Showing papers in "Natural product sciences in 2002"

Herbal Medicines Are Activated by Intestinal Microflora

Abstract: Glycosides of herbal medicines, such as glycyrrhizin, ginsenosides, kalopanaxsaponins, rutin and ponicirin, were studied regrading their metabolic fates and pharmacological actions in relation to intestinal bacterial using germ-free, gnotobiotic and conventional animals. When glycyrrhizin (GL) was orally administered, 18β-glycyrrhetinic acid (GA), not GL, was detected in plasma and intestinal contents of gnotobiotic and conventional rats. However, GA could not be detected in germ-free rats. When GL incubated with human intestinal bacteria, it was directly metabolized to GA (＞95%) or via 18 β-glycrrhetinic acid-3- β-D-glucuronide (＜5%). Orally administered GL was effective in gnotobiotic and conventional rats for liver injury induced by carbon tetrachloride, but was not effective in germ-free rats. When ginseng saponins were orally administered to human beings, compound K was active for tumor metastasis and allergy. When kalopanaxsaponins were incubated with human intestinal microflora, they were metabolized to kalopanaxsaponin, A, kalopanaxsaponin I and hederagenin. These metabolites were active for rheumatoid arthritis and diabetic mellitus while the other kalopanxsaponins were not. When flavonoid glycosides were orally administered to animals, aglycones and/or phenolic acids were detected in the urine. The metabolic pathways proceeded by intestinal bacteria rather than by liver or blood enzymes. These metabolites were active for rheumatoid arthritis and diabetic mellitus while the other kalopanxsaponins were not. When flavonoid glycosides were orally administered to animals, aglycones and/or phenolic acids were detected in the urine. The metabolic pathways proceeded by intestinal bacteria rather than by liver or blood enzymes. These metabolites, aglycones and phenolic acids, showed antitumor, antiinflammatory and antiplatelet aggregation activities. These findings suggest that glycosides of herbal medicines are prodrugs.

Antioxidant compounds from the stem bark of Sorbus commixta

Abstract: The MeOH extract of Sorbus commixta (Rosaceae) exhibited strong DPPH radical scavenging activity, and through activity-guided fractionation two antioxidant compounds were isolated and identified as catechin-7-O-β-D-xylopyranoside (1) and cetechin-7-O-β-D-apiofuranoside (2) by physicochemical and spectrometric methods. To evaluate the antioxidant effect of these compounds, some in vitro tests, such as the DPPH radical scavenging activity test, the superoxide radical scavenging activity test and lipid peroxidation inhibitory activity test, were performed. Compounds 1 and 2 showed stronger activities than both α-tocopherol and butylated hydroxy anisole (BHA) in each assay.

Coumarins and a Pyrimidine from Angelica gigas Roots

Abstract: Five coumarins and a pyrimidine were isolated from the roots of Angelica gigas Their structures were elucidated as bergapten (1), decursinol angelate (2), decursin (3), nodakenetin (4), uracil (5) and nodakenin (6) by spectral analysis Among them, bergapten (1) and uracil (5) were isolated for the first time from this plant part

Anti-platelet Effect of the Phenolic Constituents Isolated from the Leaves of Magnolia obovata

Abstract: In the course of our work on anti-platelet constituents from plants, eight phenolic compounds, (±)-syringaresinol (1), 4-hydroxybenzaldehyde (2), 4-hydroxybenzoic acid (3), vanillic acid (4), 4-hydroxy cinnamic acid (5), quercetin 3-O-rhamnoside (6), rutin (7), and quercetin 3-(2^G-rhamnosylrutinoside) (8) were isolated from the methanol extract of the leaves of Magnolia obovata. The compounds were identified based on the spectroscopic data. Compound 2, 3, 5, 6, 7 and 8 were isolated for the first time from genus Magnolia. 1 and 6 showed same order of inhibitory potencies as acetylsalicylic acid (ASA) to rat platelet aggregation induced by all the stimulators tested. The remaining six compounds showed only mild effects.

