RESUMO
Dracaena cambodiana Pierre ex Gagnep. is well known as a medicinal plant and widely distributed in Vietnam. Phytochemical investigation on the trunks of D. cambodiana lead to the isolation of four undescribed compounds (1-4) together with seven known ones (5-11). Their structures were determined to be pennogenin-24-yl-O-ß-D-glucopyranoside (1), 17α-hydroxycambodianoside C (2), (25R)-27-hydroxypenogenin 3-O-α-L-rhamnopyranosyl-(1â3)-[α-L-rhamnopyranosyl-(1â2)]-ß-D-glucopyranoside (3), (3ß,25R)-17α,22α-dihydroxy-furost-5-en-3-yl-O-α-L-rhamnopyranosyl-(1â3)-[α-L-rhamnopyranosyl-(1â2)]-ß-D-glucopyranoside (4), dracagenin A (5), 1-O-ß-D-glucopyranosyl-2-hydroxy-4-allylbenzene (6), 1-O-α-L-rhamnopyranosyl-(1â6)-ß-D-glucopyranosyl-2-hydroxy-allylbenzene (7), 2-O-α-L-rhamnopyranosyl-(1â6)-ß-D-glucopyranosyl-1-hydroxy-allylbenzene (8), cinnamrutinoside A (9), icariside D1 (10), and seco-isolariciresinol 9-O-ß-glucopyranoside (11) by extensive spectroscopic investigation, HR-ESI-MS, 1D and 2D NMR spectra. The anti-inflammatory activity of the isolated compounds was evaluated on macrophages. Compounds 1-6 significantly inhibited nitric oxide production in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Among them, compound 1 showed the best inhibitory activity with an IC50 value of 8.90±0.56â µM.
Assuntos
Derivados de Alilbenzenos , Dracaena , Saponinas , Lipopolissacarídeos/farmacologia , Estrutura Molecular , Óxido Nítrico , Saponinas/farmacologia , Saponinas/química , Glucosídeos/química , Glucosídeos/farmacologiaRESUMO
Four previously undescribed compounds named phyllancosides A and B (1 and 2), and phyllancochines A and B (3 and 4) together with ten known compounds (5-14) were isolated from the aerial parts of Phyllanthus cochinchinensis Spreng. Their chemical structures were elucidated on the basis of comprehensive analysis of IR, HR-ESI-MS, 1D and 2D NMR spectra. The absolute configurations of 1 and 2 were determined by electronic circular dichroism (ECD) spectra. Compounds 3, 4, and 10 showed antimicrobial activity against E. faecalis, S. aureus, and B. cereus with the MIC values in range of 32-256â µg/mL. Compound 11 inhibited E. faecalis and B. cereus, and 7 inhibited S. aureus with the MIC values in range of 64-128â µg/mL. In addition, compounds 1, 3, 4, 8, and 9 showed significantly NO production inhibitory activity in LPS activated RAW 264.7 cells with IC50 values ranging from 36.57 to 56.34â µM.
Assuntos
Anti-Infecciosos , Lipopolissacarídeos , Animais , Camundongos , Células RAW 264.7 , Estrutura Molecular , Lipopolissacarídeos/farmacologia , Staphylococcus aureus , Óxido Nítrico , Componentes Aéreos da Planta/química , Anti-Infecciosos/análiseRESUMO
Eight furostanol glycosides including five undescribed compounds, named tribufurostanosides A-E (1-5), and three known ones (6-8) were isolated from the fruits of Tribulus terrestris L. Their chemical structures were determined by the IR, HR-ESI-MS, 1D-, and 2D-NMR spectra. Furostanols 1-8 significantly inhibited nitric oxide production in LPS activated RAW 264.7 cells with IC50 values ranging from 14.2 to 64.7 µM, compared to that of the positive control compound, dexamethazone (IC50 13.6 µM).
RESUMO
Two undescribed triterpenes, syzyfolium A (1) and syzyfolium B (2), together with twelve known compounds, terminolic acid (3), actinidic acid (4), piscidinol A (5), threo-dihydroxydehydrodiconiferyl alcohol (6), lariciresinol-4-O-ß-D-glucoside (7), icariol A2 (8), 14ß,15ß-dihydroxyklaineanone (9), garcimangosone D (10), (+)-catechin (11), myricetin-3-O-α-L-rhamnopyranoside (12), quercitrin (13), and 3, 4, 5-trimethoxyphenyl-(6'-O-galloyl)-O-ß-D-glucopyranoside (14) were isolated from the leaves of Syzygium myrsinifolium. Their chemical structures were determined by IR, HR-ESI-MS, 1D and 2D NMR spectra. Compounds 3 and 4 inhibited significantly α-glucosidase with IC50 values of 23.99 and 36.84, respectively, and compounds 1 and 2 inhibited significantly α-amylase with IC50 values of 35.48 and 43.65â µM, respectively.
