted worldwide attention in recent decades. Since plants are recognized as important sources of natural antioxidants, our research has focused on the discovery of new naturally occurring antioxidants from medicinal plants. The purpose of this review is to open a new prospect in the field of search for natural antioxidants from medicinal plants by summarizing our recent findings. Using in vitro bioassay systems such as 2,2-diphenyl-1-picrylhydrazyl, superoxide radical scavenging tests and lipid peroxidation models, we have tested over than 350 species of medicinal plants for their antioxidant activity and selected several of them for further investigation. During the research on the discovery of effective natural antioxidants from the medicinal plants selected, we have isolated several new and known antioxidant compounds that include stilbene glycosides, phenolic glycosides, flavonoids, oligostilbenes, and coumarins. Our results suggest that the presence of antioxidant compounds in the medicinal plants might be associated with the traditional use to treat inflammation, cardiovascular disease and various chronic diseases.

Articles : A Convenient HPLC/ELSD Method for the Quantitative Analysis of Betaine in Lycium chinense

Abstract: In order to facilitate the quality control of betaine from the fruits of Lycium chinense, we have developed a rapid and simple method for quantitative determination. Determination was achieved on a Discovery C18 column with an isocratic solvent system of 0.32% perfluoropentanoic acid aqueous-acetonitrile at a flow-rate of 0.5 mL/min and detected an ELSD. The method was reproducible with intra- and inter-day variations of less than 6% (R.S.D). The recoveries were in the range of 90.01~100.05%. The method turned out to be fast and simple, furthermore, to have a good selectivity and sensitivity for the quantity determination of betaine in the fruits of L.chinense.

Chemotype Discrimination and Rapid Identification of Angelica Roots by DART-TOF-MS

Abstract: The Angelica root has been used as a medicinal herb in many Asian countries including Korea, China, and Japan. Angelica gigas, A. sinensis, and A. acutiloba have been considered as Angelicae radix in Korean, Chinese, and Japanese Pharmacopoeia, respectively. Since the origins of Angelicae radix differ from country to country, there is a need to develop an efficient analytical method to identify the origin of the Angelica root. In order to obtain chemical fingerprints, three different Angelicae Radices were analyzed by direct analysis in real time mass spectrometry (DART-MS). Significantly different DART-MS spectra were observed from three different species of Angelicae Radix. Strong peaks of decursin or decusinol angelate, and its dimer were exclusively found from A. gigas. Ligustilide and linoleic acid were detected as the major component from A. acutiloba. The strongest ligustilide peak was observed from A. sinensis. DART-MS fingerprinting is a promising method for the rapid identification and/or quality control of Angelicae Radix.

Anti-metastatic Effects of Celastrus orbiculatus Extract in B16F10 Melanoma Cells

Abstract: Celastrus orbiculatus has been widely used as a traditional medicine for the treatment of many diseases including rheumatoid arthritis and odontalgia. In the present study, anti-metastatic activity of a methanolic extract from C. orbiculatus (MCO) was studied. A gelatin zymographic assay revealed that MCO has potent inhibitory effects on MMP-2 and MMP-9 activities in B16F10 melanoma cells. Moreover, MCO attenuated MMP expression via down-regulation of NF-B translocation to the nucleus. Melanoma cell migration and invasion were also down-regulated by MCO. In addition, MCO significantly suppressed lung metastasis in an in vivo model. These results strongly suggest that MCO may possibly be used as a valuable anti-metastatic agent for cancer treatment.

Inhibition of Aldose Reductase on Rat Lens by Tartary Buckwheat

Abstract: To evaluate the potential of naturally occurring aldose reductase (AR) inhibitors from food material, MeOH extract and stepwise polarity fractions from tartary buckwheat and two common Korean buckwheat cultivars, yangjul-maemil and daesan-maemil, were tested on AR inhibition in rat lens in vitro. The EtOAc fraction from tartary buckwheat exhibited good AR inhibitory activity (IC50 value, 8.19 μg/ml). A portion of the EtOAc fraction from tartary buckwheat led to the isolation of rutin by MeOH recrystalization. Rutin exhibited good AR inhibitory activity (IC50 value, 9.28 μM). These results suggest that tartary buckwheat could be a useful food material in the development of a novel AR inhibitory agent against diabetic complications.

Cytotoxic Sesquiterpenoid from the Seeds of Amomum xanthioides

Abstract: As parts of our continuing search for biologically active compounds from medicinal plants, we investigated the constituents of the seeds of Amomum xanthioides and isolated a sesquiterpenoid, a nerolidol derivative from its MeOH extract. The chemical structure was determined by spectroscopic methods, including 1D and 2D NMR to be (,,)-2-(5'-ethenyltetrahydro-5'-methylfuran-2'-yl)-6-methylhept-5en-2-ol (1). Compound 1 was isolated for the first time from nature source. Compound 1 exhibited a good cytotoxicity against SK-OV-3 and SK-MEL-2 cells (: 16.7 and , respectively) using a SRB bioassay. In this study, we also determined the absolute configuration of 2 reported in previous paper.

Inhibition of Adipocyte Differentiation by MeOH Extract from Carduus crispus through ERK and p38 MAPK Pathways

Abstract: In this study, the effects of a methanol (MeOH) extract of Carduus crispus L. (Asteraceae) on adipogenesis was investigated in 3T3-L1 cells. To differentiate preadipocytes to adipocytes, confluent 3T3-L1 preadipocytes were treated with a hormone mixture, which included isobutylmethylxanthine, dexamethasone, and insulin (MDI). The methanol extract of C. crispus significantly decreased fat accumulation by inhibiting adipogenic signal transcriptional factors in MDI-induced 3T3-L1 cells in a dose-dependent manner. In MTT assays and on PI-staining, methanol extract of C. crispus inhibited the proliferation of 3T3-L1 cells during mitotic clonal expansion (MCE). The anti-adipogenic effect of the Carduus extract seemed to be associated with the upregulation of extracellular signal-regulated kinase (ERK) and p38 mitogen-activated protein kinase (MAPK) pathways within the first 2 days after MDI treatment. These results suggest that methanol extract of C. crispus might be beneficial for the treatment of obesity.