Antioxidant Compounds from Twig of Morus alba

Abstract: 【The MeOH extract of the twig of Morus alba L. (Moraceae) inhibited strong lipid peroxidation activity. In order to find out active principle from the plant, acivity-guided fractionation was performed and five antioxidant compounds were isolated. Their chemical structures were identified as 6-geranylapigenin (1), 6-geranylnorartocarpetin (2), resveratrol (3), oxyresveratrol (4) and quercetin (5) by physicochemical and spectrometric methods. Compounds 1-5 significantly inhibited lipid peroxidation in rat brain homogenate $(IC_{50}\;values\;of\;3.37,\;3.74,\;0.23,\;0.29\;and\;0.06\; {\mu}M,\;respectively)$ .】

An International Collaborative Program To Discover New Drugs from Tropical Biodiversity of Vietnam and Laos

Abstract: An International Cooperative Biodiversity Group (ICBG) program based at the University of Illinois at Chicago initiated its activities in 1998, with the following specific objectives: (a) inventory and conservation of of plants of Cuc Phuong National Park in Vietnam and of medicinal plants of Laos; (b) drug discovery (and development) based on plants of Vietnam and Laos; and (c) economic development of communities participating in the ICBG project both in Vietnam and Laos. Member-institutions and an industrial partner of this ICBG are bound by a Memorandum of Agreement that recognizes property and intellectual property rights, prior informed consent for access to genetic resources and to indigenous knowledge, the sharing of benefits that may arise from the drug discovery effort, and the provision of short-term and long-term benefits to host country institutions and communities. The drug discovery effort is targeted to the search for agents for therapies against malaria (antimalarial assay of plant extracts, using Plasmodium falciparum clones), AIDS (anti-HIV-l activity using HOG.R5 reporter cell line (through transactivation of the green fluorescent protein/GFP gene), cancer (screening of plant extracts in 6 human tumor cell lines - KB, Col-2, LU-l, LNCaP, HUVEC, hTert-RPEl), tuberculosis (screening of extracts in the microplate Alamar Blue assay against Mycobacterium tuberculosis all performed at UIC, and CNS-related diseases (with special focus on Alzheimer's disease, pain and rheumatoid arthritis, and asthma), peformed at Glaxo Smith Kline (UK). Source plants were selected based on two approaches: biodiversity-based (plants of Cuc Phuong National Park) and ethnobotany-based (medicinal plants of Cuc Phuong National Park in Vietnam and medicinal plants of Laos). At mc, as of July, 2001, active leads had been identified in the anti-HIV, anticancer, antimalarial, and anti- TB assay, after the screening of more than 800 extracts. At least 25 biologically active compounds have been isolated, 13 of which are new with anti-HIV activity, and 3 also new with antimalarial activity. At GSK of 21 plant samples with a history of use to treat CNS-related diseases tested to date, a number showed activity against one or more of the CNS assay targets used, but no new compounds have been isolated. The results of the drug discovery effort to date indicate that tropical plant diversity of Vietnam and Laos unquestionably harbors biologically active chemical entities, which, through further research, may eventually yield candidates for drug development. Although the substantial monetary benefit of the drug discovery process (royalties) is a long way off, the UIC ICBG program provides direct and real-term benefits to host country institutions and communities.

Review : The Chemistry of Secondary Products from Acanthopanax Species and their Pharmacological Activities

Abstract: The chemistry of secondary products from Acanthopanax species and their pharmacological activities were reviewed. A nitrogenous compound, a furan compound, a quinoid, benzoids, coumarins, phenylpropanoids, lignans, flavonoids, terpenoids, phytosterols, polyacetylenes, a pyrimidine, cyclitols, monosaccharides and an aliphatic alcohol have been isolated from Acanthopanax species and have been shown to have various levels of activities such as anti-bacterial, anti-cancer, anti-gout, anti-hepatitis, anti-hyperglycemic, anti-inflammatory, anti-leishmanicidic, anti-oxidant, anti-pyretic, anti-xanthine oxidase, choleretic, hemostatic, hypocholesterolemic, immunostimulatory and radioprotectant effects, etc.