Assuntos
Syzygium , Triterpenos , Syzygium/química , alfa-Glucosidases , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , alfa-Amilases , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/químicaRESUMO
Seven steroidal saponins including three new 16,23-cyclocholestanes (1-3) and one new pregane (4) were isolated from the roots of Dracaena cambodiana Pierre ex Gagnep. Their chemical structures were elucidated to be (23R,25R)-26-O-ß-D-glucopyranosyl-16,23-cyclocholesta-5,17(20)-dien-22-one-3ß,16α,26-triol-3-O-α-L-rhamnopyranosyl-(1â2)-[α-L-rhamnopyranosyl-(1â3)]-ß-D-glucopyranoside (1), (23R,25R)-26-O-ß-D-glucopyranosyl-16,23-cyclocholesta-5,17,20(22)-trien-3ß,22,26-triol-3-O-α-L-rhamnopyranosyl-(1â3)-ß-D-glucopyranoside (2), (23R,25R)-16,23-cyclocholesta-5,16,20(22)-trien-3ß,22,26-triol-3-O-α-L-rhamnopyranosyl-(1â3)-ß-D-glucopyranoside (3), 3ß-[(O-α-L-rhamnopyranosyl-(1â3)-[α-L-rhamnopyranosyl-(1â2)]-ß-D-gluco-pyranosyl)oxy]-pregna-5,17(20)-diene-16-one-20-carboxylic acid 4''''-O-ß-D-glucopyranosylisopentyl ester (4), cambodianoside A (5), diosbulbiside C (6), and diosbulbiside D (7), by IR, HR-ESI-MS, 1D and 2D NMR spectra. Compounds 1 and 4-7 inhibited nitric oxide (NO) production in lipopolysaccharide activated RAW 264.7 cells with IC50 values ranging from 19.03±1.84 to 67.92±3.81â µM, whereas compounds 2 and 3 were inactive with IC50 values over 100â µM.
Assuntos
Dracaena , Lipopolissacarídeos , Saponinas , Camundongos , Animais , Lipopolissacarídeos/farmacologia , Óxido Nítrico , Células RAW 264.7 , Trientina , Saponinas/farmacologia , Saponinas/química , Estrutura MolecularRESUMO
A new sesquiterpene (1) and a new norsesquiterpene (2) belonging guaiane-type skeleton together with six known compounds (3-8) were isolated from the rhizomes of Alisma plantago-aquatica. Their structures were determined by HR-ESI-MS, 1D and 2D NMR spectroscopic methods. Absolute configurations of new compounds were established by experimental and TD-DFT computational ECD spectra. Compounds 1-8 exhibited xanthine oxidase inhibitory activity with their IC50 values in range of 9.4-66.7â µM. The sesquiterpenoids 1-5 displayed the inhibitory activity and hence they could be potential xanthine oxidase inhibitors from A. plantago-aquatica.
Assuntos
Alisma , Sesquiterpenos , Estrutura Molecular , Alisma/química , Xantina Oxidase , Sesquiterpenos/farmacologia , Sesquiterpenos/químicaRESUMO
From the fruits of Schisandra cauliflora, five new dimethylbutyrylated dibenzocyclooctadiene lignans, named schisandracaurins A-E, were isolated using separation and chromatographic techniques. Their structures were determined by extensive analyses of HR-ESI-MS, NMR, and ECD spectra. The schisandracaurins A-E potentially inhibited NO production in LPS-activated RAW264.7 cells with their IC50 values from 21.4 to 30.3â µM.