Bioactive Phenolic Constituents from the Culms of Phyllostachys bambusoides

Abstract: In our search for bioactive phenolics from plants, the culms of Phyllostachys bambusoides has been selected for investigation of anti-cariogenic and 1,1-diphenylpicrylhydrazyl (DPPH) radical scavenging agents based on the initial screening results. Fractionation process of n-hexane and extracts afforded four phenolic constituents, ferulic acid (1), vanillin (2), coniferaldehyde (3), and coniferyl alcohol (4) as guided by their DPPH free radical scavenging activities. Additionally, activity-guided fractionation of EtOAc extract with anti-cariogenic activity has resulted in the isolation of coniferaldehyde (3), 2,6-dimethoxy-p-benzoquinone (5), p-methoxycinnamic acid (6), ()-balanophonin (7), and 6-methoxychromanone (8). The structures of 1 - 8 were determined by spectroscopic data interpretation, and also by comparison of their data with the published values. Phenolic compounds 1 - 4 exhibited similar DPPH radical scavenging activities compared with the synthetic antioxidant, butylated hydroxytoluene (BHT), and compounds 3 and 5 - 8 showed significant antibacterial activity against cariogenic oral streptococci, Streptococcus mutans and S. sobrinus.

Cholinesterase Inhibitory Activities of Alkaloids from Corydalis Tuber

Abstract: Several isoquinoline alkaloids (1 - 18), which have basic chemical structures as protoberberine and aporphine skeletones, were evaluated for their inhibitory activities on AChE and BuChE. Among them, compounds 3, 4, 6, 8 and 12 showed the potent AchE activity with the values ranging from to , meanwhile, compound 14 - 17 exhibited strong inhibitory activity with values from to . Compounds 14 - 17 exhibited selective inhibition for AChE compared with BuChE. The isoquinoline alkaloid possesses aromatic methylenedioxy groups and quaternary nitrogen atoms are crucial for the anti-cholinesterase inhibitory activity.

Isolation of Compounds from Cimicifugae Rhizoma and their Cytotoxic Activity

Abstract: Five known compounds, cimigenol (1), 25-O-acetylcimigenol (2), cimigenol 3-O--D-xylopyranoside (3), ferulic acid methyl ester (4), and visnagin (5), were isolated from Cimicifugae Rhizoma (Ranunculaceae). The chemical structures of these compounds were determined on the basis of spectroscopic analyses including 2D NMR. Compounds 1 - 5 were evaluated for their cytotoxic activity against the HL-60, MCF-7, and A549 cancer cell lines in in vitro. Among them, compounds 4 and 5 showed moderate inhibitory activity against HL-60 cancer cell lines with values of 24.8 and 18.1 , respectively.

Articles : Toxicological and Pharmacological Studies of New Coumarin and Furocoumarin Derivatives in Albino rats

Abstract: Synthetic coumarin and furocoumarin derivatives were evaluated for anticoagulant activity and the effect on liver and kidney function. It was found that all of the compounds under investigation proved to be neither toxic nor lethal up to 500 mg/100 g body weight as a single dose for 24 hrs. All tested compounds showed a significant increase in prothrombin time (PT) in the acute model but failed to show a significant action in the chronic model. Furthermore, all tested compounds revealed a significant increase in activated partial thromboplastin time (APTT) as compared to control value in both acute and chronic model. Also, all tested compounds did not cause any significant changes on liver and kidney functions in rats.

Cytotoxicity of Ergosterol Derivatives from the Fruiting Bodies of Hygrophorus russula

Abstract: Bioassay-guided fractionation of the -soluble fraction of a MeOH extract of the fruiting bodies of Hygrophorus russula led to the isolation of five ergosterol derivatives (1 - 5). The structures of these compounds were identified as ergosterol peroxide (1), ergosta-4,6,8(14),22-tetraen-3-one (2), ergosta-7,22-diene-3,5,6-triol (3), ergosta-7,22-diene-3,5,6,9-tetraol (4), and 5,6-epoxy-ergosta-8(14),22-diene-3,7-diol (5) by comparing their physicochemical and spectral data with those in the literature. These compounds were evaluated for in vitro cytotoxicity against A549 and XF498 cancer cell lines. Most of the tested compounds, except for compound 3, exhibited moderate cytotoxicity against both A549 and XF498 cell lines with values ranging from 10.2 to 18.3 and from 11.4 to 24.6 , respectively.

Antioxidative and Antiobesity Activity of Nepalese Wild Herbs

Abstract: A screening of Nepalese wild herbs for their antioxidant and antiobesity activity was carried out. The herbs including Allium hyposistum, Crateva unilocularis, Dryoathyrium boryanum and Cuscuta reflexa are widely used traditionally for various medicinal purposes in Nepal. The ethyl acetate fraction of D. boryanum showed polyphenol content of 266 μgGAE/mg with potent antioxidative activity assessed by DPPH free radical scavenging activity and hydrogen peroxide scavenging activity. The EtOAC fraction of D. boryanum also inhibited the lipid formation with 35% at 100 μg/mL in 3T3-L1 cell model. Along with this, butanol fraction of C. reflexa also showed potent antioxidative activity and inhibition of 80% of lipid formation at the test concentration of 75 μg/mL in 3T3-L1 cell line. This showed that these plant extracts have potential of antioxidant and antiobesity activity.