Effects of Insect Crude Drugs on Blood Coagulation Fibrinolysis System

Abstract: The in vitro anticoagulant and fibrinolytic activities of crude extracts from insects were evaluated in order to find effective therapeutic drugs for the treatment of myocardial and cerebral thrombosis. We prepared three types of extracts (water, methanol and ethylacetate) from 28 insects for use as raw materials for the activity assays. The fibrinolytic activity was tested using the fibrin plate method and the activated partial thromboplastin time and thrombin time were measured for blood clotting activity. With regards to the fibrinolytic system, water extracts of six kinds of insects displayed a remarkable level of activity with a plasmin-like action. The water extracts of [Catharsius molossus, Eupolyphaga sinensis, Huechys sanguinea, Mantidis oo¨theca, Mimela splendens, and Polistes mandarinus (Vespae Nidus)] exhibited the activity. On the other hand, the methanol extracts did not display any fibrinolytic activity. In terms of the coagulation system, an aqueous extract of silkworm Tongchunghacho (Paecilomyces japonica), Oxya japonica japonica and Buthus martensi (Scorpion) increased the clotting time significantly longer (181 times) than the control. These results suggest that crude drugs from insects are useful sources for the development of new drugs for use in treatments involving blood coagulation and fibrinolysis.

Analgesic, Anti-inflammatory and Diuretic Activities of Pisonia grandis

Abstract: In the present study, Pisonia grandis leaves were extracted with chloroform and methanol The extracts were vacuum dried to yield the respective chloroform (CE) and methanol extract (ME) CE and ME were evaluated for analgesic, anti-inflammatory (acute and chronic) and diuretic activity at 2 dose levels (250 and 500 mg/kg) Significant analgesic and anti-inflammatory activities were associated with CE and ME CE at the dose level of 500 mg/kg was found to exhibit equivalent chronic anti-inflammatory activity as diclofenac at 50 mg/kg dose level Significant diuretic activity was exhibited by ME Graded dose response for all the activities were observed for the extracts

Antioxidant activity of anthraquinones from Morinda elliptica

Abstract: Antioxidative properties of fifteen anthraquinone derivatives, including eleven atural anthraquinones isolated from the roots of Morinda elliptica and four from synthetic origin were evaluated using thin layer chromatography (TLC), ferric thiocyanate (FTC) and thiobarbituric acid (TBA) methods. Five of the compounds, nordamnacanthal, damnacanthal, 2-formyl-1-hydroxyanthraquinone, morindone and alizarin showed higher antioxidative activity than standard natural antioxidant, , on the FTC assay. Morindone and alizarin showed the strongest antioxidant activity. The results from the bioassay using TBA method correlated well with the results of the FTC method.

Chemical Constituents from Sorbus commixta

Abstract: Two lupane-type triterpenes, lupenone (1) and lupeol (2), a phytosterol, (3), two ursane-type triterpenes, ursolic acid (4) and ursolic acid (5), a lignan, (-)-lyoniresinol (6), and two flavanol glycosides, (7) and (8) were isolated from the stem bark of Sorbus commixta (Rosaceae). Their chemical structures were identified by physicochemical and spectroscopic methods.

Monoamine Oxidase Inhibitors from Aquilaria agallocha

Abstract: From the bioassay-directed fractionation and isolation of dichloromethane fraction of Aquilaria agallocha, four compounds having MAO inhibitory effect were isolated by repeated silica gel column chromatography. Their chemical structures were established as psoralen (1), bergapten (2), (3) and 5-hydroxymethylfurfural (4) on the basis of their physicochemical and spectral data. Among these compounds, psoralen and bergapten showed high inhibitory activities in vitro against mouse brain MAO with values , respectively.