Assuntos
Lignanas , Schisandra , Schisandra/química , Lipopolissacarídeos/farmacologia , Estrutura Molecular , Frutas/química , Lignanas/química , Ciclo-Octanos/farmacologia , Ciclo-Octanos/análise , Ciclo-Octanos/químicaRESUMO
A new furostane saponin, ramosaponin (1), and four known furostane saponins, protodioscin (2), dehydrotomatoside (3), (25 R)-26-O-(ß-D-glucopyranosyl)-furost-5-ene-3ß,22α,26-triol 3-O-ß-D-glucopyranosyl-(1â4)-ß-D-galactopyranoside (4), and anguivioside A (5) were isolated from the methanol extract of Allium ramosum seeds. Their structures were identified based on spectroscopic evidence and comparison with those reported in the literature. All compounds were evaluated for reduction of lipid accumulation in HepG2 cell line. As a result, compound 1 showed significant lipid accumulation inhibitory activity with an IC50 value of 64.32 ± 3.87 µM.
Assuntos
Allium , Saponinas , Allium/química , Saponinas/farmacologia , Saponinas/química , Extratos Vegetais/química , Sementes , Lipídeos , Estrutura MolecularRESUMO
Three new chromanes, malloapeltas J-L (1-3), and one new flavone C-glycoside, malloflavoside (4), together with four known compounds, apigenin 6-C-ß-D-xylopyranosyl-8-C-α-L-arabinopyranoside (5), apigenin 6-C-ß-D-glucopyranosyl-8-C-α-L-arabinopyranoside (6), apigenin 7-O-ß-D-apiofuranosyl-(1â2)-ß-D-glucopyranoside (7), and acantrifoside E (8) were isolated from the methanol extract of the leaves of Mallotus apelta. Their chemical structures were determined using spectroscopic methods, including 1D, 2D NMR, and HR-ESI-MS methods. All the isolated compounds were evaluated their cytotoxic activity against human prostate cancer (PC-3) and human breast cancer (MCF-7) cells, but none of them showed cytotoxicities on both human cancer cell lines.
Assuntos
Flavonas , Mallotus (Planta) , Humanos , Apigenina , Glicosídeos/farmacologia , Glicosídeos/química , Flavonas/farmacologiaRESUMO
Three new furostane saponins, ramofurosides A-C (1-3), and two known saponins, fistulosaponin B (4) and (25R)-26-O-ß-D-glucopyranosyl-1ß,3ß,26-trihydroxyfurosta-5,20(22)-diene-1-O-α-L-rhamnopyranosyl-(1â2)-α-L-arabinopyranoside (5) were isolated from the methanol extract of Allium ramosum seeds. Their structures were identified based on spectroscopic evidence and comparison with those reported in the literature. All compounds were evaluated for reduction of lipid accumulation in HepG2 cell lines. As a result, compounds 1 and 3 showed a significant reduction in total lipid content by 27.93±3.05 and 27.54±1.68 %, respectively, at a concentration of 100â µM.
Assuntos
Allium , Saponinas , Allium/química , Lipídeos/análise , Metanol , Estrutura Molecular , Extratos Vegetais/química , Saponinas/química , Sementes/químicaRESUMO
Mallotusapelta(Lour.) Müll.Arg has been used in traditional medicine for the treatment of chronic hepatitis. Six new chromene derivatives, malloapeltas C-H (1-6) and one known compound, malloapelta B (7) were isolated and structured from the leaves of M.apelta. Two pairs of enantiomers (1a/1b and 2a/2b) were successfully separated by chiral high-pressure liquid chromatography (HPLC). The structures and absolute configurations of compounds were determined using spectroscopic methods, including 1D, 2D NMR, and MS and quantum chemical calculation methods. All compounds were evaluated for cytotoxic activity using cell counting kit-8 (CCK-8) assay against ovariancancer cell line (TOV-21G). Compounds 1-5 and 7 exhibited significant growth and viability inhibitory effects with GI50 values ranging from 0.06 to 10.39 µM and IC50 values ranging from 1.62 to 10.42 µM on ovarian cancer cell line, TOV-21G. The most cytotoxic compounds 2, 3, and 7 were chosen for studying in apoptosis mechanism. Compounds 2, 3, and 7-induced apoptosis as evidenced by activated caspase 8, caspase 9, and PARP, increased Bak and Bax, and decreased Bcl-xL and survivin. Moreover, compounds 2, 3, and 7 significantly inhibited the NF-κB signaling pathway. Taken together, our findings propose the potential application of compounds 2, 3, and 7 for treating cancer via modulating NF-κB activity.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Benzopiranos/farmacologia , Mallotus (Planta)/química , Extratos Vegetais/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Benzopiranos/química , Benzopiranos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Camundongos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Células RAW 264.7 , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
Gymnema sylvestre, a medicinal plant, has been used in Indian ayurvedic traditional medicine for the treatment of diabetes. Phytochemical investigation of Gymnema sylvestre led to the isolation of five new pregnane glycosides, gymsylosides A-E (1-5) and four known oleanane saponins, 3ß-O-ß-D-glucopyranosyl (1â6)-ß-D-glucopyranosyl oleanolic acid 28-O-ß-D-glucopyranosyl ester (6), gymnemoside-W1 (7), 3ß-O-ß-D-xylopyranosyl-(1â6)-ß-D- glucopyranosyl-(1â6)-ß-D-glucopyranosyl oleanolic acid 28-O-ß-D-glucopyranosyl ester (8), and alternoside XIX (9). Their structures were identified based on spectroscopic evidence and comparison with those reported in the literature. All compounds were evaluated for their α-glucosidase and α-amylase inhibitory activities. Compounds 2-4 showed significant α-amylase inhibitory activity, with IC50 values ranging from 113.0 to 176.2 µM.