Evaluation of Cytotoxic Potential of Indonesian Medicinal Plants in Cultured Human Cancer Cells

Abstract: One-hundred and twenty plant extracts were prepared from 29 Indonesian plants and were primarily tested in vitro cytotoxicity in cultured human lung (A549), colon (Col2), and stomach (SNU-638) cancer cells. As a result, the 23 extracts were found to be active in the criteria of . Remarkable cytotoxicity was observed for chloroform and n-butanol extracts of Calotropis gigantea, with values ranging from 0.25 to . Five extracts derived from Eclipta alba and Excoecaria cochinchinensis displayed potent cell-line selective cytotoxicity, while the rest of 15 extracts showed modest cytotoxic activity against all of three cancer cells. In addition, the cytotoxic potential of subfractions of Zingiber cassumunar against a panel of human cancer cell lines is presented.

Antithrombotic Activity of Sunghyangjunggisan

Abstract: As apart of our continuing search for antistroke agents from the herbal medicinal resources, we examined in vitro, ex vivo and in vivo the possibility of Sunghyangjunggisan and its ingradients as a novel antithrombotic agent In vitro ADP- and collagen-induced rat platelet aggregations were potently inhibited by Arisaematis Rhizoma, Cinnamomi Cortex and Zingiberis Rhizoma in a dose-dependent manner, but not by Sunghyangjunggisan However, Sunghyangjunggisan significantly inhibited ex vivo rat platelet aggregation Arisaematis Rhizoma, Atractylodis Rhizoma Alba, and Pinelliae Rhizoma also significantly inhibited ex vivo rat platelet aggregation Sunghyangjunggisan, Alpiniae Fructus and Zingiberis Rhizoma showed significant protection from death due to pulmonary thrombosis in mice Therefore, Sunghyangjunggisan can express the antithrombotic action, when it is orally administered

The Constituents of the Aerial Part of Gastrodia elata Blume

Abstract: From the MeOH extract of the aerial part of Gastrodia elata Blume (GEB) (Family: Orchidaceae), eight compounds have been isolated on repeated column chromatography, and their structures were elucidated as dotriacontanoic acid (1), beta-sitosterol (2), 4-hydroxybenzaldehyde (3), docosanoic acid oxiranylmethyl ester (4), hentriacotanoic acid (5), octadecanoic acid (6), benzoic acid (7) and gastrodin (8) on the basis of their spectral evidences including EI-Mass and 2D-NMR spectrum. All of them were obtained from the aerial part of Gastrodia elata Blume for the first time, in which compound 4 is a novelty to our best knowledge. It is also known that a phenolic glucoside, gastrodin is a major constituent just like Gastrodia rhizome.

Flavonoids of Cinnamomum tamala

Abstract: The flavonoids kaempferol, quercetin, myrecetin, kaempferol-3-O-rhamnoside and quercetrin has been isolated from the leaves of C. tamala and their structures were established by spectral analysis and direct comparison with authentic samples. This is the first report of occurrence of these compounds from C. tamala.

Ardimerin, a New Dimeric Lactone from the Herb of Ardisia japonica

Abstract: A new ardimerin (1) was isolated from the herb of Ardisia japonica. Its structure was determined by the elucidation of spectroscopic data and a chemical transformation. Compound (1) showed potent radical scavenging effect on DPPH radical .

Cytotoxic Activities of Brominated Sesquiterpenes from the Red Alga Laurencia okamurae

Abstract: Four known sesquiterpenes, laurinterol (1), isolaurinterol (2), aplysinal (3) and aplysin (4) were isolated from the Korean red alga Laurencia okamurae off Cheju Island, Korea. Their structures were identified by comparison with the literature data. Compounds 1-4 showed potent cytotoxicity against A549, SK-OV-3, SKMEL-2, XF498, and HTl5 cell lines with values ranging from 1.2 to 17.6 .

Flavone Glucosides from the Leaves of Helianthus tuberosus

Abstract: Two flavone glucosides have been isolated from the leaves of Helianthus tuberosus (jerusalem artichoke). Their structures were identified as kaempferol 3-O-glucoside (1) and quercetin 7-O-glucoside (2) by spectroscopic analysis and confirmed by comparison with reported data. These flavonoids were isolated for the first time from this plant part.

NFAT Transcription Factor Inhibitory Constituents from Cnidium officinale

Abstract: Four hundred varieties of plant extracts were screened for inhibitory activity against the NFAT transcription factor which plays an important role in inducing immune response. Among them, the MeOH extract of Cnidium officinale showed potent activity, and the activity-guided separation yielded butylidenephthalide, senkyunolide A and falcarindiol as the active constituents. The value of butylidenephthalide was and was similar to that of senkyunolide A . Interestingly, falcarindiol showed higher activity than the two phthalides.

Terpenoid constituents from Youngia koidzumiana

Abstract: Youngia koidzumiana is an endemic plant growing in Mt. Chiri. In our ongoing research for endemic species in Korea, we investigated the chemical constituents from the MeOH extract of Y. koidzumiana whole plants. The MeOH extract was partitioned with hexane, ethyl acetate and BuOH, successively. Four known compounds were isolated from ethyl acetate fraction by repeated column chromatography. Their structures were elucidated by the physicochemical and spectral data as germanicol acetate (1), oleanolic acid (2), brachynereolide (3) and ixerin Y (4).

Composition of the Essential Oil of Chrysanthemum sibiricum, and Cytotoxic Properties

Abstract: GC-MS data on the volatile oil (CS-oil) of Chrysanthemum sibiricum herbs led to the identification of 2-methoxythioanisol, (+)-camphor, geraniol, citral, thymol, eugenol, oxide, , , juniper camphor together with an unknown substance using the mass spectral library and literature data. CS-oil exhibited significant cytotoxicities on HL-60 cell and mild on HepG-2 cell , though the antioxidant ability was found not to be potent . However, the component eugenol showed potent antioxidant ability but mild cytotoxicity. Methyleugenol with no phenolic OH showed less potent cytotoxic and antioxidative properties than eugenol suggesting that phenolic OH plays an important role for the cytotoxic and antioxidant abilities. The oil-pretreatment prevented lipid peroxidation induced by bromobenzene in the rat. Therefore, it was demonstrated that CS-oil could be a cytotoxic agent with antioxidant properties.

Sanguisorba officinalis Inhibits Immediate-type Allergic Reactions

Abstract: The effect of aqueous extract of Sanguisorba officinalis L (Rosaceae) root (SOAE) on the immediate-type allergic reactions by anal therapy was investigated SOAE (001 to 1 g/kg) dose-dependently inhibited systemic anaphylaxis induced by compound 48/80 in mice When SOAE was pretreated at the same concentrations with systemic anaphylaxis, the plasma histamine levels were reduced in a dose-dependent manner SOAE (01 and 1 g/kg) also significantly inhibited local anaphylaxis activated by anti-DNP IgE SOAE (0001 to 1 mg/ml) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE The level of cyclic AMP (cAMP) in RPMC, when SOAE (1 mg/ml) was added, transiently and significantly increased compared with that of basal cells These results provide evidence that anal therapy of SOAE may be beneficial in the treatment of allergic diseases

Cytotoxic Activities of Indigenous Plant Extracts in Cultured Human Cancer Cells

Abstract: In continuous efforts for discovery of novel potent antitumor agents from natural products, fifty-seven methanolic extracts derived from indigenous Korean plants were primarily evaluated for in vitro cytotoxic activity in cultured human lung (A549) and colon (Col2) cancer cells As a result, 16 plant extracts were found to be active against A549 cells and 15 extracts were active against Col2 cells in the criteria of In particular, the extracts of Calystegia soldanella , Heloniopsis orientalis , and Thuja koraiensis showed a potent cytotoxic activity Further study for the identification of active compounds from these lead extracts might be warranted

Cytotoxicity of lignans from Lindera erytherocarpa makino

Abstract: Three lignans were isolated from a methanol extract of Lindera erytherocarpa Makino (Lauraceae) are evaluated in vitro cytotoxicity using three cancer cell line assay. The compounds were identified as methyllinderone (1), linderone (2), and kanakugiol (3) by spectroscopic methods. Amongst the compounds, methyllinderone (1) showed significant cytotoxicity against mouse melanoma (B16-FlO), human acetabulum fibrosarcoma (HT1080), and choronic myelogenous leukemia (K562) cancer cell lines with values of 2.2, 2.5, 8.3 , respectively.