Assuntos
Glicosídeos/farmacologia , Gymnema sylvestre/química , Pregnanos/farmacologia , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Ativação Enzimática/efeitos dos fármacosRESUMO
Three new flavonol glycosides, fissflavosides A-C (1-3), together with six known flavonol glycosides, kaempferol 3-O-α-L-rhamnopyranosyl-(1â2)-ß-D-galactopyranoside (4), kaempferol 3-O-α-L-rhamnopyranosyl-(1â6)-ß-D-galactopyranoside (5), kaempferol 3-O-α-L-rhamnopyranosyl-(1â6)-ß-D-glucopyranoside (6), rhamnetin 3-O-α-L-rhamnopyranosyl-(1â2)-ß-D-glucopyranoside (7), rutin (8), and isorhamnetin 3-O-α-L-rhamnopyranosyl-(1â2)-ß-D-galactopyranoside (9) were isolated from the methanol extract of the Fissistigma pallens leaves. Their chemical structures were determined by 1D-, 2D-NMR, and MS data as well as in comparison with reported data in the literature. Compounds 1-9 showed weak cytotoxic activity on three human cancer cell lines, HT-29, A-2058, A-549 with IC50 ranging from 134.6 to 162.6 µM. In addition, the antioxidant capacities of compounds were also tested by ORAC assay. All compounds showed significant antioxidant with trolox equivalents ranging from 4.4 to 8.6 µM at the concentration of 1.0 µM. The results indicated 7 and 8 having meaningful reducing capacity of copper (I) ions of 2.7 to 6.9 µM at the concentrations of 1 and 2 µM.
Assuntos
Annonaceae/química , Flavonóis/química , Glicosídeos/isolamento & purificação , Antioxidantes/farmacologia , Configuração de Carboidratos , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Espectroscopia de Prótons por Ressonância Magnética , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
Two new naphtoquinones (smenocerones A and B, 1 and 2) and four known sesquiterpene cyclopentenones (dactylospongenones A-D, 3-6) were isolated from sponge Smenospongia cerebriformis living in the Eastern Sea of Vietnam. Their chemical structures were determined by high resolution electrospray ionization (HR-ESI)-MS, NMR spectroscopic analysis, and in comparison with the reported data. The chiroptical properties of compounds 3-6 were examined by experiment and theoretical calculation of circular dichroism (CD) spectra to prove their absolute configurations. Compound 2 significantly exhibited cytotoxic activity towards lung carcinoma (LU-1), hepatocellular carcinoma (HepG-2), promyelocytic leukemia (HL-60), breast carcinoma (MCF-7), and melanoma (SK-Mel-2) human cancer cells with IC50 values of 5.5±0.8, 3.2±0.2, 4.0±0.7, 4.1±0.8, and 5.7±1.1 µg/mL, respectively.