Studies on the Constituents of the Stem Barks of Acanthopanax gracilistylus W. W. Smith

Abstract: Ten compounds were isolated from the stem barks of Acanthopanax gracilistylus WW Smith (AGS) by steam distillation, they were p-menta-1,5,8-triene, n-butyl isobutylphthalate, p-mentha-1,5-diene-8-ol, 8-hydroxy-p-cymene, myrtenol, trans-(＋)-carveol, 1,3-di-tert-butylbenzene, 4-methyl-2,6-di-butylphenol, valencene and verbenone, respectively, characterized by GS-Mass spectra. And we have also extracted and isolated from the MeOH extracts of the stem barks of AGS, two compounds were obtained. On the basis of chemical and spectral evidence, they were syringin(1), β-sitosterol(2).

Antitumor activity of cultured mycelia of Ganoderma lucidum

Abstract: The cultured mycelia of fungus Ganoderma lucidum were investigated for the inhibitory effect on the growth of s.c. transplanted Lewis lung carcinoma (LLC) in BDF-1 mice by intraperitoneal (i.p.) administration. The cultured mycelia showed antitumor activity with T/C values of 89.6 and 50.3 % at doses of 100 and 500 mg/kg, respectively, compared to adriamycin, which was used a positive control, with T/C value of 54.6 % at 2 mg/kg.

Inhibitory Effects of Hydrolysable Tannins on Tyrosinase Activities in B16 Mouse Melanoma Cells

Abstract: To investigate skin whitening natural substances, the effects on melanogenesis by measuring the tyrosinase activity and the melanin contents of three hydrolysable tannins, 1,2,6-tri-O-galloyl-β-D-glucose (1), 2,3-(S)-HHDP-D-glucose (2) and pedunculagin (3) in B16 melanoma cells were examined. 1,2,6-Tri-O-galloyl-β-D-glucose (1), 2,3-(S)-HHDP-D-glucose (2) and pedunculagin (3) inhibited tyrosinase activity in B16 melanoma cells in a dose-dependent manner.

Effects of Eurycoma longifolia Jack on Masculine Copulatory Behaviour in Middle Aged Male Rats - A Comparison Study

Abstract: The effects of Eurycoma longifolia Jack on masculine copulatory behaviour were studied in the middle aged male Sprague-Dawley rats, 9 months old and retired breeders after dosing them with 500 mg/kg twice daily for 10 days prior to test The test lasted for 30 minutes after a 20 minute adaptation period, was carried out on the 11th day during the dark phase of the light-dark cycle (2000-0700 hours) and in subdued light, using a modified copulation cage but with the presence of a piece of mirror of appropriate size to facilitate observation Results showed that the mean values of EL-1, EL-2 and EL-3 of the control middle aged male rats were 10320 sec, 9121 sec and 8000 sec but were significantly (p

Antitumor Activities of Extract of Viscum album var. coloratum Modified with Viscum album var. coloratum Agglutinin

Abstract: The mistletoe lectins are major active components in the extract of European mistletoe (Viscum album L) that have been widely used in adjuvant chemotherapy of cancer This study was performed to investigate the antitumor activity of extract of Korean mistletoe (Viscum album var coloratum) modified with Korean mistletoe lectin (Viscum album var coloratum agglutinin, VCA) Compared with the results of VCA, survival rate was increased and experimental lung metastasis was reduced by treatment of modified extract (VCM) In addition, the treatment of VCM reduced angiogenesis and VCA-induced toxicity measured by a CAM assay And VCM inhibited proliferation and induced apoptosis in vitro in tumor cells originated from tissues which are possible to apply topically without surgery Taken together, the antitumor activities of VCM-treated group outperformed the activities of the VCA-treated group