Assuntos
Ciclopentanos/isolamento & purificação , Ciclopentanos/farmacologia , Naftoquinonas/isolamento & purificação , Naftoquinonas/farmacologia , Poríferos/química , Animais , Linhagem Celular Tumoral , Dicroísmo Circular , Humanos , Espectroscopia de Ressonância MagnéticaRESUMO
Five new oleanane-type saponins, hirsutosides A - E, were isolated from the leaves of Glochidion hirsutum (Roxb.) Voigt. Their structures were elucidated as 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-ß-d-glucopyranoside (1), 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-ß-d-glucopyranosyl-(1 â 3)-ß-d-glucopyranoside (2), 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-6-acetyl-[ß-d-glucopyranosyl-(1 â 3)]-ß-d-glucopyranoside (3), 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-ß-d-glucopyranosyl-(1 â 3)-ã-l-arabinopyranoside (4), and 21ß-benzoyloxy-3ß,16ß,23-trihydroxyolean-12-ene-28-al 3-O-ß-d-glucopyranosyl-(1 â 3)-α-l-arabinopyranoside (5). All isolated compounds were evaluated for cytotoxic activities on four human cancer cell lines, HepG-2, A-549, MCF-7, and SW-626 using the SRB assay. Compounds 1, 2, 4, and 5 showed significant cytotoxic activities against all human cancer cell lines with IC50 values ranging from 3.4 to 10.2 µm. Compound 3 containing acetyl group at glc C(6â³) exhibited weak cytotoxic activity with IC50 values ranging from 47.0 to 54.4 µm.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Magnoliopsida/química , Saponinas/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ácido Oleanólico/análogos & derivados , Folhas de Planta/químicaRESUMO
Phaeanthus vietnamensis Bân is a well-known medicinal plant which has been used for the treatment of various inflammatory diseases in traditional medicine. Using various chromatographic methods, three new compounds, (7S,8R,8'R)-9,9'-epoxy-3,5,3',5'-tetramethoxylignan-4,4',7-triol (1), 8α-hydroxyoplop-11(12)-en-14-one (5), and (1R,2S,4S)-4-acetyl-2-[(E)-(cinnamoyloxy)]-1-methylcyclohexan-1-ol (12) along with twelve known compounds were isolated from the leaves of P. vietnamensis. Their chemical structures were elucidated by physical and chemical methods. All compounds were evaluated for the inhibitory activities of nitric oxide production in LPS-stimulated BV2 cells. As the results, compound 6 showed the most potent inhibitory activity on LPS-stimulated NO production in BV2 cells with the IC50 values of 15.7 ± 1.2 µm. Compounds 2, 7, and 8 significantly inhibited inflammatory NO production with IC50 values ranging from 22.6 to 25.3 µm.
Assuntos
Annonaceae/química , Óxido Nítrico/metabolismo , Folhas de Planta/química , Animais , Annonaceae/metabolismo , Linhagem Celular , Dicroísmo Circular , Lignanas/química , Lignanas/isolamento & purificação , Lignanas/farmacologia , Espectroscopia de Ressonância Magnética , Camundongos , Microglia/citologia , Microglia/efeitos dos fármacos , Microglia/metabolismo , Conformação Molecular , Extratos Vegetais/química , Folhas de Planta/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologiaRESUMO
Inhibitory effects of NO production in RAW 264.7 macrophages guided the isolation of nine prenylated isoflavones, including a new cudraisoflavone L (1) and eight known metabolites furowanin B (2), erysubin A (3), wighteone (4), lupalbigenin (5), laburnetin (6), isolupalbigenin (7), 6,8-diprenylorobol (8), millewanin H (9) from the leaves of Cudrania tricuspidata. At the concentration of 10 µM, compounds 1, 2, and 4 significantly inhibited NO production with the inhibitory values of 72.5 ± 2.4, 66.9 ± 1.8, and 55.4 ± 2.7%, respectively. In addition, all of isolated compounds 1-9 showed promising cytotoxic effects toward HL-60 cells (IC50 4.3 ± 0.7 to 18.0 ± 1.7 µM).
Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Citoproteção/efeitos dos fármacos , Isoflavonas/isolamento & purificação , Isoflavonas/farmacologia , Óxido Nítrico/biossíntese , Animais , Anti-Inflamatórios não Esteroides/química , Células HL-60 , Humanos , Isoflavonas/química , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Moraceae/química , Raízes de Plantas/química , PrenilaçãoRESUMO
CONTEXT: Paramignya trimera (Oliv.) Burkill (Rutaceae) has been used to treat liver diseases and cancer. However, the anti-inflammatory effects of this medicinal plant and its components have not been elucidated. OBJECTIVE: This study investigated chemical constituents of the P. trimera stems and evaluated anti-inflammatory effects of isolated compounds. MATERIALS AND METHODS: Cytotoxicity of isolated compounds (5-40 µM) toward BV2 cells was tested using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) for 24 h. Inhibitory effects of isolated compounds (5-40 µM) on nitrite and PGE2 concentrations were determined using Griess reaction and PGE2 ELISA kit, respectively (pretreated with the compounds for 3 h and then stimulated for 18 h with LPS). Inhibitory effects of compounds (5-40 µM) on iNOS and COX-2 protein expression were evaluated by Western blot analysis (pretreated with the compounds for 3 h and then stimulated for 24 h with LPS). RESULTS: Seven coumarins were isolated and identified as: ostruthin (1), ninhvanin (2), 8-geranyl-7-hydroxycoumarin (3), 6-(6',7'-dihydroxy-3',7'-dimethylocta-2'-enyl)-7-hydroxycoumarin (4), 6-(7-hydroperoxy-3,7-dimethylocta-2,5-dienyl)-7-hydroxycoumarin (5), 6-(2-hydroxyethyl)-2,2-dimethyl-2H-1-benzopyran (6), and luvangetin (7). Compounds 1-4 and 7 inhibited NO and PGE2 production in LPS-stimulated BV2 cells, with IC50 values ranging from 9.8 to 46.8 and from 9.4 to 52.8 µM, respectively. Ostruthin (1) and ninhvanin (2) were shown to suppress LPS-induced iNOS and COX-2 protein expression. DISCUSSION AND CONCLUSION: The present study provides a scientific rationale for the use of P. trimera in the prevention and treatment of neuroinflammatory diseases. Ostruthin and ninhvanin might have potential therapeutic effects and should be considered for further development as new anti-neuroinflammatory agents.
Assuntos
Anti-Inflamatórios/farmacologia , Cumarínicos/farmacologia , Mediadores da Inflamação/antagonistas & inibidores , Extratos Vegetais/farmacologia , Rutaceae , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular , Cumarínicos/isolamento & purificação , Relação Dose-Resposta a Droga , Mediadores da Inflamação/metabolismo , Camundongos , Microglia/efeitos dos fármacos , Microglia/metabolismo , Extratos Vegetais/isolamento & purificação , Caules de PlantaRESUMO
Using various chromatographic methods, five new steroidal saponins named taccavietnamosides A-E (1-5) and three known, (24S,25R)-spirost-5-en-3ß,24-diol 3-O-α-l-rhamnopyranosyl-(1â2)-[α-l-rhamnopyranosyl-(1â3)]-ß-d-glucopyranoside (6), (24S,25R)-spirost-5-en-3ß,24-diol 3-O-α-l-rhamnopyranosyl-(1â2)-[ß-d-glucopyranosyl-(1â4)-α-l-rhamnopyranosyl-(1â3)]-ß-d-glucopyranoside (7), and chantrieroside A (8) were isolated from the rhizomes of Tacca vietnamensis Thin et Hoat. Their chemical structures were elucidated by physical and chemical methods. All compounds were evaluated for the inhibitory activities of nitric oxide production in LPS-stimulated RAW 264.7 macrophages and BV2 cells. As the results, compounds 3-5 showed moderate inhibition on NO production in LPS-stimulated BV2 cells and RAW 264.7 macrophages with the IC50 values ranging from 37.0 to 60.7µM.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Dioscoreaceae/química , Óxido Nítrico/antagonistas & inibidores , Saponinas/farmacologia , Espirostanos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Linhagem Celular , Relação Dose-Resposta a Droga , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Células RAW 264.7 , Saponinas/química , Saponinas/isolamento & purificação , Espirostanos/química , Espirostanos/isolamento & purificação , Relação Estrutura-AtividadeRESUMO
Nine new chromonylthiazolidine derivatives were successfully semi-synthesized from paeonol. All of the compounds, including starting materials, the intermediate compound and products, were evaluated for their cytotoxic effects toward eight human cancer cell lines. The synthesized chromonylthiazolidines displayed weak cytotoxic effects against the tested cancer cell lines, but selective cytotoxic effects were observed. Compounds 3a and 3b showed the most selective cytotoxic effects against human epidermoid carcinoma (IC50 44.1 ± 3.6 µg/mL) and breast cancer (IC50 32.8 ± 1.4 µg/mL) cell lines, respectively. The results suggest that chromoylthiazolidines are potential low-cost, and selective anticancer agents.